Pharmacology of antimuscarinic agents:
Saved in:
| Main Author: | |
|---|---|
| Format: | Book |
| Language: | English |
| Published: |
Boca Raton [u.a.]
CRC Press
1998
|
| Series: | Pharmacology and toxicology
|
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | 501 S. graph. Darst. |
| ISBN: | 0849385598 |
Staff View
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Record in the Search Index
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|---|---|
| adam_text | Table of Contents
1 Introduction 1
2 History 3
3 Nomenclature 5
4 Mechanism and Site of Action of Antimuscarinic Agents 7
4.1 Description and Classification of Acetylcholinergic
Receptor Sites 7
4.1.1 Peripheral Postganglionic Parasympathetic
(Muscarinic) Receptors 7
4.1.1.1 Historic Aspects 7
4.1.1.2 Studies of Drug Receptor Interactions with
Antimuscarinic Agents 8
4.1.2 Muscarinic Receptor Subtypes 25
4.2 The Role of ACh in Neuronal Conduction 31
4.2.1 Somatic Nerves 31
4.2.2 Sympathetic Nerves 31
4.2.3 Central Nervous System Neurons 33
4.3 Chemical Structural Aspects Related to Stimulation and
Block of the ACh Receptors 34
4.3.1 Muscarinic Receptors 36
4.3.2 Ganglionic Receptors 42
4.3.3 Nicotinic Motor Endplate ACh Receptors 43
5 The Tropane Alkaloids 47
5.1 Chemistry 47
5.1.1 Chemical Synthesis and Stereochemistry of Tropane
Alkaloids 50
5.1.2 Stereostructure of Tropine and Pseudo Tropine 51
5.1.3 Scopolamine (Hyoscine) 52
5.1.4 N Stereoisomerism 53
5.2 Absorption, Distribution, Metabolism, and Elimination of
Atropine and Related Tropane Alkaloids (Animal and
Human Data) 53
5.2.1 Absorption 53
5.2.2 Distribution 56
5.2.3 Metabolism and Elimination 57
5.2.3.1 Atropine Esterase 57
5.2.3.2 Binding to Plasma Proteins 58
5.2.3.3 Metabolism in Liver 59
5.2.3.4 Excretion 59
5.3 Animal Pharmacology of Atropine 60
5.3.1 Cardiovascular System — Introduction 60
5.3.1.1 Effects of Atropine on Heart
Rate — General Comments 61
5.3.1.2 Innervation of the Heart and
Cardiac Receptors 62
5.3.1.3 Biochemical Mechanisms and
Neurophysiologic Correlates of the
Cardiac Actions of Atropine 63
5.3.1.3.1 Chronotropic Function and
Pacemaker Mechanisms 63
5.3.1.4 Bradycardia 65
5.3.1.5 Tachycardia 66
5.3.1.6 Atropine and Cardiac Arrhythmias 69
5.3.1.7 Effect on Contractile Force and Cardiac
Output — Inotropic and Tonotropic Actions 69
5.3.1.8 Action on the Vascular System 70
5.3.2 Respiratory System 72
5.3.2.1 Respiratory Center 72
5.3.2.2 Airways 73
5.3.2.3 Lung Volumes 75
5.3.2.4 Airway Secretions 76
5.3.2.5 Pulmonary Circulation 76
5.3.3 Eye 76
5.3.3.1 Introduction 76
5.3.3.2 Pupil 76
5.3.3.3 Intraocular Pressure 78
5.3.4 Gastrointestinal Smooth Muscles 78
5.3.4.1 Pharmacologic Testing Methods 78
5.3.4.2 Esophagus 80
5.3.4.3 Stomach 82
5.3.4.4 Intestines 83
5.3.4.5 Gall Bladder and Bile Ducts 89
5.3.5 Other Smooth Muscle Organs 89
5.3.5.1 Urinary Bladder 89
5.3.5.2 Uterus 93
5.3.5.3 Nictitating Membrane 93
5.3.5.4 Vas Deferens 94
5.3.6 Secretory Functions 94
5.3.6.1 Gastric Secretions 94
5.3.6.2 Salivary Secretions 98
5.3.6.3 Pancreatic Secretions 99
5.3.6.4 Bile Secretions 100
5.3.6.5 Sweat Secretions 101
5.3.7 Actions of Atropine on Nicotinic Receptors 102
5.3.7.1 Autonomic Ganglia 102
5.3.7.2 Chromaffin Tissues 105
5.3.7.3 Chemoreceptors 106
5.3.7.4 Myoneural Junctions 107
5.3.8 Antagonism of the Effects of AntiChE Agents 108
5.3.9 The Effects of Atropine on the Central Nervous
System Ill
5.3.9.1 Introduction and General Aspects 111
5.3.9.2 Effects of Atropine on Electrocortical
Activity of Animals 115
5.3.9.3 Effects on Evoked CNS Responses,
Hippocampal Discharges, EEG Seizures,
and Spinal Reflexes 119
5.3.9.3.1 Regional (Microelectrophoretic
and Microelectrode) Studies 121
5.3.9.3.1.1 Cerebral Cortex 122
5.3.9.3.1.2 Rhinencephalon 123
5.3.9.3.1.3 Thalamus 124
5.3.9.3.1.4 Basal Ganglia 124
5.3.9.3.1.5 Brain Stem 125
5.3.9.3.1.6 Cerebellum 125
5.3.9.3.1.7 Spinal Cord 126
5.3.9.4 Effects of Atropine on Animal Behavior 126
5.3.9.4.1 Introduction 126
5.3.9.4.2 Studies in the Rat 127
5.3.9.4.3 Behavioral Studies in
Other Species 131
5.3.9.4.4 Eating and Drinking Behavior 133
5.3.9.4.5 Sexual Behavior 135
5.3.9.4.6 Reviews on the Behavioral
Pharmacology of Atropine 135
5.3.9.5 Other Effects on the Central Nervous
System 136
5.3.9.5.1 Thermoregulation 136
5.3.9.5.2 Pituitary Trophormone Release
and Hypothalamic Trophormone
Releasing Factors 138
5.3.9.5.3 Effect of Atropine on Other
Hormone Secretory
Mechanisms 140
5.3.9.5.3.1 Insulin Secretion 140
5.3.9.5.3.2 Aldosterone
Secretion 141
5.3.9.5.4 CNS ACh and Monoamine
Stores 141
5.3.9.6 Influence of Atropine on Selected
Drug Induced Effects in the CNS 143
5.4 Resistance to Atropine 143
5.5 Hyoscyamine 146
5.5.1 Central Nervous System 148
5.5.2 Derivatives of Hyoscyamine 149
5.6 L( )Hyoscine (Scopolamine) — Introduction 149
5.6.1 Peripheral Antimuscarinic Actions 150
5.6.2 Effects at the Autonomic Ganglia and at the Motor
Endplates 151
5.6.3 Effects of L( )Hyoscine on the Central Nervous
System 151
5.6.3.1 Effects on Animal Behavior 154
5.6.3.1.1 Spontaneous Motor Behavior 154
5.6.3.1.2 Learned Behavior 154
5.6.3.1.2.1 Studies in the Rat.... 154
5.6.3.1.2.2 Behavioral Studies
on Other Species 156
5.6.3.1.2.3 Possible Mechanisms
of the Behavioral
Actions of
Hyoscine 157
5.6.4 Comparison of the Central and Peripheral Effects of
Hyoscine 158
5.7 Atropine and L( )Hyoscine as Pharmacologic Probes in the
Pharmacological Exploration of the CNS 159
6 Semisynthetic Derivatives of Tropane Alkaloids and of Other
Tropine Esters 161
6.1 N Methylquaternary Derivatives of Tropane Alkaloids —
Introduction 161
6.1.1 Methylatropine 162
6.1.2 Methylhyoscine Methscopolamine Bromide
(MI 5927) 168
6.2 Other Tropeines 169
6.2.1 Homatropine (dl mandelyl tropine) 169
6.2.1.1 Derivatives of Homatropine 169
6.2.1.1.1 Homatropine Methylbromide 170
6.2.2 Other Tropine Esters 170
6.2.2.1 Influence of the Acidic Moiety on
Pharmacological Activity of Tropeines 171
6.2.2.2 Influence of the Changes in the Tropine
Component 177
6.2.3 Structure Activity Relationships of Quaternary
Ammonium Derivatives of Tropeines 178
6.2.3.1 Role of the Acid Ester Group in
Quaternary Tropeines 179
6.2.3.2 Role of the Tropane Ring 179
6.2.4 Monoquaternary Tropeines with Combined
Antimuscarinic and Ganglionic Blocking Properties 180
6.2.4.1 N Octylatropinium Bromide 180
6.2.4.2 Xenytropium, P phenyl Benzyl Atropinium
Bromide (MI 9983) 181
6.2.4.3 Fentonium, N (4 phenyl) phenacyl
I( )Hyoscyaminium Bromide (MI 3949) 181
6.2.4.4 Butyl Hyoscinium Bromide (MI 1588) and
Other Quaternary Derivatives of Hyoscine 182
6.2.4.5 Benzylyl 6 Methoxytropine Methobromide,
Tropenzile (MI 9690) 183
6.2.4.6 Anisotropine Methylbromide (MI 701) 183
6.2.4.7 Ipratropium® (MI 4690) 183
6.2.4.8 Flutropium Bromide (MI 4136) 183
6.2.4.9 Oxytropium Bromide (MI 6897) 184
6.2.4.10 Cyclotropium Bromide 184
6.2.4.11 Cimetropium Bromide (MI 2280) 184
6.2.4.12 Trospium Chloride (MI 9697) 185
6.2.4.13 8 Phenylacetyl Homatropinium Chloride
(Phenactropinium Chloride) (MI 7158) 185
6.2.4.14 Other Quaternary Ammonium Derivatives
of Tropeines 185
7 Synthetic Antimuscarinic Agents 187
7.1 Antimuscarinic Tropane Derivatives 187
7.1.1 Tropine Ethers 187
7.1.2 Other Tropanes 189
7.2 Other Bicyclic and Polycyclic Amines 193
7.2.1 Aza Bicyclooctanes Other Than Tropanes 193
7.2.2 Aza Bicyclo Nonanes (Granatanes) 195
7.2.3 Other Aza Bicyclo Nonanes 196
7.2.4 Aza Bicycloheptanes 197
7.2.5 Hexamethylene Tetramines (Tetraaza Tricyclo Decanes).... 197
7.2.6 Oxime Esters of 1 Azabicyclo (4.4.0) Decane 4 one 197
7.3 4 Acyloxy 2,6 Disubstituted Piperidines 198
7.4 Aliphatic and Alicyclic Aminoalcohol Esters of
Aromatic Acids 200
7.4.1 Diphenyl Acetyl P Diethylamino Ethanol
HC1 (Adiphenine) 222
7.4.2 Phenyl Cyclohexyl Acetyl P Diethylamino Ethanol
HC1 (Trasentin 6 H®) 222
7.4.3 Benzylyl P Diethylaminoethanol HC1 (Benactyzine,
Suavitil®) 228
7.4.4 Xanthene 9 Carboxylyl p Diethylaminoethanol
Methobromide (Methantheline Bromide) 229
7.4.5 Xanthene 9 Carboxylyl p Diisopropylaminoethanol
Methobromide (Propantheline Bromide) 230
7.4.6 a Phenyl Cyclohexane Glycolyl Diethyl (2 Hydroxy
Ethyl) Methyl Ammonium Bromide (Oxyphenonium,
Antrenyl®) 231
7.4.7 Aromatic Acid Esters of N Alkyl Piperidinols and
Pyrrolidinols . . 231
7.5 1,3 Dioxolane Derivatives 234
7.6 Amino Alkanols and Amino Alkanes Substituted with
Aromatics Groups 234
7.7 Aromatic Acid Amide and Nitrile Derivatives of
Alky! Amines 251
7.8 Aromatic Ether Derivatives of Amino Alkanols 252
7.9 Other Compounds of Various Chemical Structures with
Antimuscarinic Properties 257
7.10 Synthetic Agents with Central Acetylcholinolytic Properties
Used in Parkinson s Disease 259
8 Molecular Design of Antimuscarinic Agents 267
8.1 Muscarinic Receptor Subtype Nonspecific Agents 267
8.2 Muscarinic Receptor Subtype Specific Agents 277
9 Drug Interactions 283
10 Clinical Pharmacology and Therapeutic Uses of
Antimuscarinic Agents 293
10.1 Pharmacokinetics 293
10.2 Effects on the Cardiovascular System in Man 294
10.2.1 Effects on Heart Rate 294
10.2.1.1 Interactions Between the Actions of
Atropine and Other Drugs on Cardiac Rate 296
10.2.1.2 Dysrhythmias 297
10.2.2 Effect on Contractile Force and Cardiac Output 297
10.2.3 Clinical Uses of the Cardiac Effects of Atropine 298
10.2.3.1 Diagnostic Uses 298
10.2.3.2 Therapeutic Uses 299
10.2.3.3 Use in Acute Myocardial Infarction 302
10.2.3.4 Endotracheal Application of Atropine 303
10.3 Effects on Respiration 303
10.3.1 Effects on the Respiratory Center 304
10.3.2 Effects on Lung Volumes 305
10.3.3 Effects on the Airways 305
10.3.3.1 Larynx 305
10.3.3.2 Bronchi 306
10.3.4 Effect on Pulmonary Vessels 307
10.4 Effects on the Motor Functions of the Gastrointestinal and
Genitourinary Tract 308
10.4.1 Gastrointestinal Motility 308
10.4.1.1 Clinical Methods 308
10.4.2 Esophagus 309
10.4.3 Stomach and Intestines 310
10.4.4 Biliary Tract 311
10.4.5 Urinary Bladder 312
10.4.6 Uterus, Placenta, and Fallopian Tube 312
10.5 Action on Secretory Functions 313
10.5.1 Gastric Secretions 314
10.5.2 Bile Secretions 315
10.5.3 Salivary Secretions 316
10.5.4 Bronchial Secretions 317
10.5.5 Milk Secretions 317
10.5.6 Tear and Lymph Secretions 317
10.5.7 Nasal Secretions 318
10.5.8 Sweat Secretion 318
10.5.9 Pancreatic Secretions 319
10.5.10 Pituitary Hormone Release 319
10.5.11 Other Hormonal Release Mechanisms 321
10.6 Effects on the Eye 321
10.6.1 Pupil Size 321
10.6.2 Intraocular Pressure 322
10.7 Effects of Antimuscarinics in the CNS 323
10.7.1 Effects on Electrocortical Activity 323
10.7.2 Behavioral Effects 324
10.7.2.1 Anticholinergic Psychosis 325
10.7.2.2 Atropine Coma Therapy 326
10.7.3 Various CNS Effects of Antimuscarinic Agents 327
10.8 Clinical Studies with Other Antimuscarinic Agents and their
Therapeutic Uses 329
10.8.1 Congeners of Atropine and Hyoscine 332
10.8.1.1 Ipratropium 333
10.8.1.2 Butylhyoscinium Bromide 333
10.8.2 Homatropine and Homatropine Methyibromide 334
10.8.3 Therapeutic Uses of Various Antimuscarinic Agents 336
10.8.3.1 General Aspects 336
10.8.3.2 Gastrointestinal Disorders 336
10.9 Use of Antimuscarinic Agents as Adjunct to Anesthesia 339
10.9.1 Atropine and Glycopyrrolate 339
10.9.2 Other Antimuscarinic Agents 341
10.9.3 Pediatric Use of Antimuscarinic Agents in
Anesthesia 343
10.10 Use in Anticholinesterase Poisoning 344
10.11 Emesis and Motion Sickness 345
10.12 Use in Cerebral Injuries 347
11 Toxicity of Atropine 349
11.1 Toxicity in Animals 349
11.1.1 Introduction 349
11.1.2 Toxic Symptoms and Lethal Doses 349
11.2 Toxicity in Man 350
11.2.1 Symptoms of Atropine Toxicity 350
11.2.2 Tolerance and Hypersensitivity 354
11.2.3 Metabolism and Excretion of Atropine
During Toxicity 355
11.2.4 Management of Atropine Poisoning 355
12 Summary 357
References 361
Index 477
|
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| id | DE-604.BV012018482 |
| illustrated | Illustrated |
| indexdate | 2024-07-09T18:20:17Z |
| institution | BVB |
| isbn | 0849385598 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-008134414 |
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| physical | 501 S. graph. Darst. |
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| publisher | CRC Press |
| record_format | marc |
| series2 | Pharmacology and toxicology |
| spelling | Gyermek, Laszlo Verfasser aut Pharmacology of antimuscarinic agents Laszlo Gyermek Boca Raton [u.a.] CRC Press 1998 501 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier Pharmacology and toxicology Antagonistes muscariniques - Pharmacologie Parasympatholytiques ram Récepteurs muscariniques ram Muscarinic Antagonists pharmacology Muscarinic receptors Antagolists Parasympatholytic agents Muscarinrezeptor (DE-588)4170773-4 gnd rswk-swf Pharmakologischer Antagonist (DE-588)4198682-9 gnd rswk-swf Parasympathikolytikum (DE-588)4173326-5 gnd rswk-swf Muscarin (DE-588)4170772-2 gnd rswk-swf Muscarin (DE-588)4170772-2 s Pharmakologischer Antagonist (DE-588)4198682-9 s DE-604 Muscarinrezeptor (DE-588)4170773-4 s Parasympathikolytikum (DE-588)4173326-5 s HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008134414&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Gyermek, Laszlo Pharmacology of antimuscarinic agents Antagonistes muscariniques - Pharmacologie Parasympatholytiques ram Récepteurs muscariniques ram Muscarinic Antagonists pharmacology Muscarinic receptors Antagolists Parasympatholytic agents Muscarinrezeptor (DE-588)4170773-4 gnd Pharmakologischer Antagonist (DE-588)4198682-9 gnd Parasympathikolytikum (DE-588)4173326-5 gnd Muscarin (DE-588)4170772-2 gnd |
| subject_GND | (DE-588)4170773-4 (DE-588)4198682-9 (DE-588)4173326-5 (DE-588)4170772-2 |
| title | Pharmacology of antimuscarinic agents |
| title_auth | Pharmacology of antimuscarinic agents |
| title_exact_search | Pharmacology of antimuscarinic agents |
| title_full | Pharmacology of antimuscarinic agents Laszlo Gyermek |
| title_fullStr | Pharmacology of antimuscarinic agents Laszlo Gyermek |
| title_full_unstemmed | Pharmacology of antimuscarinic agents Laszlo Gyermek |
| title_short | Pharmacology of antimuscarinic agents |
| title_sort | pharmacology of antimuscarinic agents |
| topic | Antagonistes muscariniques - Pharmacologie Parasympatholytiques ram Récepteurs muscariniques ram Muscarinic Antagonists pharmacology Muscarinic receptors Antagolists Parasympatholytic agents Muscarinrezeptor (DE-588)4170773-4 gnd Pharmakologischer Antagonist (DE-588)4198682-9 gnd Parasympathikolytikum (DE-588)4173326-5 gnd Muscarin (DE-588)4170772-2 gnd |
| topic_facet | Antagonistes muscariniques - Pharmacologie Parasympatholytiques Récepteurs muscariniques Muscarinic Antagonists pharmacology Muscarinic receptors Antagolists Parasympatholytic agents Muscarinrezeptor Pharmakologischer Antagonist Parasympathikolytikum Muscarin |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008134414&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT gyermeklaszlo pharmacologyofantimuscarinicagents |