ISENTRESS® (raltegravir 400 mg) film-coated tablets, for oral use; chewable tablets, for oral use; oral suspension and ISENTRESS® HD (raltegravir 600 mg) film-coated tablets, for oral use

 

Frequently Asked Questions

For answers to questions you may have, select any of the topics below. To see a complete list of Q&As, scroll down.

  • ISENTRESS is a prescription HIV medicine used with other antiretroviral medicines to treat human immunodeficiency virus-1 (HIV-1) infection in adults, and in children weighing at least 4.4 pounds (2 kg). ISENTRESS HD is a prescription HIV medicine used with other antiretroviral medicines to treat HIV-1 infection in adults, and in children weighing at least 88 pounds (40 kg). HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome). ISENTRESS should not be used in children weighing less than 4.4 pounds (2 kg).

  • No. ISENTRESS and ISENTRESS HD can be taken with or without food.

  • Recommended Adult Dosing for ISENTRESS and ISENTRESS HD:

    Treatment-naïve patients:

    • ISENTRESS HD: 1200 mg (2 x 600 mg) film-coated tablet orally, once daily or
    • ISENTRESS: 400 mg film-coated tablet orally, twice daily.

    Treatment experienced patients:

    • ISENTRESS: 400 mg film-coated tablet orally, twice daily.

    For patients who are virologically suppressed on an initial regimen of ISENTRESS 400 mg twice daily:

    • ISENTRESS HD: 1200 mg (2 x 600 mg) film-coated tablet orally, once daily

    During coadministration with rifampin in adults, 800 mg (2 x 400 mg) twice daily.

    The recommended dosage for ISENTRESS is 800 mg twice daily during coadministration with rifampin. Coadministration of rifampin with ISENTRESS HD is not recommended. There are no data to guide coadministration of ISENTRESS with rifampin in patients below 18 years of age.

    Recommended Pediatric Dosing for ISENTRESS and ISENTRESS HD:

    If weighing at least 40 kg, and either

    • treatment-naïve patients or
    • patients who are virologically suppressed on an initial regimen of ISENTRESS 400 mg twice daily:
      • 1200 mg (2 x 600 mg) film-coated tablet orally, once daily or
      • 400 mg film-coated tablet orally, twice daily or
      • 300 mg (3 x 100 mg) chewable tablets, twice daily.

    Do not substitute ISENTRESS chewable tablets or ISENTRESS for oral suspension for the ISENTRESS 400 mg or 600 mg film-coated tablet. See specific dosing guidance for chewable tablets and the formulation for oral suspension.

    If weighing at least 25 kg: One 400 mg film-coated tablet orally, twice daily. If unable to swallow a tablet, consider the chewable tablet.

    If weighing at least 3 kg to less than 25 kg: Weight-based dosing using the chewable tablet or oral suspension.

    For neonates (birth to 4 weeks [28 days] of age): Weight-based dosing of the oral suspension.

  • Dosage for ISENTRESS

    • Film-Coated Tablets: 400 mg.
    • Chewable Tablets: 100 mg scored and 25 mg.
    • For Oral Suspension: Single-use packet of 100 mg.

    Dosage for ISENTRESS HD

    • Film-Coated Tablets: 600 mg.
  • 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 or ISENTRESS HD 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.

    Immune reconstitution syndrome can occur, including the occurrence of autoimmune disorders with variable time to onset, which may necessitate further evaluation and treatment.

    ISENTRESS chewable tablets contain phenylalanine, a component of aspartame, which may be harmful to patients with phenylketonuria.

    Coadministration of ISENTRESS or ISENTRESS HD with drugs that are strong inducers of uridine diphosphate glucuronosyltransferase (UGT) 1A1 may result in reduced plasma concentrations of raltegravir. Coadministration of ISENTRESS or ISENTRESS HD with drugs that inhibit UGT1A1 may increase plasma levels of raltegravir.

    Coadministration of ISENTRESS or ISENTRESS HD and other drugs may alter the plasma concentration of raltegravir. The potential for drug-drug interactions must be considered prior to and during therapy. Coadministration or staggered administration of aluminum and/or magnesium-containing antacids and ISENTRESS or ISENTRESS HD is not recommended. Coadministration of ISENTRESS HD with calcium carbonate antacids, tipranavir/ritonavir, or etravirine is also not recommended.

    Rifampin, a strong inducer of UGT1A1, reduces plasma concentrations of ISENTRESS and ISENTRESS HD. Therefore, the dose of ISENTRESS for adults should be increased to 800 mg twice daily during coadministration with rifampin. There are no data to guide coadministration of ISENTRESS with rifampin in patients below 18 years of age. Coadministration with rifampin is not recommended with ISENTRESS HD.

    The impact of other strong inducers of drug metabolizing enzymes on raltegravir is unknown (e.g., Carbamazepine, Phenobarbital, and Phenytoin). Coadministration of ISENTRESS or ISENTRESS HD with other strong inducers is not recommended.

    The most commonly reported (≥2%) drug-related clinical adverse reactions of moderate to severe intensity in treatment-naïve adult patients receiving ISENTRESS compared with efavirenz were headache (4% vs 5%), insomnia (4% vs 4%), nausea (3% vs 4%), dizziness (2% vs 6%), and fatigue (2% vs 3%), respectively. The most commonly reported (≥2%) clinical adverse reactions of all intensities (Mild, Moderate, and Severe) in treatment-naïve adult patients receiving ISENTRESS HD or ISENTRESS were abdominal pain, diarrhea, vomiting, and decreased appetite. Intensities were defined as follows: Mild (awareness of sign or symptom, but easily tolerated); Moderate (discomfort enough to cause interference with usual activity); or Severe (incapacitating with inability to work or do usual activity).

    Grade 2–4 creatine kinase laboratory abnormalities were observed in subjects treated with ISENTRESS and ISENTRESS HD. 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 and patients with a history of rhabdomyolysis, myopathy or increased serum creatine kinase.

    There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ISENTRESS or ISENTRESS HD during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.

    Women infected with HIV-1 should be instructed not to breastfeed if they are receiving ISENTRESS or ISENTRESS HD due to the potential for HIV transmission.

    No dosage adjustment of ISENTRESS is necessary for patients with mild to moderate hepatic impairment. No hepatic impairment study has been conducted with ISENTRESS HD and therefore administration in patients with hepatic impairment is not recommended. The effect of severe hepatic impairment on the pharmacokinetics of raltegravir has not been studied.

    Before prescribing ISENTRESS or ISENTRESS HD, please read the accompanying Prescribing Information. The Patient Information and Instructions for Use also are available.

  • 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 α, β, and γ.

  • ISENTRESS and ISENTRESS HD are human immunodeficiency virus integrase strand transfer inhibitors (HIV-1 INSTI).

  • The most common adverse reactions of moderate to severe intensity occurring in ≥2% of treatment-naïve adults are insomnia (4%), headache (4%), nausea (3%), dizziness (2%), and fatigue (2%).

    The most common adverse reaction of moderate to severe intensity occurring in ≥2% of treatment-experienced adults is headache (2%).

  • ISENTRESS and ISENTRESS HD do not have contraindications.

  • Yes, a dosage adjustment is not necessary in patients with any degree of renal impairment.a

    a No renal impairment study was conducted with ISENTRESS HD. Because the extent to which raltegravir may be dialyzable is unknown, dosing before a dialysis session should be avoided.

  • Yes. Your eligible, privately insured patients may pay as little as $0, up to a total program savings of $6,800.

    Not valid for patients who are uninsured or patients with Medicare or other Government Program insurance (as defined in the Terms and Conditions). Other eligibility restrictions and Terms and Conditions apply.

    Your patients can visit ISENTRESS.com to review the Terms and Conditions, as well as access and activate the coupon.

    Request vouchers and/or coupons for ISENTRESS

Indication

ISENTRESS and ISENTRESS HD are indicated in combination with other antiretroviral (ARV) agents for the treatment of HIV-1 infection in adult patients.

Selected Safety Information

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 or ISENTRESS HD 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.

Immune reconstitution syndrome can occur, including the occurrence of autoimmune disorders with variable time to onset, which may necessitate further evaluation and treatment.

ISENTRESS chewable tablets contain phenylalanine, a component of aspartame, which may be harmful to patients with phenylketonuria.

Coadministration of ISENTRESS or ISENTRESS HD with drugs that are strong inducers of uridine diphosphate glucuronosyltransferase (UGT) 1A1 may result in reduced plasma concentrations of raltegravir. Coadministration of ISENTRESS or ISENTRESS HD with drugs that inhibit UGT1A1 may increase plasma levels of raltegravir.

Coadministration of ISENTRESS or ISENTRESS HD and other drugs may alter the plasma concentration of raltegravir. The potential for drug-drug interactions must be considered prior to and during therapy. Coadministration or staggered administration of aluminum and/or magnesium-containing antacids and ISENTRESS or ISENTRESS HD is not recommended. Coadministration of ISENTRESS HD with calcium carbonate antacids, tipranavir/ritonavir, or etravirine is also not recommended.

Rifampin, a strong inducer of UGT1A1, reduces plasma concentrations of ISENTRESS and ISENTRESS HD. Therefore, the dose of ISENTRESS for adults should be increased to 800 mg twice daily during coadministration with rifampin. There are no data to guide coadministration of ISENTRESS with rifampin in patients below 18 years of age. Coadministration with rifampin is not recommended with ISENTRESS HD.

The impact of other strong inducers of drug metabolizing enzymes on raltegravir is unknown (e.g., Carbamazepine, Phenobarbital, and Phenytoin). Coadministration of ISENTRESS or ISENTRESS HD with other strong inducers is not recommended.

The most commonly reported (≥2%) drug-related clinical adverse reactions of moderate to severe intensity in treatment-naïve adult patients receiving ISENTRESS compared with efavirenz were headache (4% vs 5%), insomnia (4% vs 4%), nausea (3% vs 4%), dizziness (2% vs 6%), and fatigue (2% vs 3%), respectively. The most commonly reported (≥2%) clinical adverse reactions of all intensities (Mild, Moderate, and Severe) in treatment-naïve adult patients receiving ISENTRESS HD or ISENTRESS were abdominal pain, diarrhea, vomiting, and decreased appetite. Intensities were defined as follows: Mild (awareness of sign or symptom, but easily tolerated); Moderate (discomfort enough to cause interference with usual activity); or Severe (incapacitating with inability to work or do usual activity).

Grade 2–4 creatine kinase laboratory abnormalities were observed in subjects treated with ISENTRESS and ISENTRESS HD. 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 and patients with a history of rhabdomyolysis, myopathy or increased serum creatine kinase.

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ISENTRESS or ISENTRESS HD during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.

Women infected with HIV-1 should be instructed not to breastfeed if they are receiving ISENTRESS or ISENTRESS HD due to the potential for HIV transmission.

No dosage adjustment of ISENTRESS is necessary for patients with mild to moderate hepatic impairment. No hepatic impairment study has been conducted with ISENTRESS HD and therefore administration in patients with hepatic impairment is not recommended. The effect of severe hepatic impairment on the pharmacokinetics of raltegravir has not been studied.

Before prescribing ISENTRESS or ISENTRESS HD, please read the accompanying Prescribing Information. The Patient Information and Instructions for Use also are available.

 

US-MFA-0080901/22