Table 4. Drug interactions between rifamycin and antiretrovirals.
Rafamycin | Antretroviral agents | Effect on antiretroviral agents and/or concomitant antimycobacterial medication | Dosing recommendations and clinical comments | |
---|---|---|---|---|
Rifampin | All PI | ↓ PI concentration by >75% | Contraindicated. Consider rifabutin if a rifamycin is indicated. | |
BIC | BIC AUC ↓ 75% | Contraindicated. | ||
EVG/c | Significant ↓ EVG and cobicistat expected | Contraindicated. | ||
DTG | Rifampin with DTG 50 mg twice daily (Compared to DTG 50 mg twice daily alone): | Patients without suspected or documented INSTI-resistance mutations: | ||
DTG AUC ↓ 54% and Cmin ↓ 72% | Use DTG 50 mg twice daily suspected or documented INSTI-resistance mutations: Consider an alternative to rifampin, such as rifabutin | |||
Rifampin with DTG 50 mg twice daily (Compared to DTG 50 mg daily alone): | ||||
DTG AUC ↑ 33% and Cmin ↑ 22% | ||||
RAL | RAL 400 mg: RAL AUC ↓ 40% and Cmin ↓ 61% | Use RAL 800 mg twice daily instead of 400 mg twice daily. | ||
Rifampin with RAL 800 mg twice daily (Compared to RAL 400 mg twice daily alone): | ||||
RAL AUC ↑ 27% and Cmin ↓ 53% | Do not coadminister RAL 1,200 mg once daily with rifampin. | |||
TAF | TAF is a P-glycoprotein substrate, its plasma concentrations may be reduced by rifamycin. | Do not coadminister unless benefits outweigh risks. | ||
TAF with rifampin (Compared with TAF Alone): | ||||
TAF AUC ↓ 55% | Intracellular TFV-DP levels are higher when TAF is co-administered with rifampin compared to when TDF is administered alone, but clinical outcomes have not been studied. If co-administered, monitor virologic response. | |||
TFV-DP AUC ↓ 36% | ||||
RPV | RPV AUC ↓ 80% | Contraindicated. | ||
EFV | EFV AUC ↓ 26% | Maintain EFV dose at 600 mg daily and monitor for virologic response. | ||
Rifabutin | DRV/r | Compared with rifabutin (300 mg once daily) Alone, Rifabutin (150 mg every other day) plus DRV/r: ↔ rifabutin AUC and metabolite AUC ↑ 881% | Recommended dose is rifabutin 150 mg once daily. | |
Monitor for antimycobacterial activity and consider therapeutic drug monitoring. | ||||
PI/c | ↑ rifabutin expected | Do not coadminister. | ||
↓ cobicistat expected | ||||
BIC | Rifabutin 300 mg once daily: | Do not coadminister. | ||
BIC AUC ↓ 38% and Cmin ↓ 56% | ||||
DTG | Rifabutin 300 mg once daily: | No dose adjustment needed. | ||
↔ DTG AUC and Cmin ↓ 30% | ||||
EVG/c | Rifabutin 150 mg every other day with EVG/c once daily (Compared to Rifabutin 300 mg once daily alone): | Do not coadminister. | ||
↔ rifabutin AUC | ||||
25-O-desacetyl-rifabutin AUC ↑ 625% | ||||
EVG AUC ↓ 21% and Cmin ↓ 67% | ||||
RAL | RAL AUC ↑ 19% and Cmin ↓ 20% | No dose adjustment needed. |
AUC, area under the curve; EVG/c, elvitegravir/cobicistat; DTG, dolutegravir; Cmin, minimum concentration; INSTI, integrase strand transfer inhibitor; RAL, raltegravir; TAF, tenofovir alafenamide; TFV-DP, tenofovir-diphosphate; RPV, rilpivirine; EFV, efavirenz; DRV/r, ritonavir-boosted darunavir; PI/c, protease inhibitor/cobicistat; BIC, bictegravir; darunavir/ritonavir.