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Antimicrobial Agents and Chemotherapy, 05 1997, 1143-1145, Vol 41, No. 5
Copyright © 1997 by the American Society for Microbiology. All rights reserved.

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

U Wintergerst, B Rolinski, JR Bogner, G Notheis, FD Goebel, AA Roscher and BH Belohradsky
Children's Hospital, University of Munich, Germany.

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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