title: [Mechanism of action and pharmacokinetics of rilpivirine].
abstract: Rilpivirine is a potent nonnucleoside reverse transcriptase inhibitor (NNRTI) with high efficacy in the treatment of HIV infection in treatment-naïve patients. This drug is active against both wild-type HIV-1 and a wide variety of first-generation NNRTI. Rilpivirine has a highly favorable pharmacokinetics profile, but, because its absorption depends on gastric pH, it should be administered with food to ensure correct absorption. Rilpivirine is metabolized by cytochrome P450 (CYP) 3A and consequently potential interactions should be considered when it is administered with P450 (CYP) 3A inducers or inhibitors. Although higher doses can behave as enzyme inducers, at a dose of 25mg/day, rilpivirine is unlikely to alter the concentrations of other drugs metabolized through this pathway. Because of its prolonged half-life, rilpivirine can be administered orally once daily.
authors.affiliation: Unidad de Enfermedades Infecciosas, Servicio de Medicina Interna, Hospital General Universitario, Alicante, España. Electronic address: portilla_joa@gva.es.
authors.forename: Joaquín
authors.initials: J
authors.lastname: Portilla
authors.forename: Vicente
authors.initials: V
authors.lastname: Estrada
mesh_terms: D000225:Adenine / Q000008:administration & dosage / Q000031:analogs & derivatives; D000328:Adult; D000368:Aged; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001682:Biological Availability; D002648:Child; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D065701:Cytochrome P-450 CYP3A Inducers / Q000494:pharmacology; D065692:Cytochrome P-450 CYP3A Inhibitors / Q000494:pharmacology; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives; D004333:Drug Administration Routes; D004338:Drug Combinations; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D000068679:Emtricitabine; D018565:Food-Drug Interactions; D015658:HIV Infections / Q000188:drug therapy; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D015394:Molecular Structure; D053758:Nanoparticles; D009570:Nitriles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D063065:Organophosphonates / Q000008:administration & dosage; D054328:Proton Pump Inhibitors / Q000494:pharmacology; D011743:Pyrimidines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D000068696:Rilpivirine; D000068698:Tenofovir
chemical_list: D019380:Anti-HIV Agents; D065701:Cytochrome P-450 CYP3A Inducers; D065692:Cytochrome P-450 CYP3A Inhibitors; D004338:Drug Combinations; D009570:Nitriles; D063065:Organophosphonates; D054328:Proton Pump Inhibitors; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D003841:Deoxycytidine; D000068698:Tenofovir; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; D000068696:Rilpivirine; D000068679:Emtricitabine; D000225:Adenine
keywords: Efavirenz; Farmacocinética; Inhibidores no nucleósidos de la transcriptasa inversa; Nonnucleoside reverse transcriptase inhibitor; Pharmacokinetics; Rilpivirina; Rilpivirine