scholarly journals In Vitro Activity of Human Immunodeficiency Virus Protease Inhibitors againstPneumocystis carinii

2000 ◽  
Vol 181 (5) ◽  
pp. 1629-1634 ◽  
Author(s):  
Chiara Atzori ◽  
Elena Angeli ◽  
Annalisa Mainini ◽  
Fiorenza Agostoni ◽  
Valeria Micheli ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Human Immunodeficiency Virus Protease ◽  
Immunodeficiency Virus

scholarly journals Effects of Human Immunodeficiency Virus Protease Inhibitors on the Intestinal Absorption of Tenofovir Disoproxil Fumarate In Vitro

2007 ◽  
Vol 51 (10) ◽  
pp. 3498-3504 ◽  
Author(s):  
Leah Tong ◽  
Truc K. Phan ◽  
Kelly L. Robinson ◽  
Darius Babusis ◽  
Robert Strab ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Drug Interactions ◽  
Intestinal Absorption ◽  
Protease Inhibitors ◽  
Plasma Levels ◽  
Human Immunodeficiency Virus Protease ◽  
Mdckii Cells ◽  
Immunodeficiency Virus ◽  
Secretory Transport

ABSTRACT Human immunodeficiency virus protease inhibitors (PIs) modestly affect the plasma pharmacokinetics of tenofovir (TFV; −15% to +37% change in exposure) following coadministration with the oral prodrug TFV disoproxil fumarate (TDF) by a previously undefined mechanism. TDF permeation was found to be reduced by the combined action of ester cleavage and efflux transport in vitro. Saturable TDF efflux observed in Caco-2 cells suggests that at pharmacologically relevant intestinal concentrations, transport has only a limited effect on TDF absorption, thus minimizing the magnitude of potential intestinal drug interactions. Most tested PIs increased apical-to-basolateral TDF permeation and decreased secretory transport in MDCKII cells overexpressing P-glycoprotein (Pgp; MDCKII-MDR1 cells) and Caco-2 cells. PIs were found to cause a multifactorial effect on the barriers to TDF absorption. All PIs showed similar levels of inhibition of esterase-dependent degradation of TDF in an intestinal subcellular fraction, except for amprenavir, which was found to be a weaker inhibitor. All PIs caused a dose-dependent increase in the accumulation of a model Pgp substrate in MDCKII-MDR1 cells. Pgp inhibition constants ranged from 10.3 μM (lopinavir) to >100 μM (amprenavir, indinavir, and darunavir). Analogous to hepatic cytochrome P450-mediated drug interactions, we propose that the relative differences in perturbations in TFV plasma levels when TDF is coadministered with PIs are based in part on the net effect of inhibition and induction of intestinal Pgp by PIs. Combined with prior studies, these findings indicate that intestinal absorption is the mechanism for changes in TFV plasma levels when TDF is coadministered with PIs.

scholarly journals Ex Vivo and In Vitro Effect of Human Immunodeficiency Virus Protease Inhibitors on Neutrophil Apoptosis

2000 ◽  
Vol 182 (5) ◽  
pp. 1536-1539 ◽  
Author(s):  
Claudio M. Mastroianni ◽  
Fabio Mengoni ◽  
Miriam Lichtner ◽  
Claudia D'Agostino ◽  
Gabriella d'Ettorre ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Ex Vivo ◽  
Neutrophil Apoptosis ◽  
Human Immunodeficiency Virus Protease ◽  
Immunodeficiency Virus ◽  
Vitro Effect

scholarly journals Synergy of Human Immunodeficiency Virus Protease Inhibitors with Chloroquine against Plasmodium falciparum In Vitro and Plasmodium chabaudi In Vivo

2008 ◽  
Vol 52 (7) ◽  
pp. 2653-2656 ◽  
Author(s):  
Zhengxiang He ◽  
Li Qin ◽  
Lili Chen ◽  
Nanzheng Peng ◽  
Jianlan You ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Plasmodium Falciparum ◽  
Protease Inhibitors ◽  
Plasmodium Chabaudi ◽  
Malaria Parasites ◽  
Human Immunodeficiency Virus Protease ◽  
Immunodeficiency Virus ◽  
Antimalarial Action

ABSTRACT The synergy of the activities between chloroquine and various human immunodeficiency virus protease inhibitors was investigated in chloroquine-resistant and -sensitive malaria parasites. In both in vitro and in vivo assay systems, ritonavir was found to be the most potent in potentiating the antimalarial action of chloroquine.

scholarly journals Synergistic Interactions of the Antiretroviral Protease Inhibitors Saquinavir and Ritonavir with Chloroquine and Mefloquine against Plasmodium falciparum In Vitro

2006 ◽  
Vol 51 (2) ◽  
pp. 759-762 ◽  
Author(s):  
T. S. Skinner-Adams ◽  
K. T. Andrews ◽  
L. Melville ◽  
J. McCarthy ◽  
D. L. Gardiner
Keyword(s):  
Human Immunodeficiency Virus ◽  
Plasmodium Falciparum ◽  
Protease Inhibitors ◽  
Antimalarial Activity ◽  
Digestive Vacuole ◽  
Synergistic Interactions ◽  
Human Immunodeficiency Virus Protease ◽  
Immunodeficiency Virus ◽  
Pepstatin A

ABSTRACT The antimalarial activity of several antiretroviral protease inhibitor combinations was investigated. Data demonstrate that ritonavir and saquinavir behave synergistically with chloroquine and mefloquine. These data, and interactions with pepstatin-A, E-64, and bestatin, suggest that human immunodeficiency virus protease inhibitors do not target digestive-vacuole plasmepsins.

Sign in / Sign up

Export Citation Format

Share Document