Metabolism of radioactive cyclophosphamide.Animal tests and clinical studies

Graul, E.H.; Schaumlöffel, E; Hundeshagen, H.; Wilmanns, H.; Simón, García

doi:10.1002/1097-0142(1967)20:5<896::aid-cncr2820200551>3.0.co;2-d

Cited by 71 publications

(9 citation statements)

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“…This might be due to the presence of a very slowly exchange compartment. However, the present data are too few and previous studies (GRAUL et al 1967 have been of too short duration to allow any safe conclusions. Further studies with prolonged sampling are needed to elucidate these very important conditions.…”

Section: Discussionmentioning

confidence: 59%

“…Subsequently the concentra-tion of the metabolites increased steadily and after 2 days constituted nearly all the activity of the serum. In contrast to this only insignificant amounts of or no metabolites could be demonstrated in the serum in normal subjects some 12-24 hours after injection of cyclophosphamide (GRAUL et al 1967; DEVITA & ADAMSON 1970; BR~CK et al 1971; BAGLEY et al 1973; MOURID-SEN et al 1974).…”

Section: Discussionmentioning

confidence: 94%

“…In normal subjects cyclophosphamide is eliminated by biotransformation to metabolites and to a lesser extent by renal excretion. As regards the metabolites the major route of elimination is renal (~U L et al 1967;DEVITA & ADAMSON 1970; BAGLEY et al 1973;MOURIDSEN et al 1974).…”

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confidence: 99%

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Pharmacokinetics of Cyclophosphamide in Renal Failure

Mouridsen

Jacobsen

1975

Acta Pharmacologica et Toxicologica

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The metabolism of cyclophosphamide was determined in five patients with severe renal insufficiency. After the intravenous injection of 14C‐cyclophosphamide the activities due to unchanged cyclophosphamide and metabolites were determined in samples from urine and serum for 2–3 days. Only 22% of the injected radioactivity could be recovered in the urine during the first 3 days as against the normal of some 65%. The rate of biotransformation seemed normal and in agreement with these findings a very long term retention of metabolites could be demonstrated. The clinical implications of these results are discussed.

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Section: Discussionmentioning

confidence: 59%

Section: Discussionmentioning

confidence: 94%

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Pharmacokinetics of Cyclophosphamide in Renal Failure

Mouridsen

Jacobsen

1975

Acta Pharmacologica et Toxicologica

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“…This view would be reasonably understandable if the drug action of BLM as a cytostatic agent is considered, and would be supported by the observation that, with regard to meningioma, which is both an intracranial and an extracerebral tumour, higher concentration of BLM was found in the tumours showing histological malignancy. The second possible explanation is that the blood brain barrier in brain tumour tissue of higher malignancy might be more defective (Hossmann, 1967) and less limiting to drug entrance into the Graul et al (1967), who have made drug distribution studies using tritiated cyclophosphamide, suggested that the drug concentration in the tumour is largely dependent upon the blood supply to the tissue. If it is accepted that the tumour stain on cerebral angiography indicates abundant blood supply to the tumour, the findings obtained by us do not support the view that uptake of BLM by the tumour is dependent on blood supply.…”

Section: Discussionmentioning

confidence: 99%

Uptake of bleomycin by human brain tumours

Hayakawa

Ushio

Morimoto

et al. 1976

Journal of Neurology, Neurosurgery & Psychiatry

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SYNOPSISThe uptake of bleomycin (BLM) by various types of brain tumours after intravenous or intrathecal administration was investigated by bioassay in 67 patients. The correlation between the BLM distribution and the type and characteristics of brain tumours was studied.Bleomycin (BLM), discovered by Umezawa et al. (1966a, b) is a kind of cytostatic antibiotic complex produced by a strain of Streptomyces verticillus, and was found by Ichikawa et al. (1967Ichikawa et al. ( , 1968 to be highly effective against human squamous cell carcinoma. These authors observed relatively high concentration of BLM in the skin after subcutaneous injection in mice, and suggested that the therapeutic effect on squamous cell carcinoma might be related to the high concentration of BLM in the skin Umezawa et al., 1967Umezawa et al., , 1968a.Recently, Mamo et al. (1973) found that radioactive BLM (57Co-BLM) was superior to technetium-99m (Tc-99m) for the diagnosis of malignant intracranial tumours, and Takeuchi et al. (1969, 1972)

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“…Cyclophosphamide is converted by hepatic microsomal enzymes into the active metabolite, aldophosphamide, which is further converted to carboxyphosphamide by a soluble enzyme thought to be aldehyde oxidase GRAUL et al, 1967;RAUEN and KRAMER, 1964). Cyclophosphamide is converted by hepatic microsomal enzymes into the active metabolite, aldophosphamide, which is further converted to carboxyphosphamide by a soluble enzyme thought to be aldehyde oxidase GRAUL et al, 1967;RAUEN and KRAMER, 1964).…”

Section: Antagonistic Drug Interactionsmentioning

confidence: 99%

Concepts in Biochemical Pharmacology

Brodie¹,

Gillette²,

Ackerman³

1975

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This work is subject to copyright. All rights are reserved, whether the whole or part of the material is concerned specifically those of translation, reprinting, re-use of illustrations, broadcasting, reproduction by photocopying machine or similar means, and storage in data banks. Under § 54 of the German Copyright Law where copies are made for other than private use, a fee is payable to the publlsher, the amount of the fee to be determined by agreement with the publisher. © by Springer-Verlag Berlin· Heidelberg 1975. Softcover reprint of the hardcover ist edition 1975 Library of Congress Cataloging in Publication Data (Revised) Main entry under title: Concepts in biochemical pharmacology. Handbuch der experlmentellen Pharmakologie. Handbook of experimental pharmacology. New series, v. XXVIII, 1, etc. Includes bibliographies. I. Drug metabolism-Collected works.!. Argy, W. P. II. Brodie, B. B., ed. III. Gillette, James R., 1928-ed. IV. Ackerman, Helen S., ed. V. Series: Handbuch der experimentellen Pharmakologle, v. XXVIII, 1 QP905.H3 Bd. 28, t. 1, etc. [RM301] 615'. 7 79-135957 ISBN 0-387-05134-1. The use of general descriptive names, trade names, trade marks, etc. in this pUblication, even if the former are not especially Identified, is not to be taken as a sign that such names, as understood by the Trade Marks and Merchandise Marks Act, may accordlngiy be used freely by anyone. PrefacePart 3 of the Handbook of Experimental Pharmacology (Concepts in Biochemical Pharmacology) applies the principles enunciated in Parts 1 and 2 to clinical pharmacology and toxicology. The major objective is to elucidate the many factors that determine the relationships between pharmacokinetic aspects of the disposition and metabolism of drugs and their therapeutic or toxic actions in man.Because of the more restricted information obtainable in human studies, this volume reflects the editors' bias that an understanding of pharmacokinetics is fundamental for assessing pharmacologic or toxicologic effects of drugs in humans. The first chapter is a unique primer on when to apply and how to use pharmacokinetic tools in human pharmacology. The second chapter explains the general assumptions underlying pharmacokinetic approaches both in simple terms for the novice and in mathematical form for the more sophisticated reader.Several chapters on determinants of drug concentration and activity discuss drug absorption, drug latentiation, drugs acting through metabolites, enterohepatic drug circulation, influence of route of drug administration on response, genetic variations in drug disposition and response, age differences in absorption, distribution and excretion of drugs, and pathologic and physiologic factors affecting absorption, distribution and excretion of drugs and drug response. The focus of these chapters is data obtained in human, rather than animal, studies. Most of the chapters contain new material never summarized previously.The section on drug interactions opens with a chapter in which all drug interactions are viewed as result...

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Metabolism of radioactive cyclophosphamide.Animal tests and clinical studies

Cited by 71 publications

References 0 publications

Pharmacokinetics of Cyclophosphamide in Renal Failure

Pharmacokinetics of Cyclophosphamide in Renal Failure

Uptake of bleomycin by human brain tumours

Concepts in Biochemical Pharmacology

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