Medical Pharmacology and Therapeutics
Book information
Description
Medical Pharmacology & Therapeutics provides all the information medical and healthcare students need throughout their degree programme and beyond, including for professional qualifications such as the PSA. This all-round textbook covers basic pharmacology through to drug prescribing in clinical contexts, covering the pathogenic mechanisms of disease; drug actions, side effects, and the therapeutic principles of drug use. It takes a helpful systems-based approach that orders information according to body systems and disease areas, rather than by drug class. Now in its sixth edition, the book has been fully updated to include latest scientific understanding of drug action and administration and current best practice in prescribing medications, informed by the latest national guidelines. A clinical focus throughout – suitable for medical, nursing and other healthcare students throughout their trainingThorough update of clinically-relevant medicines to ensure best practiceInformation aligned with the British National Formulary (BNF), NICE guidelines and relevant professional benchmarks Comprehensive drug compendia allow all drugs to be identified and placed within their respective classesExtensive self-assessment questions to support learning and revisionNew to this edition Expanded discussion of the pathophysiology and management of shockRevised discussion of the management of chronic painConsideration of treatment of Covid-19Expanded discussion of the pathophysiology and management of shock Revised discussion of the management of chronic pain Consideration of treatment of Covid-19 OFC IFC Half Title Dedication Title Copyright Contents Preface Drug Dosage and Nomenclature 1 - Principles of Pharmacology and Mechanisms of Drug Action STUDYING PHARMACOLOGY FINDING DRUG INFORMATION RECEPTORS AND RECEPTOR-MEDIATED MECHANISMS ACTIONS OF DRUGS AT BINDING SITES (RECEPTORS) MAJOR TYPES OF RECEPTORS Transmembrane Ion Channels Seven-Transmembrane Receptors The G-protein system Second messenger systems Cyclic nucleotide system The phosphatidylinositol system Protease-activated receptors Enzyme-Linked Transmembrane Receptors Intracellular (Nuclear) Receptors OTHER SITES OF DRUG ACTION PROPERTIES OF RECEPTORS Receptor Binding Receptor Selectivity Drug Stereochemistry and Activity Receptor Numbers PROPERTIES OF DRUG ACTION DOSE–RESPONSE RELATIONSHIPS SELECTIVITY POTENCY EFFICACY TYPES OF DRUG ACTION AGONISTS Affinity and Intrinsic Activity Spare Receptors ANTAGONISTS PARTIAL AGONISTS INVERSE AGONISTS ALLOSTERIC MODULATORS ENZYME INHIBITORS AND ACTIVATORS NONSPECIFIC ACTIONS PHYSIOLOGICAL ANTAGONISTS TOLERANCE TO DRUG EFFECTS GENETIC VARIATION IN DRUG RESPONSES SUMMARY SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWER FURTHER READING 2 - Pharmacokinetics THE BIOLOGICAL BASIS OF CLINICAL PHARMACOKINETICS GENERAL CONSIDERATIONS Passage Across Membranes Passive diffusion Passage through membrane pores or ion channels Carrier-mediated processes Pinocytosis Drug Ionisation and Membrane Diffusion ABSORPTION ABSORPTION FROM THE GUT Drug Structure Drug Formulation Gastric Emptying First-Pass Metabolism Intestinal lumen Intestinal wall Liver Lung ABSORPTION FROM OTHER ROUTES Percutaneous (Transcutaneous) Administration Intradermal and Subcutaneous Injection Intramuscular Injection Intranasal Administration Inhalation Minor Routes DISTRIBUTION REVERSIBLE PROTEIN BINDING IRREVERSIBLE PROTEIN BINDING DISTRIBUTION TO SPECIFIC TISSUES Brain Fetus ELIMINATION METABOLISM Phase 1 Phase 2 Factors Affecting Drug Metabolism: Inducers and Inhibitors EXCRETION Excretion via the Urine Glomerular filtration Reabsorption Tubular secretion Excretion Via the Faeces THE MATHEMATICAL BASIS OF CLINICAL PHARMACOKINETICS GENERAL CONSIDERATIONS Zero-Order Reactions First-Order Reactions ABSORPTION Rate of Absorption Extent of Absorption DISTRIBUTION Rate of Distribution Extent of Distribution ELIMINATION Rate of Elimination The activity of the organ of elimination Reversible passage of drug from the blood into tissues Extent of Elimination CHRONIC ADMINISTRATION Time to Reach Steady State Plasma Concentration at Steady State Oral Administration Loading Dose PHARMACOKINETICS OF BIOLOGICAL DRUGS GENETIC VARIATION AND PHARMACOKINETICS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS DESCRIPTIVE QUESTION CASE-BASED QUESTIONS Case 1 Case 2 ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS DESCRIPTIVE ANSWERS CASE-BASED ANSWERS Case 1 Answer Case 2 Answer FURTHER READING 3 - Drug Discovery, Safety and Efficacy DRUG DISCOVERY DRUG APPROVAL SAFETY QUALITY EFFICACY ESTABLISHING SAFETY AND EFFICACY PRECLINICAL STUDIES TOXICITY TESTING CLINICAL TRIALS: PHASES I–III Phase I Studies Phase II Studies Phase III Studies Postmarketing Surveillance: Phase IV (Pharmacovigilance) SELF-ASSESSMENT ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS OBA ANSWERS FURTHER READING 4 - Neurotransmission and the Peripheral Autonomic Nervous System THE CENTRAL AND PERIPHERAL NERVOUS SYSTEMS PRINCIPLES OF NEUROTRANSMISSION PRESYNAPTIC RECEPTORS AND MODULATION OF TRANSMITTER RELEASE THE PERIPHERAL AUTONOMIC NERVOUS SYSTEM THE SYMPATHETIC NERVOUS SYSTEM AND NORADRENERGIC TRANSMISSION SYNTHESIS AND STORAGE OF CATECHOLAMINES: NORADRENALINE, ADRENALINE AND DOPAMINE NORADRENALINE RELEASE UPTAKE AND METABOLISM OF RELEASED NORADRENALINE Monoamine Oxidase Catechol-O-Methyltransferase SYMPATHETIC NERVOUS SYSTEM RECEPTORS THE PARASYMPATHETIC NERVOUS SYSTEM AND CHOLINERGIC TRANSMISSION SYNTHESIS OF ACETYLCHOLINE STORAGE OF ACETYLCHOLINE RELEASE OF ACETYLCHOLINE METABOLISM AND INACTIVATION OF RELEASED ACETYLCHOLINE CHOLINERGIC RECEPTORS Nicotinic N1 (or NG) Receptors Nicotinic N2 (or NM) Receptors Muscarinic Receptors OTHER TRANSMITTERS IN THE PERIPHERAL NERVOUS SYSTEM AMINES Dopamine Synthesis and storage of dopamine Release of dopamine Removal of activity of released dopamine Dopamine receptors Serotonin (5-Hydroxytryptamine) Synthesis of serotonin Storage of serotonin Release of serotonin Metabolism and removal of serotonin activity Serotonin receptors Histamine Synthesis of histamine Storage of histamine Release of histamine Removal of histamine activity Histamine receptors AMINO ACIDS γ-Aminobutyric Acid Synthesis and storage of γ-aminobutyric acid Release of γ-aminobutyric acid Removal of γ-aminobutyric acid activity γ-Aminobutyric acid receptors Glutamate Synthesis and storage of glutamate Release of glutamate Removal of glutamate activity Glutamate receptors Glycine Synthesis and storage of glycine Release of glycine Removal of glycine activity Glycine receptors Imidazoline receptor ligands PEPTIDES PURINES SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS 5 - Ischaemic Heart Disease MYOCARDIAL PERFUSION CLINICAL MANIFESTATIONS OF MYOCARDIAL ISCHAEMIA STABLE ANGINA PECTORIS ACUTE CORONARY SYNDROMES (UNSTABLE ANGINA, MYOCARDIAL INFARCTION AND SUDDEN CARDIAC DEATH) Unstable Angina Myocardial Infarction and Sudden Cardiac Death DRUGS FOR TREATING ANGINA ORGANIC NITRATES Mechanism of Action and Effects Pharmacokinetics Unwanted Effects BETA-ADRENOCEPTOR ANTAGONISTS (β-BLOCKERS) Mechanism of Action and Effects in Angina Pharmacokinetics Unwanted Effects CALCIUM CHANNEL BLOCKERS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects POTASSIUM CHANNEL OPENERS Mechanism of Action Pharmacokinetics Unwanted Effects SPECIFIC SINUS NODE INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects LATE SODIUM CURRENT INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects MANAGEMENT OF STABLE ANGINA MANAGEMENT OF ACUTE CORONARY SYNDROMES EARLY MANAGEMENT OF NON-ST ELEVATION ACUTE CORONARY SYNDROMES (NSTE-ACS) EARLY MANAGEMENT OF ST-SEGMENT ELEVATION MYOCARDIAL INFARCTION SECONDARY PROPHYLAXIS AFTER MYOCARDIAL INFARCTION SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING STABLE ANGINA ACUTE CORONARY SYNDROMES 6 - Systemic and Pulmonary Hypertension SYSTEMIC HYPERTENSION CIRCULATORY REFLEXES AND THE CONTROL OF SYSTEMIC BLOOD PRESSURE AETIOLOGY AND PATHOGENESIS OF SYSTEMIC HYPERTENSION CONSEQUENCES OF HYPERTENSION ANTIHYPERTENSIVE DRUGS DRUGS AFFECTING THE RENIN–ANGIOTENSIN SYSTEM Angiotensin-converting enzyme (ACE) inhibitors Mechanisms of action and uses Pharmacokinetics Unwanted effects Angiotensin II Receptor Antagonists Mechanism of action and uses Pharmacokinetics Unwanted effects Direct Renin Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Vasodilators Diuretics Mechanism of action in hypertension Thiazide and thiazide-type diuretics Loop diuretics Potassium-sparing diuretics Calcium Channel Blockers Potassium Channel Openers Mechanism of action Pharmacokinetics Unwanted effects Hydralazine Mechanism of action Pharmacokinetics Unwanted effects Nitrovasodilators Mechanism of action Pharmacokinetics Unwanted effects Drugs Acting on the Sympathetic Nervous System Beta-adrenoceptor antagonists Mechanism of action in hypertension Alpha-adrenoceptor antagonists (α-blockers) Mechanisms of action and uses Pharmacokinetics Unwanted effects Centrally acting antihypertensive drugs Selective imidazoline receptor agonists Mechanism of action Pharmacokinetics Unwanted effects Centrally acting α2-adrenoceptor agonists Mechanisms of action Pharmacokinetics Unwanted effects TREATMENT OF SYSTEMIC HYPERTENSION Drug Regimens in Hypertension Resistant and refractory hypertension Additional treatment to reduce risk of vascular complications Hypertension in Special Groups Accelerated or malignant hypertension and hypertensive emergency Renal artery stenosis Diabetic nephropathy Phaeochromocytoma Primary hyperaldosteronism Pregnancy PULMONARY ARTERIAL HYPERTENSION DRUGS FOR TREATING IDIOPATHIC PULMONARY HYPERTENSION Endothelin Receptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects Prostaglandins Selective Prostacyclin Receptor Agonist Mechanism of action Pharmacokinetics Unwanted effects Phosphodiesterase-5 Inhibitors Guanylate Cyclase Stimulator Mechanism of action Pharmacokinetics MANAGEMENT OF PULMONARY ARTERIAL HYPERTENSION SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS EXTENDED-MATCHING-ITEM QUESTION CASE-BASED QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWER FURTHER READING Systemic Hypertension Pulmonary Arterial Hypertension 7 - Heart Failure and Shock MAINTENANCE OF CARDIAC OUTPUT PATHOPHYSIOLOGY OF HEART FAILURE ACUTE LEFT VENTRICULAR FAILURE CHRONIC HEART FAILURE ROLE OF CALCIUM IN CARDIAC CONTRACTION SHOCK PATHOPHYSIOLOGY OF SHOCK Cardiogenic Shock Distributive (Vasodilatory) Shock INOTROPIC AND SYMPATHOMIMETIC DRUGS FOR THE TREATMENT OF HEART FAILURE AND SHOCK CARDIAC GLYCOSIDES Mechanism of Action and Effects Effect on myocardial contractility Effects on cardiac action potential and intracardiac conduction Pharmacokinetics Unwanted Effects Exacerbating Factors for Cardiac Glycoside Toxicity Treatment of Cardiac Glycoside Toxicity SYMPATHOMIMETICS Mechanisms of Action and Effects Pharmacokinetics Unwanted Effects PHOSPHODIESTERASE INHIBITORS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects ANGIOTENSIN RECEPTOR NEPRILYSIN INHIBITORS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects MANAGEMENT OF HEART FAILURE ACUTE LEFT VENTRICULAR FAILURE CHRONIC HEART FAILURE WITH REDUCED EJECTION FRACTION Nonpharmacological Treatment Diuretics Angiotensin-Converting Enzyme Inhibitors and Angiotensin II Receptor Antagonists Beta-Adrenoceptor Antagonists Sacubitril Valsartan Ivabradine Digoxin Other Vasodilators Cardiac Resynchronisation Therapy and Implantable Cardioverter Defibrillators HEART FAILURE WITH PRESERVED EJECTION FRACTION MANAGEMENT OF SHOCK Cardiogenic Shock Distributive (Vasodilatory) Shock SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 8 - Cardiac Arrhythmias BASIC CARDIAC ELECTROPHYSIOLOGY PACEMAKER ACTIVITY OF CELLS IN THE SPECIALISED CONDUCTING SYSTEM CONTROL OF DEPOLARISATION IN PACEMAKER AND NONPACEMAKER CELLS CONTROL OF CELL REPOLARISATION IN PACEMAKER AND NONPACEMAKER CELLS MECHANISMS OF TACHYARRHYTHMOGENESIS MECHANISMS OF ACTION AND CLASSIFICATION OF ANTIARRHYTHMIC DRUGS VAUGHAN-WILLIAMS CLASSIFICATION Class I Class II Class III Class IV Unclassified Drugs PROARRHYTHMIC ACTIVITY OF ANTIARRHYTHMIC DRUGS CLASS IA DRUGS Pharmacokinetics Unwanted effects CLASS IB DRUGS Pharmacokinetics Unwanted effects CLASS IC DRUGS Flecainide Pharmacokinetics Unwanted effects Propafenone Pharmacokinetics Unwanted effects CLASS II DRUGS Beta-Adrenoceptor Antagonists Pharmacokinetics CLASS III DRUGS Amiodarone Pharmacokinetics Unwanted effects Sotalol Pharmacokinetics Unwanted effects CLASS IV DRUGS Calcium Channel Blockers OTHER DRUGS FOR CARDIAC RHYTHM DISTURBANCES Cardiac Glycosides Adenosine Mechanism of action and effects Pharmacokinetics Unwanted effects Atropine Sulfate and Glycopyrronium Bromide Magnesium Sulfate DRUG TREATMENT OF ARRHYTHMIAS SUPRAVENTRICULAR TACHYARRHYTHMIAS Atrial Premature Beats Focal Atrial Tachycardia Atrial Flutter Atrial Fibrillation Avoiding stroke Better symptom control Junctional (Nodal) Tachycardias Immediate Management of Narrow-Complex Tachycardia of Uncertain Origin VENTRICULAR TACHYARRHYTHMIAS Ventricular Ectopic Beats Ventricular Tachycardia Ventricular Fibrillation BRADYCARDIAS Sinus Bradycardia Atrioventricular (AV) Block (‘Heart Block’) SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 9 - Cerebrovascular Disease and Dementia STROKE AETIOLOGY Ischaemic Strokes and Transient Ischaemic Attacks Haemorrhagic Strokes PREVENTION AND TREATMENT OF STROKE Primary Prevention of Ischaemic Stroke Acute Reperfusion Therapy for Ischaemic Stroke Secondary Prevention of Recurrent Ischaemic Stroke Primary Prevention of Haemorrhagic Stroke Acute Treatment of Haemorrhagic Stroke Secondary Prevention of Recurrent Haemorrhagic Stroke SUBARACHNOID HAEMORRHAGE DRUGS FOR SUBARACHNOID HAEMORRHAGE Nimodipine Pharmacokinetics Unwanted effects MANAGEMENT OF SUBARACHNOID HAEMORRHAGE DEMENTIA ALZHEIMER’S DISEASE Drugs for Alzheimer’s Disease Anticholinesterases Mechanisms of action and effects Pharmacokinetics Unwanted effects N-methyl-d-aspartate receptor antagonists Mechanism of action and effects Pharmacokinetics Unwanted effects Treatment of Alzheimer’s Disease VASCULAR DEMENTIA Treatment of Vascular Dementia DEMENTIA WITH LEWY BODIES SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING Stroke Subarachnoid Haemorrhage Dementia 10 - Peripheral Artery Disease ATHEROMATOUS PERIPHERAL ARTERY DISEASE SYMPTOMS OF PERIPHERAL ARTERY DISEASE DRUGS FOR PERIPHERAL ARTERY DISEASE Naftidrofuryl Oxalate Mechanism of action and effects Pharmacokinetics Unwanted effects Cilostazol Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF INTERMITTENT CLAUDICATION Nonpharmacological Treatment Pharmacological Treatment Surgical Treatment ACUTE AND CRITICAL LIMB ISCHAEMIA MANAGEMENT OF ACUTE AND CRITICAL LIMB ISCHAEMIA RAYNAUD’S PHENOMENON MANAGEMENT OF RAYNAUD’S PHENOMENON Nonpharmacological Treatment Pharmacological Treatment Arterial vasodilators Drugs acting primarily on blood components SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 11 - Haemostasis PLATELETS AND PLATELET AGGREGATION BLOOD COAGULATION AND THE COAGULATION CASCADE ARTERIAL AND VENOUS THROMBOSIS ANTIPLATELET DRUGS CYCLOOXYGENASE INHIBITORS Mechanism of Action on Platelets PHOSPHODIESTERASE INHIBITORS Mechanism of action Pharmacokinetics Unwanted Effects ADENOSINE DIPHOSPHATE (ADP) RECEPTOR ANTAGONISTS Mechanism of Action Pharmacokinetics Unwanted Effects GLYCOPROTEIN IIB-IIIA RECEPTOR ANTAGONISTS Mechanism of Action Pharmacokinetics Unwanted Effects Epoprostenol Mechanism of Action Pharmacokinetics Unwanted Effects CLINICAL USES OF ANTIPLATELET DRUGS ANTICOAGULANT DRUGS INJECTABLE ANTICOAGULANTS Heparins Mechanism of action and effects Pharmacokinetics Unfractionated heparin Low-molecular-weight heparins Control of heparin therapy Unwanted effects Fondaparinux Mechanism of action Pharmacokinetics Unwanted effects ORAL ANTICOAGULANTS Vitamin K Antagonists Mechanism of action Pharmacokinetics Monitoring of oral vitamin K antagonist therapy Unwanted effects Direct-Acting (Non–Vitamin K-Dependent) Oral Anticoagulants Direct factor Xa inhibitors Mechanism of action Pharmacokinetics Unwanted effects Direct thrombin inhibitors Mechanism of action Pharmacokinetics Unwanted effects CLINICAL USES OF ANTICOAGULANTS VENOUS THROMBOEMBOLISM Prevention of Deep Vein Thrombosis Mechanical methods Low-dose subcutaneous heparin Oral anticoagulants Treatment of Established Venous Thromboembolism Therapeutic anticoagulation Surgical venous thrombectomy Thrombolysis ANTICOAGULATION FOR ARTERIAL THROMBOEMBOLISM THE FIBRINOLYTIC SYSTEM FIBRINOLYTIC (THROMBOLYTIC) AGENTS Mechanism of Action Pharmacokinetics Unwanted Effects Clinical Uses of Fibrinolytic Agents ANTIFIBRINOLYTIC AND HAEMOSTATIC AGENTS Antifibrinolytic Agents Mechanisms of action Pharmacokinetics Unwanted effects Desmopressin CLINICAL USES OF ANTIFIBRINOLYTIC AND HAEMOSTATIC AGENTS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING Antiplatelet Agents Anticoagulants Fibrinolytic Drugs Haemostatic Drugs 12 - Asthma and Chronic Obstructive Pulmonary Disease ASTHMA CHRONIC OBSTRUCTIVE PULMONARY DISEASE DRUGS FOR ASTHMA AND CHRONIC OBSTRUCTIVE PULMONARY DISEASE DRUG DELIVERY TO THE LUNG Pressurised Metered-Dose Inhaler Pressurised Metered-Dose Inhaler with a Spacer Dry-Powder Inhaler Nebulisers SYMPTOM-RELIEVING DRUGS FOR AIRFLOW OBSTRUCTION (BRONCHODILATORS; ‘RELIEVERS’) β2-Adrenoceptor Agonists Mechanism of action and effects Pharmacokinetics Unwanted effects Antimuscarinics Mechanism of action and effects Pharmacokinetics Unwanted effects Methylxanthines Mechanism of action and effects Pharmacokinetics Unwanted effects Magnesium Sulfate Mechanism of action and effects Pharmacokinetics Unwanted effects ANTIINFLAMMATORY DRUGS FOR AIRWAYS OBSTRUCTION (‘PREVENTERS’) Corticosteroids Mechanism of action and effects Pharmacokinetics Unwanted effects Leukotriene Receptor Antagonist Mechanisms of action and effects Pharmacokinetics Unwanted effects Phosphodiesterase Type 4 Inhibitor Mechanism of action and effects Pharmacokinetics Unwanted effects Antibodies Targeting Type 2 Inflammatory Cytokines and IgE Mechanism of action Pharmacokinetics Unwanted effects Macrolide Antibiotics Cromones Pharmacokinetics Unwanted effects MANAGEMENT OF ASTHMA ACUTE ASTHMA PROPHYLAXIS OF CHRONIC ASTHMA ASPIRIN-INTOLERANT ASTHMA MANAGEMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS EXTENDED-MATCHING-ITEM QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING General Asthma Chronic Obstructive Pulmonary Disease 13 - Respiratory Disorders: Cough, Respiratory Stimulants, Cystic Fibrosis, Idiopathic Pulmonary Fibrosis and Neonatal Re ... COUGH DRUGS FOR TREATMENT OF COUGH Antitussives (Cough Suppressants) Centrally acting drugs (opioids) Peripherally acting drugs Locally acting drugs Expectorants Mucolytics MANAGEMENT OF COUGH RESPIRATORY STIMULANTS (ANALEPTIC DRUGS) CYSTIC FIBROSIS CFTR MODULATORS Mechanism of Action and Uses Pharmacokinetics Unwanted effects Treatment of Lung Disease Treatment of Malabsorption IDIOPATHIC PULMONARY FIBROSIS NEONATAL RESPIRATORY DISTRESS SYNDROME SELF-ASSESSMENT TRUE/FALSE QUESTIONS ANSWERS TRUE/FALSE ANSWERS FURTHER READING Cough Cystic Fibrosis Idiopathic Pulmonary Fibrosis Neonatal Respiratory Distress Syndrome 14 - Diuretics FUNCTIONS OF THE KIDNEY THE KIDNEY AND MAINTENANCE OF SALT AND WATER BALANCE The Proximal Convoluted Tubule The Loop of Henle The Distal Convoluted Tubule The Connecting Tubule and the Collecting Ducts Autoregulation of Glomerular Perfusion by Tubulo-Glomerular Feedback And Hormonal Control DIURETIC DRUGS LOOP DIURETICS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects THIAZIDE AND RELATED DIURETICS Mechanisms of Action and Effects Pharmacokinetics Unwanted Effects POTASSIUM-SPARING DIURETICS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects CARBONIC ANHYDRASE INHIBITORS Mechanism of Action and Uses Pharmacokinetics Unwanted Effects OSMOTIC DIURETIC Mechanism of Action and Uses Pharmacokinetics Unwanted Effects MANAGEMENT OF DIURETIC-INDUCED HYPOKALAEMIA MAJOR USES OF DIURETICS Diuretics for Treatment of Oedema in Heart Failure, Nephrotic Syndrome and Hepatic Cirrhosis Management of oedema resistant to diuretics Diuretics for Treatment of Hypertension Diuretic Use in Hypercalciuria with Renal Stone Formation Carbonic Anhydrase Inhibitors for Glaucoma Acetazolamide for Altitude Sickness Mannitol for Acute Brain Injury SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS EXTENDED-MATCHING-ITEM QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS EXTENDED-MATCHING-ITEM ANSWERS FURTHER READING 15 - Disorders of Micturition PATHOPHYSIOLOGY OF MICTURITION DISORDERS OF MICTURITION OVERACTIVE BLADDER AND URGE URINARY INCONTINENCE DRUGS FOR TREATMENT OF OVERACTIVE BLADDER Muscarinic Receptor Antagonists β3-Adrenoceptor Agonist MANAGEMENT OF OVERACTIVE BLADDER HYPOTONIC BLADDER URETHRAL SPHINCTER INCOMPETENCE LOWER URINARY TRACT SYMPTOMS IN MEN AND BENIGN PROSTATE ENLARGEMENT DRUGS FOR BENIGN PROSTATE ENLARGEMENT Alpha1-Adrenoceptor Antagonists 5α-Reductase Inhibitors Pharmacokinetics Unwanted effects Plant Extracts TREATMENT OF LOWER URINARY TRACT SYMPTOMS WITH BENIGN PROSTATE ENLARGEMENT SELF-ASSESSMENT TRUE/FALSE QUESTIONS EXTENDED-MATCHING-ITEM QUESTIONS CASE-BASED QUESTION ANSWERS TRUE/FALSE ANSWERS EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING 16 - Erectile Dysfunction PHYSIOLOGY OF ERECTION ERECTILE DYSFUNCTION DRUGS FOR ERECTILE DYSFUNCTION ORAL PHOSPHODIESTERASE INHIBITORS Mechanism of Action and Uses Pharmacokinetics Unwanted Effects ALPROSTADIL MANAGEMENT OF ERECTILE DYSFUNCTION PREMATURE EJACULATION SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 17 - General Anaesthetics ~ MECHANISMS OF ACTION OF GENERAL ANAESTHETICS DRUGS USED IN ANAESTHESIA INTRAVENOUS ANAESTHETICS Pharmacokinetics Unwanted Effects INTRAVENOUS OPIOIDS Pharmacokinetics Unwanted Effects INHALATIONAL ANAESTHETICS Pharmacokinetics Unwanted Effects SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 18 - Local Anaesthetics PHARMACOLOGY MECHANISM OF ACTION Structural Requirements of Local Anaesthetics Time to onset of action Receptor binding Duration of Action Binding to Other Receptors PHARMACOKINETICS UNWANTED EFFECTS Local Effects Systemic Effects TECHNIQUES OF ADMINISTRATION SURFACE ADMINISTRATION INFILTRATION ANAESTHESIA PERIPHERAL NERVE BLOCK ANAESTHESIA EPIDURAL ANAESTHESIA SPINAL ANAESTHESIA INTRAVENOUS REGIONAL ANAESTHESIA SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION EXTENDED-MATCHING-ITEM QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWER EXTENDED-MATCHING-ITEM ANSWERS FURTHER READING 19 - Opioid Analgesics and the Management of Pain PAIN AND PAIN PERCEPTION ANALGESIC DRUGS NONSTEROIDAL ANTIINFLAMMATORY DRUGS OPIOIDS NONOPIOID, NON-NSAID ANALGESICS OPIOID ANALGESICS Mechanism of Action Effects and Clinical Uses Effects on the central nervous system Analgesia Euphoria and dysphoria Respiratory depression Suppression of the cough centre Vomiting Miosis Endocrine effects Peripheral effects Gastrointestinal tract Cardiovascular system Other systems Tolerance and dependence Pharmacokinetics Unwanted Effects NONOPIOID, NON-NSAID AGENTS USED FOR ANALGESIA PAIN MANAGEMENT ACUTE PAIN CHRONIC PAIN NEUROPATHIC PAIN SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 20 - Anxiety, Obsessive-Compulsive Disorder and Insomnia ANXIETY DISORDERS BIOLOGICAL BASIS OF ANXIETY DISORDERS ANXIOLYTIC DRUGS Benzodiazepines Mechanism of action and effects Pharmacokinetics Unwanted effects Azapirones Mechanism of action and effects Pharmacokinetics Unwanted effects MANAGEMENT OF ANXIETY DISORDERS OBSESSIVE-COMPULSIVE DISORDER MANAGEMENT OF OBSESSIVE-COMPULSIVE DISORDER INSOMNIA SLEEP PATTERNS HYPNOTIC DRUGS Benzodiazepines Non-Benzodiazepine Hypnotics that Modulate the GABAA Receptor Mechanism of action and effects Pharmacokinetics Unwanted effects MANAGEMENT OF INSOMNIA SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE BEST ANSWER (OBA) QUESTION EXTENDED-MATCHING-ITEM QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING 21 - Schizophrenia and Bipolar Disorder SCHIZOPHRENIA BIOLOGICAL BASIS OF SCHIZOPHRENIA Dopamine–Glutamate Interactions and Their Possible Involvement in Schizophrenia ANTIPSYCHOTIC DRUGS CLASSIFICATION CONVENTIONAL (FIRST-GENERATION) ANTIPSYCHOTIC DRUGS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects ATYPICAL (SECOND-GENERATION) ANTIPSYCHOTIC DRUGS Mechanism of Action and Effects Pharmacokinetics Unwanted Effects MANAGEMENT OF SCHIZOPHRENIA MANIA AND BIPOLAR DISORDER BIOLOGICAL BASIS OF BIPOLAR DISORDER MOOD-STABILISING DRUGS FOR BIPOLAR DISORDER LITHIUM Mechanism of Action Pharmacokinetics Unwanted Effects ANTICONVULSANTS Mechanism of Action in Bipolar Disorder MANAGEMENT OF BIPOLAR DISORDER SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS EXTENDED-MATCHING-ITEM QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING Schizophrenia Bipolar Disorder 22 - Depression, Attention Deficit Hyperactivity Disorder and Narcolepsy DEPRESSION BIOLOGICAL BASIS OF DEPRESSION Corticotropin-Releasing Hormone in Depression Serotonergic and Noradrenergic Pathways in Depression Regulation of Brain-Derived Neurotrophic Factor (BDNF) in Depression ANTIDEPRESSANT DRUG ACTION ANTIDEPRESSANT DRUGS Tricyclic Antidepressant Drugs Mechanism of action Pharmacokinetics Unwanted effects Drug interactions Selective Serotonin Reuptake Inhibitors (SSRI) and Related Antidepressants Mechanism of action Pharmacokinetics Unwanted effects Drug interactions Serotonin and Noradrenaline Reuptake Inhibitors (SNRI) Mechanism of action and uses Pharmacokinetics Unwanted effects Noradrenaline Reuptake Inhibitors (NRI) Mechanism of action Pharmacokinetics Unwanted effects Presynaptic α2-Adrenoceptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects Serotonin Receptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects Irreversible Monoamine Oxidase A and B Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Drug interactions Reversible Inhibitors of Monoamine Oxidase A Mechanism of action and effects Pharmacokinetics Unwanted effects Drug interactions Melatonin Receptor Agonist and Serotonin Receptor Antagonist Mechanism of action and effects Pharmacokinetics Unwanted effects MANAGEMENT OF DEPRESSION ATTENTION DEFICIT HYPERACTIVITY DISORDER AND NARCOLEPSY ATTENTION DEFICIT HYPERACTIVITY DISORDER NARCOLEPSY DRUGS FOR ATTENTION DEFICIT HYPERACTIVITY DISORDER AND NARCOLEPSY Atomoxetine Mechanism of action Pharmacokinetics Unwanted effects Methylphenidate Mechanism of action Pharmacokinetics Unwanted effects Dexamfetamine Mechanism of action Pharmacokinetics Unwanted effects Modafinil Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER MANAGEMENT OF NARCOLEPSY SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION EXTENDED-MATCHING-ITEM QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING Depression Narcolepsy and ADHD 23 - Seizures and Epilepsy PATHOLOGICAL BASIS OF SEIZURES AND EPILEPSY NEUROTRANSMITTERS AND SEIZURES ANTISEIZURE DRUGS SODIUM CHANNEL BLOCKERS Carbamazepine, Oxcarbazepine, Eslicarbazepine Acetate Mechanism of action and uses Pharmacokinetics Unwanted effects Phenytoin and Fosphenytoin Mechanism of action and uses Pharmacokinetics Unwanted effects Lacosamide Mechanism of action and uses Pharmacokinetics Unwanted effects Lamotrigine Mechanism of action and uses Pharmacokinetics Unwanted effects Zonisamide Mechanism of action and uses Pharmacokinetics Unwanted effects Rufinamide Mechanism of action and uses Pharmacokinetics Unwanted effects GAMMA-AMINOBUTYRIC ACID RECEPTOR AGONISTS Benzodiazepines Mechanism of action and uses Pharmacokinetics Unwanted effects Phenobarbital and Primidone Mechanism of action and effects Pharmacokinetics Unwanted effects GAMMA-AMINOBUTYRIC ACID REUPTAKE INHIBITOR Tiagabine Mechanism of action and uses Pharmacokinetics Unwanted effects GAMMA-AMINOBUTYRIC ACID TRANSAMINASE INHIBITOR Vigabatrin Mechanism of action and uses Pharmacokinetics Unwanted effects DRUGS WITH MULTIPLE ACTIONS Sodium Valproate Mechanism of action and uses Pharmacokinetics Unwanted effects Topiramate Mechanism of action and uses Pharmacokinetics Unwanted effects NEURONAL CALCIUM CHANNEL BLOCKERS Ethosuximide Mechanism of action and uses Pharmacokinetics Unwanted effects Gabapentin and Pregabalin Mechanism of action and uses Pharmacokinetics Unwanted effects SYNAPTIC VESICLE PROTEIN 2A INHIBITORS Levetiracetam and Brivaracetam Mechanism of action and uses Pharmacokinetics Unwanted effects AMPA GLUTAMATE RECEPTOR ANTAGONIST Perampanel Mechanism of action and uses Pharmacokinetics Unwanted effects CANNABINOIDS INTERACTIONS AMONG ANTISEIZURE DRUGS MANAGEMENT OF EPILEPSY TREATMENT OF INDIVIDUAL SEIZURES PROPHYLAXIS FOR SEIZURES Refractory Epilepsy Therapeutic Drug Monitoring Duration of Treatment Childhood Febrile Seizures ANTISEIZURE DRUGS IN PREGNANCY SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 24 - Extrapyramidal Movement Disorders and Spasticity THE BASAL GANGLIA AND CONTROL OF MOTOR FUNCTION PARKINSON’S DISEASE AND RELATED SYNDROMES DRUGS FOR PARKINSON’S DISEASE DOPAMINERGIC DRUGS Levodopa Mechanism of action Pharmacokinetics Unwanted effects Dopamine Receptor Agonists Mechanism of action Pharmacokinetics Unwanted effects Selective Monoamine Oxidase Type B Inhibitors Mechanism of action and effects Pharmacokinetics Unwanted effects Catechol-O-Methyltransferase Inhibitors Mechanism of action and effects Pharmacokinetics Unwanted effects ANTIMUSCARINIC DRUGS Mechanism of action and effects Pharmacokinetics Unwanted effects AMANTADINE Mechanism of action and effects Pharmacokinetics Unwanted effects MANAGEMENT OF PARKINSON’S DISEASE AND RELATED SYNDROMES OTHER INVOLUNTARY MOVEMENT DISORDERS (DYSKINESIAS) MONOAMINE DEPLETOR FOR MOVEMENT DISORDERS Tetrabenazine Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF DYSKINESIAS AND DYSTONIAS SPASTICITY DRUGS FOR SPASTICITY Diazepam Baclofen Mechanism of action Pharmacokinetics Unwanted effects Cannabinoids Mechanisms of action, effects and uses Pharmacokinetics Unwanted effects Tizanidine Mechanisms of action Pharmacokinetics Unwanted effects Dantrolene Mechanism of action and uses Pharmacokinetics Unwanted effects MANAGEMENT OF SPASTICITY SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING Parkinson’s Disease Other Movement Disorders and Spasticity 25 - Other Neurological Disorders: Multiple Sclerosis, Motor Neuron Disease and Guillain–Barré Syndrome MULTIPLE SCLEROSIS DISEASE-MODIFYING THERAPIES MANAGEMENT OF MULTIPLE SCLEROSIS MOTOR NEURON DISEASE DRUG TREATMENT GUILLAIN–BARRÉ SYNDROME EARLY MANAGEMENT SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 26 - Migraine and Other Headaches ~ MIGRAINE PATHOGENESIS OF MIGRAINE DRUGS FOR MIGRAINE SPECIFIC DRUGS FOR THE ACUTE MIGRAINE ATTACK Triptans Mechanisms of action and effects Pharmacokinetics Unwanted effects Ergotamine Mechanism of action Pharmacokinetics Unwanted effects PROPHYLACTIC DRUGS Beta-Adrenoceptor Antagonists Antiseizure Drugs Amitriptyline Calcitonin Gene-Related Peptide (CGRP) Antagonists Mechanisms of action and effects Pharmacokinetics Unwanted effects ACE Inhibitors and Angiotensin II Receptor Antagonists MANAGEMENT OF MIGRAINE AND OTHER HEADACHES ACUTE MIGRAINE ATTACKS PROPHYLAXIS OF MIGRAINE MEDICATION-OVERUSE HEADACHE MANAGEMENT OF OTHER HEADACHES SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE BEST ANSWER (OBA) QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWER FURTHER READING 27 - The Neuromuscular Junction and Neuromuscular Blockade NEUROMUSCULAR TRANSMISSION DRUGS ACTING AT THE NEUROMUSCULAR JUNCTION ACETYLCHOLINESTERASE (AChE) INHIBITORS (ANTICHOLINESTERASES) INHIBITORS OF ACETYLCHOLINE RELEASE NEUROMUSCULAR JUNCTION BLOCKERS Competitive N2 Receptor Antagonists (Nondepolarising Blockers) Mechanism of action and effects Pharmacokinetics Unwanted effects Depolarising Neuromuscular-Blocking Drugs Mechanism of action and effects Pharmacokinetics Unwanted effects INDICATIONS FOR NEUROMUSCULAR-BLOCKING DRUGS ENDOTRACHEAL INTUBATION DURING SURGICAL PROCEDURES CRITICAL ILLNESS ANTAGONISING NEUROMUSCULAR BLOCK SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 28 - Myasthenia Gravis ACETYLCHOLINESTERASE (AChE) INHIBITORS MECHANISM OF ACTION AND EFFECTS PHARMACOKINETICS AND CLINICAL USES UNWANTED EFFECTS MANAGEMENT OF MYASTHENIA GRAVIS LAMBERT–EATON MYASTHENIC SYNDROME SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 29 - Nonsteroidal Antiinflammatory Drugs THE ROLE OF CYCLOOXYGENASE ENZYMES IN THE ACTIONS OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS NONSTEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDs) MECHANISMS OF ACTION CLASSIFICATION OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS ACTIONS AND EFFECTS OF NONSELECTIVE NONSTEROIDAL ANTIINFLAMMATORY DRUGS Analgesic Effect Antiinflammatory Effect Antipyretic Effect Reduction of Platelet Aggregation PHARMACOKINETICS UNWANTED EFFECTS Gastrointestinal Effects Renal Effects Cardiovascular Effects Hypersensitivity Effects in Pregnancy Other Unwanted Effects CYCLOOXYGENASE-2-SELECTIVE INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects PARACETAMOL Mechanism of Action Pharmacokinetics Unwanted Effects INDICATIONS FOR USING NONSTEROIDAL ANTIINFLAMMATORY DRUGS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION EXTENDED-MATCHING-ITEM/CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER EXTENDED-MATCHING-ITEM/CASE-BASED ANSWERS FURTHER READING 30 - Rheumatoid Arthritis, Other Inflammatory Arthritides and Osteoarthritis RHEUMATOID ARTHRITIS OTHER TYPES OF INFLAMMATORY ARTHRITIS: THE SPONDYLOARTHROPATHIES DRUGS FOR TREATMENT OF INFLAMMATORY ARTHRITIS CONVENTIONAL SYNTHETIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS Methotrexate Sulfasalazine Antimalarials Mechanism of action Monitoring and prevention of unwanted effects Leflunomide Mechanism of action Pharmacokinetics Unwanted effects Monitoring and prevention of unwanted effects TARGETED SYNTHETIC DISEASE-MODIFYING ANTIRHEUMATIC DRUGS Janus Kinase Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Phosphodiesterase Type 4 Inhibitors Mechanism of action and use Pharmacokinetics Unwanted effects BIOLOGICAL DISEASE-MODIFYING ANTIRHEUMATIC DRUGS Tumour Necrosis Factor Alpha (TNFα) Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Interleukin-1 Receptor Antagonist Mechanism of action Pharmacokinetics Unwanted effects Interleukin-6 Receptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects Interleukin-12 and Interleukin-23 Receptor Antagonist Mechanism of action and uses Pharmacokinetics Unwanted effects Interleukin-17A Inhibitor Mechanism of action and uses Pharmacokinetics Unwanted effects T-Cell Activation Inhibitors Mechanism of action and uses Pharmacokinetics Unwanted effects Anti-CD20 B-Cell Depleter Mechanism of action and uses Pharmacokinetics Unwanted effects MANAGEMENT OF RHEUMATOID ARTHRITIS MANAGEMENT OF SPONDYLOARTHROPATHIES OSTEOARTHRITIS MANAGEMENT OF OSTEOARTHRITIS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING Rheumatoid Arthritis and Other Inflammatory Arthritides Osteoarthritis 31 - Hyperuricaemia, Gout and Pseudogout THE PATHOPHYSIOLOGY OF GOUT PSEUDOGOUT DRUGS FOR THE TREATMENT OF GOUT AND PREVENTION OF HYPERURICAEMIA DRUGS FOR THE TREATMENT OF ACUTE GOUT Colchicine Mechanism of action and uses Pharmacokinetics Unwanted effects DRUGS FOR TREATMENT OF HYPERURICAEMIA Xanthine Oxidase Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Rasburicase Mechanism of action Pharmacokinetics Unwanted effects Uricosuric Agents Mechanism of action Pharmacokinetics Unwanted effects TREATMENT OF GOUT ACUTE GOUT PREVENTION OF GOUT ATTACKS TREATMENT OF PSEUDOGOUT SELF-ASSESSMENT ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 32 - Nausea and Vomiting NAUSEA AND VOMITING ANTIEMETIC AGENTS Antihistamines Mechanism of action and clinical use Pharmacokinetics Unwanted effects Antimuscarinic Agent Mechanism of action and clinical use Pharmacokinetics Unwanted effects Dopamine Receptor Antagonists Mechanism of action and clinical use Pharmacokinetics Unwanted effects 5-HT3 Receptor Antagonists Mechanism of action and clinical use Pharmacokinetics Unwanted effects Neurokinin 1 Receptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects Cannabinoids Mechanism of action and clinical use Pharmacokinetics Unwanted effects Corticosteroids Benzodiazepines MANAGEMENT OF NAUSEA AND VOMITING Drug-Induced Vomiting Postoperative Nausea and Vomiting Motion Sickness Vomiting in Pregnancy VERTIGO DRUGS FOR TREATMENT OF VERTIGO MANAGEMENT OF VERTIGO SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 33 - Dyspepsia, Peptic Ulcer Disease and Gastrooesophageal Reflux Disease THE SPECTRUM OF DISEASE NON-ULCER (FUNCTIONAL) DYSPEPSIA PEPTIC ULCER DISEASE AND GASTRITIS Mechanisms of Protection of Gastric and Duodenal Mucosa Aetiology of Peptic Ulceration and Gastritis Helicobacter pylori and peptic ulceration Helicobacter pylori and gastric ulceration Helicobacter pylori and duodenal ulceration Drugs and Peptic Ulceration Other Causes of Peptic Ulcer GASTROOESOPHAGEAL REFLUX DISEASE (GORD) OESOPHAGEAL SPASM CONTROL OF GASTRIC ACID SECRETION DRUGS FOR TREATING DYSPEPSIA, PEPTIC ULCER AND GASTROOESOPHAGEAL REFLUX DISEASE ANTISECRETORY DRUGS Proton Pump Inhibitors Mechanism of action Pharmacokinetics Unwanted effects Histamine H2 Receptor Antagonists Mechanism of action Pharmacokinetics Unwanted effects ANTACIDS Mechanism of action Unwanted effects Antacids with Alginic Acid CYTOPROTECTIVE DRUGS Sucralfate Mechanism of action Pharmacokinetics Unwanted effects Prostaglandin Analogues Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF DYSPEPSIA, PEPTIC ULCER AND GASTROOESOPHAGEAL REFLUX DISEASE NON-ULCER DYSPEPSIA CONFIRMED PEPTIC ULCERATION ERADICATION OF HELICOBACTER PYLORI INFECTION BLEEDING FROM PEPTIC ULCERS PEPTIC ULCERATION ASSOCIATED WITH NONSTEROIDAL ANTIINFLAMMATORY DRUGS GASTROOESOPHAGEAL REFLUX DISEASE OESOPHAGEAL SPASM SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 34 - Inflammatory Bowel Disease Inflammatory Bowel Disease DRUGS FOR INFLAMMATORY BOWEL DISEASE AMINOSALICYLATES Mechanism of Action and Effects Pharmacokinetics Unwanted Effects CORTICOSTEROIDS CYTOKINE MODULATORS (TUMOUR NECROSIS FACTOR ALPHA INHIBITORS) Mechanism of Action and Uses ANTILYMPHOCYTE ANTIBODY Mechanism of Action and Uses IMMUNOSUPPRESSANTS ANTIBACTERIALS MANAGEMENT OF INFLAMMATORY BOWEL DISEASE ULCERATIVE COLITIS CROHN’S DISEASE MICROSCOPIC COLITIS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 35 - Constipation, Diarrhoea and Irritable Bowel Syndrome CONSTIPATION LAXATIVES Bulk-Forming Laxatives Osmotic Laxatives Irritant and Stimulant Laxatives Faecal Softeners MANAGEMENT OF CONSTIPATION DIARRHOEA DRUGS FOR TREATING DIARRHOEA Opioids Adsorbent and Bulk-Forming Agents MANAGEMENT OF DIARRHOEA Clostridioides difficile-Associated Diarrhoea IRRITABLE BOWEL SYNDROME DRUGS FOR TREATING IRRITABLE BOWEL SYNDROME Antimuscarinic Drugs Mechanism of action Pharmacokinetics Unwanted effects Other Antispasmodic Agents Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF IRRITABLE BOWEL SYNDROME SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 36 - Liver Disease ACUTE LIVER FAILURE MANAGEMENT OF ACUTE AND SUBACUTE LIVER FAILURE CHRONIC LIVER DISEASE AND LIVER CIRRHOSIS AUTOIMMUNE HEPATITIS MANAGEMENT OF AUTOIMMUNE HEPATITIS PRIMARY BILIARY CHOLANGITIS MANAGEMENT OF PRIMARY BILIARY CHOLANGITIS CHRONIC VIRAL HEPATITIS DRUGS FOR TREATMENT OF CHRONIC VIRAL HEPATITIS Nucleoside and Nucleotide Analogues Mechanism of action and uses Resistance Pharmacokinetics Unwanted effects Direct-Acting Antivirals: HCV Protease Inhibitors Mechanism of action Resistance Unwanted effects Direct-Acting Antivirals: Nonstructural Protein NS5A and NS5B Inhibitors Mechanism of action Resistance Unwanted effects Interferon Alfa Mechanism of action and effects Pharmacokinetics Unwanted effects MANAGEMENT OF CHRONIC VIRAL HEPATITIS Chronic Hepatitis B Infection Chronic Hepatitis C Infection COMPLICATIONS OF DECOMPENSATED CIRRHOSIS CHRONIC HEPATIC ENCEPHALOPATHY Management of Chronic Hepatic Encephalopathy VARICEAL HAEMORRHAGE Management of Bleeding Gastrooesophageal Varices Prevention of Variceal Bleeding and Rebleeding ASCITES IN CHRONIC LIVER DISEASE Management of Ascites SELF-ASSESSMENT ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 37 - Obesity PATHOGENESIS OF OBESITY DRUGS FOR TREATMENT OF OBESITY DRUGS ACTING ON THE GASTROINTESTINAL TRACT Mechanism of Action Pharmacokinetics Unwanted Effects CENTRALLY ACTING APPETITE SUPPRESSANTS MANAGEMENT OF OBESITY SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWER FURTHER READING 38 - The Immune Response and Immunosuppressant Drugs BIOLOGICAL BASIS OF THE IMMUNE RESPONSE INNATE IMMUNITY ADAPTIVE IMMUNITY Cell-Mediated Immunity Humoral Immunity UNWANTED IMMUNE REACTIONS Hypersensitivity Reactions Type 1 (allergy, immediate) Type 2 (cytotoxic, antibody-dependent) Type 3 (immune complex disease) Type 4 (cell-mediated, delayed-type hypersensitivity) Autoimmunity Blood Transfusion and Transplant Rejection IMMUNOSUPPRESSANT DRUGS CORTICOSTEROIDS CALCINEURIN INHIBITORS Ciclosporin Mechanism of action Pharmacokinetics Unwanted effects Tacrolimus Mechanism of action and effects Pharmacokinetics Unwanted effects MECHANISTIC TARGET OF RAPAMYCIN (mTOR) INHIBITORS Mechanism of action and effects Pharmacokinetics Unwanted effects ANTIPROLIFERATIVE AGENTS Azathioprine Mechanism of action Pharmacokinetics Unwanted effects Cyclophosphamide Mycophenolate Mofetil and Mycophenolic Acid Mechanism of action and effects Pharmacokinetics Unwanted effects FOLIC ACID ANTAGONIST Mechanism of action and uses Pharmacokinetics Unwanted effects INTERLEUKIN-2 RECEPTOR ANTIBODIES Mechanism of action and uses Pharmacokinetics Unwanted effects SELECTIVE CO-STIMULATION BLOCKER Mechanism of action and uses Pharmacokinetics Unwanted effects COMPLEMENT BLOCKERS Mechanism of action and uses Pharmacokinetics Unwanted effects ANTITHYMOCYTE GLOBULIN Mechanism of action and uses Pharmacokinetics Unwanted effects IgG DEGRADING ENZYME Mechanism of action and uses Pharmacokinetics Unwanted effects IMMUNOSUPPRESSION IN INFLAMMATORY AND AUTOIMMUNE DISEASE IMMUNOSUPPRESSION IN ORGAN TRANSPLANTATION LONG-TERM EFFECTS OF IMMUNOSUPPRESSION SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 39 - Antihistamines and Allergic Disease ATOPY, ALLERGIC DISORDERS AND ANAPHYLAXIS HISTAMINE AS AN AUTACOID IN HOST DEFENCE HISTAMINE H1 RECEPTOR ANTAGONISTS (ANTIHISTAMINES) MECHANISMS OF ACTION AND EFFECTS PHARMACOKINETICS UNWANTED EFFECTS MANAGEMENT OF ALLERGIC DISORDERS ANAPHYLAXIS SEASONAL AND PERENNIAL RHINITIS URTICARIA AND ANGIOEDEMA ALLERGIC CONJUNCTIVITIS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 40 - Diabetes Mellitus CONTROL OF BLOOD GLUCOSE REGULATION OF INSULIN SECRETION AND EFFECTS OF INSULIN REGULATION OF GLUCAGON SECRETION AND EFFECTS OF GLUCAGON DIABETES MELLITUS TYPE 1 DIABETES MELLITUS TYPE 2 DIABETES MELLITUS INSULIN AND INSULIN ANALOGUES FOR TREATMENT OF DIABETES MELLITUS NATURAL INSULIN FORMULATIONS Pharmacokinetics Unwanted Effects INSULIN ANALOGUES Mechanism of Action and Effects Rapid-acting insulin analogues Long-acting insulin analogues Pharmacokinetics Unwanted Effects THERAPEUTIC REGIMENS FOR INSULIN AND INSULIN ANALOGUES OTHER PARENTERAL GLUCOSE-LOWERING DRUGS GLUCAGON-LIKE PEPTIDE-1 RECEPTOR AGONISTS Mechanism of Action Pharmacokinetics Unwanted Effects ORAL GLUCOSE-LOWERING DRUGS SULFONYLUREAS Mechanism of Action Pharmacokinetics Unwanted Effects MEGLITINIDES Mechanism of Action Pharmacokinetics Unwanted Effects BIGUANIDE Mechanism of Action and Effects Pharmacokinetics Unwanted Effects THIAZOLIDINEDIONE Mechanisms of Action and Effects Pharmacokinetics Unwanted Effects DIPEPTIDYL PEPTIDASE-4 INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects SODIUM-GLUCOSE COTRANSPORTER 2 INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects GLUCOSIDASE INHIBITOR Mechanism of Action and Effects Pharmacokinetics Unwanted Effects DRUGS TO INCREASE PLASMA GLUCOSE LEVELS GLUCAGON Mechanism of Action and Use Pharmacokinetics Unwanted Effects MANAGEMENT OF TYPE 1 DIABETES MELLITUS MANAGEMENT OF TYPE 1 DIABETES MELLITUS IN SPECIAL SITUATIONS MANAGEMENT OF TYPE 2 DIABETES MELLITUS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 41 - The Thyroid and Control of Metabolic Rate THYROID FUNCTION THYROID HORMONES THYROTOXICOSIS DRUGS FOR TREATMENT OF THYROTOXICOSIS Thionamides Mechanism of action Pharmacokinetics Unwanted effects MANAGEMENT OF THYROTOXICOSIS Graves’ Disease Toxic Nodular Goitre and Toxic Adenoma Amiodarone-Induced Thyrotoxicosis Thyroiditis HYPOTHYROIDISM MANAGEMENT OF HYPOTHYROIDISM SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 42 - Calcium Metabolism and Metabolic Bone Disease PHYSIOLOGY OF BONE TURNOVER PLASMA CALCIUM HOMEOSTASIS PARATHYROID HORMONE AND CALCIUM HOMEOSTASIS VITAMIN D AND CALCIUM HOMEOSTASIS CALCITONIN AND CALCIUM HOMEOSTASIS HYPERCALCAEMIA ANTIRESORPTIVE DRUGS FOR TREATING HYPERCALCAEMIA Bisphosphonates Mechanisms of action and effects Pharmacokinetics Unwanted effects Salmon Calcitonin (Salcatonin) Mechanism of action and effects Pharmacokinetics Unwanted effects Cinacalcet Mechanism of action and effects Pharmacokinetics Unwanted effects TREATMENT OF HYPERCALCAEMIA HYPOCALCAEMIA DRUGS FOR HYPOCALCAEMIA Vitamin D compounds Mechanism of action Pharmacokinetics Unwanted effects TREATMENT OF HYPOCALCAEMIA METABOLIC BONE DISEASE OSTEOMALACIA AND VITAMIN D DEFICIENCY RENAL BONE DISEASE OSTEOPOROSIS Drugs for Treating Osteoporosis Bisphosphonates Denosumab Mechanism of action Pharmacokinetics Unwanted effects Raloxifene Mechanism of action Pharmacokinetics Unwanted effects Prevention of Osteoporosis Management of established osteoporosis and fragility fractures PAGET’S DISEASE OF BONE SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 43 - Pituitary and Hypothalamic Hormones ANTERIOR PITUITARY AND RELATED HYPOTHALAMIC HORMONES GROWTH HORMONE Growth Hormone for Therapeutic Use Pharmacokinetics Unwanted effects Acromegaly Drugs for Acromegaly Somatostatin analogues Mechanisms of action and uses Pharmacokinetics Unwanted effects Growth hormone receptor antagonist Mechanism of action Pharmacokinetics Unwanted effects Dopamine receptor agonists Treatment of Acromegaly ADRENOCORTICOTROPIC HORMONE Adrenocorticotropic Hormone for Therapeutic Use Pharmacokinetics Unwanted effects Uses of tetracosactide PROLACTIN Hyperprolactinaemia GONADOTROPIN-RELEASING HORMONE GnRH-Related Products for Therapeutic Use Synthetic GnRH (gonadorelin) Gonadorelin analogues Mechanism of action Clinical uses of gonadorelin analogues Pharmacokinetics Unwanted effects GnRH receptor antagonists Mechanism of action and uses Pharmacokinetics Unwanted effects GONADOTROPINS Gonadotropins for Therapeutic Use Unwanted effects Clinical Uses of Gonadotropins INFERTILITY Drugs for Inducing Ovulation Clomifene Mechanism of action and use Pharmacokinetics Unwanted effects Drug Treatment of Female Infertility Preparation for Assisted Reproduction (In Vitro Fertilisation) Polycystic Ovary Syndrome Management of polycystic ovary syndrome POSTERIOR PITUITARY HORMONES VASOPRESSIN (ANTIDIURETIC HORMONE) Vasopressin Analogues Pharmacokinetics Unwanted effects Clinical Uses of Vasopressin and its Analogues Diabetes Insipidus Management of diabetes insipidus Syndrome of Inappropriate Antidiuresis Vasopressin V2 receptor antagonist Mechanism of action and uses Pharmacokinetics Unwanted effects Treatment of syndrome of inappropriate antidiuresis OXYTOCIN HYPOPITUITARISM SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 44 - Corticosteroids (Glucocorticoids and Mineralocorticoids) CORTICOSTEROID HORMONES CONTROL OF CORTICOSTEROID HORMONE SYNTHESIS AND RELEASE MODE OF ACTION OF CORTICOSTEROID HORMONES GLUCOCORTICOIDS ACTIONS OF GLUCOCORTICOIDS Immunosuppressant and Antiinflammatory Actions Antiinflammatory Effects Metabolic Effects Effects on Bone Metabolism Central Nervous System Effects Mineralocorticoid Effects PHARMACOKINETICS OF GLUCOCORTICOIDS Physiological Replacement Therapy for Corticosteroid Deficiency CLINICAL USES OF THERAPEUTIC DOSES OF SYSTEMICALLY ADMINISTERED GLUCOCORTICOIDS CLINICAL USES OF THERAPEUTIC DOSES OF TOPICALLY ADMINISTERED GLUCOCORTICOIDS UNWANTED EFFECTS OF GLUCOCORTICOIDS Cessation of Glucocorticoid Therapy CUSHING’S SYNDROME MINERALOCORTICOIDS FLUDROCORTISONE Pharmacokinetics Unwanted Effects Clinical Uses of Fludrocortisone PRIMARY HYPERALDOSTERONISM (CONN’S SYNDROME) SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTION CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWER CASE-BASED ANSWERS FURTHER READING 45 - Female Reproduction PHYSIOLOGY OF THE MENSTRUAL CYCLE PHYSIOLOGY OF PREGNANCY CELLULAR ACTION OF OESTROGENS AND PROGESTOGENS STEROIDAL CONTRACEPTIVES MECHANISMS OF HORMONAL CONTRACEPTION THE COMBINED HORMONAL CONTRACEPTIVE Monophasic Combined Contraceptive Preparations Biphasic and Triphasic Combined Contraceptive Preparations Tricycling, Continuous and Tailored Regimens for Combined Hormonal Contraceptives PROGESTOGEN-ONLY CONTRACEPTIVES Oral Progestogen-Only Contraceptives Parenteral Progestogen-Only Contraceptives Intrauterine Progestogen-Only Device EFFICACY OF HORMONAL CONTRACEPTION EMERGENCY CONTRACEPTION PHARMACOKINETICS OF CONTRACEPTIVE SEX STEROIDS Drug Interactions UNWANTED EFFECTS OF CONTRACEPTIVE SEX STEROIDS NON-CONTRACEPTIVE USES OF HORMONAL CONTRACEPTIVES Menorrhagia Primary Dysmenorrhoea Premenstrual Syndrome Endometriosis THE MENOPAUSE HORMONE-REPLACEMENT THERAPY AND RELATED DRUGS Oral Oestrogens and Progestogens Subcutaneous Oestrogen Implants Transdermal Oestrogen and Oestrogen with Progestogen Vaginal Oestrogen Tibolone Pharmacokinetics Unwanted effects MANAGEMENT OF MENOPAUSAL SYMPTOMS PREGNANCY AND LABOUR THE ONSET AND INDUCTION OF LABOUR Prostaglandins Oxytocin Oestradiol/Oestriol Progesterone STAGES OF LABOUR MYOMETRIAL RELAXANTS (TOCOLYTICS) AND PRETERM LABOUR Calcium Channel Blockers Atosiban Mechanism of action Pharmacokinetics Unwanted effects Beta2-Adrenoceptor Agonists Management of Preterm Labour DRUGS FOR INDUCING AND AUGMENTING LABOUR Dinoprostone Unwanted effects Oxytocin Pharmacological Induction and Augmentation of Labour PAIN RELIEF IN LABOUR POSTPARTUM HAEMORRHAGE Ergometrine Maleate Pharmacokinetics Unwanted effects Prevention and Management of Postpartum Haemorrhage MEDICAL ABORTION Mifepristone Mechanism of action and uses Pharmacokinetics Unwanted effects Prostaglandin Derivatives Induction of Medical Abortion SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 46 - Androgens, Antiandrogens and Anabolic Steroids ANDROGENS AND ANABOLIC STEROIDS MALE HYPOGONADISM FEMALE ANDROGEN DEFICIENCY THERAPEUTIC MALE SEX HORMONES Actions of Testosterone Pharmacokinetics Unwanted Effects Clinical Uses of Testosterone DANAZOL Mechanism of Action Pharmacokinetics Unwanted Effects Clinical Uses of Danazol ANABOLIC STEROIDS ANTIANDROGENS BICALUTAMIDE AND FLUTAMIDE Mechanism of Action Pharmacokinetics Unwanted Effects CYPROTERONE ACETATE Mechanism of Action Pharmacokinetics Unwanted Effects CLINICAL USES OF ANTIANDROGENS 5α-REDUCTASE INHIBITORS Mechanism of Action and Effects SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 47 - Anaemia and Haematopoietic Colony-Stimulating Factors ANAEMIA IRON Iron Deficiency Therapeutic Iron Preparations Oral iron Unwanted effects Parenteral iron Unwanted effects Therapeutic Use of Iron FOLIC ACID Folate Deficiency Therapeutic Use of Folic Acid VITAMIN B12 Vitamin B12 Deficiency Therapeutic Use of Vitamin B12 ERYTHROPOIETIN Pharmacokinetics Unwanted Effects Therapeutic Uses of Epoetin DRUG TREATMENT IN OTHER ANAEMIAS Aplastic Anaemia Sideroblastic Anaemia Autoimmune Haemolytic Anaemia β-Thalassaemia Major Sickle Cell Anaemia DRUGS AS A CAUSE OF ANAEMIA NEUTROPENIA DRUGS FOR NEUTROPENIA Granulocyte Colony-Stimulating Factors Pharmacokinetics Unwanted effects Therapeutic Use of Colony-Stimulating Factors SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 48 - Lipid Disorders LIPIDS AND LIPOPROTEINS CHOLESTEROL AND TRIGLYCERIDES LIPOPROTEINS PROCESSING OF LIPIDS ABSORBED FROM THE GUT PLASMA TRANSPORT AND LIVER PROCESSING OF LIPIDS FORMATION OF ATHEROMA DRUGS FOR HYPERLIPIDAEMIAS 3-HYDROXY-3-METHYLGLUTARYL-COENZYME A REDUCTASE INHIBITORS (STATINS) Mechanism of Action and Effects Pharmacokinetics Unwanted Effects SPECIFIC CHOLESTEROL ABSORPTION INHIBITOR Mechanism of Action Pharmacokinetics Unwanted Effects BILE ACID SEQUESTRANTS Mechanism of Action Unwanted Effects FIBRATES Mechanism of Action Pharmacokinetics Unwanted Effects ADENOSINE TRIPHOSPHATE CITRATE LYASE (ACL) INHIBITOR Mechanism of Action Pharmacokinetics Unwanted Effects NICOTINIC ACID AND DERIVATIVES Mechanism of Action Pharmacokinetics Unwanted Effects OMEGA-3 FATTY ACIDS Unwanted Effects PROPROTEIN CONVERTASE SUBTILISIN/KEXIN (PCSK) TYPE 9 INHIBITORS Mechanism of Action Pharmacokinetics Unwanted Effects SMALL INTERFERING RIBONUCLEIC ACID (siRNA) Mechanism of Action Pharmacokinetics Unwanted Effects MANAGEMENT OF HYPERLIPIDAEMIAS Lipid Lowering for Primary Prevention of Cardiovascular Disease Secondary Prevention of Cardiovascular Disease Mechanisms of Prevention of Coronary Events by Lipid-Lowering Drugs Management of Hypertriglyceridaemia SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 49 - Skin Disorders VEHICLES FOR TOPICAL SKIN APPLICATIONS ATOPIC AND CONTACT DERMATITIS ATOPIC ECZEMA (ATOPIC DERMATITIS) CONTACT DERMATITIS OTHER TYPES OF DERMATITIS TREATMENT OF ATOPIC ECZEMA TREATMENT OF CONTACT DERMATITIS PSORIASIS DRUGS FOR TREATMENT OF PSORIASIS Topical Therapy Emollients Keratolytics Vitamin D analogues Topical retinoid Topical calcineurin inhibitors Dithranol Coal tar preparations Phototherapy Topical corticosteroid preparations Systemic Treatments Methotrexate Retinoids Ciclosporin Biologic agents Dimethyl fumarate CHOICE OF TREATMENT FOR PSORIASIS ACNE VULGARIS DRUGS FOR TREATMENT OF ACNE Topical Treatments Systemic Treatments CHOICE OF TREATMENT FOR ACNE SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 50 - The Eye Regulation of visual acuity, pupil size and aqueous humour Accommodation Pupil Size Drainage of Aqueous Humour TOPICAL APPLICATION OF DRUGS TO THE EYE MYDRIATIC AND CYCLOPLEGIC DRUGS ANTIMUSCARINIC DRUGS SYMPATHOMIMETICS GLAUCOMA DRUGS FOR GLAUCOMA Prostaglandin Analogues β-Adrenoceptor Antagonists Sympathomimetics Carbonic Anhydrase Inhibitors Rho Kinase (ROCK) Inhibitor Miotic Drugs (Muscarinic Agonists) TREATMENT OF GLAUCOMA OTHER DRUGS ADMINISTERED TOPICALLY TO THE EYE ANTIBACTERIAL AGENTS ANTIVIRAL AGENTS CORTICOSTEROIDS ANTIALLERGIC AGENTS LOCAL ANAESTHETICS NONSTEROIDAL ANTIINFLAMMATORY DRUGS DRY EYE SYNDROME AGE-RELATED MACULAR DEGENERATION TREATMENT OF AGE-RELATED MACULAR DEGENERATION DIABETIC RETINOPATHY TREATMENT OF DIABETIC RETINOPATHY SELF-ASSESSMENT TRUE/FALSE QUESTIONS EXTENDED-MATCHING-ITEM QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS EXTENDED-MATCHING-ITEM ANSWERS CASE-BASED ANSWERS FURTHER READING 51 - Drugs for Infections ~ BACTERIAL INFECTIONS CLASSIFICATION OF ANTIBACTERIAL DRUGS ANTIMICROBIAL RESISTANCE ANTIBACTERIAL DRUG RESISTANCE Spontaneous Mutation Conjugation Transduction Transformation ANTIBACTERIAL DRUGS Drugs Affecting the Cell Wall: β-Lactam Antibacterials Mechanism of action of β-lactam antibacterials Penicillins Spectrum of activity Resistance Pharmacokinetics Unwanted effects Cephalosporins Spectrum of activity Resistance Pharmacokinetics Unwanted effects Monobactams Carbapenems Other Drugs Affecting the Cell Wall Glycopeptides Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Daptomycin Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Polymyxins Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Drugs Affecting Bacterial Nucleic Acids Quinolones (fluoroquinolones) Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Metronidazole and tinidazole Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Nitrofurantoin Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Macrocyclic antibiotic Mechanism of action and use Spectrum of activity Resistance Pharmacokinetics Unwanted effects Drugs Affecting Bacterial Protein Synthesis Macrolides Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Aminoglycosides Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Tetracyclines Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Tigecycline Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Chloramphenicol Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Lincosamides Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Fusidic acid Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Oxazolidinones Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Drugs Affecting Bacterial Metabolism Sulfonamides Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Trimethoprim Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Drugs Used for Tuberculosis Rifamycins Mechanism of action and spectrum of activity Resistance Pharmacokinetics Unwanted effects Isoniazid Mechanism of action Resistance Pharmacokinetics Unwanted effects Pyrazinamide Mechanism of action Resistance Pharmacokinetics Unwanted effects Ethambutol Mechanism of action Resistance Pharmacokinetics Unwanted effects Other drugs used in the treatment of tuberculosis Drugs Used for Leprosy Dapsone Mechanism of action and use Resistance Pharmacokinetics Unwanted effects Clofazimine Mechanism of action and use Pharmacokinetics Unwanted effects PRINCIPLES OF ANTIBACTERIAL THERAPY Empirical Treatment Spectrum of Antibacterial Activity Combination Therapy Bactericidal Versus Bacteriostatic Drugs Site of Infection Mode of Administration Duration of Therapy Chemoprophylaxis TREATMENT OF SELECTED BACTERIAL INFECTIONS Upper Respiratory Tract Infections Sinusitis and Otitis Media Lower Respiratory Tract Infections Acute bronchitis Pneumonia Suppurative lung disease Urinary Tract Infections Gastrointestinal Infection Biliary Tract Infection Osteomyelitis Septic Arthritis Cellulitis Sepsis Infective Endocarditis Meningitis Tuberculosis FUNGAL INFECTIONS ANTIFUNGAL DRUGS Drugs That Impair Fungal Cell Membrane Barrier Function Polyenes Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Drugs That Inhibit Fungal Cell Membrane or Cell Wall Synthesis Imidazoles Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Triazoles Mechanism of action and spectrum of activity Resistance Pharmacokinetics Unwanted effects Terbinafine Mechanism of action and use Resistance Pharmacokinetics Unwanted effects Echinocandins Mechanism of action Resistance Pharmacokinetics Unwanted effects Drugs That Inhibit Macromolecule Synthesis Flucytosine Mechanism of action and use Resistance Pharmacokinetics Unwanted effects Drugs That Interact with Microtubules Griseofulvin Mechanism of action and use Resistance Pharmacokinetics Unwanted effects TREATMENT OF SPECIFIC FUNGAL INFECTIONS Aspergillus Candida Cryptococcus Skin and Nail Infections Prophylaxis of Fungal Infection in Immunocompromised Individuals VIRAL INFECTIONS ANTIVIRAL DRUGS Drugs Active Against HIV Nucleoside/nucleotide reverse transcriptase inhibitors Mechanism of action Resistance Pharmacokinetics Unwanted effects Non-nucleoside reverse transcriptase inhibitors Mechanism of action Resistance Pharmacokinetics Unwanted effects HIV protease inhibitors Mechanism of action Resistance Pharmacokinetics Unwanted effects HIV fusion-entry inhibitor Mechanism of action Resistance Pharmacokinetics Unwanted effects Chemokine (C-C motif) receptor 5 co-receptor antagonist Mechanism of action Resistance Pharmacokinetics Unwanted effects HIV integrase inhibitors Mechanism of action Resistance Pharmacokinetics Unwanted effects Drugs for Herpesvirus and Cytomegalovirus Infections Nucleoside inhibitors of viral DNA polymerase Mechanism of action Spectrum of activity Resistance Pharmacokinetics Unwanted effects Non-nucleoside inhibitors of viral DNA polymerase Mechanism of action Resistance Pharmacokinetics Unwanted effects Drugs for Treating Hepatitis Viruses Drugs for Treating Influenza Virus M2 ion channel inhibitors Neuraminidase inhibitors Mechanism of action Pharmacokinetics Unwanted effects Cap-dependent endonuclease inhibitor Mechanism of action Pharmacokinetics Unwanted effects Drugs for Treating Respiratory Syncytial Virus Palivizumab Mechanism of action and use Pharmacokinetics Unwanted effects Drug for Treating Coronaviruses Nucleotide analogue Mechanism of action Pharmacokinetics Unwanted effects Other Drugs for Viral Infections Immunomodulators Interferon alpha Baricitinib IL-6 pathway inhibitors Corticosteroids TREATMENT OF SPECIFIC VIRAL INFECTIONS HIV Infection Varicella Zoster Virus Infections Herpes Simplex Virus Infections Cytomegalovirus Infection Influenza Coronavirus Disease 2019 (COVID-19) Viral Hepatitis Respiratory Syncytial Virus PROTOZOAL INFECTIONS MALARIA Antimalarial Drugs Chloroquine Mechanism of action and resistance Pharmacokinetics Unwanted effects Mefloquine Mechanism of action and resistance Pharmacokinetics Unwanted effects Primaquine Mechanism of action and resistance Pharmacokinetics Unwanted effects Quinine Mechanism of action and resistance Pharmacokinetics Unwanted effects Pyrimethamine with sulfadoxine Mechanism of action and resistance Pharmacokinetics Unwanted effects Proguanil Mechanism of action and resistance Pharmacokinetics Unwanted effects Artemether with lumefantrine Mechanism of action and resistance Pharmacokinetics Unwanted effects Treatment of Malaria Prophylaxis Against Malaria OTHER PROTOZOAL INFECTIONS Atovaquone Mechanism of action and uses Pharmacokinetics Unwanted effects Pentamidine Mechanism of action and uses Pharmacokinetics Unwanted effects Sodium Stibogluconate Mechanism of action and use Pharmacokinetics Unwanted effects HELMINTHIC INFECTIONS ANTIHELMINTHIC DRUGS Ivermectin Mechanism of action and use Pharmacokinetics Unwanted effects Diethylcarbamazine Mechanism of action and use Pharmacokinetics Unwanted effects Benzimidazoles Mechanism of action and uses Pharmacokinetics Unwanted effects Niclosamide Mechanism of action and use Pharmacokinetics Unwanted effects Praziquantel Mechanism of action and uses Pharmacokinetics Unwanted effects SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS Case 1 answers Case 2 answers Case 3 answers Case 4 answers FURTHER READING Antibacterial Drugs Antifungal Drugs Antiviral Drugs Antiprotozoal Drugs Antihelminthic Drugs 52 - Drugs for Cancer ~ THE BIOLOGY OF CANCER CYTOTOXIC ANTICANCER DRUGS MECHANISMS OF ACTION RESISTANCE DRUG COMBINATIONS UNWANTED EFFECTS Gastrointestinal Tract Bone Marrow Hair Follicle Cells Reproductive Organs Growing Tissues in Children Extravasation of Intravenous Drug Tumour Lysis Syndrome Peripheral Neuropathy SPECIFIC CYTOTOXIC ANTICANCER DRUGS DRUGS AFFECTING NUCLEIC ACID FUNCTION Alkylating Drugs Mechanism of action and uses Pharmacokinetics Unwanted effects Cytotoxic Antibiotics Mechanisms of action and uses Pharmacokinetics Unwanted effects Platinum Compounds Mechanism of action and uses Pharmacokinetics Unwanted effects Antimetabolites Folic acid antagonists Mechanism of action and uses. Pharmacokinetics. Unwanted effects Base analogue antimetabolites Mechanism of action and uses. Pharmacokinetics. Unwanted effects DRUGS THAT INHIBIT MITOSIS Vinca Alkaloids Mechanism of action and uses Pharmacokinetics Unwanted effects Taxanes Mechanism of action and uses Pharmacokinetics Unwanted effects Camptothecin Analogues (Topoisomerase I Inhibitors) Mechanism of action and uses Pharmacokinetics Unwanted effects Podophyllotoxins (Topoisomerase II Inhibitors) Mechanism of action and uses Pharmacokinetics Unwanted effects TARGETED ANTICANCER DRUGS DRUGS AFFECTING TYROSINE KINASES AND OTHER PROTEIN KINASES Growth Factor Inhibitors Mechanism of action and uses Protein Kinase Inhibitors Pharmacokinetics Unwanted effects POLY ADP RIBOSE POLYMERASE (PARP) INHIBITORS Mechanism of action Pharmacokinetics Unwanted effects PROTEASOME INHIBITORS Mechanism of action Pharmacokinetics Unwanted effects B-CELL LYMPHOMA-2 (Bcl-2) INHIBITORS Mechanism of action Pharmacokinetics Unwanted effects HEDGEHOG PATHWAY INHIBITORS Mechanism of action Pharmacokinetics Unwanted effects MISCELLANEOUS ANTICANCER DRUGS HORMONAL ANTICANCER DRUGS Glucocorticoids Oestrogens Progestogens Oestrogen Receptor Antagonists Aromatase Inhibitors Androgen Receptor Antagonists Gonadorelin Analogues IMMUNE CHECKPOINT INHIBITORS Mechanism of action Pharmacokinetics Unwanted effects OTHER IMMUNOTHERAPY FOR SPECIFIC TUMOURS CLINICAL USES OF ANTICANCER DRUGS ANTICANCER DRUG THERAPY FOR SPECIFIC MALIGNANCIES OESOPHAGEAL CANCER GASTRIC CANCER PANCREATIC CANCER COLORECTAL CANCER LUNG CANCER MELANOMA RENAL CANCER BLADDER CANCER PROSTATE CANCER TESTICULAR CANCER OVARIAN CANCER CERVICAL CANCER ENDOMETRIAL CANCER BREAST CANCER Oestrogen Receptor-Positive Tumours Oestrogen Receptor-Negative Tumours ACUTE MYELOID LEUKAEMIAS ACUTE LYMPHOBLASTIC LEUKAEMIA CHRONIC MYELOID LEUKAEMIA CHRONIC LYMPHOCYTIC LEUKAEMIA MALIGNANT LYMPHOMAS MULTIPLE MYELOMA SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE-BEST-ANSWER (OBA) QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS CASE-BASED ANSWERS FURTHER READING 53 - Drug Toxicity and Overdose ~ DRUG TOXICITY AND ADVERSE EFFECTS TYPES OF UNWANTED EFFECT PHARMACOLOGICAL TOXICITY BIOCHEMICAL TOXICITY Paracetamol Cyclophosphamide Isoniazid Spironolactone Aromatic Amines and Nitrites Methaemoglobinaemia Haemolysis IMMUNOLOGICAL TOXICITY THE YELLOW CARD SCHEME SELF-POISONING AND DRUG OVERDOSE MANAGEMENT PRINCIPLES MANAGING ADVERSE EFFECTS Immediate Measures Supportive Measures Cardiac or respiratory arrest Hypotension Arrhythmias Seizures Renal failure Hepatic failure Impaired temperature regulation REDUCING TOXICITY Prevention of Absorption of Poisons Activated charcoal Elimination of Poisons Multiple-dose activated charcoal (MDAC) Renal elimination Haemodialysis and haemoperfusion Specific Antidotes Competitive receptor antagonists Chelating agents Compounds that affect drug metabolism Antibodies SOME COMMON SPECIFIC POISONINGS Paracetamol Salicylates Antidepressants Opioid Analgesics Beta-Adrenoceptor Antagonists Ecstasy SELF-ASSESSMENT TRUE/FALSE QUESTIONS CASE-BASED QUESTIONS ANSWERS TRUE/FALSE ANSWERS CASE-BASED ANSWERS FURTHER READING 54 - Substance Abuse and Dependence THE BIOLOGICAL BASIS OF DEPENDENCE THE MESOCORTICOLIMBIC REWARD PATHWAY DRUGS OF ABUSE PSYCHOMOTOR STIMULANTS Cocaine Mechanism of action and effects Pharmacokinetics Management of cocaine dependence Amfetamine and Derivatives Mechanism of action and effects Pharmacokinetics Management of amfetamine dependence Cathinone Stimulants Mechanism of action Pharmacokinetics Nicotine and Tobacco Mechanism of action Effects of nicotine and tobacco Respiratory effects Cardiovascular effects Psychological effects Other effects Pharmacokinetics of nicotine Dependence on and withdrawal from nicotine Nicotine replacement therapy Bupropion Varenicline PSYCHOTOMIMETIC AGENTS Hallucinogens Mechanism of action and effects Pharmacokinetics Cannabis Mechanism of action and effects Uses of cannabinoids Pharmacokinetics Dissociative Anaesthetics Mechanism of action and effects Pharmacokinetics CENTRAL NERVOUS SYSTEM DEPRESSANTS Alcohol (Ethyl Alcohol, Ethanol) Mechanism of action and effects Other effects of alcohol Cardiovascular effects Liver Other gastrointestinal consequences Sexual function Neuropsychiatric effects Carcinogenesis and teratogenesis Pharmacokinetics Alcohol abuse and dependence Gamma-Hydroxybutyric Acid Mechanism of action and effects Pharmacokinetics Inhaled Solvents NEW PSYCHOACTIVE SUBSTANCES CONTROLLED DRUGS SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE BEST ANSWER (OBA) QUESTIONS ANSWERS TRUE/FALSE ANSWERS OBA ANSWERS FURTHER READING 55 - Prescribing, Adherence and Information About Medicines ~ DUTIES OF THE PRESCRIBER GENERIC PRESCRIBING DOSAGE DOSE FREQUENCY AND TIMES OF ADMINISTRATION THE ROUTE OF ADMINISTRATION THE QUANTITY TO BE SUPPLIED OR THE DURATION OF THERAPY OTHER ITEMS ON A PRESCRIPTION ADHERENCE, CONCORDANCE AND COMPLIANCE INFORMING PEOPLE ABOUT THEIR MEDICINES RATIONAL PRESCRIBING THE PRESCRIBING SAFETY ASSESSMENT (PSA) FURTHER READING General prescribing Preparation for the UK Prescribing Safety Assessment (PSA) 56 - Drug Therapy in Special Situations PRESCRIBING IN PREGNANCY PHARMACOKINETICS IN PREGNANCY DRUGS AND BREASTFEEDING PHARMACOKINETICS IN LACTATION PRESCRIBING FOR CHILDREN PHARMACOKINETICS IN NEONATES AND CHILDREN Absorption Distribution Metabolism Renal Elimination PRESCRIBING FOR OLDER PEOPLE PHARMACOKINETICS IN OLDER PEOPLE Absorption and Distribution in Older People Metabolism in Older People Renal Elimination in Older People PRESCRIBING IN RENAL FAILURE PHARMACOKINETICS IN RENAL FAILURE PRESCRIBING IN LIVER DISEASE PHARMACOKINETICS IN LIVER DISEASE PRESCRIBING IN PALLIATIVE CARE PAIN NAUSEA AND VOMITING ANOREXIA/CACHEXIA/FATIGUE SYNDROME CONSTIPATION BREATHLESSNESS HICCUPS CONTINUOUS SUBCUTANEOUS INFUSIONS DRUG INTERACTIONS PHARMACODYNAMIC INTERACTIONS PHARMACOKINETIC INTERACTIONS Absorption Distribution Metabolism Excretion SELF-ASSESSMENT TRUE/FALSE QUESTIONS ONE BEST ANSWER (OBA) QUESTION ANSWERS TRUE/FALSE ANSWERS OBA ANSWER FURTHER READING Index IBC
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