What is raltegravir, and how does it work (mechanism of action)?
- 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
What are the uses for raltegravir?
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.
What are the side effects of raltegravir?
The most common side effects of raltegravir include:
Other potential side effects of raltegravir include:
- Paranoia
- Blood disorders
- Kidney failure
- Muscle pain (myopathy)
- Rhabdomyolysis (muscle destruction)
- Increased bilirubin
- Increased levels of liver enzymes
- Increased blood glucose
-
Suicidal thoughts or actions
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.
What is the dosage for raltegravir?
- 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.
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Which drugs or supplements interact with raltegravir?
- 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.
Is raltegravir safe to take if I’m pregnant or breastfeeding?
- 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 else should I know about raltegravir?
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.