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HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use ISENTRESS safely and effectively. See full prescribing information for ISENTRESS.
ISENTRESS® (raltegravir) Tablets
Initial U.S. Approval: 2007
ISENTRESS ® (raltegravir) film-coated tablets, for oral use
ISENTRESS ® (raltegravir) chewable tablets, for oral use
ISENTRESS ® (raltegravir) for oral suspension
[Drug information / PDF]
Dosing: Click (+) next to Dosage and Administration section (drug info link)
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.
Mechanism of Action
Raltegravir is an HIV-1 antiviral drug.
Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection. Raltegravir did not significantly inhibit human phosphoryltransferases including DNA polymerases , , and .
INDICATIONS AND USAGE
ISENTRESS is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated:
In combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older (1).
The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response (14).
WARNINGS AND PRECAUTIONS
Severe, potentially life-threatening and fatal skin reactions have been reported. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis. Immediately discontinue treatment with ISENTRESS and other suspect agents if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely (5.1).
Monitor for Immune Reconstitution Syndrome (5.2).
Inform patients with phenylketonuria that the 100 mg and 25 mg chewable tablets contain phenylalanine (5.3).
Coadministration of ISENTRESS with drugs that are strong inducers of UGT1A1 may result in reduced plasma concentrations of raltegravir.
USE IN SPECIFIC POPULATIONS
ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Pregnancy registry available .
Breast-feeding is not recommended while taking ISENTRESS.
The most common adverse reactions of moderate to severe intensity (>/=2%) which occurred at a higher rate than the comparator are insomnia and headache.
Creatine kinase elevations were observed in subjects who received ISENTRESS. Myopathy and rhabdomyolysis have been reported. Use with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions.
To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
DOSAGE AND ADMINISTRATION
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.
ISENTRESS can be administered with or without food (2.1).
Do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg film-coated tablet.
See specific dosing guidance for chewable tablets and the formulation for oral suspension (2.1).
400 mg film-coated tablet orally, twice daily (2.2).
During coadministration with rifampin in adults, 800 mg twice daily (2.1).
Children and Adolescents
If at least 25 kg: One 400 mg film-coated tablet orally, twice daily. If unable to swallow a tablet, consider the chewable tablet, as specified in Table 1 (2.3).
If at least 3 kg to less than 25 kg: Weight based dosing, as specified in Table 2. For patients weighing between 11 and 20 kg, either the chewable tablet or the formulation for oral suspension can be used, as specified in Table 2 (2.3).
Method of Administration
ISENTRESS Film-Coated Tablets
Film-Coated Tablets must be swallowed whole
ISENTRESS Chewable Tablets
Chewable Tablets may be chewed or swallowed whole
ISENTRESS For Oral Suspension
Each single-use ISENTRESS packet for oral suspension contains 100 mg of raltegravir which is to be suspended in 5 mL of water giving a final concentration of 20 mg/mL.
Pour packet contents of ISENTRESS for oral suspension into 5 mL of water and mix
Once mixed, measure the recommended volume (dose) of suspension with a syringe and administer the dose orally.
The volume (dose) of suspension should be administered orally within 30 minutes of mixing.
Discard any remaining suspension.
For more details on preparation and administration of the suspension, see Instructions for Use.
DOSAGE FORMS AND STRENGTHS
Film-Coated Tablets: 400 mg
Chewable Tablets: 100 mg scored and 25 mg
For Oral Suspension: Single-use packet of 100 mg
Package Insert data:
Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.
Whitehouse Station, NJ 08889, USA
Revised November 2011
Copyright © 2007, 2009 Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.
All rights reserved
U.S. Patent Nos. US 7,169,780
PRINCIPAL DISPLAY PANEL - 400 mg Bottle Label
Each tablet contains 434.4 mg raltegravir
potassium, equivalent to 400 mg raltegravir.