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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: February 12, 2013; last reviewed: February 12, 2013)

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This table only lists drugs that should not be co-administered at any dose and regardless of RTV boosting. See Tables 18 and 19 for more detailed PK interaction data.

Table 17. Drugs That Should Not Be Used With Antiretroviral Agents
ARV Agents and Contraindicated Drugs by Drug Category
ARV Agentsa,b Cardiac Agents Lipid- Lowering Agents Antimyco-bacterials GI Drugs Neuroleptics Psycho-tropics Ergot Derivatives (Vasoconstrictors)  Herbs ARV Agents Other
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
Drgonovine
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 supp-lements 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
Salmeterol
Sildenafil for PAH
DTG Dofetilide None Rifapentinec
None
None
None
None
St. John’s wort
NVP Carbamazepine
Oxcarbazepine
Phenobarbital
Phenytoin
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 who received rifapentine as part of a treatment regimen for TB had a higher rate of TB relapse and acquired rifamycin resistance than those treated with other rifamycin-based regimens. Therefore an alternative agent to rifapentine is recommended for TB treatment.
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 18a). 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 18a and 18b
Midazolam, triazolam: temazepam, lorazepam, oxazepam

Key to Acronyms: ARV = antiretroviral; ATV = atazanavir; ATV/r = ritonavir-boosted atazanavir; cobi = cobicistat; CYP = cytochrome P; DLV = delavirdine; DRV/r = ritonavir-boosted darunavir; DTG = dolutegravir; EFV = efavirenz; ETR = etravirine; EVG = elvitegravir; FDA = Food and Drug Administration; FPV = fosamprenavir ; FPV/r = ritonavir-boosted fosamprenavir; FTC = emtricitabine; IDV = indinavir; LPV/r = ritonavir-boosted lopinavir; 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 = ritonavir-boosted saquinavir; TB = tuberculosis; TDF = tenofovir disoproxil fumarate; TPV/r = ritonavir-boosted tipranavir

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