raltegravir (Isentress, RAL)
Jump to navigation
Jump to search
Indications
- add on therapy for multi-drug resistant HIV1
- alternative to efavirenz as part of a combination regimen against HIV1 in treatment-naive patients[4]
- FDA-approved for adults & children >= 2 years of age[5]
- acceptable for use during pregnancy[6]
Dosage
Storage
- store in orginal container
- must be protected from moisture
- original container has a desiccant[7]
Dosage adjustment in renal failure
- no dosage adjustment with moderate renal insufficiency or hepatic impairment
Pharmacokinetics
- metabolized by glucuronidation
- not a known inhibitor, inducer or substrate of Cyt P450
- protein-binding 83%
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
Mechanism of action
Notes
- Cost $27/day Oct 2007
- has not been studied in pregnant women (2007)
More general terms
References
- ↑ Isentress (raltegravir tablets [prescribing information] Merk of Co Http://www.merck.com/product/usa/pi_circulars/i/isentress_pi.pdf
- ↑ 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
- ↑ Prescriber's Letter 14(11): 2007 New HIV Drug: Raltegravir (Isentress) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=231103&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 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: https://www.ncbi.nlm.nih.gov/pubmed/19647866
- ↑ 5.0 5.1 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
- ↑ 6.0 6.1 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) - ↑ 7.0 7.1 Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300622&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015