Chemotherapy (eBook)

Front Cover 1
Chemotherapy 4
Copyright Page 5
Table of Contents 6
Introduction 8
Part 1: Chemotherapy of Schistosomiasis 10
Chapter 1. Recent Advances in the Experimental Chemotherapy of Schistosomiasis 12
Chapter 2. Antischistosomal Activity of a Nitrodiphenyl-aminoisothiocyanate (C 9333-Go/CGP 4540) against Schistosoma Japonicum (Philippine Strain) in Mice and Rabbits 18
SUMMARY 18
INTRODUCTION 18
MATERIALS AND METHODS 18
RESULT 19
DISCUSSION 22
ACKNOWLEDGEMENT 25
REFERENCES 25
Chapter 3. 4-Isothioeyanato-4' -Nitrodiphenylamine (C 9333-Go/CGP 4540), an Antischistosomal Compound with an Unusual Spectrum of Anthelminthic Activity Against Intestinal Nematodes, Filariae and Trematodes 26
ABSTRACT 26
1. INTRODUCTION 26
2. MATERIALS AND METHODS 27
3. RESULTS 28
4. DISCUSSION AND CONCLUSIONS 34
5. REFERENCES 34
Chapter 4. Clinical Experience with Oxamniquine 36
PATIENTS TREATED IN THE HOSPITAL ENVIRONMENT 36
PATIENTS TREATED IN ENDEMIC AREAS 40
DISCUSSION 45
REFERENCES 47
Chapter 5. Clinical Experiences with, and Pharmacokinetics of, Oxamniquine 50
Chapter 6. Progress in the Chemotherapy of Schistosomiasis 58
METRIFONATE (BILARCIL (R) ) 58
OXAMNIQUINE (MANSIL (R) ) 59
IA-4 N-OXIDE 5 ) 60
AMOSCANATE (C9333-Go/CGP 4540) 60
R0 11-0761 60
35 972 R.P 61
80.647 (SP 647) 61
PRAZIQUANTEL (BILTRICIDE (R) ) 62
REFERENCES 64
Chapter 7. New Approaches Towards the Development of Safer Schistosomicidal Drugs 68
ABSTRACT 68
REFERENCES 74
Part 2: New Trends in Malaria Chemotherapy 78
Chapter 8. Some Promising Leads in Experimental Antimalarial Drugs 80
Quinoline methanols 81
WR142490: Mefloquine 81
9-Phenanthrenemethanols 82
Quinazolines 84
Chapter 9. Experimental Infections with Human Plasmodia in Owl Monkeys - Their Contri-butionsto Development of New Broadly Active Blood Schizonticidal Drugs 88
ABSTRACT 88
INTRODUCTION 88
EXPERIMENTAL 89
COMMENT 97
REFERENCES 98
Chapter 10. Drug Combination in Malaria 100
1. Introduction 100
2. Rationale for Combining Drugs in Anti-infectious Chemotherapy 101
3. Choice of a Combination Partner 103
4. Conclusion 106
References 107
Chapter 11. The U.S. Army Drug Development Program 108
INTRODUCTION 108
METHODS 108
RESULTS 113
SUMMARY AND CONCLUSIONS 115
REFERENCES 116
Chapter 12. The Role of the World Health Organization in the Development of New Antimalarials 118
ABSTRACT 118
INTRODUCTION 118
THE MALARIA SITUATION 119
PRESENT MEANS AND CONSTRAINTS OF MALARIA CONTROL 121
PRESENT CONCEPT OF MALARIA CONTROL 123
PRESENT ROLE OF DRUGS IN ANTIMALARIA OPERATIONS 123
MALARIA RESEARCH IN THE PROGRAMME OF WHO 125
REFERENCES 127
Part 3: New Trends in Cancer Chemotherapy and their Pharmacological Basis 128
Chapter 13. Cancer Chemotherapy - An Overview 130
References 133
Chapter 14. Recent Studies on Antitumor Antibiotics 136
BLEOMYCIN 136
ANTHRACYCLINE ANTIBIOTICS 139
NEOTHRAMYCIN 140
SMALL MOELCULAR IMMUNE-ENHANCING COMPOUNDS PRODUCED BY STREPTOMYCES 141
CONCLUSION 143
REFERENCES 144
Chapter 15. The Relation of Cell Kinetics to Cancer Chemotherapy 146
THE EMPIRICAL USE OF KINETIC DATA 147
THE RELATIONSHIP BETWEEN INITIAL CELL KILL IN TUMOURS AND THEIR KINETIC STATE 147
THE SIZE-DEPENDENCE OF THERAPEUTIC RESPONSE 148
SHORT-TERM SYNERGISM BETWEEN ANTICANCER AGENTS 150
THE RECOVERY OF TUMOURS AND NORMAL TISSUES BETWEEN TREATMENTS 151
CONCLUSIONS 153
REFERENCES 153
Chapter 16. Pharmaeokinetics and Cancer Chemotherapy 156
INTRODUCTION 156
ARABINOSYLCYTOSINE AND L1210 LEUKEMIA 157
METHOTREXATE PHARMACOKINETICS AND DRUG EFFECTS 157
RESISTANCE OF LEWIS LUNG MURINE TUMOR TO MTX TREATMENT 158
CITROVORUM FACTOR 158
PHYSIOLOGICAL PHARMACOKINETICS - APPLICATIONS 159
CONCLUSION 161
REFERENCES 162
Chapter 17. Human Toxicology and Pharmacology of the Anthracycline Antibiotics 164
INTRODUCTION 164
DOSAGE, ACTIVITY, AND TOXICOLOGY 164
PHARMACOLOGY 165
REFERENCES 167
Chapter 18. Impact of Chemotherapy on Osteogenic Sarcoma 170
ABSTRACT 170
KEYWORDS 170
INTRODUCTION 170
CHEMOTHERAPY REGIMENS 171
RESULTS 173
DISCUSSION 176
REFERENCES 177
Part 4: Cell Cultures as Tool in Pharmacological Investigations 180
Chapter 19. Opioid Action on Cultured Neuroblastoma X Glioma Hybrid Cells 182
ABSTRACT 182
INTRODUCTION 183
CONCLUSION 190
ACKNOWLEDGEMENT 191
REFERENCES 191
Chapter 20. Aryl Hydrocarbon Hydroxylase. Evidence of Receptors for Induction Process in Cell Culture 194
ABSTRACT 194
INTRODUCTION 194
ACKNOWLEDGMENT 204
REFERENCES 204
Chapter 21. NGF-Responsive Clonal PG12 Pheochromocytoma Cells as Tools for Neuropharmacologic Investigations 206
INTRODUCTION 206
PROPERTIES OF PC12 CELLS 206
RESPONSE TO NERVE GROWTH FACTOR (NGF) 208
GROWTH AND MAINTENANCE OF PC12 CELLS 211
SUMMARY AND CONCLUSIONS 213
ACKNOWLEDGEMENTS 214
REFERENCES 214
Part 5: Invited Lecture 216
Chapter 22. Drug-Receptor Interactions: The Example of ß-Lactam Antibiotics 218
BIOSYNTHESIS OF BACTERIAL CELL WALLS: THE TARGET OF PENICILLIN ACTION 219
THE TIPPER-STROMINGER HYPOTHESIS: PENICILLINS ARE STRUCTURAL ANALOGSOF THE ENDS OF NASCENT PEPTIDOGLYCAN STRANDS 219
OCCURRENCE OF MULTIPLE PENICILLIN BINDING PROTEINS IN BACTERIA 221
MULTIPLICITY OF PENICILLIN BINDING PROTEINS IN BACILLUS SUBTILIS 222
ISOLATION OF CLOXACILLIN-RESISTANT MUTANTS OF BACILLUS SUBTILIS 223
PENICILLIN BINDING PROTEINS OF STAPHYLOCOCCUS AUREUS AND ESCHERICHIA COLI 224
ISOLATION OF PENICILLOYL- AND ACYL-ENZYME COMPLEXES 225
MEMBRANE ATTACHMENT REGION OF THE D-ALANINE CARBOXYPEPTIDASES 227
REFERENCES 229
Index 234