HUF1 Pharmacology Content in Medicine Year 3 2015-2016

13. PHARMACOKINETICS
13.1. Drug ADME I, II, III
DRUG ABSORPTION
Membrane barriers and transport systems
Routes of administration
pH-partition hypothesis - ion trapping
Physiological and pathological factors that affect drug absorption
DRUG DISTRIBUTION
Factors that affect drug distribution
Drug-protein binding
Apparent volume of distribution
DRUG METABOLISM
The major drug metabolizing systems
The first-pass effect
Phase I reactions
Phase II conjugation reactions
Enzyme induction and inhibition
Genetic polymorphism on drug metabolism
Other factors that affect drug metabolism
DRUG EXCRETION
Renal excretion
Extra-renal excretion
Enterohepatic circulation
13.2. Pharmacokinetics I, II, III
PHARMACOKINETICS
Basic concepts
Compartmental models
Simple calculations
Half-life, volume of distribution, clearance, area under curve (AUC), bioavailability
Multiple-dose regimens
Calculation of loading and maintenance doses
Drug accumulation
Clinical implications

14. DRUG ACTION ON THE PERIPHERAL NERVOUS SYSTEM

14.1. Drug actions in the autonomic nervous system I

Sites of actions for cholinergic drugs
Classification of cholinergic receptors
Drug actions at postganglionic parasympathetic synapses
Drug actions at autonomic ganglia
Drugs that inhibit acetylcholine release
Drugs that inhibit acetylcholinesterase
14.2. Drug actions in the autonomic nervous system II
Sites of actions for adrenergic drugs
Classification of adrenergic receptors
Examples of adrenergic drugs
Drug actions at postganglionic sympathetic synapses
Clinical uses of adrenergic drugs

15. DRUG ACTION ON THE CARDIOVASCULAR SYSTEM

15.1. Drugs used in cardiovascular diseases I
Causes and Consequences of Intermittent Claudication
Goals of therapy
Drugs for treating Intermittent Claudication: Vasodilators; Anti-platelet agents; Cilostazol;
Pentoxifylline; Naftidrofuryl
Mechanisms of action
Causes and Consequences of Cardiac Arrest
Drugs for treating Cardiac Arrest: Vasoconstrictor sympathomimetics; Ionotropic
sympathomimetics
Mechanisms of action
Causes and Consequences of Septic Shock
Drugs for treating Septic Shock
Mechanisms of action
Importance of Cardiopulmonary Resuscitation
Drugs for treating global ischemia
Mechanisms of action
Blood Coagulation Cascades and Formation of Blood Clots
Uses of anti-fibrinolytic agent
Mechanisms of action
Pheochromocytoma and High Blood Pressure
Drug for treating Pheochromocytoma
Mechanisms of action
Alpha-adrenoceptors and Blood Pressure Regulation
Uses of alpha1-adrenoceptor blockers in treating hypertension
Mechanisms of action
15.2. Drugs used in cardiovascular diseases II
Clinical case of Intermittent claudication is introduced.
Discussion on the proper uses of appropriate and non-effective drugs in treating Intermittent
claudication.
15.3. Pharmacology I: anti-arrhythmic drugs
Introduction of electrical activities / ion channels / action potential of the heart
Causes of cardiac arrhythmias
Drugs for treating cardiac arrhythmias
Class I: Na+ channel block
Class II: β-Adrenoceptor block
Class III: Lengthening of refractoriness (without Na + channel block)
Class IV: Ca2+ channel block
Mechanisms of action
Clinical uses and Precautions
15.4. Pharmacology II: anti-hypertensive drugs
Introduction of physiological regulation of blood pressure and the development of hypertension.
Causes of high blood pressure
Non-pharmacologcial strategies in lowering blood pressure
Drugs for treating hypertension
Diuretics
-adrenoceptor (-AR) Blockers
Angiotensin Converting Enzyme (ACE) Inhibitor
Angiotensin Receptor (AR) Antagonist
Ca2+ Channel Blockers
-Adrenoceptor (a-AR) Blockers
Direct Acting Vasodilators
Diuretic plus b-AR Blocker
Diuretic plus ACE Inhibitor (or AR Blocker)
 Ca2+ Channel Blocker plus -AR Blocker
Ca2+ Channel Blocker plus ACE Inhibitor
-AR Blocker plus b-AR Blocker: Mechanisms of action
15.5. Pharmacology III: drugs for ischaemic heart disease
Physiological factors affecting coronary blood flow
Risk Factors
Non-pharmacological strategies in alleviating ischemic heart disease
Uses of drugs
Lipid Regulating Drugs
Malfunction of coagulation cascades
Uses of drugs
Anti-platelet drugs
Anti-coagulants
Thrombolytic Drugs
-adrenoceptor blocker
Angiotensin-converting enzyme inhibitor
Nitrates
Ca2+ channel blockers
Metabolic modulator
Mechanisms of action
15.6. Pharmacology IV: drugs for heart failure
Introduction of heart failure and risk factors for heart
failure development
Management of heart failure
Objectives of treatment
Uses of drugs
Diuretics
Digoxin
Angiotensin-converting enzyme inhibitor
-Adrenoceptor blockers
Nitrate plus Hydralazine
Spironolactone
Mechanisms of action

16. DRUGS AND THE GASTROINTESTINAL SYSTEM

16.1 Overview of drugs acting on the GI tract I
Control of acid secretion
Pathways and receptor targets modulating acid secretion/mucous secretion
Causes of ulcer (drugs, H. pylori)
Ulcer treatment
Antacids; misprostol; sucralfate; carbenoxolone
Anti-muscarinic; Anti-histamines; proton pump inhibitor
Triple therapy; bismuth
16.2. Overview of drugs acting on the GI tract II
Mechanisms of Peristalsis
GERD
Mechanism of prokinietic drugs; metoclopramide; domperidone; ertyhromycin; motilin; ghrelin
Drugs causing constipation
Drugs to facilitate defecation: bulk/osmotic/stimulant laxatives
Diarrhoea: causes, anti-diarrhoeal drugs, loperamide; diphenoxylate; kaolin; bismuth; charcoal
16.3. Antiemetics
Causes of nausea and emesis: Central and peripheral pathways involved in nausea and emesis control
Drugs used to induce emesis for emergency purposes: apomorphine, ipecacuanha
 Drugs used to prevent nausea and emesis: dopamine receptor antagonist (different classes), 5-HT3
receptor antagonist, NK1 receptor antagonists, other agents including dexamethasone
16.4. Antiemetics and drugs used for GI disorders
Understanding affinity and mechanisms of action of anti-emetic drugs
Receptor selectivity of dopamine, 5-HT3, muscarinic, histamine antagonists
Side effect profile
Brain penetration mechanism of chemotherapy-induced emesis