II B. PHARM FOURTH SEMESTER ALL SUBJECTS
TWO MARKS
S.NO
SUBJECT CODE
SUBJECT
1.
BP 401 T
PHARMACEUTICAL ORGANIC CHEMISTRY –III
2.
BP 402 T
MEDICINAL CHEMISTRY – I
3.
BP 403 T
PHYSICAL PHARMACEUTICS-II
4.
BP 404 T
PHARMACOLOGY-I
5.
BP 405 T
PHARMACOGNOSY AND PHYTOCHEMISTRY I
PHARMACEUTICAL ORGANIC CHEMISTRY- III
UNIT-I
1. Define Stereo chemistry
Stereochemistry is a branch of organic chemistry which deals with structure of compounds in three
dimensions and hence can be termed as chemistry with respect to the arrangements and movements of
different atoms or group of atoms in space.
2. Define Isomerism
Some compounds have same molecular formula, but differ from each other in physical and chemical
properties, and are called isomers. This phenomenon exhibited by such compounds is called as isomerism.
3. Define Structural/ Constitutional Isomerism
Compounds which have same molecular formula but, different structural formula are called structural
isomers. When the isomerism is due to difference in the arrangement of atoms within the molecule without
any reference to space, it is called structural isomerism
4. Classify stereoisomers
Stereo isomers can be classified into two types. They are configurational and conformational isomers.
5. Define configurational isomers
Configurational isomers are stereoisomers that cannot be converted into one another by rotation around a
single bond. The two main types of configurational isomers are geometric isomers and optical isomers.
6. Define conformational isomers/ Confermers/ Rotamers.
Conformational isomers are stereoisomers that can be converted into one another by rotation around a
single bond. Therefore the molecule exist in number of forms.
7. Define chiral compounds
Chirality means “handedness”. A chiral molecule is non-superimposable on its mirror image. The presence
of an asymmetric carbon center is one of several structural features that induce chirality in organic
molecules.
8. Define optical isomers
The stereo isomers having the same structures, but different configurations and bearing an ability to rotate
the plane polarized light are called optical isomers.
9. Define Enantiomers with example
A pair of non-superimposable mirror image isomers are called enantiomes
10. Define epimer with example
An epimer is one of a pair of stereoisomers that differ in configuration only at the chiral center.
11. Define Diastereomers with example
Diastereomers are non-enatiomeric stereoisomers that are not mirror image of each other. They have two
or more stereo centers and differ in the orientation of atleast one of them.
12. Define Anomers with example
An anomer is actually an epimer that differs in configuration at the acetal/hemiacetal carbon.
13. What is plane of symmetry?
A plane of symmetry is an imaginary plane that bisects a molecule into halves that are mirror images of each other.
Example:
14. What is a meso compound?
An achiral compound with chiral centres is called a meso compound. And it has a plane of symmetry
15. Name different system of nomenclature
DL and RS system of nomenclature
16. Define centre of symmetry
A point in the center of the molecule is a center of symmetry if a line drawn from it to any element, when
extended an equal distance in the opposite direction, encounters an identical element.
17. Define axis of symmetry
A molecules possess an alternating axis symmetry (Sn) of n fold if rotation of the molecule about the axis
by 2π / n followed by reflection through a plane perpendicular to this axis produces an indistinguishable
with the original.It is also called rotation or reflection of symmetry.
18. Define specific rotation
The angle of rotation in degrees of the plane of polarization of a ray of monochromatic light that passes
through a tube 1 decimeter long containing the substance in solution at a concentration of 1 gram per
millimeter in a polarimeter.
[α]D =
α (observed rotation)
l (Path length,dm) X d (concentration or density,g/ml)
19. Define plane polarized light
Plane polarized light is a light wave in which all photons have the same polarization i.e. the waves
oscillate in only one direction.
20. Define racemic modification
An equimolar mixture of a pair of enantiomers is called as racemate, racemic mixture or racemic
modification. It is denoted by (+-)
21. Name any two methods of resolution
Chromatographic separation and biochemical separation
22. Name any two important reactions of chiral molecules
Stereospecific and stereo selective reactions
23. Define Racemisation
The process of converting an optically active compound in to the racemic modification is called as
racemisation. The (+) and (-) forms of most of the compounds are capable of racemisation under the
influence of heat, light or chemical reagent.
24. Fischer projection.
Fischer projections provide an easy way to draw three dimentional molecules on paper. All atoms are
projected on to one plane. Eg: One of the enantiomers of lactic acid.
COOH
COOH
C
OH
H
H3C
C
H
HO
H3C
Fischer projection of (+) Lactic acid
Fischer rules for showing the arrangement around an asymmetric carbon are as follows:
i)
The carbon chain of the compound is arranged vertically with the most oxidized carbon at the top
or put the number 1 at the top.
ii)
Represent the asymmetric carbon at the intersection of crossed line.
a
d
b
C
asymmetric carbon
c
iii)
Groups attached to the vertical lines are understood to be going back behind the plane of the paper.
That is the vertical lines represent bonds going away from the observer. The asymmetric carbon is
in the paper plain.
iv)
Groups attached to the horizontal lines are understood to be coming forward out of the paper plain.
25. Add a note on sequence rule
Rule 1: when four different atoms are attached to the chiral carbon atom priority depends on atomic
number with the atom higher atomic number getting higher priority. If two atoms are isotopes then the
higher mass number has high priority.
Rule 2: when two or more groups attached to the asymmetric carbon atom are identical, priority order is
determined by considering the atomic number of the second atom.
Rule 3: A doubly or triply bonded atom ‘X’ is equivalent to two or three such atoms. Thus we can compare
the priority order of –CHO and -CH2OH the former get the higher priority order than the -CH2OH since
the third atom in –CHO is O while it is H in - CH2OH.
Rule 4: in case of geometrical stereoisomer groups the cis group precedes trans group. Similarly in case
of optical isomer the (R) group precedes (S) group. In case of pseudoasymmetriccentre the symbols (R)
or(S) are replaced by (r) and (s).
26. What is Stereomutation?
Any change in the stereochemical configuration of a molecule is called stereomutation.
27. Explain the D and L system in optical isomerism
Any material which rotates the plane of the polarized light is termed "optically active." Compounds
featuring chiral centers are optically active unless they possess symmetry plane or a symmetry center (see
above). An isomer of optically active compound can rotate the plane of polarized light to the left
(levorotatory), in which case it will be designated (l, or -), or to the right (dextrorotatory) in which case
it will be termed (d, or +).
28. What are elements of symmetry?
The elements of symmetry are: a) A plane of symmetry; b) A centre of symmetry and c) An alternate axis
of symmetry. If the molecule contains at least one of these elements of symmetry, the molecule is
symmetric.
29. Define asymmetric synthesis
The synthesis which converts a prochiral unit into a chiral unit and results in unequal amounts of
stereoisomers is known as asymmetric synthesis. Thus, asymmetric synthesis is a special case of
stereoselective synthesis, i.e., the stereoselective synthesis involving creation of an element of chirality in
substrate molecule.
30. Define Conformational analysis.
The different spatial arrangements that a molecule can adopt due to rotation about single bonds are
called conformations and hence conformational isomers orconformers. The study of the energy changes
that occur during these rotations is called conformationalanalysis.
31. What is Walden inversion?
Walden inversion is the inversion of a chiral center in a molecule in a chemical reaction. Since a molecule
can form two enetiomers around a chiral center, the Walden inversion converts the configuration of the
molecule from one enantiomeric form to the other.
32. What is 1,3-diaxial interaction?
An interaction (usually repulsive) between two axial substituents on a cyclohexane ring. On the top face
of this chair cyclohexane, the axial methyl groups and axial hydrogen atom experience diaxial repulsion
(indicated with the dashed line).
33. Define asymmetric synthesis.
Synthesis of asymmetric compounds from symmetric compounds is called asymmetric synthesis.
Depending on the nature of substances used, it is divided into two types:
(i) Partial asymmetric synthesis
(ii) Absolute asymmetric synthesis
UNIT-II
1. Define Cis-Trans isomers with example
Cis-trans isomers are stereoisomers, that is, pairs of molecules which have the same formula but differ in
their configuration. The prefixes "cis" and "trans" indicates that the functional groups are on the same side
of the double bond while trans conveys that functional groups are on opposing sides of the double bond.
2. Draw the staggered Newmannconformation of butane
3. What is E-Z system of nomenclature?
This system of nomenclature is based on the priorities of groups. The prefix "Z" (E=Zusammen–
together)indicates that the functional groups of higher priority are on the same side of the double
bond and"E" (E=Entegegen – opposite) functional groups are on opposing sides of the double bond.
4. Define “syn” addition
In an addition reaction if the groups added to the reacting molecule in the same faces of the molecule,
the addition is referred to as syn addition.
5. Define “syn” elimination
In an elimination reaction if the groups removed from the reacting molecule from the same faces of
the molecule, the elimination is referred to as syn elimination.
6. Define “anti” addition
In an addition reaction if the groups added to the reacting molecule to the different faces of the
molecule, the addition is referred to as anti addition.
7. Define “anti” elimination
In an elimination reaction if the groups removed from the reacting molecule from the different faces
of the molecule, the elimination is referred to as anti elimination.
8. Name any two methods of determining configuration of geometrical isomers
Absolute method and spectroscopic method
9. Define conformational isomerism
Conformational isomerism is a form of stereoisomerism in which the isomers can be interconverted
just by rotations about formally single bonds (refer to figure on single bond rotation).
10. Define conformations
Any two arrangements of atoms in a molecule that differ by rotation about single bonds can be referred
to as different conformations, conformations that correspond to local minima on the energy surface are
specifically called conformational isomers or conformers.
11. Define Staggered conformation
A conformation about a carbon- carbon single bond in which the atoms or groups on one carbon are
as far apart as possible from the atoms or groups on an adjacent carbon.
12. Define Eclipsed conformation
A conformation of a carbon- carbon single bond in which the atoms or groups of atoms on one carbon
are as close as possible to the atoms or groups of atoms on an adjacent carbon.
13. Draw the staggered conformation of ethane
staggered conformation of ethane
14. Define strain
Strain is produced in a molecule, when a molecule is less stable due to electron repulsion or when it is
not in its ideal geometry.
15. Define torisonal strain
Torisonal strain is a strain developed by bond pair-bond pair repulsion between atoms or groups of
atoms on each carbon atom
16. Define Dihedral angle (Q):
Dihedral angleis the angle created by two intersecting planes. For eclipsed Q=0◦, for staggered
conformation Q=60◦.
17. Define angle strain
Any bond angle other than the ideal bond angle, i.e., 109◦28" (normal tetrahedral angle) results in
strain, known as angle strain.
18. Draw the favoured conformations of cyclohexane
There are four favoured stable conformations for cyclohexane. They are chair, half chair; twist boat,
and boat.
19. What are axial and equatorial bonds in cyclohexane?
There are twelve carbon-hydrogen bonds in cyclohexane molecule consisting of two sets of six bonds
each. A set of six bonds are parallel to the axis of symmetry or perpendicular to the plane of molecule
(above or below) termed as axial bonds. Other set of six bonds are inclined at an angle of 109 ◦ 28"to
the axis of symmetry or parrelel to the plane of ring are termed as equatorial bonds.
20. What is ring flipping?
Cyclohexane has two identical and readily interconvertible chair forms and is mirror images of each
other. This interconversion process is called “ring flipping”.
21. Define atropisomers
Atropisomers are stereoisomers arising because of hindered rotation about a single bond,
where energydifferences due to steric strain or other contributors create a barrier to rotation that is high
enough to allow for isolation of individual conformers.
22. Define Stereo selective reaction
A reaction that yields predominately one stereoisomer (or one pair of enantiomers) irrespective of
reactant and of several diastereomers is called a stereoselective reaction.
23. Define Stereo specific reaction
A reaction in which stereo chemically different molecules react differently is called a stereospecific
reaction. The cisandtrans stereoisomers give different products.
24. Define chemoselective reaction
In a bifunctional compound, if the reagent reacts with one of the functional group preferentially over
the other, the reaction is called as chemo selective reaction.
25. Define regio selective reaction
The reaction is said to be region selective when it selectively generates one constitutional isomer
rather than the other.
UNIT III
1. Define heterocyclic chemistry
Heterocyclic compounds are organic compounds that contain a ring structure containing atoms in addition
to carbon, such as sulfur, oxygen or nitrogen, as the heteroatom. The chemistry which deals with
preparation, reactions and structures of such compounds is known as heterocyclic chemistry.
2. What is Hansch-Wildman system of nomenclature?
Hansch-Wildman system is the most common systematic method of nomenclature which specifies ring
size, nature/type and positions of hetero atoms.
3. What are the prefixes given for nitrogen, oxygen and sulphur heteroatoms?
The prefixes indicate the heteroatoms present in the ring. For nitrogen-aza, for oxygen-oxa and for
sulphur-thia is specified in the nomenclature.
4. How will you classify hetero cyclic compounds?
Hetero cyclic compounds are generally classified according to the total number of atoms present in the
ring and electronic structure.
3. Draw the structure of furan and number it
4. Draw the structure of thiophene and pyrrole
5. Draw the structure of any two fivemembered ring with three hetero atoms
1,2,4-tiazole & 1,3,4-oxadiazole
6. Draw the resonance structures of pyrrole
7. Predict the product
?
8. Write the structure of Indole and pyrimidine
N
N
N
H
pyrimidine
1H-indole
9. Mention the product formed when furan is subjected to Friedal – Craft’s reaction.
Acylation by Friedal craft reaction take place in the presence of BF3 to form 2-acetyl furan.
(CH3CO)2O
BF3
or
CH3COCl/AlCl3
O
Friedal-craft acylation
COCH3
O
furan
10.
1-(furan-2-yl)ethanone
Name the natural compound having tetrahydrothiophene nucleus.
Biotin (or) Vitamin-H
11. Write the friedal craft’s reaction and coupling reaction of Pyrrole.
friedal craft's Acylation
CH3COCl/No Catalyst
N
H
COCH3
N
H
2-acetyl pyrrole
1H-pyrrole
N2Cl
HCl
Diazocoupling
N
H
1H-pyrrole
N N
N
H
2-phenylazo pyrrole
12. Write what happens when Pyrrole treated with methyl iodide?
H
N
N
+
CH2I2
+ 2 CH ONa
3
+
2 NaI
+ 2 CH3OH
13. Write what happens when Pyrrole treated with aq. K2CO3?
H
N
H
N
+
Aq. K2CO3
O
OH
Kolbe-schimt carboxylation takes place to form pyrrole-2-carboxylic acid.
14. Write what happens Furan with aceticanhydride?
O
O
+
O
BF3
(CH3CO)2O
CH3
15. What product is formed in friedal craft acetylation of furan?
Friedal craft acetylation takes place to form 2-acetylfuran
O
O
+
O
BF3
(CH3CO)2O
CH3
Friedal craft acetylation takes place to form 2-acetylfuran
16. Write the Reduction product of furan
Reduction
O
O
Tetrahydro furan.
Furan is catalytically reduced over Raney-nickel or palladium oxide to form tetrahydro furan.
17. Wrie the formylation reaction of Pyrrole
18.
i)
Describe the reactions of thiazole.
Thiazole reacts with sodamide to form 2-aminothiazole which undergoes diazotization.
N
N
NaNH2
S
S
ii)
NH2
thiazol-2-amine
thiazole
N
HCl/HNO2
S
N2Cl
2-chloro-1-(thiazol-2-yl)diazene
2-methyl thiazole condenses readily with benzaldehyde in presence of alkali.
CHO
N
N
S
Alkali
CH3
2-methylthiazole
19.
S
benzaldehyde
C
H
C
H
H2O
2-styrylthiazole
What happens when methyl substituted pyrazole is oxidized by pottasium permanganate?
20.
Write the paal-knorr synthesis of pyrrole
Paal-knorr synthesis
UNIT IV
1. Write the structure of oxazole and isoxazole
a)
Oxazole
b)Isoxazole
2. Write two examples of piperazine nucleus containing medicinal compounds
a)
Diethyl Carbamazine Citrate (DEC)
3. Reaction of Indole with chloroform in NaOH?
b) Piperazine citrate
O
OH
H
+
N
H
Cl
NaOH
Cl Cl Cl
+
N
H
N
Electrophilic substitution reaction takes place to form 3-formyl indole and 3- chloroquinoline
4. Write any two reactions given by pyridine.
Electrophilic substitution reactions of pyridine
5.
Write the structure and numbering of heterocylic compounds pyrimidine and pyrrole.
a)
Pyrimidine
b)
Pyrrole
6. Give any two reaction of indole.
Nitration and sulphonation are examples of aromatic electrophilic substitution reactions. Nitration and
sulphonation ae examples of indole lead to the formation of 3-nitro indole and indole-3-sulphonic acid as
products.
7.
8.
Write any two reactions given by pyrimidine.
Write any two reaction of Acridine.
9.
Give two methods of synthesis of imidazole
Debus-Radziszewski imidazole synthesis
In the second stage, this diimine condenses with the aldehyde:
10.
i)
A modification of this general method, where one equivalent of ammonia is
replaced
ii)
by an amine, affords N-substituted imidazoles in good yields
Structure and uses of azepines
a) Azepine b) 5H-dibenzo(b,f)azepine
Imipramine and desipramine are the derivatives of azepines used as antidepressants
11.
Write the structure and numbering of any two 5-membered heterocyclic compounds containing
two similar hetero atoms.
12.
a) pyrazoleb) Imidazole
Give the structure and numbering of (a) Isoquinoline (b) Phenothiazine.
(a) Isoquinoline
(b) Phenothiazine
13.
Write the halogenation reaction of Quinoline
Quinoline undergoes bromination and forms 8-bromo quinoline and 4-bromo quinoline
14.
Write any synthesis of Acridine
Bernthsen acridine synthesis is the chemical reaction of a diarylamine heated with a carboxylic
acid (or acid anhydride) and zinc chloride to form a 9-substituted acridine.
15.
Sketch the structure of caffeine and theobromine
a)Caffeine
b)Theobromine
16.
Write the structure and medicinal uses of Theophylline.
17.
c) Theophylline Use: CNS Stimulant
Write the structures of Xanthine bases
a) Caffeine
18.
b) Theobromine
c) Theophylline
Write the structure and uses of caffeine
USES: Used as a CNS Stimulant, Weak Diuretic and also used in the treatment of
Migraine Headache.
19.
Write the structures of histamine and metranidazole
a) Histamine
b) Metranidazole
20. Write the medicinal uses of quinoline and isoquinoline
Quinoline derivatives are used as antimalarial, antibacterial and anti-amoebic drugs. Isoquinoline
derivatives are used as anti-hypertensive and anaesthetic drugs.
UNIT V
1. Define Catalytic hydrogenation.
Hydrogenation is a process of adding hydrogen and converting a carbon- carbon double bond to carboncarbon single bond in presence of catalyst like Wilkinson’s catalyst, Palladium and Raney Nickel etc.
Hydrogenation are three types, they are:
a) Homogenous (one phase).
b) Heterogeneous (two phases)
c) Transfer hydrogenation.
2. Catalytic Dehydrogenation
Catalytic dehydrogenation is the process by which hydrogen is removed or eliminated by the use of catalyst.
The various catalysts used are selenium, platinium and palladium & alumina
Ex. Dehydrogenation of hydrocarbon
Se
3H2
3. Write any two uses of Lithium aluminium hydride.
It is a powerful reducing agent used in the organic synthesis for reducing various type of
as aldehydes, ketone and carboxylic acids.
Eg:
O
1.
OH
LiAlH4
C
H3C
dry ether
C2H5
CH
H3C
C2H5
butan-2-ol
butan-2-one
O
OH
LiAlH4
2.
compounds such
C
H3C(H2C)16
OH
dry ether
stearic acid
CH
H3C(H2C)16
OH
octadecane-1,1-diol
4. Define Clemmenson reaction with example.
It is defined as the reduction of carbonyl group of aldehydes and ketones(-C=O) to alkanes group (-CH2-) with
Zinc amalgam and HCl.
O
4H
HCl
C
R
H2
C
Zn/Hg
H
O
4H
H2
C
Zn/Hg
HCl
C
R
H2O
H
R
R
H2O
R
R
5.Give the uses of metal hydrides.
Metal hydrides used for reduction are
1. LiAlH4
2. NaBH4
LiAlH4: It is a powerful reducing agent used in the organic synthesis for reducing various types of
compounds such as aldehydes, ketone and carboxylic acids.
Eg:
O
OH
LiAlH4
C
CH
dry ether
H3C
H3C
C2H5
C2H5
butan-2-ol
butan-2-one
NaBH4: reduce the carbonyl group to respective alcohol.
O
R
C
NaBH4
H
O
R
C
OH
R
NaBH4
R
CH
H
OH
R
CH
R
It does not affect other groups like carbonyl, nitro ester, amide etc.
Reduction of ketonic group in to alcoholic by NaBH4 is used in the synthesis of pseudotropine and
cholesterol.
Also used in the qualitative reduction of glucose and sorbitol.
5. What is Schmidt rearrangement?
The Schmidt reaction is an organic reaction involving alkyl migration over the carbon–nitrogen chemical
bond in an azide with expulsion of nitrogen. A key reagent introducing this azide group is hydrazoic
acid and the reaction product depends on the type of reactant.Carboxylic acids form amines through
an isocyanate intermediate and ketones form amides.
6. What is Birch reduction?
The Birch reduction is the dissolving-metal reduction of aromatic rings in the presence of an alcohol,
where addition of hydrogen takes place at position 1,4 to give unconjugated diene. Liquid ammonia serves
as a solvent.
7. Why is nitrobenzene mostly used as an oxidizing agent in Skraup’s synthesis?
Generally, nitrogen is used as the oxidizing agent in Skraup synthesis because aniline, a reactant is
produced, i.e., in the reaction, nitrobenzene is reduced to aniline which may be further utilized.
8. Write any two uses of sodium borohydride
i. The principal application of sodium borohydride is the production of sodium dithionite from sulfur
dioxide. Sodium dithionite is used as a bleaching agent for wood pulp and in the dyeing industry.
ii. Sodium borohydride is used as reducing agent in the synthesis of alcohol from aldehyde and also in
the reduction of ozonides
9. Write any two uses of Lead tetra acetate.
Lead tetra acetate is generally employed as:
a) Acetylating agent
b) Methylating agent
c) Oxidizing agent
Eg: Oxidation of hydroquinones
Oxidation of glycols
11. Define metal hydride reduction
The reduction of carbonyl compounds into alcohols by using most common metal hydrides are sodium
borohydride(NaBH4) and lithium aluminium hydride (LiAlH4).
12. Write the reaction for metal hydride reduction
13. What is Wolf Kishner reduction?
Reduction of hydrazones and semi carbazones or azines of aldehydes and ketones to hydrocarbons in
presence of strong base, hydrazine and in high boiling point solvent like glycols with evolution of nitrogen
is known as wolk kishner reduction. It is used for the reduction of acid sensitive carbonyl compounds.
14. Write the applications of Wolf Kishner reduction
Wolf kishner reduction is used for the reduction of carbonyl groups to methylene groups in various
synthetic methods. It is also used for the reduction of higher molecular weight acid sensitive carbonyl
compounds.
15. Write the reaction for the following
Acetophenone
?
Ethylbenzene
Acetophenone
Ethylbenzene
16. Write the reaction mechanism of wolf kishner reduction
17. Write the applications of birch reduction
Birch reduction is applied in the synthesis of aromatic alkyl substituted ether, aromatic carboxylic acid,
aromatic hydrocarbons and alkylation of aromatic nitrile compounds.
18. Define Oppenauer oxidation
Oppenauer oxidation, named after Rupert Viktor Oppenauer, is a gentle method for selectively
oxidizing secondary alcohols to ketones. The alcohol is oxidized with aluminium isopropoxide in excess
acetone.
19. Give one example reaction for Oppenauer oxidation
20. How will you prepare resorcinol from m-hydroxy Benzaldehyde?
Resorcinol is prepared from m-hydroxy Benzaldehyde by Dakin’s reaction using alkaline hydrogen
peroxide.
21. Define Dakin’s reaction
The replacement of aldehyde group of o-hydroxy, p-hydroxy or o-amino Benzaldehyde by a hydroxyl
group by the action of alkaline hydrogen peroxide is known as Dakin’s reaction.
22. What are the applications of Dakin’s reaction?
Dakin’s reaction is useful in the preparation of polyhydric phenols from naturally occurring hydroxy
aldehydes.
23. What are the applications of Claisen-Schmidt reaction?
Claisen-Schmidt condensation is useful in the preparation of flavones and the perfumery commercial
products cinnamaldehyde and benzylidene acetone.
24. How will you prepare of Cinnamaldehyde?
Cinnamaldehyde is prepared from benzaldehyde by the claisen-schmidt condensation reaction.
25. What are the applications of schmidt reaction?
Schmidt reaction is used in the preparation of primary amines and lactams.
MEDICINAL CHEMISTRY –I
Unit I
1. Define solubility.
Solubility is the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the
important parameters to achieve desired concentration of drug in systemic circulation for desired
pharmacological response. Any drug to be absorbed must be present in the form of solution at the site of
absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which
include physical and chemical modifications of drug and other methods like particle size reduction, crystal
engineering, salt formation, and solid dispersion, use of surfactant, complexation, and so forth. Selection
of solubility improving method depends on drug property, site of absorption, and required dosage form
characteristics.
2. Define partition coefficient.
Partition coefficient is the ratio of concentrations of a compound in a mixture of two immiscible phases
at equilibrium. This ratio is therefore a measure of the difference in solubility of the compound in these
two phases. The partition coefficient generally refers to the concentration ratio of un-ionized species of
compound.
Partition coefficients are useful in estimating the distribution of drugs within the body.
3.
4.
5.
6.
7.
Also termed as or distribution coefficient refers to the concentration ratio of all species of the compound
(ionized plus un-ionized).
Define active transport.
The process of drug molecules against the concentration gradient and through the specialised carrier is
termed as active transport.
This is characterised by
• Utilisation of energy from metabolic activity.
• Proceed against concentration gradient.
• Absorption rate is independent of concentration.
Define Phagocytosis and pinocytosis.
Phagocytosis and pinocytosis is the process where extracellular fluid along with solute molecules is carried
into the cell through the vacuoles. In this substances are dissolves in extracellular fluid by engulfing.
Simply, Phagocytosis is cell eating process and pinocytosis is cell drinking process.
Define chelation.
Chelation involves the formation or presence of two or more separate coordinate bonds between
a polydentate (multiple bonded) ligand and a single central atom.
Usually these ligands are organic compounds, and are called chelants, chelators, chelating agents, or
sequestering agents.
EDTA is a common example.
Define hydrogen bonding and its types.
The hydrogen bond is a special type of dipole-dipole interaction between the hydrogen atom in a polar
bond such as N-H, O-H, or F-H and an electronegative atom O, N, or F atom.
These interactions are written as A-H………B.
A and B represent O, N or F. Generally, hydrogen bonding is classified into 2 types
• Intermolecular hydrogen bonding (between 2 molecules)
• Intramolecular hydrogen bonding (same molecule)
Define receptors
Receptors are membrane bound proteins and generally have helicies that span the membrane by total
occupation of backbone H-bonding sites. The interior of the lipid membrane being hydrophobic,
extracellular region often glycosylated and intracellular region attached or bound to other proteins such as
kinase G proteins, the receptor function as signal transmitters.
8. List the factors of drug metabolism
• Age /sex
• Species and strain
• Hereditary or genetic factors
• Enzyme induction and
• Enzyme inducing.
9. Enumerate the physicochemical properties in relation to biological action.
• Solubility
• Partition co-efficient
• Ionisation and pKa value
• Hydrogen bonding
• Surface activity
10. Define drug metabolism.
Drug metabolism is basically a process that introduces hydrophilic functionalities on to the drug molecule
to facilitate excretion or it converts lipophilic chemical compound into readily excreted polar product. Liver
is the principle organ of drug metabolism and other including gastrointestinal tract, lungs, kidneys and the
skin. This enzymatic biotransformation is known as drug metabolism. These sites are usually responsible
for localised toxicity reactions.
Drug metabolism involves two general types of reactions.
They are Phase-I reaction and phase-II reactions.
Phase-I: they are enzyme biotransformation reaction in which drug may undergo a wide variety of oxidation
reduction and hydrolysis.
Phase-II reaction undergoes conjugation reactions.
11. What is the role of functionalisation reaction?
The purpose of these reactions is to introduce a functional polar group(s) (e.g.,OH, COOH, NH2, SH) into
the xenobiotic molecule to produce a more water-soluble compound. This can be achieved by direct
introduction of the functional group (e.g., aromatic and aliphatic hydroxylation) or by modifying or
“unmasking” existing functionalities (e.g., reduction of ketones and aldehydes to alcohols; oxidation of
alcohols to acids; hydrolysis of ester and amides to yield COOH, NH2, and OH groups; reduction of azo
and nitro compounds to give NH2 moieties; oxidative N-, O-, and S-dealkylation to give NH2, OH, and SH
groups).
Phase I reactions may not produce sufficiently hydrophilic or inactive metabolites; they generally tend to
provide a functional group or “handle” on the molecule that can undergo subsequent phase II reactions.
12. Define steric effect?
Steric effects arise from the fact that each atom within a molecule occupies a certain amount of space. If
atoms are brought too close together, there is an associated cost in energy due to overlapping electron
clouds, and this may affect the molecule's preferred shape (conformation) and reactivity.Other types of
steric effects are Steric shielding, steric attraction, steric repulsion, chain crossing.
13. What is pKa value?
The pka or dissociation constant is a measure of the strength of the acid or a base and is sometimes called
the acidity constant or the ionisation constant. It is a numeric representative of the relative proton transfer
for that substance or the compound donating proton is calculating the same method as the equilibrium
constant.The equation for the protolysis of proton by acidic drug
14. Define protein binding with example?
The reversible binding of drug with non-specific and non-functional site on the body protein without
showing any biological effect is called as protein binding.
Drug + albumin ↔ drug + albumin complex.
Acid-glycoprotein structures with basic entities and lipoproteins bind with basic & neutral drugs. Protein
binding values are normally given as the percentage of total plasma concentration of drug that is bound to
all plasma protein.
Free drug (Dj)+ free protein (Pf) ↔ drug/ protein complex (Dp)
The total plasma concentration of the drug is expressed as the sum of the percentage of free drug &percent
bound.
Total plasma concentration (Dt) = (Df)+ (Dp) e.g. hepatic diseases that alter the concentration of albumin
in the plasma uremia that can cause changes in the binding affinity of some drugs.
15. Define prodrug with example?
Prodrug can be defined as a drug derivative that undergoes biotransformation, enzymatically or nonenzymatically inside the body before exhibiting its therapeutic effect. Ideally the prodrug is converted to
original drug as soon as the derivative reaches the site of action followed by rapid elimination of the
released derivatizing group without causing sideeffects in the process. The derivatising group is covalently
linked to the drug molecule.
16. Classify the chemical pathway of drug metabolism?
They are classified in to
Phase I reaction (Oxidation, reduction and hydrolysis)
Phase II reaction (Conjugation)
17. What are various sites of drug metabolism in the body?
Liver is the Primary site for metabolism; virtually all tissue cells have same metabolic activities. Other
organs have significant metabolic activities include gastrointestinal tract, kidney and lungs.
18. Add a note on Phase –I reaction
Phase I metabolism is the predominant pathway of biotransformation. The enzymes involved in phase I
reaction are primarily located in the endoplasmic reticulum of the liver cell, they are called microsomal
enzymes . Phase I reactions are non-synthetic in nature and generally produced more water soluble and less
active metabolite. The most common phase I reactions are oxidative process, reductive and hydroxylation
reactions.
19. Add a note on prodrugs.
A prodrug is a chemically inert drug precursor, which upon biotransformation liberates the
pharmacologically active parent compound. A prodrug is also called pro-agent, bio reversible derivative,
latentiated drug and congeners.
20. Define Bioisosterism and give one example.
Bioisosteres are chemical substituents or groups with similar physical or chemical properties which
produce broadly similar biological properties to another chemical compound. In drug design, the purpose
of exchanging one bioisostere for another is to enhance the desired biological or physical properties of a
compound without making significant changes in chemical structure. The main use of this term and its
techniques are related to pharmaceutical sciences. Bioisosterism is used to reduce toxicity,
change bioavailability, or modify the activity of the lead compound, and may alter the metabolism of the
lead.
Examples: Classical Bioisosteres and
Non-classicalbioisosteres
21. Define Non-classical bioisosteres and give example.
They donot rigidly fit the steric qnd electronic rules vof the classic bio-iososteres. They are divided into
exchangeable groups and ring versus non-cyclic structures.
Example: diethyl stilbesterol has the same potency as the naturally occurring estradiol.
Phenyl ephrine phenolic alcoholic group may be sunstituted alkylsulphonamido group.
22. Define optical and geometrical isomerism.
Optical isomers are molecules that differ three-dimensionally by the placement of substituents around one
or more atoms in a molecule. Optical isomers were given their name because they were first able to be
distinguished by how they rotated plane-polarized light.Geometric isomerism (also known as cistrans isomerism or E-Z isomerism) is a form of stereoisomerism.
23. Give two reactions of Phase-I Metabolism.
1. Oxidation of secondary amine
2. Hydrolytic reactions (hydrolysis of esters)
24. What is oxidative biotransformation processes.
The general stoichiometry that describes the oxidation of many xenobiotics (R-H) to their corresponding
oxidized metabolites (R-OH) is given by the following equation The enzyme systems carrying out this
biotransformation is referred to as mixed-function oxidases or monooxygenases. There is a large family
that carry out the same basic chemical reactions. Phase I reactions are enzymatic which involve the
biotransformation of drug to a more polar metabolite by introducing or unmasking the functional group.
Unit 2
1. Define Sympathomimetic drugs.
Drugs which exert similar action like adrenaline are called sympathomimetics drugs or adrenergic drugs.
Adrenaline is a hormone secreted by the adrenal medulla which mediates all the action of sympathetic
nervous system.
They are classified in to:
• Drugs acting on adrenergic receptors i.e. acting on α-receptor, β-receptors and acting on both
α and β-receptors eg: phenylepherine, clonidine
• Drugs acting on adrenergic receptor as well as by releasing neurotransmitter, eg: Ephedrine
and amphetamine.
2. Synthesis of acetylcholine.
Acetylcholine synthesis takes place in the nerve endings by the transfer of an acyl group from acetyl
coenzyme A (CoA) to choline. The reaction is catalyzed by choline acetyl transferase enzyme synthesized
in neuron.
O
HOH2CH2C N
C
H3C
S
Acetyl CoA
CoA
Choline
CH3
CH3
CH3
Choline Acetyl
transferase
O
C
H3C
OH2CH2C N
Acetylcholine
CH3
CH3
CH3
HSCoA
3. Mechanism of Adrenergic antagonists.
Adrenergic antagonists are Alpha adrenergic blockers, Beta adrenergic blockers.
Alpha adrenergic blockers: α-adrenergic blockers compete with nor-epinephrine for binding to the αadrenergic receptors. When α-blockers bind to the receptors it will prevent norepinephrine from producing
sympathetic response.
Beta adrenergic blockers: β adrenergic blockers competete with epinephrine and nor-epinephrine by
binding to β-adrenergic receptor and antagonizes the effects of epinephrine and nor-epinephrine.Adrenergic
neuron blockers prevent the formation and storage of norepinephrine at adrenergic nerve
endings.Catecholamine antagonists behave as a false transmitter and interfere with the synthesis of
norepinephrine on the nerve endings.
4. Give the structural requirement for adrenergic agonistic activity.
• A phenylethylamine ring structure.
• 3, 4 dihydroxy substitution on the phenyl ring.
• The phenol group in the catechol may be replaced by alkyl or arylsulphonamide functions.
5. Name the drugs under the category of aryloxypropanalmines.
Propranolol.
Oxyprenolol
Alprenolol
Metoporolol
Practolol
6. Give the structure and uses of carvedilol.
Used as non-selective betablockers.
7. Give the structural requirement for beta2 agonist.
• Aromatic hydroxyl group is necessary for the activity (para or meta position).
• An alpha methyl or ethyl for vascular effects.
8. Write the name and structure of a drug acting as alpha2 adrenergic agonist.\
Naphazoline.
9. What is adrenergic antagonist?
Drugs which antagonise the action of adrenergic transmitters or sympathomimetics are called as adrenergic
antagonist or antiadrenergic agents or sympatholytics. They are classified in to adrenergic receptor blockers
adrenergic neuron blocking agents Agents inhibiting the synthesis of catacholamines.eg: prazosin,
yohimbine, phentolamine, propranolol, butoxamine, guanithidine and methyldopa.
10.
List the functions of muscarinic receptors.
• Cardiac inhibition,
• peripheral inhibition.
• Constriction of the pupil.
• Increased salivation and flow of secretary glands.
• Contraction and peristaltic action on the GIT and urinary tract.
11. Give two examples as Anti-asthmatic drugs.
• Salbutamol
• Salmeterol
• Metaproterenol
12. Give a note on β2-stimulants?
β2-stimulants are also called as β-adrenergic receptor agonist. These agents relax the smooth muscle of the
bronchi, uterus and blood vessels. Generally they have far less action on the heart than isoproterenol and
other agents. Increased β2 agonist activity is conferred by the substitution of increasing bulky lipophilic
groups on the amino group of isoproterenol. These drugs must be administered orally or by inhalation.
Eg: Salbutamol, Terbutaline, Ritodrine etc.
13. Define neurotransmitter and give examples?
A neurotransmitter is a chemical messenger used by neurons to communicate in one direction with
other neurons. They are synthesized primarily in the nerve terminals, stored in vesicles of nerve terminals
and released in to the extra cellular space using calcium ions. Examples are:
1)
Acetylcholine
2)
Biogenic amines such as serotonin, tryptamine.
3)
Catecholamine- dopamine, norepinephrine, epinephrine.
4)
Amino acid such as GABA, glycin, glutamic acid and aspartate.
14. Write the synthesis of salbutamol.
H3COOC
ClCOCH2Cl
COCH2Cl
H3COOC
Friedal-Craft's
acylation
-HCl
2-chloroacetyl chloride
HO
HO
Methyl salicylate
CH2NHC(CH3)3
N-benzyl-2-methylpropan-2-amine
HOH2C
COCH2NC(CH3)3
CH2
CH2
Selective
-reduction
HO
COCH2NC(CH3)3
H3COOC
LiAlH4
HO
NaBH4
OH
HOH2C
CHCH2NC(CH3)3
OH
CH2
HO
HOH2C
CHCH2NHC(CH3)3
Pd-C2H2
HO
Salbutamol
15. Synthesis of Propranolol.
OCH2CH
OH
CH2
O
ClH2C
CH
CH2
O
2-(chloromethyl)oxirane
naphthalen-1-ol
OH
OCH2CHCH2NHCH(CH3)2
NH2CH(CH3)2
Propranolol
16. Write the structure and use of salbutamol.
OH
CHCH2NHC(CH3)3
HOH2C
HO
Salbutamol
Use: Used in the treatment of bronchial asthama
UNIT 3
1. Define the term Parasympatholytics with examples
A parasympatholytic agent is a substance or activity that reduces the activity of the parasympathetic
nervous system. (The parasympathetic nervous system is often colloquially described as the "Feed and
Breed" or "Rest and Digest" portion of the autonomic nervous system. The parasympathetic nervous
system becomes strongly engaged during or after a meal and during times when the body is at rest.)
Example : Atropine ,scopolamine, dicyclomine
2. Give any two structures of cholinergic drug.
Pyridostigmine
3.
Atropine
Define the term neuromuscular blockers.
Neuromuscular-blocking
drugs block
neuromuscular
transmission
at
the neuromuscular
junction,causing paralysis of the affected skeletal muscles. This is accomplished either by
acting presynaptically via the inhibition of acetylcholine (ACh) synthesis or release or by
acting postsynaptically at the acetylcholine receptors of the motor nerve end-plate. While some drugs act
presynaptically (such as botulinum toxin and tetanus toxin), those of current clinical importance work
postsynaptically.
4.
5.
6.
Agents that block the transmission of Ach at the motor end plate are called neuromuscular blocking agent.
The therapeutic use of these compounds is primarily as adjuvant in surgical anaesthesia to obtain relaxation
of skeletal muscle. They are also used in various orthopedic procedures, such as alignment of fractures and
correction of dislocation.
Structure and medicinal uses of Tropicamide.
USES: It is very short acting mydriatic and cycloplegic in ophthalmologic practice.
Write short notes on neuromuscular blockers.
Neuromuscular-blocking agents: drug which blocks the transmission of nerve impulse at the neuromuscular
junction and thereby producing relaxation of the skeleton muscle are known as neuromuscular blocking
agents or skeleton muscle relaxants
They are classified as;
Peripherally acting drug eg: Gallamin, Pancuranium, Succinylcholine
Centrally acting muscle relaxant. eg: Mephenicin
Directly acting muscle relaxant eg: Dantrolene.
Write the structure of any two cholinergic blocking agents.
Use: It is used to treat myasthenia gravis. Also in constipation, post-operative distention and urinary
retention.
O
O
N
CH3
OCCH
CH2OH
Atropine
N
CH3
OCCH
OH
Homatropine
Use: To reduce intraocular pressure. Used to induce miosis and relieve glaucoma.
7.Structure and use of Neostigmine
It is used in the treatment of myasthenia gravis.
8.Structure and medicinal uses of Pyridostigmine.
It is used in the treatment of myasthenia gravis.
9.Write the uses of pilocarpine, acetylcholine.
Uses of pilocarpine: Pilocarpine is a non-selective agonist on the muscarinic receptors. .it is used for the
treatment of symptoms of dry mouth caused by radiotherapy for cancer of head and neck.
Uses of acetylcholine: Topical ophthalmic drug to induce miosis, during certain intraocular surgical
procedures such as cataract surgery, iridectomy
10. Irreversible anticholinesterase agents
They belong to a class of organophosphorus esters and both AchE and BuChE are inhibited irreversibly. These
are nerve poisons and have been used in warfare and agricultural pesticides.
11. Add a note on neurochemistry of cholinergics
Cholinergic neurotransmitters such acetylcholine, indolamines, catecholamines, GABA neuropeptides are
chemical messengers used by neurons to communicate in one direction with other neurons. Communication
between neurons is accomplished by the recognition by a receptor for a specific chemical messenger.
PICTURE A BALL(neurotransmitter)IN A CUP(receptor). They are synthesized primarily in the nerve
terminals and are released into the extracellular space using calcium ions. Their action is terminated by Re
uptake into the presynaptic terminal or glial cells by specific transporter proteins or by catabolism in
synaptic cleft or in presynaptic terminal.
12. Cholinergic Blocking agents.
Cholinergic blocking agents or cholinergic antagonists or antimuscaranic drugs inhibit the actions of
endogenous acetylcholine and muscarinic agonists at muscarinic receptor sites in peripheral tissue and in
the CNS. These are highly specific reversible competitive antagonist for muscarinic receptors. The
pharmacological effects are blockage of parasympathetic stimulation at effector organs. They are rapidly
absorbed from the GIT slowly absorbed when applied locally on eye or skin. These agents cause decreased
gastric secretion, dry mouth, drying of the mucous membrane. In generalmydriasis urinary retention,
decreased sweating bronchial and biliary dilatum and tachycardia
Example; Homatropine, Tropicamide, dicylamine, Clidinium, Glycopyrolate
13. Structure and medicinal uses of Pyridostigmine.
Uses: It is used in the treatment of myasthenia gravis.
Unit 4
1. What are hydantoins?
Hydantoin, which is also known as glycolylurea, is a heterocyclic organic compound that can be thought
of as a cyclic "double-condensation reaction" product of glycolic acid and urea.
2. Write the chemistry of hydantoins.
• Hydantoin is imidazolinedione which is 5 membered ring system nitrogen as hetero atom in 1,3 positions
and two keto group 2,4 carbon
• weaker organic acids than barbiturates and thus their sodium salt (e.g., phenytoin sodium) generates
stronger alkaline solution
• Most of the clinically used drugs in this class possess bulky aromatic ring in position C-5 that confers
usefulness in generalized seizures, partial seizures and status epilepticus but not well for absence seizures.
3. Write the structure and therapeutic uses of any two benzodiazepine derivatives?
Chlordiazepoxide:
7-chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepine-4-oxide
Uses:
• It is used as antipsychotic.
• Sedative and muscle relaxant.
Clonazepam:
Chemical name:5-(2-chlorophenyl)-7-nitro-2,3-dihydro-1,4 benzodiazepin-2-one.
Uses: It has anxiolytics and anticonvulsant activity.
4. Write the structure and use of Chlorpromazine HCl
S
N
Cl
CH2CH2CH2N(CH3)2
Chlorpromazine
Use: management of psychotic condition. It also controls excitement, aggression and agitation. It has
antiemetic, antipruritic, antihistaminic and sedative properties.
5. Give the chemical name structure of any two phenothiazine derivatives posses’ antipsychotic
activity?
Chlorpromazine
S
N
Cl
CH2CH2CH2N(CH3)2
Chlorpromazine
Chemical name:3-(2-chloro-10H-phenothiazin-10-yl)-N, N-dimethyl-propan-1-amine.
Trifluoperazine:
Chemical name: 10-[3-(4-methylpiperazin-1-yl) propyl]-2-(trifluoromethyl)-10H- phenothiazine
6. Write the structure for Haloperidol and Trifluperazine.
Haloperidol
O
OH
CCH2CH2CH2
F
N
Trifluperazine
Cl
7. Structure, chemical name and uses of phenobarbitone.
O
HN
C2H5
HN
CHCH2CH2CH3
NaO
O
CH3
butyl) barbiturate
IUPAC Name:Sodium-5-allyl-5-(1-methyl
Sodium 5-allyl -5-(1-methylbutyl)
barbiturate
USES: In the treatment of insomnia, as a basal aneasthetic and in strychnine poisoning.
8. Mechanism of action of diazepam.
Diazepam binds and modifies the GABA receptor chloride ionphore complex in the central nervous system
as an agonist, facilitating the physiological effects of GABA (Gama amino butyric acid) or the GABA
receptor complex of the α,β,γ and subunits of the receptor, α,β subunit determine the function of anxiolysis
or sedation, while the γ subunit renders the receptor itself sensitive to benzodiazepine.
9. Give the structure and medicinal uses of Diazepam.
Uses: Hypnotic, anticonvulsant and antianixety agent
10. Discuss the SAR of phenothiazine.
6
5
4
S
7
3
8
2
9
10N
1
R1
CH2CHCH2N
R2
R3
Ring substitution
• The best position for substitution is the 2nd position. Activity increase as the electron withdrawing ability
of the substituents increase.
• Presence of unshared electron pair of an atom or atom of 2nd substituent increase the potency of the
compound
• Substituent at 3rd position shows significant activity when compared to unsubstituted.
• Substitution at 1 and 4 has a deleterious effect on antipsychotic activity.
• Oxidation of the 5th sulphur of phenothiazine decrease neuroleptic activity.
Alkyl side chain substitution:
• Three carbon atom chains between position 10 and the amino nitrogen is required.
• Shortening or lengthening of the chain, at this position decrease the activity
• Substitution on the propylene chain of 10-(3-amino propyl) phenothiazine may also influence antipsychotic
potncy.
11. Define Antipsychotics agents with examples.
Antipsychotic drugs are used to psychoses like schizophrenia, mania and senile dementia and behavioral
disorders in children. These drugs act by depressing the CNS i.e by decreasing dopamine levels and by
producing sedation without inducing sleep. They are employed to reduce excitation, agitation,
aggressiveness and impulsiveness. Hence they are also known as major tranquilisers, neuroleptics or
psychotropic i.e chlorpromazine, prochlorperazine and Haloperidol.
12. Mechanism of action of methohexital?
Methohexital concentrate in the more lipid soluble hydrophobic region of neuronal cell membrane and
causes swelling of these membrane due to this swelling the structure of membrane alters, there by blocks
the Na + channels. Thus the generation of action potential is inhibited and produces anaesthesia.
Weak analeptic employed as respiratory stimulant
13. Define sedative and hypnotics and give one drug as example for each.
The term sedative refers to a quieting effect accompanied by relaxation and rest but not necessarily sleep.
Sedative drugs are used to allay excitement and reduce motor activity without inducing sleep.
Example: Phenobarbitone
Hypnotics drugs are used to induce sleep when sleepness is not due to a definite stimulus such as pain,
itching which prevents sleep or awakens the patient.Example: butobarbitone
Unit 5
1. Define General anesthetics
General anesthetics or CNS depressant that extends to the entire body and is characterized by a state of
unconsciousness analgesia and amnesia with skeletal muscle relaxation and loss of reflexes which are
reversible.
General anaesthetics inhibit CNS neuronal activity. They are classified into inhalational anaesthetics and
intravenous anaesthetics
Example; Halothane, Methohexital and Ketamine.
2. Enumerate the charecteristics of general anaesthetics.
They are nonspecific in action.they donot interact with specific receptors.
They are used at high concentration and reach all parts of the body.
3. Brief the stages of anaesthesia.
• Stage 1. Anagesia.
Consciousness is maintained, analgesia is produced.
• Stage 2. Delirium or excitement.
Consciousness is lost. Patient may salivate, vomit or develop cough.
• Stage 3. Surgical anaesthesia.
Skeletal muscle relaxed, most of the operative procedures are performed.
• Stage 4. Respiratory paralysis or medullary paralysis.
This is a toxic or overdose stage in which there is respiratory and cardiovascular collapse and tissue
rapidly become anoxic.
4. Give the statement of Overton Meyer hypothersis.
• All neutral lipid soluble substances have depressant properties on neurons.
• Anaesthetic activity is most pronounced in lipid rich cells.
• The effect increases with partition coefficient not on the structure.
5. Define general anaesthetics and write the structure of any two drugs.
General anaesthetics are agents that produce loss of consciousness and therefore loss of all sensation. These
agents are used to produce unconsciousness and loss of perception to painful surgical procedure.
F
F
H
C
C
F
Br
Halothane
Cl
H
Cl
F
C
C
Cl
F
OCH3
2,2-dichloro-1,1-difluoro-1-methoxyethane
6. Mechanism of action of general anesthetics?
General anesthetic inhibits CNS neuronal activity. But their precise mechanism of neuronal inhibit ion is
not clear several mechanisms were proposed to explain General anaesthetic, they are
) Lipid theory: According to this the more lipid soluble general anesthetics concentrate the hydrophobic
region of neuronal cell membrane and cause swelling of this membrane. Due to this swelling the
structure of the membrane alters thereby blocks the Na+ channels. Thus the generation of action potential
is inhibited and produces anesthesia.
) As per “Protein theory” the anaesthetic binds to the hydrophobic sites of protein molecules thus the
membrane of function is altered and produces anaesthesia.
7. Write mode of action on Halothane
The more lipid soluble Halothane, a general Anaeasthetic, concentrate in hydrophobic regions of Neuronal
cell membrane and causes swelling of these membranes.Due to this swelling structure of membrane of
Alters, there by blocks the Sodium Ion channels,thereby Generation of action potential is inhibited and
produces Anaeasthesia.
8. Write the structure and therapeutic uses of any one ultra-short acting barbiturate possess general
anaesthetic activity.
O
HN
CH2CH CH2
O
CHC
N
H3C
O
CCH2CH3
CH3
Methohexital
It is useful for short surgical operation such as oral surgery, gynecological investigation and
electroconvulsive therapy.
9. Give the structure and uses of Halothane.
Halothane
Use: potent general inhalational anaesthetic agent
10. Write the structure and therapeutic uses of Ketamine.
Use: It is an intravenous agent of choice for surgical operation of short duration.
11. Mechanism of action of Indomethacin.
Indomethacin inhibits prostaglandin synthesis i.e it inhibits cyclooxygenase that catalyse the synthesis of
cycloendoperoxides from arachidonic acid to form prostaglandins. Indomethacin selectively inhibit
Cyclooxygenase-I enzyme (COX-I).
12. Write the structure for a) ketamine b) thiopental sodium.
O
N
C2H5
NaS
HN
CHCH2CH2CH3
O
CH3
13. Structure and uses of methohexital sodium.
USES: It is used as General Anaeasthetic and Hypnotic.
14. List the advantages of short acting barbiturates.
• Smooth inductiuon.
• Fair muscular relaxation.
• Absence of salivary secretion.
• Nonexplosive nature.
• Short and uncomplicated recovery.
15. Define Opioid antagonist
An opioid antagonist is a receptor antagonist that acts on opioid receptors. Naloxane and Naltrexone
commonly used opioid antagonist drugs which are competitive antagonist the opioid receptors with higher
affinity than agonists but do not activate the receptors. This effectively blocks the receptor, preventing the
body from responding to opiates and endorphins. Some opioid antagonists are not pure antagonists but in
fact do produce some weak opioid partial agonist effects.
Examples : Nalorphine and Levallorphan.
16. Define antitussive?
Antitussives are agents that are employed in the symptomatic control of cough by way of depressing the
cough-centre strategically situated in the medulla. Antitussive can act either by raising the threshold of
the cough centre or by reducing the number of impulses transmitted to the cough centre from the
peripheral receptors.
17. Write the name structure and uses of any one oxicam derivative possesses anti-inflammatory
activity?
piroxicam
Use: It is used in the treatment of rheumotoid arthritis and osteoarthritis.
18. Give the chemical name structure and uses of two arylpropionic acid analogue used as antiinflamatory agent?
Ibuprofen
Chemical name: 2-(4-(2-methylpropyl) phenyl) propanoic acid.
Uses: It is an anti-inflammatory drug possess antipyretic and analgesic activity. It is useful in the treatment
of rheumatoid arthritis and osteoarthritis.
Naproxen
Chemical name: 2-(6-methoxynaphthalen-2-yl) propanoic acid
Uses: It is an analgesic antipyretic and anyi-inflammatory drug and also useful in the treatment of rheumatic
arthritis,dysmenorrhea and in acute gout.
19. Give the structure and uses Indomethacin.
CH2COOH
H3CO
CH3
N
C
O
Cl
Indomethacin
Use: anti-inflammatory and analgesic agent.
20. Write the structure of i) Salsalate ii) Oxymorphine
Salsalate
Oxymorphine
21. Draw the structure and medicinal uses of Nalorphine HCl
23. Structure and uses of salsalate and phenylbutazone.
Uses: Antipyretic, Analgesic, and anti inflammatory
Uses: used in Osteoarthritis, rheumatoid arthritis, spondylitis
22. Draw the structure and medicinal uses of Meperidine HCl.
Used as synthetic Narcotic analgesic
23. Sketch the structure and medicinal uses of Morphine analogues.
Analgesic and cough suppressant
24. Structure and uses of Piroxicam
It is an anti-inflammatory agent used in the treatment of rheumatoid arthritis and osteo arthritis
25. Give the structure and uses of Aspirin.
OCOCH3
COOH
Aspirine
Use: antipyretic, analgesic and antirheumatic.
PHYSICAL PHARMACEUTICS – II
UNIT – 1
1. Define Colloids?
A disperse system consists essentially of one component, the disperse phase, dispersed as particles or
droplets throughout another component, the continuous phase. By definition, dispersions in which
the ize of the dispersed particles is within the range 1 nm to about 1 µrn are termed colloidal.
2. Classification of colloidal dispersion system?
a) Molecular dispersion
eg; oxygen gas, glucose
b) Colloidal dispersion
eg; natural and synthetic polymer, silver solutions
c) Coarse dispersion
eg; sand, RBC, emulsions
3. Define lyophilic colloids with examples?
These are also known as solvent loving colloids as the dispersed particles interact to an appreciable
extent with the dispersion medium.These colloidal solutions are reversible in nature.They may be
hydrophilic or lipophilic.
Eg: Starch, gelatin, rubber, protein etc.
4. Define lyophobic colloids with examples?
Generally lyophobic colloids are solvent hating. Lyophobic colloidal solutions are those in which
dispersed phase has no affinity for the dispersion medium. They are irreversible by nature and
stabilised by adding small amount of electrolyte.
Eg; Metals such as gold, silver and their hydroxides or sulphides etc.
5. Define association colloids with example?
These colloids behave as normal electrolytes at normal concentrations but behave as colloids at
higher concentrations. These associated colloids are also referred to as micelles.
Eg; soaps, polythene oxides etc.
6. List the kinetic properties off of colloids?
a. Brownian movement
b. Diffusion
c. Osmotic pressure
d. Sedimentation
e. viscosity
7. List the electric properties off of colloids?
a) Electric double layer
b) Electrophoresis
c) Electro osmosis
d) Streaming potential
e) Sedimentation potential
8. Define peptization?
It is a method accountable for the development of stable dispersion of colloidal particles in
dispersion medium. Generally in this method changing a precipitate to colloidal solution via shaking
with dispersion medium in the existence of slight quantity of electrolyte.
9. Define DLVO THEORY?
The stability of lyophobic colloids is described by DLVO theory. According to this theory the distance
between dispersed particles influences particle particle interactions. Interactions like attractions and
repulsions are responsible for stability of colloids.
10. Define Protective colloids?
The lyophobic particles will be covered by a thin layer of a lyophilic (or hydrophilic) colloid. For
example, the addition of gelatin (a lyophilic colloid) to a gold sol (lyophobic sol) protects the latter
from being coagulated on addition of sodium chloride solution.
11. Write note on gold number with examples.
The protective power a lyophilic colloid is usually expressed in terms of a number called gold
number introduced by Zsigmondy. It may be defined as follows.
The gold number of a protective colloid is its minimum amount in milligrams which is just sufficient
to prevent the coagulation of 10 ml of a gold sol on the addition of 1 mL of 10% sodium chloride
solution.
It is to be noted that the smaller the value of gold number, the greater is the protective power of the
protective colloid. The gold numbers of a few protective colloids are given in the Table below.
Protective (Lyophilic)
Colloid
Gold
Number
Gelatin
0.005-0.01
Casein
0.01-0.02
Haemoglobin
0.03-0.07
Egg albumin
0.08-0.10
Gum Arabic
0.10-0.15
Dextrin
6-20
Starch
20.25
12. Define Brownian movement?
Brownian motion Colloidal particles are subject to random collisions with the molecules of the
dispersion medium, with the result that each particle pursues an irregular and complicated zigzag
path.
13. Write note on Tyndall effect
When a beam of light is passed through a colloidal sol some of the light may be absorbed (when light
of certain wavelengths is selectively absorbed a colour is produced), some is scattered and the
remainder is transmitted undisturbed through the sample. Because of the scattered light the sol
appears turbid: this is known as the Tyndall effect.
14. Define Zeta potential?
Zeta potential is a scientific term for electrokinetic potential in colloidal systems. In the colloidal
chemistry literature, it is usually denoted using the Greek letter zeta (ζ), hence ζ-potential. Zeta
potential is the potential difference between the tightly bound layer to electro neutral region layer.
15. What is the importance of Zeta potential in Pharmacy?
The significance of zeta potential is that its value can be related to the stability of colloidal
dispersions. The zeta potential indicates the degree of repulsion between adjacent, similarly charged
particles in dispersion.
For molecules and particles that are small enough, a high zeta potential will confer stability, i.e., the
solution or dispersion will resist aggregation. When the potential is low, attraction exceeds repulsion
and the dispersion will break and flocculate. So, colloids with high zeta potential (negative or
positive) are electrically stabilized while colloids with low zeta potentials tend to coagulate or
flocculate as outlined in the table.
Zeta potential [mV]
Stability behavior of the colloid
from 0 to ±5,
Rapid coagulation or flocculation
from ±10 to ±30
Incipient instability
from ±30 to ±40
Moderate stability
from ±40 to ±60
Good stability
more than ±61
Excellent stability
16. Applications of colloidal system.
●
Colloidal silver iodide, silver chloride & silver protein are effective germicides & not cause
irritation as ionic silver salts.
●
Colloidal copper used in cancer.
●
Colloidal gold used as diagnostic agent.
●
Colloidal mercury used in syphilis.
●
Association colloids (SAA) are used to increase solubility & stability of certain compounds
in aqueous & oily pharmaceutical preparations.
●
Blood plasma substitutes as dextran, PVP & gelatin are hydrophilic colloids used to restore or
maintain blood volume.
●
Iron - dextran complex form non-ionic hydrophilic sols used for treatment of anemia.
17. Define diffusion?
Diffusion generally is a movement of particles from an area of higher concentration to the lower
concentrations until the concentration of the system attains equilibrium and it is due to brownian
motion
Diffusion is given by Fick’s law
dq= -DS dc/dx.dt
18. Electric double layer
It is a electrical property of colloids. It consists of layer of ions bonded firmly to the surface is called
stern layer surrounded by oppositely charged ions. The surface seperating the two layers is called
shear plane. The region outside the double layer with equal cations and anions is called electroneutral region.
19. Electrophoresis
It is a method which comprises the movement of colloidal particles either to cathode or anode under
the impact of electrical field.
20. Define coacervation
The phenomenon which involves separation of macromolecular solutions into two liquid layers is
called coacervation.
UNIT-2 (RHEOLOGY)
1. What is rheology?
Rheology is the study of the flow of matter; mainly liquids but also some solids or solids under
conditions in which they flow rather than deform elastically.
It applies to substances which have a complex structure, including muds, sludges, suspensions,
polymers, many foods, bodily fluids and other biological materials.
2. Define viscosity?
Viscosity is qualitatively defined as the resistance of a liquid to flow due to internal friction between
different layers of liquid when it flows.
3. Kinematic Viscosity?
The kinematic viscosity (v) is also used and may be defined as the dynamic viscosity divided by the
density of the fluid.
4. Define Rheopexy?
The time period to regain its original viscosity may be reduced by applying gentle shaken (rolling or
tumbling) to the sytems.
• Rheopexy helps in bringing the particles to original state.
• Positive rheopexy (Shear thining -Plastic and Pseudoplastic system)
• Negative rheopexy (Shear thickening - Dilatant system)
5. Define Yield value in plastic systems?
• Normally flocculated suspensions are associated with the plastic flow, where yield value represents
the stress required to break the inter-particular contacts so that particles behave individually.
• Thus yield value is indicative of the forces of flocculation.
6. Define Thixotrophy?
Thixotropy is defined as the isothermal reversible conversion of gel to sol in shear thining system and
sol to gel in shear thickening system with time dependent manner.
7. What is meant by plug flow? What is it due to?
Plug flow development observed within the sample across the gap between the cup and bob viscometer.
The material at the inner surface of the cup remains as a solid plug without any flow. This phenomenon
is plug flow.
Plug flow can be minimised by:
1. Using largest bob possible so as to reduce the gap.
2. Increasing the speed of rotation of bob so that stress exceeds yield value and system undergoes
laminar flow.
8. Write note on dilatant flow
A dilatant (also termed shear thickening) material is one in which viscosity increases with the rate
of shear strain. Such a shear thickening fluid, also known by the acronym STF, is an example of a nonNewtonian fluid.
A shear thickening fluid, also called a dilatant, is a Non-Newtonian fluid where the shear viscosity
increases with applied shear stress. This behavior is only one type of deviation from Newton’s Law, and
it is controlled by such factors as particle size, shape, and distribution.
9. Newtonian system
Newtonian system can be characterized by a single coefficient of viscosity for a specific temperature.
Although this viscosity will change with temperature, it does not change with the strain rate. Only a
small group of fluids exhibit such constant viscosity, and they are known as Newtonian system. Eg.
Water, organic solvents.
10. Types off viscometer?
(A) Single Point Viscometer
Capillary viscometer (Ostwald viscometer)
Falling sphere viscometer
(B) Multi point viscometer
Cup and bob viscometer
Cone and Plate viscometer
11.
Define viscoelasticity?
The materials which exhibit both viscous property of liquid and elastic property of solid are known as
viscoelastic. Eg. Lotion, cream, blood, sputum.
12.
Write a note on Heckels equation?
For the compressional method Heckel has suggested the following equation known as Heckels
equation.
InV/V-V𝞪=KP+V0/V0-V𝞪
Where, v= Volume at the applied pressure “P”
V0= Original volume of the powder including the voids.
V𝞪= Volume of the solid powder excluding the voids
K= A constant related to “yield pressure” of the powder
P= Applied pressure
13. Differentiate between elastic and plastic deformation?
Elastic deformation
Plastic deformation
It is a spontaneous and reversible. The
work spent for deformation is
recoverable when the body returns to
the original position.
It is permanent and irreversible. The
work spent for the deformation is
dissipated as heat.
14. Define elastic modulus?
It is the ratio of stress , less than the proportional limit, to the resultant strain.It is the amount of
rigidity or stiffness of a material.
15. Types of modulus?
a) Young’s modulus
b) Shear modulus
c) Bulk modulus
16. Explain rheology of suspension and emulsion
Rheology of suspension:
The flow property of suspensions depends upon their rheological characters. The rheology of
suspension decides the pourability, easy of injectability, sedimentation and elegancy of separation.
Rheology of emulsions:
Dilute emulsions shows newtonian type flow, highly concentrated emulsions and cream show plastic
flow and has excellent thixotropic properties.
17. Define stress
Stress is a deformation force, which measures the internal forces acting within a (deformable) body.
18. Define strain
It is a deformation in terms of relative displacement of the particles comprising the body.
19. Define bulges?
Bulge is a hysteresis loop with a characteristic bulge in the up-curve.
20. Define Spur?
Spur is a sharp point of structural breakdown at lower shear rate in up-curve.
21. Explain the effect of temperature on viscosity?
As the temperature increases , the viscosity of liquid decreases. It is mathematically given as
ɳ= AeEa/RT
Where,
A= A constant
R= Gas constant
T= Thermodynamic temperature
Ea= Energy of activation to move one molecule past another
UNIT III
1. Define emulsion?
An emulsion is a thermodynamically unstable system comprising of atleast two immicible liquid
phases,one is dispersed as globules (dispersed phase) in other liquid phase( continuous phase), stabilized
by the existence of emulsifying agent.
2. Types of emulsion?
a) Oil/ water type emulsion
b) water/ oil type emulsion
c) micro emulsion
d) multiple emulsion or complex emulsion
3. Classification emulsifying agent?
a) synthetic
eg; anionic, cationic, non-ionic
b) semisynthetic
eg; methyl cellulose
c) Natural
eg;gum acacia, starch, gelatin
d) inorganic
eg;milk of magnesia, MgO
e) alcohol
eg; cholesterol
4. Define Multiple emulsions?
Multiple emulsions are emulsions whose disperse phase contains droplets of another phase.
They are made by emulsifying a water-in-oil emulsion with a hydrophilic surfactant to produce a
water-in-oil-in-water system, or an oil-in-water system with a low HLB surfactant to produce an oilin-water-in-oil system. Other forms can be made.
The main disadvantage of a water-in-oil emulsion is its high viscosity because of the oil continuous
phase. Emulsifying a water-in-oil emulsion using surfactants which stabilise an oily disperse phase
can produce multiple water-in-oil-in-water emulsions with an external aqueous phase and lower
viscosity than the primary emulsion.
5. What are instability of emulsion?
a) Flocculation and creaming
b) Coalescence and breaking
c) Phase inversion
6. Define Microemulsions?
Microemulsions are homogeneous transparent systems of low viscosity which contain a high
percentage of both oil and water and high concentrations (15–25%) of emulsifier mixture.
Microemulsions form spontaneously when the components are mixed in the appropriate ratios and
are thermodynamically stable.
In their simplest form, microemulsions are small droplets (diameter 5–140 nm) of one liquid
dispersed throughout another. The droplet size is therefore very much smaller than that of normal
emulsions (which is why microemulsions are transparent) and the droplets are very much more
uniform in size.
To achieve the very low interfacial tension required for their formation it is usually necessary to
include a second amphiphile (the cosurfactant) such as a short-chain alcohol in the formulation. This
cosurfactant is incorporated into the interfacial film around the droplets.
7. How to overcome creaming?
a) Reducing the particle size by means of homogenization.
b) Increasing the viscosity of external phase through adding the thickening agents like methyl
cellulose, tragacanth or sodium alginate.
c) Decreasing the difference in the densities among the dispersed phase and dispersion medium.
8. Factors causing breaking in emulsion?
• The addition of a chemical that is incompatible with the emulsifying agent, thus destroying its
emulsifying ability. Examples include surface active agents of opposite ionic charge, e.g. the
addition of cetrimide (cationic) to an emulsion stabilized with sodium oleate (anionic); the
addition of large ions of opposite charge, e.g. neomycin sulphate (cationic) to aqueous cream
(anionic); and the addition of electrolytes such as calcium and magnesium salts to emulsion
stabilized with anionic surface-active agents;
• Bacterial growth: protein materials and non-ionic surface-active agents are excellent media for
bacterial growth.
• Temperature change: protein emulsifying agents may be denatured and the solubility
characteristics of non-ionic emulsifying agents change with a rise in temperature, heating above
70°C destroys most emulsions. Freezing will also crack an emulsion; this may be due to the ice
formed disrupting the interfacial film around the droplet.
9. Critical point cracking in emulsion?
It is defined as the concentration of the internal phase above which the emulsifying agent can not
produce a stable emulsion. In some emulsion the value may be as high as 74%.
10. Define Phase inversion?
Phase inversion includes the change of emulsion type from o/w to w/o vice versa. Normally it occurs
due to change in temperature as well as composition. This can be prevented by selecting right
emulsifying agents in appropriate concentrations.
11. Identification test for emulsion.
• Dye test
• Electrical conductivity test
• Dilution test
12. Define suspension?
Suspension is a heterogeneous (biphasic) system consisting of a solid phase in a liquid phase. The
solid phase is subdivided in the liquid medium in which the solid is insoluble or sparingly soluble.
Size of the particles approx. 0.1µ.
13. Define Sedimentation volume?
Sedimentation volume is a ratio of the final or ultimate volume of sediment (Vu) to the original volume
of sediment (VO) before settling
14. Degree of flocculation (β)
It is the ratio of the sedimentation volume of the flocculated suspension (F) to the sedimentation
volume of the suspension when deflocculated (Fα).
β = F/ Fα
15. Define Zeta Potential?
The zeta potential is defined as the difference in potential between the surface of the tightly bound
layer (shear plane) and electro-neutral region of the solution.
16. Flocculated Suspensions
In flocculated suspension, formed flocs (loose aggregates) will cause increase in sedimentation rate
due to increase in Size of sedimenting particles. Hence, flocculated suspensions sediment more
rapidly.
In flocculated suspension the loose structure of the rapidly sedimenting flocs tends to preserve in the
sediment, which contains an appreciable amount of entrapped liquid.
The volume of final sediment is thus relatively large and is easily redispersed by agitation.
17. Deflocculated suspensions
In deflocculated suspension, individual particles are settling, so rate of sedimentation is slow which
prevents entrapping of liquid medium which makes it difficult to re-disperse by agitation. This
phenomenon also called ‘cracking’ or ‘claying’.
In deflocculated suspension larger particles settle fast and smaller remain in supernatant liquid So
supernatant appears cloudy in deflocculated suspension
18. Flocculating Agents
Flocculating agents decreases zeta potential of the suspended charged particle and thus cause
aggregation (floc formation) of the particles.
Examples of flocculating agents are:
➢ Neutral electrolytes such as KCl, NaCl.
➢ Calcium salts, Alum
➢ Sulfate, citrates, phosphates salts
19. Write a note on Stoke’s law
Vs = d2 (ρs- ρl) g
……………..
18 η
where vs is the particle's settling velocity (m/s), g is the gravitational acceleration (m/s2), ρp is
the mass density of the particles (kg/m3), and ρf is the mass density of the fluid (kg/m3), η is the
viscosity of the medium.
20. Define creaming?
Creaming is the upward movement of the internal phase in an emulsion. Creaming is the
concentration of globules at the top or bottom of emulsion There are two types of creaming,
a) Upward creaming
b) Downward creaming
UNIT 4
1. What is Micromeritics?
The Science and Technology of small particles is known as Micromeritics.
2. Define Porosity?
Porosity is defined as the ratio of the void volume to the bulk volume of powder. Porosity =
Bulk vol. – true vol./ bulk volume
3. Define Angle of repose.
The angle of repose, of a granular material is the steepest angle of descent or dip of the slope relative to
the horizontal plane when material on the slope face is on the verge of sliding. This angle is in the range
0°–90°.
When granular materials are poured onto a horizontal surface, a conical pile will form. The internal
angle between the surface of the pile and the horizontal surface is known as the angle of repose and is
related to the density, surface area and shapes of the particles, and the coefficient of friction of the
material.
Tan θ = h/r
4. Define Glidants with suitable examples.
Flow activators are commonly referred as glidants. Improve the flowability of powders by reducing
adhesion and cohesion. Eg. Talc, Meg. Stearate
5. Methods of determining surface area.
Adsorption method
Air permeability method
6. Explain particle size.
For a symmetric particle like sphere, it is easy to describe the size by its diameter. But most of the
particle do not show symmetry in their shape. Hence it is expressed in terms of equivalent spherical
diameters. The various ways of expressing equivalent spherical diameter are the following;
a) Surface diameter
b) Volume diameter
c) Projected diameter
d) Stoke’s diameter
7. Explain particle size distribution.
Distribution of different sized particles in a powder is called particle size distribution.
From the data of particle size distribution, average particle size of a powder can be
calculated.
8. What are the various methods for determination of particle size.
a) Microscopic techniques
b) Sieving techniques
c) Sedimentation techniques
d) Low angle light scattering technique
e) Coulter counter (electrical method) technique
9. What are the advantages and disadvantages of microscopic techniques.
Advantages:
A) Presence of agglomerates can be easily detected and avoided
Disadvantages:
a) The diameter of the particles represents only length and breadth and not the width.
b) Atleast 300 to 500 particles should be counted to get a reliable data and hence the
method is tedious.
10. Explain sieving techniques and various grades of powder.
Sieving technique is normally a separation technique. It can measure projected perimetersquare and circle and particle size ranging from 5-125000μm. This technique gives
average weight.
Grades of powder:
a) Coarse powder
b) Moderately coarse powder
c) Moderately fine powder
d) Fine powder
e) Very fine powder
11. Define stoke’s law.
V=d2(ρs – ρl)g/18ηl
Where,
V = Average velocity of sedimentation of particles (cm/sec)
d= diameter of the particle in cm
ρs – ρl= density of the dispersed phase and dispersion medium respectively
g= acceleration due to gravity
ηl= viscosity of the dispersion medium
12. Define LALLS
In this laser diffraction principle particle size is measured accurately and precisely. LALLS technique is
speedy, easy and reproducible for particle size distribution. Particle ranging from 0.5μm to 3500μm can be
measured. This technique is non-destructive and only small amount of sample (10mg) is enough.
13. What is meant by coulter counter method?
It is used for measuring particle volume which is converted into diameter. The particle ranging from 0.5500μm can be measured by this method and gives number distribution. The size expressed as volume
diameter(dv).
14. What is meant by specific surface.
The specific surface is the surface area per unit volume Sv or per unit weight Sw
Sv= surface area of particles / volume of particles
15. Define determination of surface area of powder.
Surface area of the powder can be derived indirectly from the size and size distribution
obtained by the methods such as microscopy, sieving, sedimentation. Direct calculation of
surface area can be done using adsorption and air permeability method.
16. BET equation?
17. Explain the properties of powder.
The size distribution and the surface area are the two fundamental properties of the
powders.
18. Define density of powder and its types.
Density is the ratio of mass to volume of the materials through considering the three sorts
of volume of powders.
Types
a) Bulk density
b) True density
c) Granular density
19. Define bulk density.
It is the ratio between given mass of a powder and its bulk volume.
Bulk density = mass of the powder/ bulk volume of the powder
20. Define true density.
It is the ratio between given mass of the powder and its true volume(v) is called true
density.
True volume = bulk volume – void volume
21. Define granular density.
Granular density is the ratio of mass of powder to the granule volume of the powder.
Granular density (ρg)= mass of the granular powder/ granule volume
22. Define porosity of powder.
Porosity of powder is defined as the ratio of void volume to bulk volume of the powder
packing.
Porosity (ε) = void volume/ bulk volume
Porosity is usually expressed as percent i.e, εx100
23. What are the flow properties of powder and granules.
a) Shape
b) Size
c) Porosity and density
d) Moisture of the powder
24. Define compaction of powder.
Transformation of powders into coherent specimen caused by applied pressure. It is the
compression and consolidation of two phases due to applied force.
Compaction = compression + consolidation
25. Determine the air permeability method
Air permeability method is used to determine the surface area with an instrument
called Fisher sub-sieve sizer. This method is widely used to control batch to batch
variations in specific surface of powders.
UNIT 5
1. Define stability and types
➢ Stability is stated as the time period through which a bio active or drug product maintain its
same properties and characteristics that is obsessed during manufacturing period.
➢ Types - physical, chemical, therapeutic, toxicology
2. Define Order of reaction?
The manner in which the concentration of drug (or reactants) influences the rate of reaction or
process is called as order of reaction.
3. Define zero-order reaction?
In a zero-order reaction the rate of reaction (decomposition, dissolution, drug release) is independent
of the concentration of the reactants, i.e. the rate is constant.
A constant rate of drug release from a dosage form is highly desirable.
4. Define First-order reaction?
In a First-order reaction the rate of reaction is directly proportional to the concentration of the drug)
(i.e. greater the concentration, faster the reaction)
Eg: Hydrogen peroxide degradation
5. Define Half-life (t1/2)?
This is the time taken for the concentration (of, say, a drug in solution) to reduce by a half.
Zero order half life – t1/2 = Co/2k
First order - t1/2 = 0.693/k
6. Define pseudo first-order reaction?
If there are two reactants and one is in large excess, the reaction may still follow first-order kinetics
because the change in concentration of the excess reactant is negligible. This type of reaction is a
pseudo first-order reaction.
7. Write a note on importance of stability studies
• Employed for delivering evidences of the change in quality of drug product with time
• Governing endorsed storage conditions
• Confirming shelf life for the drug product
• Determining container closure system suitability
8. Define solid state drug stability
It is defined as the capability of a particular formulation in a specific container /closure system, to
retain its physical, chemical, microbiology, therapeutic specification.
9. Define hydrolysis
Hydrolysis is a process of decomposition involving the splitting of a bond and the addition of the
hydrogen cation and the hydroxide anion of water
10. Define oxidation
Oxidation is the loss of electrons during a reaction by a molecule, atom or ion. Oxidation occurs
when the oxidation state of a molecule, atom or ion is increased
What is meant by chemical degradation of drugs
This is a separation of chemical compound into elements or simpler compounds. Change in the
chemical nature of the drug is called chemical degradation.
11. Define accelerated stability studies
Stability study is performed to detect the product shelf life via accelerating the rate of
decomposition rather by increasing the temperature of reaction conditions.
12. Explain Arrhenius equation
It describes the effect of temperature on rate of a reaction. According to Arrhenius for every 10ᵒ
increase in temperature the speed of reaction surges about 2-3 times.
k=Ae-Ea/RT
13. Define storage of pharmaceutical products
Drug storage and maintenance, it must be ensure that drugs which are stored remain preserved
during the storage. There should not be any damage due to high temperature or exposure to sunlight.
The drugs are to be stored as per the prescribed conditions.
14. Define reaction kinetics
In chemical kinetics reaction order within the relation with specific reactants is stated as the index,
or exponent, to which its concentration term in the rate reaction is raised
r= k[A]2[B]1
15. Equation of zero order reaction
A zero order reaction is a reaction having rate independent of concentration of reactant i.e.
concentration of reactant will not speed up or slow down the reaction
Rate= -d[A]/dt=k[A]0=k=constant
16. Define pseudo zero order reaction
A reaction which is not first order reaction naturally but made first order by increasing or decreasing
the concentration of one or other reactant is known as pseudo zero order reaction
17. Equation of first order reaction
First order reaction is a reaction that continues at a rate that depends linearly only on one reactant
concentration.
Rate = -d[A]/A=k[A]1=k[A]
18. Define second order reaction
In a second order reaction the sum of the exponents in the rate law is equal to two.
19. Define rate constant
When the concentration of the reactant is unity then the rate of reaction is known as rate constant it
is also called specific reaction rate
20. Define photolytic degradation
The drug molecule is degrading by exposure of light it affects substantial degradation of drug molecule.
21. Define dielectric constant
It is the ratio of the permittivity of a substance to the permittivity of free space
logK=logKᵋ-KZAZB/ᵋ
22. Mechanism of solid drug degradation
• Dehydration
• Racemization
• Isomerization
• Oxidation
• Photo degradation
• Decarboxylation
23. Define the physical chemical factors influencing the chemical degradation of pharmaceutical
products
Physical:
• Loss of water
• Absorption of water
• Crystal growth
• Polymorphism with colour changes
Chemical:
• Hydrolysis
• Oxidation
• Carboxylation
• Isomerization
• polymerization
• Decarboxylation
PHARMACOLOGY - I
UNIT-I
.
1. Define drug?
It is derived from French word “drogue – means dry herb”. It is a single active chemical entity present
in medicine that is used for diagnosis prevention, treatment or palitation disease or intended to modify or
explore physiological system
2. Define pharmacology?
Pharmacology is the science of drugs (Greek: Pharmacon—drug; logos—study). It deals with interaction
of exogenously administered chemical molecules with living systems, or any single chemical substance
which can produce a biological response is a ‘drug’.
3. Pharmacokinectics?
Pharmacokinetics (Greek: Kinesis—move- ment)—What the body does to the drug. This refers to
movement of the drug in and alteration of the drug by the body; includes absorption, distribution, binding/
localization/ storage, biotransformation and excretion of the drug.
4. Toxicology?
It is the study of poisonous effect of drugs and other chemicals (household, environmental pollutant,
industrial, agricultural, homicidal) with emphasis on detection, prevention and treatment of poisonings. It also
includes the study of adverse effects of drugs.
5. Chemotherapy?
It is the special type of treatment for systemic infection/ malignancy with specific drugs that have
selective toxicity for the infecting organism/ malignant cell with no/minimal effects on the host cells.
6. Disadvantages of oral routes?
• Action of drugs is slower and thus not suitable for emergencies.
• Unpalatable drugs are difficult to Administer
• Absorption of drugs may be variable and erratic; certain drugs are not absorbed.
• May cause nausea and vomiting (emetine).
• Drugs are destroyed by low gastric pH or by the digestive enzymes before enter into the circulation
7. Advantages of sublingual route?
• Absorption is relatively rapid—action can be produced in minutes.
• The chief advantage is that liver is bypassed and drugs with high first pass metabolism can be absorbed
directly into systemic circulation.
8. Absorption?
Absorption is movement of the drug from its site of administration into the systemic circulation. Except
when given i.v., the drug has to cross biological membranes.
9. Bio availability?
Bioavailability refers to the rate and extent amount of drug enter in to the systemic circulation in its
unchanged form by given dosage form. It is a measure of the fraction (F) of administered dose of a drug that
reaches the systemic circulation in the unchanged form.
F= amount of drug that enter systemic circulation
Dose administered
10. Bioequivalence?
It is the study of comparison of bioavailability of different formulation of same drug.
11. Distribution?
Distribution is a branch of pharmacokinetics which describes the reversible transfer of a drug from one
location to another within the body. Once a drug enters into systemic circulation by absorption or direct
administration, it must be distributed into interstitial and intracellular fluids.
12. Volume of distribution?
Volume of distribution (VD, also known as apparent volume of distribution) is the theoretical volume
that would be necessary to contain the total amount of an administered drug at the same concentration that it
is observed in the blood plasma. It is defined as the distribution of a medication between plasma and the rest
of the body after oral or parenteral dosing.
V=
dose administered i.v
Plasma concentration
13. Biotransformation?
Biotransformation means chemical alteration of the drug in the body. The primary site for drug
metabolism is liver; others are—kidney, intestine, lungs and plasma. Biotransformation of drugs may lead to
the following.
(i)
Inactivation
(ii)
Active metabolite from an active drug
(iii) Activation of inactive drug
14. Excretion?
Excretion is a process by which metabolic waste is eliminated from an organism. Excretion is the
passage out of systemically absorbed drug. Drugs and their metabolites are excreted in urine, feces, exhaled
air, saliva and sweat and milk. Kidney is the major organ for excretion.
15. Prodrug?
A prodrug is a medication or compound that, after administration, is metabolized (i.e., converted
within the body) into a pharmacologically active drug. Eg. Levodopa – dopamine
16. Tachyphylaxis?
Tachyphylaxis (Tachy-fast,phylaxis-protection). It refers to rapid development of tolerance when
doses of a drug repeated in quick succession result in marked reduction in response.
17. Tolerance?
It refers to the requirement of higher dose of a drug to produce a given response. Loss of therapeutic
efficacy (e.g. of sulfonylureas in type 2 diabetes, or of β 2 agonists in bronchial asthma), which is a form of
tolerance, is often called ‘refractoriness’. Tolerance is a widely occurring adaptive biological phenomenon.
18. Routes of administration?
Local/topical: deeper tissues, arterial supply
Systemic : oral, sublingual, rectal, cutaneous, inhalation, nasal , parental
Parental : subcutaneous, Transdermal, intramuscular, intravenous.
19. Enzyme induction?
Enzyme induction is a process in which a drug induces the expression of an enzyme. Apparent increase
in enzyme activity can also occur by enzyme induction, i.e. synthesis of more enzyme protein. An enzyme
inducer is a type of drug that increases the metabolic activity of an enzyme either by binding to the enzyme
and activating it, or by increasing the expression of the gene coding for the enzyme.
20. Plasma clearance?
The clearance of a drug is the theoretical volume of plasma from which the drug is completely removed
in unit time. It can be calculated as
CL = Rate of elimination/C
where C is the plasma concentration.
21. Plasma half life?
The Plasma half-life (t½) of a drug is the time taken for its plasma concentration to be reduced to half
of its original value.
22. Agonist?
An agent which binds and activates a receptor to produce an effect similar to that of the physiological
signal molecule. It have both affinity and maximal intrinsic activity (IA = 1), e.g. adrenaline, histamine,
morphine.
23. Source of drugs?
PLANTS: Quinine, Digoxin, ephedrine
ANIMALS: Insulin extracted from the pork and beef pancreas
MINERALS: Ferrous sulphate for anaemia
SYNTHETIC: Synthetic corticosteroids
RECOMBINANT DNA TECHNOLOGY: Production of human insulin by introducing coded DNA into
harmless strain of E. coli.
SEMISYNTHETIC: Homatropine
UNIT-II
1. Receptor?
It is defined as a macromolecule or binding site located on the surface or inside the effector cell that serves
to recognize the signal molecule/drug and initiate the response to it, but itself has no other function.
a. G-protein coupled receptors (GPCRs)
b. Ion channel receptor
c. Enzyme linked receptor
d. Nuclear receptor
2. Partial agonist?
An agent which activates a receptor to produce sub-maximal effect but antagonizes the action of a full
agonist. It have affinity and sub-maximal intrinsic activity (IA between 0 and 1), e.g. dichloroisoproterenol
(on β adrenergic receptor), pentazocine (on μ opioid receptor)
3. Inverse agonist?
An agent which binds and activates a receptor to produce an effect in the opposite direction to that of
the agonist. It have affinity but intrinsic activity with a minus sign
4. Antagonist?
An agent which binds and prevents the action of an agonist on a receptor or the subsequent response,
but does not have any effect of its own. Eg. Atropine
5. Pharmacodynamics?
Pharmacodynamics (Greek: dynamis—power)—What the drug does to the body. This includes
physiological and biochemical effects of drugs and their mechanism of action at organ system /subcellular/
macromolecular levels.
6. Functions of receptors?
✓ To propagate regulatory signals from outside to inside the effector cell when the molecular species
carrying the signal cannot itself penetrate the cell membrane.
✓ To amplify the signal.
✓ To integrate various extracellular and intracellular regulatory signals.
✓ To adapt to short term and long term changes and maintain homeostasis.
7. Drug potency and drug efficacy?
Drug potency which refers to the amount of drug needed to produce a certain response. Drug
efficacy and refers to the maximal response that can be elicited by the drug. Aspirin is less potent as well
as less efficacious analgesic than morphine.
8. Synergism?
Synergism (Greek: Syn—together; ergon—work) When the action of one drug is facilitated or
increased by the other, they are said to be syner- gistic. The combined effect of two drugs effect is higher
than the individual effect. Aspirin + paracetamol as analgesic/ antipyretic.
9. Competitive antagonism?
Competitive antagonism (equilibrium type) The antagonist is chemically similar to the agonist,
competes with it and binds to the same site to the exclusion of the agonist molecules. Because the
antagonist has affinity but no intrinsic activity no response is produced.
10. Factors affecting absorption?
Aqueous solubility, Concentration, Lipophilicity, 𝑃 𝐻 and ionization, GI motility, disintegration and
dissolution time, Local blood flow and route of administration
11. First pass metabolism?
The first pass effect is a phenomenon of drug metabolism whereby the concentration of a drug is
greatly reduced before it reaches the systemic circulation. It a process in which a drug administered by
mouth is absorbed from the gastrointestinal tract and transported via the portal vein to the liver, where it
is metabolized. As a result, in some cases only a small proportion of the active drug reaches the systemic
circulation and its intended target tissue. First-pass metabolism can be bypassed by giving the drug via
sublingual or buccal routes.
12. Teratogenicity?
It refers to the capacity of a drug to cause foetal abnormalities when administered to the pregnant
mother. Teratogens halt pregnancy or produce birth defect. Eg: Thalidomide produce phocomelia.
13. Idiosyncrasy?
It is genetically determined abnormal reactivity to a chemical. In addition, certain bizarre drug effects
due to peculiarities of an individual (for which no definite genotype has been described) are included
among idiosyncratic reactions e.g Barbiturates cause excitement and mental confusion in some
individuals.
14. Carcinogenicity?
Carcinogenicity is the ability or tendency of a chemical to induce tumors (benign or malignant),
increase their incidence or malignancy, or shorten the time of tumor occurrence when it is inhaled,
ingested, dermally applied, or injected. Eg. Chlorambucil , Cyclosporine
15. What are the secondary messengers in g protein coupled receptor?
✓ Adenyl cyclase- cAMP-opens calcium channels
✓ Phospholipase C: Inositol triphosphate-increases intracellular calcium levels
✓ Diacylglycerol: recruits protein kinase C and phosphorylated intracellular proteins.
16. JAK-STAT binding receptors?
These receptors differ from RTKs in not having any intrinsic catalytic domain. Agonist induced
dimerization alters the intracellular domain conformation to increase its affinity for a cytosolic tyrosine
protein kinase JAK (Janus Kinase). On binding, JAK gets activated and phosphorylates tyrosine
residues of the receptor, which now bind another free moving protein STAT (signal transducer and
activator of transcription). This is also phosphorylated by JAK. Pairs of phosphorylated STAT
dimerize and translocate to the nucleus to regulate gene transcription resulting in a biological response.
17. Physiological antagonism?
Two drugs act on different receptors or by different mechanisms, but have opposite overt effects
on the same physiological function, i.e. have pharmacological effects in opposite direction.
✓ Histamine and adrenaline on bronchial muscles and BP.
✓ Hydrochlorothiazide and triamterene on urinary K + excretion.
✓ Glucagon and insulin on blood sugar level.
18. Receptor down regulation?
Receptor down regulation is mediated by specific loss of cell surface receptors,which occurs
via an energy-dependent internalization of the ligand-receptor complex,in which the principal
internalization pathway involves processing of the receptor-ligand complex into lysosomes and
subsequent degradation of the receptor
19. Drug – Drug interaction
It is the modification of the effect of one drug by the prior concomitant administration of another
(precipitant drug
20. Pharmacovigilance?
Pharmacovigilance has been defined by the WHO (2002) as the ‘science and activities relating to the
detection, assessment, understanding and prevention of adverse effects or any other drug related problems
UNIT-III
1. What are the contraindications for the use of propranolol?
• Reversible airways diseases, particularly asthma or chronic obstructive pulmonary disease (COPD)
• Slow heart rate (bradycardia) (<60 beats/minute)
• Shock
• Severe low blood pressure
• Cocaine toxicity
• Propranolol can accentuate myocardial insufficiency and can precipitate CHF/edema by blocking
sympathetic support to the heart, especially during cardiovascular stress.
2. Neurotransmitter and examples?
Neurotransmitters are endogenous chemicals that enable neurotransmission. It is a type of chemical
messenger which transmits signals across a chemical synapse, such as a neuromuscular junction, from one
neuron (nerve cell) to another "target" neuron, muscle cell, or gland cell. Eg: Serotonin, Acetylcholine,
Dopamine, Norepinephrine
3. Neurotransmitters of CNS and ANS?
ANS: Adrenaline,nor adrenaline, acetylcholine.
CNS: .Amino Acids: GABA, glycine, glutamate (glutamic acid) and aspartate (aspartic acid). Amines:
Noradrenaline, adrenaline, dopamine, serotonin. peptides: substance p
4. Drugs to treat glaucoma?
• β Adrenergic blockers: Timolol, betaxolol
• α Adrenergic agonists: Dipivefrine
• Prostaglandin analogues: Latanoprost Travoprost
• Carbonic anhydrase inhibitors: Acetazolamide
• Miotics: Brimonidine/dorzolamide
• Hypertonic mannitol, Acetazolamide, Topical β blocker: Timolol, Apraclonidine
5. Mechanism of succinylcholine?
Succinylcholine have affinity and sub-maximal intrinsic activity at Nmreceptor.It acts on sodium
channels, open them and causes initial twitching and fasciculation. It does not dissociate rapidly from the
receptors resulting in prolonged depolarisation and inactivation of Na+ channels
6. Therapeutic use of adrenaline?
✓ Treatment of acute and moderately severe attacks of bronchial asthma,
✓ Potent antiallergic agent,
✓ Treatment of heart block,
✓ Topical haemostatic agent to produce vasoconstriction
7. Examples of ion channel?
Ligand gated ion channels [nicotinic receptors]
voltage gated ion channels [Na+ channels, Calcium channel]
8. How does a local anaesthetics work?
The LAs block nerve conduction by decreasing the entry of Na + ions during upstroke of action
potential (AP). As the concentration of the LA is increased, the rate of rise of AP and maximum depolarization
decreases causing slowing of conduction. Finally, local depolarization fails to reach the threshold potential
and conduction block ensues.
9. Advantages of combining adrenaline along with local anaesthetics?
• Adrenaline is combined with lignocaine to enhance the duration of action, decreases toxicity to
achieve vasoconstriction.
• When lignocaine and adrenaline are injected they prevent pain signals passing from the area of
injection to the brain and so numb the area.
10. Name two anticholinergics used in parkinsonism?
Biperiden
Benzhexol Procyclidine
11. Symptoms and treatment of organophosphorus poisoning?
Symptoms: Fall in BP, bradycardia or tachycardia, cardiac arrhythmias, vascular collapse. Irritation of
eye, lacrimation, salivation, swea-ting, copious tracheo-bronchial secretions, miosis, blurring of vision,
bronchospasm, breathlessness, colic, involuntary defecation and urination. Muscular fasciculations, weakness,
respiratory Paralysis
Treatment:
1. Termination of further exposure to the poison— fresh air, wash the skin and mucous membranes
with soap and water, gastric lavage according to need.
2. Maintain patent airway, positive pressure respiration if it is failing.
3. Supportive measures—maintain BP, hydration, control of convulsions with judicious use of
diazepam.
4. Specific antidotes—atrophine, Cholinesterase reactivators(pralidoxime).
12. Name any two neuromuscular blocking agents? And its clinical uses?
d-Tubocurarine, Succinylcholine, Pancuronium and Decamethonium. Used in endotracheal intubation,
relief of laryngospasm, endoscopy and electroconvulsive therapy.
13. Name any two cholinomimetic alkaloids?
1. Pilocarpine
2. Lobeline
3. Dimethylphenyl piperazium
4. Oxotremorine
14. Mention four drugs which cause bronchospam?
• Bethanachol
• Propranolol
• Pancuronium
15. Neostigmine How does a local Anaesthetic work?
• The LAs block nerve conduction by decreasing the entry of Na+ ions during upstroke of action
potential (AP).
• As the concentration of the LA is increased, the rate of rise of AP and maximum depolarization
decreases causing slowing of conduction.
• Finally, local depolarization fails to reach the threshold potential and conduction block ensues.
16. Drugs used for Myasthenia gravis?
Cholinesterase inhibitors. Drugs like Pyridostigmine, Neostigmine
Corticosteroids: Prednisone
Immunosuppressants like azathioprine, cyclosporine or mycophenolate
17. Treatment for Belladonna poisoning
✓ Physostigmine 0.5–2 mg i.v. repeated as required is the specific antidote for poisoning with belladonna
or other anticholinergics.
✓ It penetrates bloodbrain barrier and antagonizes both central and peripheral actions.
✓ Neostigmine does not block the central effect, but is less risky.
18. Name the drugs acting on autonomic ganglia?
Nicotine Acetylcholine Lobeline Carbachol Pilocarpine Tetramethyl ammonium Varenicline
19. α and β adrenergic blockers?
Labetalol
Carvedilol
20. Reversible anticholinesterases?
Physostigmine Tacrine Neostigmine Pyridostigmine
Edrophonium Rivastigmine, Donepezil,
Galantamine
UNIT-IV
1. Stages of anaesthesia?
• Stage of analgesia
• Stage of excitement and delirium
• State of surgical anaesthesia
• Stage of medullary paralysis
2. Define genral anaesthetics?
General anaesthetics (GAs) are drugs which produce reversible loss of all sensation and consciousness.
The cardinal features of general anaesthesia are:
• Loss of all sensation, especially pain
• Sleep (unconsciousness) and amnesia
• Immobility and muscle relaxation
• Abolition of somatic and autonomic reflexes.
3. Name 2 inhalation general anaesthetics?
• Nitrous oxide
• Ether
• Halothane
• Isoflurane
• Desflurane
4. Pre anaesthetic medication?
Preanaesthetic medication refers to the use of drugs before anaesthesia to make it more pleasant and
safe. Eg: Diazepam Promethazine Pethidine Atropine Metoclopramide
5. Dissociative anaesthetics?
Dissociative anaesthesia is a state in which the anaesthetized patient feels totally dissociated from the
surroundings. Two drugs ketamine and fentanyl are used in certain situations when an anaesthesia like
state is desired but unconsciousness would be disadvantageous.
6. What are hypnotics? Give examples?
A drug that induces and/or maintains sleep, similar to normal arousable sleep. Eg: Diazepam
Flurazepam Nitrazepam Alprazolam Temazepam
7. Sedatives?
A drug that subdues excitement and calms the subject without inducing sleep, though
drowsiness may be produced. Sedation refers to decreased responsiveness to any level of stimulation
8. Name two effects of phenytoin?
✓ Phenytoin prolongs the inactivated state of voltage sensitive neuronal Na+ channel and reduces the
neuronal excitability.
✓ Phenytoin is not a CNS depressant; some sedation occurs at therapeutic doses, but this does not
increase further with dose; rather toxic doses produce excitement and muscular rigidity.
✓ The most outstanding action is abolition of tonic phase of maximal electroshock seizures, with no
effect on or prolongation of clonic phase
9. Acute alcoholism?
Acute alcoholic intoxication Unawareness, unresponsiveness, stupor, hypotension, gastritis,
hypoglycaemia, respiratory depression, collapse, coma and death.
10. Centrally acting muscle relaxants?
Mephenesin, Carisoprodol, Chlorzoxazone, Chlormezanone, Methocarbamol.
UNIT-V
1. What are atypical antipsychotics?
These are drugs having a salutary therapeutic effect in psychoses. Clozapine ,Aripiprazole, Risperidone
Ziprasidone, Olanzapine Amisulpiride, Quetiapine, Zotepine.
2. Name any two dopaminergic agonist?
✓ Bromocriptine
✓ Ropinirole and Pramipexole
✓ Selegiline (Deprenyl)
3. Enlist four antiparkinsonism agents?
✓ Rasagiline
✓ Amantadine
✓ Ropinirole and Pramipexole
✓ Selegiline (Deprenyl)
✓ Trihexyphenidyl
4. What are Endogenous peptides?
Dynorphins
Enkephalins Endomorphins
5. Give two symptoms of morphine poisoning?
Stupor or coma, flaccidity, shallow and occasional breathing, cyanosis, pinpoint pupil, fall in BP and
shock; convulsions may be seen in few, pulmonary edema occurs at terminal stages, death is due to respiratory
failure.
6. Define drug dependence and give examples of drug showing dependence?
Drug dependence is a state in which use of drugs for personal satisfaction is accorded a higher priority
than other basic needs, often in the face of known risks to health.
Drugs producing physical dependence are—opioids, barbiturates and other depressants including alcohol
and benzodiazepines. Stimulant drugs, e.g. amphetamines, cocaine produce little or no physical
dependence.
7. Write the mechanism of action of carbamazepine?
Carbamazepine modifies maximal electroshock seizures as well as raises threshold to PTZ and
electroshock convulsions. Though its action on Na + channels (prolongation of inactivated state) is similar to
phenytoin, the profile of action on neuronal systems in brain is different.
8. Narcotic Analgesics and its Antagonists?
A drug that selectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without
significantly altering consciousness through opioid receptors. Eg: Morphine Codeine
The opioid antagonists bind with high affinity to opioid receptors but fail to activate the receptor-mediated
response. Eg: Naloxone, Naltrexone
9. Classify Antidepressants Drugs
✓ MAO inhibitors: Isocarboxazid, Iproniazid, Phenelzine and Tranylcypromine
✓ Tricyclic antidepressants: Imipramine, Amitryptiline, Doxepin, Dothiepin
✓ Selective Serotonin reuptake inhibitors: Fluoxetine, Fluvoxamine, Sertraline
10. Name any two antianxiety drugs?
Diazepam Chlordiazepoxide Oxazepam Lorazepam Alprazolam
11. Anti Parkinsonian drugs?
• Trihexyphenidyl
• Levodopa and carbidopa
• Biperiden
• Promethazine
• Procyclidine
12. Drug dependence?
Drugs capable of altering mood and feelings are liable to repetitive use to derive euphoria, recreation,
withdrawal from reality, social adjustment, etc. Drug dependence is a state in which use of drugs for personal
satisfaction is accorded a higher priority than other basic needs, often in the face of known risks to health.
13. Drugs used for the treatment of Mania?
• Lithium carbonate
• Sodium valproate
• Carbamazepine
• Olanzapine
• Risperidone
14. Name two COMT inhibitors?
Entacapone, Tolcapone
15. Psychotomimetics?
These are drugs which alter mood, behaviour, thought and perception in a manner similar to that seen
in psychosis. Eg: Lysergic acid diethylamide (LSD), Mescaline, Phencyclidine, Tetrahydrocannabinol
16. CNS stimulants?
Drugs that primarily stimulate the central nervous system through non selective excitation are known
as CNS stimulants. Eg; Caffeine Theophylline Theobromine
Nicotine Cocaine Amphetamine
Methyl phenidate.
17. SSRI’s ?
Fluoxetine, Fluvoxamine, Sertraline
18. MAO inhibitors?
Isocarboxazid, Iproniazid, Phenelzine and Tranylcypromine
19. DOPAMINERGIC AGONISTS?
The DA agonists can act on striatal DA receptors even in advanced patients who have largely lost the
capacity to synthesize, store and release DA from levodopa. Eg; Bromocriptyne, Ropinirole and
Pramipexole
20. Name two Peripheral decarboxylase inhibitors?
• Carbidopa
• Benserazide
PHARMACOGNOSY AND PHYTOCHEMISTRY - I
UNIT-I
1. Define Pharmacognosy.
Pharmacognosy is defined as scientific and systematic study of crude drugs obtained from plants,
animals and mineral origin along with history, method of cultivation, collection and preparation for the market.
2. Write about Hippocrates.
• Hippocrates (460-370 BC) was a Greek Physician, he worked on human anatomy and physiology
particularly on circulatory and nervous system.
• He prepared famous oath for physicians which are still taken by the physicians. He is known as father
of medicine.
3. Write about C.A.Seydler.
• He is the father of Pharmacognosy.
• Seydler was a German scientist he wrote a book ANALECTA PHARMACOGNOSTICA in 1815.
• In this book he used word “Pharmakognosie” first time he coined this word by two greek words.
• Pharmakon-Drug, Gnosis-to acquire knowledge of.
4. Who introduced the molecular pharmacognosy in which university?
• In 1995 Huang luqi proposed the idea of molecular pharmacognosy.
• He distributed molecular pharmacognosy in Peking University Medical Press in June 2000.
5. What are the different sources of crude drugs?
• Plant sources of drugs.
• Animal sources of drugs.
• Mineral sources of drugs.
• Marine sources of drugs.
• Plant tissue culture techniques as a source of drugs.
6. Give the example for plant sources of drug.
• Entire plants e.g.ergot, ephedra
• Parts of plant e.g.senna leaves, nux vomica seeds
• Exudation of plants e.g. gums, resins
7. Write the animal sources of drugs with examples.
• Entire animals. E.g. cantharides
• Glandular secretion e.g. Thyroid, insulin.
• Animal extractives e.g. Liver extract.
• Enzymes e.g. Pancreatin, pepsin
8. Write the uses of marine sources of drugs.
• Antiviral substances.
• Antitumor compounds.
• Antiparasitic compounds.
• Anticoagulants.
• Antimicrobial compounds.
• Cardiovascular agents.
• Proteins
• Prostaglandin
• Agrochemical usage
9. What are cardiovascular agents obtained from marine sources of drugs?
• Anthopleurins
• Eptatretin
• Saxitoxina
• Laminine
• Spongosine
• Holothurine
• Asterosaponine
10. Give examples of phytoconstituents developed by plant tissue culture.
• Atropa belladonna-Hairy root culture-Atropine
• Rauwolfia serpentine-suspension culture-Reserpine
• Carica papaya-Cell culture-Papain
• Digitalis lanata-suspension culture-Digoxin
11. What are the antimicrobial agents obtained from marine sources of drugs?
• Cephalosporin
• Istamycin A and B
• Cephalothin sodium
12. Define Organogenesis.
Organogenesis is the common technique of micro propagation which involves development of tissue
of adventitious or axillary buds directly or indirectly from the explants.
13. Define somatic embryogenesis.
Somatic embryogenesis is a developmental method which produces soma clonal variants, developing
artificial seeds and secondary metabolites.
14. Define Plant tissue culture.
Plant tissue culture is a group of techniques used to encourage or grow plant cells, tissues or organs
under sterile conditions on a nutrient culture medium of known compositions.
15. Define Crude drugs.
Crude drugs can be regarded as the substance either used directly or indirectly as a drug which have
not been changed or modified in its chemical composition.
16. Define organized drugs with examples.
Organized drugs are those materials which consist of cellular material or which contain cells. These
drugs are mostly from plant sources.
E.g. senna leaf, nuxvomica seeds
17. Define unorganized drugs with examples.
Unorganized drugs are those materials which have uniform structure and are not made up of cells.
They are usually derived from plants parts or animals by means of extraction process such as incision.
E.g. Acacia, Tragacanth
18. Biological source, family, constituents and uses of Opium.
• Biological source – Papaver somniferum Linn
• Family – Papaveraceae
• Constituents – It contains more than 30 alkaloids. They are classifies as:
a) Phenanthrene alkaloids – Morphine, codeine, thebain
b) Benzylisoquinoline alkaloids – Papaverine, noscapine
Uses: as astringent, Sedative and hypnotic.
5. Chemical test for Aloes.
Bromine test: To some clear solution of aloes, freshly prepared saturated bromine solution is added. A
yellow precipitate is observed due to the formation of tetrabromaloin.
Nitric acid test: To some clear solution of aloes, 2 ml of nitric acid is added
Cape aloes – Vivid green colour
Curacao aloes – pale brownish yellow colour
Socotrine aloes – pale brownish yellow colour
6. Define latex and give examples.
Latex is an emulsion or suspension in which the continuous phase is an aqueous solution of mineral
salts, proteins, sugars, tannins, alkaloids etc. and the suspended particles are oil droplets, resin, gum, proteins
etc.
It is generally white in color.
E.g. Opium
7. Define dried juice and give examples.
The incisions are made with respective plant part e.g. fleshy leaves of aloes or trees stem of Kino. The
juicy material which oozes out is collected and dried. E.g. aloes
8. Define extract and give examples.
Extracts are prepared by evaporating aqueous decoction of plant parts or by animal source. E.g. Black
catechu, Gelatin
9. Define resin and give examples.
Resins are amorphous mixtures of essential oils and oxygenated products of terpenes, transparent or
translucent solids, semisolid or liquid substances. They have complex chemical nature.
E.g. Asafoetida
10. Write chemical constituents, uses and adulterants of Pale catechu.
• Chemical constituents: catechin, catechutannic acid, other constituents Catechu red, Quercetinand
gambier fluorescin.
• Uses: Mainly used as astringent in the treatment of diarrhea and a local astringent in the form of
lozenges. Used for tanning and dyeing purposes.
• Adulterants: The starch, astringent extracts and mineral matters like clay, ferric hydroxide etc.
11. Write chemical constituents, uses and adulterants of Asafoetida.
• Chemical constituents: Volataile oil which contains pinene and disulphides, resin and gum. It also
contains free ferulic acid and ferulic acid with asaresinol.
• Uses: It is a powerful nervine tonic used in the treatment of hysteria. It is bowel stimulant, also used
as flavouring agent.
• Adulterants: Red clay, wheat flour, chalk and gum acacia
12. Write chemical constituents, uses and adulterants of balsam of Peru.
• Chemical constituents: Cinnamein, benzyl benzoate, benzyl cinnamate.
• Uses: Used internally as expectorant and antiseptic,
Externally as parasiticide and antiseptic.
• Adulterants: Alcohol, fixed oils, turpentine, copaiba, perugen etc.
13. Biological source, family, constituents and uses of balsam of tolu.
• Biological source –obtained by making incision in the trunk of Myroxylon balsamum, Family –
Leguminosae
• Constituents – oily liquid (benzyl benzoate and benzyl cinnamate), esters of toluresinotannol, free
benzoic acid, styrol and cinnamic acid.
21. Chemical constituents and uses of myrrh.
Resin, volatile oil and gum.along with this contains α, β, γ-cummiphoric acid and phenolic resins α, β, heerabomyrrhol. Others terpene, eugenol and cuminic aldehyde.
CHAPTER – 4
CLASSIFICATION OF DRUGS
1. Classify organized drugs with examples.
• Woods – Quassia, Sandalwood
• Leaves – Digitalis, Senna
• Barks – Cinchona, Cinnamon
• Flowering parts – Clove, Saffron
• Fruits – Amla, Capsicum
• Seeds – Bitter almond, Cardamom
• Roots and rhizomes – Ashwagandha, Ginger
2. Classify unorganized drugs with examples.
• Dired latex – Opium, Papain
• Dried juice – Aloe, Kino
• Dried extracts – Agar, Black and pale catechu
• Waxes – Beeswax, Carnauba wax
• Gums – Acacia, Tragacanth
• Resins – Asafoetida, Benzoin
• Volatile oils – Peppermint, Clove
3. Define chemical classification and write its disadvantages.
The crude drugs are arranged into different groups depending upon chemical nature of their most
important chemical constituent. The main drawback of this system is it does not give any indication about the
drug part used and their arrangement in standard books.
4. Write different groups of chemical constituents with examples.
• Alkaloids – Ephedra, Cinchona
• Glycosides – Aloe, Senna
• Tannins- Amla, Black catechu
• Resins – Asafoetida, Myrrh
• Volatile oils- Fennel, Coriander
• Lipids- Bees wax, Shark liver oil
• Carbohydrates- Acacia, Tragacanth
• Proteins – Gelatin, Papain
• Vitamins - Yeast
5. Write some examples of the drugs under pharmacological classification.
Drugs acting on GIT – Gentian, Ipecacuanha
Drugs acting on respiratory system – Liqourice , Opium
Drugs acting on Cardio vascular system – Digitalis, Ephedra
6. Define chemo taxonomical classification.
The pattern of this classification depends upon the chemical similarity of a taxon. It is based on the
occurrence of chemical constituents with their distribution in different families.
7. Define serology and serotaxonomy.
Serology is defined as the study of the antigen antibody reaction.
The serotaxonomy can be explained as the study about the application or the utility of serology in solving the
taxonomical problems.
CHAPTER – 5
QUALITY CONTROL OF DRUGS OF NATURAL ORIGIN
1. Define drug adulteration.
It is defined as admixing or substitution of original crude drug with spoiled drug, deteriorated drug,
substandard drug/inferior drug or harmful substances.
2. What are different types of drug adulteration?
Direct or intentional adulteration
Indirect or unintentional adulteration
3. Define direct and indirect adulteration.
Direct or intentional adulteration is deliberately by substituting the genuine drug partially or fully with
other inferior products.
Indirect or Unintentional adulteration mainly takes place due to faulty collection of drugs, improper
storage and imperfect preparations.
4. Define drug evaluation.
Determination of identity, purity and quality of a drug is known as drug evaluation.
5. Different methods of drug evaluation.
• Organoleptic property
• Microscopic property
• Physical property
• Chemical property
• Biological property
6. Write physical parameters for drug evaluation.
• Moisture content
• Ash values
• Viscosity
• Extractive values
• Melting point
• Volatile oil content
• Solubility
• Foreign organic matter
• Optical rotation
• Swelling factor
• Refractive index
7. Different Chromatographic techniques.
• Thin layer chromatography
• High performance thin layer chromatography
• High performance/pressure liquid chromatography
• Gas chromatography
• Column chromatography
• Gel permeation chromatography
• Affinity chromatography
8. Different Spectrophotometric methods.
• Ultra violet/visible spectroscopy
• Infrared spectroscopy
• Fluorescence analysis
• NMR – Nuclear magnetic resonance spectroscopy
• Mass spectroscopy
• X-ray diffraction
• Radio immune assay
9. Write about TLC.
Principle of TLC is adsorption chromatography. In this method the chromatographic plates are coated
with adsorbent silica gel G to a uniform thickness and dried. For the activation of plates it should be kept in
oven for 20 minutes at a temperature of 120 C. After activation of plates, the spot of concentrated extract of
crude drug is made and it is placed in chromatographic chamber which contains the mobile phase and the R f
value is calculated.
Rf = Distance travelled by solute/distance travelled by solvent front
10. Define chemical evaluation.
It is the determination of active constituents in a drug by chemical tests.
11. Test for alkaloids.
Dragendorff’s test – To 2 ml of the test solution, add 1 ml of dragendoff’s reagent (potassium bismuth
iodide solution). Formation of orange or reddish brown precipitate takes place.
Mayer’s test – To 1 ml of the test solution, add one or two drops of mayer’s reagent (potassium mecuric
iodide solution). White or a creamy precipitate is formed.
Hager’s test – To 1 ml of the test solution, add one or two drops of hager’s reagent (saturated solution
of picric acid). Formation of yellow precipitate occurs.
Wagner’s test – To 1 ml of the test solution, add two drops of wagner’s reagent (Aqueous iodine
solution). Formation of yellow or brown precipitate takes place.
12. Define biological evaluation.
The responses of tested drug on animals are compared with the standard drug. This method is employed
when the drug cannot be evaluated by chemical and physical methods.
13. Significance of biological evaluation.
• It is generally used when standardization cannot be done satisfactorily by chemical or physical
methods.
• When the quantity of the drug sample is not sufficient, then evaluation should be done by
biological methods
14. Write types of bioassay.
• Toxic
• Symptomatic
• Tissue or organ method
15. What is microbiological assay?
Microbiological assays are performed to determine the antimicrobial activity of drugs. Vitamins are
assayed by using living bacteria yeast and molds.
16. Write the following naming reactions
Goldbeater’s skin test:
Add 2% hydrochloric acid to small piece of goldbeater’s skin and rinse with distilled water. Place the
skin in test solution for five minutes and again wash with distilled water and transfer to 1% ferrous
sulphate solution. Brown or black color is developed which indicates the presence of tannins.
Liebermann Burchard’s test:
Dissolve extract (2 g) in 2 ml of acetic anhydride, heat to boil, cool and then add 1 ml conc. sulfuric
acid into the solution. A brown ring is formed at the junction and turning of the upper layer to dark
green color confirms the test for the presence of phytosterols.
Salkowski test:
Take 2 mg of dry extract and shake it with 1 ml of chloroform and add few drops of conc. Sulfuric
acid. Reddish brown color formed at the interface indicates the presence of triterpenoids.
Shinoda test:
Add few magnesium turnings and 5 drops of conc. Hydrochloric acid into 1 ml of test solution. Pink,
scarlet, crimson red or occasionally green to blue color is developed after some time.
Killer Killani test:
Add 0.4 ml of glacial acetic acid and few drops of 5% ferric chloride solution to a little quantity of
chloroform extract. Further add 0.5 ml of conc. Sulfuric acid carefully into solution. The formation of
blue color in acetic acid layer confirms the test.
Raymond’s test:
Add hot methanolic alkali solution into test solution and observe the formation of violet color which
confirms the presence of cardiac glycosides.
Legal’s test:
Treat the test solution with pyridine and add alkaline nitroprusside. Crimson red color appears.
Baljet’s test:
Formation of orange color appears upon addition of picric acid or sodium picrate into the test solution.
Molisch’s test:
To 1 ml of test solution, add few drops of 1% alpha – napthol and 2-3ml conc. Sulfuric acid. The
reddish violet or purple ring formed at the junction of two liquids confirms the test.
Barfoed’s test:
Add 2 ml of reagent into 2 ml of the test solution, mix it keep in boiling water bath for 1 min. Red
precipitate formed indicates the presence of monosaccharide.
Selivanoff’s test
Take 3 ml of selivanoff’s reagent and add 1 ml of the test sample. Heat it on the water bath for one
minute. The formation of rose red color confirms the test.
Fehling’s test:
Dissolve 2 mg dry extract in 1 ml of distilled water and add 1 ml of Fehling’s solution A and B. Shake
it and heat on water bath for 10 minutes. The brick red precipitate formation confirms the test.
Borntrager’s test:
Take test material in a test tube and boil it with 1 ml of sulfuric acid for 5 min, filter it and allow
cooling. Shake it with dichloromethane or chloroform and separate the lower layer. Shake it again with
dilute ammonia. A pink rose to red color develops.
Modified Borntrager’s test:
Take 200 mg of test material and boil it with 2 ml of dil. Sulfuric acid. Then add 2 ml of 5% aqueous
ferric chloride solution; shake it with chloroform and continue the test as above (Borntrager’s test).
Biuret test:
Take 2 ml of test solution; add 5 drops of 1% copper sulfate solution and
2 ml of 10% sodium
hydroxide solution. Mix thoroughly. Formation of purple or violet color confirms the presence of
proteins.
Millon’s test:
Add 5 drops of millon’s reagent to 1 ml of test solution and heat on a water bath for 10 minutes; cool
and add 1% sodium nitrite solution. Appearance of red color confirms the test.
Saponification test:
Add 0.5 N alcoholic potassium hydroxide in little amount of extract, add one drop of phenolphthalein
into it and heat on water bath for few hours. Formation of soap or partial neutralization confirms the
test.
Haemolysis test:
Add 0.2 ml saponin solution prepared in normal saline in 0.2 ml of blood solution prepared in normal
saline. Mix them and centrifuge the solution. Note the red supernatant obtained after centrifugation
and compare with control tube. Control tube contains 0.2 ml of blood (10%) in normal saline which is
diluted with 0.2 ml of normal saline.
Foam test:
Take 5 ml of the test solution in a test tube and shake well for five minutes. Formation of stable foam
confirms the test.
CHAPTER – 6
QUANTITATIVE MICROSCOPY OF CRUDE DRUGS
1. What is quantitative microscopy? Enlist the different types of microscopical evaluation.
Microscopy is used for quantitative evaluation of drugs and evaluation of adulterated powdered drugs.
Quantitative microscopy is done by counting specific histological features.
Lycopodium spore method, stomatal number, stomatal index, vein – islet number, veinlet termination number
and palisade ratio.
2. Importance of stage micrometers.
Stage micro is glass slide having dimensions 7.5 cm length and 2.5 cm width and has a scale in the
center of slide. It is used to study particle size diameter of starch grains, calcium oxalate crystals and fibre
length measurement in powdered drugs.
3. Importance of ocular micrometers.
It is a small disc of glass with scale of approx. 10 mm which is equally divided into many divisions.
One small division of ocular micrometer is calibrated with the help of stage micrometer whose standard value
is known. It is used to study particle size diameter of starch grains, calcium oxalate crystals and fibre length
measurement in powdered drugs.
4. Define vein islet number.
The vein-islet number defined as the number of vein-islets in area of 4 sq. mm of the central part of
leaf surface between midrib and margin.
5. Define veinlet termination number
The number of veinlet termination per sq.mm of the leaf surface midway between midrib and margin
is called as veinlet termination number.
6. What is camera Lucida and write its models.
It is an instrument used for tracing of any object in magnified image formed under the microscope.
With the help of camera Lucida, it is possible to correctly record the position, dimension of cells and other
cell structures on drawing paper.
Models off camera Lucida: Abbe model, Swift Ives model
7. Define stomatal number.
The average number of stomata present per sq.mm of the epidermis is known as stomatal number.
8. Define stomatal Index.
Stomatal index is the percentage proportion of number of stomata to the total number of epidermal
cells. Stomatal number can vary with age of the leaf, but stomatal index is relatively constant for a given
species.
I = S/E+S x 100
Where, I = stomatal index
S = stomatal number per unit area
E = Number of epidermal cells in the same area
9. Define palisade ratio.
The average number palisade cells beneath each epidermal cell.
10. What are micrometers?
Micrometers are used in the study of size of any object, particle size diameter of starch grains, calcium
oxalate crystals and fibre length measurement in powdered drugs.
UNIT-II
CHAPTER – 7
CULTIVATION AND COLLECTION OF DRUGS OF NATURAL ORIGIN
1. Vacuum drying and its significance.
This is conducted in steam heated ovens with perfect closure, and a pump is used to exhaust the air.
The low air pressure maintained within oven ensures rapid and complete drying. E.g. digitalis
Significance of Vacuum drying
• Rapid drying
• Relatively low temperature
• Cleanliness and freedom from odour and dust
• Independence of climate conditions
• Control of temperature
• Elimination of risk of fire
• Compactness
2. Methods of drying medicinal plants.
• In the open air under shade to avoid direct sunlight
• Placed in thin layers on drying frames, wire-screened rooms or buildings
• By direct sunlight, if appropriate
• In drying ovens/rooms and solar dryers
• Vacuum drying
• Spray dryers: papaya latex, pectin
• By indirect fire: baking, lyophilization, microwave or infrared devices
3. Define fertilization.
It is one of the seed propagation techniques. Fusion of male and female gametes takes place which
results in the formation of zygote.
4. Methods of vegetative propagation with examples.
• Cutting
• Layering
• Grafting
• Micro propagation
5. Methods of sexual or seed propagation.
• Microsporogenesis
• Megagametogenesis
• Pollination
• Fertilization
• Embryogen
• Microgametogenesis
6. Significance of Asexual propagation.
• Genetically similar plants are developed by this method.
• It is inexpensive, easier and fast method of multiplication.
• Micro propagation is useful in developing disease free plants, homozygous diploids.
CHAPTER -8
FACTORS INFLUENCING CULTIVATION OF MEDICINAL PLANTS
1. What is the primary factors influencing cultivation of medicinal plants?
• Environmental conditions
• Collection
• Cultivation
• Drying
• Storage and humidity
2. List out the environmental conditions which affect the quality of secondary metabolites.
• Temperature
• Aerobic oxidation
• Rainfall
• Atmospheric condition
• Length of the day
• Radiation characteristic
• Altitude
• Moisture/humidity
3. Classify soil based on particle size.
• Fine clay – less than 0.002 mm
• Silt – 0.002 to 0.02 mm
• Fine sand – 0.02 to 0.2 mm
• coarse clay – 0.2 to 2mm
4. Classify soil based on chemical nature.
• Oryphilic soil: acidic soil
• Halophilic soil: basic soil
• Psamnophilic soil: soil contains rock
• Lithophilic soil: it contains sandy soil
• Chosmophilic soil: it contains fissure
• Calcareous soil: it contains calcium
• Clay: it consists of fine particles
5. The soil factors which affect the vegetation.
• Soil reaction
• Soil nutrients
• Soil temperature
• Soil aeration
• Soil fertility
6. What are the secondary factors influencing cultivation of medicinal plants?
i) Bacteria and moulds, ii) Insects and moths iii) mites and nematode
CHAPTER- 9
PLANT HORMONES AND THEIR APPLICATIONS
1. Define plant growth regulators.
Plant hormones or plant growth regulators are used in plants to promote the morphological structure
and physiological processes. These are other than nutrients and are used in low concentration.
2. What are different plant hormones?
• Auxins
• Abscisic acid
• Gibberellins
• Ethylene
• Cytokinins
3. Examples of natural and synthetic auxins.
• Natural auxins: Indole acetic acid, Indole-3-acetonitrile, Phenyl acetic acid
• Synthetic auxins: Indole-3-butyric acid, 2-napthyl oxyacetic acid, α-napthyl acetic acid.
4. What is role of auxins?
• Internode elongation
• Leaf growth
• Initiation of vascular tissue
• Fruit setting in absence of pollination
• Fruit growth
• Inhibition of root growth
5. Mechanism of action of gibberellins.
• It mainly includes activity of gluconeogenesis enzymes during early stage of seed germination and
this specificity ensures a rapid conversion of lipid to sucrose which is used in growth and
development of embryonic axis to competent root and shoot.
• Gibberellins include the synthesis of α-amylase and other hydrolytic enzymes during germination of
seeds
6. What are Gibberellins?
• Gibberellins are the class of endogenous plant growth regulator. At present 50 gibberellins are
known in which 40 of them occur in green plant, while other from fungi.
• It is used for promoting vegetative and fruit growth, breaking dormancy, flower initiation and
induction of parthenocarpy.
7. Write about ethylene.
• It is a simple organic molecule present in the form of volatile oil and shows profound physiological
effect.
• It is commercially used for promotion of flowering and fruit ripening, induction of fruit abscission,
breaking dormancy.
8. Role of cytokinins.
• Promotion of lateral bud development and inhibition of senescence.
• Promotion of cell division
• Development of embryos during seed development
• Delaying breakdown of chlorophyll
9. Mechanism of action of abscisic acid.
In an inhibitory way ABA interacts with other plant growth substances
It inhibits the gibberellic acid induced synthesis of amylase and other hydrolytic enzymes
ABA accumulates in many seed and helps in seed dormancy
CHAPTER- 10
POLYPLOIDY, MUTATION AND HYBRIDIZATION WITH REFERENCE TO MEDICINAL
PLANTS
1. Define polyploidy.
An increase in the number of chromosomes in certain tissue or entire organism in multiplies of the
basic or haploid number is expressed as polyploidy.
2. Define mutation.
Mutation is the change in nucleotide sequence of a gene. This gives rise to a new genetic trait or
changed genotype.
3. Define hybridization.
Hybridization is a method of union or crossing of genetically two dissimilar plants. As a result,
individual produced by crossing of genetically two different parents is known as hybrid.
4. Define point mutation and write its types.
Point mutation occurs as a result of the substitution of one nucleotide for another in the specific
nucleotide sequence of a gene.
Types: Transition type and transversion type
5. Define frame shift mutation and write its types.
Frame shift mutation results from an addition or loss of one or more nucleotides in a gene and is termed
as insertion or deletion mutation respectively.
Types: Artificial mutation
Radiation mutation
Chemical mutation
6. Types of hybridization.
• Intra-varietal hybridization
• Inter-varietal or Intraspecific hybridization
• Interspecific hybridization or Intrageneric hybridization
7. Steps involved in hybridization.
a) Selection of parents
b) Selfing of parents or artificial self-pollination
c) Emasculation
d) Bagging
e) Tagging
f) Crossing
g) Harvesting and storing the F1 generation
h) Raising the F1 generation
8. Methods of emasculation.
• Hand emasculation or forceps or scissor method
• Hot water treatment
• Cold water treatment
• Alcohol treatment method
• Suction method
• Male sterility or self-incompatibility method
• Chemical gametocides
9. Significance of hybridization.
• It forms a single variety by combining two desirable characters which are not found in parent and
produces a new hybrid plant.
• Hybridization between two varieties of Withaniasomnifera Israeli chemotype II and
WithaniasomniferaSouthh African chemotype develops a new hybrid contains 3 new withanolides.
• The other example of developed hybrids by crossing over between Solanumincanumand
Solanummelongenacontains 0.5% of solasodine in first generation which increases in second
generation.
CHAPTER- 11
CONSERVATION OF MEDICINAL PLANTS
1. Name few endangered species of medicinal plants.
• Asparagus racemosus
• Celastrus paniculatus
• Drosera burmannii
2. Different strategies for conservation of medicinal plants.
• Ex-situ – protection of species outside their natural habitats
• In-situ – in their natural surroundings conservation
3. Cyrobanks for conservation of medicinal plants.
Cryopreservation of plant cells and meristems is a critical device for long term stockpiling of
germplasm or experimental material without hereditary change utilizing a minimum space and support.
UNIT-III
CHAPTER- 12
PLANT TISSUE CULTURE
1. Define explants.
Any piece of a plant taken out and developed in test tube under sterile conditions in special supplement
media is called explant.
2. Define cell totipotency.
Ability to build up an entire plant from any cell or explant is known as cell totipotency.
3. Basic requirements for plant tissue culture.
• Nutrient medium
• Aseptic condition
• Aeration of the tissue
• Plant material - explant
4. Who introduced plant tissue culture?
This method was first presented in 1902 by Sir Gottlieb Haberlandt.
5. Define cell cloning.
Cells got from a solitary cell through mitosis constitute a clone and the way towards acquiring clone
is called cloning.
6. Techniques of cell cloning.
• Bergmann’s plating technique
• Filter paper raft nurse tissue technique
7. Define hardening.
Hardening is progressive exposure of plantlets to an ecological-conditions
8. Define meristem culture.
Meristem is a limited group of cells, which are effectively divided and undifferentiated and finally
offer permanent tissue. Development of axillary or apical shoot meristems is called meristem culture.
9. Define haploid.
An individual or cell having the single set of chromosome number found in the gametes of the species
is called haploid.
10. Define micro propagation.
Micro propagation is the tissue culture method utilized for quick vegetative duplication of fancy plants
and fruit trees by utilizing little sized explants.
11. Define protoplast.
The plant cells without cell wall are known as protoplasts.
12. Define somatic hybridization.
At the point when hybrid is created by combination of physical cells of two assortments or species, it
is known as somatic crossover. The way towards delivering somatic hybrids is called somatic hybridization.
13. Define artificial seed.
An artificial seed is a globule of gel containing a somatic embryo and the supplements, growth regulators,
antibiotic required for the advancement of a total plantlet.
CHAPTER-13
EDIBLE VACCINES
1. Define vaccine.
A biological preparation which improves immunity towards a particular disease is called vaccine. The
term vaccine is derived from a latin word ‘vacca’ means usage of cowpox.
2. Define pathogen.
Pathogen is a tiny living organism, such as a bacterium or an agent which resembles with disease causing
micro organism.
3. What are the types of vaccines?
Prophylactic vaccines - which prevents the effect of future infection.
Therapeutic vaccines - against certain disease.
4. What are the methods for transformation of DNA/gene into plant?
• Plasmid vector carrier system: Agrobacterium tumefaciens method
• Micro projectile bombardment method.
5. Define transformation.
Microorganism used to transfer a small segment DNA into plant genome is called transformation.
6. What is Peyer’s patch?
Peyer’s patches are an enriched source of IgA producing plasma cells and have the potential to populate
mucosal tissue and serves as mucosal immune effector site.
7. Name some examples of edible vaccine used for various disease.
S.NO
1.
2.
3.
VACCINES
Hepatitis b
HIV
Vibrio cholerae
USED VECTOR
Tobacco, potato, lettuce
Tomato
Potato
DISEASE
Hepatitis b
AIDS
Cholera
UNIT IV
CHAPTER – 14
ROLE OF PHARMACOGNOSY IN TRADITIONAL SYSTEM OF MEDICINES
1. Ayurveda.
Ayurveda is originated from two words Ayur meaning life and veda meaning science. Ayurveda means
science of life.
2. Ashtanga ayurveda.
Kaya chikitsa – medicine
Shalya chikitsa – surgery
Shalakya chikitsa – ENT treatment
Bala chikitsa - pediatric treatment
Jara chikitsa – treatment related to genetics
Rasayana chikitsa- treatment with chemicals
Vajikarana chikitsa – treatment with rejuvenation and aphrodisiac
Graham chikitsa – planetary effects
Visha chikitsa- toxicology
3. Tridosha or five elements of ayurveda.
Vata- ether and air – controlled by central and autonomous nervous system
Pitta – fire- manifestation of energy
Kapha- water and earth – function of thermotaxis or heat regulation
4. Eight examinations in ayurveda diagnosis.
Pulse, urine, faeces, tongue, eyes, visual/sensual examination and interference.
5. Define sodhana.
All the metals and minerals used are completely in detoxified state as per the method mentioned in siddha
system.
6. Define shuddhi suthal.
In siddha system detoxification is a common phenomenon for any given drug to increase their therapeutic
potency, by minimizing the toxicity known as shuddhi suthal.
7. Classify drugs used by siddhars.
Thavaram(herbal product)
Thadu (inorganic product)
Jangamam (animal product)
8. Classify thadu drugs.
Uppu (thavanam)
Pashanam
Uparasam
Ratnas and uparatnas
Loham
Rasam
Gandhakam
9. Homeopathy
German physician Dr. Christian Frederic Samuel Hahnemann introduced fundamental principle of
homeopathy “Simillia Similibus Curentur” means ‘let likes be cured by likes’.
10. Fundamental principles of Homeopathy.
• Law of Similia
• Law of simplex
• Law of minimum
• Drug proving
• Drug potentization
• Vital force
• Acute and chronc disease
• Individualization
• Direction of cure
11. Unani system.
Unani medicine owes its origin to Greece. Greek Philosopher Physician Hippocrates freed medicine from
the realm of superstition and magic and gives it the status of science.
12. Chinese system of medicine.
Chinese system of medicine came into existence from the Shang dynasty 14th to 11th Centuries BC based
on Yinyangism with yin –yang theory.
CHAPTER – 15
INTRODUCTION TO SECONDARY METABOLITES
1. Define secondary metabolism.
Secondary metabolites do not involve in growth pattern and development of any plant. e.g. alkaloids,
terpenoids, peptides, growth hormones etc.
2. Define Alkaloids.
Alkaloids mean alkali like. It a group of naturally occurring chemical compounds, that contains one or
more basic nitrogen atoms in heterocyclic ring.
3. Define glycosides.
Glycosides are the naturally occurring organic compounds found in plants and some animals, which upon
hydrolysis give one or more sugar moiety (glycone) and non sugar moiety (aglycone).
4. Classify glycosides on the basis of linkage.
• O-Glycosides
• S-Glycosides
• N-Glycosides
• C-Glycosides
5. Define Tannins.
Tannins are complex natural organic compounds which are polyphenolic, polyhydroxy benzoic acid
derivatives or flavanol derivatives having astringent action.
6. Classify Tannins.
Tannins are classified into
• True Tannins:
• Hydrolysable Tannins and Non hydrolysable tannins.
• Pseudo Tannins
7. Classify Resins based on their constituents.
Acid Resins e.g. Colophony
Ester resins e.g. Benzoin
Resin alcohols e.g. Peru balsam.
8. Define terpenoids or volatile oils.
Terpenoids are the hydrocarbons of plant origin having general formula (C5H8)n. They are volatile
substance which gives fragrance or aroma to plants.
UNIT V
CHAPTER – 16
STUDY OF DRUGS OF NATURAL ORIGIN
1. Classify fibres.
Vegetable fibres e.g. Cotton, jute
Animal fibres e.g. Silk, wool
Mineral fibres e.g. Asbestos, glass wool
Synthetic fibres e.g. Terylene, nylon
Regenerated fibres
From carbohydrates e.g. Rayon
From proteins e.g. Fibrolin
2. Biological source and family of hemp.
Hemp fibres can be produced from the plant Cannabis sativa
Family: Cannabinaceae.
3. Chemical constituent and uses of cotton.
Chemical constituents: Cellulose, fat, protoplasm wax and ash.
Uses: surgical dressing, filter medium, insulation medium and adsorbent cotton.
4. Uses of Honey.
Demulsent, sweetening agent, antiseptic, and used in ayurvedic formulations.
5. Adulterant and substituent’s of Tragacanth.
Caramania gum, hog gum, vermicelli tragacanth, Indian tragacanth and katira gum.
6. Chemical constituents and uses of acacia.
Chemical constituents:Arabic acid combined with potassium, magnesium and calcium, enzymes diastase
and oxidase.
Uses:Demulsifying agent, suspending agent, emulsifying agent and as a binder for compressed tablets
7. Biological source and family of agar.
It is dried gelatinous substance obtained from Gelidium amansii
Family: Rhodophyceae
8. Chemical constituents and uses of castor oil.
Chemical constituents: Fixed oil consists of glycoside of resinolic, iso-resinolic, stearic and dihydro stearic
acid
Use: Cathartic, emoluments, abortificient and used in the preparation of contraceptives, creams and jellies.
9. Bioloigical source and family of wool fat.
Wool fat is anhydrous lanolin obtained from wool of sheep of Ovis aries
Family: Bovidae
10. Bioloigical source, family and adulterants of bees wax.
Yellow bees wax is purified wax obtained from the honey comb of the bees Apis mellifera. Family: Apidae.
Adulterants: Japan waxes
11. Chemical constituent and uses of hydnocarpus oil.
Hydnocarpus acid, chaulmoogric acid, gorlic acid, cyclopentyl fatty acids.
Uses: Treatment of tuberculosis, leprosy, psoriasis, and rheumatism.
CHAPTER- 17
PROTEINS AND ENZYMES
1. Define enzymes.
Enzymes are organic catalysts found in living organisms, performs many complex chemical reaction
which make life process.
2. Classify enzymes.
Amylolytic enzymes – have tendency to digest carbohydrates. E.g. Diastase, Hyaluronidase etc.
Proteolytic enzymes – have role in digestion of proteins. E.g. pepsin, trypsin etc.
3. Uses of Urokinase.
Treatment of pulmonary embolism, coronary artery thrombosis and in restroring the potency of
intravenous catheters.
4. Streptokinase and its uses.
Streptokinase is purified bacterial protein obtained from culture filtrates of group c Streptococci griseus.
Uses: as a agent for dissolving blot clots
Treatment of pulmonary embolism, coronary artery thrombosis, arteriovenous cannula occlusion and
deep vein thrombosis.
5. Chemical constituents and uses of papain.
Chemical constituents: Papain contains proteolytic enzymes peptidase I, clotting enzyme pectase.
Uses: treatment of dyspepsia, intestinal and gastric disorders and diphtheria.
Internally as protein digestant
6. Biological source and uses of casein.
It is a proteolytic enzyme extracted from the milk proteins in the form of voluminous globules.
Uses: as a binder, adhesive, protectant, fabrics, food additives.
CHAPTER – 18
HALLUCINOGENS, TERATOGENS, NATURAL ALLERGENS
1. Define hallucinogens with examples.
Hallucinogens are the psychoactive substances which modify the thought, mood and perception.
Natural hallucinogens: Datura – Datura stramonium
Belladona - Atropa belladonna
Betel nut – Areca catechu
Synthetic hallucinogens: PCP – Phencyclidine
LSD- Lysergic acid diethyl amide
MDMA – methylene dioxy meth amphetamine
2. Define teratogens with examples.
Teratogens are various agents which affect the development of foetus.
Synthetic teratogens: Thalidomide, lysergic acid, diethylamide, metronidazole, phenytoin
Natural teratogens: Artemisinin, ginseng
3. What are the factors responsible for teratogenecity.
Radiation, maternal conditions like obesity, diabetes, hypo/hyperthyroidism, toxic metals, infectious
agents like mumps virus, influenza etc.
4. Define natural allergens.
Allergens are from chemical, biological or synthetic origin and made up of glycoproteins which are
responsible to produce the allergy.
5. Types of allergens.
Inhalants - airborne matter like dust, pollens etc.
Ingestants – food materials e.g. egg, peanut, milk, cashew
Injectants- sting of bees e.g. honey bees
Contactants- constituents present in plants e.g. phenolic constituents, sesquiterpenoids
Infectants – metabolic waste product of microorganism e.g. protozoa moulds, bacteria etc.
CHAPTER – 19
NOVEL MEDICINAL AGENTS FROM MARINE SOURCES
1. Name some antiviral compounds.
S.NO MARINE PRODUCT
OBTAINED FROM
BIOLOGICAL SOURCE
1.
ARA A
SPONGE
Tethyacrypta
2.
DIDEMNINS
TUNICATES
TRIDIDEMNUM SPESIES
3.
EUDISTOMINS
TUNICATES
EUDISTOMA OLIVACEUM
2. Name some cardio vascular agents.
S.NO MARINE PRODUCT
1.
ANTHOPLEURINS
2.
EPTATRETIN
3.
SAXITOXIN
OBTAINED FROM
COELENTRATES
PACIFIC HOG FISH
BUTTER CLAM
3. List of anti coagulants with their occurrence.
S.NO MARINE PRODUCT
OBTAINED FROM
1.
Carragenean
Red green algae
2.
Fucoidan
Brown algae
3.
Proteoglycans
Green algae
BIOLOGICAL SOURCE
Anthro elegantissima
Eptatretus stoutii
Saxidomus giganteus
BIOLOGICAL SOURCE
Chondru scrispus
Fucus vesiculosus
Codium fragile ssp.