Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV
The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.
Last Updated: December 18, 2019; Last Reviewed: December 18, 2019
Table 20. Mechanisms of Antiretroviral-Associated Drug Interactions
PK interactions may occur during absorption, metabolism, or elimination of the ARV drug and/or the interacting drug. This table does not include a comprehensive list of all possible mechanisms of interactions for individual ARV drugs (e.g., transporters); however, the table lists the most common mechanisms of known interactions and focuses on absorption and CYP- and UGT1A1-mediated interactions.
Note: N/A indicates that there are no clinically relevant interactions by the mechanism. Identified mechanisms are specific to the ARV drugs described in the row and may not be reflective of complete ARV regimens. The older PIs FPV, IDV, NFV, and SQV are not commonly used in clinical practice and are not included in this table. Please refer to the FDA product labels for FPV, IDV, NFV, and SQV for information regarding drug interactions with these PIs.
|ARV Drugs by Drug Class||Mechanisms That May Affect Oral Absorption of ARV Drugs||Enzymes That Metabolize or are Induced or Inhibited by ARV Drugs|
|Increasing Gastric pH||Cationic Chelation||P-gp||CYP Substrate||CYP Inhibitor||CYP Inducer||UGT1A1|
|BIC||N/A||Concentration decreased by products that contain polyvalent cations (e.g., Ca, Mg, Al, Fe, Zn)
|ATV||Concentration decreased||N/A||Substrate, Inducer, Inhibitor||3A4||3A4, 2C8||N/A||Inhibitor|
|ATV/c||Concentration decreased||N/A||Substrate, Inhibitor||3A4||3A4, 2D6, 2C8||N/A||Inhibitor|
|ATV/r||Concentration decreased||N/A||Substrate, Inhibitor||3A4, 2D6||3A4, 2D6, 2C8||1A2, 2B6, 2C8, 2C9, 2C19||ATV: Inhibitor
|DRV/c||N/A||N/A||Substrate, effect on P-gp unknown||3A4||3A4, 2D6||N/A||No data|
|DRV/r||N/A||N/A||Substrate, effect on P-gp unknown||3A4, 2D6||3A4, 2D6||1A2, 2B6, 2C8, 2C9, 2C19||Inducer|
|LPV/r||N/A||N/A||Substrate||3A4, 2D6||3A4||1A2, 2B6, 2C8, 2C9, 2C19||Inducer|
|TPV/r||N/A||N/A||Substrate, Inducer||3A4, 2D6||3A4, 2D6||No data||Inducer|
|EFV||N/A||N/A||N/A||2B6 (primary), 2A6, 3A4||3A4||3A4, 2B6, 2C19||N/A|
|ETR||N/A||N/A||N/A||3A4, 2C9, 2C19||2C9, 2C19||3A4||N/A|
|NVP||N/A||N/A||N/A||3A4, 2B6||N/A||3A4, 2B6||N/A|
|Key: 3TC = lamivudine; ABC = abacavir; Al = aluminum; ARV = antiretroviral; ATV = atazanavir; ATV/c = atazanavir/cobicistat; ATV/r = atazanavir/ritonavir; BIC = bictegravir; Ca = calcium; COBI = cobicistat; CYP = cytochrome P; DOR = doravirine; DRV = darunavir; DRV/c = darunavir/cobicistat; DRV/r = darunavir/ritonavir; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; Fe = iron; FPV = fosamprenavir; FTC = emtricitabine; IBA = ibalizumab; IDV = indinavir; INSTI = integrase strand transfer inhibitor; LPV/r = lopinavir/ritonavir; Mg = magnesium; MVC = maraviroc; NFV = nelfinavir; NNRTI = non-nucleoside reverse transcriptase inhibitors; NRTI = nucleoside reverse transcriptase inhibitors; NVP = nevirapine; P-gp = P-glycoprotein; PK = pharmacokinetic; PI = protease inhibitor; RAL = raltegravir; RPV = rilpivirine; RTV = ritonavir; SQV = saquinavir; T-20 = enfuvirtide; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TPV/r = tipranavir/ritonavir; UGT = uridine diphosphate glucuronosyltransferase; ZDV = zidovudine; Zn = zinc|