Drugs affecting the afferent innervationlib.sumdu.edu.ua/library/docs/rio/2011/m3078.doc · Web...

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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 3

Transcript of Drugs affecting the afferent innervationlib.sumdu.edu.ua/library/docs/rio/2011/m3078.doc · Web...

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MINISTRY OF PUBLIC HEALTH OF UKRAINEMINISTRY OF EDUCATION, SCIENCE, YOUTH AND

SPORTS OF UKRAINESUMY STATE UNIVERSITY

3078 METHODOLOGICAL INSTRUCTIONSfor practical training

on the topic “DRUGS AFFECTING PERIPHERAL AND CENTRAL NERVOUS

SYSTEM”

in Pharmacology coursefor foreign students

of speciality 7.110101 «Medical science»full-time training

Sumy Sumy State University

2011

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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.

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Biological chemistry and pharmacology departmentThematic Module “Drugs Affecting

Peripheral Nervous System”

Drugs Affecting the Afferent InnervationTopical 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 prescriptionPrescribe 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.

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8. Menthol in alcoholic solution and in ointment.

Table 1 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Anaesthesinum Orally 0.3 g through rectum 0.05–0.1 g; on the skin 5–10% ointment

Powder;tablets 0.3 g; suppositories 0.05 and 0.1 g;5% ointment

Novocainum For infiltration anesthesia 0.25-0.5% solution; for conduction anesthesia 1–2% solution; for permeation anesthesia 10–20% solution and 5–10% ointment; through rectum – suppository containing 0.1 g

Ampoules 0.25% and 0.5% solution – 1, 2, 5, 10 and 20 ml; 1% and 2% solution – 1, 2, 5, and 10 ml; bottle 200 or 400 ml of 0.25% or 0.5% solution; suppositories 0.1 g; 5% and 10% ointments

Trimecainum For infiltration anesthesia – 0.125%, 0.25% or 0.5% solution; for conduction anesthesia – 1–2% solution; for permeation anesthesia – 2–5% solution; for epidural anesthesia – 1–2% solution; for spinal anesthesia – 5% solution

Ampoules 10 ml of 0.25% solution; 2, 5, or 10 ml 0.5% or 1% solution; 1, 2, 5, or 10 ml 2% solution; 1 or 2 ml 5% solution

Lidocainum For infiltration anesthesia –0.25% or 0.5% solution; for conduction anesthesia – 0.5–2% solution; for permeation anesthesia –

Ampoules 10 or 20 ml of 1% solution; 2 or 10 ml of 2% solution; 2 ml of 10% solution

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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

There are no made forms at the plant. Pharmacist prepares these forms (the prescriptions can be written in short or full forms)

Bismuthi subnitras

Orally – 0.25–0.5 g; on the skin – 5–10% ointment and aspersion

Powder;tablets 0.25 or 0.5 g; 10% ointment

Carbo activatus Orally – 1–2 g for meteorism; 20–30 g (in the form of suspension in water) for poisonings

Powder; tablets 0.25 or 0.5 g

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)

1%, 2% or 5% alcoholic solution; 1% ointment

Cholinomimetics. Cholinesterase InhibitorsTopical 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.

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4. Direct M-, N-cholinomimetics: mechanism of action, pharmacological effects, peculiarities of pharmacokinetics, clinical applications, adverse effects.

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

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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.

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. Proserin in tablets, eye drops, and ampoules. 2. Galantamine in ampoules. 3. Pilocarpine in eye drops and eye ointment.4. Aceclidine in ampoules, eye drops, and eye ointment. 5. Carbacholine in eye drops.6. Dipiroxim in ampoules.7. Lobeline in ampoules.8. 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 gangliaSynapses of sympathetic fibers in adrenal medullaCarotid bodiesSynapses of postganglionic parasympathetic fibers in innervated organs Synapses of postganglionic sympathetic fibers in genital glands and vessels of skeletal musclesSynapses of motor nerves in

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skeletal musclesSynapses of central nervous system

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 VesselsSmooth muscles: - bronchi;- gastrointestinal tract;- urinary tract;- biliary tract;- uterus;- sphincters of GITExcretory glands activityEye muscles:- muscle – sphincter of pupil;- radial muscle;- ciliary muscle

Table 4 – Comparison characteristics of M-cholinomimetics

Effect Pilocarpine AceclidineReduction of intraoccular pressure Increase of tone and peristalsis of intestineIncrease of tone and contractibility of uterusIncrease of secretion of excretory glandsBradycardiaIndications for use

“+” – weak effect;10

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“++” – moderate effect;“+++” – marked effect

Table 5 – Comparison characteristics of cholinesterase inhibitors

Physostigmine Proserin Galantamine ArminMode of administrationDuration of actionIndications for useSymptoms of poisoningAntidotes

Table 6 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Proserinum Orally 0.01–0.015 g;subcutaneously 0.0005 g;in eyes 1–2 drops

Tablets 0.015 g;ampoules 1 ml of 0.05% solution;eye drops: 0.5% solution

Galanthamini hydrobromidum

Subcutaneously 0.0025–0.005 g Ampoules 1 ml of 0.1%, 0.25%, 0.5% or 1% solution

Pilocarpini hydrochloridum

In eyes: 1–2% solution (1–2 drops) or eye ointment

Eye drops: 1% or 2% solution in bottles 5 or 10 ml;1% or 2% eye ointment

Aceclidinum In eyes: 2-5% solution (1–2 drops) or 3–5% eye ointment;subcutaneously 0.002 g

2-5% solution of eye drops;3% and 5% eye ointment;ampoules 1 or 2 ml of 0.2% solution

Carbacholinum In eyes 1–2 drops of 0.5–1% solution

Eye drops: 0.5% or 1% solution in bottles 5 or 10 ml

Dipiroximum Subcutaneously, intramuscularly Ampoules 1 ml of 11

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or intravenously 0.15–0.3 g 15% solutionLobelini hydrochloridum

Intravenously slowly 0.005 g Ampoules 1 ml of 1% solution

Cytitonum Intravenously slowly 0.5 ml Ampoules 1 mlM-Cholinoceptor Antagonists

Topical questions1. 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 pharmacokinetics1. 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.

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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.

Fill in the following table

Table 7 – Comparison characteristics of М-cholinoceptor antagonists effects

Effects DrugAtropine Scopolamine Platyphyllin Methacin

Relaxation of bronchiDecrease of bronchial and digestive glands secretionReduction of spasm of intestine, biliary and urinary tractsDegree of М-cholinoceptor antagonists actionDirect myotropic antispasmodic actionTachycardiaReduction of vestibular disturbancesAntiparkinsonian actionMydriasisDuration of paralysis of accommodationIndications for use

“+” – weak action;“++” – moderate action;“+++” – marked action.

Tasks for prescription

Prescribe the following drugs and list indications for their use:13

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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.Table 8 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Atropini sulfas 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)

Tablets 0.0005 g;ampoules 1 ml of 0.1% solution;eye drops: 0.5% or 1% solution; 1% eye ointment

Extractum Belladonnae siccum

Orally 0.02–0.04 g 2-3 times daily;Through rectum 0.02–0.04 g 1–2 times daily

Powders for internal use;suppositories 0.02 or 0.04 g

Scopolamini hydrobromidum

Orally or subcutaneously 0.00025g;in eyes: 1–2 drops of 0.25% solution 1–2 times daily

Powders for internal use;ampoules 1 ml of 0.05% solution

Platyphyllini hydrotartras

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

Tablets 0.005 g;ampoules 1 ml of 0.2% solution;eye drops 1% or 2% solution

Methacinum Orally 0.002–0.004 g 2–3 times daily;subcutaneously, intramuscularly or intravenously 0.0005–0.001

Tablets 0.002 g;ampoules 1 ml of 0.1% solution

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g 1–2 times dailyTablets “Aeronum”

Orally 1–2 tablets before or during travel (for treatment or prevention of motion sickness)

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?

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Fill in the following tablesTable 9 – Comparison characteristics of ganglionic blockers

Hygronium Benzohexonium PachycarpineMode of drug administrationDuration of actionPenetration power through blood-brain barrierIndications for useSide effects

Table 10 – Comparison characteristics of peripheral myorelaxants

Dithylinum Tubocurarin chloridePeculiarities of chemical structure Mechanism of actionInteraction with cholinesterase inhibitorsDuration of actionMode of administrationIndications for useSide effects

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Tasks for prescriptionPrescribe the following drugs and list indications for their use:

1. Benzohexonium in tablets and ampoules.2. Pirilenum in tablets.3. Pentaminum in ampoules.4. Hygronium in ampoules and bottles.5. Tubocurarine in ampoules.6. Dithylinum in ampoules.

Table 11 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Benzohexonium

Orally 0.1–0.2 g 3–6 times daily;subcutaneously or intramuscularly 0.025 g 1–2 times daily

Tablets 0.1 g;

ampoules 1 ml of 2.5% solution

Pirilenum Orally 0.0025–0.005 g 2–5 times daily

Tablets 0.005 g

Pentaminum 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)

Ampoules 1 or 2 ml of 5% solution

Hygronium Intravenous drop by drop 0.04–0.08 g (as 0.1% solution)

Ampoules or bottles 0.1 g of dry medicinal remedy

Tubocurarini chloridum

Intravenously 0.0004–0.0005 g/kg

Ampoules 1 ml of 1.5% solution

Dithylinum Intravenously 0.0015–0.002 g/kg Ampoules 5 or 10 ml of 2% solution

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Adrenomimetic and Sympathomimetic DrugsTopical 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 pharmacokinetics1. What groups and certain drugs are used for prevention of bronchial

asthma attacks? Explain your answer.

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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.

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 prescriptionPrescribe 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 tablesTable 12 – Effects of excitation of alpha- and beta-adrenergic receptors

Tissue, organ ExcitationAlpha-adrenoceptor Beta-adrenoceptor

HeartBronchial smooth muscles Smooth muscles of vesselsSmooth muscles of intestineUterusRadial muscle of irisBladder

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Salivary glandsLiverAdipocytesPlatelets

Table 13 – Comparison characteristics of adrenomimetics

Drug Alpha-adrenomimetic action

Beta-adrenomimetic action

NoradrenalineAdrenalineMesatonumIsadrinumEphedrine

Table 14 – Comparison characteristics of pharmacological effects of adrenomimetics

Effect Adrenaline

Noradre-naline

Mesatonum

Isadrinum

Ephedrine

Cardiac pacingInfluence on blood pressureBroncho-lytic actionInfluence on carbohyd-rate metabolismExcitation of CNS

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Table 15 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Adrenalini hydrochloridum

Subcutaneously or intramuscularly 0.0003–0.00075 g;in eyes: 1-2 drops of 1–2% solution

Ampoules 1 ml of 0.1% solution;eye drops: 1% or 2% solution

Noradrenalini hydrotartras

Intravenously drop by drop 0.004–0.008 g in 1 L of 5% glucose solution

Ampoules 1 ml of 0.2% solution

Ephedrini hydrochloridum

Orally, subcutaneously, intramuscularly or intravenously 0.025 g 2–3 times a day

Tablets 0.025 g;ampoules 1 ml of 5% solution

Mesatonum 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

Powders for internal use;ampoules 1 ml of 1% solution;eye drops 1% or 2% solution

Naphthyzinum In nose 1–2 drops of 0.05–0.1% solution 3 times daily

Bottles 10 ml of 0.05% or 0.1% solution

Isadrinum Sublingually 0.005 g;inhalationly: 1–2 inhalations of 0.5-1% solution

Tablets 0.005 g;bottles 25 ml or 100 ml of 0.5% or 1% solution

Salbutamol Orally 0.002 g 3 times daily; Tablets 0.002 g;

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inhalationly: 1–2 inhalations 3 times daily

aerosol 10 ml

Adrenoceptor AntagonistsTopical 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?

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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.

Fill in the following tablesTable 16 – Comparison characteristics of adrenoceptor antagonists and sympatholytics

Drug name Main effects Indication for use

Side effects

PhentolamineTropaphenumPropranololOctadinumReserpine

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 Single dose and mode of administration

Drug product

Phentolamini hydrochloridum

Orally 0.05 g 3–5 times daily

Tablets 0.025 g

Tropaphenum Subcutaneously or intramuscularly 0.01–0.02 g

Ampoules 0.02 g of dry medicinal remedy

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1–3 times daily; intravenously 0.01 g

(before administration, substance of 1 ampoule should be dissolved in 1–2 ml of sterile water)

Prazosinum Orally 0.0005–0.002 g 3–4 times daily

Tablets 0.001, 0.002 or 0.005 g

Table 17 continuationAnaprilinum Orally 0.01–0.04 g 3–4

times daily;intravenously slowly 0.001 g

Tablets 0.01 or 0.04 g;ampoules 1 or 5 ml of 0.1% solution

Metoprololum Orally 0.05–0.1 g 2–4 times daily;intravenously slowly 0.005–0.015 g

Tablets 0.05 or 0.1 gampoules 5 ml of 1% solution

Talinololum Orally 0.05–0.1 g 3 times daily

Dragee 0.05 g

Octadinum Orally 0.025–0.05 g once daily

Tablets 0.025 g

Reserpinum Orally 0.00005–0.0001 g 1-3 times daily

Tablets 0.0001 or 0.00025 g

General AnestheticsTopical 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.

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6. The characteristic of some drugs for intravenous anesthesia: propanidid, ketamine, predionum, thiopental sodium, hexenalum, sodium oxybutiras.

Situational tasks in pharmacodynamics and pharmacokinetics1. 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?

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 actionSpeed of introduction in anesthesiaSeverity of anesthesia stagesSeverity of excitement stageIrritating actionRelaxation of skeletal muscles

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Influence on cardiovascular systemHepatotoxicity and nephrotoxicityIndications for use

Table 19 – Comparison characteristics of intravenous anesthetics

Characteristics Propanidid Ketamine Thiopental sodium

Sodium oxybutiras

Speed of anesthesia developmentDuration of anesthesiaInfluence upon respirationInfluence on cardiovascular systemTolerance of brain to hypoxiaIndications for use

Tasks for prescription

Prescribe the following drugs: Propanidid in ampoules.

1. Thiopental sodium in bottles. 2. Hexenalum in bottles.3. Sodium oxybutiras in ampoules. 4. Ketamine in ampoules.

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Table 20 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Propanididum Intravenously 0.005–0.01 g/kg

Ampoules 10 ml of 5% solution

Thiopentalum-natrium

Intravenously 0.4–0.5 g 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)

Hexenalum Intravenously 0.5–0.7 g Bottles 1.0 g of dry substance (should be dissolved before administration in 50 ml of sterile 0.9% solution of sodium chloride)

Natrii oxybutyras

Intravenously 0.07–0.12 g/kg Ampoules 10 ml of 20% solution

Orally 0.1–0.2 g/kg (for general anesthesia);

Bottles 400 ml of 5% syrup

2-3 table spoons before sleep (for treatment of insomnia)

Ketaminum Intramuscularly 0.006 g/kg;

intravenously 0.002 g/kg

Bottles 10 ml of 5% solution; or 20 ml of 1%

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solution

Hypnotic Drugs. Ethyl AlcoholTopical 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 pharmacokinetics1. 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

28

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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.

Fill in the following table

Table 21 – Comparison characteristics of hypnotic drugs

Characteristics Phenobarbital Nitrasepam Sodium oxybutiras

Speed of sleep developmentDuration of sleepMechanism of actionInfluence on sleep structureIndications for useSide 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 prescription29

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Drug name Single doses and mode of administration

Drug product

Nitrazepamum Orally 0.005–0.01 g before sleep)

Tablets 0.005 or 0.01 g

Phenobarbital Orally 0.1 g before sleep Tablets 0.05 or 0.1 gAethaminalum-natrium

Orally 0.1–0.2 g before sleep

Tablets 0.1 g

Zolpidem Orally 0.01 g before slee Tablets 0.01 gNatrii oxybutiras Orally 2–3 table spoons

before sleepBottles 400 ml of 5% syrup

Teturamum Orally 0.5 g once a day Tablets 0.25 gAntiepileptic 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

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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 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

PhenobarbitalDipheninumCarbamazepineEthosuximideLamotrigineSodium valproateClonazepam

Table 24 – Comparison characteristics of antiparkinsonian drugs

Cyclodolum Midantanum LevodopaMechanism of actionSide effects

Tasks for prescription

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Prescribe the following drugs: 1. Dipheninum in tablets.2. Carbamazepinum in tablets.3. Phenobarbital in tablets and powders for internal use.4. Ethosuximidum in capsules.5. Levodopa in tablets and capsules.6. Midantanum in coated tablets.7. “Nacom”.8. Cyclodolum in tablets.

Table 25 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Dipheninum Orally 0.117 g 3 times a day

Tablets 0.117 g

Carbamazepinum

Orally 0.2–0.4 g 2 or 3 times a day

Tablets 0.1, 0.2 or 0.4 g

Phenobarbitalum

Orally 0.05 g 2 times a day

Tablets 0.05 or 0.1 g

Ethosuximidum Orally 0.25 g 3 times a day

Capsules 0.25 g

Clonazepamum Orally 0.001–0.002 g 3–4 times a day

Tablets 0.001 g

Levodopa Orally 0.25–1.0 g 3 times a day

Tablets 0.25 or 0.5 g;capsules 0.25 or 0.5 g

Midantanum Orally 0.1–0.2 g 2–4 times a day

Coated tablets 0.1 g

“Nacom” 1 tablets 1–4 times a day TabletsCyclodolum Orally 0.001–0.005 g 2-

3 times a dayTablets 0.001, 0.002 or 0.005 g

Opioid AnalgesicsTopical questions

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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. 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 pharmacokinetics1. 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 MorphineCentral nervous systemNociceptive systemCough centerRespiratory center

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Vomiting centerVasomotor centerOculomotor centerVagal centerCenter of thermoregulationPeripheral tissues and organsCardiac rhythmBlood pressureTone of urinary and biliary tractsIntestinal toneDiuresisTable 27 – Comparison characteristics of opioid analgesics

Mor

phin

e

Om

nopo

n

Prom

edol

um

Fent

anyl

Pent

azoc

ine

Cod

eine

Analgesic activityDuration of actionDrug dependenceInhibition of respiratory centerSpasm of smooth musclesIndications for use

Notation: “+++”– pronounced effect; “++” – moderate effect; “+” – weak effect; “-“ – depressing effect.

Tasks for prescription

Prescribe the following drugs:

1. Morphine in ampoules.2. Omnopon in ampoules. 3. Promedolum in ampoules and tablets.

34

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4. Phentanyl in ampoules.5. Pentazocine in tablets.6. Pentazocine in ampoules and rectal suppositories.7. Naloxone hydrochloridum in ampoules.

Table 28 – Drugs for prescription

Drug name Single doses and mode of administration

Drug product

Morphini hydrochloridum

Orally 0.01 g;subcutaneously 0.01 g

Powders; ampoules 1 ml of 1% solution

Omnoponum Orally 0.01–0.02 g;subcutaneously 0.01–0.02 g

Powders; ampoules 1 ml of 1% or 2% solution

Promedolum Orally 0.025 gsubcutaneously 0.01–0.02 g

Tablets 0.025 gampoules 1 ml of 1% or 2% solution

Phentanylum Intramuscularly or intravenously 0.00005–0.0001 g

ampoules 2 ml or 5 ml of 0.005% solution

Pentazocini lactas Subcutaneously or intramuscularly 0.03 gthrough rectum 0.05 g

Ampoules 1 ml of 3% solution;suppositories 0.05g

Pentazocini hydrochloridum

Orally 0.05 g Tablets 0.05 g

Naloxoni hydrochloridum

Subcutaneously, intramuscularly or intravenously 0.0004–0.0008 g

Ampoules 1 ml or 2 ml of 0.04% solution

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Nonopioid AnalgesicsTopical 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, anti-

inflammatory, and antipyretic. 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 pharmacokinetics1. 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

Table 29 – Clinical use of analgesics

Indication for use

Mor

phin

e

Prom

edol

Fent

anyl

Pent

azoc

ine

Asp

irin

Ana

lgin

But

adio

ne

Traumatic pain

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Neuralgia, myositisSpastic painHeadache Myocardial infarctionAnalgesia of deliveryRheumatoid arthritis

Table 30 – Comparison characteristics of non-opioid analgesics

Drug Chemical structure

Indications for use

Side effects

Acetylsalicylic acidAnalginButadioneIndometacinOrtophen

Tasks for prescriptionPrescribe the following drugs:

1. Acetylsalicylic acid in tablets.2. Analgin in tablets and ampoules.3. Butadione in tablets and ointment.4. Diclofenac-sodium in tablets and ampoules.5. Paracetamol in tablets.

Table 31 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Acidum acetylsalicylicum

Orally 0.25–1.0 g 3-4 times a day

Tablets 0.1, 0.25 or 0.5 g

Analginum Orally 0.25–0.5 g 2-3 times a day;intramuscularly or

Tablets 0.5 g;

ampoules 1 or 2 ml of

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intravenously 0.25–0.5 g 2–3 times a day

25% or 50% solution

Butadionum Orally 0.1–0.15 g 2–4 times a day;for external application as 5% ointment

Tablets 0.15 g

5% ointment

Diclofenac-natrium

Orally 0.025–0.05 g 1-3 times a day;intramuscularly 0.075 g once a day

Coated tablets 0.025 g

Ampoules 3 ml of 2.5% solution

Table 31 continuation Paracetamolum Orally 0.2–0.4 g 2–3

times a dayTablets 0.2 g

Neuroleptic and Antidepressant Drugs

Topical questions1. 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 pharmacokinetics38

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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?

Fill in the following tables

Table 32 – Comparison characteristics of neuroleptics

Effect Degree of effectaminazine chlorprothixene haloperidol

Antipsychotic Decrease of motor activitySedativeHypnoticAnalgesics and general anesthetics potentiationAntiemeticHypotensiveExtrapyramidal disorder

Tasks for prescription

Prescribe the following drugs and list indications for their use: 1. Aminazinum in dragee and ampoules.2. Triftazinum in tablets and ampoules.3. Haloperidolum in tablets and ampoules. 4. Droperidolum in ampoules.5. Imizinum in tablets and ampoules.

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6. Amitriptylinum in tablets and ampoules.7. Fluoxetine in tablets. 8. Lithii carbonas in tablets.

Table 33 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Aminazinum Orally 0.025–0.05 g 1–3 times a day;intramuscularly 0.1 g 1–3 times a day;intravenously 1–2 ml of 2.5% solution with 20 ml of 40% glucose solution (in case of acute psychomotor agitation)

Dragee 0.025, 0.05 or 0.1 g;ampoules 1, 2, 5 or 10 ml of 2.5% solution

Triftazinum Orally 0.005–0.01 g once a day;intramuscularly 0.001–0.002 g 1 once a day

Tablets 0.001, 0.005 or 0.01 g;ampoules 1 ml of 0.2% solution

Haloperidolum

Orally 0.0015–0.005 g 3 times a day;intramuscularly 0.002–0.005 g

Tablets 0.0015 or 0.005 g;ampoules 1 ml of 0.5% solution

Droperidolum Intramuscularly or intravenously 0.0025–0.005 g

Ampoules 5 or 10 ml of 0.25% solution

Imizinum Orally 0.025-0.05 g 1–3 times a day;intramuscularly 0.025 g 1–3 times a day

Tablets 0.025 g;

ampoules 2 ml of 1.25% solution

Amitriptylinu Orally 0.025–0.05 g 3–4 Tablets 0.025 g;

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m times a dayintramuscularly or intravenously 0.025–0.04 g 3–4 times a day

ampoules 2 ml of 1% solution

Fluoxetinum Orally 0.02 g 1–2 times daily

Capsules 0.01 and 0.02 g

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 pharmacokinetics1. 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

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Table 34 – Comparison characteristics of tranquilizers Effect Degree of effect

chlozepidum diazepam buspirone amizylumAnxiolyticSedativeHypnoticAnalgesics potentiation Muscular relaxationAnticonvulsiveAmnestic

Table 35 – Comparison characteristics of psychotropic drugs, which inhibit central nervous system

Effect Neuroleptics Tranquilizers Sedative drugsAntipsychotic SedativeInhibition of vegetative reflexesAnalgesics and general anesthetics potentiationRelaxation of skeletal musclesAnticonvulsive AntiemeticHypotonicIatrogenic parkinsonism

Tasks for prescription

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Prescribe the following drugs: 1. Diazepam in tablets and ampoules.2. Phenazepam in tablets.3. Nitrazepam in tablets. 4. Lithium carbonate in tablets. 5. Sodium bromide in tablets.6. Tincture Valeriana.7. Tincture Leonurus.

Table 36 – Drugs for prescription

Drug name Single doses and mode of administration

Drug product

Diazepamum Orally 0.005–0.015 g 3 times a day;

intramuscularly or intravenously 0.01–0.02 g 1-3 times a day

Tablets 0.005 g;

ampoules 2 ml of 0.5% solution

Phenazepamum Orally 0.00025–0.001 g 1–2 times a day

Tablets; 0.0005 or 0.001 g

Nitrazepamum Orally 0.005–0.01 g 1–2 times a day

Tablets 0.005 or 0.01 g

Gidazepamum Orally 0.02–0.05 g 3 times daily

Tablets 0.02 or 0.05 g

Lithii carbonas Orally 0.3–0.6 g Tablets 0.3 gNatrii bromidum Orally 0.5–1.0 g 3–4

times a dayTablets 0.5 g

Tinctura Valerianae Orally 20–30 drops 3–4 times a day

Tincture 30 ml

Tinctura Leonuri Orally 30–50 drops Tincture 25 ml

Psychostimulants. Nootropic Drugs. Analeptics. Adaptogens 43

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Topical questions1. 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. Tasks for prescription

Prescribe the following drugs: 1. Sydnocarbum in tablets.2. Coffeinum-natrii benzoas in tablets and in ampoules.3. Pyracetamum in tablets, capsules, and ampoules.4. Bemegridum in ampoules.5. Cordiaminum in ampoules. 6. Camphora in ampoules.7. Aethimizolum in ampoules.8. Sulfocamphocainum in ampoules.

Table 37 – Comparison characteristics of psychostimulants

Degree of effect Phenaminum Sydnocarbum CaffeinePsychostimulativeDecrease of need for sleep Rise of blood pressureIncrease of heart work IndicationsSide effects

Table 38 – The main effects of analeptics

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Effect Caffeine Bemegride LobelineStimulation of respiratory centerStimulation of vasomotor centerAwakening effectConvulsive action

Table 39 – Drugs for prescription

Drug name Single dose and mode of administration

Drug product

Sydnocarbum Orally 0.005–0.025 g 1–2 times a day (in the first part of day)

Tablets 0.005, 0.01 or 0.025 g

Coffeinum-natrii benzoas

Orally 0.1–0.2 g 1-2 times a day;subcutaneously 0.1–0.2 g 1–2 times a day

Tablets 0.1 or 0.2 g;

ampoules 1 or 2 ml of 10% or 20% solution

Pyracetamum Orally, intramuscularly or intravenously 0.4–1.2 g 3 times a day

Tablets 0.2 g;capsules 0.4 g;ampoules 5 ml of 20% solution

Bemegridum Intravenously slowly 0.01–0.05 g

Ampoules 10 ml of 0.5% solution

Cordiaminum Subcutaneously, intramuscularly or intravenously 1 ml

Ampoules 1 ml

Camphora Subcutaneously 0.2–1 g Ampoules 1 or 2 ml of 20% oil solution

Aethimizolum

Intravenously or intramuscularly 0.03–0.06 g 1–2 times daily

Ampoules 3 or 5 ml of 1% or 1.5% solution

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Sulfocampho-cainum

Subcutaneously, intramuscularly or intravenously 0.2 g 2–3 times daily

Ampoules 2 ml of 10% solution

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REFERENCES1. 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 English-spiking 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.

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CONTENTS

P.Drugs Affecting the Afferent Innervation……………………………....... …..3Cholinomimetics. Cholinesterase inhibitors……………………………... …..5M-cholinergic antagonists………………………………………………...….10N-cholinergic antagonists: Ganglion Blocking Drugs and Skeletal Muscles Relaxants……………………………………………………...... ….13Adrenomimetics and Sympathomimetics………………………………... ….16Adrenergic Antagonists……………………………………………….......….20General Anesthetics…………………………...………………………..... .…22Hypnotic Drugs. Ethyl Alcohol ……………………………………….... .....26Antiepileptic Drugs. Antiparkinsonian Drugs ………………………….. ….28Opioid Analgesics…………………………………………………….......….30Nonopioid Analgesics………………………………………………….....….33Neuroleptics and Antidepressants ……………………………………......….36Anxiolytic Drugs. Lithium Salts. Sedative Drugs …………………….....….39Psychostimulants. Nootropic Drugs. Analeptics. Adaptogens ………...... ….41REFERENCES……………...…………………………………………….….44

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