Lack of absorption of didanosine after rectal administration in human immunodeficiency virus-infected patients.
The feasibility of rectal administration of didanosine (DDI) was studied in six human immunodeficiency virus-infected patients. After oral intake of a DDI solution (100 mg/m2 of body surface area) combined with an antacid (Maalox), pharmacokinetic parametric values were in accordance with previously published data; the mean +/- standard deviation for terminal half-life was 59.5 +/- 15.0 min, that for peak concentration was 5.2 +/- 3.9 mumol/liter, and that for the area under the time-concentration curve (AUC) was 494 +/- 412 min.mumol/liter. After rectal administration of a similarly prepared DDI solution (100 mg/m2 of body surface area), plasma DDI levels were below the detection limit (0.1 mumol/liter) at all time points in five of the six patients, and in the remaining patient the AUC after rectal application was only 5% of that after oral administration. We conclude that oral administration of DDI cannot be easily replaced by rectal application.
Wintergerst
U
U
Children's Hospital, University of Munich, Germany. uwe.wintergerst@KK-i.med.uni-muenchen.de
Rolinski
B
B
Sölder
B
B
Bogner
J R
JR
Wolf
E
E
Jäger
H
H
Roscher
A A
AA
Belohradsky
B H
BH
D000285:Administration, Rectal; D000293:Adolescent; D000328:Adult; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002648:Child; D016049:Didanosine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D015658:HIV Infections / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008875:Middle Aged
D019380:Anti-HIV Agents; D016049:Didanosine