title: [Pharmacokinetic interactions].
abstract: Rilpivirine (RPV) is a nonnucleoside reverse transcriptase inhibitor (NNRTI) that has been approved for use in treatment-naïve patients and which has potent antiviral activity. Its adverse effects profile differs from that of first-generation NNRTs. The pharmacological interactions produced by RPV are due to its effects on the CYP450 system; RPV is a substrate and mild inducer of CYP3A4. Moreover, in vitro, RPV inhibits glycoprotein-P. RPV has clinically significant pharmacological interactions, especially with protease inhibitors (except boosted darunavir and lopinavir) and the NNRTIs efavirenz and nevirapine. Coadministration of RPV with drugs that increase gastric pH, such as omeprazole, or those inducing CYP3A4, such as rifampicin, can significantly reduce RPV concentrations and is contraindicated. The concomitant use of RPV with a CYP3A4 inhibitor (such as clarithromycin) can increase RPV concentrations. Administration of PRV with food is recommended to obtain better absorption and adequate plasma values.
authors.affiliation: Servicio de Medicina Interna, Unidad de Enfermedades Infecciosas, Hospital Universitario Miguel Servet, Zaragoza, España. Electronic address: parazo@salud.aragon.es.
authors.forename: Piedad
authors.initials: P
authors.lastname: Arazo Garcés
authors.forename: Ignacio
authors.initials: I
authors.lastname: de los Santos Gil
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000890:Anti-Infective Agents / Q000493:pharmacokinetics; D000927:Anticonvulsants / Q000493:pharmacokinetics; D003276:Contraceptives, Oral / Q000493:pharmacokinetics; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism*; D065701:Cytochrome P-450 CYP3A Inducers / Q000493:pharmacokinetics*; D065692:Cytochrome P-450 CYP3A Inhibitors / Q000493:pharmacokinetics; D004347:Drug Interactions; D018565:Food-Drug Interactions; D005765:Gastrointestinal Agents / Q000493:pharmacokinetics; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000493:pharmacokinetics; D007408:Intestinal Absorption; D009570:Nitriles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D054328:Proton Pump Inhibitors / Q000493:pharmacokinetics; D011743:Pyrimidines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000068696:Rilpivirine
chemical_list: D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D000927:Anticonvulsants; D003276:Contraceptives, Oral; D065701:Cytochrome P-450 CYP3A Inducers; D065692:Cytochrome P-450 CYP3A Inhibitors; D005765:Gastrointestinal Agents; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D009570:Nitriles; D054328:Proton Pump Inhibitors; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D000068696:Rilpivirine
keywords: Drug interactions; HIV infection; Infección VIH; Interacciones medicamentosas; Rilpivirina; Rilpivirine