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Drug Interactions with Hepatitis C Virus NS3/4A Protease Inhibitors and HIV
Medications: A Quick Guide for Clinicians – Updated September 2012
John J Faragon, PharmD, BCPS, AAHIVE,
Douglas Fish, MD
Marshall Glesby, MD, PhD
Contraindicated Medications with HCV NS3/4A Protease Inhibitors*
Medication and or Class
Contraindicated with Boceprevir
Contraindicated with Telaprevir
Alpha blockers
Alfluzosin
Alfluzosin
Anticonvulsants
Carbamazepime, phenobarbital,
phenytoin
Antimycobacterials
Rifampin
Rifampin
Ergot derivatives
Dihydroergotamine, ergonovine,
Dihydroergotamine, ergonovine,
ergotamine, methylergonovine
ergotamine, methylergonovine
GI motility medications
Cisapride
Cisapride
Herbal products
St John’s Wort
St. John’s Wort
HMG CoA Reductase Inhibitors
Lovastatin, simvastatin
Atrovastatin, lovastatin, simvastatin
Oral contraceptives
Drospirenone
Neuroleptic
Pimozide
Pimozide
Erectile Dysfunction Medications
Sildenafil or tadalafil when used for
Sildenafil or tadalafil when used for
pulmonary hypertension
pulmonary hypertension
Sedative Hypnotics
Triazolam and orally administered
Orally administered midazolam
midazolam
*This table includes medications listed as contraindicated in the current Product Information for boceprevir and telaprevir.
Other medications may also be contraindicated or should be co-administered with caution. Consult additional resources.
Boceprevir (VictrelisTM) Drug Interactions with HIV Medications
Concurrent Medication
Recommendation
Atazanavir/ritonavir (Reyataz®/Norvir®)  Atazanavir AUC decreased 35%
 Co-administration not
 Atazanavir Cmin decreased 49%
recommended
 Ritonavir AUC decreased 36%
 Boceprevir AUC unchanged
Darunavir/ritonavir (Prezista®/Norvir®)  Darunavir AUC decreased 44%
 Co-administration not
 Darunavir Cmin decreased 59%
recommended
 Ritonavir AUC decreased 26%
 Boceprevir AUC decreased 29%
 Boceprevir Cmin decreased 35%
Lopinavir/ritonavir (Kaletra®)
 Lopinavir AUC decreased 34%
 Co-administration not
 Lopinavir Cmin decreased 43%
recommended
 Ritonavir AUC decreased 23%
 Boceprevir AUC decreased 44%
 Boceprevir Cmin decreased 35%
Efavirenz (Sustiva®)
 Efavirenz AUC increased 20%
 Co-administration not
 Boceprevir AUC decreased 19%
recommended
 Boceprevir Cmin decreased 44%
Etravirine (Intelence®)
 Etravirine AUC decreased 23%
 Co-administration possible, clinical
 Etravirine Cmin decreased 29%
implications of reduced etravirine
 Boceprevir AUC increased 10%
levels unclear
 Boceprevir Cmin decreased 12%
Tenofovir (Viread®)
 No significant changes reported
 No dose adjustment necessary
Raltegravir (Isentress®)
 No significant changes reported
 No dose adjustment necessary
Telaprevir (IncivekTM) Drug Interactions with HIV Medications
Concurrent Medication
Recommendation
Atazanavir/ritonavir (Reyataz®/Norvir®)  Telaprevir AUC decreased 20%
 No dose adjustment necessary
 Atazanavir AUC increased 17%
 Atazanavir Cmin increased 85%
Darunavir/ritonavir (Prezista®/Norvir®)
 Darunavir AUC decreased 40%
 Co-administration not
 Telaprevir AUC decreased 35%
recommended
Fosamprenavir/ritonavir
 Amprenavir AUC decreased 47%
 Co-administration not
(Lexiva®/Norvir®)
 Telaprevir AUC decreased 32%
recommended
Lopinavir/ritonavir (Kaletra®)
 Lopinavir levels unchanged
 Co-administration not
 Telaprevir AUC decreased 54%
recommended
Efavirenz (Sustiva®)
 Efavirenz AUC unchanged
 Increase telaprevir dose to 1125mg
 Telaprevir AUC decreased 26%
 Telaprevir Cmin decreased 47%
When used with tenofovir
 Efavirenz AUC decreased 15% to 18%
 Telaprevir AUC decreased 18% to 20%
Etravirine (Intelence®)
 Etravirine levels unchanged
 No dosage adjustment necessary
 Telaprevir AUC decreased 16%
 Telaprevir Cmin decreased 25%
Rilpivirine (Edurant®)
 Rilpivirine AUC increased 78%
 No dosage adjustment necessary
 Rilpivirine Cmin increased 93%
 Telaprevir AUC decreased 5%
 Telaprevir Cmin decreased 11%
Tenofovir (Viread®)
 Tenofovir AUC increased 30%
 Monitor for tenofovir-associated
 Tenofovir Cmin increased 6% to 41%
toxicity
Raltegravir (Isentress®)
 Raltegravir AUC increased 31%
 No dose adjustment necessary
 Telaprevir levels unchanged
Definitions: AUC – Area under the curve; used as a measure of overall drug exposure. Cmin – Minimum concentration; often referred to as the trough concentration
References: Department of Health and Human Services Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents. March 27,2012. Accessed on
September 22, 2012. Product Information. Victrelis®, Merck and Co. Whitehouse Station NJ. May 2011. Product Information. Incivek®, Vertex. Cambridge, MA. May 2011. 13th
International Workshop on Clinical Pharmacology of HIV Therapy, April 2012, Abstracts O-15 and O-18

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