Guideline of Pharmacology for International Student

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1 Guideline of Pharmacology for International Student I Character and Objective of the Course 1. Character of the Course: Basic Medical Course. 2. Preparatory Course: Physiology, biochemistry, and pathophysiology. 3. Textbook: Pharmacology (5th edition), Michelle A. Clark, Richard Finkel, Jose A. Rey, Karen Whalen. LWW.com. 4. Objective of the Course: pharmacological effects, mechanism of action, clinical uses, and adverse effects of the main and typified drugs. II Contents and requirements of teaching Unit I: Introduction to pharmacology Chapter Content Hours 1 Pharmacokinetics 4 2 Pharmacodynamics 4 Chapter 1 Pharmacokinetics 1. Absorption of drugs 1) The first-pass elimination 2) Bioavailability

2 2. Distribution of drugs 1) One-compartment open model and two-compartment open model. 2) Volume of distribution 3) Binding to plasma proteins 4) Blood-brain barrier. 3. Biotransformation of drugs 1) Enzyme inducers 2) Enzyme inhibitors 4. Excretion of drugs 1) Clearance 2) First-order kinetics and zero-order kinetics 3) Drug half-life (t 1/2 ) 4) The steady-state drug concentration (Css) 3) Hepatoenteral circulation Drug permeation across membranes: 1) Lipid diffusion and influence of PH on drug absorption. 2) The properties of filtration, facilitated diffusion and active transport. 1. Influencing factors of absorption, distribution, metabolism, and excretion. 2. The cytochrome P450 system (microsomal mixed-function oxidases).

3 3. Concentration-time curves. Chapter 2 Pharmacodynamics 1. Basic action of drugs: 1) Excitation and inhibition 2) Therapeutic action 3) Adverse reaction (side reaction, toxic effect, allergic reaction, residual reaction, dependence). 2. Dose-response relationship (dose-response curves): 1) Graded dose-response relations: efficacy, potency. 2) Quantal response relations: LD 50, ED 50, the therapeutic index. 3. Agonists and antagonists 1) Agonists: full agonists, partial agonists. 2) Antagonists: competitive antagonists, noncompetitive antagonists. 1. Drug receptor theory 2. Mechanism of drug action Unit II: Drugs affecting the autonomic nervous system Chapter Content Hour

4 3 The autonomic nervous system 2 4 Cholinergic agonists 2 5 Cholinergic antagonists 2 6 Adrenergic agonists 2 7 Adrenergic antagonists 2 Chapter 3 The Autonomic Nervous System Nerve:classification (according to transmitter). Nervous system: anatomy, function. : Transmitter: acetylcholine and noradrenaline (synthesis/storage/release/ termination). Receptor:classification. Drug:classification. Chapter 4 Cholinergic agonists Pharmacological effects, action mechanism, and therapeutic uses of

5 pilocarpine. Pharmacological profiles and therapeutic uses of reversible anticholinesterases (physostigmine, neostigmine). 1. Neurotransmission at cholinergic neurons and cholinoceptors. 2. Pharmacological properties of bethanechol, carbachol, irreversible anticholinesterases, and reactivators. Chapter 5 Cholinergic antagonists Pharmacological actions, therapeutic uses, and adverse reactions of atropine. Pharmacological properties of scopolamine. 1. Pharmacological properties of ipratropium and tiotropium. 2. Pharmacological properties of succinylcholine and D-tubocurarine. 3. Pharmacological properties of cholinesters and stimulating ganglionic drugs.

6 Chapter 6 Adrenergic agonists The pharmacological actions, clinical applications, and adverse reactions of epinephrine and dopamine. Pharmacokinetics, pharmacological effects, clinical applications, and adverse reactions of norepinephrine and isoproterenol. Pharmacological properties of metaraminol. Chapter 7 Adrenergic antagonists Pharmacological properties, therapeutic uses, and adverse effects of β-adrenoceptor antagonists. Classification and representative drug of β-adrenoceptor antagonists. Pharmacological properties, therapeutic uses, and adverse effects of phentolamine.

7 Unit III Drugs affecting the central nervous system Chapter Content Hour 8 Neurodegenerative Diseases 2 9 Anxiolytic and hypnotic drugs 2 12 Antidepressants 1 13 Antipsychotic drugs 2 14 Opioids 2 15 Epilepsy 1 41 Anti-inflammatory drugs and autacoids 2 Chapter 8 Neurodegenerative Diseases Pharmacological effects and uses of L-dopa. 1. Mechanism of action and uses:carbidopa, selegiline, tolcapone. 2. Pharmacokinetics, adverse effects, and drug interaction of L-Dopa. 1. Pathophysiology and clinical manisfestations of Parkinson s disease. 2. Classification of treatment of AD, mechanism of action, and representative drugs.

8 Chapter 9 Anxiolytic and hypnotic drugs Pharmacological effects, mechanism of action, and clinical uses of diazepam. 1. Pharmacokinetics and adverse effects of benzodiazepines and barbiturates. 2. Pharmacological effects of novel benzodiazepine receptor agnoists. 1. Clinic uses of flumazenil. 2. Pharmacological effects of chloral hydrate. Chapter 12 Antidepressants Pharmacological effects, mechanism of action, and clinical uses of imipramine. Mechanism of action and uses: fluoxetine, desipramine. Chapter 13 Antipsychotic drugs

9 1. Pharmacological effects, mechanism of action, clinical uses, and adverse effects of chlorpromazine. 2. Pharmacological effects, mechanism of action, and clinical uses of lithium carborate. 1. The action characters of phenothiazines, thioxanthines, and butyrophenones. 2. Mechanism of action and uses of clozapine. Chapter 14 Opioids Pharmacological effects, uses, and adverse effects of morphin and pethidine. 1. Action characters of codeine, fentanyl, methadone, and pentazocine. 2. Action and uses of naloxane. Tolerance and physical dependence of opioid.

10 Chapter 15 Epilepsy 1. Pharmacological effects, uses and adverse effects of phenytoinn sodium, carbamazepine, sodium valproate, primidone, ethosuximide, phenobarbital, and benzodiazepines. 2. Effect of carbamazepine on peripheral neuralgia. 3. Pharmacological effects, mechanism, and uses of magnesium sulfate.. Classification of epilepsy. Chapter 41 Anti-inflammatory drugs and autacoids 1. The effects and their respective mechanisms of NSAIDs. 2. The pharmacological effects, therapeutic uses, and adverse reactions of acetaminophen and aspirin. The characteristics of effects, clinic uses, and advantages of selective COX-2 inhibitors (celecoxib). Unit IV Drugs affecting the cardiovascular system

11 Chapter Content Hour 16 Heart failure 4 17 Antiarrhythmics 3 18 Antianginal drugs 2 19 Antihypertensives 4 21 Hyperlipidemias 1 22 Diuretics 2 Chapter 16 Heart failure 1. Pharmacological effects, mechanism of action, clinical uses, and adverse reactions of angiotension-converting enzyme inhibitors (enalapril). 2. Pharmacological effects, mechanism of action, and clinical uses of AT1 receptor antagonists (losartan). 3. Pharmacological effects, mechanism of action, clinical uses, and adverse reactions of cardiac glycosides (digoxin). 1. Pharmacological effects, mechanism of action, and clinical uses of β-adrenergic receptor antagonists (metoprolol). 2. Pharmacological effects and mechanism of diuretics (thiazides and loop diuretics).

12 1. Pathophysiology of congestive heart failure: regulation of sympathetic nervous system activity. 2. Ventricular remodeling in CHF. 3. The rennin-angiotensin system activation. Chapter 17 Antiarrhythmics Pharmacological effects, clinical uses, and adverse effects of quinidine, lidocaine, propafenone, propranolol, amiodarone, and verapamil. 1. Mechanisms of antiarrhythmic drug action. 2. Classifying of antiarrhythmic drugs. 3. Pharmacological effects, mechanism of action, and clinical uses of procainamide and phenytoin sodium. 1. Principles of cardiac electrophysiology. 2. Common arrhythmias and their mechanisms. Chapter 18 Antianginal drugs

13 1. Mechanism of action, therapeutic uses, and adverse effects of nitrates (nitroglycerin). 2. Mechanism of action and therapeutic uses of Ca 2+ channel blockers and β adrenergic receptor antagonists. The advantage of concomitant use of nitrates and β-blocking agents. Pathophysiology and classification of angina pectoris. Chapter 19 Antihypertensives Mechanism of action, therapeutic uses, and adverse effects of angiotensin converting enzyme inhibitors (ACEI), angiotensin Ⅱ-receptor antagonists, Ca 2+ channel blockers, βadrenergic antagonists, and α 1 adrenergic antagonists. Mechanism of action, therapeutic uses, and adverse effects of mixed adrenergic antagonists, centrally acting agents, diuretics, direct vasodilators, and K + ATP channel openers. Classification of antihypertensive drugs.

14 Chapter 21 Hyperlipidemias Mechanism of action and therapeutic uses of HMG-CoA reductase inhibitors, cholestyramine, fibrates, and nicotinic acid. 1. Definition and classification of hyperlipoproteinemia. 2. Adverse effects of HMG-CoA reductase inhibitors, cholestyramine, fibrates, and nicotinic acid. Chapter 22 Diuretics 1. Sites of action, mechanism of action, clinical uses, and adverse effects of loop diuretic (furosemide). 2. Sites of action, mechanism of action, clinical uses, and adverse effects of hydrochlorothiazide. 3. Sites of action, mechanism of action, clinical uses, and adverse effects of potassium-sparing diuretics (spironolactone and amiloride). 1. Pharmacokinetics of hydrochlorothiazide and loop diuretic.

15 2. Clinical uses of osmotic agents and carbonic anydrase inhibitor. Mechanism of action, clinical uses, and adverse effects of bumetanide. Unit V Drugs affecting the blood and other systems Chapter Content Hour 20 Blood drugs 3 27 Respiratory system 1 28 Gastrointestinal and antiemetic Drugs 2 Chapter 20 Drugs acting on the blood system 1. Anticoagulation features, mechanisms, clinical applications, and adverse reactions of heparin and warfarin. 2. Pharmacological effects and clinical applications of folic acid and vit-b Antiplatelet mechanism of aspirin, dipyridamole, and abciximab. 2. Pharmacological effects of streptokinase and urokinase. 3. Pharmacological effects of VitK and PAMBA.

16 Pharmacological effects and application of erythropoietin, GM-CSF, and TPO. Chapter 27 Drugs acting on respiratory system Pharmacological effects and mechanisms, clinical use, and adverse reactions of aminophylline and adrenergic receptor agonists. 1. The types of anti-asthmatic drugs, representative drug of each type. 2. Pharmacological effects and mechanisms, clinical use, and adverse reactions of glucocorticoids, M receptor blockers, and mast cell stabilizing drugs. Chapter 28 Gastrointestinal and antiemetic Drugs Pharmacological effects and clinical uses (H 2 receptor blockers and H + -K + -ATPase inhibitor). 1. The classification of inhibitors of gastric acid secretion and representative drugs.

17 2. Pharmacological effects and clinical uses (M receptor blockers, gastrin receptor antagonist, mucosal protective agents). Unit VI Drugs affecting the endocrine system Chapter Content Hour 23 Drugs acting on thyroid 1 24 Insulin and other glucose-lowering drugs 2 26 Adrenal hormones 3 Chapter 23 Drugs acting on thyroid 1. Pharmacologic effects and therapeutic uses of thyroid hormone. 2. Classification of antithyroid agents. 3. Pharmacologic effects, therapeutic uses, and adverse reactions of thioureas. Pharmacologic effects, therapeutic uses, and adverse reactions of iodine, radioiodine, and β adrenergic receptor antagonists. Synthesis, release and regulation of thyroid hormone.

18 Chapter 24 Insulin and other glucose-lowering drugs 1. Pharmacological effects, clinic uses and adverse reaction of insulin. 2. Pharmacokinetics, mechanism, clinic uses, and adverse reaction of oral hypoglycemic agents. Pharmacokinetics and mechanism of insulin. Pharmcological effects and clinic uses of insulin sensitizer. Chapter 26 Adrenal hormones The pharmacological effects, anti-inflammatory mechanism, clinical application, and adverse reactions of glucocorticoids. 1. Dosage and schedule of glucocorticoids. 2. Structure-activity relationships of adrenocorticosteroids. Pharmacokinetics of glucocorticoids. Physiological regulation of glucocorticoids.

19 Unit VII Chemotherapeutic drugs Chapter Content Hour 30 Principles of antimicrobial therapy 1 31 Cell wall inhibitors 2 32 Protein synthesis inhibitors 5 33 Quinolones, folic acid antagonists 2 Chapter 30 Principles of antimicrobial therapy 1. Terminology. 2. Classification and mechanisms of antibacterial drugs (targets). 3. Mechanisms that bacteria produce drug resistance to agents and mothods of avoiding drug resistance. Knowing the relationships among the human body, pathogenic microorganism and antiinfective drugs. Chapter 31 Cell wall inhibitors

20 1. Mechanisms of action of beta-lactams. 2. Antibacterial spectrum, therapeutic uses, and adverse effects of penicillin G. The measures used to prevent the anaphylactic shock of penicillin G. 3. Pharmacologic characteristics of semi-synthetic penicillins such as acid-stable penicillins, penicillinase-resistant penicillins, broad-spectrum penicillins, and antipseudomonal penicillins. 4. Pharmacologic characteristics, therapeutic uses, and adverse effects of cephalosporins of 4 generations. 1. Pharmacokinetics of both penicillin G and cephalosporins, and drug-resistant mechanisms. 2. Pharmacologic characteristics of carbapenems and beta-lactamase inhibitors. Chapter 32 Protein synthesis inhibitors 1. Mechanisms of action, antibacterial spectrum, therapeutic uses, and adverse effects of macrolides, lincomycin, and clindamycin. 2. Mechanisms of action, antibacterial spectrum, therapeutic uses, and adverse effects of aminoglycosides.

21 3. Mechanisms of action, therapeutic uses, and adverse effects of tetracylines and chloramphenicol. 1. Pharmacokinetics of aminoglycosides, tetracylines, and chloramphenicol. 2. Pharmacologic characteristics of glycopeptide vancomycin. Chapter 33 Quinolones, folic acid antagonists Mechanisms of action, therapeutic uses of quinolones, sulfonamides, and trimethoprim. Antibacterial spectrum and adverse effects of quinolones, sulfonamides, and trimethoprim. Pharmacokinetics of quinolones and sulfonamides.

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