Ritonavir: Clinical efficacy for treatment of HIV-1 infected patients (original) (raw)

Journal of symptoms and signs, 2015

Abstract

Ritonavir was one of the four potent synthetic protease inhibitors (PI), approved by FDA between 1995 and 1997 that revolutionised HIV therapy. Boosted protease inhibitor regimens combine ritonavir with a second protease inhibitor to enhance patient exposure to the latter agent, preventing or overcoming resistance and allowing less frequent dosing, potentially improving adherence. The advantages offered by ritonavir boosting are primarily attributable to the drug’s pharmacokinetics properties. Ritonavir inhibition’s of the cytochrome P-450 CYP3A4 enzyme reduces the metabolism of concomitantly administered PI and changes minimum concentration and half-life. As a result, the bioavailability of the boosted PI is increased and improved penetration into HIV reservoirs may be achieved. Moreover, at low dose ritonavir boosts the second inhibitor without contributing significantly to the side effect profile of the regimen. The very recent finding that ritonavir, despite administered at a low dose, can reach intracellular levels sufficient to exert an antiviral activity itself, suggests several hypothetic issues for its use in clinical practice and further in vitro and in vivo studies, before definitely switching therapy to other booster molecules. Keywords: ritonavir; boosted protease inhibitor; pharmacokinetics properties; cytochrome P450. Received: June 5, 2014; Accepted: October 21, 2014; Published: January 19, 2015 Corresponding Author: Massimiliano Lanzafame, Via Strada Romana 11, San Bonifacio 37047 (Verona), Italy. E-mail: lanzafame.massimiliano@gmail.com .

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