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1996-03-30
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Document 1084
DOCN M9651084
TI The effect of food on pharmacokinetics of zalcitabine in HIV-positive
patients.
DT 9505
AU Nazareno LA; Holazo AA; Limjuco R; Passe S; Twardy SK; Min B; Massarella
JW; Hoffmann-La Roche Inc., Department of Clinical Pharmacology,;
Nutley, New Jersey 07110, USA.
SO Pharm Res. 1995 Oct;12(10):1462-5. Unique Identifier : AIDSLINE
MED/96117509
AB PURPOSE. The purpose of this study was to determine the effect of food
on the pharmacokinetics of zalcitabine in HIV-positive patients.
METHODS. Twenty patients received single oral 1.5 mg doses of
zalcitabine with and without a standard breakfast in an open-label,
randomized crossover study with at least a one week washout period
between treatments. Serial blood and urine samples were collected over
24 hours and assayed for zalcitabine by a modified GC/MS method.
RESULTS. Administration with food delayed and prolonged absorption
resulting in a decrease of approximately 39% in maximal plasma
concentrations compared to dosing under fasting conditions. Comparison
of plasma AUC values indicated a small (14%) reduction in
bioavailability when given with food. Approximately 59% and 45% of the
dose were excreted unchanged in the urine under fasting and fed
conditions, respectively. CONCLUSIONS. The results of this study show
that the administration of zalcitabine with food results in a mild
reduction in bioavailability. Although these changes are not expected to
be of clinical importance, further studies must be conducted for
confirmation.
DE Acquired Immunodeficiency Syndrome/DRUG THERAPY/*METABOLISM Adult
Antiviral Agents/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS/ THERAPEUTIC
USE AIDS-Related Complex/DRUG THERAPY/*METABOLISM Biological
Availability Female *Food Human HIV Infections/DRUG
THERAPY/*METABOLISM Male Middle Age Reverse Transcriptase
Inhibitors/ADMINISTRATION & DOSAGE/ *PHARMACOKINETICS/THERAPEUTIC USE
Zalcitabine/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS/THERAPEUTIC USE
JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).