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)
Table 14. Drugs That Should Not Be Used With Antiretroviral Agents
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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.
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