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Michael J. Neal. Medical Pharmacology at a Glance
Table of Contents
Guide
Pages
Medical Pharmacology at a Glance
Preface
Acknowledgements
Further reading
List of abbreviations
Core drugs
Chapter 10 Ocular pharmacology
Chapter 11 Asthma, hay fever and anaphylaxis
Chapters 12 and 13 Gastrointestinal tract
Chapters 15–20 Cardiovascular system
Chapters 5, 6 and 23–32 Nervous system
Chapters 33–36 Endocrine system
Chapters 37–43 Infectious disease
Chapter 44 Drugs used in cancer
Chapter 45 Immunosuppressants and antirheumatoid drugs
Chapter 46 Poisoning
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
Phase I reactions
Phase II reactions
Drugs
Liver
Phase I reactions
The P450 monooxygenase system
Phase II reactions
Factors affecting drug metabolism. Enzyme induction
Enzyme inhibition
Genetic polymorphisms
Drug‐acetylating enzymes
Plasma pseudocholinesterase
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 (ACh)
Exocytosis
ACh receptor
Myasthenia gravis
Presynaptic agents. Drugs inhibiting ACh release
Competitive neuromuscular blocking drugs
Depolarizing neuromuscular blocking drugs
Note
7 Autonomic nervous system
Effects of sympathetic stimulation
Adrenoceptors
Acetylcholine
Acetylcholine receptors (cholinoceptors)
Muscarinic receptors
Nicotinic receptors
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. Histamine H2‐receptor antagonists
Proton pump inhibitors
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 (see also Chapters 16 and 17)
α1‐Adrenoceptor antagonists
Other vasodilators
Centrally acting drugs
Acute severe hypertension
16 Drugs used in angina
Nitrates. Short‐acting nitrates
Adverse effects
Mechanism of action
β‐Adrenoceptor antagonists
Calcium‐channel blockers
Tobacco smoking
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
Direct effects (bottom, )
Indirect 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
Dependence
Drug interactions
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. Valproate
Benzodiazepines
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
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)
Cannabis (marijuana, hashish)
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
Metabolic effects
Fluid retention, hypokalaemia and hypertension
Adrenal suppression
Infections
Other complications
Mineralocorticoids
34 Sex hormones and drugs
Infertility
Testosterone
Effects
Oestrogens
Progestogens. Progestogens 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
Mechanism of action
Adverse effects
Emergency contraception
Therapeutic termination of pregnancy
35. Thyroid and antithyroid drugs
Hyperthyroidism (thyrotoxicosis)
Antithyroid drugs
Hypothyroidism
Replacement therapy
36 Antidiabetic agents
Insulin release
Incretins
Insulin receptors
Insulin preparations
Short‐acting insulins
Intermediate‐ and long‐acting insulins
Adverse effects
Insulin regimens
Oral antidiabetic drugs. Biguanides
Sulphonylureas and repaglinide
Dipeptidyl peptidase 4 inhibitors
37. Antibacterial drugs that inhibit nucleic acid synthesis: sulphonamides, trimethoprim, quinolones and nitroimidazoles
Selective toxicity
Sulphonamides
Adverse effects
Quinolones
5‐Nitroimidazoles
Notes
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
Notes
39 Antibacterial drugs that inhibit protein synthesis: aminoglycosides, tetracyclines, macrolides and chloramphenicol
Aminoglycosides
Macrolides
Tetracyclines
Chloramphenicol
Note
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)
Whipworms
Filarial infections
Trematodes (flukes)
Cestodes (tapeworms)
Anthelmintics
43 Drugs acting on parasites II: protozoa
Blood schizonticides (rapid‐acting)
Chloroquine
Mechanism of action
Blood schizonticides (slow‐acting)
Mechanism of action
Tissue schizonticide
Other protozoal diseases
Giardiasis
Trichomoniasis
Pneumocystosis
Leishmaniasis
Trypanosomiasis
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
Heavy metals
47. Adverse drug reactions
Drug interactions
Pharmacodynamic interactions
Pharmacokinetic interactions. Absorption
Distribution
Metabolism
Excretion
Drug allergy
Teratogenesis
Carcinogenesis
Case studies and questions. Case 1 Deliberate poisoning
Case 2 Adverse drug effect
Case 3 Duodenal ulcer
Case 4 Hypertension
Case 5 Myocardial infarction
Case 6 Atrial fibrillation and congestive heart failure
Case 7 Insomnia
Case 8 Drug abuse
Case 9 Suicide attempt
Case 10 Collapse
Case 11 Alcohol dependence
Case 12 Corticosteroid withdrawal
Case 13 Peptic ulcer
Case 14 Drug interaction
Answers. Case 1 Deliberate poisoning
Case 2 Adverse drug effect
Case 3 Duodenal ulcer
Case 4 Hypertension
Case 5 Myocardial infarction
Case 6 Atrial fibrillation and congestive heart failure
Case 7 Insomnia
Case 8 Drug abuse
Case 9 Suicide attempt
Case 10 Collapse
Case 11 Alcohol dependence
Case 12 Corticosteroid withdrawal
Case 13 Peptic ulcer
Case 14 Drug interaction
Note
Index
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