Weisser M, Battegay M
Medizinische Universitäts-Poliklinik, Kantonsspital Basel.
Ther Umsch. 1998 May;55(5):310-22.
In recent years the availability of highly active antiretroviral therapies and prophylaxis and treatment of opportunistic infections in patients with HIV-disease have reduced morbidity and mortality. Many different drugs may be prescribed in a patient simultaneously. Therefore, the potential for interactions between different substances is increased. The possible mechanisms of drug interaction concern pharmakokinetics (absorption, metabolism, elimination) and pharmakodynamics. They can lead to significant changes in plasma concentrations and may affect efficacy and toxicity of a drug. One of the most important mechanisms of interaction is the inhibition or induction of the hepatic cytochrome P-450 enzyme system. All protease-inhibitors are metabolized by CYP450, mostly by the subunit 3A4. Proteinase-inhibitors are themselves very potent inhibitors of CYP4503A4 and increase the concentration of drugs metabolized this way. This article summarises the most important mechanisms of drug interactions and demonstrates the most frequent and clinical significant consequences.
近年来，高效抗逆转录病毒疗法以及对HIV疾病患者机会性感染的预防和治疗降低了发病率和死亡率。患者可能会同时服用多种不同药物。因此，不同物质之间相互作用的可能性增加。药物相互作用的可能机制涉及药代动力学（吸收、代谢、消除）和药效学。它们可导致血浆浓度发生显著变化，并可能影响药物的疗效和毒性。最重要的相互作用机制之一是肝细胞色素P-450酶系统的抑制或诱导。所有蛋白酶抑制剂均由CYP450代谢，主要通过亚基3A4代谢。蛋白酶抑制剂本身就是CYP4503A4的强效抑制剂，并会增加以这种方式代谢的药物浓度。本文总结了药物相互作用的最重要机制，并阐述了最常见且具有临床意义的后果。
