Preoperative use of raltegravir-containing regimen as induction therapy: very rapid decline of HIV-1 viral load

AIDS (London, England) (Impact Factor: 6.56). 04/2009; 23(6):739. DOI: 10.1097/QAD.0b013e328325a4bd
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    ABSTRACT: Objective To describe the indications for use, in medical practice, of next-generation antiretroviral drugs (NGA): darunavir, raltegravir, maraviroc and etravirine.
    Farmacia Hospitalaria 01/2011; 35(1):14-22. DOI:10.1016/j.farma.2010.01.017
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    ABSTRACT: BACKGROUND AND PURPOSE: Warfarin is often used with etravirine to prevent HIV related thromboembolic events. Due to similar plasma protein binding and hepatic metabolism by cytochrome P450, we evaluated the effect of etravirine on pharmacokinetics and blood clotting time of warfarin using rat. EXPERIMENTAL APPROACH: Two groups of jugular vein-cannulated, male Sprague Dawley rats were studied. Control group (n=10) received intravenous dose of 1mg kg(-1) racemic warfarin, and test group (n=13) received 1mg kg(-1) of racemic warfarin followed by 25mg kg(-1) etravirine intravenously. Serial blood samples collected up to 144 hours. International Normalized Ratio (INR) in rat blood plasma measured at each sample point. Plasma concentrations of R-warfarin, S-warfarin, R-7-hydroxywarfarin and S-7-hydroxywarfarin measured by a LC-MS/MS method using chiral lux cellulose-1 column. Pharmacokinetic parameters were analyzed using noncompartmental methods. Statistical comparisons were made using Student t test or Mann - Whitney U-test. KEY RESULTS: There was significant 3-fold increase in S-warfarin systemic clearance in presence of etravirine (4.13 mL hr (-1) kg(-1) to 12.99 ml hr(-1) kg(-1) ), and volume of distribution (115.0mL kg(-1) to 394.2mL kg(-1) ), but not for R-warfarin. Total area under the curve was significantly decreased when warfarin was co-administered with etravirine, but there was no change in elimination half life. Interestingly, the effect of warfarin on blood clotting time represented as INR, was significantly increased in the presence of etravirine. CONCLUSIONS AND IMPLICATIONS: Our data suggest that etravirine may potentiate anticoagulant effect of warfarin with clinical significance.
    British Journal of Pharmacology 12/2012; DOI:10.1111/bph.12082 · 4.99 Impact Factor
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    ABSTRACT: Vertical transmission of human immunodeficiency virus (HIV) represents an important worldwide health problem and rapid decline in viral load is essential for HIV pregnant women to prevent mother to child transmission. Specific issues such as late presentation of pregnant HIV-infected women remain a clinical challenge. We present a case of an HIV-infected woman who presented to our hospital at 35 weeks of pregnancy, who was successfully treated with raltegravir-based first-line combined antiretroviral regimen. Even though there is limited information about safety and tolerability of the use of raltegravir in pregnancy, in our case this drug resulted in a rapid decline in HIV-RNA viral load, without side effects. The aim of the present study and literature review was to demonstrate that raltegravir can be a good treatment choice for very late presenting pregnant women.
    Journal of chemotherapy (Florence, Italy) 06/2013; 25(3):181-3. DOI:10.1179/1973947812Y.0000000066 · 1.07 Impact Factor