| Alteration of zidovudine pharmacokinetics by probenecid in patients with AIDS or AIDS-related complex. | |
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MedLine Citation:
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PMID: 2582706 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The anti-human immunodeficiency virus drug zidovudine is metabolized extensively in human beings to the 5'-glucuronide (GAZT) and is cleared rapidly, resulting in a short half-life and the need for frequent dosing. This study explores whether probenecid, which is also metabolized by glucuronidation, reduces zidovudine clearance when zidovudine is administered orally to patients with acquired immunodeficiency syndrome (AIDS) or AIDS-related complex (ARC). The mean zidovudine plasma levels were significantly higher after concurrent administration of probenecid than in its absence, resulting in a twofold increase in the mean AUC, a corresponding decline in the apparent total clearance, and a prolongation in the mean half-life. Similar alterations were observed in GAZT disposition. There was a marked reduction in the urinary excretion ratio of GAZT to zidovudine and a decline in the renal clearance of GAZT after probenecid coadministration. Probenecid inhibits zidovudine glucuronidation and renal excretion of GAZT. |
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Authors:
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P de Miranda; S S Good; R Yarchoan; R V Thomas; M R Blum; C E Myers; S Broder |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Clinical pharmacology and therapeutics Volume: 46 ISSN: 0009-9236 ISO Abbreviation: Clin. Pharmacol. Ther. Publication Date: 1989 Nov |
Date Detail:
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Created Date: 1989-12-26 Completed Date: 1989-12-26 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0372741 Medline TA: Clin Pharmacol Ther Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 494-500 Citation Subset: AIM; IM; X |
Affiliation:
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Wellcome Research Laboratories, Research Triangle Park, NC. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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AIDS-Related Complex
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metabolism* Acquired Immunodeficiency Syndrome / metabolism* Adult Drug Interactions Drug Therapy, Combination Half-Life Humans Male Middle Aged Probenecid / pharmacokinetics, pharmacology* Regression Analysis Zidovudine / analogs & derivatives, blood, pharmacokinetics*, urine |
| Chemical | |
Reg. No./Substance:
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117675-21-5/3'-azido-3'-deoxy-5'-O-beta-glucopyranuronosylthymidine; 30516-87-1/Zidovudine; 57-66-9/Probenecid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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