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Database of Antiretroviral Drug Interactions

Interactions with Rifampin (Rifampicin) and Antiretrovirals

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Amprenavir340
(APV)(Agenerase)
1200 mg BID600 mg QD x 14 daysAUC: decreased 82%No significant changeDecreased amprenavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Amprenavir60
(APV)(Agenerase)
1200 mg BID x 4 days300 mg QD x 4 daysAmprenavir AUC: decreased 82%; Cmax: decreased 70%; Cmin: decreased 92%No significant changeDecreased amprenavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Atazanavir
(ATV)(Reyataz)
----Decreased atazanavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Atazanavir247
(ATV)(Reyataz)
300 mg with ritonavir 100 mg QD x 10 d600 mg QD x 10 dAtazanavir AUC: decreased 57%; Cmax: decreased 56%; Cmin: decreased 93%(compared to atazanavir 400 mg QD)-Decreased atazanavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister; consider rifabutin

Atazanavir727
(ATV)(Reyataz)
300 mg with ritonavir 100 mg QD x 21 d600 mg QD x 10 dAtazanavir AUC: decreased 72%; Cmax: decreased 53%; Cmin: decreased 98%-Decreased atazanavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Atazanavir247
(ATV)(Reyataz)
300 mg with ritonavir 200 mg QD x 10 d600 mg QD x 10 dAtazanavir AUC: decreased 31%; Cmax: decreased 40%; Cmin: decreased 80%(compared to atazanavir 400 mg QD)-Decreased atazanavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister; consider rifabutin

Atazanavir247
(ATV)(Reyataz)
400 mg with ritonavir 200 mg QD x 10 d600 mg QD x 10 dAtazanavir AUC: no significant change; Cmax: decreased 18%; Cmin: decreased 40%(compared to atazanavir 400 mg QD)-Decreased atazanavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister; consider rifabutin

Bictegravir759
(Biktarvy)
75 mg daily600 mg daily (fed state) Cmax decreased 28%; AUC decreased 75% Not studied Potential loss of antiviral efficacyInduction of CYP3A4

Contraindicated. Use alternative agents

Darunavir161
(DRV)(Prezista)
--Not studied; may decrease darunavir/ritonavir levels-Decreased darunavir/ritonavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Delavirdine88
(DLV)(Rescriptor)
400 mg TID600 mg QDDelavirdine AUC: decreased 96%Not studiedDecreased delavirdine effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Dolutegravir641
(Tivicay)
50 mg BID600 mg QDDolutegravir AUC: decreased 54%; Cmin: decreased 72% (when compared to dolutegravir 50 mg BID without rifampin)-Decreased dolutegravir effectiveness-

If no InSTI resistance, increase dolutegravir dosage to 50 mg BID. If known or clinically suspected INSTI resistance, use alternative or consider rifabutin

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Dolutegravir641
(Tivicay)
50 mg BID600 mg QDDolutegravir AUC: increased 33%; Cmin: increased 22% (when compared to dolutegravir 50 mg QD)---

If no INSTI resistance, increase dolutegravir dosage to 50 mg BID. If known or clinically suspected INSTI resistance, use alternative or consider rifabutin

Efavirenz357
(EFV)(Sustiva)
600 mg QD x 14 days600 mg QD x 14 daysEfavirenz AUC: decreased 22%; Cmax: decreased 24%; Cmin: decreased 25%No significant changeDecreased efavirenz effectsInduction of CYP450 3A4 by rifampin

Dose adjustment not established; may consider increasing efavirenz to 800 mg QD when used with rifampin

Alternative Agents:
Rifabutin

Efavirenz90, 345
(EFV)(Sustiva)
600 mg x 7 days600 mg x 7 daysEfavirenz AUC: decreased 26%; Cmax: decreased 20%- Decreased efavirenz effectsInduction of CYP450 3A4 by rifampin

Dose adjustment not established; may consider increasing efavirenz to 800 mg QD when used with rifampin

Alternative Agents:
Rifabutin

Elvitegravir/cobicistat639, 623
(Genvoya, Stribild)
-- Expected decrease in elvitegravir and cobicistat levels-Potential loss of antiretroviral efficacyInduction of CYP450 by rifampin

Do not coadminister; consider alternative antiretrovirals

Elvitegravir/ritonavir-boosted protease inhibitor639
--Expected significant decrease in elvitegravir, cobicistat, and protease inhibitor levels-Potential loss of antiretroviral efficacyInduction of CYP3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Enfuvirtide6,
(ENF)(Fuzeon)
90 mg SQ BID on days 1-3 and 11-13600 mg QD on days 4-13No significant changeNo significant change--

No dose adjustment necessary

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Indinavir16
(IDV)(Crixivan)
800 mg Q8H x 1 week600 mg QD x 1 weekIndinavir AUC: decreased 89%-Decreased indinavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Indinavir353
(IDV)(Crixivan)
800 mg with ritonavir 100 mg BID300 mg QD x 4 daysIndinavir Cmin: decreased 87%; Cmax: no significant change; half-life: decreased 39%;Ritonavir Cmin: decreased 94%; Cmax: decreased 38%; half-life: decreased 53%Not studiedDecreased indinavir and ritonavir effectsInduction of P450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Indinavir355
(IDV)(Crixivan)
800 mg with ritonavir 100 mg BID x 1, administered with food- Indinavir AUC: decreased 81%; ritonavir AUC: decreased 89%Rifampin AUC: increased 25%; desacetylrifampin AUC: increased 63%Increased rifampin effects; decreased indinavir and ritonavir effectsInduction of CYP450 3A4 by rifampin; inhibition of CYP450 3A4 by indinavir/ritonavir

Do not coadminister

Alternative Agents:
Rifabutin

Lopinavir/ritonavir78
(LPV/r)(Kaletra)
400 mg/100 mg BID x 20 days600 mg QD x 10 daysLopinavir AUC: decreased 75%; Cmax: decreased 55%; Cmin: decreased 99%-Decreased lopinavir/ritonavir effectsInduction of CYP450 3A4 by rifampin

Avoid coadministration. If combination can not be avoided consider alternate dosing for lopinavir/ritonavir (800/200 mg Q12H) or additional ritonavir.

Alternative Agents:
Rifabutin

Lopinavir/ritonavir351, 350, 352
(LPV/r)(Kaletra)
400/100 mg BID on days 1-15, then 800/200 mg BID or 400/400 mg BID on days 16-24600 mg QD on days 11-24Lopinavir AUC: decreased 16% (in 800/200 mg BID group when compared to 400/100 mg BID); Cmin: decreased 57%; Cmax: no significant change. Ritonavir AUC: increased 42%; Cmax: increased 75%; Cmin: no significant change.Lopinavir pharmacokinetics: No significant change (in 400/400 mg BID group)Ritonavir AUC: increased 612%; Cmax: increased 738%; Cmin: increased 389% (in 400 mg/400 mg BID group)Not studiedDecreased lopinavir effectsInhibition of CYP450 3A4 by ritonavir; Induction of CYP450 3A4 by rifampin

Avoid coadministration. If combination can not be avoided consider using lopinavir/ritonavir 400 mg BID with ritonavir 400 mg BID when coadministering with rifampin

Lopinavir/ritonavir459
(LPV/r)(Kaletra)
400/100 mg Q12h x 7 days, 600/150 mg Q12H x 7 days then 800/200 Q12H x 7 days600 mg QDLopinavir AUC: decreased 71% (on 400/100 mg Q12H); AUC: decreased 40% (on 600/150 mg Q12H); AUC: no significant change (on 800/200 mg Q12H)-Decreased lopinavir effects at lower dosagesInduction of CYP450 3A4 by rifampin

Avoid coadministration. If combination can not be avoided lopinavir/ritonavir dosage of 800/200 mg Q12H appears to compensate for rifampin induced 3A4 induction

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Maraviroc2
(MVC)(Selzentry)
100 mg BID600 mg QDMaraviroc AUC: decreased 63%; Cmax: decreased 67%; Cmin: decreased 78%- Decreased maraviroc effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Nelfinavir254, 24
(NFV)(Viracept)
750 mg Q8H x 5-6 days600 mg QD x 8 daysNelfinavir AUC: decreased 82%; Cmax: decreased 76%-Decreased nelfinavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Nevirapine95, 351
(NVP)(Viramune)
--Nevirapine Cmin: decreased 37%Not studiedDecreased nevirapine effectsInduction of CYP450 3A4 by rifampin

Avoid if possible

Alternative Agents:
Rifabutin

Nevirapine
(NVP)(Viramune)
200 mg BID600 mg QDNevirapine AUC: decreased 27% (at week 4); Nevirapine AUC: no significant change (at week 10)Nevirapine AUC with rifampicin approximates nevirapine baseline without rifampicin at week 10.-Decreased nevirapine effects-

Regimen most appropriate for countries where rifabutin is not available; Avoid nevirapine and rifampicin/rifampin if rifabutin is available (rifabutin preferred agent)

Alternative Agents:
Rifabutin

Nevirapine356, 351
(NVP)(Viramune)
200 mg BID600 mg QDNevirapine AUC: decreased 31%; Cmax: decreased 36%; Cmin: decreased 21%No significant changeDecreased nevirapine effectsInduction of CYP450 3A4 by rifampin

Avoid if possible

Alternative Agents:
Rifabutin

Nevirapine347
(NVP)(Viramune)
200 mg x 1450 mg if < 55 kg and 600 mg if > 55 kg x 7 daysNevirapine AUC: decreased 79%; Cmax: decreased 20%; Cmin: decreased 60%; half-life: decreased 66%-Decreased nevirapine effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Raltegravir438
(RAL)(Isentress)
400 mg QD x 1600 mg QDRaltegravir AUC: decreased 40%; Cmin: decreased 61%; Cmax: decreased 38%-Decreased raltegravir effectsInduction of UGT1A1 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Raltegravir436, 3
(RAL)(Isentress)
400 mg x 1600 mg QDRaltegravir AUC: decreased 40%; Cmax: decreased 38%; Cmin: decreased 61%-Possibly decreased raltegravir effectsInduction of UGT 1A1

Do not coadminister

Alternative Agents:
Possibly rifabutin

Raltegravir3
(RAL)(Isentress)
800 mg BID600 mg QDRaltegravir AUC: increased 27%; Cmax: increased 62%; Cmin: decreased 53% (all compared to raltegravir 400 mg BID)--Induction of UGT1A1 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Raltegravir418
(RAL)(Isentress)
800 mg Q12H600 mg QDRaltegravir AUC: increased 27%; Cmin: decreased 53%; Cmax: increased 62% (compared to 400 mg raltegravir Q12H when given alone)- - -

Use caution if this combination must be used

Alternative Agents:
Rifabutin

Rilpivirine567
(RPV)(Edurant)
150 mg QD600 mg QDRilpivirine AUC: decreased 80%; Cmin: decreased 89%; Cmax: decreased 69%No significant changeDecreased rilpivirine effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Ritonavir197, 55
(RTV)(Norvir)
500 mg Q12H x 20 days300 mg or 600 mg x 10 daysRitonavir AUC: decreased 35%; Cmax: decreased 25%-Decreased ritonavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Alternative Agents:
Rifabutin

Antiretroviral (ARV)Dose of ARVDose of RifampinEffect on ARV LevelsEffect on Rifampin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Saquinavir282
(SQV)(Fortovase, Invirase)
1200 mg TID600 mg QD x 14 daysSaquinavir AUC: decreased 46%; Cmax: decreased 43% when studied in HIV-infected patients-Decreased saquinavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Saquinavir282
(SQV)(Fortovase, Invirase)
1200 mg TID600 mg QD x 14 daysSaquinavir AUC: decreased 70%; Cmax: decreased 65%-Decreased saquinavir effectsInduction of CYP450 3A4 by rifampin

Do not coadminister

Saquinavir44, 351
(SQV)(Fortovase, Invirase)
600 mg (hard gel caps) TID x 14 days600 mg QD x 7 daysAUC: decreased 84%; Cmax: decreased 79%-Decreased saquinavir effectsInduction of CYP450 3A4 by rifampin

Avoid if possible; may consider saquinavir 400 mg BID with ritonavir 400 mg BID

Alternative Agents:
Rifabutin

Tenofovir disoproxil fumarate348, 349
(TDF)(Viread)
300 mg QD on days 1-20600 mg QD on days 11-21No significant changeNo significant change--

No dose adjustment necessary

Zidovudine81
(AZT, ZDV)(Retrovir)
200 mg QD600 mg QDZidovudine AUC: decreased 48%---

No dose adjustment necessary

"-" indicates that there are no data available
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