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THEMATIC PLAN of PRACTICAL CLASSES FOR THE SECOND YEAR STUDENTS OF FOREIGN CITIZENS FACULTY IN 4th SEMESTER

Dates Theme of practical classes 16.03.-21.03.20 drugs. 23.02.-28.03.20 Antiadrenergic drugs. 30.03.-04.04.20 Final control N 1: «Autonomic drugs»

PRACTICAL CLASS THEME: DRUGS AFFECTING THE SYMPATHETIC NERVOUS SYSTEM. ADRENERGIC DRUGS

I. DRUGS OF LESSON’S THEME: α-β-adrenomimetics β-adrenomimetics 1. Epinephrini hydrochloridum* 1. Isoprenalini hydrochloridum

2. Ephedrini hydrochloridum β1-adrenomimetics α-adrenomimetics 1. Dobutaminum

1. Levarterenoli bitartras β2-adrenomimetics 2. Phenylephrini hydrochloridum 1. Salbutamolum* 3. Naphasolini nitras 2. Fenoterolum* 4. Oxymethazolini hydrochloridum 5. Xylomethazolini hydrochloridum

II. BASIC QUESTIONS FOR STUDYING: 1. Classification of adrenergic drugs. 2. α-β-adrenergic receptors agonists. Pharmacokinetics. Site and mechanism of action of direct-acting and indirect-acting agents. Basic effects (influence on cardiovascular system, smooth muscles, metabolism). Use. Adverse effects. 3. α-adrenergic receptors agonists. Pharmacokinetics. Mechanism of action, basic effects. Use. Adverse effects. 4. β-adrenergic receptors agonists. Pharmacokinetics. Mechanism of action and

basic effects of selective β2-adrenomimetics. Use. Adverse effects. III. ADDITIONAL INFORMATION FOR SELF-PREPARING OF STUDENTS CLASSIFICATION OF ADRENERGIC AGENTS 1. --adrenomimetics • Epinephrine – directly-acting • – indirectly-acting 2. -adrenomimetics • Levarterenol • • Nafazoline • Oxymethazoline • Xylomethazoline 3. -adrenomimetics

• (1, 2)

• (β1)

• (2)

• (2)

Figure 5-1. Schematic diagram of a generalized adrenergic junction. is transported into the noradrenergic ending or varicosity by a sodium-dependent carrier (A). Tyrosine is converted to , which is transported into the vesicle by a carrier (B) that can be blocked by reserpine. The same carrier transports (NE) and several other amines into these granules. Dopamine is converted to NE in the vesicle by dopamine--hydroxylase. Release of transmitter occurs when an action potential opens voltage-sensitive calcium channels and increases intracellular calcium. Fusion of vesicles with the surface membrane results in expulsion of norepinephrine, cotransmitters, and dopamine-- hydroxylase. Release can be blocked by drugs such as and bretylium. After release, norepinephrine diffuses out of the cleft or is transported into the cytoplasm of the terminal (uptake 1 [1], blocked by cocaine, tricyclic ) or into the postjunctional cell (uptake 2 [2]). Regulatory receptors are present on the presynaptic terminal. (SNAPs, synaptosome-associated proteins; VAMPs, vesicle-associated membrane proteins.)

Table 5-1. PHARMACODYNAMICS OF Drug Location Mechanism of Uses of action action Epinephrine α, β Stimulates Allergic reactions, cardiac arrest, postsynaptic for cardiac stimulation in Stokes- adrenergic Adams syndrom, hypotension receptors and shock, for in local anesthesia, bronchial asthma and chronic obstructive pulmonary diseases, ophthalmic conditions Ephedrine α, β Stimulates the Bronchodilation, cardiac release of stimulation, for nasal norepinephrine and decongestion in allergic postsynaptic and cold adrenergic receptors Levarterenol α, β1 Stimulates Hypotension and shock postsynaptic adrenergic receptors Phenylephrine α1,2 Stimulates Hypotension and shock, for nasal postsynaptic decongestion in adrenergic and cold, ophthalmic conditions receptors Nafazoline α1 Stimulates For nasal decongestion in allergic postsynaptic rhinitis and cold adrenergic receptors Isoprenaline β1,2 Stimulates Bronchial asthma and chronic postsynaptic obstructive pulmonary diseases, adrenergic cardiac stimulation, preterm labor receptors Dobutamine β1 Stimulates Cardiac stimulation postsynaptic adrenergic receptors Salbutamol β2 Stimulates Bronchial asthma and chronic postsynaptic obstructive pulmonary diseases, adrenergic preterm labor receptors

IV. PICK OUT TRUE ANSWERS 1. αβ-adrenomimetics are… 1. epinephrine* 4. 6. isoprenaline 2. ephedrine* 5. xylometazoline 7. salbutamol 3. levarterenol 2. Nonselective β-adrenomimetics drugs are… 1. epinephrine 3. levarterenol 5. isoprenaline* 2. ephedrine 4. xylometazoline 6. salbutamol

3. Selective β1-adrenomimetics cause… 1. hypertension 4. bradycardia 2. bronchodilation 5. increasing of force of contraction* 3. tachycardia* 6. decreasing of force of heart contraction 4. Indirect-acting αβ-adrenomimetics… 1. stimulate alpha- and beta-adrenoreceptors 2. block alpha- and beta-adrenoreceptors 3. stimulate the release of epinephrine* 4. stimulate the release of acetylcholine 5. inhibite the synthesis of epinephrine 5. Indications to use of epinephrine are… 1. shock* 2. bronchial asthma* 3. complete heart block and cardiac arrest* 4. hypoglycemic conditions* 5. paroxysmal tachycardia 6. prolongation of the duration of local anesthetics by vasoconstriction* 7. arterial hypertension 6. Direct-acting αβ-adrenomimetics are… 1. epinephrine* 3. levarterenol 5. xylometazoline 2. ephedrine 4. naphazoline 6. isoprenaline 7. salbutamol

7. Selective α1-adrenomimetics produce… 1. hyperclicemia 3. bronchodilation 5. bradycardia 2. hypotension* 4. contraction of prostate* 6. mydriasis* 8. Indications to use of isoprenaline are… 1. shock 4. hypertension 2. bronchial asthma* 5. paroxysmal tachycardia 3. sinus bradycardia* 6. atrioventricular block* 9. Indirect-acting αβ-adrenomimetics are… 1. epinephrine 3. ephedrine* 5. levarterenol 2. naphazoline 4. xylometazoline 6. isoprenaline

10. Selective α1-adrenomimetic drugs are… 1. epinephrine 3. levarterenol 5. xylometazoline* 2. ephedrine 4. naphazoline* 6. isoprenaline 11. Non-selective β-adrenomimetics produce… 1. hyperglycemia* 4. relaxation of uterine muscles* 2. hypertension* 5. tachycardia* 3. bronchodilation 6. mydriasis 12. Directly-acting αβ-adrenomimetics produce hypertension due to…

1. stimulation of α1-adrenoreceptors*

2. blocking of α2-adrenoreceptors 3. stimulation the release of epinephrine

4. stimulation of β1-adrenoreceptors

5. blocking of β2-adrenoreceptors 13. Indications to use of salbutamol are 1. shock 3. sinus bradycardia 5. premature labor* 2. bronchial asthma* 4. hypoglycemic conditions 6. arterial hypertension

14. Selective β2-adrenomimetics are … 1. epinephrine 3. naphazoline 5. isoprenaline 2. fenoterol* 4. dobutamine 6. salbutamol* 15. Indirect-acting αβ-adrenomimetic ephedrine produces… 1. hypertension* 4. bronchodilation* 6. tachycardia* 2. hyperglycemia* 5. dilation of blood vessels 7. stimulation of CNS* 3. constriction of mucous membrane vessels* 16. Non-selective β-adrenomimetics increase the rate and force of contraction of heart due to…

1. stimulation of beta 1-adrenoreceptors* 4. stimulation of beta 2-adrenoreceptors

2. blocking of beta 1-adrenoreceptors 5. blocking of beta 2-adrenoreceptors 3. stimulation of the release of epinephrine 17. Indications to use of naphazoline are 1. shock 4. hypoglycemic conditions 6. allergic rhinitis* 2. bronchial asthma 5. paroxysmal tachycardia 7. sinus bradycardia 3. in respiratory infections* 18. Non-selective β-adrenomimetics produce the relaxation of bronchial muscles because …

1. stimulation of β1-adrenoreceptors 4. stimulation of β2-adrenoreceptors*

2. blocking of β1-adrenoreceptors 5. blocking of β2-adrenoreceptors 3. stimulation of the release of epinephrine 19. Indications to the use of ephedrine are… 1. shock* 2. sinus bradycardia* 3. paroxysmal tachycardia 4. hypertension 5. bronchial asthma* 6. hypoglycemic conditions* 7. nasal congestion* 20. Epinephrine is used in… 1. bronchoconstriction* 3. anaphylactic shock* 5. hypoglycemic coma* 2. hypertension 4. open-angle glaucoma* 6. cardiac arrest* V. PROBLEM-ORIENTED CLINICAL CASES 1. Patient T.W., 22 years of age, female, complains nasal congestion due to acute respiratory viral infection. Please, administer P-drug for patient. 2. Patient M.A., 18 years of age, male, sportsmen, after excessive training complains severe weakness, vertigo and physician has diagnosed hypoglycemic coma. Please, administer P-drug for patient. 3. Patient O.P., 32 years of age, female, complains severe bleeding after teeth extraction. Please, administer P-drug for patient. 4. Patient S.C., 36 years of age, male, has immediate hypersensitivity reaction and bronchoconstriction. Please, administer P-drug for patient. 5. Patient B.J., 52 years of age, male, has cardiac arrest. Please, administer P-drug for patient.

VI. FILL IN THE BLANKS

Use the following terms to fill in the blanks in the Adrenergic drugs. Each term may be used more than once. Increase Decreases Constricts Dilates Contracts Relaxes αβ-ADRENERGIC DRUGS Body Sympathetic response tissue/organ 1 1 2 Blood vessels 1. ______Heart 2. ______rate 3. ______force Bronchi 4. ______GI tract 5. ______motility Eyes 6. ______pupil size 7. ______Intraocular pressure Urinary 8. ______bladder Prostate 9. ______Myometrium 10. ______Liver 11. ______Lipocytes 12. ______

VII. IDENTIFY THE LOCATION OF ACTION AND PHARMACOLOGICAL EFFECTS OF α-ADRENERGICS AND β- ADRENERGICS

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α PRACTICAL CLASS THEME: DRUGS AFFECTING THE SYMPATHETIC NERVOUS SYSTEM. ANTIADRENERGIC DRUGS

I. DRUGS OF LESSON’S THEME: α - adrenergic blockers β- adrenergic blockers 1. Phentolamini hydrochloridum 1. Propranololi hydrochloridum* 2. Prazosini hydrochloridum 2. Nadololum 3. Doxazosinum* 3. Atenololum* Sympatholytics 4. Metoprololum 1. Reserpinum 5.Bisoprololum

II. BASIC QUESTIONS FOR STUDYING: 1. Classification antiadrenergic agents.

2. Location and mechanism of action of α-adrenergic blockers. Selective α1- adrenergic blockers. Pharmacokinetics. Pharmacodynamics. Indications to the

use. Selective β1-adrenergic blockers.

3. Location and mechanism of action of β-adrenergic blockers. Selective β1- adrenergic blockers. Pharmacokinetics. Pharmacodynamics. Indications to the use. 4. Location and mechanism of action of α,β-adrenergic blockers. Pharmacokinetics. Pharmacodynamics. Indications to the use. 5. Indirect-acting antiadrenergic drugs or sympatholytics (reserpine). Pharmacokinetics. Location and mechanism of action, main therapeutic effects of sympatholytics. Adverse effects. Indications to the use.

III. ADDITIONAL INFORMATION FOR SELF-PREPARING OF STUDENTS CLASSIFICATION OF ANTIADRENERGIC AGENTS Direct-acting Antiadrenergics 1. --adrenoblocking drugs 3. -adrenoblocking drugs • • (1, 2) • • (1, 2) 2. -adrenoblocking drugs • (1) • (1, 2) • (1) • (1, 2)

• (1) • (1) • (α1) Indirect-acting Antiadrenergics Sympatholytics (α,β) • Reserpine • Guanethedine

Table 6-1. PHARMACODYNAMICS OF ANTIADRENERGIC AGENTS Drugs Location Mechanism of Uses of action action Labetalol α, β Blocks postsynaptic Hypertension, including adrenergic hypertensive emergencies receptors Phentolamine α1, α2 Blocks postsynaptic Hypertension caused by adrenergic pheochromocytoma, peripheral receptors endarteritis, Raynaud’s disorder, prevention of tissue necrosis from extravasation of vasoconstricive drugs, frostbite Prazosin α1 Blocks postsynaptic Hypertension, benign prostatic adrenergic hyperplasia receptors Propranolol β1, β2 Blocks postsynaptic Hypertension, angina pectoris, adrenergic cardiac arrhythmias, myocardial receptors infarction, migraine prophylaxis, panic paroxysms, hypertrophic obstructive cardiomyopathy Atenolol β1 Blocks postsynaptic Hypertension, angina pectoris, adrenergic myocardial infarction receptors Reserpine α, β Inhibits the Hypertension, mild stage synthesis of norepinephrine in presynaptic membrane of adrenergic receptors

IV. PICK OUT TRUE ANSWERS 1. αβ-adrenoblocking drugs are… 1. phentolamine 3. labetalol* 5. reserpine 2. prazosin 4. propranolol 6. carvedilol*

2. Cardioselective β1-adrenoblockers are… 1. phentolamine 3. prazosin 5. labetalol 2. propranolol 4.metoplolol* 5. atenolol*

3. Selective α1-adrenoblockers produce… 1. hypotension* 3. hypoglycemia 5. relaxation of prostate* 2. tachycardia 4. bronchoconstriction 6. vasoconstriction

4. Selective a1-adrenoblockers are… 1. phentolamine 3. labetalol 5. reserpine 2. prazosin* 4. propranolol 6. doxazosin* 5. Nonselective β-adrenoblockers are… 1. prazosin 3. propranolol* 5. atenolol 2. labetalol 4. * 6. nadolol* 6. Sympatholytics… 1. stimulate αβ-adrenoreceptors 4. stimulate the release of acetylcholine 2. block αβ-adrenoreceptors 5. inhibit the synthesis of norepinephrine 3. block the release of norepinephrine* 6.inhibit acethylcholinesterase 7. Indications to the use of propranolol are… 1. angina pectoris* 3. anxiety disorders* 5. prostatic hyperplasia 2. cardiac arrest 4. paroxysmal tachycardia* 6. hypertension* 8. Non-selective β-adrenoblockers produce… 1. hypoglycemia* 3. bronchoconstriction* 5. bradycardia* 2. hypotension* 4. relaxation of prostate 6. decreasing of intraocular pressure* 9. Reserpine… 1. stimulates αβ-adrenoreceptors 4. stimulates the release of acetylcholine 2. blocks αβ-adrenoreceptors 5. inhibits the synthesis of norepinephrine* 3. blocks the release of norepinephrine 6. promotes the synthesis of norepinephrine 10. Indications to the use of phentolamine are… 1. pheochromocytoma* 3. paroxysmal tachycardia 5. hypertension* 2. benign prostatic hyperplasia 4. peripheral vascular occlusive disease* 11. Indirect-acting antiadrenergic drugs (sympatholytics) are… 1. guanethidine* 3. labetalol 5. reserpine* 2. prazosin 4. propranolol 6. doxazosin 12. Non-selective α-adrenomimetic drugs are… 1. phentolamine* 3. labetalol 5. reserpine 2. prazosin 4. propranolol 6. phenoxybenzamine*

13. Selective β1-adrenoblockers produce… 1. hypoglycemia 3. bronchoconstriction 5. decreasing of oxygen demand* 2. hypotension* 4. bradycardia* 6. decreasing of intraocular pressure 14. Prazosin produces hypotension due to…

1. stimulation of α2-adrenoreceptors 4. stimulation of β1-adrenoreceptors

2. blocking of α1-adrenoreceptors* 5. blocking of β2-adrenoreceptors 3. stimulation the release of epinephrine 6. inhibition of epinephrine synthesis 15. Indications to the use of reserpine are… 1. prostatic hyperplasia 3. paroxysmal tachycardia 5. hypertension* 2. angina pectoris 4. cardiac arrest 6. frostbite 16. Pick out drugs used for treatment of hypertension initiated by pheochromocytoma and hyperthyroidism … 1. phentolamine* 3. labetalol 5. reserpine 2. prazosin 4. propranolol 6. phenoxybenzamine* 17. Drugs for emergency therapy of hypertensive crisis are ... 1. phentolamine 3. labetalol* 5. reserpine 2. prazosin 4. propranolol 6. phenoxybenzamine 18. Drugs for prolonged therapy of hypertension are… 1. atenolol* 3. labetalol 5. reserpine* 2. prazosin* 4. propranolol* 6. phentolamine 19. Drugs producing adverse effects such as tolerance and withdrawal syndrome are following: 1. metoprolol* 3. labetalol 5. reserpine 2. prazosin 4. propranolol* 6. atenolol* 20. The principal side effect of phentolamine is… 1. tolerance 3. bradycardia 5. withdrawal syndrom 2. hypotension 4. tachycardia* 6. bronchospasm

V. PROBLEM-ORIENTED CLINICAL CASES 1. Patient D.W., 42 years of age, female, has hypertension and chronic obstructive pulmonary disease. Physician administered atenolol, but she prefers low price of propranolol and wants to use it. Please, select suitable drug for this patient. 2. Patient B.A., 18 years of age, male, has frostbites after severe cold. Please, administer P-drug for patient. 3. Patient K.P., 56 years of age, female, has hypertension. She abruptly discontinued to use antihypertensive drug that was resulted in hypertensive crisis. Last 6 months she used atenolol. What is happened? Please, define and solve this problem. 4. Patient C.V., 63 years of age, male, has benign prostatic hyperplasia and hypertension. Please, administer P-drug for this patient. 5. Patient B.J., 32 years of age, male, has anxiety disorder such as panic paroxysm. Please, administer P-drug for this patient. VI. FILL IN THE BLANKS Use the following terms to fill in the blanks in the Antiadrenergic drugs. Each term may be used more than once. Increase Decreases Constricts Dilates Contracts Relaxes Αβ-Antiadrenergic drugs Body Sympathetic response tissue/organ 1 1 2 Blood vessels 1. ______Heart 2. ______rate 3. ______force Bronchi 4. ______GI tract 5. ______motility Eyes 6. ______pupil size 7. ______Intraocular pressure Urinary 8. ______bladder Prostate 9. ______Myometrium 10. ______Liver 11. ______Lipocytes 12. ______

VII. IDENTIFY THE LOCATION OF ACTION AND PHARMACOLOGICAL EFFECTS OF α-ADRENOBLOCKERS AND β- ADRENOBLOCKERS

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α 1.Drug used in vascular collapse Rp.: Sol. Phenylephrini hydrochloridi 1% - 1 ml D.t.d.N. 6 in amp. S. 0,5 ml (5 mg) is dissolved in 40 ml 20 % of glucose solution for intravenous administration in collapse. # 2. Drug used in rhinitis. Rp.: Sol. Naphazolini nitratis 0,1% - 10 ml D. S. 2 drops 3 times in a day in acute rhinitis. # 3. Drug used in bronchial asthma Rp.: Aeros. Salbutamoli N 1 D. S. For symptomatic treatment of bronchial asthma. # 4. Drug used in paroxysmal tachycardia Rp.: Propranololi hydrochloridi 0, 04 (40 мг) D.t.d.N. 50 in tab. S. 1 tablet 3 times in a day in paroxysmal tachycardia # 5. Drug used in hypertonia Rp.: Prazosini hydrochloridi 0, 001 (1 мг) D.t.d.N. 30 in tab. S.1 tab.2 - 3 times in a day. #

THEMATIC PLAN OF SELF STUDY CLASSES FOR THE THIRD YEAR STUDENTS OF FOREIGN CITIZENS FACULTY IN 4th SEMESTER Hou № Thematic plan rs Prescription writing. * Study of normative documents (Laws, orders, information letters); * analysis of the structure of the prescription. Solid dosage forms (Tablets, capsules, granules , sachets, capsules). * work with educational and methodical literature in the library and available database; 1. 2 * performing prescription writing tasks; * analysis of prescriptions. Semisolid dosage forms (ointment, paste, suppositories, gel, plasters, film). * work with educational literature in the library and available database; • performing prescription writing tasks * analysis of prescriptions. * performing tests. 2. Liquid dosage forms (Solutions for external and internal use. 2 Suspensions. Infusions and decoctions. Tinctures and extracts (liquid). Liniments. Mixtures. Aerosols. * work with educational literature in the library and available database; • performing prescription writing tasks * analysis of prescriptions. * performing tests. Dosage forms for injection.  work with educational literature in the library and available database; • performing prescription writing tasks * analysis of prescriptions. * performing tests. Presentation on "Modern methods of sterilization of drugs for injection". 3. Pharmacokinetics of drugs. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 4. Pharmadynamic of drugs. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 5. Drugs affecting the afferent nervous system. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 6. Cholinergic drugs 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 7. Cholinergic receptors blockers. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 8. Adrenergic drugs. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 9. Antiadrenergic drugs. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 10. General anesthetics. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 11. Anticonvulsants. Drugs for Parkinson's disease. 1 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 12. Analgesics. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 13. Central nervous system depressants. 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; 14. Central nervous system stimulants 2 * performing tests; * work with educational, methodical, reference literature; * solving problem-oriented cases; Total 27 h.

CURRENT RATING CONTROL «DRUGS AFFECTING THE PERIPHERAL NERVOUS SYSTEM»

1. Repeate: classification, location and mechanism of action, pharmacological effects, adverse effects and indications for the use of drugs affecting the peripheral nervous system. 2. Prepare: lecture copy-book and personal formulary.