January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 16 

Table 11. Drug Interactions between Antiretroviral Agents and Drugs Used to Treat 

Page 1 of 2 Opioid Addiction (January 10, 2011)

Concomitant 

Drug Antiretroviral Class/Drug Pharmacokinetic InteractionsRecommendations/Clinical Comments

Buprenorphine EFV buprenorphine AUC ↓ 50%; norbuprenorphine* AUC ↓ 71%

No withdrawal symptoms reported. No dosage adjustment 

recommended; however, monitor for withdrawal symptoms. 

ATV buprenorphine AUC ↑ 93%; norbuprenorphine AUC ↑ 76%;

↓ ATV levels possible

Do not coadminister buprenorphine with unboosted ATV.

ATV/r buprenorphine AUC ↑ 66%; norbuprenorphine AUC ↑ 105%

Monitor for sedation. Buprenorphine dose reduction may be 

necessary. 

DRV/r buprenorphine: no significant effect, 

norbuprenorphine AUC ↑ 46% and Cmin ↑ 71%

No dose adjustment necessary. 

TPV/r buprenorphine: no significant effect;

norbuprenorphine AUC, Cmax, and Cmin ↓ 80%;

TPV Cmin ↓ 19%–40%

Consider monitoring TPV level.

3TC, ddI, TDF, ZDV, NVP, 

LPV/r, NFV

No significant effect

No dosage adjustment necessary.

ABC, d4T, FTC, ETR,

FPV +/- RTV, IDV +/- RTV, 

SQV/r, RAL, MVC, T20

No data
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Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 17 

Concomitant 

Drug

Antiretroviral Class/Drug Pharmacokinetic Interactions

Recommendations/Clinical Comments

Methadone ABC methadone clearance ↑ 22%

No dosage adjustment necessary.

d4T d4T AUC ↓ 23% and Cmax ↓ 44% 

No dosage adjustment necessary.

ZDV ZDV AUC ↑ 29%–43%

Monitor for ZDV-related adverse effects.

EFV methadone AUC ↓ 52%

Opioid withdrawal common; increased methadone dose often 

necessary.

NVP methadone AUC ↓ 41% 

NVP: no significant effect

Opioid withdrawal common; increased methadone dose often 

necessary.

ATV/r, DRV/r, 

FPV/r, IDV/r, 

LPV/r, SQV/r, 

TPV/r

With ATV/r, DRV/r, FPV/r: R-methadone† AUC ↓ 16%−18%;

With LPV/r: methadone AUC ↓ 26%–53%;

With SQV/r 1,000/100mg BID: R-methadone AUC ↓ 19%;

With TPV/r: R-methadone AUC ↓ 48%

Opioid withdrawal unlikely but may occur. No adjustment in 

methadone usually required; however, monitor for opioid 

withdrawal and increase methadone dose as clinically indicated.

FPV No data with FPV (unboosted)

With APV: R-methadone Cmin ↓ 21%, AUC no significant change

Monitor and titrate methadone as clinically indicated.

The interaction with FPV is presumed to be similar.

NFV methadone AUC ↓ 40%

Opioid withdrawal rarely occurs. Monitor and titrate dose as 

clinically indicated. May require increased methadone dose.

ddI (EC capsule), 3TC, TDF, 

ETR, RTV, ATV, IDV, RAL

No significant effect

No dosage adjustment necessary.

FTC, MVC, T20 No data

*

Norbuprenorphine is an active metabolite of buprenorphine.

† R-methadone is the active form of methadone.

Acronyms: 3TC = lamivudine, d4T = stavudine, T20 = enfuvirtide, ABC = abacavir, APV = amprenavir,

ATV = atazanavir, ATV/r = atazanavir/ritonavair, ddI = didanosine, DRV/r = darunavir/ritonavir, EFV = efavirenz,

ETR = etravirine, FPV = fosamprenavir, FPV/r = fosamprenavir/ritonavir, FTC = emtricitabine, IDV = indinavir,

IDV/r = indinavir/ritonavir, LPV/r = lopinavir/ritonavir, MVC = maraviroc, NFV = nelfinavir, NVP = nevirapine,

RAL = raltegravir, RTV = ritonavir, SQV/r = sacquinavir/ritonavir, TDF = tenofovir, TPV = tipranavir, TPV/r = tipranavir/ritonavir,

ZDV = zidovudine

Table 11. Drug Interactions between Antiretroviral Agents and Drugs Used to Treat Opioid Addiction

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