raltegravir (Isentress)

• Raltegravir (Isentress) is an antiretroviral medicine approved for the treatment of human immunodeficiency virus (HIV) infection. Raltegravir is an integrase inhibitor similar to elvitegravir (Vitekta) and dolutegravir (Tivicay). Raltegravir slows the spread of HIV infection by blocking the HIV integrase enzyme required for virus multiplication. To improve the chance of fighting HIV-1 infection, raltegravir must be taken with other HIV medicines. Although raltegravir does not cure HIV or AIDS, continuous HIV treatment with raltegravir can help patients control the infection and decrease their risk of acquiring HIV-related illnesses. Raltegravir helps to improve the immune system by increasing the number of white blood cells called CD4+ (T) cells, and consequently reduce the risk of death or getting opportunistic infections that can happen when the immune system is weak.
• Raltegravir was initially approved by the FDA in October 2007.

What brand names are available for raltegravir?

Isentress

Is raltegravir available as a generic drug?

No

Do I need a prescription for raltegravir?

Yes

Raltegravir is a prescription HIV medicine used with other antiretroviral medicines to treat human immunodeficiency virus-1 (HIV-1) infection in patients 4 weeks or age and older. Raltegravir does not cure the HIV-1 infection or AIDS. It works to reduce the viral load which is the amount of HIV virus in the blood.

The most common side effects of raltegravir include:

• Trouble sleeping insomnia)
• Headache
• Dizziness
• Nausea
• Tiredness

Other potential side effects of raltegravir include:

• Depression
• Hepatitis (a type of viral infection of the liver)
• Paranoia
• Blood disorders
• Kidney failure
• Kidney stones
• Indigestion or stomach pain
• Muscle pain (myopathy)
• Rhabdomyolysis (muscle destruction)
• Increased bilirubin
• Increased levels of liver enzymes
• Increased blood glucose
• Vomiting
• Suicidal thoughts or actions
• Weakness

Some patients taking raltegravir experience serious skin and allergic reactions. These reactions can be severe or life-threatening if not treated promptly. Patients who develop any type of skin rash with other symptoms should call their doctor right away.

• Raltegravir can be taken with or without food. The different formulations of raltegravir do not deliver the same amount of medicine in the body. Therefore, raltegravir chewable tablets or oral suspension should not be substituted for the film-coated tablets.
• If taken with rifampin the recommended dosage of raltegravir is 800 mg twice a day in adults.
• The maximum dose of chewable tablets is 300 mg twice daily and 100 mg twice daily for the oral suspension.
• Adults: The recommended dosage for the treatment of HIV-1 infection is one 400 mg film coated tablet taken by mouth twice day.
• Pediatrics: Dosing is children and adolescents are weight based. For patients weighing at least 25 kg, administer one 400 mg film-coated tablet by mouth twice daily. Patients unable to swallow tablets may be prescribed chewable tablets. The weight based dosing recommendation for the chewable tablets is 6 mg/kg/dose twice daily.
• Doctors can use specific weight based dosing recommendations provided by the manufacturer for patients who are at least 4 weeks of age and weight at least 3 kg to less than 25 kg.

• Raltegravir is primarily broken down by UGT1A1 enzymes. Medicines which alter the activity of these enzymes may affect blood levels of raltegravir. For example, rifampin (Rimactane) is known to increase the activity of UGT1A1 enzymes, and consequently reduces the blood levels of raltegravir.
• Patients should avoid taking raltegravir with aluminum or magnesium containing antacids which may reduce blood levels of raltegravir.

• Use of raltegravir in pregnant women has not been adequately evaluated. Due to the lack of conclusive safety data, raltegravir should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. Raltegravir is classified as FDA pregnancy risk category C.
• Breastfeeding is not recommended while taking raltegravir. To avoid transmitting the HIV-1 virus to the nursing infant, it is not recommended that HIV-1-infected mothers breastfeed their infants. It is not known if raltegravir is excreted into human milk.

What preparations of raltegravir are available?

• Film coated oral tablets: 400 mg
• Chewable oral tablets: 25 mg and 100 mg
• Granules for oral suspension: single use packet of 100 mg

How should I keep raltegravir stored?

• Raltegravir should be stored at room temperature between 20 C to 25 C (68 F to 77 F).
• For best protection the chewable tablets and granules for oral suspension should be stored in the original container.