Medical Pharmacology at a Glance

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Medical Pharmacology at a Glance 8th Edition Prelims Title Copyright Contents Preface Acknowledgements Further reading How to use your textbook About the companion website 1 Introduction: principles of drug action Receptors Transport systems Enzymes Second messengers G-proteins 2 Drug–receptor interactions Binding of drugs to receptors Intermolecular forces Affinity Antagonists Other types of antagonism Receptor reserve Partial agonists Intrinsic efficacy Bioassay Binding assays Localization of receptors Tachyphylaxis, desensitization, tolerance and drug resistance 3 Drug absorption, distribution and excretion Routes of administration Distribution and excretion Excretion 4 Drug metabolism Drugs Liver Phase I reactions The P450 monooxygenase system Phase II reactions Factors affecting drug metabolism Enzyme induction Enzyme inhibition Genetic polymorphisms Age Metabolism and drug toxicity 5 Local anaesthetics Na+ channels Action potential Mechanism of local anaesthetics Chemistry Unwanted effects Central nervous system Cardiovascular system Duration of action Methods of administration Surface anaesthesia Infiltration anaesthesia Nerve block Intravenous regional anaesthesia 6 Drugs acting at the neuromuscular junction Acetylcholine Exocytosis Acetylcholine receptor Myasthenia gravis Presynaptic agents Drugs inhibiting acetylcholine release Competitive neuromuscular blocking drugs Depolarizing neuromuscular blocking drugs 7 Autonomic nervous system Effects of sympathetic stimulation Adrenoceptors Acetylcholine Acetylcholine receptors (cholinoceptors) Actions of acetylcholine 8 Autonomic drugs acting at cholinergic synapses Cholinomimetics Muscarinic agonists Choline esters Anticholinesterases Mechanism of action Muscarinic antagonists (antimuscarinics) 9 Drugs acting on the sympathetic system Sympathomimetics Indirectly acting sympathomimetics Directly acting sympathomimetics β-receptor-selective drugs Adrenoceptor antagonists α-blockers β-blockers 10 Ocular pharmacology Ciliary body Trabecular meshwork Glaucoma Drugs that reduce IOP by increasing outflow Drugs that reduce IOP by decreasing aqueous secretion Mydriatics Age-related macular degeneration 11 Asthma, hay fever and anaphylaxis Mediators Bronchodilators β-Adrenoceptor stimulants Xanthines Cromoglicate Corticosteroids Acute severe asthma Antihistamines 12 Drugs acting on the gastrointestinal tract I: peptic ulcer Acid secretion Protective factors Mucus layer Ulcer healing drugs Acid secretion reducers Mucosal protectants Antacids 13 Drugs acting on the gastrointestinal tract II: motility and secretions Motility stimulants Laxatives Antidiarrhoeal drugs Drugs used in inflammatory bowel disease Drugs used to dissolve gallstones Pancreatic supplements 14 Drugs acting on the kidney: diuretics Thiazides Mechanism of action Adverse effects Loop diuretics Mechanism of action Adverse effects Potassium-sparing diuretics 15 Drugs used in hypertension Thiazide and other diuretics β-adrenoceptor antagonists Vasodilator drugs ACE inhibitors Calcium-channel blockers α1-adrenoceptor antagonists Other vasodilators Centrally acting drugs Acute severe hypertension 16 Drugs used in angina Nitrates β-Adrenoceptor antagonists Calcium-channel blockers Revascularization 17 Antiarrhythmic drugs Cardiac action potential Pacemaker cells Acetylcholine Norepinephrine Drugs used in supraventricular arrhythmias Drugs effective in supraventricular and ventricular arrhythmias Drugs used in ventricular arrhythmias Alternatives to drugs 18 Drugs used in heart failure ACE inhibitors and ARBs β-blockers Inotropic drugs Mechanical effects and therapeutic benefit Mechanism of action Electrical effects Effects on other organs Toxicity Sympathomimetic agents 19 Drugs used to affect blood coagulation Anticoagulants Antiplatelet drugs Fibrinolytic drugs (thrombolytics) 20 Lipid-lowering drugs Lipoproteins Hyperlipidaemias Atherosclerosis Lipid-lowering drugs Drug combinations 21 Agents used in anaemias Iron Absorption Iron preparations Iron toxicity Vitamin B12 Methylmalonyl-CoA mutase Folic acid Erythropoietin 22 Central transmitter substances Amino acids Monoamines Other transmitters/modulaters 23 General anaesthetics Reticular activating system (RAS) Mechanism of action of anaesthetics Premedication Relief from anxiety (Chapter 24) Reduction of secretions and vagal reflexes Analgesics Postoperative antiemesis Intravenous agents Inhalation agents Uptake and distribution (bottom left figure) 24 Anxiolytics and hypnotics GABA receptors Barbiturate receptor Benzodiazepines Antidepressants Drugs acting at serotonergic (5HT) receptors 25 Antiepileptic drugs Causes of epilepsy Mechanisms of action of anticonvulsants Inhibition of sodium channels Enhancement of GABA action Inhibition of calcium channels Drugs used in partial and generalized tonic–clonic (grand mal) seizures Drugs used to treat absences (petit mal) Drugs effective in tonic–clonic (grand mal) and absence (petit mal) seizures Drug withdrawal Pregnancy 26 Drugs used in Parkinson’s disease Aetiology Dopaminergic drugs Mechanism of action Adverse effects Problems with long-term treatment Dopamine agonists Drugs causing dopamine release MAOB and COMT inhibitors Antimuscarinics 27 Antipsychotic drugs (neuroleptics) Dopamine receptors Mechanism of action of neuroleptics Chemical classification Phenothiazines Other chemical classes Depot preparations 28 Drugs used in affective disorders: antidepressants Monoamine theory of depression Mechanism of action of antidepressants Drugs that inhibit amine uptake Receptor blockers Monoamine oxidase inhibitors Mechanism of action 29 Opioid analgesics Strong opioid analgesics Weak opioid analgesics 30 Drugs used in nausea and vertigo (antiemetics) Drug-induced vomiting Motion sickness Vestibular disease Acute labyrinthitis Pregnancy 31 Drug misuse and dependence Central stimulants Opioids Hallucinogens (psychedelics) General depressants Tobacco 32 Non-steroidal anti-inflammatory drugs (NSAIDs) Mechanisms of action Adverse effects Gastrointestinal tract Nephrotoxicity Other adverse effects Other NSAIDs Gout Prophylactic treatment of gout 33 Corticosteroids Glucocorticoids Mechanisms of action Effects Adverse effects Mineralocorticoids 34 Sex hormones and drugs Infertility Testosterone Oestrogens Progestogens Oral contraceptives 35 Thyroid and antithyroid drugs Hyperthyroidism (thyrotoxicosis) Antithyroid drugs Hypothyroidism Replacement therapy 36 Antidiabetic agents Insulin release Insulin preparations Adverse effects Insulin regimens Oral antidiabetic drugs 37 Antibacterial drugs that inhibit nucleic acid synthesis: sulphonamides, trimethoprim, quinolones and nitroimidazoles Selective toxicity Sulphonamides Adverse effects Quinolones 5-Nitroimidazoles 38 Antibacterial drugs that inhibit cell wall synthesis: penicillins, cephalosporins and vancomycin Penicillins Penicillinase-resistant penicillins: flucloxacillin Broad-spectrum penicillins Antipseudomonal penicillins Cephalosporins Other β-lactam antibiotics Vancomycin 39 Antibacterial drugs that inhibit protein synthesis: aminoglycosides, tetracyclines, macrolides and chloramphenicol Aminoglycosides Macrolides Tetracyclines Chloramphenicol Streptogramins 40 Antifungal drugs Fungal infections Polyenes Flucytosine Imidazoles Triazoles Echinocandins 41 Antiviral drugs Drugs that prevent the virus entering or leaving the host cells Immunoglobulins Amantadine Neuraminidase inhibitors Drugs that inhibit viral DNA polymerase Drugs that inhibit viral reverse transcriptase Protease inhibitors Integrase inhibitors Immunomodulators 42 Drugs acting on parasites I: helminths (worms) Nematodes (roundworms) Trematodes (flukes) Cestodes (tapeworms) Anthelmintics 43 Drugs acting on parasites II: protozoa Blood schizonticides (slow-acting) Blood schizonticides (rapid-acting) Tissue schizonticide Other protozoal diseases 44 Drugs used in cancer Selectivity Adverse effects Drug resistance Alkylating agents Cytotoxic antibiotics Vinca alkaloids and taxanes Antimetabolites Monoclonal antibodies Hormones and hormone antagonists 45 Immunosuppressants and antirheumatoid drugs Corticosteroids Antiproliferative drugs Calcineurin inhibitors Monoclonal antibodies Disease-modifying antirheumatoid drugs (DMARDs) Anticytokine drugs 46 Poisoning Reduction of absorption Emesis Gastric aspiration and lavage Activated charcoal Enhancement of elimination Aspirin Paracetamol Opioids Tricyclic antidepressants 47 Adverse drug reactions Drug interactions Pharmacodynamic interactions Pharmacokinetic interactions Drug allergy Teratogenesis Carcinogenesis Case studies and questions Answers Index EULA