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Pharmacological Control of Heart and Circulation (eBook)

Proceedings of the 3rd Congress of the Hungarian Pharmacological Society, Budapest, 1979
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2013 | 1. Auflage
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Pharmacological Control of Heart and Circulation, Volume 1, documents the proceedings of the 3rd Congress of the Hungarian Pharmacological Society held in Budapest, 1979. Because the papers published in this volume cover diverse areas of the cardiovascular field, they had to be arranged into several smaller symposia. The common thread running through these symposia is their focus on some pathological condition of the heart and circulation as well as on their control by drugs. The first symposium is devoted to the pharmacological control of the adverse effects of coronary insufficiency including disturbances in rhythm. The second symposium is dedicated to cardiac hypertrophy; to the action of cardiac hypertrophy on the sensitivity of the heart to drugs; and to the changes in the biochemical parameters of the myocardium due to cardiomegaly. The third symposium deals with hypertension and its pharmacological control. Two separate symposia are devoted to new drugs, namely the fourth symposium to the cerebrovascular activity of Cavinton-a synthetic Vinca-derivative; and the fifth to a newly developed beta-adrenergic blocking agent, Tobanum, to its anti-arrhythmic action, its effect in myocardial ischemia and in hypertension. Finally, a short symposium on serotonin and serotonin antagonists, both of great importance in cardiovascular pharmacology, is included.
Pharmacological Control of Heart and Circulation, Volume 1, documents the proceedings of the 3rd Congress of the Hungarian Pharmacological Society held in Budapest, 1979. Because the papers published in this volume cover diverse areas of the cardiovascular field, they had to be arranged into several smaller symposia. The common thread running through these symposia is their focus on some pathological condition of the heart and circulation as well as on their control by drugs. The first symposium is devoted to the pharmacological control of the adverse effects of coronary insufficiency including disturbances in rhythm. The second symposium is dedicated to cardiac hypertrophy; to the action of cardiac hypertrophy on the sensitivity of the heart to drugs; and to the changes in the biochemical parameters of the myocardium due to cardiomegaly. The third symposium deals with hypertension and its pharmacological control. Two separate symposia are devoted to new drugs, namely the fourth symposium to the cerebrovascular activity of Cavinton-a synthetic Vinca-derivative; and the fifth to a newly developed beta-adrenergic blocking agent, Tobanum, to its anti-arrhythmic action, its effect in myocardial ischemia and in hypertension. Finally, a short symposium on serotonin and serotonin antagonists, both of great importance in cardiovascular pharmacology, is included.

Front Cover 1
Pharmacological Control of Heart and Circulation 4
Copyright Page 5
Table of Contents 6
PREFACE 12
Part I: PHARMACOLOGICAL CONTROL OF THE ADVERSE EFFECTS OF CORONARY INSUFFICIENCY 14
CHAPTER 1. PHARMACOLOGICAL CONTROL OF THE ADVERSE EFFECTS OF CORONARY INSUFFICIENCY. INTRODUCTION 16
CHAPTER 2. METABOLIC CHANGES DUE TO MYOCARDIAL ISCHEMIA 18
I. CARBOHYDRATE METABOLISM 18
II. LIPID METABOLISM 20
III. ATTEMPTS TO INTERFERE WITH CONSEQUENCES OF ISCHEMIA 21
IV. SUMMARY 22
V. REFERENCES 22
CHAPTER 3. EFFECTS OF ISCHEMIC METABOLITES ON THE MITOCHONDRIAL MEMBRANE 24
Introduction 24
Methods 24
Results 24
Discussion 27
References 29
CHAPTER 4. ANTIANGINAL AND ANTIARRHYTHMIC AGENTS AND CELLULAR COMPONENTS 30
RESULTS AND DISCUSSION 30
SUMMARY 32
REFERENCES 32
CHAPTER 5. EFFECT OF MYOCARDIAL ISCHAEMIA ON THE BASIC ELECTRICAL PHENOMENA IN THE HEART CELL 34
REFERENCES 41
CHAPTER 6. ARRHYTHMOGENIC ACTION OF LOCAL MYOCARDIAL ISCHEMIA 44
SUMMARY 49
REFERENCES 49
CHAPTER 7. SIGNIFICANCE OF THE AUTONOMIC NERVOUS SYSTEM IN THE APPEARANCE OF ARRHYTHMIAS DUE TO CORONARY OCCLUSION 52
REFERENCES 55
CHAPTER 8. INFLUENCE OF HYPOTHYROIDISM ON CARDIAC ARRHYTHMIAS INDUCED BY CORONARY OCCLUSION 56
REFERENCES 60
CHAPTER 9. INFLUENCE OF THYROTOXICOSIS ON DISORDERS OF CARDIAC RHYTHM APPEARING IN CORONARY INSUFFICIENCY 62
REFERENCES 65
CHAPTER 10. ACUTE EFFECT OF ANTIARRHYTHMIC DRUGS IN HEART RHYTHM DISTURBANCES DUE TO MYOCARDIAL ISCHEMIA 68
REFERENCES 71
CHAPTER 11. EFFECT OF PROLONGED TREATMENT WITH ANTIARRHYTHMIC AND ANTIANGINAL DRUGS ON THE INCIDENCE OF VENTRICULAR FIBRILLATION AND DEATH IN THE ACUTE PHASE OF MYOCARDIAL INFARCTION IN AWAKE RATS 72
Introduction 72
Methods 72
Discussion 74
Summary 74
REFERENCES 74
CHAPTER 12. EFFECT OF PENTOBARBITONE ANESTHESIA, AGE AND SEX IN THE ACUTE PHASE OF MYOCARDIAL INFARCTION IN RATS 76
Summary 78
REFERENCES 78
CHAPTER 13. IMPORTANCE OF METABOLIC CHANGES IN THE ANTIANGINAL EFFECT OF DRUGS AT THE SUBCELLULAR LEVEL 80
Introduction 80
Methods 80
Results and Discussion 80
Summary 82
References 83
CHAPTER 14. SIGNIFICANCE OF METABOLIC ALTERATIONS IN THE EFFECT OF ANTIANGINAL DRUGS AT THE CELLULAR LEVEL 84
REFERENCES 86
CHAPTER 15. IMPORTANCE OF METABOLIC CHANGES IN THE ANTIANGINAL ACTION OF DRUGS AT THE ORGAN LEVEL 88
REFERENCES 92
CHAPTER 16.ROLE OF HEMODYNAMICS IN THE ANTIANGINAL ACTION OF DRUGS 94
REFERENCES 97
CHAPTER 17. EFFECT OF A DRUG COMBINATION IN THE EXPERIMENTAL OF ANGINA PECTORIS 98
REFERENCES 101
CHAPTER 18. EFFECT OF DRUGS ON CEREBRAL CIRCULATION IN CHRONIC CEREBRAL ISCHEMIA 102
REFERENCES 105
CHAPTER 19. ADRENERGIC MECHANISMS IN CORONARY VASCULAR CONTROL AND OXYGEN METABOLISM FOLLOWING BRIEF REGIONAL MYOCARDIAL ISCHEMIA 106
REFERENCES 110
Part II: CARDIAC HYPERTROPHY 112
CHAPTER 20. CHANGES IN THE CONTRACTILITY AND CATECHOLAMINE-SENSITIVITY OP MYOCARDIUM IN ISOPROTERENOL-INDUCED CARDIAC HYPERTROPHY 114
Introduction 114
Methods 114
Results 115
Discussion 116
Summary 116
References 117
CHAPTER 21. THE ROLE OP THYROID STATE IN THE INOTROPIC EFFECT OF ADENOSINE ON VENTRICULAR MYOCARDIUM 118
Introduction 118
Methods 118
Results 118
Discussion 120
Summary 121
References 121
CHAPTER 22. ALTERATION OE CATECHOLAMINE-SENSITIVITY IN THYROXINE-INDUCED MYOCARDIAL HYPERTROPHY 122
Introduction 122
Methods 122
Results 122
Discussion 124
Summary 124
References 125
CHAPTER 23. REGULATION OP ß-ADRENERGIC RECEPTORS IN HEART MUSCLE SOME ASPECTS 126
References 133
CHAPTER 23. INVESTIGATION ON THE ALTERED PROPERTIES OP MYOSIN ASSOCIATED WITH CARDIAC HYPERTROPHY 138
Introduction 138
Methods 138
ATPase activity measurement 138
Results 139
Discussion 140
Summary 140
References 141
CHAPTER 24. BIOCHEMICAL PARAMETERS RELATED TO CARDIOMEGALY 142
Introduction 142
Methods 142
Results 142
Discussion 144
Summary 144
References 145
CHAPTER 25. STUDIES ON THE MYOSIN ATPase ACTIVITY IN EXPERIMENTALLY-INDUCED CARDIAC HYPERTROPHY IN RATS 146
Introduction 146
Methods 146
Results 146
Discussion 148
Summary 148
References 149
CHAPTER 26. CARDIAC AEBHYTHMIAS INDUCED BY ELECTRICAL AND CHEMICAL STIMULATION OF SOME HYPOTHALAMIC NUCLEI IN THE RATS 150
Introduction 150
Methods 150
Results and discussion 151
References 154
Part III: HYPERTENSION PHARMACOLOGICAL AND CLINICAL ASPECTS 156
CHAPTER 27. AN ANALYSIS OF ANTIHYPERTENSIVE DRUGS 158
1. Sympathetic regulation of blood pressure 158
2. Vasodilators acting on vascular smooth muscle 163
3. Drugs which increase sodium and water excretion 164
4. Drugs which interfere with the renin-angiotensin system 165
Some pharmacokinetic considerations 167
Outlook 167
Summary 169
References 170
CHAPTER 28.PHARMACOLOGIC CONTROL OF HYPERTENSIVE EMERGENCIES 176
PHARMACOLOGY OF USEFUL DRUGS 177
PHARMACO-CLINICAL CORRELATIONS 179
References 180
CHAPTER 29. PHARMACOLOGIC CONTROL OF HYPERTENSIVE EMERGENCIES 176
PHARMACOLOGY OF USEFUL DRUGS 177
PHARMACO-CLINICAL CORRELATIONS 179
References 180
CHAPTER 30. SOME STUDIES ON THE CENTRAL ACTIONS OF BETA-ADRENOCEPTOR BLOCKING DRUGS IN MAN 182
Experimental evidence in man 182
Concentrations in brain and cerebrospinal fluid 183
Other central nervous pharmacological effects of beta-blocking drugs 184
Conclusions 184
References 185
CHAPTER 31. MODE OF ACTION OF CENTRALLY ACTING ANTIHYPERTENSIUE DRUGS 186
Introduction 186
Clonidine and related imidazolidines the central a-adrenoceptor
Characteristics of the central a-adrenoceptor 187
Pre- or postsynaptic central a-adrenoceptor? 187
Central hypotensive activity not mediated via ct-adrenoceptors 188
Summary 188
References 189
CHAPTER 32. THE INFLUENCE OF HYPOTENSIVE DRUGS ON ADAPTIVE HEMODYNAMIC REACTIONS 192
1. Introduction 192
2. Methods 192
3. Results 193
4. Comments 196
SUMMARY 196
REFERENCES 196
CHAPTER 33. THE CARDIOVASCULAR PATTERN OF CLONIDINE-LIKE ANTIHYPERTENSIVE SUBSTANCES AND THEIR MODE OF ACTION 198
References 201
CHAPTER 34. INVOLVENMENT OF PRESYNAPTIC AND POSTSYNAPTIC a-ADRENOCEPTORS IN THE ACTION 
204 
References 207
CHAPTER 35. TACHYPHYLAXIS TO THE HYPOTENSIVE EFFECT OF CLONIDINE ON RATS 210
Introduction 210
Methods 210
Results 211
Summary 214
References 214
CHAPTER 36. HYPOTENSIVE EFFECT OF CLOUIDINE AND REGIONAL NORADRENALINE CONCENTRATION IN THE BRAIN OF NORMOTENSIVE AND HYPERTENSIVE RATS AFTER ACUTE AND CHRONIC TREATMENT 216
References 221
CHAPTER 37. THE EFFECT OF INDOMETHACIN ON RENIN-ANGIOTENCIN-ALDOSTERONS SYSTEM IN ESSENTIAL HYPERTENSION 222
INTRODUCTION 222
MATERIALS AND METHODS 222
RESULTS 223
DISCUSSION 226
Summary 227
References 227
CHAPTER 38. CROSS-OVER TRIAL FOR COMPARING ANTIHYPERTENSIVE EPPECTS OP PRAZOSIN AND HYDRALAZINE 228
INTRODUCTION 228
MATERIALS AND METHODS 229
RESULTS 230
DISCUSSION 232
SUMMARY 233
References 233
Acknowledgement 233
CHAPTER 39. TAURINE AND HYPERTENSION 234
Blood pressure, platelet-taurine and age in rats 235
Hypertension in rats induced by subtotal nephrectomy 235
Taurine in platelets of congestive heart and hypertensive patients 236
Comments 237
Summary 238
References 238
CHAPTER 40. PLANNING OF ANTIHYPERTENSIVE PYRIDAZINE COMPOUNDS 240
Methods 241
Results and Discussion 241
Summary 242
References 244
CHAPTER 41. PHARMACOLOGY OF GYKI-11.679, A NEW ANTIHYPERTENSIVE DRUG 246
Methods 246
Results 247
Conclusions 249
References 250
CHAPTER 42. THE ANTIHYPERTENSIVE EFFECT OF MORPHOLINO-PYRIDAZINYL HYDRAZINE AND ITS HYDRAZONE DERIVATIVE 252
Material and Methods 252
Results 253
Conclusions 255
References 256
CHAPTER 43. PHARMACOLOGICAL CONTROL OF DISSEMINATED INTRAVASCULAR COAGULATION (DIC) 258
Introduction 258
Methods 258
Results 259
Discussion 262
Summary 262
References 263
PART IV: THE BETA-ADRENERGIC BLOCKER TOBANUM® 264
CHAPTER 44. PHARMACOLOGY OF GYKI-41099 /CHLORPROPANOL, ....NUM®/ A NEW POTENT BETA-ADRENERGIC ANTAGONIST 266
INTRODUCTION 266
METHODS AND MATERIALS 266
RESULTS 268
SUMMARY 273
REFERENCES 273
CHAPTER 45. EFFECTS OF TOBANUM(GYK1 41099) ON CARDIAC TRANSMEMBRANE POTENTIALS 276
Introduction 276
Methods 276
Results 276
Conclusion 277
References 279
CHAPTER 46. HUMAN PHARMACOKINETIC STUDY ON TOBANUM 280
MATERIAL AND METHODS 280
RESULTS 282
SUMMARY 285
References 285
CHAPTER 47. TOBANUM /GYKI-41099/ EFFECT ON INTRINSIC HEART RATE 286
METHOD 286
RESULTS 288
DISCUSSION 288
SUMMARY 289
REFERENCES 289
CHAPTER 48. ANTIARRHYTHMIC PROPERTIES OF TOBANUM A NEW BETA-BLOCKING AGENT 290
RESULTS 291
DISCUSSION 293
SUMMARY 294
REFERENCES 294
CHAPTER 49. THE HAEMODINAMIC EFFECT OF THE BETA-BLOCKING AGENT GYKT-41099 /TOBANUM®/ ON ISCHEMIC CARDIAC PATIENTS 296
METHODS 296
RESULTS 297
CONCLUSION 299
References 300
CHAPTER 50. TOBANUM /GYKI 41099/ IN HYPERTENSION - A MULTICENTRE CLINICAL TRIAL 302
Methods 302
Results 304
Conclusions 307
Summary 307
Acknowledgement 307
References 307
CHAPTER 51. THE EFFECT OF GYKI-41099 ON PLASMA RENIN ACTIVITY AND BLOOD PRESSURE OF ESSENTIAL HYPERTENSION 308
INTRODUCTION 308
MATERIALS AND METHODS 308
RESULTS 309
DISCUSSION 312
SUMMARY 313
REFERENCES 313
CHAPTER 52. COMPARATIVE STUDY ON TOBANUM® /GYKI-41099/ AND PINDOLOL ON PATIENTS SUPPERING PROM MODERATE OR SEVERE HYPERTENSION 314
MATERIAL AND METHOD 314
SUMMARY 317
REFERENCES 317
CHAPTER 52. EFFECT OF GYKI-41099, A NEW BETA-ADRENERGIC RECEPTOR BLOCKING AGENT, ON THE RESPONSES OF CAROTID SINUS BARORECEPTOR REFLEX IN MAN 320
MATERIAL AND METHODS 321
RESULTS 323
DISCUSSION 325
SUMMARY 325
REFERENCES 326
CHAPTER 53. STUDIES ON A NEW ß -RECEPTOR BLOCKING DRUG: TOBANUM® (1-/2,5-DICHLOROPHENOXY/-3-TERTIARY-BUTYLAMINOPROPANOL-2-HC1). EXPERIENCES IN CARDIOVASCULAR HYPERKINETIC SYNDROME AND ANGINA PECTORIS. EFFECT ON THE RESPIRATION 328
Material and methods 328
Results 328
Summary 332
References 332
CHAPTER 54. PRINCIPLES OF CLINICAL TREATMENT WITH TOBNUM/GYK 1 41099/ IN CARDIAC DYSRHYTHMIAS 334
METHODS 334
RESULTS AND DISCUSSION 335
SUMMARY 337
References 337
CHAPTER 55. COMPARATIVE STUDY OF THE BETA-ADRENERGIC BLOCKING AGENTS GYKI-41099 /TOBANUM/ AND PROPRANOLOL IN THYROTOXIC PATIENTS 338
Methods 340
Results 340
Discussion 341
Summary 342
References 342
CHAPTER 55. COMPARATIVE STUDY OP THE BETA-ADRENERGIC BLOCKING AGENTS GYKI-41099 /TOBANUM/ AND PROPRANOLOL IN THYROTOXIC PATIENTS 338
Methods 340
Results 340
Discussion 341
Summary 342
References 342
PART V: SEROTONIN AND SEROTONIN ANTAGONISTS 344
CHAPTER 56. ON THE EFFECTS OF COMPOUND GYKI-32.594, A NEW POTENT SEROTONIN ANTAGONIST 346
Material and methods 347
Results 348
Conclusion 352
References 353
CHAPTER 57. EFFECTS OF DRUGS AFFECTING SEROTONERGIC SYSTEM ON ACTIVITY OF CENTRAL DOPAMINERGIC AND SEROTONERGIC SYSTEMS IN RATS 354
METHODS AND MATERIALS 354
RESULTS 355
DISCUSSION 357
SUMMARY 358
REFERENCES 358
CHAPTER 58. DOSE-DEPENDENT OPPOSITE EFFECTS OF THE 5-HT RECEPTOR ANTAGONISTS ON THE 5-HT-INDUCED RESPONSES IN THE RAT 360
Introduction 360
Material and methods 360
Results 361
Discussion 362
Summary 363
References 363
CHAPTER 59. EFFECTS OF SOME INDOLINES IN COMPARISON WITH SEROTONIN ON THE GUINEA-PIG ISOLATED ILEUM 364
Introduction 364
Material and Methods 364
Results 365
Discussion 367
Summary 368
References 369
CHAPTER 60. DETECTION OF 5-HYDROXYTRYPTAMINE RECEPTORS IN SOME VASCULAR SMOOTH MUSCLE PREPARATIONS 370
Introduction 370
Materials and methods 370
Results 372
Discussion 373
Summary 373
References 373
PART VI: CLINICAL AND PHARMACOLOGICAL EFFECTS OF CAVINTON® AND RELATED COMPOUNDS 374
CHAPTER 61. THE MODIFICATION OF THE PATHOLOGICAL CEREBRAL CIRCULATION ON THE EFFECT OF CAVINTON 376
Introduction 376
Results 377
Discussion 380
Summary 380
References 380
CHAPTER 62. THE EFFECT OF CAVINTON1 AND XAVIN2 ON THE REDOX CHANGES IN THE BRAIN OF STROKE PATIENTS 382
Introduction 382
Material and methods 382
Results 384
Discussion 386
Summary 387
References 387
CHAPTER 63. CLINICAL STUDIES ON CAVINTON R 388
Introduction 388
Material and Methods 388
CHAPTER 64. THE EFFECT OF CAVINTON® IN ISCHAEMIC DISTURBANCES OF THE CEREBRAL CIRCULATION 394
Introduction 394
Material and Methods 394
Results 395
Discussion 396
Summary 397
References 397
CHAPTER 65. TREATMENT OF ACUTE AND CHRONIC ISCHEMIC CEREBROVASCULAR DISEASE WITH CAVINTON 400
Introduction 400
Material and Methods 400
Summary 405
References 406
CHAPTER 66. EVALUATION OF CAVINTON EFFECTS IN PATIENTS WITH CEREBRAL VASCULAR LESIONS 408
Introduction 408
Material and Methods 408
Results 410
Summary 412
CHAPTER 67. THE VALUE OF CAVINTON THERAPY IN RETINAL AND CHOROIDAL DISORDERS 414
Introduction 414
Material and Methods 414
General results 415
Comments 418
Conclusions 419
Summary 420
CHAPTER 68. EFFECT OF ETHYL-APOVINCAMINATE ON THE COCHLEO-VESTIBULAR SYSTEM - A COMPARATIVE INVESTIGATION 422
Introduction 422
Materials and Methods 422
Results 423
Discussion 425
Summary 426
References 426
CHAPTER 69. CEREBRAL CIRCULATORY, ANTIHYPOXIC AND CNS ACTIVITY OF INDOLE DERIVATIVES 428
Introduction 428
Material and Methods 428
Results 431
Discussion 434
Summary 435
References 435
CHAPTER 70. NEW INDOLE DERIVATIVES INCREASE THE ABILITY OF THE BRAIN TO TOLERATE THE EFFECTS OF SERIAL ASPHYXIC HYPOXIA IN RAT 436
Methods and materials 436
Results 437
Discussion 440
Summary 440
Acknowledgement 440
References 441
CHAPTER 71. BIOCHEMICAL EFFECTS OF SEMI-SYNTHETIC VINCA-ALKALOIDS ON THE CYCLIC AMP SYSTEM 442
Introduction 442
Materials and Methods 443
Results 443
Discussion 445
Summary 446
References 446
CHAPTER 72. A NEW CLASS OF 3' ,5' –cAMP PHOSPHODIESTERASE INHIBITORS: APOVINCINE DERIVATIVES 448
Introduction 448
Material and Methods 448
Results and discussion 449
Summary 451
References 452
SUBJECT INDEX 454

Erscheint lt. Verlag 22.10.2013
Sprache englisch
Themenwelt Medizin / Pharmazie Gesundheitsfachberufe
Medizin / Pharmazie Medizinische Fachgebiete Pharmakologie / Pharmakotherapie
Studium 2. Studienabschnitt (Klinik) Pharmakologie / Toxikologie
ISBN-10 1-4831-4778-9 / 1483147789
ISBN-13 978-1-4831-4778-9 / 9781483147789
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