MINISTRY OF PUBLIC HEALTH OF UKRAINE
MINISTRY OF EDUCATION, SCIENCE, YOUTH AND
SPORTS OF UKRAINE
SUMY STATE UNIVERSITY
3078 METHODOLOGICAL INSTRUCTIONS
for practical training
on the topic “DRUGS AFFECTING
PERIPHERAL AND CENTRAL NERVOUS
SYSTEM”
in Pharmacology course
for foreign students
of speciality 7.110101 «Medical science»
full-time training
Sumy
Sumy State University
2011
3
Methodological instructions for practical training on the topic
“Drugs affecting peripheral and central nervous system” /
compiler A.A. Kachanova. – Sumy : Sumy State University,
2011. – 46 p.
4
Biological chemistry and pharmacology
departmentThematic Module “Drugs Affecting
Peripheral Nervous System”
Drugs Affecting the Afferent Innervation
Topical questions
1. The classification of drugs affecting the afferent innervation.
2. The classification of local anesthetics according to chemical
structure.
3. The types of local anesthesia. Primary use of local anesthetics for
this or that type of local anesthesia.
4. The mechanism of action of local anesthetics.
5. Expediency of combination of local anesthetics with adrenoceptor
agonists.
6. The comparison characteristics of local anesthetics: duration of
anesthesia, clinical use, influence on the central nervous system
and internals, biotransformation in organism, and side effects.
7. Astringent drugs: classification, mechanism of action, local effects,
and clinical use.
8. The characteristic of covering drugs and adsorbents: mechanism of
action, local effects, and clinical use.
9. Irritant drugs: mechanism of action, effects, and clinical use.
Tasks for prescription
Prescribe the following drugs and list the indications for their use:
1. Novocaine (procaine) in ampoules for different types of anesthesia.
2. Anesthesin (benzocaine) in suppositories, powders for internal use,
in ointment.
3. Lidocaine in ampoules for different types of anesthesia.
4. Trimecaine in ampoules for different types of anesthesia.
5. Tannin in ointment and in solution for the gastric lavage at a
poisoning.
6. Bismuth subnitrate in tablets, ointment and powders for external
use.
7. Activated charcoal (Carbo activatus) in tablets and non-dosage
powders for internal use.
5
8. Menthol in alcoholic solution and in ointment.
Table 1 – Drugs for prescription
Drug name
Anaesthesinum
Novocainum
Trimecainum
Lidocainum
6
Single dose and mode of
administration
Orally 0.3 g
through rectum 0.05–0.1 g;
on the skin 5–10% ointment
Drug product
Powder;
tablets 0.3 g;
suppositories 0.05 and
0.1 g;
5% ointment
For infiltration anesthesia
Ampoules 0.25% and
0.25-0.5% solution;
0.5% solution – 1, 2,
for conduction anesthesia 1– 5, 10 and 20 ml; 1%
2% solution;
and 2% solution – 1,
for permeation anesthesia
2, 5, and 10 ml;
10–20% solution and 5–10% bottle 200 or 400 ml
ointment;
of 0.25% or 0.5%
through rectum –
solution;
suppository containing 0.1 g suppositories 0.1 g;
5% and 10%
ointments
For infiltration anesthesia –
Ampoules 10 ml of
0.125%, 0.25% or 0.5%
0.25% solution; 2, 5,
solution;
or 10 ml 0.5% or 1%
for conduction anesthesia –
solution; 1, 2, 5, or
1–2% solution;
10 ml 2% solution;
for permeation anesthesia –
1 or 2 ml 5% solution
2–5% solution;
for epidural anesthesia –
1–2% solution;
for spinal anesthesia – 5%
solution
For infiltration anesthesia –
Ampoules 10 or 20 ml
0.25% or 0.5% solution;
of 1% solution; 2 or
for conduction anesthesia –
10 ml of 2% solution;
0.5–2% solution;
2 ml of 10% solution
for permeation anesthesia –
1–5% solution
Table 1 continuation
Tanninum
For oral, nasal, a pharyngeal
rinsing, and throat gargling
– 1–2% water or glyceric
solutions;
for application on injured
surfaces – 3–10% solution
or ointment;
for gastric lavage – 0.5%
solution
Bismuthi subnitras Orally – 0.25–0.5 g;
on the skin – 5–10%
ointment and aspersion
Carbo activatus
Orally – 1–2 g for
meteorism;
20–30 g (in the form of
suspension in water) for
poisonings
Mentholum
For applying on the skin –
0.5–2% alcoholic solution,
1% ointment;
sublingually – 2–3 drops of
5% alcoholic solution (on a
slice of sugar)
There are no made
forms at the plant.
Pharmacist prepares
these forms (the
prescriptions can be
written in short or full
forms)
Powder;
tablets 0.25 or 0.5 g;
10% ointment
Powder;
tablets 0.25 or 0.5 g
1%, 2% or 5%
alcoholic solution;
1% ointment
Cholinomimetics. Cholinesterase Inhibitors
Topical questions
1. The types of efferent nerves. The peculiarities of structure and
physiology of vegetative nervous system.
2. The structure and work of cholinergic synapse. Different types of
cholinoceptors and their localization.
3. The classification of cholinergic drugs depending on their
influence upon different types of cholinoceptors.
4. Direct M-, N-cholinomimetics: mechanism of action,
pharmacological effects, peculiarities of pharmacokinetics, clinical
applications, adverse effects.
7
5. Cholinesterase inhibitors: drugs classification, mechanism of
action, pharmacological effects, peculiarities of pharmacokinetics, clinical
applications, adverse effects. The symptoms and treatment of poisoning
with cholinesterase inhibitors. Mechanism of action of cholinesterase
regenerators; peculiarities of their use.
6. M-cholinomimetics: mechanism of action, pharmacological
effects, peculiarities of pharmacokinetics, clinical applications, and adverse
effects. The comparison characteristics of pilocarpine and aceclidine.
7. N-cholinomimetics: mechanism of action, pharmacological effects,
peculiarities of pharmacokinetics, clinical applications. The toxicology of
nicotine. The treatment of nicotine abuse.
Situational tasks in pharmacodynamics and pharmacokinetics
1. An eye was denervated. Describe the carbacholine effects on this
eye.
2. An eye was denervated. Describe the proserin effects on this eye.
3. M-cholinoceptor antagonist was administered to animal. Describe
the change in its blood pressure owing to the following acetylcholine
administration.
4. M- cholinoceptor antagonist was administered to animal. Describe
the change in its blood pressure owing to the following proserin
administration.
5. The doctor has 3 preparations. All of them are miotic, reduce
intraocular pressure, cause bradycardia, and increase glands secretion and
tone of smooth muscles.
Two preparetions also have an ability to ease the neuromuscular
transmission and transmission through autonomic ganglia. But one of them
acts in full loss of function, while another – only in decreased function.
What groups do these drugs belong to?
6. Patient with poisoning was hospitalized with the following
symptoms: profuse sweating, myosis, nausea, vomiting, diarrhea, and
bradycardia. Blood pressure is low. What is the cause of poisoning?
Institute treatment for this patient.
7. The side effects in digestive system and in bronchi develop in
patient suffering from myasthenia that is treated with proserin. What are
these side effects? What drug should be administered for prevention of
these side effects?
8. A patient suffers from glaucoma. What drugs may be used for
reduction of intraocular pressure? Explain the mechanism of drugs action.
8
9. A patient suffers from myasthenia. Choose drugs for treatment of
patient. Explain the mechanism of drugs action.
Tasks for prescription
Prescribe the following drugs and list indications for their
use:
1.
2.
3.
4.
5.
6.
7.
8.
Proserin in tablets, eye drops, and ampoules.
Galantamine in ampoules.
Pilocarpine in eye drops and eye ointment.
Aceclidine in ampoules, eye drops, and eye ointment.
Carbacholine in eye drops.
Dipiroxim in ampoules.
Lobeline in ampoules.
Cytitonum in ampoules.
Fill in the following tables
Table 2 – Localization of cholinergic synapses and cholinoceptors
Synapses localization
Receptors localization
M-cholinoceptor N-choliniceptor
Synapses of sympathetic and
parasympathetic ganglia
Synapses of sympathetic fibers
in adrenal medulla
Carotid bodies
Synapses of postganglionic
parasympathetic
fibers
in
innervated organs
Synapses of postganglionic
sympathetic fibers in genital
glands and vessels of skeletal
muscles
Synapses of motor nerves in
skeletal muscles
Synapses of central nervous
system
9
Table 3 – Organs reaction upon the excitation of vegetative nerves
Organ, tissue, function
Change of function owing to
excitation of
sympathetic nerve parasympathetic
nerve
Heart:
- heart rate;
- force of cardiac contraction;
- automatism;
- conductibility
Vessels
Smooth muscles:
- bronchi;
- gastrointestinal tract;
- urinary tract;
- biliary tract;
- uterus;
- sphincters of GIT
Excretory glands activity
Eye muscles:
- muscle – sphincter of pupil;
- radial muscle;
- ciliary muscle
Table 4 – Comparison characteristics of M-cholinomimetics
Effect
Reduction of intraoccular pressure
Increase of tone and peristalsis of intestine
Increase of tone and contractibility of uterus
Increase of secretion of excretory glands
Bradycardia
Indications for use
“+” – weak effect;
“++” – moderate effect;
“+++” – marked effect
10
Pilocarpine
Aceclidine
Table 5 – Comparison characteristics of cholinesterase inhibitors
Physostigmine
Proserin
Galantamine
Armin
Mode of
administration
Duration of action
Indications for use
Symptoms
of
poisoning
Antidotes
Table 6 – Drugs for prescription
Drug name
Proserinum
Single dose and mode of
administration
Orally 0.01–0.015 g;
subcutaneously 0.0005 g;
in eyes 1–2 drops
Galanthamini
Subcutaneously 0.0025–0.005 g
hydrobromidum
Pilocarpini
In eyes: 1–2% solution (1–2
hydrochloridum drops) or eye ointment
Aceclidinum
In eyes: 2-5% solution (1–2
drops) or 3–5% eye ointment;
subcutaneously 0.002 g
Carbacholinum In eyes 1–2 drops of 0.5–1%
solution
Dipiroximum
Subcutaneously, intramuscularly
or intravenously 0.15–0.3 g
Intravenously slowly 0.005 g
Lobelini
hydrochloridum
Cytitonum
Intravenously slowly 0.5 ml
Drug product
Tablets 0.015 g;
ampoules 1 ml of
0.05% solution;
eye drops: 0.5%
solution
Ampoules 1 ml of
0.1%, 0.25%, 0.5% or
1% solution
Eye drops: 1% or 2%
solution in bottles 5 or
10 ml;
1% or 2% eye ointment
2-5% solution of eye
drops;
3% and 5% eye
ointment;
ampoules 1 or 2 ml of
0.2% solution
Eye drops: 0.5% or
1% solution in bottles
5 or 10 ml
Ampoules 1 ml of
15% solution
Ampoules 1 ml of 1%
solution
Ampoules 1 ml
11
M-Cholinoceptor Antagonists
Topical questions
1. Types and localization of M-cholinoceptors. The effects of excitation
of different M-cholinoceptors types.
2. Classification of М-cholinoceptor antagonists.
3. The mechanism of action of М-cholinoceptor antagonists.
4. Influence of М-cholinoceptor antagonists upon the eye.
5. Influence of М-cholinoceptor antagonists upon cardiovascular
system.
6. Influence of М-cholinoceptor antagonists upon the smooth muscular
organs (the gastrointestinal tract, bronchi, and urinary ways).
7. Influence of М-cholinoceptor antagonists upon the functions of
excretory glands.
8. Central effects of М-cholinoceptor antagonists (influence upon
CNS).
9. The comparison characteristics of М-cholinoceptor antagonists
(peculiarities of atropine, scopolamine, platyphyllin, methacin).
10. Indication for application of М-cholinoceptor antagonists.
11. Adverse effects of М-cholinoceptor antagonists and
contraindications to their use.
12. The symptoms and treatment of poisoning with М-cholinoceptor
antagonists.
Situational tasks in pharmacodynamics and pharmacokinetics
1. An eye was denervated. Describe the effects of pilocarpine and
atropine on this eye.
2. A child with poisoning was hospitalized with the following
symptoms: tachycardia, marked mydriasis, dry mouth, agitation, and
hallucinations. What substance is the cause of poisoning? Institute
treatment for this child.
3. A patient suffers from spastic pain owing to urolithiasis. What drugs
may be used for pain relief of spasm? Explain mechanism of drugs action.
4. A patient suffers from atrioventricular blockade. What drugs may be
used for improving of conductivity?
5. A patient with ulcer disease suffers from hypersecretion and pain
owing to pylorus spasm. Propose drugs for treatment of this patient.
Explain the mechanism of drugs action.
12
Fill in the following table
Table 7 – Comparison characteristics of М-cholinoceptor antagonists
effects
Effects
Drug
Atropine Scopolamine Platyphyllin
Methacin
Relaxation of bronchi
Decrease of bronchial
and digestive glands
secretion
Reduction of spasm of
intestine, biliary and
urinary tracts
Degree of
М-cholinoceptor
antagonists action
Direct myotropic
antispasmodic action
Tachycardia
Reduction of vestibular
disturbances
Antiparkinsonian action
Mydriasis
Duration of paralysis of
accommodation
Indications for use
“+” – weak action;
“++” – moderate action;
“+++” – marked action.
Tasks for prescription
Prescribe the following drugs and list indications for their use:
1. Atropine in tablets, ampoules, eye ointment, and eye drops.
2. Dry extract of belladonna.
3. Scopolamine in powders, ampoules, and eye drops.
4. Platyphyllin in ampoules and tablets.
5. Methacin in tablets and ampoules.
6. “Aeron” in tablets.
13
Table 8 – Drugs for prescription
Drug name
Atropini sulfas
Extractum
Belladonnae
siccum
Scopolamini
hydrobromidum
Platyphyllini
hydrotartras
Methacinum
Tablets
“Aeronum”
14
Single dose and mode of
administration
Orally 0.00025–0.0005 g 1-3
times daily;
subcutaneously or
intramuscularly 0.00025–
0.0005 g 1-2 times daily;
intravenously 0.00025–
0.0005 g;
in eyes: 1% ointment or 1–2
drops of 0.5–1% solution
(once daily)
Orally 0.02–0.04 g 2-3 times
daily;
Through rectum 0.02–0.04 g
1–2 times daily
Orally or subcutaneously
0.00025g;
in eyes: 1–2 drops of 0.25%
solution 1–2 times daily
Orally 0.003–0.005 g 2–3
times daily;
subcutaneously 0.002–0.004 g
1-2 times daily;
in eyes: 1–2 drops of 1–2%
solution
Orally 0.002–0.004 g 2–3
times daily;
subcutaneously,
intramuscularly or
intravenously 0.0005–0.001
g 1–2 times daily
Orally 1–2 tablets before or
during travel (for treatment
or prevention of motion
sickness)
Drug product
Tablets 0.0005 g;
ampoules 1 ml of 0.1%
solution;
eye drops: 0.5% or 1%
solution;
1% eye ointment
Powders for internal
use;
suppositories 0.02 or
0.04 g
Powders for internal
use;
ampoules 1 ml of
0.05% solution
Tablets 0.005 g;
ampoules 1 ml of 0.2%
solution;
eye drops 1% or 2%
solution
Tablets 0.002 g;
ampoules 1 ml of 0.1%
solution
Tablets (10 tablets in
package)
N-Cholinoceptor Antagonists: Ganglionic Blocking Drugs
and Skeletal Muscle Relaxants
Topical questions
1. Types and localization of N-cholinoceptors.
2. Classification of ganglionic blocking drugs.
3. The mechanism of action of ganglionic blocking drugs.
4. Pharmacological effects of ganglionic blockers:
- influence on the cardiovascular system;
- influence on the smooth muscular organs (digestive tract, bronchi, and
urinary ways);
- influence on the eye functions;
- central effects of ganglionic blocking drugs (influence on CNS).
5. Indications for application of ganglionic blocking drugs.
6. Adverse effects of ganglionic blockers and contraindications to their
use.
7. The classification of skeletal muscle relaxants.
8. Characteristics of nondepolarizing muscle relaxants: mechanism of
action, clinical use, and adverse effects.
9. Characteristics of depolarizing drugs: peculiarities of mechanism of
action, clinical use, and adverse effects.
Situational tasks in pharmacodynamics and pharmacokinetics
1. Benzohexonium was administered to animal. Describe the effects of
the following aceclidine administration to this animal.
2. Benzohexonium was administered to animal. Describe the influence
of cytitonum on blood pressure and respiration.
3. Benzohexonium was administered to animal. Describe the influence
of atropine on bronchi and intestine.
4. A doctor administered proserin to patient with overdose of
dithylinum. Were his actions correct? Why?
5. A doctor administered proserin to patient with overdose of
tubocurarin chloride. Were his actions correct? Why?
15
Fill in the following tables
Table 9 – Comparison characteristics of ganglionic blockers
Hygronium
Benzohexonium
Pachycarpine
Mode of drug
administration
Duration of
action
Penetration
power through
blood-brain
barrier
Indications for
use
Side effects
Table 10 – Comparison characteristics of peripheral myorelaxants
Dithylinum
Tubocurarin chloride
Peculiarities of
chemical
structure
Mechanism of
action
Interaction with
cholinesterase
inhibitors
Duration of
action
Mode of
administration
Indications for
use
Side effects
Tasks for prescription
Prescribe the following drugs and list indications for their use:
1. Benzohexonium in tablets and ampoules.
2. Pirilenum in tablets.
3. Pentaminum in ampoules.
16
4. Hygronium in ampoules and bottles.
5. Tubocurarine in ampoules.
6. Dithylinum in ampoules.
Table 11 – Drugs for prescription
Drug name
Benzohexoniu
m
Pirilenum
Pentaminum
Hygronium
Tubocurarini
chloridum
Dithylinum
Single dose and mode of
administration
Orally 0.1–0.2 g 3–6 times
daily;
subcutaneously or
intramuscularly 0.025 g 1–2
times daily
Orally 0.0025–0.005 g 2–5
times daily
Intramuscularly 0.05–0.1 g 2–3
times daily;
intravenously slowly 0.01–0.025
g (before administration, single
dose should be mixed with 20
ml of sterile isotonic sodium
chloride solution or glucose
solution)
Intravenous drop by drop 0.04–
0.08 g (as 0.1% solution)
Drug product
Tablets 0.1 g;
ampoules 1 ml of
2.5% solution
Tablets 0.005 g
Ampoules 1 or 2 ml of
5% solution
Ampoules or bottles
0.1 g of dry medicinal
remedy
Intravenously 0.0004–0.0005 g/kg Ampoules 1 ml of
1.5% solution
Intravenously 0.0015–0.002 g/kg Ampoules 5 or 10 ml
of 2% solution
17
Adrenomimetic and Sympathomimetic Drugs
Topical questions
1. The structure and functions of adrenergic synapse.
2. The types of adrenoceptors. The basic localization and
physiological meaning of different types of adrenoceptors.
3. Classification of drugs stimulating adrenergic receptors.
4. Pharmacological characteristics of adrenaline:
- mechanism of action;
- influence on cardiovascular system;
- influence on eye;
- influence on smooth-muscular organs (gastrointestinal tract,
bronchi, uterus);
- influence on metabolic processes;
- influence on CNS;
- peculiarities of pharmacokinetics;
- indication for application;
- adverse effects and contraindications.
5. Pharmacological characteristic of noradrenaline.
6. Classification of α-adrenomimetics according to influencing on
different subtypes of α-adrenoceptors. Pharmacological effects and clinical
use of α-adrenomimetics.
7. Classification of β-adrenomimetics according to influencing upon
different subtypes of β-adrenoceptors. Pharmacological effects, clinical use,
and adverse effects of β-adrenomimetics.
8. The characteristics of sympathomimetic drugs. Features of the
mechanism of ephedrine action. Force and duration of ephedrine effects in
comparison with adrenaline. Tachyphylaxis concept. The indications and
contraindications to use.
Situational tasks in pharmacodynamics and pharmacokinetics
1. What groups and certain drugs are used for prevention of bronchial
asthma attacks? Explain your answer.
2. What groups and certain drugs are effective in atrio-ventricular
blockage? Explain your choice.
3. A patient suffers from glaucoma. The use of cholinomimetics is
contraindicated owing to concomitant ulcer disease of stomach. What drugs
may be used for treatment of glaucoma in this patient? Explain the
mechanism of drugs action.
18
4. A patient with frequent bronchial asthma attacks used inhalations
of adrenomimetic agent for its reduction. In several days, patient began to
complain of tachycardia, chest pain, tremor, and headache. Which drug
does cause such complications? Explain the mechanism of complications
development.
5. Acute vascular insufficiency was developed in a patient. For
improvement of this state, doctor has the following drugs: cytitonum,
adrenaline, and noradrenaline. Which drug should be administered? Why?
Which mode of drug administration should be chosen?
Tasks for prescription
Prescribe the following drugs:
1. Adrenaline in ampoules and eye drops.
2. Noradrenaline in ampoules.
3. Ephedrine hydrochloride in ampoules and tablets.
4. Mesatonum (phenylephrine) in ampoules and tablets.
5. Naphthizin in drops for nose.
6. Isadrinum in tablets and solution for inhalations.
7. Salbutamol in tablets and aerosol.
Fill in the following tables
Table 12 – Effects of excitation of alpha- and beta-adrenergic receptors
Tissue, organ
Excitation
Alpha-adrenoceptor Beta-adrenoceptor
Heart
Bronchial smooth muscles
Smooth muscles of vessels
Smooth
muscles
of
intestine
Uterus
Radial muscle of iris
Bladder
Salivary glands
Liver
Adipocytes
Platelets
19
Table 13 – Comparison characteristics of adrenomimetics
Drug
Alpha-adrenomimetic
action
Beta-adrenomimetic
action
Noradrenaline
Adrenaline
Mesatonum
Isadrinum
Ephedrine
Table 14 – Comparison characteristics of pharmacological effects of
adrenomimetics
Effect
Cardiac
pacing
Influence
on blood
pressure
Broncholytic action
Influence
on
carbohydrate
metabolism
Excitation
of CNS
20
Adrenaline
Noradrenaline
Mesatonum
Isadrinum
Ephedrine
Table 15 – Drugs for prescription
Drug name
Adrenalini
hydrochloridum
Noradrenalini
hydrotartras
Ephedrini
hydrochloridum
Mesatonum
Naphthyzinum
Isadrinum
Salbutamol
Single dose and mode of
administration
Subcutaneously or
intramuscularly 0.0003–
0.00075 g;
in eyes: 1-2 drops of 1–2%
solution
Intravenously drop by drop
0.004–0.008 g in 1 L of 5%
glucose solution
Orally, subcutaneously,
intramuscularly or
intravenously 0.025 g 2–3
times a day
Orally 0.01–0.025 g 2–3
times daily;
subcutaneously or
intramuscularly 0.003–0.005 g
1-2 times daily;
intravenously 0.001–0.003 g
with 40 ml of sterile isotonic
NaCl solution;
in eyes: 1–2 drops of 1–2%
solution
In nose 1–2 drops of 0.05–
0.1% solution 3 times daily
Sublingually 0.005 g;
inhalationly: 1–2 inhalations
of 0.5-1% solution
Orally 0.002 g 3 times daily;
inhalationly: 1–2 inhalations
3 times daily
Drug product
Ampoules 1 ml of 0.1%
solution;
eye drops: 1% or 2%
solution
Ampoules 1 ml of 0.2%
solution
Tablets 0.025 g;
ampoules 1 ml of 5%
solution
Powders for internal
use;
ampoules 1 ml of 1%
solution;
eye drops 1% or 2%
solution
Bottles 10 ml of 0.05%
or 0.1% solution
Tablets 0.005 g;
bottles 25 ml or 100 ml
of 0.5% or 1% solution
Tablets 0.002 g;
aerosol 10 ml
21
Adrenoceptor Antagonists
Topical questions
1. The structure and function of adrenergic synapse.
2. The types of adrenoceptors. The basic localization and
physiological meaning of different types of adrenoceptors.
3. Classification of adrenoceptor blocking drugs.
4. Pharmacological characteristics of -adrenoceptor blocking drugs:
classification according to influence on different kinds of -adrenoceptors,
mechanism of action, phenomenon of “epinephrine reversal”, influence on
cardiovascular system, indications for application, adverse effects.
5. Pharmacological characteristics of -receptor antagonists:
classification according to influence on different kinds of -adrenoceptors,
mechanism of action, influence on cardiovascular system, metabolic
processes, and eye, indications for application, adverse effects. The concept
of intrinsic sympathomimetic activity and membrane-stabilizing action of
-adrenergic antagonists.
6. -, -adrenergic antagonists: representatives, mechanism of action,
pharmacological effects, clinical use, and adverse effects.
7. Sympatholytics:
representatives, mechanism of action,
pharmacological effects, indications for use, and adverse effects.
Situational tasks in pharmacodynamics and pharmacokinetics
1. Hypertensive crisis was developed in patient. Which drugs can be
used for quick blood pressure reduction?
2. A patient suffers from obliterative endarteritis. Which drugs
should be prescribed to him for reduction of vascular spasm? Explain your
answer.
3. Administration of which groups of drugs may trigger asthma
attacks?
4. An elderly patient suffers from ischemic heart disease with marked
atherosclerosis of coronary vessels. Which drugs should be prescribed to
him for prevention of heart strokes? Substantiate your answer and explain
mechanism of drugs action.
22
Fill in the following tables
Table 16 – Comparison characteristics of adrenoceptor antagonists and
sympatholytics
Drug name
Main effects
Indication for
use
Side effects
Phentolamine
Tropaphenum
Propranolol
Octadinum
Reserpine
Tasks for prescription
Prescribe the following drugs:
1. Phentolamine in tablets.
2. Tropaphenum in ampoules.
3. Prazosin in tablets.
4. Propranolol in tablets and ampoules.
5. Metoprolol in tablets and in ampoules.
6. Talinolol in dragee.
7. Octadinum in tablets.
8. Reserpine in tablets.
Table 17 – Drugs for prescription
Drug name
Phentolamini
hydrochloridum
Tropaphenum
Prazosinum
Single dose and mode of
administration
Orally 0.05 g 3–5 times daily
Subcutaneously or
intramuscularly 0.01–0.02 g
1–3 times daily;
intravenously 0.01 g
Orally 0.0005–0.002 g 3–4
times daily
Drug product
Tablets 0.025 g
Ampoules 0.02 g of dry
medicinal remedy
(before administration,
substance of 1 ampoule
should be dissolved in
1–2 ml of sterile water)
Tablets 0.001, 0.002 or
0.005 g
23
Table 17 continuation
Anaprilinum
Orally 0.01–0.04 g 3–4 times
daily;
intravenously slowly 0.001 g
Metoprololum
Orally 0.05–0.1 g 2–4 times
daily;
intravenously slowly 0.005–
0.015 g
Talinololum
Orally 0.05–0.1 g 3 times
daily
Octadinum
Orally 0.025–0.05 g once
daily
Reserpinum
Orally 0.00005–0.0001 g 1-3
times daily
Tablets 0.01 or 0.04 g;
ampoules 1 or 5 ml of
0.1% solution
Tablets 0.05 or 0.1 g
ampoules 5 ml of 1%
solution
Dragee 0.05 g
Tablets 0.025 g
Tablets 0.0001 or
0.00025 g
General Anesthetics
Topical questions
1. What is “general anesthesia”? The characteristics of general
anesthesia stages.
2. The different types of general anesthesia: initial anesthesia, basis
anesthesia, combined anesthesia.
3. The classification of general anesthetics.
4. Peculiarities of mechanisms of action of different drugs from
general anesthetics group.
5. The characteristics of some drugs for inhalational anesthesia: ether,
halothane, nitrous oxide.
6. The characteristic of some drugs for intravenous anesthesia:
propanidid, ketamine, predionum, thiopental sodium, hexenalum, sodium
oxybutiras.
Situational tasks in pharmacodynamics and pharmacokinetics
1. During the introduction of a patient to general anesthesia with ether,
the bradycardia up to cardiac arrest was observed. What is the cause of
cardiac arrest in the first stage of ether action? What drugs are used for
prevention of this complication?
24
2. During surgical operation, the symptoms of asphyxia were
developed in patient. Explain the cause of this complication and propose
drugs for its prevention.
3. A patient with traumatic brain edema and hypoxic convulsions was
admitted to a hospital. What general anesthetic may be used for relief of
convulsions? Explain your answer.
4. Bradycardia and reduction of blood pressure was developed in
patient during halothane anesthesia. Anesthesiologist administered to him
noradrenaline. Did the doctor make the right choice?
Suggest pressor drugs for restoration of blood pressure and explain
your choice.
5. A patient with amputation of leg needs dressing. What general
anesthetics may be used for analgesia in this case? Explain your answer.
Fill in the following tables
Table 18 – Comparison characteristics of inhalational anesthetics
Characteristics
Diethyl
ether
Halothane
Nitrous oxide
Degree of anesthetic
action
Speed of introduction in
anesthesia
Severity of anesthesia
stages
Severity of excitement
stage
Irritating action
Relaxation of skeletal
muscles
Influence on
cardiovascular system
Hepatotoxicity
and
nephrotoxicity
Indications for use
25
Table 19 – Comparison characteristics of intravenous anesthetics
Characteristics
Propanidid
Ketamine
Thiopental
sodium
Speed
of
anesthesia
development
Duration
of
anesthesia
Influence upon
respiration
Influence
on
cardiovascular
system
Tolerance
of
brain
to
hypoxia
Indications for
use
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
26
Propanidid in ampoules.
Thiopental sodium in bottles.
Hexenalum in bottles.
Sodium oxybutiras in ampoules.
Ketamine in ampoules.
Sodium
oxybutiras
Table 20 – Drugs for prescription
Drug name
Propanididum
Single dose and mode of
administration
Intravenously 0.005–0.01 g/kg
Thiopentalumnatrium
Intravenously 0.4–0.5 g
Hexenalum
Intravenously 0.5–0.7 g
Natrii
oxybutyras
Intravenously 0.07–0.12 g/kg
Orally 0.1–0.2 g/kg (for
general anesthesia);
2-3 table spoons before sleep
(for treatment of insomnia)
Ketaminum
Intramuscularly 0.006 g/kg;
intravenously 0.002 g/kg
Drug product
Ampoules 10 ml of 5%
solution
Bottles 0.5 g or 1.0 g of
dry substance (should
be dissolved before
administration in 50 ml
of sterile 0.9% solution
of sodium chloride)
Bottles 1.0 g of dry
substance (should be
dissolved before
administration in 50 ml
of sterile 0.9% solution
of sodium chloride)
Ampoules 10 ml of
20% solution
Bottles 400 ml of 5%
syrup
Bottles 10 ml of 5%
solution;
or 20 ml of 1% solution
27
Hypnotic Drugs. Ethyl Alcohol
Topical questions
1. The physiology of sleep: characteristics of recovering and sleeping
system; REM and nonREM sleep.
2. Types of sleep disorders.
3. Classification of hypnotic drugs.
4. Characteristic of hypnotic drugs from group of benzodiazepine:
mechanism of action, influence on the CNS, peculiarities of drugs
pharmacokinetics, indications for use, adverse effects, and possible
complications.
5. Zolpidem and zopiclone: mechanism of action and advantages of
their use for treatment of insomnia.
6. Characteristic of hypnotic drugs – derivatives of barbituric acid:
mechanism of action, influence on the CNS, peculiarities of drugs
pharmacokinetics, indications for use, adverse effects, and possible
complications. The signs of acute barbiturates poisoning and treatment of
this condition.
7. Pharmacological and toxicological characteristic of ethyl alcohol.
The use of ethyl alcohol in medical practice. The signs of acute and chronic
ethyl alcohol poisoning (alcoholism). The treatment of this condition.
Mechanism of action of teturamum (desulfiram).
Situational tasks in pharmacodynamics and pharmacokinetics
1. A patient with insomnia suddenly stops the use of phenobarbital after
regular drug intake during 1.5 months. The following symptoms develop
after drug withdrawal: anxiety, irritability, fear, vomiting, visual
disturbances, convulsions, orthostatic hypotension, and cardioinhibitory
reflex.
Explain the cause of symptoms observed in patient. Suggest the drugs
for treatment of this pathological state.
2. Patient took phenobarbital on the background of evident alcohol
intoxication. Death occurred at night during sleep. Explain why
combination of ethyl alcohol and phenobarbital resulted in death.
28
Fill in the following table
Table 21 – Comparison characteristics of hypnotic drugs
Characteristics
Phenobarbital
Nitrasepam
Sodium
oxybutiras
Speed of sleep
development
Duration of sleep
Mechanism of action
Influence on sleep
structure
Indications for use
Side effects and
complications
Tasks for prescription
Prescribe the following drugs:
1. Nitrazepamum in tablets.
2. Phenobarbital in tablets.
3. Aethaminalum-natrium in tablets.
4. Zolpidem in tablets.
5. Natrii oxybutiras in syrup for internal use.
6. Teturamum in tablets.
Table 22 – Drugs for prescription
Drug name
Nitrazepamum
Phenobarbital
Aethaminalumnatrium
Zolpidem
Natrii oxybutiras
Teturamum
Single doses and mode of
Drug product
administration
Orally 0.005–0.01 g before
Tablets 0.005 or 0.01 g
sleep)
Orally 0.1 g before sleep
Tablets 0.05 or 0.1 g
Orally 0.1–0.2 g before sleep Tablets 0.1 g
Orally 0.01 g before slee
Orally 2–3 table spoons
before sleep
Orally 0.5 g once a day
Tablets 0.01 g
Bottles 400 ml of 5%
syrup
Tablets 0.25 g
29
Antiepileptic and Antiparkinsonian Drugs
Topical questions
1. Classification of antiepileptic drugs according to their mechanisms
of action and their clinical use for treatment of different types of epilepsy.
2. Drugs which block the sodium channel: mechanism of action;
characteristics of some drugs (clinical use in epilepsy and adverse effects).
3. Drugs which activate GABA-system in brain (the derivatives of
benzodiazepine, phenobarbital): mechanism of action, clinical use for
treatment of different types of epilepsy, adverse effects.
4. Agents that block calcium channels (mechanism of action, clinical
use and adverse effects of ethosuximide).
5. Drugs which are used for discontinuance of epileptic status.
6. The causes of Parkinson’s disease (pathological changes in
mediators balance).
7. Classification of antiparkinsonian drugs according to their
mechanism of action.
8. Levodopa: mechanism of action, clinical use and adverse effects.
Expediency of combination the levodopa with inhibitors peripheral DOPA
decarboxylase (carbidopa and benseraside).
9. Agonists of dopamine receptors.
10. Drugs that inhibit MAO-B.
11. Drugs from group of central cholinergic antagonists.
12. Midantanum.
Situational tasks in pharmacodynamics and pharmacokinetics
1. Tonoclonic spasms periodically develop in patient after cranial
trauma. What drugs should be prescribed to him for prevention of spasms?
2. Generalized convulsions developed in patient owing to unknown
substance intoxication. Prescribe the drugs for its cessation. Explain the
choice of mode of drugs administration and mechanism of drugs action.
3. Periodical short loss of consciousness is observed in patient after
encephalitis. Simultaneously, contractions of muscles of the right half of
face and neck are observed. Prescribe the drugs for its cessation. Explain
the choice of mode of drugs administration and mechanism of drugs action.
4. The increased striated muscles tone, rigidity, and tremor are
developed in patient due to long-term treatment with haloperidol. Explain
30
the mechanism of development of these complications and suggest drugs
for their reduction.
Fill in the following tables
Table 23 – Comparison characteristics of antiepileptic drugs
Drug
Group
name
Antiepileptic activity
Mechanism
of action
Side
effects
Phenobarbital
Dipheninum
Carbamazepine
Ethosuximide
Lamotrigine
Sodium
valproate
Clonazepam
Table 24 – Comparison characteristics of antiparkinsonian drugs
Cyclodolum
Mechanism
action
Side effects
Midantanum
Levodopa
of
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
5.
6.
7.
8.
Dipheninum in tablets.
Carbamazepinum in tablets.
Phenobarbital in tablets and powders for internal use.
Ethosuximidum in capsules.
Levodopa in tablets and capsules.
Midantanum in coated tablets.
“Nacom”.
Cyclodolum in tablets.
31
Table 25 – Drugs for prescription
Drug name
Single dose and mode of
administration
Dipheninum
Orally 0.117 g 3 times a
day
Carbamazepinum Orally 0.2–0.4 g 2 or 3
times a day
Phenobarbitalum Orally 0.05 g 2 times a
day
Ethosuximidum
Orally 0.25 g 3 times a
day
Clonazepamum
Orally 0.001–0.002 g
3–4 times a day
Levodopa
Orally 0.25–1.0 g 3 times
a day
Midantanum
Orally 0.1–0.2 g 2–4
times a day
“Nacom”
1 tablets 1–4 times a day
Cyclodolum
Orally 0.001–0.005 g 2-3
times a day
Drug product
Tablets 0.117 g
Tablets 0.1, 0.2 or 0.4 g
Tablets 0.05 or 0.1 g
Capsules 0.25 g
Tablets 0.001 g
Tablets 0.25 or 0.5 g;
capsules 0.25 or 0.5 g
Coated tablets 0.1 g
Tablets
Tablets 0.001, 0.002 or
0.005 g
Opioid Analgesics
Topical questions
1. The physiological mechanism of pain perception: nociceptive and
antinociceptive systems. The concept about opioid receptors and their
endogenous ligands.
2. The classification of drugs that influence opioid receptors (agonists,
partial agonists, and antagonists).
3. The mechanism of analgesic action of opioid analgesics.
4. The characteristics of other effects of opioid analgesics (byway of
example of morphine): influence on the CNS and peripheral organs and
systems.
5. The comparion characteristics of other drugs from group of opioid
analgesics. Peculiarities of promedolum, omnopon, fentanyl, pentazocine.
6. The indications for use of opioid analgesics.
32
7. The adverse effects of opioid analgesics. Contraindications to their
use.
8. The signs of acute opioid analgesics poisoning. The treatment of
this poisoning. Use of antagonists of opioid receptors.
9. Phenomena that can develop as a result of long-time use of opioid
analgesics. The causes of opioid analgesics dependence. The treatment of
dependence.
Situational tasks in pharmacodynamics and pharmacokinetics
1. A woman with pathological pregnancy needs analgesia of delivery.
What opioid analgesic may be used? Why?
2. A patient with acute morphine poisoning is admitted to a hospital.
Suggest treatment for this patient. Explain your choice of drugs.
3. A patient with acute pain owing to biliary colics is admitted to a
hospital. What opioid analgesic may be used for pain relief in this patient?
Explain your answer.
4. A doctor prescribed Talamonal to patient with acute myocardial
infarction. What is Talamonal? Were his actions correct?
Fill in the following tables
Table 26 – Influence of morphine upon the systems and organs
System, organ
Central nervous system
Nociceptive system
Cough center
Respiratory center
Vomiting center
Vasomotor center
Oculomotor center
Vagal center
Center of thermoregulation
Peripheral tissues and organs
Cardiac rhythm
Blood pressure
Tone of urinary and biliary tracts
Intestinal tone
Diuresis
Morphine
33
Analgesic activity
Duration of action
Drug dependence
Inhibition of respiratory center
Spasm of smooth muscles
Indications for use
Notation: “+++”– pronounced effect;
“++” – moderate effect;
“+” – weak effect;
“-“ – depressing effect.
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
5.
6.
7.
34
Morphine in ampoules.
Omnopon in ampoules.
Promedolum in ampoules and tablets.
Phentanyl in ampoules.
Pentazocine in tablets.
Pentazocine in ampoules and rectal suppositories.
Naloxone hydrochloridum in ampoules.
Codeine
Pentazocine
Fentanyl
Promedolum
Omnopon
Morphine
Table 27 – Comparison characteristics of opioid analgesics
Table 28 – Drugs for prescription
Drug name
Morphini
hydrochloridum
Omnoponum
Promedolum
Phentanylum
Pentazocini lactas
Pentazocini
hydrochloridum
Naloxoni
hydrochloridum
Single doses and mode of
administration
Orally 0.01 g;
subcutaneously 0.01 g
Drug product
Powders;
ampoules 1 ml of 1%
solution
Orally 0.01–0.02 g;
Powders;
subcutaneously 0.01–0.02 g ampoules 1 ml of 1%
or 2% solution
Orally 0.025 g
Tablets 0.025 g
subcutaneously 0.01–0.02 g ampoules 1 ml of 1%
or 2% solution
Intramuscularly or
ampoules 2 ml or 5 ml
intravenously 0.00005–
of 0.005% solution
0.0001 g
Subcutaneously or
Ampoules 1 ml of 3%
intramuscularly 0.03 g
solution;
through rectum 0.05 g
suppositories 0.05g
Orally 0.05 g
Tablets 0.05 g
Subcutaneously,
intramuscularly or
intravenously 0.0004–
0.0008 g
Ampoules 1 ml or 2 ml
of 0.04% solution
Nonopioid Analgesics
Topical questions
1. The classification of nonopioid analgesics.
2. The mechanism of action of nonopioid analgesics. The concepts of
COX-1 and COX-2.
3. The main effects of nonopioid analgesics: analgesic, antiinflammatory, and antipyretic.
35
4. The characteristics of the salicylic acid derivatives: therapeutic
effects, influence on internal organs and systems, indications for use,
adverse effects, and signs of overdose.
5. The characteristics of pyrazolone derivatives drugs effects,
indications for use, and adverse effects.
6. The characteristics of p-aminophenol derivatives. Advantage and
disadvantage of paracetamolum.
7. The comparison characteristics of derivatives of anthranilic,
indoleacetic, phenylacetic, phenilpropionic, and naphtylpropionic acid. The
peculiarities of ketorolac.
8. The COX-2 inhibitors.
Situational tasks in pharmacodynamics and pharmacokinetics
1. A patient suffers from pain owing to inflammation of knee-joint.
What drugs may be prescribed to him? Why?
2. A student complains of a headache during classes. What drugs can
you suggest him? Why?
Fill in the following tables
Traumatic pain
Neuralgia, myositis
Spastic pain
Headache
Myocardial infarction
Analgesia of delivery
Rheumatoid arthritis
36
Butadione
Analgin
Aspirin
Pentazocine
Fentanyl
Promedol
Indication for use
Morphine
Table 29 – Clinical use of analgesics
Table 30 – Comparison characteristics of non-opioid analgesics
Drug
Chemical
structure
Indications for
use
Side effects
Acetylsalicylic
acid
Analgin
Butadione
Indometacin
Ortophen
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
5.
Acetylsalicylic acid in tablets.
Analgin in tablets and ampoules.
Butadione in tablets and ointment.
Diclofenac-sodium in tablets and ampoules.
Paracetamol in tablets.
Table 31 – Drugs for prescription
Drug name
Single dose and mode of
administration
Acidum
Orally 0.25–1.0 g 3-4
acetylsalicylicum times a day
Tablets 0.1, 0.25 or
0.5 g
Analginum
Tablets 0.5 g;
Butadionum
Diclofenacnatrium
Orally 0.25–0.5 g 2-3
times a day;
intramuscularly or
intravenously 0.25–0.5 g
2–3 times a day
Orally 0.1–0.15 g 2–4
times a day;
for external application as
5% ointment
Orally 0.025–0.05 g 1-3
times a day;
intramuscularly 0.075 g
once a day
Drug product
ampoules 1 or 2 ml of
25% or 50% solution
Tablets 0.15 g
5% ointment
Coated tablets 0.025 g
Ampoules 3 ml of 2.5%
solution
37
Table 31 continuation
Paracetamolum
Orally 0.2–0.4 g 2–3
times a day
Tablets 0.2 g
Neuroleptic and Antidepressant Drugs
Topical questions
1. The classification of neuroleptics.
2. The mechanism of action of neuroleptics (influence on different
types of CNS receptors).
3. The main effects of neuroleptics: antipsychotic and sedative; their
clinical displays.
4. The characteristic of other effects of neuroleptics: hypnotic,
myorelaxation, hypothermic, antiemetic, hypotensive, and antispasmodic.
5. The peculiarities of different antipsychotic drugs – phenothiazine
derivatives: aminazinum, triftazinum, phthorphenasinum. The typical
adverse effects of phenothiazine derivatives.
6. The characteristics of derivatives of butyrophenone, thioxanthene.
7. The characteristics of “atypical” neuroleptics: sulpiride and
clozapine. Advantage of “atypical” neuroleptics.
8. The indications for use of neuroleptics.
9. Antidepressant drugs. Drugs which inhibit the neuronal reuptake of
monoamines: classification, mechanisms of action of different subgroups,
clinical use, adverse effects.
10. MAO inhibitors: classification, mechanism of action, clinical use,
and adverse effects.
Situational tasks in pharmacodynamics and pharmacokinetics
1. A patient suffers from psychosis with psychomotor excitement.
Which neuroleptics should be prescribed to him? Why?
2. A pregnant woman suffers from gestosis with frequent vomiting.
Which neuroleptics may be used for interruption of vomiting? Explain
mechanism of drug action.
3. Together with other drugs, aminazine was prescribed to patient with
ulcer disease of stomach. Which pharmacological effects of aminazine are
useful in this case?
38
Fill in the following tables
Table 32 – Comparison characteristics of neuroleptics
Effect
aminazine
Degree of effect
chlorprothixene
haloperidol
Antipsychotic
Decrease of motor
activity
Sedative
Hypnotic
Analgesics
and
general anesthetics
potentiation
Antiemetic
Hypotensive
Extrapyramidal
disorder
Tasks for prescription
Prescribe the following drugs and list indications for their use:
1.
2.
3.
4.
5.
6.
7.
8.
Aminazinum in dragee and ampoules.
Triftazinum in tablets and ampoules.
Haloperidolum in tablets and ampoules.
Droperidolum in ampoules.
Imizinum in tablets and ampoules.
Amitriptylinum in tablets and ampoules.
Fluoxetine in tablets.
Lithii carbonas in tablets.
39
Table 33 – Drugs for prescription
Drug name
Single dose and mode of
Drug product
administration
Aminazinum
Orally 0.025–0.05 g 1–3
Dragee 0.025, 0.05 or
times a day;
0.1 g;
intramuscularly 0.1 g 1–3
ampoules 1, 2, 5 or 10 ml
times a day;
of 2.5% solution
intravenously 1–2 ml of 2.5%
solution with 20 ml of 40%
glucose solution (in case of
acute psychomotor agitation)
Triftazinum
Orally 0.005–0.01 g once a
Tablets 0.001, 0.005 or
day;
0.01 g;
intramuscularly 0.001–0.002 g 1 ampoules 1 ml of 0.2%
once a day
solution
Haloperidolum Orally 0.0015–0.005 g 3 times Tablets 0.0015 or 0.005
a day;
g;
intramuscularly 0.002–0.005 g ampoules 1 ml of 0.5%
solution
Droperidolum
Intramuscularly or
Ampoules 5 or 10 ml of
intravenously 0.0025–0.005 g 0.25% solution
Imizinum
Orally 0.025-0.05 g 1–3 times Tablets 0.025 g;
a day;
intramuscularly 0.025 g 1–3
ampoules 2 ml of 1.25%
times a day
solution
Amitriptylinum Orally 0.025–0.05 g 3–4 times Tablets 0.025 g;
a day
intramuscularly or
ampoules 2 ml of 1%
intravenously 0.025–0.04 g 3– solution
4 times a day
Fluoxetinum
Orally 0.02 g 1–2 times daily Capsules 0.01 and 0.02 g
40
Tranquilizers. Lithium Salts. Sedative Drugs
Topical questions
1. The classification of tranquilizers.
2. The mechanism of action of tranquilizers – derivatives of
benzodiazepine.
3. The main effects of benzodiazepine derivatives: tranquilizing,
sedative, hypnotic, myorelaxation, and anticonvulsive.
4. The indications for use of benzodiazepine derivatives.
5. The side effects of benzodiazepine derivative. The sings of
overdosage and treatment of this condition.
6. The characteristics of “daily” anxiolytics: buspirone, propranolol,
nootropil. Clinical use of these drugs.
7. Lithium salts:
representatives,
mechanism of
action,
pharmacological effects, clinical use, and adverse effects.
8. The characteristics of sedative drugs: mechanism of action, effects,
clinical use. The cause, sings, and treatment of bromism.
Situational tasks in pharmacodynamics and pharmacokinetics
1. A patient complains of anxiety, fear, and internal tension. What
drugs should be prescribed to him? Explain the mechanism of drugs action.
2. An airport manager, came to consult a doctor with complaints of
anxiety, internal tension, and fear. Doctor prescribed diazepam 3 times a
day. Did doctor prescribe drug correctly? Give necessary explanations.
Fill in the following tables
Table 34 – Comparison characteristics of tranquilizers
Effect
Degree of effect
chlozepidum diazepam
buspirone
Anxiolytic
Sedative
Hypnotic
Analgesics
potentiation
Muscular
relaxation
Anticonvulsive
Amnestic
amizylum
41
Table 35 – Comparison characteristics of psychotropic drugs, which inhibit
central nervous system
Effect
Antipsychotic
Sedative
Inhibition of
vegetative reflexes
Analgesics and
general anesthetics
potentiation
Relaxation of skeletal
muscles
Anticonvulsive
Antiemetic
Hypotonic
Iatrogenic
parkinsonism
Neuroleptics Tranquilizers
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
5.
6.
7.
42
Diazepam in tablets and ampoules.
Phenazepam in tablets.
Nitrazepam in tablets.
Lithium carbonate in tablets.
Sodium bromide in tablets.
Tincture Valeriana.
Tincture Leonurus.
Sedative drugs
Table 36 – Drugs for prescription
Drug name
Diazepamum
Phenazepamum
Nitrazepamum
Gidazepamum
Lithii carbonas
Natrii bromidum
Tinctura Valerianae
Tinctura Leonuri
Single doses and mode of
administration
Orally 0.005–0.015 g 3
times a day;
intramuscularly or
intravenously 0.01–0.02 g
1-3 times a day
Orally 0.00025–0.001 g
1–2 times a day
Orally 0.005–0.01 g 1–2
times a day
Orally 0.02–0.05 g 3 times
daily
Orally 0.3–0.6 g
Orally 0.5–1.0 g 3–4 times
a day
Orally 20–30 drops 3–4
times a day
Orally 30–50 drops
Drug product
Tablets 0.005 g;
ampoules 2 ml of
0.5% solution
Tablets; 0.0005 or
0.001 g
Tablets 0.005 or 0.01 g
Tablets 0.02 or 0.05 g
Tablets 0.3 g
Tablets 0.5 g
Tincture 30 ml
Tincture 25 ml
Psychostimulants. Nootropic Drugs. Analeptics. Adaptogens
Topical questions
1. The classification of psychostimulants.
2. The mechanism of action of psychostimulants – derivatives of
phenylalkylamine, piperidine, and sidnonimine. Their pharmacological
effects.
3. The mechanism of action of caffeine. Influence of caffeine upon
different organs and systems.
4. The indications for use of psychostimulants. Side effects and
contraindications for their use.
5. Nootropic drugs: mechanism of action, effects, indications for use.
6. The classification of analeptics. Mechanisms of action and
pharmacological effects. Clinical use of analeptics.
7. Adaptogens: mechanism of action, effects, and indication for their
use.
43
Tasks for prescription
Prescribe the following drugs:
1.
2.
3.
4.
5.
6.
7.
8.
Sydnocarbum in tablets.
Coffeinum-natrii benzoas in tablets and in ampoules.
Pyracetamum in tablets, capsules, and ampoules.
Bemegridum in ampoules.
Cordiaminum in ampoules.
Camphora in ampoules.
Aethimizolum in ampoules.
Sulfocamphocainum in ampoules.
Table 37 – Comparison characteristics of psychostimulants
Degree of effect
Psychostimulative
Decrease of need for sleep
Rise of blood pressure
Increase of heart work
Indications
Side effects
Phenaminum
Sydnocarbum
Caffeine
Table 38 – The main effects of analeptics
Effect
Stimulation
respiratory
center
Stimulation
vasomotor
center
Awakening
effect
Convulsive
action
44
Caffeine
of
of
Bemegride
Lobeline
Table 39 – Drugs for prescription
Drug name
Sydnocarbum
Coffeinumnatrii benzoas
Pyracetamum
Bemegridum
Cordiaminum
Camphora
Single dose and mode
of administration
Orally 0.005–0.025 g 1–2
times a day (in the first
part of day)
Orally 0.1–0.2 g 1-2
times a day;
subcutaneously 0.1–0.2 g
1–2 times a day
Orally, intramuscularly or
intravenously 0.4–1.2 g
3 times a day
Intravenously slowly
0.01–0.05 g
Subcutaneously,
intramuscularly or
intravenously 1 ml
Subcutaneously 0.2–1 g
Aethimizolum Intravenously or
intramuscularly 0.03–
0.06 g 1–2 times daily
Sulfocampho- Subcutaneously,
cainum
intramuscularly or
intravenously 0.2 g 2–3
times daily
Drug product
Tablets 0.005, 0.01 or 0.025 g
Tablets 0.1 or 0.2 g;
ampoules 1 or 2 ml of 10% or
20% solution
Tablets 0.2 g;
capsules 0.4 g;
ampoules 5 ml of 20% solution
Ampoules 10 ml of 0.5%
solution
Ampoules 1 ml
Ampoules 1 or 2 ml of 20% oil
solution
Ampoules 3 or 5 ml of 1% or
1.5% solution
Ampoules 2 ml of 10%
solution
45
REFERENCES
1. Chekman I.S. Pharmacology: Textbook / I.S. Chekman,
N.O. Gorchakova, N.I. Panasenko, P.O. Bekh. – Vinnytsya :
NOVA KNYHA Publishers, 2006. – 384 p.
2. Kresyun V.A. General pharmacology: Cource of Lectures /
V.A. Kresyun, D.Yu. Andronov, K.F. Shemonaeva. – Odessa :
OSMU, 2005. – 215 p.
3. Polevik I.V. Lectures on Pharmacology: For the Foreign Students
Being Educated in English / I.V. Polevik, A.I. Beketov,
M.G. Kurchenko. – Simferopol, 2003. – Part 1. – 100 p.
4. Polevik I.V. Lectures on Pharmacology: For the Foreign Students
Being Educated in English / I.V. Polevik, A.I. Beketov,
M.G. Kurchenko. – Simferopol, 2003. – Part 2. – 108 p.
5. Stefanov O. Pharmacology with General Prescription: Textbook for
English-speaking medical students / O. Stefanov, V. Kurcher. – К. :
Вид-во «Ельіньо». – 2004. – 156 p.
6. Pharmacology with General Prescription: Text-book for Englishspiking medical students. / O. Stefanov, V. Kurcher. – К. : Вид-во
«Ельіньо». – 2007. - 318 p.
7. Газій T.В. Study guide to basic pharmacology. Навчальний
посібник з фармакології / T.В. Газій. – Харків : “Факт”, 2005. –
126 c.
8. Harvey R.A. Pharmacology / Richard A. Harvey, Pamela C.
Chempe – 2nd edition. – Lippincott Williams & Wilkins, 1997. –
564 p.
9. Goodman. The pharmacological basis of therapeutics. / Goodman,
Gilman’s. – 9th edition. – McGraw-Hill, 1996. – 1811 p.
10. Bertram G.K. Basic and Clinical Pharmacology: Textbook
/ Bertram G. Katzung. – 10th edition. – McGraw-Hill Companies,
2007. – 1200 p.
11. Vysotsky I.Yu. Medical Prescription (for foreign students being
educated in English) / I.Yu. Vysotsky, R.A. Chramova,
A.A. Kachanova. – Sumy : Sumy State University Publishers,
2008. – 40 p.
12. Vysotsky I.Yu. Drugs affecting peripheral nervous system: for
foreign students being educated in English / I.Yu. Vysotsky,
R.A. Chramova, A.A. Kachanova. – Sumy : Sumy State University
Publishers, 2009. – 62 p.
46
CONTENTS
P.
Drugs Affecting the Afferent Innervation……………………………....... …..3
Cholinomimetics. Cholinesterase inhibitors……………………………... …..5
M-cholinergic antagonists………………………………………………... ….10
N-cholinergic antagonists: Ganglion Blocking Drugs and Skeletal
Muscles Relaxants……………………………………………………...... ….13
Adrenomimetics and Sympathomimetics………………………………... ….16
Adrenergic Antagonists……………………………………………….......….20
General Anesthetics…………………………...………………………..... .…22
Hypnotic Drugs. Ethyl Alcohol ……………………………………….... .....26
Antiepileptic Drugs. Antiparkinsonian Drugs ………………………….. ….28
Opioid Analgesics……………………………………………………....... ….30
Nonopioid Analgesics…………………………………………………..... ….33
Neuroleptics and Antidepressants ……………………………………...... ….36
Anxiolytic Drugs. Lithium Salts. Sedative Drugs …………………….....….39
Psychostimulants. Nootropic Drugs. Analeptics. Adaptogens ………...... ….41
REFERENCES……………...…………………………………………….….44
47