King Saud University
College of Pharmacy
PHL 313
Outline (1)
Dr. Nouf AL-Rasheed
Reference course textbook: Pharmacology (Rang and dale, 6th ed.).
This lecture focus on explanation of some common pharmacological terms and
pharmacokinetic of drugs in particular (refer to Chapter 7 of the textbook, pp. 98111).
Lecture outlines:
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Definition of some pharmacological terms such as pharmacology, drug,
pharmacokinetic and pharmacodynamics.
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The four main ways by which drugs cross cell membrane. See Fig7.1, pp.99.
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Factors influence the diffusion through lipids: these include pH and
ionsisation, pH partition (see summary box, pp.102; also refer to Fig7.3,
pp.101).
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Other factors have a major influence on drug distribution and elimination.
These include binding to plasma proteins (summary box, pp. 103) and
partition into body fat and other tissues
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Drug disposition
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Drug absorption and this include the main routes of drug administration (Fig
7.6). In addition, for each route of drug administration, the advantages and
disadvantages will be highlighted.
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Distribution of drugs (discussed briefly).
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Blood-brain barrier.
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Concept of pro-drug.
King Saud University
College of Pharmacy
PHL 313
Outline (2)
Dr. Nouf AL-Rasheed
This lecture will focus on drug elimination and pharmacokinetics (refer to
Range and Dale, 6th ed, Chapter 8, pp. 113-119
The main outlines for this lecture are:
Drug metabolism
In drug metabolism the following issues will be discussed:
The phases of drug metabolism
A. Phase I: This includes the different kind of reactions
The P450 monooxygenase system (nature, classification and mechanisms)
Enzyme inducers.
Enzyme inhibitors.
Other phase I reactions.
B. Phase II reactions.
C. First-pass (presystemic) metabolism: this will include Table 8.2 (pp. 117) and
summary box (pp. 117).
Pharmacologically active drug metabolites (also see Table 8.3, pp. 118).
Drug elimination
In drug elimination the following issues will be discussed
A. Renal excretion of drugs and drug metabolites particularly:
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Glomerular filtration.
Active tubular secretion.
Passive diffusion across tubular epithelium.
In addition to summary box (pp. 119).
B. Biliary excretion and enterohepatic circulation.
King Saud University
College of Pharmacy
PHL 313
Outline (3)
Dr. Nouf AL-Rasheed
This lecture will focus on how drugs act: General priniciples (Drugreceptor interaction and pharmacodynamics (refer to Rang and Dale, 6th
ed., Chapter 2, PP. 9-20)
The main outlines for this lecture
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Protein targets for drug binding.
(Refer also to summary box, PP. 9).
Drug-receptor interactions (Fig 2.1, pp.10), the following terms will
be discussed:
 Agonist.
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Antagonist.
Affinity.
Efficacy (intrinsic activity).
Specificity.
Full agonists.
Partial agonists.
Spare receptors.
Agonist concentration-effect curves (Emax and EC50 or ED50, pp. 11-12)
(Refer to summary boxes, pp.16 and 17).
Drug antagonism
(Chemical antagonism, pharmacokinetic antagonism, antagonism by receptor block
(competitive antagonism either reversible or irreversible), non-competitive
antagonism and physiological antagonism.
Refer also to summary box, pp. 19.
Desensitisation and tachyphylaxis (tolerance, refractoriness and drug resistance).
Therapeutic index (Attached sheet from Lippincott textbook will be given).
King Saud University
College of Pharmacy
PHL 313
Outline (4)
Dr. Nouf AL-Rasheed
This lecture will focus on how drugs act: molecular aspects (refer to Rang
and Dale, 6th ed., Chapter 3; pp.24-28 and pp.48-50; Chapter 4: pp.5556 and pp.61-63).
The main outlines for this lecture
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Target for drug action (pp.24).
Ion channels (pp.25, 48-50).
Enzymes (pp.25-26).
Carrier molecules (pp.27).
Refer to Table 3.1. (some examples of targets for drug action) (pp.2527).
Gating (pp.49-50) and this include:
 Voltage-gated channels this will include sodium
channels (pp.61), potassium channels (pp.61-63),
Calcium channels (pp. 55-57).
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Ligand-gated channels (pp.49).
Calcium release channels (pp.49, 57-58).
Store-operated calcium channels (pp.50).
Types of receptors (pp.27-34)
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Ligand-gated ion channels
G-protein-coupled receptors (GPCRs)
Kinase-linked receptor
Nuclear receptors
Refer to Fig. 3.2 (pp. 28) and Table 3.2 (pp.30) and Fig 3.3 (pp.29) and summary
box (pp.33)
King Saud University
College of Pharmacy
PHL 313
Outline (5)
Dr. Nouf AL-Rasheed
This lecture will focus on how drugs act: molecular aspects (refer to Rang
and Dale, 6th ed., Chapter 3; pp.33-47)
The main outlines for this lecture:
Type 2: G-protein-coupled receptors.
G-protein-coupled receptor families.
Table 3.3 (pp. 34)
G-proteins and their role (pp. 34-39) (also see a copy sheet from Brody’s human
pharmacology, 4th ed. pp.15, Box 2-2 will be given to students for an additional
reading)
Refer to Fig 3.8 (Rang and Dale, pp.35)
Refer to the summary Box (pp.37).
Refer to Table 3.4 (pp. 36)
Targets for G-proteins
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Adenylate cyclase/cAMP system (pp. 37) and Fig 3.10
The Phospholipase C/inositol phosphate system (pp.38-39) and see Fig
3.12
In addition this section include:
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Inositol phosphates and intracellular calcium (pp.38-39).
Diacylglycerol and protein kinase C (pp. 39).
Ion channels as targets for G-proteins (pp.39)
See Fig 3.14 (pp.42) which illustrates GPCRs desensitisation and summary box
(pp.43).
For additional reading:
 Integrated Pharmacology by Page et al, 2nd ed., Chapter 3; pp.29-34 (a
hard copy will be given to students).
 http://en.wikipedia.org/wiki/G_protein.
King Saud University
College of pharmacy
PHL 313
Outline (6)
Dr.Nouf AL-Rasheed
This lecture will focus on chemical mediators and the autonomic nervous
system (refer to Rang and Dale, 6th ed., Chapter 9; pp.131-143)
The main outline for this lecture:
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The peripheral nervous system (pp.132)
Basic anatomy and physiology of the autonomic nervous system (132136) and Fig 9.1 and Fig 9.2
Refer to two Summary Boxes (pp125)
Transmitters in the autonomic nervous system (pp.136)
Table 9.1 The main effects of the autonomic nervous system (pp.134135)
Table 6-2 and Table 9-1 autonomic receptor types with documented
or probable effects on peripheral autonomic effector tissues (from
Basic and clinical pharmacology textbook by Katzung, 9th ed., a copy
of the table will be given to students)
King Saud University
College of Pharmacy
PHL 313
Outline (7)
Dr. Nouf AL-Rasheed
This lecture will focus on chemical mediators and autonomic nervous
system (refer to Rang and Dale, 6th ed., Chapter 9; pp.139-141)
The main outline for this lecture
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Transmitters other than acetylcholine and noradrenaline (pp.139) and
refer to Table 9.2 (pp.140).
Refer to summary boxes (pp. 141).
Autonomic regulation of peripheral organs (attached sheet from
Brody’s human pharmacology, 4th ed., pp91-92 will be given to the
students).
Neurotransmission and neurotransmitters in the autonomic nervous
system (attached sheet from Brody’s human pharmacology, 4th ed.,
pp89-99 will be given to the students). In addition, refer to Fig 8-3,
pp92; Fig 8-4,pp. 94; Fig. 8-9,pp. 98. In addition, refer to Table 8-2,
pp. 99.
Classification of cholinergic receptors (refer to Rang and Dale,
Chapter 10, pp. 145-146 read only the classification of cholinergic
receptors into muscarinic receptor and nicotinic receptor subtypes).
Classification of adrenoceptors ( and  adrenoceptors) (refer either to
principles of neuropharmacology textbook, pp. 110-111, a copy of it
will be given to students or to Rang and Dale textbook, Chapter 11,
pp.168-170 and also in this chapter see a summary box (pp.171).
Refer to Table 11.1, pp.169 (Rang & Dale).
NB: The first midterm exam is not indicated yet and the exam will cover all aspects
that have been discussed until the end of this lecture.
N.B: The exam will cover all pervious topics discussed in the lectures until the end
of this lecture.
All best wishes in the exam
King Saud University
College of Pharmacy
PHL 313
Outline (8)
Dr. Nouf AL-Rasheed
This lecture will focus on noradrenergic transmission (refer to Rang and
Dale, 6th ed., Chapter 11; pp.168-175)
The main outline for this lecture
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Classification of adrenoceptors (pp.168-170)
Refer to summary box (pp.171) and Table 11.1 (pp.170)
Noradrenaline synthesis (pp.171-172)
Noradrenaline storage and release (pp.172)
Regulation of noradrenaline release (pp.172-173) and see Fig 11.3
(pp.174) and refer to Summary Box (pp.174)
Uptake and degradation of catecholamines (pp. 173-175) and also read
this in principles of neuropharmacology textbook (pp.108-110) also see
F.g 8.2 in this reference. NB: a copy of this indicated pages in this
textbook will be given to students
King Saud University
College of Pharmacy
PHL 313
Outline (9)
Dr. Nouf AL-Rasheed
This lecture will focus on noradrenergic transmission (refer to Rang and
Dale, 6th ed., Chapter 11; pp.176-178)
The main outline for this lecture
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Classification of sympathomimetic amines (adrenoceptors agonists) (a
sheet of this classification will be given to students) and refer to Table
11.3; pp.186
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Pharmacological actions of adrenoceptors agonists (pp.176-177)
This include their effects on the following aspects:
1. Smooth muscle.
2. Heart.
3. metabolism.
4. Other effects.
Refer to Table 11.1 (pp.170) and summary box (pp.177).
King Saud University
College of Pharmacy
PHL 313
Outline (10)
Dr. Nouf AL-Rasheed
This lecture will focus on noradrenergic transmission (refer to Rang and
Dale, 6th ed., Chapter 11; pp.177 and principles of pharmacology
textbook as acopy of it will be given to students, pp.111-117)
The main outline for this lecture
Clinical uses of adtrenoceptors (refer to a summary box in Rang and Dale textbook,
pp. 177)
In addition, the clinical uses and the unwanted effects of individual adrenoceptor
agonists will be highlighted in the lecture (for details refer to a given sheet from
principles of pharmacology textbook. Moreover, refer to a summary table 11.3
(pp.186; Rang and Dale) of the most characteristic clinical indications and adverse
effects of sympathomimetic amines such as
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Noradrenaline
Adrenaline
Dobutamine
Isoprenaline (isoproterenol)
Salbutamol
Terbutaline
Formoterol
Clonidine
Apraclonidine
Guanfacine
Guanabenz
Oxymetazoline, methoxamine and phenylephrine
Ritodrine
Dopamine
In addition, Read the attached sheets from the pharmacological basis of
therapeutics (pp. 220-235).
King Saud University
College of Pharmacy
PHL 313
Outline (11)
Dr. Nouf AL-Rasheed
This lecture will focus on noradrenergic transmission (refer to Rang and
Dale, 5th ed., Chapter 11; pp.183-188 and principles of pharmacology
textbook as acopy of it will be given to students, pp.111-117)
The main outline for this lecture
This lecture will focus on indirect acting sympathomimetic amines (amphetamine,
tyramine, and ephedrine) particularly:
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The mode of action of indirect acting sympathomimetic amines
Refer to Fig 11.8 (pp.184; Rang and Dale)
Drugs affecting indirect acting symapthomimetic amines and this will
involve the effect of reserpine, imipramine/desipramine (TCA, uptake
1 inhibitors), and Monamine oxidase inhibitors on indirect acting
sympathomimetics (pp.183-188; Rang and Dale)
Amphetamine and the following aspects will be discussed (Refer to a
given sheet of principle pharmacology textbook):
- M.O.A
- Pharmacological actions
-Clinical uses
-Adverse effects
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Clinical indications of methylphenidate (Refer to a given sheet of
principle pharmacology textbook):
Clinical indications of ephedrine, pseudoephedrine and
phenylpropranolamine (Refer to a given sheet of principle
pharmacology textbook):
Inhibitors of noradrenaline uptake (Rang and Dale, pp. 184)
Refer to Table 11.3 (Rang and Dale, pp.186) which summarized the
main action, clinical uses, and the unwanted effects of indirect acting
sympathomimetic amines
In addition refer to the attached sheets from The Pharmacological Basis of
Therapeutics (By Goodman and Gilman), pp. 235-241.
King Saud University
College of pharmacy
PHL 313
Outline 12
Dr. Nouf AL-Rasheed
This lecture will focus on noradrenergic transmission (refer to Rang and
Dale, 5th ed., Chapter 11; pp.177-183 and principles of pharmacology
textbook as acopy of it will be given to students, pp.111-117)
The main outline for this lecture
This lecture will focus on the adrenoceptor antagonists and the following aspects
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Classification of sympatholytics
Non-selective -adrenoceptor antagonists (phenoxybenzamine and
phentolamine)
Mixed - and -arenoceptor antagonists (Labetalol and carvedilol)
Selective 1-antagonists
Tamsulosin)
(Prazosin,
terazosin,
doxazosin
and
Selective 2-antagonist (Yohimbine)
General clinical uses and unwanted effects of -adrenoceptor
antagonists
-adrenoceptor antagonists ((non-selective such as propranolol,
nadolol and timolol) while 1-selective antagonists include atenolol,
metoprolol and esmolol))
Pharmacological action of -adrenoceptor antagonists
Clinical uses of -adrenoceptor antagonists
Adverse effects of -adrenoceptor antagonists
Drugs that affect noradrenaline synthesis (methyldopa)
Noradrenergic neuron-blocking drugs (Guanethidine)
Drug affecting noradrenaline storage (reserpine)
Summary boxes, pp., 179, 182.
Fig 11.9, pp., 185.
In addition refer to Therapeutic Basis of Pharmacology by Goodman and
Gilman, pp. 241-261 (a hard copy of it was given to the students).