Drug Database: Raltegravir

What is raltegravir?

Raltegravir (brand names: Isentress and Isentress HD) is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV infection in adults and children. One form of raltegravir, Isentress, is approved for adults and children weighing at least 4 lb and 4 oz (2 kg). Another form of raltegravir, Isentress HD, is approved for adults and children weighing at least 88 lb (40 kg). Raltegravir is always used in combination with other HIV medicines.

For more information on the use of raltegravir in people with HIV, please refer to the Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV and the Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection.

Raltegravir may also be used to prevent perinatal transmission of HIV. When used to prevent perinatal transmission, raltegravir, along with other HIV medicines, may be given to infants after birth. For more information, please refer to the Recommendations for the Use of Antiretroviral Drugs During Pregnancy and Interventions to Reduce Perinatal HIV Transmission in the United States.

HIV medicines cannot cure HIV/AIDS, but taking HIV medicines every day helps people with HIV live longer, healthier lives. HIV medicines also reduce the risk of HIV transmission. If you are taking HIV medicines, do not cut down on, skip, or stop taking them unless your health care provider tells you to.

What should I tell my health care provider before taking raltegravir?

Before taking raltegravir, tell your health care provider:

• If you are allergic to raltegravir or any other medicines.
• If you have liver problems.
• If you have a history of a muscle disorder called rhabdomyolysis or myopathy.
• If you have increased levels of creatine kinase (an enzyme found mainly in the heart, brain, and skeletal muscle) in your blood.
• If you have phenylketonuria (PKU). The artificial sweetener (aspartame) in raltegravir chewable tablets contains phenylalanine. Phenylalanine may be harmful to people with PKU.
• If you are on kidney dialysis treatment.
• If you have any other medical conditions.
• If you are pregnant or plan to become pregnant. Talk to your health care provider about the risks and benefits of taking raltegravir during pregnancy. For more information on the use of raltegravir during pregnancy, please refer to the Recommendations for the Use of Antiretroviral Drugs During Pregnancy and Interventions to Reduce Perinatal HIV Transmission in the United States.
• If you are breast/chestfeeding or plan to breast/chestfeed. For people with HIV in the United States, the Guideline recommends speaking with your health care provider to discuss options for feeding your baby. People with suppressed viral load have a less than 1% chance of transmitting HIV to their baby via their own milk.
• If you are using hormone-based birth control (such as pills, implants, or vaginal rings). For more information about using birth control and HIV medicines at the same time, view the HIVinfo HIV and Birth Control infographic.
• About other prescription and nonprescription medicines, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Raltegravir may affect the way other medicines or products work, and other medicines or products may affect how raltegravir works. Taking raltegravir together with certain medicines or products may cause serious side effects.

How should I take raltegravir?

Raltegravir comes in the following forms and strengths:

• 400-mg and 600-mg film-coated tablets
• 25-mg and 100-mg chewable tablets
• 100-mg single-use packets of granules for oral suspension

Take raltegravir according to your health care provider’s instructions. Do not miss a dose of raltegravir, and do not change your dose or stop taking raltegravir without first talking with your health care provider.

Take raltegravir by mouth, with or without food. If you are taking any other medicines or supplements, including antacids, carefully follow instructions on how to take them with raltegravir. Antacids containing aluminum and/or magnesium should NOT be taken with any form of raltegravir. Antacids containing calcium carbonate should NOT be used with raltegravir HD (600-mg film-coated tablets).

Always swallow raltegravir film-coated tablets whole.

Raltegravir chewable tablets may be chewed or swallowed whole. If your child has trouble chewing the 25-mg chewable tablet, the tablet may be crushed as follows:

• Place the chewable tablet in a small, clean cup. For each tablet, add about 1 teaspoonful of liquid (such as water, juice, or breast milk) to the cup.
• The chewable tablet(s) will fall apart in the liquid within 2 minutes. Use a spoon to crush any remaining pieces of the tablet(s). Give your child the entire mixture to swallow right away.
• If any of the mixture is left in the cup, add another teaspoonful of liquid to the cup, swirl, and give to the child to swallow right away.

Raltegravir for oral suspension must be mixed with water before use and given within 30 minutes of mixing. Raltegravir for oral suspension comes in a kit that contains the packets of raltegravir and reusable syringes and cups needed to mix and give the medicine. See the "Instructions for Use" that come with the kit for information about the correct way to mix and give a dose of raltegravir for oral suspension. If you have questions about how to mix or give raltegravir for oral suspension, talk to your health care provider or pharmacist.

Do not switch between the film-coated tablets, the chewable tablets, or the oral suspension without talking with your health care provider first.

Always take raltegravir in combination with other HIV medicines.

If you have taken too much raltegravir, contact your health care provider or local poison control center (1-800-222-1222 or online) right away, or go to the nearest hospital emergency room.

For more information on how to take raltegravir, see the FDA drug label.

What should I do if I forget a dose?

If you miss a dose of raltegravir, take the missed dose as soon as you remember it. But if it is almost time for your next dose, skip the missed dose and just take your next dose at the regular time. Do not take two doses at the same time to make up for a missed dose.

What side effects can raltegravir cause?

Raltegravir may cause side effects. Some side effects of raltegravir can be serious as noted above. Many side effects from HIV medicines, such as nausea or occasional dizziness, are manageable. See the HIVinfo fact sheet on HIV Medicines and Side Effects for more information.

Other possible side effects of raltegravir include:

• Changes in your immune system (called immune reconstitution inflammatory syndrome or IRIS). IRIS is a condition that sometimes occurs when the immune system begins to recover after treatment with an HIV medicine. As the immune system gets stronger, it may have an increased response to a previously hidden infection.
• Unexplained muscle pain, tenderness, or weakness. This may be a sign of a rare but serious muscle problem that can lead to kidney problems.

Tell your health care provider if you have any side effect that bothers you or that does not go away.

These are not all the possible side effects of raltegravir. To learn more about possible side effects of raltegravir, read the drug label or package insert or talk to your health care provider or pharmacist.

You can report side effects to FDA at 1-800-FDA-1088 (1-800-332-1088) or online.

How should raltegravir be stored?

• Store raltegravir film-coated tablets, chewable tablets, and granules for oral suspension at room temperature, 68°F to 77°F (20°C to 25°C).
• Keep raltegravir film-coated and chewable tablets in the container that they came in and keep the container tightly closed. If the container has a small packet of drying agent (called a desiccant), do not remove it. The desiccant protects the medicine from moisture.
• Keep raltegravir for oral suspension in the foil packets it came in. Do not open the packets until ready for use.
• Do not use raltegravir if the original seal over the container opening is broken or missing.
• Throw away raltegravir that is no longer needed or expired (out of date). Follow FDA guidelines on how to safely dispose of unused medicine.
• Keep raltegravir and all medicines out of reach of children.

Where can I find more information about raltegravir?

• For more information on the use of raltegravir in people with HIV, please refer to the Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV and the Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection.
• This Patient Version drug summary is based on the following FDA label(s): Tablet (chewable), tablet (film coated), granule for oral suspension. The Patient Package Insert and Instructions For Use include information for people taking raltegravir.
• The American Hospital Formulary Service (AHFS) Patient Medication Information for raltegravir available from MedlinePlus.
• Raltegravir-related research studies, from ClinicalTrials.gov. (The ClinicalTrials.gov search can be modified so that you can get results that better match your interests.)
• A list of FDA-approved HIV medicines, from HIVinfo.