Pharmacokinetics. Antibiotics and Chemotherapy. Vol. 25

Transcription

1 Pharmacokinetics Antibiotics and Chemotherapy Vol. 25 Series Editors H. SCHNFELD, Grenzach; R. W. BROCKMAN, Birmingham, Ala, and F.E. HAHN, Washington, D.C. S. Karger Basel Mnchen. Paris London New York Sydney Pharmacokinetics Volume Editor H. SCHNFELD, Grenzach 58 figures and 70 tables, 1978 S. Karger Basel Mnchen Paris London New York Sydney Antibiotics and Chemotherapy Vol. 23: Fundamentals in Cancer Chemotherapy. Anticancer Symposium held in Connection with the 10th International Congress of Chemotherapy, Zurich, September Ed.: F. M. SCHABEL, Jr. (Birmingham, Ala.). VIII p., 62 fig., 1 cpl., 91 tab., 1978 ISBN Vol. 24: Application of Cancer Chemotherapy. Anticancer Symposium held in Connection with the 10th International Congress of Chemotherapy, Zurich, September Ed.: F.M. SCHABEL, Jr. (Birmingham, Ala). VIII p., 42 fig., 96 tab., 1978 ISBN Cataloging in Publication Pharmacokinetics Volume editor, H. Schnfeld. - Basel, New York, Karger, (Antibiotics and chemotherapy, vol. 25) 1. Kinetics 2. Pharmacology 1. Schnfeld, HANS, ed. II. Title III. Series WI AN855G v.25/qv 38 P533 ISBN All rights reserved.

2 No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Copyright 1978 by S.Karger AG, 4011 Basel (Switzerland), Arnold-Bocklin-Strasse 25 Printed in Switzerland by Genossenschaftsdruckerei, Zurich ISBN Contents Penicillins T. BERGAN (Oslo)... 1 Introduction... 2 History... 3 Molecular Synthesis... 3 Chemical Structure of Penicillin Chemical Properties of Penicillins Methods of Determination Evaluation Influence of Chemical Structure on Pharmacokinetics of Penicillin Synergism Biopharmaceutics Metabolism Protein Binding Pharmacokinetics Penetration of Penicillins Renal Function and Excretion Characteristics of the Different Penicillins Adicillin Amoxycillin Ampicillin Ancillin Azidocillin Azlocillin Bacampicillin Bacmecillinam Basic Penicillins Benzylpenicillin Early Penicillins Phenoxymethylpenicillin... 67

3 Phenoxyalkylpenicillins Contents VI Betacin Carbenicillin Carfecillin Clometocillin Cyclacillin Epicillin Guanylureidopenicillin Hetacillin Indanylcarbenicillin (Carindacillin) Isoxazolypenicillins Mecillinam Metampicillin Methicillin Mezlocillin Nafcillin Pirbenicillin Piperacillin Pirazocillin Pivampicillin Pivmecillinam Quinacillin Sulfocillin (Sulbenicillin) Suncillin Talampicillin Ticarcillin Appendix References Pharmacokinetics of Cephalosporin Antibiotics J. M. BROGARD, F. CoMTE and M. PINGET (Strasbourg) Cephalothin Absorption Distribution Elimination Cephaloridine Absorption Distribution

4 Elimination Cephacetrile Absorption Distribution Elimination Cefazolin Absorption Distribution Elimination Contents VII Cephradine Absorption Distribution Elimination Cephapirin Absorption Distribution Elimination Cephanone Absorption Distribution Elimination Cefamandole Absorption Distribution Elimination Cefoxitin Absorption Distribution Elimination Cefuroxime Absorption Distribution Elimination Cefatrizine Absorption Distribution Elimination Ceftezole Cefazaflur

5 Cefalexin Absorption Distribution Elimination Cephaloglycin Absorption Distribution Elimination References Pharmacokinetics of Aminoglycosides in Subjects with Normal and Impaired Renal Function A. LEROY, G. HUMBERT, G. OKSENHENDLER and J.P. FILLASTRE (Rouen) I. Introduction II. General Pharmacokinetic Properties of Aminoglycoside Antibiotics Contents VII III. Pharmacokinetic Parameters of Aminoglycoside Antibiotics A. Subjects with Normal Renal Function B. Uraemic Patients C. In Haemodialyzed Patients D. Correlations Correlation between Serum Elimination Half-Lives (TYo) and Serum Creatinine Levels Linear Correlation between Overall Elimination Rate Constant (Ke) and Endogenous Creatinine Clearances (Ccr) IV. Dosage Schedules A. In Normal Healthy Individuals B. In the Uraemic Patient C. In the Haemodialyzed Patient V. Conclusion Summary References Pharmacokinetics of Erythromycin in Man J. T. WILSON and C.J. VAN BOXTEL (Nashville, Tenn) I. Absorption II. Distribution III. Elimination

6 IV. Miscellaneous Information References Lincomycin and Clindamycin D.M.D. RIMMER and S.E.L. SALES Clindamycin Solubility Bioavailability Studies Clindamycin HCI Hydrate Clindamycin Palmitate HCl Clindamycin Phosphate Protein Binding Concentration of Clindamycin in Human Tissues and Fluids Biological Half-Life Excretion of Clindamycin Lincomycin Solubility Data Lincomycin - BioavaiIability Studies Lincomycin Hydrochloride Solution Lincomycin Hydrochloride Syrup Contents IX Protein Binding Concentrations of Lincomycin Hydrochloride in Various Human Tissues and Fluids Biological Half-Life Excretion of Lincomycin References The Combination Trimethoprim-Sulphamethoxazole I. HANSEN (Copenhagen) Absorption Distribution Metabolism Elimination Interaction with Other Substances Physico-Chemical Properties Method of Determination TMP SMZ

7 References The Pharmacokinetics of Nitrofurantoin and its Related Bioavailability J.D. CoNKLIN (Norwich, N.Y.) Introduction Physical Properties Drug Analysis Absorption Distribution Excretion Metabolism Bioavailability Summary Acknowledgements References Antifungal Agents E. DROUHET (Paris) Introduction Polyene Antifungal Antibiotics Contents XI 1. Chemical Structure and Physico-Chemical Properties Biological Properties Nystatin Chemical and Miscellaneous Data Absorption, Distribution, Elimination Amphotericin Chemical and Miscellaneous Data Absorption Distribution Elimination Local Injections Hamycin Saramycetin Griseofulvin Chemical and Miscellaneous Data Absorption Distribution and Elimination

8 5-F1uorocytosine or 5-Flucytosine Chemical and Miscellaneous Data Absorption Distribution Elimination Imidazole Antifungals Clotrimazole Chemical and Miscellaneous Properties Systemic Administration a) Absorption b) Distribution c) Elimination Dermal Application Miconazole Chemical and Miscellaneous Data Absorption Distribution Elimination Econazole Chemical and Miscellaneous Data Absorption, Distribution, Elimination References Interactions between Antibiotics and Other Drugs A.J. BINT and D.S. REEVES (Bristol) I. Classification of Interactions II. Absorption Contents XI A. Complexation Tetracyclines - Metals Lincomycin - Kaolin-Pectin Lincomycin - Cyclamate B. Alteration of Motility Isoniazid - Antacids Para-Aminosalicyclic Acid (PAS) - Diphenhydramine C. Induced Malabsorption States Neomycin - Digoxin Para-Aminosalicyclic Acid (PAS) - Rifampicin Neomycin - Penicillin

9 D. Parenteral Sulphonamides - Local Anaesthetics III. Distribution Sulphonamides - Tolbutamide Sulphonamides - Methotrexate Sulphonamides - Warfarin Sulphonamides - Thiopentone Sulphonamides - Diphenylhydantoin (DPH) Nalidixic Acid - Warfarin Sulphonamides - Displacing Agents Penicillins - Displacing Agents IV. Sites of Action Aminoglycosides - Muscle Relaxants Colistin - Muscle Relaxants Aminoglycosides - Diuretics Aminoglycosides - Cephalosporins Cephalosporins - Diuretics Tetracycline - Methoxyflurane Aminoglycosides - Methoxyflurane Colistin - Cephalothin Tetracycline - Diuretics Rifampicin - Halothane Rifampicin - Isoniazid Ampicillin - Allopurinol Co-Trimoxazole - Pyrimethamine V. Metabolism A. Increased Metabolism Rifampicin - Warfarin Rifampicin - Tolbutamide Rifampicin - Oral Contraceptives Rifampicin - Corticosteroids Doxycycline - Antiepileptic Drugs and Barbiturates B. Decreased Metabolism Sulphonamides - Diphenylhydantoin (DPH) Sulphonarnides - Tolbutamide Sulphonamides - Warfarin Contents XII 4. Chloramphenicol - Diphenylhydantoin (DPH) Chloramphenicol - Tolbutamide Chloramphenicol - Dicoumarol

10 7. Chloramphenicol- Cyclophosphamide Triacetyloleandomycin - Carbamazepine Isoniazid, Para-Aminosalicylic Acid - Diphenylhydantoin (DPH) Para-Acetylsalicylic Acid (PAS) - Isoniazid Isoniazid - Disulfiram Metronidazole - Disulfiram Metronidazole - Alcohol Furazolidone - Monoamine Oxidase Inhibitors, etc VI. Excretion Penicillins and Cephalosporins - Probenecid Penicillin - Other Drugs Para-Aminosalicyclic Acid (PAS) - Probenecid VII. Miscellaneous Antibiotics - Oral Contraceptives Neomycin - Warfarin Penicillins - Coumarins Rifampicin - Probenecid Pyrazinamide - Para-Aminosalicylic Acid (PAS), etc Sulphamethoxypyridazine - Multiple Drug Therapy VIII. Conclusion References