Managing Drug Interactions in the
Treatment of HIV-Related
Tuberculosis
Table 2. Recommendations
for Coadministering Antiretroviral
Drugs with RIFAMPIN – 2007
Non-nucleoside reverse transcriptase inhibitors |
|
Recommended change in dose of antiretroviral drug |
Recommended change in dose of rifampin |
Comments |
Efavirenz |
None (some experts recommend 800
mg for patients > 60 kg) |
No change
(600 mg/day) |
Efavirenz
AUC ¯ by 22%; no change in rifampin concentration.
Efavrirenz should not be used during the 1st trimester of pregnancy. |
Nevirapine |
No change |
No change
(600 mg/day) |
Nevirapine AUC ¯ 37-58% and Cmin ¯ 68% with 200 mg 2x/day dose. |
Delavirdine |
Rifampin
and delavirdine should not be used together |
Delavirdine
AUC ¯ by 95% |
Etravirine |
Etravirine
and rifampin should not be used together |
Marked
decrease in etravirine predicted, based on data on the interaction with
rifabutin |
Single
protease inhibitors |
|
Recommended change in dose of antiretroviral drug |
Recommended change in dose of rifampin |
Comments |
Ritonavir |
No change |
No change
(600 mg/day) |
Use
with caution. Ritonavir AUC
¯ by 35%; no
change in rifampin concentration. Monitor for antiretroviral activity
of ritonavir. |
fos-Amprenavir |
Rifampin
and fos-amprenavir should not be used together |
|
Atazanavir |
Rifampin
and atazanavir should not be used together |
Atazanavir
AUC ¯ by >95% |
Indinavir |
Rifampin
and indinavir should not be used together |
Indinavir
AUC ¯ by 89%. |
Nelfinavir |
Rifampin
and nelfinavir should not be used together |
Nelfinavir
AUC ¯ 82% |
Saquinavir |
Rifampin
and saquinavir should not be used together |
Saquinavir AUC
¯ by 84% |
Dual protease-inhibitor combinations |
|
Recommended change in dose of antiretroviral drug |
Recommended change in dose of rifampin |
Comments |
Saquinavir / ritonavir |
Saquinavir
400 mg + ritonavir 400 mg twice-daily |
No change
(600 mg/day) |
Use with caution; the
combination of saquinavir (1000 mg twice-daily), ritonavir (100 mg
twice-daily), and rifampin caused unacceptable rates of hepatitis among
healthy volunteers |
Lopinavir / ritonavir (Kaletra
ä) |
Increase the dose of lopinavir / ritonavir
(Kaletra
ä) to 4 tablets (200 mg of lopinavir with 50 mg of ritonavir)
twice-daily |
No change
(600 mg/day) |
Use
with caution; this combination resulted in hepatitis in all adult healthy
volunteers in an initial study. |
“Super-boosted” lopinavir / ritonavir (Kaletra
ä)® |
Lopinavir / ritonavir (Kaletra
ä) – 2 tablets (200 mg of lopinavir with 50 mg of ritonavir) + 300 mg of
ritonavir twice-daily |
No change
(600 mg/day) |
Use
with caution; this combination resulted in hepatitis among adult healthy
volunteers. However, there are favorable pharmacokinetic and clinical
data among young children |
Atazanavir / ritonavir |
The
standard dose of ritonavir-boosted atazanavir (300 mg once daily with
100 mg of ritonavir) should not be used with rifampin |
Atazanavir trough concentration
¯ by > 90% |
Tipranavir / ritonavir |
Rifampin
and tipranavir/ritonavir should not be used together |
|
Darunavir / ritonavir |
Rifampin
and darunavir/ritonavir should not be used together |
|
CCR-5
receptor antagonists |
|
Recommended change in dose of antiretroviral drug |
Recommended change in dose of rifampin |
Comments |
Maraviroc |
Increase maraviroc to 600 mg twice-daily |
No change
(600 mg/day) |
Maraviroc
Cmin ¯ by 78%. No reported clinical experience
with increased dose of maraviroc with rifampin |
Integrase
inhibitors |
|
Recommended change in dose of antiretroviral
drug |
Recommended change in dose of rifampin |
Comments |
Raltegravir |
No change |
No change
(600 mg/day) |
No
clinical experience; raltegravir concentrations
¯ by 40-61% |
|
Last Reviewed: 05/18/2008 Content Source: Division of Tuberculosis Elimination
National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention
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