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

Drug Interactions

Drugs That Should Not Be Used With Antiretroviral Agents

(Last updated:2/12/2013; last reviewed:2/12/2013)

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This table only lists drugs that should not be co-administered at any dose and regardless of ritonavir (RTV) boosting. See Tables 15 and 16 for more detailed pharmacokinetic (PK) interaction data.

Table 14. Drugs That Should Not Be Used With Antiretroviral Agents
Drug Categories
Antiretroviral Agentsa,b Cardiac Agents Lipid- Lowering Agents Antimyco-bacterials Gastro-intestinal Drugs Neuroleptics Psycho-tropics Ergot Derivatives (vasoconstrictors)  Herbs Anti-retroviral Agents Others 
ATV +/− RTV amiodarone
dronedarone
lovastatin
simvastatin
rifampin
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort ETR
NVP
alfuzosin
irinotecan
salmeterol
sildenafil for PAH
DRV/r amiodarone
dronedarone
lovastatin
simvastatin
rifampin
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort none alfuzosin
salmeterol
sildenafil for PAH
FPV +/− RTV amiodarone
dronedarone
flecainide
propafenone
lovastatin
simvastatin
rifampin
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort ETR alfuzosin
salmeterol
sildenafil for PAH
LPV/r amiodarone
dronedarone
lovastatin
simvastatin
rifampind
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort none alfuzosin
salmeterol
sildenafil for PAH
SQV/r amiodarone
dronedarone
dofetilide
flecainide
lidocaine
propafenone
quinidine
lovastatin
simvastatin
rifampind
rifapentinec
cisapridee pimozide midazolamf
triazolam
trazodone
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort garlic supplements none alfuzosin
salmeterol
sildenafil for PAH
TPV/r amiodarone
dronedarone
flecainide
propafenone
quinidine
lovastatin
simvastatin
rifampin
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort ETR alfuzosin
salmeterol
sildenafil for PAH
EFV none none  rifapentinec cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergonovine
ergotamine
methylergonovine
St. John’s wort other NNRTIs none
ETR none none rifampin
rifapentinec
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  rifapentinec none  none  none  none  St. John’s wort ATV +/− RTV
other NNRTIs
ketoconazole
RPV none none rifabutin
rifampin
rifapentinec
proton pump inhibitors none none  none  St. John’s wort other NNRTIs carbamazepine
oxcarbazepine
phenobarbital
phenytoin
MVC none none  rifapentinec none none none none St. John’s wort none none
EVG/COBI/TDF/FTC none lovastatin
simvastatin
rifabutin
rifampin
rifapentinec
cisapridee pimozide midazolamf
triazolam
dihydroergotamine
ergotamine
methylergonovine
St. John’s wort All other ARVs alfuzosin
sildenafil for PAH
a DLV, IDV, NFV, and RTV (as sole PI) are not included in this table. Refer to the appropriate FDA package insert for information regarding DLV-, IDV-, NFV-, and RTV (as sole PI)-related drug interactions.
b Certain listed drugs are contraindicated on the basis of 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.
c HIV-infected patients treated with rifapentine have a higher rate of tuberculosis (TB) relapse than those treated with other rifamycin-based regimens. Therefore an alternative agent to rifapentine is recommended.
d 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 and therefore, these dosing strategies should not be used.
e The manufacturer of cisapride has a limited-access protocol for patients who meet specific clinical eligibility criteria.
f 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: Fluvastatin, pitavastatin, and pravastatin (except for pravastatin with DRV/r) have the least potential for drug-drug interactions (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


Key to Abbreviations
: ATV +/- RTV = atazanavir +/- ritonavir, ATV/r = atazanavir/ritonavir, COBI = cobicistat, CYP = cytochrome P, DLV = delavirdine, DRV/r = darunavir/ritonavir, EFV = efavirenz, ETR = etravirine, EVG = elvitegravir, FDA = Food and Drug Administration, FPV +/- RTV = fosamprenavir +/- ritonavir, FPV/r = fosamprenavir/ritonavir, 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, PK = pharmacokinetic, RPV = rilpivirine, RTV = ritonavir, SQV = saquinavir, SQV/r = saquinavir/ritonavir, TB = tuberculosis, TPV/r = tipranavir/ritonavir