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raltegravir (Isentress, RAL)

Indications: 1) add on therapy for multi-drug resistant HIV1 2) alternative to efavirenz as part of a combination regimen against HIV1 in treatment-naive patients [4] 3) FDA-approved for adults & children >= 2 years of age [5] 4) acceptable for use during pregnancy [6] Dosage: - 400 mg PO BID Storage: - store in orginal container - must be protected from moisture - original container has a desiccant [7] Pharmacokinetics: - metabolized by glucuronidation - not a known inhibitor, inducer or substrate of Cyt P450 - protein-binding 83% Dosage adjustment in renal failure: - no dosage adjustment with moderate renal insufficiency or hepatic impairment Adverse effects: - diarrhea, nausea, headache (most common, but > placebo ?) - elevated creatinine kinase - possibly myopathy, rhabdomyolysis Drug interactions: - rifampin can reduce raltegravir levels by inducing enzymes that glucuronidate raltegravir Laboratory: - raltegravir in serum/plasma Mechanism of action: - inhibits HIV integrase - resistant strains Notes: - Cost $27/day Oct 2007 - has not been studied in pregnant women (2007)

Interactions

drug interactions drug adverse effects of antiretroviral agents

General

integrase inhibitor; integrase strand transfer inhibitor (InSTI)

References

  1. Isentress (raltegravir tablets [prescribing information] Merk of Co Http://www.merck.com/product/usa/pi_circulars/i/isentress_pi.pdf
  2. Taltegravir Review Team. Memoradum to the [Antiviral Drugs] Advisory Committe: Background package for NDA 22-145; retegravir, August 8, 2007 http://www.fda.gov/ohrms/dockets/ac/07/briefing/2007-4314b1-02-fda.pdf
  3. Prescriber's Letter 14(11): 2007 New HIV Drug: Raltegravir (Isentress) Detail-Document#: 231103 (subscription needed) http://www.prescribersletter.com
  4. Lennox JL et al Safety and efficacy of raltegravir-based versus efavirenz- based combination therapy in treatment-naive patients with HIV-1 infection: A multicentre, double-blind randomised controlled trial. Lancet 2009 Sep 5; 374:796. PMID: 19647866
  5. FDA NEWS RELEASE: Dec. 21, 2011 FDA expands use of HIV drug Isentress to children and adolescents http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm284473.htm
  6. 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)
  7. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  8. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015