Arazo Garcés Piedad, de los Santos Gil Ignacio
Servicio de Medicina Interna, Unidad de Enfermedades Infecciosas, Hospital Universitario Miguel Servet, Zaragoza, España.
Enferm Infecc Microbiol Clin. 2013 Jun;31 Suppl 2:12-9. doi: 10.1016/S0213-005X(13)70138-1.
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.
利匹韦林（RPV）是一种非核苷类逆转录酶抑制剂（NNRTI），已被批准用于初治患者，具有强大的抗病毒活性。其不良反应谱与第一代NNRTIs不同。RPV产生的药物相互作用是由于其对细胞色素P450（CYP450）系统的作用；RPV是CYP3A4的底物和轻度诱导剂。此外，在体外，RPV可抑制糖蛋白-P。RPV具有临床上显著的药物相互作用，尤其是与蛋白酶抑制剂（增强型达芦那韦和洛匹那韦除外）以及NNRTIs依非韦伦和奈韦拉平。RPV与增加胃pH值的药物（如奥美拉唑）或诱导CYP3A4的药物（如利福平）合用，可显著降低RPV浓度，因此禁忌合用。RPV与CYP3A4抑制剂（如克拉霉素）同时使用可增加RPV浓度。建议在进食时服用PRV以获得更好的吸收和足够的血浆浓度。
