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Extrahepatic metabolism of zidovudine.

Title: Extrahepatic metabolism of zidovudine.
Authors: Howe, JL; Back, DJ; Colbert, J
Source: British Journal of Clinical Pharmacology ; volume 33, issue 2, page 190-192 ; ISSN 0306-5251 1365-2125
Publisher Information: Wiley
Publication Year: 1992
Collection: Wiley Online Library (Open Access Articles via Crossref)
Description: The metabolism of zidovudine (3′‐azido‐3′‐deoxythymidine; AZT) has been studied in human renal, gut and hepatic microsomes. Metabolism of AZT to the ether glucuronide (3'azido‐3'‐deoxy‐5'‐beta‐D‐glucopyranosyl thymidine; GAZT) occurred in the kidney with Km and Vmax values of 1.50 +/‐ 0.49 mM and 14.5 +/‐ 2.6 nmol h‐1 mg‐1 respectively (mean +/‐ s.d.; n = 3 batches of microsomes from a single kidney). Comparative values obtained in liver were 2.19 +/‐ 0.6 mM and 43.0 +/‐ 9.5 nmol h‐1 mg‐1, respectively. Morphine caused inhibition of AZT conjugation in kidney microsomes. Metabolism of AZT by the kidney could contribute significantly to the overall elimination of AZT. In contrast to the kidney findings, AZT was not metabolised to GAZT by either non‐ activated (Brij‐58) or activated gut microsomes.
Document Type: article in journal/newspaper
Language: English
DOI: 10.1111/j.1365-2125.1992.tb04024.x
Availability: https://doi.org/10.1111/j.1365-2125.1992.tb04024.x; https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1111%2Fj.1365-2125.1992.tb04024.x; https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1365-2125.1992.tb04024.x
Rights: http://onlinelibrary.wiley.com/termsAndConditions#vor
Accession Number: edsbas.5B932145
Database: BASE