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

Uwe Wintergerst | Zendy; Boris Rolinski | Zendy; J. R. Bogner | Zendy; Gundula Notheis | Zendy; F.-D. Goebel | Zendy; A. Roscher | Zendy; B. H. Belohradsky | Zendy

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

Author(s) -

Uwe Wintergerst,

Boris Rolinski,

J. R. Bogner,

Gundula Notheis,

F.-D. Goebel,

A. Roscher,

B. H. Belohradsky

Publication year - 1997

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.41.5.1143

Subject(s) - zidovudine , pharmacokinetics , liter , bioequivalence , rectal administration , oral administration , sida , medicine , half life , pharmacology , viral disease , human immunodeficiency virus (hiv) , virology

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.

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