January 10, 2011

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents Page 22 

Table 14. Drugs That Should Not Be Used With PI, NNRTI, or CCR5 Antagonist 

 (Updated January 10, 2011)

This table lists only drugs that should not be coadministered at any dose and regardless of RTV boosting. See Tables 15 and 16 for more detailed 

pharmacokinetic interaction data and dosage adjustments.

1 DLV, IDV, and NFV are not included in this table. Refer to the FDA package insert for information regarding DLV-, IDV-, and NFV-related drug interactions.

2 Certain listed drugs are contraindicated based on theoretical considerations. Thus, drugs with narrow therapeutic indices and suspected metabolic involvement with CYP450 3A, 2D6, or unknown 

pathways are included in this table. Actual interactions may or may not occur in patients.

3 HIV-infected patients treated with rifapentine have a higher rate of TB relapse than those treated with other rifamycin-based regimens; an alternative agent is recommended.

4 A high rate of Grade 4 serum transaminase elevation was seen when a higher dose of RTV was added to LPV/r or SQV or when double-dose LPV/r was used with rifampin to compensate for rifampin’s 

induction effect, so these dosing strategies should not be used.

5 The manufacturer of cisapride has a limited-access protocol for patients who meet specific clinical eligibility criteria.

6 Use of oral midazolam is contraindicated. Parenteral midazolam can be used with caution as a single dose and can be given in a monitored situation for procedural sedation.

Suggested alternatives to: 

Lovastatin, simvastatin: Pravastatin and fluvastatin have the least potential for drug-drug interactions (except for pravastatin with DRV/r, see Table 15a). Use atorvastatin and rosuvastatin with 

caution; start with the lowest possible dose and titrate based on tolerance and lipid-lowering efficacy.

Rifampin: Rifabutin (with dosage adjustment – see Tables 15a and 15b) 

Midazolam, triazolam: temazepam, lorazepam, oxazepam

Acronyms: ATV +/- RTV = atazanavir +/- ritonavir, DLV = delavirdine, DRV/r = darunavir/ritonavir, EFV = efavirenz, ETV = etravirine, FDA = Food and Drug Administration, 

FPV +/- RTV = fosamprenavir +/- ritonavir, HIV = human immunodeficiency virus, IDV = indinavir, LPV/r = lopinavir/ritonavir, MVC = maraviroc, NFV = nelfinavir, 

NNRTI = non-nucleoside reverse transcriptase inhibitor, NVP = nevirapine, PAH = pulmonary arterial hypertension, PI = protease inhibitor, RTV = ritonavir, SQV/r = saquinavir/ritonavir, 

TPV/r = tipranavir/ritonavir

Drug Categories

Antiretroviral 

Agents1, 2

Cardiac 

Agents

Lipidlowering 

Agents

Antimycobacterials

Gastrointestinal 

Drugs

Neuroleptics

PsychotropicsErgot Derivatives 

(vasoconstrictors) Herbs Antiretroviral Agents Others

ATV +/− RTV

none lovastatin

pitavastatin

simvastatin 

rifampin

rifapentine3

cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

ETR

NVP

alfuzosin

irinotecan

salmeterol

sildenafil for PAH

DRV/r

none lovastatin

pitavastatin

simvastatin

rifampin

rifapentine3

cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

none alfuzosin

salmeterol

sildenafil for PAH

FPV +/− RTV

flecainide

propafenone

lovastatin

pitavastatin

simvastatin

rifampin

rifapentine3

cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

ETR alfuzosin

salmeterol

sildenafil for PAH

LPV/r

none lovastatin

pitavastatin

simvastatin

rifampin4

rifapentine3

cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

none alfuzosin

salmeterol

sildenafil for PAH

RTV

amiodarone

flecainide

propafenone

quinidine

lovastatin

pitavastatin

simvastatin

rifapentine3 cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

none alfuzosin

sildenafil for PAH

SQV/r

amiodarone

dofetilide

flecainide

lidocaine

propafenone

quinidine

lovastatin

pitavastatin

simvastatin

rifampin4

rifapentine

cisapride5 pimozide midazolam6

triazolam

trazodone

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

garlic 

supplements

none alfuzosin

salmeterol

sildenafil for PAH

TPV/r

amiodarone

flecainide

propafenone

quinidine

lovastatin

pitavastatin

simvastatin

rifampin

rifapentine3

cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

ETR alfuzosin

salmeterol

sildenafil for PAH

EFV

none none rifapentine3 cisapride5 pimozide midazolam6

triazolam

dihydroergotamine

ergonovine

ergotamine

methylergonovine

St. John’s 

wort

other NNRTIs none

ETR

none none rifampin

rifapentine3

none none none none St John’s 

wort

unboosted PIs 

ATV/r, FPV/r, 

or TPV/r

other NNRTIs

carbamazepine 

phenobarbital 

phenytoin

clopidogrel

NVP none none rifapentine3 none none none none St. John’s 

wort

ATV +/− RTV

other NNRTIs

ketoconazole

MVC none none rifapentine3 none none none none St. John’s 

wort

none none