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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5726_Библиотеки_им_академика_М_И_Перельмана.pdf
X
- •Preface
- •Contents
- •1.3.2 Solubility Parameters
- •1.1 Introduction
- •1.2 Types of Drug Action Theories
- •1.2.1 The Ferguson Principle
- •1.2.2 Structure and Activity
- •1.2.3 Relationship between Molecular Structure and Biological Action
- •1.3 Physicochemical Parameters and Pharmacological Activity
- •1.3.1 Introduction
- •1.3.3 Steric Parameters
- •1.4 Stereochemistry Consideration
- •1.4.1 Chirality
- •1.4.2 Stereochemistry and Drug Action
- •1.4.3 Isomers Types
- •1.5 Isosterism and Bioisosterism
- •1.5.1 Pharmacophore or Lead
- •1.5.2 Isosteres
- •1.5.3 Bioisosteres
- •1.6 Drug-Receptor Interaction
- •1.6.1 Receptor
- •1.6.2 Requirement for Agonist Activity
- •1.6.3 Receptor Families
- •1.6.4 Role of Chemical Bonding
- •1.6.5 Types of Receptors
- •1.7 Prodrugs
- •1.7.1 Introduction
- •1.7.2 Concept of Prodrug
- •1.7.3 Prodrugs are Designed for the Following Purposes
- •1.7.4 Classification of Prodrugs
- •Exercise
- •Autonomic Nervous System
- •2.1 Introduction
- •2.2 Cholinergic Drugs
- •2.2.1 Definition
- •2.2.2 Cholinergic Receptors
- •2.2.3 Biosynthesis of Ach
- •2.2.4 Classification
- •2.2.5. Action of Cholinesterase Inhibitors
- •2.2.6 Structural Activity Relationship (SAR) of Musarinic Agonist/Cholinomimetics
- •2.2.7 Cholinomimetic Agents
- •2.2.9 Classification of Anticholinergic Agents
- •2.2.10 Structural Activity Relationship (SAR) of Anticholinergic Agent
- •2.2.11 Anticholinergic Agent
- •2.2.12 Newer Drug
- •2.3 Adrenergic Agents
- •2.3.1 Introduction
- •2.3.2 Mechanism of Action
- •2.3.3 Biosynthesis of Catecholamines
- •2.3.4 Pharmacological Action
- •2.3.5 Adrenergic
- •2.3.6 Classification
- •2.3.7 SAR of Phenylethanolamine Derivatives/Direct Acting Agonist
- •2.3.8 SAR of Indirect Acting Agonist/Arylethylamine Derivatives
- •2.3.9 Adrenergic Agents
- •2.3.10 Newer Drugs
- •Exercise
- •3.1 Introduction
- •3.2 Ideal Characteristics of General Anaesthetics
- •3.4 Concepts of Mechanism of Anaesthesia
- •3.5 Minimum Alveolar Concentration (MAC)
- •3.6 Stages of Anaesthesia
- •3.7 Classification of General Anaesthesia
- •3.8 Receptors Involved in the Mechanism
- •3.9 Stereochemistry of Volatile Anaesthetics
- •3.10 Toxicity of Fluorinated General Anaesthetics
- •3.11 General Anaesthetics Agents
- •3.12 Newer Agents
- •Exercise
- •4.1 Introduction
- •4.2 Methods of Administration
- •4.3 Classification of Local Anaesthetics
- •4.4 Mechanism of Action of Local Anaesthetics
- •4.6 Local Anaesthetic Agents
- •4.7 Newer Agents
- •Exercise
- •5.1 Introduction
- •5.3 Classification of Sedative and Hypnotics
- •5.3.1 Barbiturates
- •5.3.2 Benzodiazepines
- •5.3.3 Halogenated Sedative and Hypnotics
- •5.3.4 Heterocyclic Sedative and Hypnotics
- •5.3.5 Miscellaneous Sedative and Hypnotics
- •5.4 Mechanism of Action
- •5.5 Barbiturates
- •5.5.1 General Synthetic Approach of Sedative and Hypnotics
- •5.6 SAR of (Barbiturates) Sedative and Hypnotics
- •5.7 Benzodiazepines
- •6.7 Morphines and Derivatives
- •5.8 SAR of Benzodiazepines
- •5.9 Heterocyclic Sedative and Hypnotics
- •5.10 Halogenated Sedative and Hypnotics
- •5.11 Recent Development of Sedative and Hypnotics
- •Exercise
- •6.1 Introduction
- •6.2 Opioid Receptors
- •6.3 Opioid Peptides
- •6.4 Classification
- •6.5 Mechanism of Action (Signal Transduction)
- •6.6 Central Side Effects of Opioid Analgesics
- •6.8 SAR of Morphines Derivatives
- •6.9 Piperidine Derivatives
- •6.10 SAR of Piperidines Derivatives
- •6.11 Diphenyl Haptanones Derivatives (Acyclic Analgesics)
- •6.12 SAR of Diphenyl Haptanone Derivatives
- •6.13 Benzazocin Derivatives/Morphan Derivatives
- •6.14 Narcotics Antagonists/Opioid Antagonists
- •6.15 Newer Drugs
- •6.16 Antitussive Agents
- •Exercise
- •7.1 Introduction
- •7.2 Classification of Epilepsy
- •7.3 Seizure Initiation and Propagation
- •7.4 Receptors Involved in the Mechanism
- •7.5. Classification of Antiepileptic Agnents
- •7.5.1 Ureid Derivatives/First Generation Antiepileptic Agents
- •7.5.2 Benzodiazepines
- •7.5.3 Urea and MonoAcyl Urea-Derivatives/Iminostilbenes
- •7.5.4 Miscellaneous Agents
- •7.6 Hydantoins Agents
- •7.7 Oxazolidinediones Agents
- •7.8 Succinimides Agents
- •7.9 Iminostilbens Agents
- •7.10 Aliphatic Acid Agent
- •7.11 Second Generation Antiepileptic Drugs
- •7.12 Other Miscellaneous Antiepileptic Agents
- •7.13 Models Requirements for Antiepileptic Agents/SAR
- •7.14 Newer Drugs Development
- •Exercise
- •8.1 Introduction
- •8.2 Etiology of Parkinson
- •8.3 Initiation of Therapy
- •8.4 Classification of Antiparkinsonism Agents
- •8.4.1 Dopaninergic Treatment
- •8.4.2 Agents Action on Nondopaminergic System
- •8.5 Dopaminergic Agents
- •8.6 Non-Dopaminergic Agents
- •8.7.1 Conformational Aspects
- •8.7.2 PKa Aspects
- •Exercise
- •9.1 Introduction
- •9.2 Clinical Uses of CNS Stimulants
- •9.3 Classification
- •9.4 Mechanism of Action
- •9.5 CNS Stimulants Agents
- •9.5.1 Amphetamine Related Agents
- •9.5.2 SAR or Structural Requirements of Amphetamines
- •9.5.3 Xanthine Alkaloids
- •9.5.4 Cocaine Related CNS stimulating Agents
- •9.5.5 Miscellaneous CNS Stimulants Agents
- •9.5.6 Newer Agents
- •9.6 Metabolic Patterns of Some CNS Stimulants Agents
- •9.7 Analeptics or Respiratory Stimulants
- •Exercise
- •10.1 Introduction
- •10.2 Causes of Schizophrenia
- •10.2.1 Adverse Effects
- •10.3 Antipsychotic Agents
- •10.3.1 Mechanism of Action
- •10.4 Classification
- •10.5 Tricyclic Neuroleptics/Phenothiazines
- •10.5.1 Phenothiazines Structure and Structure Activity Relationship
- •10.5.2 Specific Derivatives
- •10.6 Thioxanthene Derivatives
- •10.7 Dibenzoxazepine and Dibenzdiazepine Derivatives
- •10.8.1 SAR of Butyrophenones
- •10.8.2 Butyrophenones Agents
- •10.9 Benzamides Derivatives
- •10.9.1 Structure Activity Relationship of Benzamides
- •10.9.2 Specific Derivatives
- •10.10 Dihydroindolone Derivative
- •10.11 Diphenylbutylpiperidine Derivatives
- •10.12 Miscellaneous Agents
- •10.13 Newer Agents
- •Exercise
- •11.1 Introduction
- •11.2 Management of Depression
- •11.3 Classification
- •11.4 Tricyclic Antidepressants
- •11.4.1 Mechanism of Action
- •11.4.2 Structural Activity Relationship (SAR) of Tricyclic Antidepressants (TCAs)
- •11.4.3 Metabolic Pattern of Tricyclic Antidepressants
- •11.4.4 Specific Drugs
- •11.6 Specific Drugs
- •11.7 Selective Serotonine Reuptake Inhibitors (SSRI)
- •11.7.1 Mechanism of Action
- •11.7.2 Structure Activity Relationship (SAR) of (SSRIs)
- •11.7.3 Specific Drugs
- •11.8 Newer Atypical Antidepressants
- •11.8.1 Specific Drugs
- •11.9 Newer Agents
- •Exercise
- •12.1 Introduction
- •12.2 Causes of Anxiety
- •12.2.1 Receptor Involve
- •12.3 Classification
- •12.4 Benzodiazepines
- •12.4.1 Mechanism of Action
- •12.4.2 Metabolic Pattern
- •12.5 Structure Activity Relationship (SAR) of Benzodiazepines
- •12.6 Benzodiazepines Derivatives (Specific Drugs)
- •12.7 Non-benzodiazepine Derivatives (Specific Drugs)
- •12.8 Newer Agents
- •Exercise
- •13.1 Introduction
- •13.2 Mechanism of Action
- •13.3 Classification
- •13.4 Specific Derivatives
- •13.4.1 Glycerol Monoethers Derivatives
- •13.4.2 Alkanediols Derivatives
- •13.4.3 Benzazole Derivative
- •13.4.4 Imidazolin Derivative
- •13.4.5 Miscellaneous Agents
- •13.5 Newer Agents
- •Exercise
- •14.1 Introduction
- •14.2 Mechanism of Action
- •14.3 Classification
- •14.4 Non-depolarizing Muscle Relaxants
- •14.5 Structural Activity Relationship of Aminosteroids NMB Agents
- •14.6 SAR of Tetrahydroisoquinoline Derivatives
- •14.7 Depolarizing Muscle Relaxants (DPR)
- •14.8 SAR of Depolarizing Muscle Relaxants
- •14.9 Newer Agents
- •Exercise
- •15.1 Introduction
- •15.2 Nomenclature of Heterocyclic Compounds
- •15.3 Naming of Heterocyclic Rings
- •15.4 Nomenclature of Fused Ring System
- •Exercise
- •References
- •Index

Index
A
Acetylcholine, biosynthesis of 24
Ach, biosynthesis of 25
Acid base properties 4
Acyloxy group, modifi cation of 30
Adrenergic agents 39
mechanism of action of 40
Adrenergic agents 47
Adrenergic receptors 41
Agonist activity 15
Aliphatic acid agent 116
Amide linkage derivatives 65
Aminosteroids NMB agents, SAR
*
of 220
Amphetamine related agents 139
Amphetamines, structural requirements of 142
Anaesthesia
mechanism of 54
stages of 55
Analeptics 147
Anticholinergic agent 36, 128
Anticholinergic agent, SAR of 36
Anticholinergic agents, classifi cation of 34
Anticonvulsant agents 107
Antidepressant drugs 174
Antiepileptic agents 120
classifi cation of 109
Antiparkinsonism agents 124
classifi cation of 125
Antipsychotic agents 152
Antipsychotic drugs 151
Antitussive agents 105
Anxiety 190
causes of 191
classifi cation 191
Arylcyclo hexylamine agents 60
Arylcyclo hexylamine derivatives 57
Arylethylamine derivatives, SAR of 47
Autonomic nervous system 23
B
Barbiturates 73, 77, 110
mechanism of action 76
Benzamides derivatives 168
Benzazocin derivates 91
Benzazocin derivatives 102
Benzodiazepines 57, 74, 81, 112, 195
basic pharmacophore of 85
derivatives 198
mechanism of action 76
SAR of 85, 197
Bioisosteres 11
Bioisosterism 11
Bioprecursor prodrugs 20, 21
Butyrophenones, SAR of 165
Butyrophenones agents 166
C
Carbachol 32
Carrier linked prodrugs 18, 21
Catecholamines, biosynthesis of 40
Catechol-o-methyl transferase inhibitor 128
Central nervous system stimulants 136, 137
classifi cation of 137
clinical uses of 136
stimulants agents 139
Chemical bonding, role of 15
Chemical messengers 17
Chirality 7
Cholinergic drugs 24
Cholinergic receptor agonist 26
Cholinergic receptors 25
*
SAR = Structural activity relationship

236 Index
Cholinesterase inhibitors, action of 30
Cholinomimetic agents 31
Cholinomimetics, SAR of 30
Classical bioisoster 12
CNS stimulants agents, metabolic patterns of 147
COMT inhibitors 128
Constitutional isomers 9
Covalent bond 15
D
Decarboxylase inhibitors 128
Depolarizing muscle relaxants 222, 218
SAR of 224
Depression 174
classifi cation 175
management of 175
Dextroamphetamine 139
Diastereomers 10
Dibenzdiazepine derivatives 163
Dibenzoxazepine 163
Dihydroindolone derivatives 169
Diphenyl haptanone derivatives, SAR of 100, 101
Diphenyl haptanones analogues 91
Diphenylbutylpiperidine derivatives 170
Di-receptor agonists 127
Direct acting agonist 42
SAR of 45
Direct acting cholinomimetics 27
Dopamine agonist 128
Dopamine receptor agonist
SAR of 134
structural modeling for 134
Dopamine-D
2
receptor agonists 125
Dopaminergic agents 130
Drug action theories 1
Drug-receptor interaction 13
Drugs, water solubility of 6
E
Enantiomers 9
Epilepsy
classifi cation of 107
propagation 108
seizure initiation 108
Ester linkage derivatives 64
SAR of 66
Ethylene bridge, modifi cation of 31
F
Ferguson principle 1
First generation antiepileptic agents 110
Fluorinated general anaesthetics, toxicity of 58
Fluorinated hydrocarbons 59
Fused ring system, nomenclature of 230
G
Gaseous anaesthetics 56
General anaesthesia
classifi cation of 55
General anaesthetics
agents 59
characteristics of 53
Glutamate antagonist 130
G-protein-coupled receptors (7-tm) 17
H
Halogenated sedative, and hypnotics 74, 86
Heterocyclic chemistry, concept of 227
Heterocyclic compounds, nomenclature of 227
Heterocyclic rings, naming of 228
Heterocyclic sedative, and hypnotics 75, 86
Hydantoins 111
Hydantoins agents 112
Hydantoins, synthetic approach of 113
Hydrogen bond 16
Hydrophobic interaction 16
Hypnotics (barbiturates), SAR of 80
Hypnotics 72
classifi cation of 73
general synthetic approach of 77
recent developments 87
I
Ideal hypnotics drugs 72
Iminostilbenes 112
Iminostilbens agents 115
Indirect acting agonist 44
SAR of 47

Index 237
Indirect acting cholinomimetics 28
Indirect-mixed action 44
Inhalation anaesthetics 55
Intravenous anaesthetics 56
Ion channel theory 54
Ionic bond 15
Irreversible cholinesterase inhibitors 30
Isomers, types of 9
Isoptocarachol 32
Isoptocarpine 32
Isosteres 11
Isosterism 11
L
Lead 11
Ligand gated ion channel receptor 16
Liquid anaesthetics 55
Local anaesthetics 63
administration of 63
agents 68
classifi cation of 64
mechanism of 66
M
Mao inhibitors 127
Membrane-bound enzymes 14
Methacholine 31
Methamphetamine 140
Meyer-Overton theory 54
Minimum alveolar concentration 54
Miscellaneous antiepileptic agents 119
Miscellaneous CNS stimulants agents 145
Miscellaneous drugs 58
Miscellaneous sedative, and hypnotics 76
Molecular structure, and biological action 3
Monoacyl urea derivatives 112
Monoamine oxidase inhibitors 184
Morphan derivatives 102
Morphines 92
derivatives of 89
pharmacophore of 89
SAR of 95
Musarinic agonist, SAR of 30
Muscarinic antagonists 33
Muscarinic receptors 25
Mutual prodrugs 21
N
Narcotic analgesics 57
Narcotic anaesthesia 61
Narcotics antagonists 103
Neostigmine 33
Nervous system, anatomy of 24
Neuromuscular blocking agents 215
classifi cation 216
mechanism of action 215
Newer agents 212, 225
Newer atypical antidepressants 187
Nicotinic receptor antagonists 215
Nicotinic receptors 25
Non-benzodiazepine derivatives 201
Non-classical bioisosters 12, 13
Non-depolarizing muscle relaxants 216, 218
Non-dopaminergic agents 132
Non-specifi c drugs 2
O
Opioid 92
analgesics side effects of 92
mechanism of action of 92
Opioid analgesics 88
Opioid antagonists 103
Opioid peptides 89
Opioid receptors 88
Optical isomers 9
Oxazolidinedinones 111
agents 113
synthetic approach of 114
P
Parkinson’s disease 124
Peripherally acting muscles relaxants 215
Pharmacophore 11
Phenothiazines 157
Phentermine 140
Phenylethanolamine derivatives, SAR of 45
Physostigmine 32
Pilocarpine 32

238 Index
Piperidine analogues 90
Piperidines derivatives, SAR of 96, 100
Positional isomers 9
Prodrugs 17
classifi cation of 18
purposes of 18
Prostigmine 33
Provocholine 31
Q
Quaternary amine series 35
Quaternary ammonium group, modifi cation of 31
R
Receptor 13
types of 16
Receptor families 15
Relative acid strength theory 6
Respiratory stimulants 147
Reversible cholinesterase inhibitors 28
S
SAR of
aminosteroids NMB agents 220
anticholinergic agent 36
arylethylamine derivatives 47
benzodiazepines 197
butyrophenones 165
cholinomimetics 30
depolarizing muscle relaxants 222, 218, 214
diphenyl haptanone derivatives 100, 101
direct acting agonist 42, 45
dopamine receptor agonist 134
ester linkage derivatives 64, 66
hypnotics (barbiturates) 80
indirect acting agonist 44, 47
morphines 92, 95
musarinic agonist 30
phenylethanolamine 45
piperidines derivatives 96, 100
sedative (barbiturates) 80
tetrahydroisoquinoline derivatives 222
SAR models, requirements for 120
Schizophrenia 151
adverse effects 152
causes of 151
Second generation anticonvulsant 117
Second generation antiepileptic drugs 117
Sedative (barbiturates), SAR of 80
Sedative 72, 87
classifi cation of 73
general synthetic approach of 77
Selective serotonine reuptake inhibitors 185
Selectively α-adrenoceptors agonist 43
Selectively β-adrenoceptors agonist 42
Serotonin agonists 130
Signal transduction 17, 92
Skeletal muscle relaxants 205
Solubility parameters 3
Spasmolytic agents 205
classifi cation 206
Specifi c derivatives 208
Specifi c drugs 2, 184
Stereo isomers 9
Stereochemistry, and drug action 8
Steric parameters 7
Succinimides 112
agents 114
synthetic approach of 114
T
Tertiary amine series 34
Tetrahydroisoquinoline derivatives, SAR of 222
Thioxanthene derivatives 161
Tricyclic antidepressants 178
Tricyclic neuroleptics 157
U
Ultra short acting barbiturates 56, 59
Unverferth model 121
Urea 112
Ureid derivatives 110
V
Volatile anaesthetics, stereochemistry of 58
X
Xanthine alkaloids 143
a and β adrenomimetics 44

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