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Clinical Pharmacology - E-Book

Clinical Pharmacology - E-Book

Morris J. Brown | Pankaj Sharma | Fraz A. Mir | Peter N. Bennett

(2018)

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Book Details

Abstract

‘The very last thing a drug regulator wishes to be able to say is, like Lord Byron (1788-1824), on the publication of his poem Childe Harold’s Pilgrimage, ‘I awoke one morning and found myself famous.’

The twelfth edition of this long-established textbook of clinical pharmacology (first published in 1960) continues its fine tradition of balancing science and practice for improved evidence-based drug therapy and good prescribing in therapeutic settings increasingly complicated by intercurrent disease and polypharmacy.

  • Coverage of all major therapeutic topics by body system.
  • Introductory sections give brief chapter synopses.
  • Case studies where relevant.
  • Covers the needs of the developing world with a focus on practical prescribing and health technology assessment.
  • Definition, tips, brief explanation boxes throughout.
  • Interesting histories, etymologies and provenances of terms throughout.
  • Entertaining footnotes throughout.

‘The very last thing a drug regulator wishes to be able to say is, like Lord Byron (1788-1824), on the publication of his poem Childe Harold’s Pilgrimage, ‘I awoke one morning and found myself famous.’

  • Fully updated throughout.
  • New co-editor: Fraz Mir, Addenbrooke’s Hospital and Department of Medicine, University of Cambridge, Royal College of Physicians Associate International Director for South Asia.
  • Now with free e-book on StudentConsult.

Table of Contents

Section Title Page Action Price
Front Cover cover
Inside Front Cover ifc1
Half title page i
Dedication ii
Clinical Pharmacology iii
Copyright Page iv
Table Of Contents v
Preface vii
Contributors ix
Acknowledgements xiii
1 General 1
1 Clinical pharmacology 2
Synopsis 2
Guide to further reading 4
2 Topics in drug therapy 5
Synopsis 5
The therapeutic situation 5
Some background 5
Treating patients with drugs 6
Drugs can do good 6
Drugs can do harm 6
Uses of drugs/medicines 7
Cure 7
Suppression 7
Prevention 7
Physician-induced (iatrogenic) disease 7
Benefits and risks of medicines 8
Unavoidable risks 8
Reduction of risk 8
Two broad categories of risk 8
Elements of risk 9
Three major grades of risk 9
Whenever a drug is taken a risk is taken 9
Public view of drugs and prescribers 10
Criticisms of modern drugs 10
Drug-induced injury (see also Ch. 9) 11
Negligence and strict and no-fault liability 11
Complementary, alternative and traditional medicine 12
Homoeopathy 14
Conclusion 15
Placebo medicines 15
Guidelines, ‘essential’ drugs and prescribing 16
‘Essential’ drugs 17
Cost-containment 17
Taking a drug history 18
Repeat prescriptions 18
Warnings and consent 18
Legal hazards for prescribers 19
Compliance 19
Patient compliance 19
Suggestions for doctors to enhance patient compliance/adherence 21
Directly observed therapy 21
Over-compliance. 21
Evaluation of patient compliance. 21
Doctor compliance 22
Underdosing 22
The clinical importance of missed dose(s) 22
Pharmacoeconomics (see also Ch. 5) 23
The economists’ objective 23
Quality of life 24
Guide to further reading 25
Appendix: the prescription 26
Example of a prescription for a patient with an annoying unproductive cough: 26
Medicine containers. 26
Unwanted medicines. 27
Drugs liable to cause dependence 27
Abbreviations 27
Weights and measures 27
Equivalents: 27
Abbreviations: 27
Home/domestic measures. 27
Percentages, proportions, weight in volume 27
3 Discovery and development of drugs 28
Synopsis 28
Making a new medicine 28
Techniques of discovery 30
Molecular modelling and structural biology 30
High throughput screening 30
Fragments. 30
Proteins as medicines: biotechnology. 30
Antisense approaches. 31
Gene therapy 32
Stem cells. 32
Immunopharmacology. 32
Older approaches 32
Drug quality 32
Studies in animals 33
Pharmacodynamics 33
Pharmacokinetics 33
Toxicology 33
Genotoxicity 34
Carcinogenicity 34
Reproductive and developmental toxicity 34
Local tolerance 34
Biotechnology-derived pharmaceuticals 34
Ethics and legislation 34
Safety prediction 35
Orphan drugs and diseases 36
Guide to further reading 36
4 Evaluation of drugs in humans 37
Synopsis 37
Experimental therapeutics 37
Research involving human subjects 38
Ethics of research in humans 38
The ethics of the randomised and placebo-controlled trial 39
Injury to research subjects 40
Payment of subjects in clinical trials 40
Rational introduction of a new drug to humans 40
Phases of clinical development 40
Official regulatory guidelines and requirements 42
Therapeutic investigations 42
Therapeutic evaluation 43
Need for statistics 44
Concepts and terms 44
Hypothesis of no difference 44
A statistical significance test 44
Confidence intervals. 44
Types of error 45
Type I error 45
Type II error 45
Types of therapeutic trial 45
Dose–response trials. 46
Superiority, equivalence and non-inferiority in clinical trials. 46
Design of trials 47
Techniques to avoid bias 47
Randomisation 47
Blinding. 47
Some common design configurations 48
Parallel group design 48
Crossover design 48
Factorial designs 48
Multicentre trials 48
N-of-1 trials 48
Historical controls 49
Size of trials 49
Fixed sample size and sequential designs 49
Sensitivity of trials 50
Meta-analysis 50
Results: implementation 51
Relative and absolute risk 51
Pharmacoepidemiology 52
Observational cohort studies 52
Case–control studies 53
Surveillance systems: pharmacovigilance 53
Voluntary reporting. 53
Prescription event monitoring. 54
Medical record linkage 54
Population statistics, 54
Strength of evidence 54
In conclusion 54
Guide to further reading 55
5 Health technology assessment 56
Synopsis 56
The scope 56
Clinical effectiveness 57
1. Developing the protocol 57
2. Defining the methods 57
3. Analysing the data 57
Qualitative synthesis 58
Quantitative synthesis (meta-analysis) 58
4. Drawing conclusions 59
Cost-effectiveness 59
1. Costs 60
2. Benefits 60
Natural units 60
Health utilities 60
3. Type of analysis 60
Cost-effectiveness analysis 60
Cost-utility analysis 61
In conclusion 61
Guide to further reading 62
6 Regulation of medicines 63
Synopsis 63
Basis for regulation 63
Historical background 64
Current medicines regulatory systems 65
Rare diseases 65
Requirements 65
Authorisation for clinical trials in the UK 65
Regulatory review of a new drug marketing application 66
Regulatory review 66
Post-licensing responsibilities 67
Discussion 67
Licensed medicines for unlicensed indications 68
Unlicensed medicines and accelerated licensing 68
Decision-taking 68
Counterfeit drugs 69
Complementary and alternative medicine 69
Medicines regulation: the future 70
Guide to further reading 70
7 Classification and naming of drugs 71
Synopsis 71
Classification 71
Nomenclature (names) 71
Non-proprietary names 72
Clarity. 72
Economy. 72
Convenience. 72
Proprietary names 73
Confusing names. 73
Guide to further reading 74
2 From pharmacology to toxicology 75
8 General pharmacology 76
Synopsis 76
3 Infection and inflammation 165
12 Chemotherapy of infections 166
Synopsis 166
History 166
Classification of antimicrobial drugs 168
How antimicrobials act – sites of action 168
The cell wall. 169
The cytoplasmic membrane. 169
Protein synthesis. 169
Nucleic acid metabolism. 169
Principles of antimicrobial chemotherapy 169
Make a diagnosis 169
Remove barriers to cure, 169
Decide whether chemotherapy is really necessary. 169
Select the best drug. 169
Administer the drug 169
Continue therapy 170
Test for cure. 170
Prophylactic chemotherapy 170
Carriers of pathogenic or resistant organisms 170
Use of antimicrobial drugs 170
Choice 170
Knowledge of the likely pathogens 170
Rapid diagnostic tests. 170
Route of administration. 171
Combinations 171
Chemoprophylaxis and pre-emptive suppressive therapy 171
Chemoprophylaxis in surgery 172
Antimicrobials should be selected 172
Antimicrobials should be given 172
Problems with antimicrobial drugs 173
Resistance 173
Mechanisms of resistance 174
Limitation of resistance 174
Superinfection 175
Antibiotic-associated (or Clostridium difficile-associated) colitis 175
Opportunistic infection 176
Masking of infections 176
Drugs of choice 176
Guide to further reading 177
13 Antibacterial drugs 178
Synopsis 178
Classification 178
Inhibition of cell wall synthesis 178
β-lactams 178
Inhibition of protein synthesis 178
Aminoglycosides. 178
Tetracyclines, 178
Macrolides: 178
Inhibition of nucleic acid synthesis 178
Sulfonamides. 178
Quinolones 178
Azoles 178
Inhibition of cell wall synthesis 179
β-lactams 179
Penicillins 179
Mode of action. 179
Pharmacokinetics. 179
Adverse effects. 179
Narrow-spectrum penicillins 180
Benzylpenicillin 180
Uses. 180
Adverse effects 180
Preparations and dosage for injection. 180
Preparations and dosage for oral use. 180
Antistaphylococcal penicillins 180
Broad-spectrum penicillins 180
Amoxicillin 181
Ampicillin 181
Co-amoxiclav 181
Adverse effects. 181
Mecillinam 181
Temocillin 181
Antipseudomonal penicillins 181
Carboxypenicillins 181
Ticarcillin 181
Ureidopenicillins 181
Piperacillin 182
Cephalosporins 182
Mode of action 182
Pharmacokinetics. 182
Classification and uses. 183
Adverse effects. 183
Ceftobiprole 184
Other β-lactam antibacterials 184
Monobactam 184
Carbapenems 184
Imipenem 184
Adverse effects. 184
Meropenem 184
Ertapenem 184
Penems 184
Other inhibitors of cell wall synthesis and membrane function 184
Vancomycin 184
Uses. 185
Adverse effects. 185
Teicoplanin 185
Daptomycin 185
Oritavancin, dalbavancin and telavancin 186
Inhibition of protein synthesis 186
Aminoglycosides 186
Mode of action. 186
Pharmacokinetics. 186
Antibacterial activity. 186
Uses 186
Adverse effects. 187
Individual aminoglycosides 187
Gentamicin 187
Dose 187
Tetracyclines and glycylcyclines 188
Mode of action. 188
Pharmacokinetics. 188
Uses. 188
Adverse reactions. 188
Interactions. 188
Individual tetracyclines 188
Tetracycline 188
Doxycycline 188
Minocycline 189
Tigecycline 189
Macrolides and lincosamides 189
Erythromycin 189
Uses. 189
Dose 189
Adverse reactions. 189
Interactions. 189
Clarithromycin 190
Azithromycin 190
Telithromycin 190
Clindamycin, 190
Other inhibitors of protein synthesis 191
Chloramphenicol 191
Pharmacokinetics. 191
4 Nervous system 287
18 Pain and analgesics 288
Synopsis 288
Pain and analgesics 288
Definition of pain 288
Nociception 289
Classification of clinical pain 290
Acute pain, 291
Chronic pain 291
Neuropathic pain 291
Cancer-related pain 291
Evaluation of pain 291
Pharmacotherapy 291
Non-opioid analgesics 292
NSAIDS (non-steroidal anti-inflammatory drugs) 292
Mechanism of analgesia 292
Clinical use 292
Choice of NSAID and route of administration 292
Adverse effects 292
Acetaminophen (Paracetamol) 292
Nefopam (3,4,5,6-tetrahydro-5-methyl-l-phenyl-1H-2.5-benoxazocine hydrochloride) 293
Opioid analgesics 293
Mechanism of action of opioids 293
Classification of opioid drugs 293
Opioid pharmacodynamics 293
Systemic effects of opioid analgesics 294
Central nervous system 294
Cardiovascular system 295
Gastrointestinal tract 295
Urogenital tract 295
Others 295
Opioid pharmacokinetics 295
Route of administration 296
Pharmacology of individual opioids 296
Opioid agonist drugs 296
Morphine 296
Diamorphine 296
Codeine 297
Dihydrocodeine 297
Oxycodone 297
Hydromorphone 297
Methadone 297
Fentanyl 297
Alfentanil 298
Remifentanil 298
Papaveretum 298
Partial agonist opioid analgesics 298
Buprenorphine 298
Meptazinol 298
Mixed agonist-antagonist opioid analgesics 298
Opioids with action on other systems 299
Meperidine 299
Tramadol 299
Tapentadol 299
Opioid antagonists 299
Naloxone 299
Choice of opioid analgesic 299
Tolerance, dependence and addiction 300
Tolerance 300
Dependence 301
Addiction 301
Pain management in opioid addicts 301
Co-analgesics 301
Multipurpose adjuvant analgesics 301
Corticosteroids 301
Neuroleptics 301
Benzodiazepines 302
Adjuvant analgesics used in neuropathic pain 302
Antidepressants 302
Anticonvulsants 302
Local anaesthetics 303
Capsaicin 303
Clonidine 303
Cannabinoids 303
Ziconotide 303
Ketamine 304
Adjuvants used for bone pain 304
Bisphosphonates 304
Pharmacotherapy of acute migraine headaches 304
Management of migraine 304
Abortive treatment of migraine 305
Selective 5-HT1 agonists (triptans) 305
Sumatriptan 305
Ergotamine 305
Preventive treatment for migraine 306
Beta-adrenergic Blockers 306
Valproic acid 306
Topiramate 306
Other drugs used in migraine prevention 306
Guide to further reading 307
19 Anaesthesia and neuromuscular block 308
Synopsis 308
General anaesthesia 308
Phases of general anaesthesia 309
Before surgery, 309
During surgery, 309
After surgery, 309
Before surgery (premedication) 309
Anxiolysis and amnesia. 309
Analgesia 309
Timing. 309
Gastric contents. 309
During surgery. 309
Induction 309
Maintenance 310
After surgery 310
Relief of pain 310
Postoperative nausea and vomiting 310
Some special techniques 310
Dissociative anaesthesia 310
Sedation and amnesia 310
Entonox, 310
Methoxyflurane, 310
Pharmacology of anaesthetics 310
Mode of action 311
Inhalation anaesthetics 311
Pharmacokinetics (volatile liquids, gases) 311
Nitrous oxide 311
Advantages. 311
Disadvantages. 311
Uses. 311
Dosage and administration. 311
Contraindications. 312
Precautions. 312
Adverse effects. 312
Halogenated anaesthetics 312
Isoflurane 312
Respiratory effects. 312
Cardiovascular effects. 312
Other effects. 312
Sevoflurane 312
Desflurane 312
Halothane 312
Oxygen in anaesthesia 313
Intravenous anaesthetics 313
Pharmacokinetics 313
Propofol 313
Central nervous system. 313
Cardiovascular system. 313
5 Cardiorespiratory and renal systems 391
22 Cholinergic and antimuscarinic (anticholinergic) mechanisms and drugs 392
Synopsis 392
Cholinergic drugs (cholinomimetics) 392
Classification 392
Direct-acting (receptor agonists) 392
Indirect-acting 393
Sites of action (see Fig. 22.1) 393
Pharmacology 393
Autonomic nervous system 393
Parasympathetic division. 393
Sympathetic division. 394
Neuromuscular (voluntary) junction 394
Central nervous system 394
Blood vessels 394
Choline esters 394
Acetylcholine 394
Other choline esters 394
Alkaloids with cholinergic effects 395
Nicotine 395
Pilocarpine, 395
Arecoline 395
Muscarine 395
Anticholinesterases 395
Physostigmine 395
Neostigmine 396
Pyridostigmine 396
Distigmine 396
Edrophonium 396
Carbaryl 396
Anticholinesterase poisoning 396
Typical features 396
Treatment. 397
Poisoning 397
Disorders of neuromuscular transmission 397
Myasthenia gravis 397
Pathogenesis. 398
Diagnosis. 398
Treatment 398
Excessive dosing 398
Lambert–Eaton syndrome 399
Drug-induced disorders of neuromuscular transmission 399
Antimicrobials. 399
Cardiovascular drugs. 399
Other drugs. 399
Drugs that oppose acetylcholine 399
Antimuscarinic drugs 399
Atropine 399
Exocrine glands. 400
Smooth muscle 400
Ocular effects. 400
Cardiovascular system. 400
Central nervous system. 400
Antagonism to cholinergic drugs. 400
Pharmacokinetics. 400
Dose. 400
Poisoning 400
Other antimuscarinic drugs 400
Hyoscine 401
Hyoscine butylbromide 401
Homatropine 401
Tropicamide 401
Ipratropium 401
Tiotropium 401
Flavoxate 401
Oxybutynin 402
Glycopyrronium 402
Propantheline 402
Dicyclomine 402
Benzhexol 402
Solifenacin, darifenacin 402
Promethazine. 402
Propiverine, 402
Guide to further reading 402
23 Adrenergic mechanisms and drugs 403
Synopsis 403
Adrenergic mechanisms 403
Classification of sympathomimetics 403
By mode of action 403
Tachyphylaxis 404
Interactions of sympathomimetics 404
History. 405
Consequences of adrenoceptor activation 405
Selectivity for adrenoceptors 405
Adrenoceptor agonists (see Table 23.1) 405
α + β effects, non-selective: 405
α1 effects: 405
α2 effects in the central nervous system: 405
β effects, non-selective (i.e. β1 + β2): 405
β1 effects, with some α effects: 405
β1 effects: 405
β2 effects, 405
Adrenoceptor antagonists (blockers) 405
Effects of a sympathomimetic 405
Physiological note. 407
Synthetic non-catecholamines 407
Pharmacokinetics 407
Catecholamines 407
Adverse effects 407
Sympathomimetics and plasma potassium. 408
Overdose of sympathomimetics 408
Individual sympathomimetics 408
Catecholamines 408
Adrenaline/epinephrine 408
Adrenaline/epinephrine is used in anaphylactic shock 408
Accidental overdose 408
Noradrenaline/norepinephrine (chiefly α and β1 effects) 409
Isoprenaline (isoproterenol) 409
Dopamine 409
Dobutamine 409
Dopexamine 409
Non-catecholamines 409
Salbutamol (see also Asthma) 409
Salmeterol 410
Ephedrine 410
Phenylephrine 410
Mucosal decongestants 410
Shock 410
Definition. 410
Treatment 411
Types of shock 411
In poisoning by a cerebral depressant 411
In central circulatory failure 411
Septic shock 411
Choice of drug in shock 412
Monitoring drug use 412
Restoration of intravascular volume 412
Dextran 70 412
Gelatin products 412
Etherified starch. 412
Chronic orthostatic hypotension 412
Detrusor relaxation for urinary frequency, urgency and urge incontinence 413
Guide to further reading 414
24 Arterial hypertension, angina pectoris, myocardial infarction and heart failure 415
Synopsis 415
Hypertension: how drugs act 415
Angina pectoris: how drugs act 416
Drugs used in hypertension and angina 416
Diuretics (see also Ch. 27) 416
Vasodilators 416
Organic nitrates 416
Pharmacokinetics. 417
Tolerance 417
Uses. 417
Adverse effects. 417
Interactions. 417
Glyceryl trinitrate (see also above) 417
For prophylaxis, 418
Venepuncture. 418
Isosorbide dinitrate 418
Isosorbide mononitrate 418
Pentaerithrityl tetranitrate 418
Calcium channel blockers 418
Vascular smooth muscle cells. 418
Pharmacokinetics. 418
Indications for use 418
Adverse effects. 419
Interactions 419
Individual calcium channel blockers 419
Nifedipine 419
Amlodipine 419
Verapamil 419
Diltiazem 420
Nimodipine 420
Other members 420
Angiotensin-converting enzyme (ACE) inhibitors, angiotensin (AT) II receptor blockers (ARBs) and renin inhibitors 420
Uses 420
Hypertension. 420
Cardiac failure 420
Diabetic nephropathy. 421
Myocardial infarction (MI). 421
Cautions 421
Adverse effects 421
ACE inhibitors: 421
ARBs 422
6 Blood and neoplastic disease 511
29 Drugs and haemostasis 512
Synopsis 512
Introduction 512
The coagulation system 512
Procoagulant drugs 513
Vitamin K 513
Phytomenadione 514
Menadiol 514
Vitamin K is used to treat the following: 514
Coagulation factor concentrates 514
Use of coagulation factor concentrates 514
Desmopressin (DDAVP) 515
Adverse effects. 515
Other agents 515
Adrenaline/epinephrine 515
Fibrin glue 515
Sclerosing agents 515
Anticoagulant drugs 515
Oral vitamin K antagonists (VKA) 516
Pharmacokinetics. 516
Pharmacodynamics. 516
Dose. 516
Adverse effects. 517
Withdrawal of oral anticoagulant therapy. 517
Reversal of anticoagulation 517
Drug interactions. 517
Analgesics. 517
Antimicrobials. 517
Anticonvulsants. 517
Antiarrhythmics. 517
Antidepressants. 517
Gastrointestinal drugs. 517
Lipid-lowering drugs. 518
Sex hormones and hormone antagonists. 518
Sedatives and anxiolytics. 518
Uses of oral VKA 518
Surgery in patients receiving oral VKA 518
Elective surgery. 518
Emergency surgery. 518
Dental extractions. 518
Other vitamin K antagonists 518
Oral direct thrombin and factor Xa inhibitors 518
Dabigatran 518
Rivaroxaban, apixaban and edoxaban 519
Parenteral anticoagulants 519
Heparin 519
Pharmacokinetics. 520
Pharmacodynamics. 520
Monitoring heparin therapy. 520
Adverse effects. 520
Heparin reversal. 521
Use of heparin 521
Treatment of established venous thromboembolism. 521
Prevention of venous thromboembolism. 521
Cardiac disease. 521
Peripheral arterial occlusion. 521
Other anticoagulant drugs 521
Anticoagulant drugs under development 521
Fibrinolytic (thrombolytic) system 522
Plasminogen activators 522
Fibrinolysis inhibitors. 522
Drugs that promote fibrinolysis 522
Uses of thrombolytic drugs 523
Vascular occlusion 523
Adverse effects. 523
Drugs that prevent fibrinolysis 523
Tranexamic acid 523
Aprotinin 523
Platelet function 523
Drugs that inhibit platelet activity (antiplatelet drugs) 524
Aspirin 524
Dipyridamole 524
Clopidogrel 524
Prasugrel 524
Ticagrelor. 524
Epoprostenol 525
Glycoprotein (GP) IIb–IIIa antagonists 525
Abciximab 525
Eptifibatide 525
Adverse effects. 525
Uses of antiplatelet drugs 525
Guide to further reading 527
30 Red blood cell disorders 528
Synopsis 528
Iron 528
Iron deficiency 529
Management of iron deficiency and prophylactic iron administration 530
Oral iron preparations 530
Liquid iron formulations 530
Sustained or slow-release iron preparations 530
Adverse effects 530
Parenteral iron 530
Adverse effects 531
Drug interactions 531
Anaemia of chronic disease 531
Functional iron deficiency 532
Chronic iron overload 532
Parenteral iron chelator. 532
Oral iron chelators. 532
Deferiprone 532
Deferasirox. 532
Iron poisoning and acute overdose 532
Vitamin B12 533
Vitamin B12 deficiency 533
Management of vitamin B12 deficiency and prophylactic administration 534
Contraindications to cobalamin 535
Folic acid (pteroylglutamic acid) 535
Folic acid deficiency 535
Management of folic acid deficiency and prophylactic administration 536
Haemolytic anaemia 536
Autoimmune haemolytic anaemia 536
Drug-induced haemolytic anaemia 536
Glucose-6-phosphate dehydrogenase deficiency 537
Haemoglobinopathies 538
Sickle cell anaemia 538
Thalassaemia 538
Aplastic anaemia 538
Polycythaemia vera 539
Management of PV 539
Haemopoietic growth factors 540
Erythropoiesis-stimulating agents 540
Clinical uses of ESAs 540
Anaemia of chronic renal failure. 540
Anaemia due to cancer chemotherapy. 540
Other clinical uses of EPO. 540
Adverse effects 540
Granulocyte colony-stimulating factor 541
Adverse effects 541
Thrombopoietin receptor agonists 541
Guide to further reading 541
31 Neoplastic disease and immunosuppression 543
Synopsis 543
Neoplastic disease 543
Cancer treatments and outcomes 543
Systemic cancer therapy 544
Rationale for cytotoxic chemotherapy 545
Classes of cytotoxic chemotherapy drugs 545
Adverse effects of cytotoxic chemotherapy 548
Nausea and vomiting 548
Suppression of bone marrow and the lymphoreticular system. 548
Opportunistic infection 548
Diarrhoea and mouth ulcers 548
Alopecia 548
Urate nephropathy 548
Local extravasation 548
Hypersensitivity reactions 548
Specific organ damage 548
Delayed wound healing 548
Germ cells and reproduction 548
Carcinogenicity 548
Classes of cytotoxic agents 549
Alkylating agents 549
Antimetabolites 549
Anthracyclines and related compounds 549
Topoisomerase inhibitors 549
Spindle poisons 549
Platinum drugs 549
Miscellaneous agents 550
Chemotherapy in clinical practice 550
Drug use and tumour cell kinetics 550
Cytotoxic drugs 550
The selection of drugs 550
Drug resistance 551
Resistance 551
Multiple drug resistance 551
Improving efficacy of chemotherapy 551
Hazards to staff handling cytotoxic agents 551
A note of caution. 552
Interactions of anticancer agents with other drugs 552
Endocrine therapy 552
Hormonal influence on cancer 552
Hormonal agents 552
Breast cancer 552
Prostatic cancer 553
Benign prostatic hypertrophy 553
Adrenocortical steroids 553
In general, 553
Immunotherapy 553
ATRA 554
Development of anticancer drug therapy 554
Targeted biological therapies 555
Passive immunotherapy using monoclonal antibodies raised against specific tumour-associated antigens on the cell surface 555
Radioimmunotherapy 555
Chemo-immunotherapy 556
Signal transduction inhibitors 556
Targeting the cell cycle 557
Protease inhibition 557
Chemoprevention of cancer 557
Viral immunisation and cancer prevention 558
Immunosuppression 558
Ciclosporin 558
Pharmacokinetics. 558
Uses. 558
Adverse reactions. 559
Interactions. 559
Tacrolimus 559
Antilymphocyte immunoglobulin 559
Mycophenolate 559
Hazards of immunosuppressive drugs 559
Carcinogenicity 559
Active immunisation during immunosuppressive therapy 559
Guide to further reading 560
7 Gastrointestinal system 561
32 Oesophagus, stomach and duodenum 562
Synopsis 562
The oesophagus in health and disease 562
Gastric acid secretion and mucosal protection 562
Gastric acid secretion 563
Gastrin 563
Acetylcholine (ACh) 563
Histamine 563
Prostaglandins 563
Mucosal protective mechanisms 563
Helicobacter pylori (H. pylori): an occasionally silent killer 563
NSAIDs: enemies of the gut 563
Drugs affecting oesophageal motility and the lower oesophageal sphincter 564
Drugs to reduce or neutralise gastric acid 564
Proton pump inhibitors (PPIs) 564
Pharmacology. 564
Pharmacokinetics. 564
Adverse reactions and interactions. 565
H2-receptor antagonists (H2RAs) 565
Pharmacology. 565
Pharmacokinetics and dosage. 565
Adverse effects and interactions. 565
Antacids 565
Individual antacids 565
Other targets for acid suppression 565
Drugs to enhance mucosal protection 566
Sucralfate (SUCRose sulFATE and ALuminium hydroxide complex) 566
Adverse effects and interactions. 566
Bismuth chelate (tripotassium dicitratobismuthate, bismuth sub-citrate) 566
8 Endocrine system, metabolic conditions 593
35 Adrenal corticosteroids, antagonists, corticotropin 594
Synopsis 594
Adrenal steroids and their synthetic analogues 594
Mechanism of action 595
On inorganic metabolism. 595
On organic metabolism 595
Individual adrenal steroids 598
Hydrocortisone 599
Prednisolone 599
Methylprednisolone 599
Fluorinated corticosteroids (triamcinolone, fludrocortisone) 599
Triamcinolone 599
Fludrocortisone 599
Dexamethasone and betamethasone 599
Aldosterone 599
Spironolactone 599
Beclometasone, budesonide, fluticasone, mometasone and ciclesonide 599
Pharmacokinetics of corticosteroids 599
Dosage schedules 600
Adverse effects of systemic adrenal steroid pharmacotherapy 600
Endocrine. 600
Musculoskeletal. 600
Immune. 600
Gastrointestinal. 600
Central nervous system. 600
Ophthalmic effects 600
Other effects 600
Adrenal steroids and pregnancy 600
Precautions during chronic adrenal steroid therapy 601
Treatment of intercurrent illness 601
Dosage and routes of administration 601
Systemic commencing doses: 601
Topical applications 602
Contraindications 602
Long-term use of adrenal steroids in children 602
Uses of adrenocortical steroids 602
Replacement therapy 602
Acute adrenocortical insufficiency (Addisonian crisis) 602
Chronic primary adrenocortical insufficiency (Addison’s disease) 602
Chronic secondary adrenocortical insufficiency 603
Iatrogenic adrenocortical insufficiency: abrupt withdrawal 604
Pharmacotherapy 604
Suppression of adrenocortical function 604
Use in inflammation and for immunosuppression 604
Further specific uses 604
Use in diagnosis. 605
Withdrawal of pharmacotherapy 605
Inhibition of synthesis of adrenal and other steroid hormones 606
Competitive antagonism of adrenal steroids 606
Adrenocorticotrophic hormone (ACTH) (corticotropin) 606
Natural corticotropin 606
Synthetic corticotropins 606
Actions 606
The effects 607
Uses. 607
Diagnostic use 607
Therapeutic use 607
Preparations 607
Guide to further reading 607
36 Diabetes mellitus, insulin, oral antidiabetes agents, obesity 608
Synopsis 608
Diabetes overview 608
History of insulin therapy in diabetes 608
Sources of insulin 609
Insulin receptors 609
Actions of insulin 610
Uses 610
Pharmacokinetics 610
Preparations of insulin (Table 36.1) 610
Notes for prescribing insulin 613
Allergy 613
Antibodies 613
Compatibility. 613
Intravenous insulin. 613
The standard strength 613
Choice of insulin regimen 613
Dose and injection technique 613
Adverse effects of insulin 614
Hypoglycaemia 614
Non-insulin antidiabetes drugs 615
(i) Insulin secretagogues 615
Meglitinides 615
Incretin analogues and mimetics. 615
Dipeptidyl peptidase-4 (DPP-4) inhibitors. 616
(ii) Insulin sensitisers 616
Biguanides 616
Thiazolidinediones. 617
(iii) Agents that increase urinary glucose excretion 617
SGLT-2 inhibitors. 617
(iv) Agents which reduce glucose absorption 617
Acarbose 617
Antidiabetics and cardiovascular outcome studies. 617
Choice of oral antidiabetic drugs in type 2 diabetes 618
Diet and diabetes 618
Interactions with non-diabetes drugs 618
Adrenal steroids, 619
Growth hormone 619
Oral contraceptives 619
Thyroid hormone 619
Drug-induced diabetes 619
Diazoxide 619
Pregnancy and diabetes 619
Surgery in diabetic patients 619
Principles of management 619
Type 1 diabetes 619
Elective major surgery 620
Minor surgery/procedures 620
Emergency surgery 620
Type 2 diabetes 620
Diabetic ketoacidosis 620
Intravenous fluid. 620
Soluble insulin 620
Potassium. 620
Bicarbonate 621
Success in treatment 621
Euglycaemic ketoacidosis 621
Diabetic ketosis without acidosis. 621
Ketosis-prone type 2 diabetes (“Flatbush diabetes”). 621
Hyperosmolar Hyperglycaemic State (HHS) 621
Preventing complications other than by glucose lowering 621
Obesity and appetite control 622
Orlistat 623
Adverse effects 623
Leptin 623
Newer agents 623
GLP-1 agonist 623
Lorcaserin 623
Obesity and diabetes 623
Guide to further reading 624
37 Thyroid hormones, antithyroid drugs 625
Synopsis 625
Thyroid hormones 625
Calcitonin. 625
Physiology and pharmacokinetics 625
T4 (levothyroxine). 625
T3 (liothyronine) 626
Pharmacodynamics 626
Levothyroxine for hypothyroidism 626
Treatment of hypothyroidism 626
Levothyroxine tablets 626
Liothyronine tabs. 626
Subclinical hypothyroidism. 626
Adverse effects 627
In pregnancy 627
Antithyroid drugs and hyperthyroidism 627
Thionamides (thiourea derivatives) carbimazole, methimazole, propylthiouracil 627
Mode of action (Fig. 37.1) 627
Carbimazole and methimazole 628
Propylthiouracil 628
Immunosuppression 628
Doses 628
Use 628
Adverse reactions 628
Pregnancy. 628
Control of antithyroid drug therapy 629
β-Adrenergic blockade. 629
Iodine (iodide and radioactive iodine) 629
Effects 629
Uses 629
Potassium iodate 629
As an antiseptic 630
Bronchial secretions. 630
Organic compounds 630
Adverse reactions 630
Symptoms of iodism 630
Radioiodine (131I) 630
Risks 630
Radioisotope tests 631
Preparation for surgery 631
Thyroid storm 631
Graves’ ophthalmopathy 631
Treatment of subclinical hyperthyroidism 632
Drugs that cause hypothyroidism 632
Drugs causing either hyper- or hypothyroidism 632
Amiodarone 632
Biological therapies 633
Miscellaneous 634
Treatment of thyroiditis 634
Calcitonin. 634
Guide to further reading 634
38 Hypothalamic, pituitary and sex hormones 635
Synopsis 635
Hypothalamic and anterior pituitary hormones 635
Corticotropin-releasing hormone (CRH) 635
Adrenocorticotrophic hormone (ACTH) 635
Thyrotrophin-releasing hormone (TRH) 636
Thyroid-stimulating hormone (TSH) thyrotrophin, 636
Sermorelin 636
Octreotide 636
Growth hormone, somatrophin 636
Pegvisomant 637
Gonadotrophin-releasing hormone (GnRH), 637
Follicle-stimulating hormone (FSH) 637
Chorionic gonadotrophin 637
Prolactin 637
Hypopituitarism 638
Posterior pituitary hormones and analogues 638
Vasopressin: antidiuretic hormone (ADH) 638
Desmopressin 639
Diabetes insipidus: vasopressin deficiency 639
Desmopressin replacement therapy 639
Syndrome of inappropriate antidiuretic hormone secretion (SIADH) 639
Emergency treatment of hyponatraemia 640
Oxytocin. 640
Sex (gonadal) hormones and antagonists: steroid hormones 640
Steroid hormone receptors 640
Selectivity. 640
Pharmacokinetics. 640
Androgens 640
Indications for androgen therapy 641
Preparations and choice of androgens 641
Oral preparations 641
Parenteral preparations 641
Transdermal preparations 641
Buccal preparations 641
Testosterone implants 641
Adverse effects 641
Antiandrogens (androgen antagonists) 642
Cyproterone 642
Uses. 642
Anabolic steroids 642
Oestrogens 642
Pharmacokinetics 642
Preparations of oestrogens 643
Choice of oestrogen 643
Oestrogen formulations and routes of administration 643
Oral. 643
Transdermal 643
Subcutaneous implants. 643
Vaginal (ring, cream, tablet or pessary). 643
Others. 643
Indications for oestrogen therapy 643
Replacement therapy in hypo-oestrogenaemia 643
Post-menopausal hormone replacement therapy (HRT) 643
Preparations used for HRT. 644
Contraception. 644
Adverse effects of HRT. 644
Contraindications 644
Anti-oestrogens 644
Clomifene 644
Cyclofenil 645
Tamoxifen 645
Progesterone and progestogens 645
Uses 645
Preparations 645
Adverse effects 645
Antiprogestogens 645
Mifepristone 646
Other progesterone derivatives 646
Gestrinone 646
Fertility regulation 646
Infertility 646
For women, 646
For men, 646
Polycystic ovary syndrome (PCOS) 646
Contraception by drugs and hormones 647
Hormonal contraception in women 647
Combined contraceptives (the ‘pill’) 647
Combined oestrogen–progestogen 647
Important aspects 647
Subsequent fertility. 647
Effect on an existing pregnancy. 647
Carcinomas 647
The effect on menstruation 647
Libido 648
Cardiovascular complications. 648
Major surgery 648
Plasma lipoproteins 648
Plasma proteins. 648
Other adverse effects 648
Absolute contraindications 648
Relative contraindications 648
Duration of use 649
Benefits additional to contraception 649
Formulations of oestrogen–progestogen combination 649
Oestrogen: 649
Progestogen 649
Combined oral contraceptives 649
Choice of oestrogen–progestogen combination 649
Common problems 649
Missed pill. 649
Intercurrent gut upset. 649
Changing of preparation. 649
Breakthrough bleeding 649
Progestogen-only contraception 649
Postcoital (‘morning after pill’) and emergency contraception 650
Progestogen-only treatment 650
Drug interaction with steroid contraceptives 650
Enzyme induction. 650
Hypothalamic/pituitary hormone approach to contraception 650
Other methods of contraception 650
Copper intrauterine devices 650
The intrauterine levonorgestrel system 651
Vaginal preparations, 651
Oil-based lubricants 651
Risks of contraception in relation to benefit 651
Menstrual disorders 651
Amenorrhoea, 651
Menorrhagia 651
The timing of menstruation. 651
Endometriosis. 651
Dysmenorrhoea 652
Premenstrual tension syndrome 652
Cyclical breast pain 652
Myometrium 652
Oxytocics 652
Oxytocin 652
Ergometrine 653
Prostaglandins 653
Dinoprost 653
Gemeprost 653
Carboprost 653
Induction of abortion 653
Induction and augmentation of labour 653
Prevention and treatment of uterine haemorrhage 653
Uterine relaxants 654
Guide to further reading 654
39 Vitamins, calcium, bone 655
Synopsis 655
Vitamin A: retinol 655
Therapeutic uses 655
Psoriasis 656
Acne 656
Acute promyelocytic leukaemia 656
Vitamin A deficiency 656
Adverse effects 656
Teratogenicity. 656
Vitamin B complex 656
Thiamine (B1). 656
Cobalamins (B12). 656
Folic acid. 656
Pyridoxine (B6) 656
Niacin (nicotinic acid, B3) 656
Vitamin C: ascorbic acid 657
Indications 657
Scurvy 657
Methaemoglobinaemia 657
Adverse effects 657
Vitamin D, calcium, parathyroid hormone, calcitonin, bisphosphonates, bone 657
Vitamin D 657
Pharmacokinetics 659
Actions 659
Indications 659
Vitamin D deficiency 659
Osteoporosis 660
Hypoparathyroidism 660
Psoriasis 660
Renal osteodystrophy 660
Prevention of acute respiratory tract infections 660
Index 667
A 667
B 672
C 674
D 678
E 681
F 682
G 683
H 684
I 686
J 688
K 688
L 688
M 689
N 691
O 693
P 694
Q 698
R 698
S 699
T 702
U 704
V 704
W 705
X 705
Y 705
Z 705
Inside Back Cover ibc1