Classes
DEA Class; Rx
Common Brand Names; Isentress, Isentress HD
- HIV, Integrase Inhibitors
Description
First FDA-approved HIV integrase strand transfer inhibitor (HIV-1 INSTI)
Used for treatment of HIV-1 infection in combination with other antiretrovirals
Elevated CPK, muscle weakness, and rhabdomyolysis reported
Indications
Indicated in combination with other antiretroviral agents for HIV-1 infection
Adverse Effects
- Serum alanine aminotransferase, Grade 2-4 (2-11%)
- Serum aspartate aminotransferase, Grade 2-4 (1-8%)
- Fasting serum glucose test, Grade 2-4 (7%)
- Total serum bilirubin, Grade 2-4 (≤5%)
- Headache (4%)
- Insomnia (4%)
- Nausea (3%)
- ANC, Grade 2-4 (1-3%)
- Serum alkaline phosphate, Grade 2-4 (≤3%)
- Dizziness (2%) Fatigue (2%)
- Creatinine (≤1%)
- Hemoglobin, Grade 2-4 (≤1%)
- Platelet count, Grade 2-3 (≤1%)
Warnings
Risk of immune reconstitution syndrome if used with HAART; during initial phase of combination antiretroviral treatment, patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jiroveci pneumonia, tuberculosis), which may necessitate further evaluation and treatment
Autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution, however, the time to onset is more variable, and can occur many months after initiation of treatment
Concomitant medications known to increase risk of myopathy or rhabdomyolysis
Coadministration with drugs that are strong inducers of UGT1A1 may result in reduced plasma concentrations of raltegravir
Drug rash with eosinophilia and systemic symptoms (DRESS) reported
Severe, potentially life-threatening and fatal skin reactions reported; skin reactions include cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis; immediately discontinue treatment if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely
Chewable tablets contain phenylalanine, a component of aspartame; phenylalanine can be harmful to patients with phenylketonuria
Pregnancy and Lactation
Available data from APR show no difference in rate of overall birth defects for raltegravir compared to background rate for major birth defects of 2.7% in U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP)
No data are available on presence of raltegravir in human milk, effects on breastfed infant, or on milk production; when administered to lactating rats, raltegravir was present in milk
Maximum Dosage
800 mg/day PO for the 400 mg film-coated tablet; 1,600 mg/day PO with concomitant rifampin; 1,200 mg/day for the 600 mg film-coated tablet; safety and efficacy of other formulations have not been established.
800 mg/day PO for the 400 mg film-coated tablet; 1,600 mg/day PO with concomitant rifampin; 1,200 mg/day for the 600 mg film-coated tablet; safety and efficacy of other formulations have not been established.
weight 40 kg or more: 600 mg/day PO for the chewable tablet; 800 mg/day PO for the 400 mg film-coated tablet; 1,200 mg/day for the 600 mg film-coated tablet; safety and efficacy have not been established for the oral suspension.
weight 28 to 39 kg: 400 mg/day PO for the chewable tablet; 800 mg/day PO for the 400 mg film-coated tablet; safety and efficacy of other formulations have not been established.
weight 40 kg or more: 600 mg/day PO for the chewable tablet; 800 mg/day PO for the 400 mg film-coated tablet; 1,200 mg/day for the 600 mg film-coated tablet; safety and efficacy have not been established for the oral suspension.
weight 28 to 39 kg: 400 mg/day PO for the chewable tablet; 800 mg/day PO for the 400 mg film-coated tablet; safety and efficacy of other formulations have not been established.
weight 25 to 27 kg: 300 mg/day PO for the chewable tablet; 800 mg/day PO for the 400 mg film-coated tablet; safety and efficacy of other formulations have not been established.
weight 20 to 24 kg: 300 mg/day PO for the chewable tablet; safety and efficacy of other formulations have not been established.
weight 14 to 19 kg: 200 mg/day PO for the oral suspension or chewable tablet; safety and efficacy have not been established for the film-coated tablets.
weight 11 to 13 kg: 160 mg/day PO for the oral suspension; 150 mg/day PO for the chewable tablet; safety and efficacy have not been established for the film-coated tablets.
weight 8 to 10 kg: 120 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
weight 11 to 13 kg: 160 mg/day PO for the oral suspension; 150 mg/day PO for the chewable tablet; safety and efficacy have not been established for the film-coated tablets.
weight 8 to 10 kg: 120 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
weight 6 to 7 kg: 80 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
weight 4 to 5 kg: 60 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
weight 3 kg: 50 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 8 days and older weighing 4 kg: 30 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 8 days and older weighing 3 kg: 20 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 8 days and older weighing 2 kg: 16 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 0 to 7 days weighing 4 kg: 7 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 0 to 7 days weighing 3 kg: 5 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Term Neonates 0 to 7 days weighing 2 kg: 4 mg/day PO for the oral suspension; safety and efficacy of other formulations have not been established.
Premature and Term Neonates weighing less than 2 kg: Safety and efficacy have not been established.
How supplied
Raltegravir
tablet, film-coated
- 400mg (Isentress)
- 600mg (Isentress HD)
