PHARMACOKINETICS OF RIBAVIRIN AND URINARY-EXCRETION OF THE MAJOR METABOLITE 1,2,4-TRIAZOLE-3-CARBOXAMIDE IN NORMAL VOLUNTEERS
Articolo
Data di Pubblicazione:
1989
Citazione:
PHARMACOKINETICS OF RIBAVIRIN AND URINARY-EXCRETION OF THE MAJOR METABOLITE 1,2,4-TRIAZOLE-3-CARBOXAMIDE IN NORMAL VOLUNTEERS / R. PARONI, M. DELPUPPO, C. BORGHI, C.R. SIRTORI, M.G. KIENLE. - In: INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY THERAPY AND TOXICOLOGY. - ISSN 0174-4879. - 27:6(1989 Jun), pp. 302-307.
Abstract:
Ribavirin (1-B-D-ribofuranosyl-1,2,4-trtazole-3-carboxamide) is a broad spectrum
antiviral agent, with a primary indication in human immunodeficiency virus (HIV) infection,
but with significant activity against more common viral pathogens. Since the available kinetic
data are only in HIV patients, a study was carried out in normal volunteers, also with the
objective of obtaining data on the biotransformation of the drug. A specific HPLC method
was used to determine both the unchanged drug and its major metabolite (7,2,4-triazole-3-
carboxamide). The unchanged drug was confirmed to have a long plasma half-life, ranging
from 30.4 to 61.0 h with a total clearance of 20.3 +/- 10.6 l/h. The comparison of oral and
i.v. administrations, showed 32.6 +/- 16.7% oral bioavailability. By investigating the urinary
excretion of the unchanged drug and its metabolite, it was shown that the percentage of the
metabolite is almost doubled after oral administration (28.8% vs 6.2% after i.v.) with a corresponding inverse difference in the percentages of urinary unchanged ribavirin (16.7%
after i.v. vs 4.1% after oral administration).
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
ribavirin kinetics; 1,2,4-triazole-3-carboxamide excretion; HPLC; healthy
volunteers
Elenco autori:
R. PARONI, M. DELPUPPO, C. BORGHI, C.R. SIRTORI, M.G. KIENLE
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