Additional Information
Book Details
Abstract
Medical Pharmacology & Therapeutics, now in its fifth edition, offers medical students all they need to know to become safe and effective prescribers. It forms a complete, integrated resource for basic pharmaceutical science, pathophysiology, clinical pharmacology, and therapeutics.
The fifth edition has been extensively revised and updated throughout. Key features include:
- Clear, disease-based approach.
- Presentation of how drugs are used in clinical practice.
- Succinct explanations of the major pathogenic mechanisms of each disease and consequent clinical signs and symptoms.
- Comprehensive reviews of major drug classes relevant to each disease.
- Structured approach to the principles of disease management – outlining core principles of drug choice and planning a therapeutic regimen for common diseases.
- Quick-reference drug compendia illustrating key similarities and differences among all BNF-listed drugs in each class.
- Comes with free e-book on StudentConsult.
- New sections on key and evolving topics, including prescribing safety and pharmacovigilance.
- Updated figures to further clarify complex areas.
- Revised multiple-choice and case-based questions for self-assessment.
Table of Contents
| Section Title | Page | Action | Price |
|---|---|---|---|
| Front Cover | cover | ||
| Inside Front Cover | ifc1 | ||
| Half title page | i | ||
| Dedication | ii | ||
| Medical Pharmacology and Therapeutics | iii | ||
| Copyright Page | iv | ||
| Table Of Contents | v | ||
| Preface | vii | ||
| Drug dosage and nomenclature | ix | ||
| Drug Nomenclature | ix | ||
| Drug Dosages | ix | ||
| 1 General Principles | 1 | ||
| 1 Principles of pharmacology and mechanisms of drug action | 3 | ||
| Studying Pharmacology | 3 | ||
| Finding Drug Information | 4 | ||
| Receptors and Receptor-Mediated Mechanisms | 4 | ||
| Actions of Drugs at Binding Sites (Receptors) | 4 | ||
| Major Types of Receptors | 5 | ||
| Transmembrane ion channels | 5 | ||
| Seven-transmembrane receptors | 6 | ||
| The G-protein system | 6 | ||
| Second messenger systems | 7 | ||
| Cyclic nucleotide system | 7 | ||
| The phosphatidylinositol system | 7 | ||
| Protease-activated receptors | 8 | ||
| Enzyme-linked transmembrane receptors | 8 | ||
| Intracellular (nuclear) receptors | 9 | ||
| Other Sites of Drug Action | 12 | ||
| Properties of Receptors | 13 | ||
| Receptor binding | 13 | ||
| Receptor selectivity | 14 | ||
| Drug stereochemistry and activity | 15 | ||
| Receptor numbers | 15 | ||
| Properties of Drug Action | 15 | ||
| Dose–Response Relationships | 16 | ||
| Selectivity | 16 | ||
| Potency | 16 | ||
| Efficacy | 17 | ||
| Types of Drug Action | 17 | ||
| Agonists | 17 | ||
| Affinity and intrinsic activity | 17 | ||
| Spare receptors | 18 | ||
| Antagonists | 18 | ||
| Partial Agonists | 18 | ||
| Inverse Agonists | 18 | ||
| Allosteric Modulators | 19 | ||
| Enzyme Inhibitors and Activators | 19 | ||
| Nonspecific Actions | 19 | ||
| Physiological Antagonists | 19 | ||
| Tolerance to Drug Effects | 19 | ||
| Genetic Variation in Drug Responses | 20 | ||
| Summary | 21 | ||
| Self-Assessment | 21 | ||
| True/false questions | 21 | ||
| Answers | 22 | ||
| True/false answers | 22 | ||
| Further Reading | 22 | ||
| 2 Pharmacokinetics | 33 | ||
| The Biological Basis of Pharmacokinetics | 33 | ||
| General Considerations | 34 | ||
| Passage across membranes | 34 | ||
| Passive diffusion | 34 | ||
| Passage through membrane pores or ion channels | 35 | ||
| Carrier-mediated processes | 35 | ||
| Pinocytosis | 35 | ||
| Drug ionisation and membrane diffusion | 35 | ||
| Absorption | 38 | ||
| Absorption From the Gut | 38 | ||
| Drug structure | 38 | ||
| Drug formulation | 38 | ||
| Gastric emptying | 38 | ||
| First-pass metabolism | 38 | ||
| Intestinal lumen | 38 | ||
| Intestinal wall | 38 | ||
| Liver | 39 | ||
| Lung | 39 | ||
| Absorption From Other Routes | 39 | ||
| Percutaneous (transcutaneous) administration | 39 | ||
| Intradermal and subcutaneous injection | 39 | ||
| Intramuscular injection | 39 | ||
| Intranasal administration | 39 | ||
| Inhalation | 39 | ||
| Minor routes | 39 | ||
| Distribution | 39 | ||
| Reversible Protein Binding | 40 | ||
| Irreversible Protein Binding | 41 | ||
| Distribution to Specific Organs | 41 | ||
| Brain | 41 | ||
| Fetus | 42 | ||
| Elimination | 42 | ||
| Metabolism | 42 | ||
| Phase 1 | 42 | ||
| Phase 2 | 44 | ||
| Factors affecting drug metabolism: inducers and inhibitors | 45 | ||
| Excretion | 45 | ||
| Excretion via the urine | 46 | ||
| Glomerular filtration | 46 | ||
| Reabsorption | 46 | ||
| Tubular secretion | 46 | ||
| Excretion via the faeces | 47 | ||
| The Mathematical Basis of Pharmacokinetics | 48 | ||
| General Considerations | 48 | ||
| Zero-order reactions | 48 | ||
| First-order reactions | 48 | ||
| Absorption | 49 | ||
| Rate of Absorption | 49 | ||
| Extent of Absorption | 50 | ||
| Distribution | 51 | ||
| Rate of Distribution | 51 | ||
| Extent of Distribution | 52 | ||
| Elimination | 53 | ||
| Rate of Elimination | 53 | ||
| The activity of the organ of elimination | 53 | ||
| Reversible passage of drug from the blood into tissues | 53 | ||
| Extent of Elimination | 54 | ||
| Chronic Administration | 54 | ||
| Time to Reach Steady State | 55 | ||
| Plasma Concentration at Steady State | 55 | ||
| Oral Administration | 55 | ||
| Loading Dose | 56 | ||
| Pharmacokinetics of Biological Drugs | 56 | ||
| Genetic Variation and Pharmacokinetics | 56 | ||
| Self-Assessment | 57 | ||
| True/false questions | 57 | ||
| One-best-answer (OBA) questions | 57 | ||
| Descriptive question | 59 | ||
| Case-based questions | 59 | ||
| Case 1 | 59 | ||
| Case 2 | 60 | ||
| Case 3 | 60 | ||
| Answers | 60 | ||
| True/false answers | 60 | ||
| OBA answers | 60 | ||
| Descriptive answers | 61 | ||
| Case-based answers | 61 | ||
| Case 1 | 61 | ||
| Case 2 | 61 | ||
| Case 3 | 62 | ||
| Further Reading | 62 | ||
| 3 Drug discovery, safety and efficacy | 63 | ||
| Drug Discovery | 64 | ||
| Drug Approval | 65 | ||
| Safety | 65 | ||
| Quality | 66 | ||
| Efficacy | 66 | ||
| Establishing Safety and Efficacy | 66 | ||
| Preclinical Studies | 66 | ||
| Toxicity Testing | 66 | ||
| Clinical Trials: Phases I–III | 67 | ||
| Phase I studies | 67 | ||
| Phase II studies | 68 | ||
| Phase III studies | 68 | ||
| Postmarketing Surveillance: Phase IV (Pharmacovigilance) | 69 | ||
| Self-Assessment | 70 | ||
| One-best-answer (OBA) questions | 70 | ||
| Answers | 70 | ||
| OBA answers | 70 | ||
| Further Reading | 71 | ||
| 4 Neurotransmission and the peripheral autonomic nervous system | 73 | ||
| The Central and Peripheral Nervous Systems | 73 | ||
| Principles of Neurotransmission | 73 | ||
| Presynaptic Receptors and Modulation of Transmitter Release | 75 | ||
| The Peripheral Autonomic Nervous System | 75 | ||
| The Sympathetic Nervous System and Noradrenergic Transmission | 77 | ||
| Synthesis and Storage of Catecholamines: Noradrenaline, Adrenaline and Dopamine | 78 | ||
| Noradrenaline Release | 78 | ||
| Uptake and Metabolism of Released Noradrenaline | 80 | ||
| Monoamine oxidase | 80 | ||
| Catechol-O-methyltransferase | 80 | ||
| Sympathetic Nervous System Receptors | 81 | ||
| The Parasympathetic Nervous System and Cholinergic Transmission | 81 | ||
| Synthesis of Acetylcholine | 81 | ||
| Storage of Acetylcholine | 81 | ||
| Release of Acetylcholine | 81 | ||
| Metabolism and Inactivation of Released Acetylcholine | 81 | ||
| Cholinergic Receptors | 83 | ||
| Nicotinic N1 (or ganglion type) receptors | 84 | ||
| Nicotinic N2 (or muscle type) receptors | 84 | ||
| Muscarinic receptors | 84 | ||
| Other Transmitters in the Peripheral Nervous System | 84 | ||
| Amines | 84 | ||
| Dopamine | 84 | ||
| Synthesis and storage of dopamine | 84 | ||
| Release of dopamine | 84 | ||
| Removal of activity of released dopamine | 84 | ||
| Dopamine receptors | 84 | ||
| Serotonin (5-hydroxytryptamine) | 85 | ||
| Synthesis of serotonin | 85 | ||
| Storage of serotonin | 85 | ||
| Release of serotonin | 85 | ||
| Metabolism and removal of serotonin activity | 85 | ||
| Serotonin receptors | 86 | ||
| Histamine | 86 | ||
| Synthesis of histamine | 86 | ||
| Storage of histamine | 86 | ||
| Release of histamine | 86 | ||
| Removal of histamine activity | 86 | ||
| Histamine receptors | 86 | ||
| Amino Acids | 87 | ||
| γ-Aminobutyric acid | 87 | ||
| Synthesis and storage of γ-aminobutyric acid | 87 | ||
| Release of γ-aminobutyric acid | 87 | ||
| Removal of γ-aminobutyric acid activity | 87 | ||
| γ-Aminobutyric acid receptors | 87 | ||
| Glutamate | 87 | ||
| Synthesis and storage of glutamate | 87 | ||
| Release of glutamate | 87 | ||
| Removal of glutamate activity | 87 | ||
| Glutamate receptors | 87 | ||
| Glycine | 87 | ||
| Synthesis and storage of glycine | 88 | ||
| Release of glycine | 88 | ||
| Removal of glycine activity | 88 | ||
| Glycine receptors | 88 | ||
| Imidazoline receptor ligands | 88 | ||
| Peptides | 88 | ||
| Purines | 88 | ||
| Self-Assessment | 88 | ||
| True/false questions | 88 | ||
| One-best-answer (OBA) question | 89 | ||
| Answers | 89 | ||
| True/false answers | 89 | ||
| OBA answer | 89 | ||
| Further Reading | 90 | ||
| 2 The Cardiovascular System | 91 | ||
| 5 Ischaemic heart disease | 93 | ||
| Myocardial Perfusion | 93 | ||
| Clinical Manifestations of Myocardial Ischaemia | 95 | ||
| Stable Angina Pectoris | 95 | ||
| Acute Coronary Syndromes (Unstable Angina, Myocardial Infarction and Sudden Cardiac Death) | 95 | ||
| Unstable angina | 95 | ||
| Myocardial infarction and sudden cardiac death | 95 | ||
| Drugs for Treating Angina | 96 | ||
| Organic Nitrates | 96 | ||
| Mechanism of action and effects | 96 | ||
| Pharmacokinetics | 96 | ||
| Unwanted effects | 97 | ||
| Beta-Adrenoceptor Antagonists (β-Blockers) | 97 | ||
| Mechanism of action and effects in angina | 97 | ||
| Pharmacokinetics | 98 | ||
| Unwanted effects | 98 | ||
| Calcium Channel Blockers | 99 | ||
| Mechanism of action and effects | 99 | ||
| Pharmacokinetics | 101 | ||
| Unwanted effects | 101 | ||
| Potassium Channel Openers | 102 | ||
| 3 The Respiratory System | 191 | ||
| 12 Asthma and chronic obstructive pulmonary disease | 193 | ||
| Asthma | 193 | ||
| Chronic Obstructive Pulmonary Disease | 194 | ||
| Drugs for Asthma and Chronic Obstructive Pulmonary Disease | 197 | ||
| Drug Delivery to the Lung | 197 | ||
| Pressurised metered-dose inhaler | 197 | ||
| Pressurised metered-dose inhaler with a spacer | 197 | ||
| Dry-powder inhaler | 198 | ||
| Nebulisers | 198 | ||
| Symptom-Relieving Drugs for Airflow Obstruction (Bronchodilators; ‘Relievers’) | 198 | ||
| β2-Adrenoceptor agonists | 198 | ||
| Mechanism of action and effects | 198 | ||
| Pharmacokinetics | 198 | ||
| 4 The Renal System | 217 | ||
| 14 Diuretics | 219 | ||
| Functions of the Kidney | 219 | ||
| The Kidney and Maintenance of Salt and Water Balance | 219 | ||
| The proximal convoluted tubule | 219 | ||
| The loop of Henle | 220 | ||
| The distal convoluted tubule | 221 | ||
| The connecting tubule and the collecting ducts | 222 | ||
| Autoregulation by Tubuloglomerular Feedback and Hormonal Control | 222 | ||
| Diuretic Drugs | 222 | ||
| Loop Diuretics | 222 | ||
| Mechanism of action and effects | 222 | ||
| Pharmacokinetics | 222 | ||
| 5 The Nervous System | 245 | ||
| 17 General anaesthetics | 247 | ||
| Mechanisms of Action of General Anaesthetics | 248 | ||
| Drugs Used in Anaesthesia | 249 | ||
| Intravenous Anaesthetics | 249 | ||
| Pharmacokinetics | 249 | ||
| Unwanted effects | 250 | ||
| Intravenous Opioids | 251 | ||
| 6 The Musculoskeletal System | 349 | ||
| 27 The neuromuscular junction and neuromuscular blockade | 351 | ||
| Neuromuscular Transmission | 351 | ||
| Drugs Acting at the Neuromuscular Junction | 351 | ||
| Acetylcholinesterase Inhibitors (Anticholinesterases) | 351 | ||
| Inhibitors of Acetylcholine Release | 352 | ||
| Neuromuscular Junction Blockers | 352 | ||
| Competitive N2 receptor antagonists (nondepolarising blockers) | 353 | ||
| Mechanism of action and effects | 353 | ||
| Pharmacokinetics | 353 | ||
| 7 The Gastrointestinal System | 391 | ||
| 32 Nausea and vomiting | 393 | ||
| Nausea and Vomiting | 393 | ||
| Anti-Emetic Agents | 393 | ||
| Antihistamines | 393 | ||
| Mechanism of action and clinical use | 393 | ||
| Pharmacokinetics | 393 | ||
| Unwanted effects | 394 | ||
| Antimuscarinic agent | 394 | ||
| Mechanism of action and clinical use | 394 | ||
| 8 The Immune System | 437 | ||
| 38 The immune response and immunosuppressant drugs | 439 | ||
| Biological Basis of the Immune Response | 439 | ||
| Innate Immunity | 439 | ||
| Adaptive Immunity | 440 | ||
| Cell-mediated immunity | 442 | ||
| Humoral immunity | 442 | ||
| Unwanted Immune Reactions | 442 | ||
| Hypersensitivity reactions | 442 | ||
| Type 1 (allergy, immediate) | 442 | ||
| Type 2 (cytotoxic, antibody-dependent) | 442 | ||
| Type 3 (immune complex disease) | 442 | ||
| Type 4 (cell-mediated, delayed-type hypersensitivity) | 442 | ||
| Autoimmunity | 443 | ||
| Blood transfusion and transplant rejection | 443 | ||
| Immunosuppressant Drugs | 443 | ||
| Corticosteroids | 443 | ||
| Calcineurin Inhibitors | 443 | ||
| Ciclosporin | 443 | ||
| Mechanism of action | 443 | ||
| Pharmacokinetics | 443 | ||
| Unwanted effects | 443 | ||
| Tacrolimus | 444 | ||
| 9 The Endocrine System and Metabolism | 457 | ||
| 40 Diabetes mellitus | 459 | ||
| Control of Blood Glucose | 459 | ||
| Diabetes Mellitus | 460 | ||
| Type 1 Diabetes Mellitus | 461 | ||
| Type 2 Diabetes Mellitus | 461 | ||
| Insulin and Insulin Analogues for Treatment of Diabetes Mellitus | 461 | ||
| Natural Insulin Formulations | 461 | ||
| Pharmacokinetics | 462 | ||
| Unwanted effects | 462 | ||
| Insulin Analogues | 463 | ||
| Mechanism of action and effects | 463 | ||
| Rapid-acting insulin analogues | 463 | ||
| Long-acting insulin analogues | 463 | ||
| Pharmacokinetics | 463 | ||
| Unwanted effects | 463 | ||
| Therapeutic Regimens for Insulin and Insulin Analogues | 463 | ||
| Other Parenteral Glucose-Lowering Drugs | 464 | ||
| Glucagon-Like Peptide-1 Receptor Agonists | 464 | ||
| Mechanism of action | 464 | ||
| 10 The Skin and Eyes | 559 | ||
| 49 Skin disorders | 561 | ||
| Vehicles for Topical Skin Applications | 561 | ||
| Atopic and Contact Dermatitis | 561 | ||
| Atopic Eczema (Atopic Dermatitis) | 561 | ||
| Contact Dermatitis | 562 | ||
| Other Types of Dermatitis | 562 | ||
| Treatment of Atopic Eczema | 562 | ||
| Treatment of Contact Dermatitis | 562 | ||
| Psoriasis | 562 | ||
| Drugs for Treatment of Psoriasis | 563 | ||
| Topical therapy | 563 | ||
| Emollients | 563 | ||
| Keratolytics | 563 | ||
| Vitamin D analogues | 563 | ||
| Topical retinoid | 563 | ||
| Topical calcineurin inhibitors | 563 | ||
| Dithranol | 563 | ||
| Coal tar preparations | 563 | ||
| Phototherapy | 563 | ||
| Topical corticosteroid preparations | 563 | ||
| Systemic treatments | 563 | ||
| Methotrexate | 564 | ||
| Retinoids | 564 | ||
| Ciclosporin | 564 | ||
| Biologic agents | 564 | ||
| PDE4 inhibitor | 564 | ||
| Fumaric acid esters | 564 | ||
| Choice of Treatment for Psoriasis | 564 | ||
| Acne Vulgaris | 564 | ||
| Drugs for Treatment of Acne | 565 | ||
| Topical treatments | 565 | ||
| Systemic treatments | 565 | ||
| Choice of Treatment for Acne | 565 | ||
| Self-Assessment | 565 | ||
| True/false questions | 565 | ||
| One-best-answer (OBA) question | 566 | ||
| Case-based questions | 566 | ||
| Answers | 566 | ||
| True/false answers | 566 | ||
| One-best-answer (OBA) answer | 566 | ||
| Case-based answers | 566 | ||
| Further Reading | 566 | ||
| 50 The eye | 569 | ||
| Accommodation | 569 | ||
| Pupil size | 569 | ||
| Drainage of aqueous humour | 570 | ||
| Topical Application of Drugs to the Eye | 570 | ||
| Glaucoma | 570 | ||
| Drugs for Glaucoma | 571 | ||
| β-Adrenoceptor antagonists | 571 | ||
| Sympathomimetics | 571 | ||
| Carbonic anhydrase inhibitors | 571 | ||
| Prostaglandin analogues | 571 | ||
| Miotic drugs (muscarinic agonists) | 571 | ||
| Treatment of Glaucoma | 571 | ||
| Mydriatic and Cycloplegic Drugs | 572 | ||
| Antimuscarinics (Muscarinic Receptor Antagonists) | 572 | ||
| Sympathomimetics | 572 | ||
| Other Topical Applications for the Eye | 572 | ||
| Antibacterial Agents | 572 | ||
| Antiviral Agents | 572 | ||
| Corticosteroids | 572 | ||
| Antiallergic Agents | 573 | ||
| Local Anaesthetics | 573 | ||
| Nonsteroidal AntiInflammatory Drugs | 573 | ||
| Dry Eye Syndrome | 573 | ||
| Age-Related Macular Degeneration | 573 | ||
| Treatment of Age-Related Macular Degeneration | 573 | ||
| Diabetic Retinopathy | 574 | ||
| Treatment of Diabetic Retinopathy | 574 | ||
| Self-Assessment | 574 | ||
| True/false questions | 574 | ||
| Extended-matching-item questions | 574 | ||
| Case-based questions | 574 | ||
| Answers | 575 | ||
| True/false answers | 575 | ||
| Extended-matching-item answers | 575 | ||
| Case-based answers | 575 | ||
| Further Reading | 575 | ||
| 11 Chemotherapy | 579 | ||
| 51 Chemotherapy of infections | 581 | ||
| Bacterial Infections | 581 | ||
| Classification of Antibacterial Drugs | 581 | ||
| Antimicrobial Resistance | 582 | ||
| Antibacterial Drug Resistance | 582 | ||
| Spontaneous mutation | 582 | ||
| Conjugation | 582 | ||
| Transduction | 583 | ||
| Transformation | 583 | ||
| Antibacterial Drugs | 583 | ||
| Drugs affecting the cell wall: β-lactam antibacterials | 583 | ||
| Mechanism of action of β-lactam antibacterials | 583 | ||
| Penicillins | 583 | ||
| Spectrum of activity | 584 | ||
| Resistance | 584 | ||
| Pharmacokinetics | 584 | ||
| Unwanted effects | 585 | ||
| Cephalosporins | 585 | ||
| Spectrum of activity | 585 | ||
| Resistance | 587 | ||
| Pharmacokinetics | 587 | ||
| Unwanted effects | 587 | ||
| Monobactams | 587 | ||
| Carbapenems | 587 | ||
| Other drugs affecting the cell wall | 587 | ||
| Glycopeptides | 587 | ||
| Mechanism of action | 587 | ||
| Spectrum of activity | 587 | ||
| 12 General Features: Drug Toxicity and Prescribing | 657 | ||
| 53 Drug toxicity and overdose | 659 | ||
| Drug Toxicity and Adverse Effects | 659 | ||
| Types of Unwanted Effect | 660 | ||
| Pharmacological Toxicity | 660 | ||
| Biochemical Toxicity | 662 | ||
| Paracetamol | 662 | ||
| Cyclophosphamide | 663 | ||
| Isoniazid | 663 | ||
| Spironolactone | 664 | ||
| Aromatic amines and nitrites | 664 | ||
| Methaemoglobinaemia | 664 | ||
| Haemolysis | 664 | ||
| Immunological Toxicity | 665 | ||
| The Yellow Card Scheme | 665 | ||
| Self-Poisoning and Drug Overdose | 666 | ||
| Management Principles | 667 | ||
| Managing Adverse Effects | 667 | ||
| Immediate measures | 667 | ||
| Supportive measures | 667 | ||
| Cardiac or respiratory arrest | 667 | ||
| Hypotension | 667 | ||
| Arrhythmias | 668 | ||
| Seizures | 668 | ||
| Renal failure | 668 | ||
| Hepatic failure | 668 | ||
| Impaired temperature regulation | 669 | ||
| Reducing Toxicity | 669 | ||
| Prevention of absorption of poisons | 669 | ||
| Index | 707 | ||
| A | 707 | ||
| B | 710 | ||
| C | 711 | ||
| D | 713 | ||
| E | 715 | ||
| F | 715 | ||
| G | 716 | ||
| H | 717 | ||
| I | 718 | ||
| J | 719 | ||
| K | 719 | ||
| L | 719 | ||
| M | 720 | ||
| N | 721 | ||
| O | 722 | ||
| P | 723 | ||
| Q | 725 | ||
| R | 725 | ||
| S | 725 | ||
| T | 727 | ||
| U | 728 | ||
| V | 728 | ||
| W | 729 | ||
| X | 729 | ||
| Y | 729 | ||
| Z | 729 |