Adapted from Ref 5

An additional consideration when stopping or changing therapy is a staggered discontinuation of antiretrovirals with different half-lives. For example, in patients taking Atripla (tenofovir, emtricitabine, and efavirenz) tenofovir and emtricitabine should be continued for at least 4 days after discontinuation of efavirenz due to the much prolonged half-life of efavirenz as compared to tenofovir and emtricitabine. Otherwise, the potential for monotherapy with efavirenz exists. If new antiretroviral therapy is to be initiated immediately, no overlap is necessary; however, it should be noted that efavirenz concentrations will persist for some period of time.

Drug interactions between antiretrovirals and between antiretrovirals and concomitant medications should be evaluated for each patient to avoid under- and/or overexposure of either therapy. NNRTIs and PIs are metabolized by CYP450 enzymes and are inducers and/or inhibitors of this enzyme system. In addition, some of the antiretrovirals are substrates, inhibitors, and/or inducers of transporters such as P-glycoprotein, and therefore may lead to drug interactions. Information provided in Table 87-5 describes the drug interaction potential of each antiretroviral. Due to the ever-changing drug interactions with this class of medications, the regularly updated DHHS Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents are a recommended source of specific drug interactions.5

Table 87-5 Summary of Currently Available Antiretroviral Agents

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