Raltegravir

Raltegravir is a prescription medication used in combination with other antiretroviral agents for HIV-1 infection. 

• Raltegravir is available under the following different brand names: Isentress, Isentress HD 

Common side effects of Raltegravir include:

• Nausea,
• Vomiting,
• Diarrhea,
• Stomach pain,
• Headache,
• Tired feeling,
• Dizziness,
• Sleep problems (insomnia), or
• Changes in the shape or location of body fat (especially in arms, legs, face, neck, breasts, and trunk).

Serious side effects of Raltegravir include:

• Pale skin,
• Easy bruising or bleeding,
• Signs of a new infection (such as fever or chills, cough, or flu symptoms),
• Drowsiness,
• Confusion,
• Increased thirst,
• Lower back pain,
• Urinating less than usual or not at all,
• Depression,
• Thoughts about hurting yourself,
• Itching,
• Loss of appetite,
• Dark urine,
• Clay-colored stools,
• Yellowing of the skin or eyes,
• Muscle pain,
• Tenderness,
• Weakness with fever or flu symptoms and
• Dark-colored urine, or
• A severe skin reaction.

Rare side effects of Raltegravir include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet, film-coated

• 400 mg (Isentress)
• 600 mg (Isentress HD)

Tablet, chewable

• 25 mg
• 100 mg (scored)

HIV-1 Infection

Adult dosage

• Treatment-naïve or virologically suppressed
• Treatment-naïve patients or patients who are virologically suppressed on an initial regimen of 400 mg two times a day
• Isentress (400-mg tablet): 400 mg orally two times a day
• Isentress HD (600-mg tablet): 1200 (two 600-mg tabs) orally once a day

Treatment-experienced

• 400 mg orally two times a day

Pediatric dosage

• Film-coated tablet, Isentress 400-mg tab
  • Children above 25 kg to below 40 kg: 400 mg orally two times a day
  • Children above 40 kg and treatment naïve or virologically suppressed on an initial regimen: 400 mg orally two times a day
• Film-coated tablet, Isentress HD 600-mg tablet
  • Children above 40 kg and treatment naïve or virologically suppressed on an initial regimen:1200 mg orally once a day
  • Chewable tablet, Isentress 25 mg- or 100-mg tablet
  • Below 4 weeks: Safety and efficacy not established; not recommended in preterm neonates
  • Above 4 weeks
    • Not to exceed daily dose is 300 mg orally two times a day; dosing recommendations are based on approximately 6 mg/kg/dose
    • 11 to below 14 kg: 75 mg orally two times a day (3 x 25 mg tablets)
    • 14 to below 20 kg: 100 mg orally two times a day (1 x 100 mg tablet)
    • 20 to below 28 kg: 150 mg orally two times a day (1.5 x 100 mg tablets)
    • 28 to below 40 kg: 200 mg orally two times a day (2 x 100 mg tablet)
    • Above 40 kg: 300 mg orally two times a day (3 x 100 mg tablets)
• Oral Suspension
  • Not to exceed 100 mg orally two times a day; see the age and weight-based dosing listed below
  • Preterm neonates: Safety and efficacy not established
  • For full-term neonates (birth to 1 week)
    • Dosing recommendations are based on approximately 1.5 mg/kg/dose
    • 2 to below 3 kg: 4 mg (0.4 mL) orally once a day
    • 3 to below 4 kg: 5 mg (0.5 mL) orally once a day
    • 4 to below 5 kg: 7 mg (0.7 mL) orally once a day
  • For full-term neonates (1 to 4 weeks)
    • Dosing recommendations are based on approximately 3 mg/kg/dose
    • 2 to below 3 kg: 8 mg (0.8 mL) orally once a day
    • 3 to below 4 kg: 10 mg (1 mL) orally once a day
    • 4 to below 5 kg: 15 mg (1.5 mL) orally once a day
  • Age at least 4 weeks and weight of 3-20 kg
    • 3 to below 4 kg: 25 mg (2.5 mL) orally two times a day
    • 4 to below 6 kg: 30 mg (3 mL) orally two times a day
    • 6 to below 8 kg: 40 mg (4 mL) orally two times a day
    • 8 to below 11 kg: 60 mg (6 mL) orally two times a day
    • 11 to below 14 kg: 80 mg (8 mL) orally two times a day
    • 14 kg to below 20 kg: 100 mg (10 mL) orally two times a day

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Raltegravir has severe interactions with the following drugs:
  • aluminum hydroxide
  • aluminum hydroxide/magnesium carbonate
  • aluminum hydroxide/magnesium trisilicate
  • elvitegravir/cobicistat/emtricitabine/tenofovir DF
  • magnesium supplement
• Raltegravir has serious interactions with the following drugs:
  • betibeglogene autotemcel
  • cabotegravir
  • elivaldogene autotemcel
  • magnesium hydroxide
  • sodium sulfate/magnesium sulfate/potassium chloride
  • sodium sulfate/potassium sulfate/magnesium sulfate
• Raltegravir has moderate interactions with the following drugs:
  • apalutamide
  • fosamprenavir
  • nirmatrelvir
  • nirmatrelvir/ritonavir
  • orlistat
  • rifabutin
  • rifampin
  • selenium
  • sodium zirconium cyclosilicate
  • zinc
• Raltegravir has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Raltegravir?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Raltegravir?”

Cautions

• Risk of immune reconstitution syndrome if used with HAART; during the 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 (. g, Graves’ disease, polymyositis, Guillain-Barré syndrome) are 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 are known to increase the 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 were reported; skin reactions include cases of Stevens-Johnson syndrome, hypersensitivity reaction, and toxic epidermal necrolysis; immediately discontinue treatment of 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
• Drug interactions overview
  • Coadministration of raltegravir with drugs that inhibit UGT1A1 (. g, rifampin) may reduce plasma levels of raltegravir (see Dosage Modifications)
  • Coadministration with other strong inducers (. g, carbamazepine, phenobarbital, phenytoin) of drug-metabolizing enzymes on raltegravir is unknown and therefore not recommended

Pregnancy and Lactation

• There is a pregnancy exposure registry that monitors pregnancy outcomes in women; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1- 800-258-4263
• Available data from APR show no difference in the rate of overall birth defects for raltegravir compared to the background rate for major birth defects of 2.7% in the U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP); the rate of miscarriage is not reported in the APR; the MACDP population is not disease-specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at below 20 weeks gestation
• Lactation
  • The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection
  • No data are available on the presence of raltegravir in human milk, its effects on the breastfed infant, or milk production; when administered to lactating rats, raltegravir was present in milk
  • Owing to the potential for HIV transmission (in HIV-negative infants), developing viral resistance (in HIV- positive infants), and adverse reactions in a breastfed infant, instruct mothers not to breastfeed if they are receiving therapy