Selected CYP3A4 Substrates/Rifampin Interactions

This information is generalized and not intended as specific medical advice. Consult your healthcare professional before taking or discontinuing any drug or commencing any course of treatment.

Medical warning:

Severe. These medicines may interact and cause very harmful effects and are usually not taken together. Contact your healthcare professional (e.g. doctor or pharmacist) for more information.

How the interaction occurs:

When these two medicines are taken together, your body may process your HIV medicine more quickly.

What might happen:

Your blood levels of HIV medicine may decrease and reduce its beneficial effects.

What you should do about this interaction:

Contact your healthcare professionals (e.g. doctor or pharmacist) as soon as possible about taking these two medicines together. They may already be aware of this interaction and may be monitoring you for it. Do not start, stop, or change the dosage of any medicine before checking with them first.

  • 1.Invirase (saquinavir mesylate) US prescribing information. Roche Laboratories, Inc. March, 2019.
  • 2.Agenerase (amprenavir) Capsules US prescribing information. GlaxoSmithKline May, 2005.
  • 3.Reyataz (atazanavir sulfate) US prescribing information. Bristol-Myers Squibb Company March, 2018.
  • 4.Reyataz (atazanavir sulfate) Australian product information. Bristol-Myers Squibb Pharmaceuticals January 8, 2004.
  • 5.Prezista (darunavir) US prescribing information. Tibotec Inc. May, 2019.
  • 6.Lexiva (fosamprenavir calcium) US prescribing information. GlaxoSmithKline March, 2019.
  • 7.Crixivan (indinavir sulfate) US prescribing information. Merck & Co., Inc. September, 2016.
  • 8.Kaletra (lopinavir/ritonavir tablets) US prescribing information. Abbott Laboratories December, 2019.
  • 9.Viracept (nelfinavir mesylate) US prescribing information. Agouron Pharmaceuticals, Inc. September, 2016.
  • 10.Norvir (ritonavir) US prescribing information. Abbott Laboratories December, 2019.
  • 11.Fortovase (saquinavir) US prescribing information. Roche Laboratories, Inc. December, 2004.
  • 12.Aptivus (tipranavir) US prescribing information. Boehringer Ingelheim Pharmaceuticals, Inc. June, 2018.
  • 13.Stribild (elvitegravir, cobicistat, emtricitabine, tenofovir) prescribing information. Gilead Sciences, Inc. February 6, 2019.
  • 14.Rifadin (rifampin) US prescribing information. Sanofi-Aventis U.S. LLC May, 2020.
  • 15.Dear Healthcare Provider Letter. Subject: Important drug interaction warning for saquinavir. Roche Laboratories, Inc. February 9, 2005.
  • 16.Dear Canadian Healthcare Professional letter: Subject: Drug-induced hepatitis with marked transaminase elevations in healthy volunteers receiving rifampin 600 mg once daily in combination with ritonavir 100 mg / saquinavir 1000 mg twice daily. (ritonavir boosted saquinavir) Hoffmann-La Roche Limited February 10, 2005.
  • 17.Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in adults and adolescents with HIV. Department of Health and Human Services. Available at http://aidsinfo.nih.gov/contentfiles/AdultandAdolescentGL.pdf July 10, 2019.
  • 18.Panel on Opportunistic Infections in Adults and Adolescents with HIV. Mycobacterium tuberculosis Infection and Disease. Guidelines for the prevention and treatment of opportunistic infections in adults and adolescents with HIV: recommendations from the CDC, the NIH, and the HIV Medicine Association of the IDSA. Available at http://aidsinfo.nih.gov/contentfiles/lvguidelines/adult_oi.pdf. September 22, 2017.
  • 19.CDC. Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis online. Available at http://www.cdc.gov/tb/TB_HIV_Drugs/default.htm June, 2013.
  • 20.Polk RE, Brophy DF, Israel DS, Patron R, Sadler BM, Chittick GE, Symonds WT, Lou Y, Kristoff D, Stein DS. Pharmacokinetic Interaction between amprenavir and rifabutin or rifampin in healthy males. Antimicrob Agents Chemother 2001 Feb;45(2):502-8.
  • 21.Justesen US, Andersen AB, Klitgaard NA, Brosen K, Gerstoft J, Pedersen C. Pharmacokinetic interaction between rifampin and the combination of indinavir and low-dose ritonavir in HIV-infected patients. Clin Infect Dis 2004 Feb 1;38(3):426-9.
  • 22.Jaruratanasirikul S, Sriwiriyajan S. Effect of indinavir on the pharmacokinetics of rifampicin in HIV-infected patients. J Pharm Pharmacol 2001 Mar;53(3):409-12.
  • 23.la Porte CJ, Colbers EP, Bertz R, Voncken DS, Wikstrom K, Boeree MJ, Koopmans PP, Hekster YA, Burger DM. Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers. Antimicrob Agents Chemother 2004 May;48(5):1553-60.
  • 24.Decloedt EH, Maartens G, Smith P, Merry C, Bango F, McIlleron H. The safety, effectiveness and concentrations of adjusted lopinavir/ritonavir in HIV-infected adults on rifampicin-based antitubercular therapy. PLoS One 2012;7(3):e32173.
  • 25.Decloedt EH, McIlleron H, Smith P, Merry C, Orrell C, Maartens G. Pharmacokinetics of lopinavir in HIV-infected adults receiving rifampin with adjusted doses of lopinavir-ritonavir tablets. Antimicrob Agents Chemother 2011 Jul;55(7):3195-200.
  • 26.Sunpath H, Winternheimer P, Cohen S, Tennant I, Chelin N, Gandhi RT, Murphy RA. Double-dose lopinavir-ritonavir in combination with rifampicin-based anti-tuberculosis treatment in South Africa. Int J Tuberc Lung Dis 2014 Jun;18(6):689-93.
  • 27.Ribera E, Azuaje C, Lopez RM, Domingo P, Soriano A, Pou L, Sanchez P, Mallolas J, Sambea MA, Falco V, Ocana I, Lopez-Colomes JL, Gatell JM, Pahissa A. Once-daily regimen of saquinavir, ritonavir, didanosine, and lamivudine in HIV-infected patients with standard tuberculosis therapy (TBQD Study). J Acquir Immune Defic Syndr 2005 Nov 1;40(3):317-23.
  • 28.Grub S, Bryson H, Goggin T, Ludin E, Jorga K. The interaction of saquinavir (soft gelatin capsule) with ketoconazole, erythromycin and rifampicin: comparison of the effect in healthy volunteers and in HIV-infected patients. Eur J Clin Pharmacol 2001 May;57(2):115-21.
  • 29.Phansalkar S, Desai AA, Bell D, Yoshida E, Doole J, Czochanski M, Middleton B, Bates DW. High-priority drug-drug interactions for use in electronic health records. J Am Med Inform Assoc 2012 Sep-Oct; 19(5):735-43.

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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.