DRUGS

G L David Krupadanam • D Vijaya Prasad

K Varaprasad Rao • K L N Reddy
C Sudhakar

Universities Press
Contents
Preface , vii
1 Introduction 1
1.1 The requirements of an ideal drug 2
1.2 Sources of drugs 3
1.2.1 Plant origin drugs 4
1.2.2 Animal origin drugs 4
1.2.3 Synthetic drugs 5
1.2.4 Biotechnology 7
1.2.5 Human gene therapy 7
1.3 Historical evolution of drugs 8
1.4 Terminology and description of the terms 12
1.4.1 Pharmacology 12
1.4.2 Pharmacy 13
1.4.3 Molecular pharmacology 13
1.4.4 Medicinal chemistry 14
1.4.5 Nomenclature 15
1.5 Pharmacokinetics 17
1.5.1 Absorption 18
1.5.2 Distribution 20
1.5.3 Metabolism 20
1.5.4 Excretion 21
1.6 Pharmacodynamics 21
1.6.1 Receptors 22
1.6.2 Protein receptors 24
1.6.3 DNA as receptors 27
1.7 Metabolites and antimetabolites 27
1.7.1 Metabolites 27
1.7.2 Antimetabolites 29
1.8 Pharmacophore 32
1.9 Bacteriai 33
1.9.1 Structure of a typical bacterial cell 34
1.9.2 Gram stain 35
1.9.3 Importance of bacteria 36
1.10 Fungi . 37
1.11 Viruses 39
1.12 Mutations 42
Pharmacodynamic agents 43
2.1 Classification of drugs-criteria 43
2.2 Structure-activity relationship (SAR) in drugs . 45
iv Drugs

2.3 Drugs acting on the central nervous system (CNS) 50

2.3.1 Non-selective CNS depressants 51
2.3.1.1 Anaesthetics 51
2.3.1.2 Sedatives and hypnotics - 54
2.3.1.3 Antipyretics 56
2.3.1.4 Analgesics 57
2.3.2 Non-selective CNS stimulants 59
2.3.2.1 Analeptics 60
2.3.2.2 Anxiolytics 60
2.3.2.3 Antidepressants 61
2.3.2.4 Psychotomimetics (Hallucinogens) 61
2.3.3 Selective modifiers of CNS 62
2.3.3.1 Anticonvulsants 62
2.3.3.2 Antitussives 63
2.3.3.3 Antiparkinsonian drugs 64
2.3.3.4 Neuroleptics 64
2.4 Drugs acting on the peripheral nervous system (PNS) 65
2.4.1 Sympathetic nervous system 66
2.4A A Adrenergic stimulants 66
2.4.1.2 Adrenergic blocking agents 67
2.4.2 Parasympathetic nervous system 68
2.4.2.1 Cholinergic drugs 68
2.4.2.2 Anticholinergic drugs 69
2.5 Drugs acting on the cardiovascular system 70
2.5.1 Antihypertensive drugs 70
2.5.2 Anti-arrythmic drugs 72.
2.5.3 Cardiotonic drugs 73
2.5.4 Vasodilators 73
2.5.5 Antihypercholesterolemic drugs 74
2.6 Drugs acting on the hematopoietic system 75
2.6.1 Anticoagulant and coagulant drugs 77
2.6.1.1 Anticoagulant drugs 77
2.6.1.2 Coagulant drugs 79
2.6.2 Anti-anemic drugs 80
2.7 Drugs acting on the renal system ^ 81
2.7.1 Nephron 81
2.7.2 Purine or xanthine diuretics 83
2.7.3 Aldosterone inhibitors 83
2.7.4 High-ceiling diuretics or loop diuretics 84
2.7.5 Carbonic anhydrase inhibitors 85
2.7.6 Thiazide diuretics 85
3 Vitamins, hormones and synthetic drugs 92
3:1 Introduction 92
3.2 Vitamins: a class of nutrients 92
3.2.1 Classification of vitamins 93
3.2.2 Structure, biochemical functions 94
3.3 Hormones: the chemical messengers 96
3.4 Svntheitic and natural drues 98
 Contents v

3.5 Synthetic drugs 98

3.5.1 Sulphanilamide: an example of a sulpha drug 98
3.5.2 Paracetamol (Acetaminophen) 101
3.5.3 Aspirin (Acety I salicylic acid) 102
3.5.4 Oil of wintergreen 103
3.5.5 Mephensin: a muscle relaxant 103
3.5.6 Ibuprofen: an anti-inflammatory drug 104
3.5.7 L-dopa - cures Parkinson's disease 106
3.5.8 Albuterol (Salbutamol): a bronchodilator 108
3.5.9 Analgin 110
3.5.10 Metoclopramide: an anti-emetic drug 111
3.5.11 Chloroquine: an antimalarial drug 113
3.5.12 Chlorpromazine: an antipsychotic agent 114
3.5.13 Phenobarbital: a barbiturate - 116
3.5,14 Omeprazole: an anti-ulcer drug 117
3.5.15 Nifedipine 119
3.5.16 Ciprofloxacin: an antibacterial drug 120
3.6 Natural drugs 122
3.6.1 Penicillin: a group of antibiotics 122
3.6.2 Production and isolation of penicillin 124;
Appendix: Vitamin B)2 131'
4 Formulation of drugs 133
4.1 Introduction 133
4.2 Need for the conversion of drugs into medicine 133
4.3 Additives and their role 135
4.4 Classification 138
4.4.1 Route-wise dosage forms 138
4.4.2 Form-wise dosage forms 139
4.5 Solid dosage forms 139
4.5.1 Tablets 140
4.5.2 Capsules 143
4.5.2.1 Hard gelatin capsules 144
4.5.2.2 Soft gelatin capsules 145
4.6 Liquid <dosage forms 146
4.6.1 Parenterals (Injectables) 146
4.6.1.1 Total parenteral nutrition (TPN) 149
4.6.2 Liquid oral dosage forms 150
4.6.2.1 Syrups 151
4.6.2.2 Suspensions 152
4.7 Semi-solid dosage forms 154
4.7.1 Ointments 154
4.7.2 Creams 155
Bibliography 158
Glossary 159
Index 162