Cargando…

The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.

OBJECTIVE: The transfer of abacavir, a new nucleoside inhibitor, and amprenavir, a new protease inhibitor, used for the treatment of human immunodeficiency virus, has been studied in the ex vivo human placental model. METHODS: The ex vivo human placental model used C14 antipyrine to determine the tr...

Descripción completa

Detalles Bibliográficos
Autor principal: Bawdon, R E
Formato: Texto
Lenguaje:English
Publicado: 1998
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1784821/
https://www.ncbi.nlm.nih.gov/pubmed/9972485
http://dx.doi.org/10.1002/(SICI)1098-0997(1998)6:6<244::AID-IDOG4>3.0.CO;2-B
_version_ 1782132112111960064
author Bawdon, R E
author_facet Bawdon, R E
author_sort Bawdon, R E
collection PubMed
description OBJECTIVE: The transfer of abacavir, a new nucleoside inhibitor, and amprenavir, a new protease inhibitor, used for the treatment of human immunodeficiency virus, has been studied in the ex vivo human placental model. METHODS: The ex vivo human placental model used C14 antipyrine to determine the transport fraction and clearance index of these compounds at both the peak and trough serum concentrations. The clearance index accumulation and tissue concentrations were determined for each drug by high pressure liquid chromatography. RESULTS: The clearance index of abacavir was 0.47 +/- 0.19 and 0.50 +/- 0.07 at peak and trough concentrations, respectively. The clearance index of amprenavir was 0.38 +/- 0.09 and 0.14 +/- 0.08 at peak and trough concentrations, respectively. There was no unusual accumulation of either drug in the media or tissue when the perfusion system was closed. CONCLUSION: Abacavir is the first nucleoside compound studied in the perfusion system with a high clearance index. The transfer of the protease inhibitor amprenavir had a clearance index 2.75 times greater than the clearance index of ritonavir at peak concentration determined in a previous study. At trough concentration the clearance index was much less than at the peak concentration. A similar result was found with ritonavir.
format Text
id pubmed-1784821
institution National Center for Biotechnology Information
language English
publishDate 1998
record_format MEDLINE/PubMed
spelling pubmed-17848212007-02-05 The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir. Bawdon, R E Infect Dis Obstet Gynecol Research Article OBJECTIVE: The transfer of abacavir, a new nucleoside inhibitor, and amprenavir, a new protease inhibitor, used for the treatment of human immunodeficiency virus, has been studied in the ex vivo human placental model. METHODS: The ex vivo human placental model used C14 antipyrine to determine the transport fraction and clearance index of these compounds at both the peak and trough serum concentrations. The clearance index accumulation and tissue concentrations were determined for each drug by high pressure liquid chromatography. RESULTS: The clearance index of abacavir was 0.47 +/- 0.19 and 0.50 +/- 0.07 at peak and trough concentrations, respectively. The clearance index of amprenavir was 0.38 +/- 0.09 and 0.14 +/- 0.08 at peak and trough concentrations, respectively. There was no unusual accumulation of either drug in the media or tissue when the perfusion system was closed. CONCLUSION: Abacavir is the first nucleoside compound studied in the perfusion system with a high clearance index. The transfer of the protease inhibitor amprenavir had a clearance index 2.75 times greater than the clearance index of ritonavir at peak concentration determined in a previous study. At trough concentration the clearance index was much less than at the peak concentration. A similar result was found with ritonavir. 1998 /pmc/articles/PMC1784821/ /pubmed/9972485 http://dx.doi.org/10.1002/(SICI)1098-0997(1998)6:6<244::AID-IDOG4>3.0.CO;2-B Text en
spellingShingle Research Article
Bawdon, R E
The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title_full The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title_fullStr The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title_full_unstemmed The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title_short The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
title_sort ex vivo human placental transfer of the anti-hiv nucleoside inhibitor abacavir and the protease inhibitor amprenavir.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1784821/
https://www.ncbi.nlm.nih.gov/pubmed/9972485
http://dx.doi.org/10.1002/(SICI)1098-0997(1998)6:6<244::AID-IDOG4>3.0.CO;2-B
work_keys_str_mv AT bawdonre theexvivohumanplacentaltransferoftheantihivnucleosideinhibitorabacavirandtheproteaseinhibitoramprenavir
AT bawdonre exvivohumanplacentaltransferoftheantihivnucleosideinhibitorabacavirandtheproteaseinhibitoramprenavir