Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors.

摘要: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a diverse group of compounds that induce allosteric changes in the human immunodeficiency virus type 1 (HIV-1) transcriptase, thus rendering enzyme incapable converting viral RNA to DNA. Unlike nucleoside analogue NNRTIs do not require sequential phosphorylation elicit antiretroviral activity. There currently 3 approved NNRTIs: nevirapine, delavirdine and efavirenz. Although possessing common mechanism action, these agents can be differentiated by both molecular pharmacokinetic characteristics. Each is metabolised some degree cytochrome P450 (CYP) system enzymes, making them prone clinically significant drug interactions. In addition, they variable effects on other medications, acting as either inducers or drugs CYP. These interactions an important consideration clinical use part combination therapy. Additional factors such influence food pH oral absorption, protein binding, must also considered.