Rilpivirine: a second-generation nonnucleoside reverse transcriptase inhibitor

American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists
Christopher JamesMeryn Sweet

Abstract

The pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, dosage and administration, and place in therapy of rilpivirine are reviewed. Rilpivirine is a human immunodeficiency virus type 1 (HIV-1)-specific nonnucleoside reverse transcriptase inhibitor (NNRTI) indicated for use in combination with other antiretroviral agents in adult patients not previously treated with antiretroviral therapy. Rilpivirine is primarily metabolized by the cytochrome P-450 (CYP)3A isoenzyme system. Therefore, providers should be cautious when administering drugs that are inhibitors or inducers of this pathway. Coadministration with CYP 3A inhibitors may lead to increased concentrations of rilpivirine, thereby increasing the risk of adverse effects. Coadministration with inducers of CYP3A isoenzymes or drugs that increase gastric pH may lead to decreased concentrations of rilpivirine, thus promoting virological failure or resistance to rilpivirine. Two Phase III, randomized, double-blind, double-dummy, active-controlled trials compared rilpivirine with efavirenz in HIV-infected adults not previously treated with an antiretroviral. The investigators concluded that rilpivirine, when combined with two nucleoside or nucle...Continue Reading

References

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Citations

Apr 17, 2014·Tree Physiology·Jean-Sébastien JacquetHervé Jactel
Feb 18, 2016·European Journal of Clinical Microbiology & Infectious Diseases : Official Publication of the European Society of Clinical Microbiology·R PalaciosJ Santos
Jul 23, 2019·Expert Opinion on Drug Delivery·Yuqing GongSantosh Kumar
Oct 25, 2013·Journal of the American Chemical Society·Won-Gil LeeWilliam L Jorgensen

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