OBJECTIVE The use of the HIV protease inhibitor ritonavir (RTV) is frequently associated with hypertriglyceridemia and lipodystrophy. The aim of our study was to determine the mechanism underlying the observed hypertriglyceridemia. METHODS AND RESULTS Feeding female APOE*3-Leiden transgenic mice a Western-type diet supplemented with RTV (35 mg/kg per day) for 2 weeks resulted in a 2-fold incr...

The mechanism-based inactivation of human CYP2B6 by ritonavir (RTV) in a reconstituted system was investigated. The inactivation is time, concentration, and NADPH dependent and exhibits a K(I) of 0.9 μM, a k(inact) of 0.05 min⁻¹, and a partition ratio of approximately 3. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis showed that the protonated molecular ion of RTV exhibits a...

A simple and accurate method to determine Darunavie ethanolate (DRV) and ritonavir (RTV), in binary mixture, was developed and validated using liquid chromatography (LC). The LC separation was achieved on a Phenomenex Luna C18 column (250 mm, 4.6mm i.d., 5μm), in the isocratic mode using acetonitrile: water (60: 40, v/v), pH adjusted to 3.2 ± 0.02 with formic acid at a flow rate of 1 mL/min. Th...

BACKGROUND Patients with HIV have an increased incidence of pulmonary artery hypertension. This study was designed to determine if the naturally occurring antioxidant dihydroxybenzyl alcohol (DHBA) could counteract the deleterious effects of ritonavir (RTV), an HIV-protease inhibitor known to impair endothelial function and increase oxidative stress. MATERIAL/METHODS Antioxidant assays were p...

A new feature set derived from the fractal geometry, called the random threshold vector (RTV) is proposed for texture analysis. The RTV is computed for different run length entropy dimensions. The run length entropy dimensions are calculated based on different thresholds. To test the rotationally invariant feature, the run length entropies are calculated in different directions. The experimenta...

Using measured free fraction and 50% inhibitory concentration (IC50) values for the human immunodeficiency virus protease inhibitors lopinavir (LPV) and ritonavir (RTV) in tissue culture media with various protein concentrations ranging from 5 to 50%, we estimated serum-free IC50 values for each drug. The range of serum-free IC50 values (0.64 to 0.77 ng/ml for LPV and 3.0 to 5.0 ng/ml for RTV) ...

BACKGROUND Cognitive theories of attention-deficit/hyperactivity disorder (ADHD) propose that high within-subject fluctuations of cognitive performance in ADHD, particularly reaction time (RT) variability (RTV), may reflect arousal dysregulation. However, direct evidence of arousal dysregulation and how it may account for fluctuating RTs in ADHD is limited. We used skin conductance (SC) as a me...

OBJECTIVE To investigate the pharmacokinetics of once-daily saquinavir (SQV) hard-gelatin capsule (HGC)/ritonavir (RTV), 1600/100 mg, compared with once-daily SQV soft-gelatin capsule (SGC)/RTV, 1600/100 mg. METHODS We evaluated 13 randomly selected HIV-1-infected subjects taking once-daily SQV SGC/RTV, 1600/100 mg, plus dual nucleoside reverse transcriptase inhibitors (NRTIs) in this pharmac...