Brand and Other Names:Isentress
- Classes: HIV, Integrase Inhibitors
Dosing & Uses
Dosage Forms & Strengths
Indicated in combination with other antiretroviral agents for HIV-1 infection
400 mg PO BID with or without food
Coadministration with rifampin: 800 mg PO BID
Combination regimen is based on analyses of plasma HIV-1 RNA levels in 3 double-blind controlled studies; 2 of these studies were conducted in clinically advanced, 3-class antiretroviral (NNRTI, NRTI, PI) treatment-experienced adults through 96 wk and 1 study was conducted in treatment-naïve adults through 240 wk
The use of other active agents with raltegravir is associated with a greater likelihood of treatment response
Dosage Forms & Strengths
- 100mg (scored)
powder for oral suspension
Indicated in combination with other antiretroviral agents for HIV-1 infection in children and adolescents aged 4 weeks or older
Film-coated tablet (weight ≥25 kg): 400 mg PO BID
- 10 to <14 kg: 75 mg PO BID
- 14 to <20 kg: 100 mg PO BID
- 20 to <28 kg: 150 mg PO BID
- 28 to <40 kg: 200 mg PO BID
- ≥40 kg: 300 mg PO BID
Powder for oral suspension
- Age at least 4 weeks and weight 3-20 kg
- 3 to <4 kg: 20 mg (1 mL) PO BID
- 4 to <6 kg: 30 mg (1.5 mL) PO BID
- 6 to <8 kg: 40 mg (2 mL) PO BID
- 8 to <11 kg: 60 mg (3 mL) PO BID
- 11 to <14 kg: 80 mg (4 mL) PO BID
- 14 kg to <20 kg: 100 mg (5 mL) PO BID
Combination regimen is based on safety, tolerability, pharmacokinetic parameters, and efficacy data through at least 24-wk in a multicenter, open-label, noncomparative study in HIV-1 infected children and adolescents aged 4 wk to 18 yr
May administer with or without food
Chewable tablets and film-coated tablets are not bioequivalent; and therefore, are not interchangeable
Powder for oral suspension
- Suspend 1 packet (100 mg) in 5 mL of water; final concentration of 20 mg/mL
- Administer suspension within 30 minutes of mixing
- Discard any remaining suspension
Serious - Use Alternative
Significant - Monitor Closely
Total cholesterol increased (16%)
AST increased (9%)
Glucose increased (9%)
Abdominal pain (5%)
Extremity pain (3%)
Drug related hypersensitivity
Psychiatric disorders: anxiety, depression (particularly in patients with a pre-existing history of psychiatric illness), including suicidal ideation and behaviors, paranoia
Skin: rash, Steven’s-Johnson syndrome
Risk of immune reconstitution syndrome if used with HAART
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
Phenylketonurics: Chewable tablets contain phenylalanine, a component of aspartame
Pregnancy & Lactation
Pregnancy Category: C
Lactation: HIV+ women shouldn't breastfeed
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Inhibits catalytic activity of HIV-1 integrase, an HIV encoded enzyme required for viral replication
Peak Plasma Time: 3 hr in fasted state
Protein Bound: 83%
Half-Life: 9 hr
Excretion: Feces 51%; urine 32%
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