Last Updated: April 16, 2019; Last Reviewed: April 16, 2019
Raltegravir (RAL, Isentress)
|Raltegravir (RAL, Isentress)
For additional information see Drugs@FDA: https://www.accessdata.fda.gov/scripts/cder/daf/
|Tablet: 400 mg (film-coated poloxamer tablet)
HD Tablet: 600 mg (film-coated poloxamer tablet)
Chewable Tablets: 100 mg (scored) and 25 mg
Granules for Oral Suspension: Single-use packet of 100 mg of raltegravir, suspended in 10 mL of water for a final concentration of 10 mg/mL.
Note: Film-coated tablets, chewable tablets, and oral suspension are not interchangeable.
||Selected Adverse Events
|Note: No dosing information is available for preterm infants or infants weighing <2 kg at birth. (See Antiretroviral Management of Newborns with Perinatal HIV Exposure or Perinatal HIV and Table 12 for information about using raltegravir for the prevention of perinatal HIV transmission).
Neonate (Weighing ≥2 kg) Dose
Raltegravir Oral Suspension Dosing Table for Full-Term Neonates from Birth to Age 4 Weeks:
Neonates Aged ≥37 Weeks and Weighing ≥2 kg
Note: If the mother has taken raltegravir 2 hours to 24 hours prior to delivery, the neonate’s first dose should be delayed until 24 hours to 48 hours after birth.
Note: Metabolism by uridine diphosphate glucuronyl transferase (UGT1A1) is low at birth and increases rapidly during the next 4 to 6 weeks of life.
Infant and Child (Weighing ≥3 kg to <20 kg) Dose
Raltegravir Oral Suspension Dosing Table for Patients Aged ≥4 Weeksa
Note: The maximum dose of oral suspension is 10 mL (raltegravir 100 mg) twice daily.
Note: For children weighing 11 kg to 20 kg, either oral suspension or chewable tablets can be used.
Child and Adolescent Dose for Chewable Tablets, Film-Coated Tablets, and HD Tablets
Children Weighing ≥11 kg:
Children and Adolescents Weighing ≥50 kg:
- Weighing <25 kg: Chewable tablets twice daily. See table below for chewable tablet dose.
- Weighing ≥25 kg: Raltegravir 400-mg, film-coated tablet twice daily or chewable tablets twice daily. See table below for chewable tablet dose.
Chewable Tablet Dosing Tablea
- Two raltegravir 600-mg HD tablets (1,200 mg) once daily
- This dose is for treatment-naive or virologically suppressed patients who are on an initial dose of raltegravir 400 mg twice daily.
- See the Approval section under the Pediatric Use heading below for more information.
Note: Maximum dose of chewable tablets is raltegravir 300 mg twice daily.
- Rash, including Stevens-Johnson syndrome, hypersensitivity reaction, and toxic epidermal necrolysis
- Nausea, diarrhea
- Headache, dizziness, fatigue
- Creatine phosphokinase elevation, muscle weakness, and rhabdomyolysis
- Raltegravir can be given without regard to food.
- Coadministration or staggered administration of aluminum-containing and magnesium-containing antacids is not recommended with any raltegravir formulations.
- Significant drug interactions are more likely to occur when the raltegravir HD formulation is used once daily. The following drugs should not be coadministered: calcium carbonate, rifampin, tipranavir/ritonavir, and etravirine.
- Chewable tablets can be chewed, crushed (before administration), or swallowed whole.
- Film-coated tablets, including HD tablets, must be swallowed whole.
- The chewable tablets and oral suspension have better bioavailability than the film-coated tablets. Because the formulations are not interchangeable, do not substitute chewable tablets or oral suspension for film-coated tablets. See specific recommendations for proper dosing of different formulations.
- The chewable tablets should be stored in the original package with a desiccant to protect them from moisture.
- The chewable tablets contain phenylalanine. Therefore, patients with phenylketonuria should make the necessary dietary adjustments.
- The oral suspension comes in a kit that includes mixing cups, oral dosing syringes, and 60 foil packets. Detailed instructions for preparation are provided in the Instructions for Use document. Each foil packet is single-use and contains 100 mg of raltegravir, which will be suspended in 10 mL of water for a final concentration of raltegravir 10 mg/mL. Gently swirl the mixing cup for 45 seconds in a circular motion to mix the powder into a uniform suspension.
- Do not shake the oral suspension. Dose should be administered within 30 minutes of mixing; unused solution should be discarded as directed in the Instructions for Use document.
Raltegravir Dosing in Patients with Hepatic Impairment:
- UGT1A1-mediated glucuronidation
Raltegravir Dosing in Patients with Renal Impairment:
- No dose adjustment is necessary in patients who have mild-to-moderate hepatic insufficiency and are receiving twice daily dosing of raltegravir.
- No dose adjustment is necessary for patients with mild-to-moderate hepatic insufficiency who are receiving either raltegravir 1,200 mg once daily or 400 mg twice daily.
- No studies have been conducted on the use of raltegravir HD in patients with hepatic impairment. Therefore, administration of raltegravir HD is not recommended in patients with hepatic impairment.
- The effect of severe hepatic impairment on raltegravir pharmacokinetics has not been studied.
- No dose adjustment is necessary in patients with any degree of renal impairment.