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利匹韦林的作用机制和药代动力学

[Mechanism of action and pharmacokinetics of rilpivirine].

作者信息

Portilla Joaquín, Estrada Vicente

机构信息

Unidad de Enfermedades Infecciosas, Servicio de Medicina Interna, Hospital General Universitario, Alicante, España.

出版信息

Enferm Infecc Microbiol Clin. 2013 Jun;31 Suppl 2:2-5. doi: 10.1016/S0213-005X(13)70136-8.

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.

摘要

利匹韦林是一种有效的非核苷类逆转录酶抑制剂(NNRTI),在初治患者的HIV感染治疗中具有高效性。该药物对野生型HIV-1和多种第一代NNRTI均有活性。利匹韦林具有非常良好的药代动力学特征,但由于其吸收取决于胃内pH值,应与食物同服以确保正确吸收。利匹韦林经细胞色素P450(CYP)3A代谢,因此与P450(CYP)3A诱导剂或抑制剂合用时应考虑潜在的相互作用。虽然较高剂量可表现为酶诱导剂,但在每日25mg的剂量下,利匹韦林不太可能改变通过该途径代谢的其他药物的浓度。由于其半衰期较长,利匹韦林可每日口服一次。

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