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etravirine (Intelence)

Indications: - NNRTI for treatment of advanced HIV-1 infection (treatment-experienced adults with HIV1) - administer with: ritonavir-bloosted darunavir or ritonavir-bloosted saquiunavir - ok with raltegravir - ok with maraviroc, dose of maraviroc - 600 mg BID without HIV protease inhibitor - 150 mg BID with HIV protease inhibitor Contraindications: - concurrent use of - all unboosted HIV protease inhibitors - ritonavir-boosted tipranavir - fosamprenavir - use during pregnancy (data insufficient) [4] Dosage: - 200 mg PO BID following meals Tablets: 100 mg Storage: - store in orginal container - must be protected from moisture - original container has a desiccant [5] Pharmacokinetics: - hepatically metabolized by Cyt P4503A4 - also induces Cyt P450 3A4 - inhibits Cyt P450 2C9 & Cyt P450 2C19 Monitor: - liver function tests - discontinue if severe hypersensitivity, severe rash, or rash with systemic symptoms or serum ALT or serum AST elevations [3] Adverse effects: - nausea [6] - Stevens-Johnson syndrome - toxic epidermal necrolysis & erythema multiforme - hypersensitivity reactions characterized by a) rash b) constitutional findings c) sometimes organ dysfunction, including hepatic failure [2] Drug interactions: - drugs that induced or inhibit Cyt P450 3A4 or are metabolized by Cyt P450 3A - drugs metabolized Cyt P450 2C9 & Cyt P450 2C19 may increase in concentration Laboratory: - etravirine in serum/plasma Mechanism of action: - non-nucleoside reverse transcription inhibitor (NNRTI) Notes: - Manufacturer: Tibotec - cost 2008 $22/day

Interactions

drug interactions drug adverse effects of antiretroviral agents

General

non-nucleoside reverse transcriptase inhibitor (NNRTI)

Database Correlations

PUBCHEM cid=193962

References

  1. Prescriber's Letter 16(2): 2009 New Drugs Approved by the FDA in 2008 Detail-Document#: 250213 (subscription needed) http://www.prescribersletter.com
  2. FDA MedWatch, 08/27/2009 http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm180579.htm
  3. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  4. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  5. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  6. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  7. Intelence (etravirine) tablets [prescribing information] NJ Tibotec Inc, 2008 http://www.intelence-info.com