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Lack of absorption of didanosine after rectal administration in human immunodeficiency virus-infected patients.
Wintergerst U; Rolinski B; Solder B; Bogner JR; Wolf E; Jager H; Roscher
August 30, 1999
Antimicrob Agents Chemother. 1999 Mar;43(3):699-701. Unique Identifier :

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.

CLINICAL TRIAL JOURNAL ARTICLE Administration, Rectal Adolescence Adult Anti-HIV Agents/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS Area Under Curve Child Didanosine/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS Half-Life Human HIV Infections/*METABOLISM Intestinal Absorption Male Middle Age