Pharmacokinetics of zidovudine after rectal administration in human immunodeficiency virus-infected patients.
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.
Wintergerst
U
U
Children's Hospital, University of Munich, Germany.
Rolinski
B
B
Bogner
J R
JR
Notheis
G
G
Goebel
F D
FD
Roscher
A A
AA
Belohradsky
B H
BH
D000284:Administration, Oral; D000285:Administration, Rectal; D000293:Adolescent; D000328:Adult; D000368:Aged; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D015658:HIV Infections / Q000188:drug therapy / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D015215:Zidovudine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D015215:Zidovudine