Document Detail

Alteration of zidovudine pharmacokinetics by probenecid in patients with AIDS or AIDS-related complex.
MedLine Citation:
PMID:  2582706     Owner:  NLM     Status:  MEDLINE    
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.
P de Miranda; S S Good; R Yarchoan; R V Thomas; M R Blum; C E Myers; S Broder
Related Documents :
9608706 - An illustrated guide to rflp troubleshooting.
18249936 - Perceiving geometric patterns: from spirals to inside-outside relations.
16769436 - Global change ecology.
25250406 - Preventing suicide at suicide hotspots: a case study from australia.
4009826 - Early problems encountered with the mentor inflatable penile prosthesis.
19412186 - Active nuclear import and cytoplasmic retention of activation-induced deaminase.
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Clinical pharmacology and therapeutics     Volume:  46     ISSN:  0009-9236     ISO Abbreviation:  Clin. Pharmacol. Ther.     Publication Date:  1989 Nov 
Date Detail:
Created Date:  1989-12-26     Completed Date:  1989-12-26     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0372741     Medline TA:  Clin Pharmacol Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  494-500     Citation Subset:  AIM; IM; X    
Wellcome Research Laboratories, Research Triangle Park, NC.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
AIDS-Related Complex / metabolism*
Acquired Immunodeficiency Syndrome / metabolism*
Drug Interactions
Drug Therapy, Combination
Middle Aged
Probenecid / pharmacokinetics,  pharmacology*
Regression Analysis
Zidovudine / analogs & derivatives,  blood,  pharmacokinetics*,  urine
Reg. No./Substance:
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

Previous Document:  Catheter-induced aortic thrombus masquerading as coarctation of the aorta.
Next Document:  Sulfation pharmacogenetics: correlation of human platelet and small intestinal phenol sulfotransfera...