Pronunciation:

ral-TEG-ra-vir

Brand Names:

• Isentress
• Isentress HD

Dosage Forms:

• Tablet
• Powder for Suspension
• Tablet, Chewable

Classifications:

Therapeutic—

Antiretroviral Agent

Pharmacologic—

Integrase Inhibitor

Uses of This Medicine:

Raltegravir is used together with other medicines for the treatment of the infection caused by human immunodeficiency virus (HIV). HIV is the virus that causes acquired immune deficiency syndrome (AIDS). This medicine is usually given to patients who have already received HIV medicines in the past.

Raltegravir will not cure or prevent HIV infection or AIDS. It helps keep HIV from reproducing and appears to slow down the destruction of the immune system. This may help delay problems that are usually related to AIDS or HIV disease from occurring. Raltegravir will not keep you from spreading HIV to other people. People who receive this medicine may continue to have other problems usually related to AIDS or HIV disease.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of Isentress® film-coated tablets, chewable tablets, or oral suspension in children weighing 2 kilograms (kg) or more. Safety and efficacy have not been established in children weighing less than 2 kg.

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of Isentress HD® film-coated tablets in children weighing 40 kilograms (kg) or more. Safety and efficacy have not been established in children weighing less than 40 kg.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of raltegravir in the elderly. However, elderly patients are more likely to have age-related kidney, liver, or heart problems, which may require caution and an adjustment in the dose for patients receiving raltegravir.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aluminum
• Aluminum Carbonate, Basic
• Aluminum Hydroxide
• Aluminum Phosphate
• Amprenavir
• Cabotegravir
• Calcium
• Dihydroxyaluminum Aminoacetate
• Dihydroxyaluminum Sodium Carbonate
• Fosamprenavir
• Iron
• Levoketoconazole
• Magaldrate
• Magnesium
• Magnesium Carbonate
• Magnesium Hydroxide
• Magnesium Oxide
• Magnesium Trisilicate
• Methotrexate
• Orlistat
• Sucralfate
• Zinc

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Etravirine
• Omeprazole
• Rifampin

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Liver disease, severe—Use with caution. This medicine has not been studied in patients with severe liver problems.

• Myopathy (muscle weakness), history of or
• Rhabdomyolysis (muscle problem that could lead to kidney problem), history of—Use with caution. May make these conditions worse.

• Phenylketonuria (PKU)—The chewable tablet contains phenylalanine, which can make this condition worse.

Proper Use of This Medicine:

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. Also, do not change the dose or stop using this medicine without checking first with your doctor. When your supply of this medicine is running low, contact your doctor or pharmacist ahead of time. Do not allow yourself to run out of this medicine.

This medicine comes with a patient information leaflet. Read and follow the instructions carefully. Read it again each time you refill your prescription in case there is new information. Ask your doctor if you have any questions.

Keep using raltegravir for the full time of treatment, even if you begin to feel better. It is also important to take this medicine together with other medicines for HIV. Be sure to take all of the medicines your doctor ordered at the right times.

You may take this medicine with or without food.

You may chew or swallow the chewable tablets whole. However, the film-coated tablets must be swallowed whole.

If you have trouble chewing the 25-mg chewable tablet:

• Place the tablet in a clean cup and add 5 milliliters (ml) of liquid (including water, juice, or breast milk).
• Use a spoon to crush any remaining tablet and take the medicine right away.
• You may add another 5 ml of liquid if any part of the medicine is left in the cup, mix and drink right away.

If you are using the oral suspension:

• Pour the contents of one single-use packet in 10 milliliters (mL) of water and mix by swirling the mixing cup carefully and slowly in a circle for 45 seconds. Do not shake the cup.
• Use the dosing syringe that comes with the package to measure the right dose.
• The dose should be taken within 30 minutes after mixing the suspension.
• Throw away any remaining suspension.

Do not substitute the chewable tablets or oral suspension with the film-coated tablets. Ask your doctor or pharmacist if you have any questions.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For treatment of HIV infection (patient already had HIV treatment):
  • For oral dosage form (Isentress® film-coated tablets):
    • Adults—400 milligrams (mg) two times a day. For patients who are also taking rifampin, the dose is usually 800 mg (two 400 mg tablets) two times a day.
    • Children—Use and dose must be determined by your doctor.
• For treatment of HIV infection (patient never had HIV treatment):
  • For oral dosage form (chewable tablets):
    • Children weighing 40 kilograms (kg) or more—300 milligrams (mg) (three 100 mg tablets) two times a day.
    • Children weighing less than 40 kg—Dose is based on body weight and must be determined by your doctor:
      • Weighing 28 to less than 40 kg—The dose is usually 200 mg (two 100 mg tablets) two times a day.
      • Weighing 25 to less than 28 kg—The dose is usually 150 mg (one and a half 100 mg tablets) two times a day.
    • Children 4 weeks of age and older—Dose is based on body weight and must be determined by your doctor:
      • Weighing 20 to less than 25 kg—The dose is usually 150 mg (one and a half 100 mg tablets) two times a day.
      • Weighing 14 to less than 20 kg—The dose is usually 100 mg two times a day.
      • Weighing 10 to less than 14 kg—The dose is usually 75 mg (three 25 mg tablets) two times a day.
      • Children 4 weeks of age and older and weighing less than 110 kg—Use of oral suspension is recommended.
    • Children younger than 4 weeks of age—Use and dose must be determined by your doctor.
  • For oral dosage form (Isentress® film-coated tablets):
    • Adults—400 milligrams (mg) two times a day. For patients who are also taking rifampin, the dose is usually 800 mg (two 400 mg tablets) two times a day.
    • Children weighing 40 kilograms (kg) or more—400 mg two times a day.
    • Children weighing 25 kg or more and can swallow the tablet—400 mg two times a day.
    • Children weighing less than 25 kg and unable to swallow the tablet—Use of chewable tablets are recommended.
    • Children 4 weeks of age and older and weighing less than 11 kg—Use of oral suspension is recommended.
    • Children younger than 4 weeks of age—Use and dose must be determined by your doctor.
  • For oral dosage form (Isentress HD® film-coated tablets):
    • Adults—1200 milligrams (mg) (two 600 mg tablets) once a day.
    • Children weighing 40 kilograms (kg) or more—1200 mg (two 600 mg tablets) once a day.
    • Children weighing less than 40 kg—Use and dose must be determined by your doctor.
  • For oral dosage form (suspension):
    • Children 4 weeks of age and older—Dose is based on body weight and must be determined by your doctor:
      • Weighing 14 to less than 20 kilograms (kg)—The dose is usually 10 milliliters (mL) (100 mg) two times a day.
      • Weighing 10 to less than 14 kg—The dose is usually 8 mL (80 mg) two times a day.
      • Weighing 8 to less than 10 kg—The dose is usually 6 mL (60 mg) two times a day.
      • Weighing 6 to less than 8 kg—The dose is usually 4 mL (40 mg) two times a day.
      • Weighing 4 to less than 6 kg—The dose is usually 3 mL (30 mg) two times a day.
      • Weighing 3 to less than 4 kg—The dose is usually 2.5 mL (25 mg) two times a day.
    • Children 1 to 4 weeks of age—Dose is based on body weight and must be determined by your doctor:
      • Weighing 4 to less than 5 kg—The dose is usually 1.5 mL (15 mg) two times a day.
      • Weighing 3 to less than 4 kg—The dose is usually 1 mL (10 mg) two times a day.
      • Weighing 2 to less than 3 kg—The dose is usually 0.8 mL (8 mg) two times a day.
    • Children younger than 1 week of age—Dose is based on body weight and must be determined by your doctor:
      • Weighing 4 to less than 5 kg—The dose is usually 0.7 mL (7 mg) once a day.
      • Weighing 3 to less than 4 kg—The dose is usually 0.5 mL (5 mg) once a day.
      • Weighing 2 to less than 3 kg—The dose is usually 0.4 mL (4 mg) once a day.
    • Children weighing less than 2 kg—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Store the chewable tablets and film-coated tablets in its original package with the bottle tightly closed. Do not open the foil packet of the powder for suspension until you are ready to use it.

Precautions While Using This Medicine:

It is very important that your doctor check your or your child's progress at regular visits to make sure this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Serious skin and allergic reactions (eg, Stevens-Johnson Syndrome, toxic epidermal necrosis) can occur with this medicine. These could be life-threatening and require immediate medical attention. Check with your doctor right away if you have a severe rash, blistering, peeling, or loosening skin, fever or chills, muscle or joint pain, sores or ulcers on the skin, swelling of the face, lips, tongue, or throat, unusual tiredness or weakness, or yellow eyes or skin while you or your child are using this medicine.

Your immune system may get stronger when you start taking HIV medicines. Tell your doctor right away if you or your child notice any changes in your health. Sometimes the immune system will start to fight infections that were hidden in your body, such as pneumonia, herpes, or tuberculosis. Autoimmune disorders (eg, Graves' disease, polymyositis, Guillain-Barré syndrome) may also occur.

Tell your doctor right away if you or your child have unexplained muscle pain, tenderness, or weakness, especially if you also have unusual tiredness or a fever. These could be symptoms of a serious muscle problem called myopathy.

Check with your doctor right away if you or your child have dark urine, fever, muscle cramps or spasms, muscle pain or stiffness, or unusual tiredness or weakness. These could be symptoms of a serious muscle problem called rhabdomyolysis, which can cause kidney problems.

This medicine will not keep you from giving HIV to your partner during sex. Make sure you understand this and practice safe sex, even if your partner also has HIV, by using a latex condom or other barrier method. This medicine will also not keep you from giving HIV to other people if they are exposed to your blood. Do not re-use or share needles with anyone.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common or rare

Blood in the urine

burning or stinging of the skin

dark urine

decreased frequency or amount of urine

fast heartbeat

fever

hoarseness

increased thirst

irritation

joint pain, stiffness, or swelling

light-colored stools

loss of appetite

lower back or side pain

nausea

pain in the groin or genitals

painful blisters on the trunk of the body

painful cold sores or blisters on the lips, nose, eyes, or genitals

rash, hives, or itching

redness of the skin

sharp back pain just below the ribs

swelling of the eyelids, face, lips, hands, lower legs, or feet

tightness in the chest

trouble breathing or swallowing

unusual tiredness or weakness

upper right stomach pain

vomiting

weight gain

yellow eyes and skin

Incidence not known

Black, tarry stools

bleeding gums

headache

muscle cramps, spasms, pain, or stiffness

pinpoint red spots on the skin

stomach pain, continuing

unusual bleeding or bruising

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

Dizziness

trouble sleeping

Less common or rare

Belching

depression

heartburn

indigestion

lack or loss of strength

stomach discomfort, upset, or tenderness

thoughts of killing oneself or changes in behavior

Incidence not known

Delusions of persecution, mistrust, suspiciousness, or combativeness

diarrhea

fear or nervousness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.