Antibacterial Drugs Today

174 Pages·1979·3.57 MB·English

by  A. P. Ball, J. A. Gray

Antibacterial Drugs Today
Antibacterial Drugs Today
A .P. Ball, * J.A. Gray t and J.McC. Murdoch t
• Department of Medicine (Sub-department of Communicable and Tropical Diseases)
The University of Birmingham. England
t Infectious Diseases Unit. City Hospital. Greenbank Drive. Edinburgh EH I 0 5SB. Scotland
~~ MTPPRESS LIMITED International Medical Publishers
Antibacterial Drugs Today
Published in UK, Europe and Middle East
by MTP Press Limited
Falcon House
Lancaster
England
Second Edition
ISBN 978-0-85200-505-7 ISBN 978-94-011-8004-7 (eBook)
DOT 10.1007/978-94-011-8004-7
~ MTPPRESS LIMITED International Medical Publishers
© Copyright 1978 by ADIS Press
All rights reserved including that of translation into other languages. No part of this book
may be reproduced or transmitted in any form or by any means, electronic or mechanical, in-
cluding photocopying, recording, or any information storage and retrieval system, without
permission in writing from ADIS Press.
Preface
Since the first edition there has been a great demand for this book. It has been
revised to include up-to-date and new entries covering recent additions to the availa-
ble drugs. As well there are now sections on clinical situations, or types of patient,
presenting especial problems. The authors hope this new material will enhance the
effectiveness of the book as a guide to this rapidly advancing and changing therapeutic
situation.
A.P.B.
J.A.G.
J.McC.M.
July, 1978
v
Contents
I. Antibacterial Drugs
1.1 Mechanisms of Action
I .2 Side Effects and Toxicity 2
2. The Sulphonamides .............................. . 2
2.1 Antibacterial Activity .... 2
2.2 Mode of Antibacterial Action
2.3 Pharmacology 3
2.4 Therapeutic Indications ... 4
2.5 Dosage ....................... . 4
2.5.1 Short Acting Sulphonamides ..................... . 4
2.5.2 Long Acting Sulphonamides 5
2.5.3 Non-absorbable Sulphonamides 5
2.6 Side Effects and Toxicity 5
2.6.1 Nephrotoxicity ............................... . 5
2.6.2 Haematological Abnormalities 5
2.6.3 Pulmonary Disease .. . 5
2.6.4 Hypersensitivity .................................................. . 6
2.7 Drug Interactions ... 6
3. The Natural Penicillins - Benzylpenicillin (Penicillin G) and Phenoxymetbylpeni-
cillin (Penicillin V) .......................... . ..................... . 6
3. I Physicochemical Properties 8
3.2 Mode of Antibacterial Action ... 8
3. 3 Antibacterial Activity ..... . 9
3.3. I Activity Against Streptococci 9
3.3.2 Activity Against Staphylococci 9
3.3.3 Activity Against Other Organisms 10
3.4 Pharmacology 10
3.4.1 Penicillin G 10
3.4.2 Benzatbine and Procaine Salts of Penicillin G II
3.4.3 Penicillin V ..................... . II
3.5 Therapeutic Indications . 12
3.5. I Streptococcal Infections .. 12
3.5.2 Meningococcal Infections 12
3.5.3 Gonorrhoea 12
3.5.4 Other Infections 13
3.6 Dosage ...................................... . 13
3.6.1 Penicillin G .................................................................................. . 13
3.6.2 Procaine and Benzathine Penicillin .................................................. . 13
3.6.3 Penicillin V ........................................ . ............................................ . 13
3.7 Side Effects and Toxicity 15
3.7.1 Neurotoxicity 15
viii Contents
3.7.2 Nephritis ............................ . 15
3.7.3 Haemolysis 15
3.7.4 Hypersensitivity 15
3.7.5 Side Effects of Penicillin V 18
4. The Semi-synthetic Penicillins . 18
4.1 Phenoxy penicillins 18
4.2 Penicillinase Resistant Penicillins 19
4.2.1 Methicillin 19
4.2.2 Isoxazolyl Penicillins 20
4.3 Other Penicillina~e Resistant Penicillins 21
4.4 Broad Spectrum Penicillins 21
4.4.1 Ampicillin 21
4.4.2 Amoxycillin 24
4.4.3 Epicillin 25
4.4.4 Hetacillin. Pivampicillin and Talampicillin . 25
4.4.5 Carbenicillin ......................................................................................... . 25
4.4.6 Carindacillin (Indanyl Carbenicillin) .. 26
5. Mecillinam and Pivmecillinam ................................ . 26
5.1 Antibacterial Activity 26
5.2 Mode of Action ............... . 27
5.3 Pharmacology . 27
5.4 Indications 28
5.5. Dosage . 28
5.6 Side Effects 29
6. Co-trimoxazole (Trimethoprim-sulphamethoxazole) 29
6.1 Antibacterial Activity .................................................... . 29
6.1.1 Gram-positive Bacteria. 29
6.1.2 Gram-negative Bacteria 29
6.1.3 Miscellaneous 30
6.2 Mode of Action ........................................ . 30
6.3 Pharmacology 31
6.4 Indications 32
6.4.1 Urinary Tract Infections. 32
6.4.2 Bacteraemic Syndromes 32
6.4.3 Gonorrhoea 33
6.4.4 Chest Infections 33
6.4.5 Enteric Fever 33
6.4.6 Brucellosis 33
6.4.7 Miscellaneous 33
6.5 Dosage .................... . 34
6.6 Contraindications 34
6.7 Side Effects and Toxicity 34
6.7.1 Haematological Abnormalities 34
6.7.2 Hypersensitivity 35
6.7.3 Nephrotoxicity 35
6.8 Drug Interactions 35
7. Chloramphenicol 35
7. I Therapeutic Indications 36
7. I . I Enteric Fever 36
7.1.2 Other Indications 36
ix
Contents
8. The Tetracycl ines 37
8.1 Antibacterial Activity 37
8.1.1 Spectrum of Activity 37
8.1.2 Development of Resistance 38
8.2 Pharmacology. 38
8.3 Therapeutic Indications 38
8.4 Side Effects and Toxicity 39
8.4.1 Tooth Discoloration 40
8.4.2 Renal Toxicity 40
8.4.3 Liver Toxicity .. 40
9. The Macrolides 40
9. I Erythromycin 41
9.1.1 Physicochemical Properties 41
9.1.2 Antibacterial Activity 41
9.1.3 Pharmacology .. 42
9.1.4 Therapeutic Indications 43
9. 1.5 Dosage 43
9. I .6 Side Effects and Toxicity 43
9.2 Spiramycin and Triacetyloleandomycin 44
10. Lincomycin and Clindamycin 44
10.1 Mode of Action 44
10.2 Antibacterial Activity 45
10.3 Pharmacology .. 45
10.4 Therapeutic Indications 45
10.5 Dosage 46
10.6 Side Effects and Toxicity 46
II. Fusidic Acid (Sodium Fusidatel 46
11.1 Mode of Action 47
11.2 Antibacterial Activity 47
I 1.3 Pharmacology . 47
11.4 Therapeutic Indications 47
11.5 Dosage ...................... . 48
11.6 Side Effects and Toxicity 48
12. The Urinary Antiseptics 48
12.1 Nitrofurantoin 48
12.1.1 Physicochemical Properties 49
12.1.2 Antibacterial Activity.. ...................... ..... .. .............. . 49
12. 1.3 Pharmacology 49
12.1.4 Therapeutic Indications 50
12.1.5 Dosage 50
12. I. 6 Side Effects and Toxicity 50
12.2 Nalidixic Acid 51
12.2.1 Antibacterial Activity 51
12.2.2 Pharmacology .. 51
12.2.3 Therapeutic Indications and Dosage 52
12.2.4 Side Effects and Toxicity 52
12.3 Oxolinic Acid ........................ . 52
13. Cephalosporins .... 53
I 3. I Cephaloridine 54
13.1.1 Antibacterial Activity 54
Content~
13.1.2 Pharmacology .................................................................................................. 54
13.1.3 Indications .................................................................................................... . 54
13.1.4 Dosage 55
I 3. 1.5 Side Effects and Toxicity ............................................................................... . 55
13.2 Cephalothin ............................................................................................................... . 56
13.2.1 Dosage ........................................................................................................... . 56
13.3 Cephalexin ................................................................................................................. . 56
13.4 Cephradine ................................................................................................................. . 57
13.5 The Cephamycins ....................................................................................................... . 57
I 3. 5. I Cefoxitin ......................................................................................................... . 58
13.6 Newer Cephalosporin Derivatives ............................................................................. . 58
14. Peptide Antibiotics (Polymyxin B and Polymyxin E) ........................................................... . 59
14.1 Antibacterial Activity ............ ..................................................................................... . 59
14.2 Pharmacology ........ ..................................................................................................... . 59
14.3 Therapeutic Indications and Dosage ........................................................................... . 60
14.3.1 Topical Therapy ............................................................................................. . 60
14.3.2 Parenteral Therapy ......................................................................................... . 60
14.3.3 Intrathecal Therapy ....................................................................................... . 61
14.3.4 Oral Therapy ................................................................................................ . 61
14.4 Side Effects and Toxicity ........................................................................................... . 61
14.4.1 Neurotoxicity ................................................................................................. . 61
14.4.2 Nephrotoxicity ............................................................................................... . 61
15. The Aminoglycosides .......................................................................................................... . 62
15.1 Streptomycin ............................................................................................................. . 62
15.1.1 Antibacterial Activity ..................................................................................... . 63
15. 1.2 Pharmacology ................................................................................................. . 63
15.1.3 Indications ..................................................................................................... . 63
15.1.4 Dosage ........................................................................................................... . 65
15.1.5 Side Effects and Toxicity ............................................................................... . 65
15.2 Kanamycin ................................................................................................................. . 65
15.2.1 Antibacterial Activity ..................................................................................... . 66
15.2.2 Pharmacology ................................................................................................. . 66
15.2.3 Indications ................................................................................................... . 67
15.2.4 Dosage ........................................................................................................... . 67
15.2.5 Side Effects and Toxicity ............................................................................... . 68
15.3 Gentamicin ................................................................................................................ . 70
15.3.1 Antibacterial Activity ..................................................................................... . 70
15.3.2 Pharmacology ................................................................................................. . 71
15.3.3 Indications ..................................................................................................... . 72
15.3.4 Dosage ........................................................................................................... . 73
15.3.5 Side Effects and Toxicity ............................................................................... . 73
15.4 Tobramycin ............................................................................................................... . 74
15.4.1 Antibacterial Activity ..................................................................................... . 74
15.4.2 Pharmacology ................................................................................................. . 75
15.4.3 Indications ..................................................................................................... . 76
15.4.4 Dosage ........................................................................................................... . 76
15.4.5 Side Effects and Toxicity ............................................................................... . 77
15.5 Neomycin. Framycetin and Paromomycin ................................................................. . 77
15.5.1 Antibacterial Activity ................................................................................... .. 77
15.5.2 Pharmacology ................................................................................................. . 78
Content~ xi
15.5.3 Indications .............................................. . 78
15.5.4 Side Effects and Toxicity 79
15.6 Newer Aminoglycosides ... 79
15.6.1 Sissomicin 79
15.6.2 Amikacin 79
15.6.3 Netilmicin 80
16. Metronidazole ................ .. 80
16.1 Antibacterial Activity 81
16.2 Mode of Action ... 81
16.3 Pharmacology ....... 81
16.4 Therapeutic Indications .............. .. 81
16.4.1 Intra-abdominal Sepsis and Wound Infections 82
16.4.2 Gynaecological Surgery 82
16.4.3 General Anaerobic Sepsis 82
16.4.4 Protozoal Infection .. . 82
16.5 Dosage ................................. .. 82
16.6 Toxicity and Interactions ..................... .. 83
17. Antituberculosis Drugs 83
I 7. I Isoniazid 83
17.1.1 Toxicity 83
17.2 Rifampicin 83
17.3 Ethambutol .............................................. . 84
17.4 Streptomycin .................................................. . 84
17.4.1 Pharmacology 84
17.4.2 Dosage ...................... . 84
17.4.3 Toxicity .. " ................ .. 84
17.5 Para-aminosalicylic Acid (PAS) 85
17.5.1 Toxicity 85
17.6 Capreomycin .................................................... .. 86
17.7 Other Drugs ................................................ .. 86
18. Chemotherapy of Gram-negative Bacillary Infections ............ . 86
18. I General Considerations ... 86
18.2 Organisms 87
18.3 Choice of Antibacterial Agents 88
18.4 Routes of Administration and Duration of Therapy 88
18.5 Precautions ................................................ . 88
18.6 Specific Infections .................... . 89
18.6.1 Urinary Tract Infections .......... . 89
18.6.2 Gastrointestinal Infections .............. .. 90
18.6.3 Biliary Tract Infections ........ . 91
18.6.4 Respiratory Tract Infections .................................... .. 91
18.6.5 Endocarditis .................................................................. . 92
18.6.6 Meningitis ............................... .. 93
19. Anaerobic Infections .............................................. .......................... 93
19.1 Clostridial Infections .................................................................................................. 93
19.2 Non-clostridial Anaerobic Infections .......................................................................... 94
19.2.1 Pulmonary Infection ........................................................................................ 94
19.2.2 Cerebral Abscess ............................................................................................ 95
19.2.3 Intra-abdominal Sepsis .................................................................. 95
19.2.4 Female Genital Tract Infection ......................................................... 96
xii Content~
19.2.5 Other Infections 97
20. Antibacterial Therapy in Renal and Hepatic Disease 97
20. I Renal Disease 98
20.1.1 Sulphonamides 98
20.1.2 Penicillins 99
20.1.3 Co-trimoxazole 99
20.1.4 Chloramphenicol 99
20.1.5 Tetracyclines. 99
20.1.6 Macrolides 100
20.1.7 Lincomycin and Ciindamycin 100
20.1.8 Fusidic Acid 100
20.1.9 Nitrofurantoin 100
20.1 10 Nalidixic Acid 100
20.1.11 Cephalosporins 100
20.1 12 Peptide Antibiotics 101
20.1 13 Aminoglycosides 101
20.1 14 Cycloserine. 101
20.1 15 Antituberculosis Drugs. 102
20.2 Hepatic Disease 102
20.2.1 Drugs Causing Hepatocellular Damage 102
20.2.2 Drugs Causing Hepatitis-like Reactions 103
20.2.3 Drugs Causing Cholestasis 103
20.2.4 Drugs Mainly Metabolised or Detoxicated in the Liver 103
21. Antibacterial Therapy in Infant~ and Children 105
21. I General Considerations 105
21.2 Dosage 106
21.3 Clinical Pharmacology in Premature Infants and the Newborn . 107
21.3.1 Protein Binding 107
21.3.2 Metabolism and Detoxication 107
2 I. 3.3 Renal Excretion 108
21.3.4 Genetic Factors 108
21.4 Special Considerations with Individual Drugs 108
21.4. I Sulphonamides 109
21.4.2 The Penicillins 109
21.4.3 Co-trimoxazole 112
21.4.4 Chloramphenicol 113
21.4.5 Tetracyclines. 113
21.4.6 Macrolides 114
21.4.7 Novobiocin . 114
21.4.8 Lincomycin and Clindamycin 114
21.4.9 Fusidic Acid 114
21.4.10 Nitrofurantoin 114
21 .4. II Nalidixic Acid 114
21.4.12 Cephalosporins 115
21.4.13 Polypeptide Antibiotics .. 115
21.4.14 Aminoglycosides 115
21.4.15 Hexachlorophane 116
21.5 Specific Infections in Infant~ 116
21.5.1 Congenital Syphilis. 116
21.5.2 Gonococcal Ophthalmia 116