Isentress HD

Raltegravir comes as a tablet, a chewable tablet, and as an oral suspension to take by mouth. Raltegravir (Isentress^®) tablets, chewable tablets, and oral suspension are usually taken with or without food twice a day. Raltegravir (Isentress^® HD) tablets are usually taken with or without food once a day. Take raltegravir at the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take raltegravir exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the tablets whole; do not split, chew, or crush them. If you are taking the chewable tablets, you may chew or swallow them whole.

Before you take raltegravir oral suspension for the first time, read the written instructions that come with it that describe how to prepare the medication. Use the dosing syringe provided to measure the amount of medication that your doctor has prescribed. Use the mixture within 30 minutes of preparation and discard any remaining suspension.

Continue to take raltegravir even if you feel well. Do not stop taking raltegravir or your other anti-HIV medications without talking to your doctor. If you stop taking raltegravir or skip doses, your condition may become worse and the virus may become resistant to treatment.

Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient.

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.

Pediatric

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 4 weeks of age and older. Safety and efficacy have not been established in children younger than 4 weeks of age.

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) and over. Safety and efficacy have not been established in children weighing less than 40 kg.

Geriatric

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.

Pregnancy

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.

Interactions with 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 Carbonate, Basic
• Aluminum Hydroxide
• Aluminum Phosphate
• Amprenavir
• Dihydroxyaluminum Aminoacetate
• Dihydroxyaluminum Sodium Carbonate
• Fosamprenavir
• Magaldrate
• Magnesium Carbonate
• Magnesium Hydroxide
• Magnesium Oxide
• Magnesium Trisilicate
• Orlistat

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

Interactions with Food/Tobacco/Alcohol

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.

This section provides information on the proper use of a number of products that contain raltegravir. It may not be specific to Isentress HD. Please read with care.

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 are using the oral suspension:

• Pour the contents of one single-use packet in 5 milliliters (mL) of water and mix.
• 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 at least 40 kilograms (kg)—300 milligrams (mg) (three 100 mg tablets) two times a day.
    • Children weighing 28 to less than 40 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 200 mg (two 100 mg tablets) two times a day.
    • Children weighing 25 to less than 28 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 150 mg (one and a half 100 mg tablets) two times a day.
    • Children 4 weeks of age and older and weighing 20 to less than 25 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 150 mg (one and a half 100 mg tablets) two times a day.
    • Children 4 weeks of age and older and weighing 14 to less than 20 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 100 mg two times a day.
    • Children 4 weeks of age and older and weighing 11 to less than 14 kg—Dose is based on body weight and must be determined by your doctor. 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 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® 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 at least 40 kilograms (kg)—400 mg two times a day.
    • Children weighing at least 25 kilograms (kg) 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 at least 40 kilograms (kg)—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 and weighing 14 less than 20 kilograms (kg)—Dose is based on body weight and must be determined by your doctor. The dose is usually 5 milliliter (mL) (100 mg) two times a day.
    • Children 4 weeks of age and older and weighing 11 less than 14 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 4 mL (80 mg) two times a day.
    • Children 4 weeks of age and older and weighing 8 less than 11 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 3 mL (60 mg) two times a day.
    • Children 4 weeks of age and older and weighing 6 less than 8 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 2 mL (40 mg) two times a day.
    • Children 4 weeks of age and older and weighing 4 less than 6 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 1.5 mL (30 mg) two times a day.
    • Children 4 weeks of age and older and weighing 3 less than 4 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 1 mL (20 mg) two times a day.
    • Children younger than 4 weeks of age and weighing less than 3 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.

US CDC recommendations:
Film-coated tablets: 400 mg orally twice a day
Duration of therapy: 28 days

Comments:
-This drug is recommended as a component of a preferred 3-drug regimen for nonoccupational postexposure prophylaxis of HIV infection; if other alternatives are considered, this drug is recommended as a component in various regimens.
-Prophylaxis should be started as soon as possible, within 72 hours of exposure.
-Current guidelines should be consulted for additional information.

At least 4 weeks of age:
Oral suspension:
3 to less than 4 kg: 20 mg orally twice a day
4 to less than 6 kg: 30 mg orally twice a day
6 to less than 8 kg: 40 mg orally twice a day
8 to less than 11 kg: 60 mg orally twice a day
11 to less than 14 kg: 80 mg orally twice a day
14 to less than 20 kg: 100 mg orally twice a day

Chewable tablets:
11 to less than 14 kg: 75 mg orally twice a day
14 to less than 20 kg: 100 mg orally twice a day
20 to less than 28 kg: 150 mg orally twice a day
28 to less than 40 kg: 200 mg orally twice a day
At least 40 kg: 300 mg orally twice a day

Film-coated tablets:
At least 25 kg: 400 mg orally twice a day

Maximum dose:
-Oral suspension: 100 mg twice a day
-Chewable tablets: 300 mg twice a day

Comments:
-The weight-based dosing recommendation for the oral suspension and chewable tablets is based on about 6 mg/kg/dose twice a day.
-The oral suspension can be used as long as weight is less than 20 kg; either the oral suspension or the chewable tablet formulation can be used for weight between 11 and 20 kg.
-The film-coated tablet is the recommended formulation for patients weighing at least 25 kg; if unable to swallow a tablet, the chewable tablet regimen should be considered.

Use: In combination with other antiretroviral agents, for the treatment of HIV-1 infection

US CDC recommendations for pediatric patients at least 4 weeks of age:
Oral suspension:
3 to less than 4 kg: 20 mg orally twice a day
4 to less than 6 kg: 30 mg orally twice a day
6 to less than 8 kg: 40 mg orally twice a day
8 to less than 11 kg: 60 mg orally twice a day
11 to less than 14 kg: 80 mg orally twice a day
14 to less than 20 kg: 100 mg orally twice a day

Chewable tablets:
11 to less than 14 kg: 75 mg orally twice a day
14 to less than 20 kg: 100 mg orally twice a day
20 to less than 28 kg: 150 mg orally twice a day
28 to less than 40 kg: 200 mg orally twice a day
At least 40 kg: 300 mg orally twice a day

Film-coated tablets:
At least 25 kg: 400 mg orally twice a day

Maximum dose:
-Oral suspension: 100 mg twice a day
-Chewable tablets: 300 mg twice a day

Duration of therapy: 28 days

Comments:
-This drug is recommended as a component of a preferred (or alternative) 3-drug regimen for nonoccupational postexposure prophylaxis of HIV infection; if other alternatives are considered, this drug is recommended as a component in various regimens.
-Prophylaxis should be started as soon as possible, within 72 hours of exposure.
-The oral suspension can be used as long as weight is less than 20 kg; either the oral suspension or the chewable tablet formulation can be used for weight between 11 and 20 kg.
-The film-coated tablet is the recommended formulation for patients weighing at least 25 kg; if unable to swallow a tablet, the chewable tablet regimen should be considered.
-Current guidelines should be consulted for additional information.

No adjustment recommended.

Safety and efficacy have not been established in patients younger than 4 weeks.

Consult WARNINGS section for additional precautions.