Michael J. Neal - Medical Pharmacology at a Glance

1 Cover

2 Preface

3 Acknowledgements

4 Further reading

5 List of abbreviations

6 Core drugs Core drugs

7 About the companion website

8 1 Introduction Receptors Transport systems Enzymes Second messengers G‐proteins

9 2 Drug–receptor interactions Binding of drugs to receptors Antagonists Receptor reserve Partial agonists Intrinsic efficacy Bioassay Binding assays Localization of receptors Tachyphylaxis, desensitization, tolerance and drug resistance

10 3 Drug absorption, distribution and excretion Routes of administration Distribution and excretion Excretion

11 4 Drug metabolism Drugs Liver Phase I reactions Phase II reactions Factors affecting drug metabolism Metabolism and drug toxicity

12 5 Local anaesthetics Na +channels Action potential Mechanism of local anaesthetics Chemistry Unwanted effects Methods of administration

13 6 Drugs acting at the neuromuscular junction Presynaptic agents Competitive neuromuscular blocking drugs Depolarizing neuromuscular blocking drugs

14 7 Autonomic nervous system Effects of sympathetic stimulation Acetylcholine

15 8 Autonomic drugs acting at cholinergic synapses Cholinomimetics Muscarinic antagonists (antimuscarinics)

16 9 Drugs acting on the sympathetic system Sympathomimetics Adrenoceptor antagonists

17 10 Ocular pharmacology Glaucoma Mydriatics

18 11 Asthma, hay fever and anaphylaxis Mediators Bronchodilators Cromoglicate Corticosteroids Acute severe asthma Antihistamines

19 12 Drugs acting on the gastrointestinal tract I Acid secretion Protective factors Ulcer healing drugs Antacids

20 13 Drugs acting on the gastrointestinal tract II Motility stimulants Laxatives Antidiarrhoeal drugs Drugs used in inflammatory bowel disease Drugs used to dissolve gallstones Pancreatic supplements

21 14 Drugs acting on the kidney Thiazides Loop diuretics Potassium‐sparing diuretics

22 15 Drugs used in hypertension Thiazide and other diuretics β‐adrenoceptor antagonists Vasodilator drugs Centrally acting drugs Acute severe hypertension

23 16 Drugs used in angina Nitrates β‐Adrenoceptor antagonists Calcium‐channel blockers Revascularization

24 17 Antiarrhythmic drugs Cardiac action potential Pacemaker cells Drugs used in supraventricular arrhythmias Drugs effective in supraventricular and ventricular arrhythmias Drugs used in ventricular arrhythmias Alternatives to drugs

25 18 Drugs used in heart failure ACE inhibitors and ARBs β‐blockers Inotropic drugs Sympathomimetic agents

26 19 Drugs used to affect blood coagulation Anticoagulants Antiplatelet drugs Fibrinolytic drugs (thrombolytics)

27 20 Lipid‐lowering drugs Lipoproteins Hyperlipidaemias Atherosclerosis Drug combinations

28 21 Agents used in anaemias Iron Iron preparations Vitamin B 12 Folic acid Erythropoietin

29 22 Central transmitter substances Amino acids Monoamines Other transmitters/modulaters

30 23 General anaesthetics Reticular activating system (RAS) Mechanism of action of anaesthetics Premedication Intravenous agents Inhalation agents

31 24 Anxiolytics and hypnotics GABA receptors Barbiturate receptor Benzodiazepines Antidepressants Drugs acting at serotonergic (5HT) receptors

32 25 Antiepileptic drugs Causes of epilepsy Mechanisms of action of anticonvulsants 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

33 26 Drugs used in Parkinson’s disease Aetiology Dopaminergic drugs Dopamine agonists Drugs causing dopamine release Antimuscarinics

34 27 Antipsychotic drugs (neuroleptics) Dopamine receptors Chemical classification Depot preparations

35 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

36 29 Opioid analgesics Strong opioid analgesics Weak opioid analgesics

37 30 Drugs used in nausea and vertigo (antiemetics) Drug‐induced vomiting Motion sickness Vestibular disease Pregnancy

38 31 Drug misuse and dependence Central stimulants Opioids Hallucinogens (psychedelics) General depressants Tobacco

39 32 Non‐steroidal anti‐inflammatory drugs (NSAIDs) Mechanisms of action Adverse effects Other NSAIDs Gout

40 33 Corticosteroids Glucocorticoids Mineralocorticoids

41 34 Sex hormones and drugs Infertility Testosterone Oestrogens ProgestogensProgestogens are used for hormonal contraception and for producing long‐term ovarian suppression for other purposes (e.g. dysmenorrhoea, endometriosis, hirsutism and bleeding disorders) when oestrogens are contraindicated. Oral contraceptives

42 35 Thyroid and antithyroid drugs Hyperthyroidism (thyrotoxicosis) Antithyroid drugs Hypothyroidism Replacement therapy

43 36 Antidiabetic agents Insulin release Insulin preparations Oral antidiabetic drugs

44 37 Antibacterial drugs that inhibit nucleic acid synthesis Selective toxicity Sulphonamides Quinolones 5‐Nitroimidazoles

45 38 Antibacterial drugs that inhibit cell wall synthesis Penicillins Cephalosporins Other β‐lactam antibiotics Vancomycin

46 39 Antibacterial drugs that inhibit protein synthesis Aminoglycosides Macrolides Tetracyclines Chloramphenicol

47 40 Antifungal drugs Fungal infections Polyenes Flucytosine Imidazoles Triazoles Echinocandins

48 41 Antiviral drugs Drugs that prevent the virus entering or leaving the host cells Drugs that inhibit viral DNA polymerase Drugs that inhibit viral reverse transcriptase Protease inhibitors Integrase inhibitors Immunomodulators

49 42 Drugs acting on parasites I Nematodes (roundworms) Trematodes (flukes) Cestodes (tapeworms) Anthelmintics

50 43 Drugs acting on parasites II Blood schizonticides (rapid‐acting) Blood schizonticides (slow‐acting) Tissue schizonticide Other protozoal diseases

51 44 Drugs used in cancer Alkylating agents Cytotoxic antibiotics Vinca alkaloids and taxanes Antimetabolites Monoclonal antibodies Hormones and hormone antagonists

52 45 Immunosuppressants and antirheumatoid drugs Corticosteroids Antiproliferative drugs Calcineurin inhibitors Monoclonal antibodies Disease‐modifying antirheumatoid drugs (DMARDs) Anticytokine drugs

53 46 Poisoning Reduction of absorption Enhancement of elimination Aspirin Paracetamol Opioids Tricyclic antidepressants Heavy metals

54 47 Adverse drug reactions Drug interactions Drug allergy Teratogenesis Carcinogenesis

55 Case studies and questions

56 Answers

57 Index

58 End User License Agreement

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2 Table of Contents

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