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Literature DB >> 9145885

Pharmacokinetics of zidovudine after rectal administration in human immunodeficiency virus-infected patients.

U Wintergerst¹, B Rolinski, J R Bogner, G Notheis, F D Goebel, A A Roscher, B H Belohradsky.

Abstract

We evaluated the pharmacokinetics of rectally administered zidovudine (ZDV) in 10 human immunodeficiency virus-infected adults. After rectal administration of an aqueous ZDV solution (250 mg of ZDV), mean peak ZDV levels were 1.3 +/- 0.7 micromol/liter (mean +/- standard deviation) versus 5.0 +/- 2.2 micromol/liter (P < 0.0001) after oral intake of a 250-mg ZDV capsule. The half-life at beta phase was 87.8 +/- 39.6 min for rectally administered ZDV versus 55.8 +/- 20.1 min (P = 0.035) for orally administered ZDV. The mean area under the concentration-time curve from 0 min to infinity was 232 +/- 181 micromol/liter x min after rectal administration versus 362 +/- 110 micromol/liter x min after oral intake. Although the two routes were not bioequivalent, ZDV was absorbed considerably after rectal administration, with a pharmacokinetic profile resembling that of a sustained-release device.

Entities: Chemical Disease Species

Mesh：

Substances：
Zidovudine

Year: 1997 PMID： 9145885 PMCID： PMC163866

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

15 in total

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Journal: Chem Pharm Bull (Tokyo) Date: 1990-11 Impact factor: 1.645

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Authors: M A Hedaya; R J Sawchuk
Journal: J Pharm Sci Date: 1989-09 Impact factor: 3.534

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Journal: N Engl J Med Date: 1994-11-03 Impact factor: 91.245