AIDS InfoNet Logo
This website is certified by Health On the Net Foundation. Click to verify.
This site complies with the HONcode standard for trustworthy health information:
verify here.

The Henry J. Kaiser Family Foundation
Site of the Week
November 2003

The Health Leader Award 2006
The Health Leader Award 2006

The HOPE Reward

Med411.com Medical Award

HealthAtoZ.com Featured Site Award

BuscaSalud.com

IBS Tales Hope Award

HealingWell.com Editor's Choice Award

Listed in Listed in Treasures of the Internet


AIDS InfoNet Logo.  The AIDS InfoNet - Reliable, Up-to-Date AIDS Treatment Information
International Association of Providers of AIDS Care
Reviewed October 17, 2017

Fact Sheet 465

Raltegravir (Isentress; Isentress HD)


WHAT IS RALTEGRAVIR?
WHO SHOULD TAKE IT?
WHAT ABOUT DRUG RESISTANCE?
HOW IS RALTEGRAVIR TAKEN?
WHAT ARE THE SIDE EFFECTS?
HOW DOES IT REACT WITH OTHER DRUGS?
THE BOTTOM LINE
 


WHAT IS RALTEGRAVIR?

Raltegravir (Isentress) is a drug used for antiviral therapy against HIV. It was formerly known as MK-0518. It is manufactured by Merck.

Raltegravir is the first integrase inhibitor. When HIV infects a cell, it combines its genetic code into the cell's own code. This is shown in fact sheet 400, step 5. Raltegravir blocks this process. When raltegravir blocks integration, HIV infects a cell but cannot make more copies of itself.

 


 WHO SHOULD TAKE IT?

Raltegravir (Isentress) was approved in 2007 as an antiretroviral drug against HIV as part of an antiretroviral regimen. It is approved for use for initial treatment or for people who have had other treatment regimens.

Isentress HD is a once-daily formulation of raltegravir that was approved in 2017 for use as initial treatment or for people already taking initial treatment with twice-daily raltegravir.

While antiretroviral therapy (ART) is recommended for all people living with HIV, independent of your symptoms or CD4 count, you and your health care provider should consider your CD4 cell count, your viral load, any symptoms you are having, and your attitude about taking HIV medications. Fact Sheet 404 has more information about guidelines for the use of antiretroviral medications.

Raltegravir (Isentress) is dosed one pill twice a day; Isentress HD is taken two pills, once-daily. If you take raltegravir with other antiretroviral drugs, you can reduce your viral load and increase your CD4 cells. This should mean staying healthier longer.

 


 WHAT ABOUT DRUG RESISTANCE?

The HIV virus is sloppy when it makes copies of its genetic code (RNA). Many new copies of HIV are mutations: they are slightly different from the original virus. Some mutations can continue to multiply even when you are taking an antiretroviral drug. When this happens, the drug will stop working. This is called "developing resistance" to the drug. See Fact Sheet 126 for more information on resistance.

Raltegravir has shown activity against HIV that already has resistance to several other HIV medications.

With combination therapy (taking more than one antiretroviral drug at the same time), HIV mutates much more slowly. Resistance takes longer to develop. It is very important to take antiretroviral medications according to instructions, on schedule, and not to skip or reduce doses.

Sometimes, if you develop resistance to one drug, you will also have resistance to other antiretroviral drugs. This is called "cross-resistance". Resistance to raltegravir is uncommon. Because Raltegravir is an integrase inhibitor, resistant virus may be resistant to other integrase inhibitors, but not drug types..

 


 HOW IS RALTEGRAVIR TAKEN?

Raltegravir may be taken with or without food. The adult dosage of Isentress is one 400 mg tablet twice daily.  The dose of Isentress HD is two 600 mg tablets, once daily.

Raltegravir can be used by children who are 4 weeks and older. Dosage for children less than 12 years old is based on their weight and is available as chewable tablets or an oral suspension.

 


WHAT ARE THE SIDE EFFECTS?

Raltegravir is usually very well tolerated. In studies, the most common side effects in people taking raltegravir were diarrhea, nausea, and headache.  Reports from people using raltegravir also include rash and depression. In rare cases, skin rash can be severe and life-threatening. Contact your health care provider immediately if you develop a serious rash while taking raltegravir.

Elevations in creatine kinase, a lab test of muscle injury, have been seen in people taking raltegravir. There have been reports of muscle injury.

 


 HOW DOES IT REACT WITH OTHER DRUGS?

Raltegravir has been studied to see if it interacts with other drugs. Rifampin, used to treat tuberculosis (see fact sheet 518) decreases blood levels of raltegravir. A higher dose of raltegravir must be used.

Aluminum- or magnesium containing antacids interfere with the absorption of raltegravir. This effect is not changed by separating the dose of raltegravir. It is recommended that you do not take aluminum or magnesium antacids if you take raltegravir.  Isentress HD should not be taken with calcium carbonate or rifampin.

Raltegravir has not been studied with all medicines, over-the-counter drugs or vitamin or herbal supplements. Be sure your doctor knows about all medications and supplements that you are taking.

 


 THE BOTTOM LINE

Raltegravir is the first integrase inhibitor. It stops HIV from inserting its genetic code into an infected cell. This prevents the virus from making new copies of HIV. 

Raltegravir is one of several medications recommended for use for initial treatment of HIV. It is also approved for use in people who have earlier treatment experience.

 


 

 


Back to Fact Sheet Categories



International Association of Providers of AIDS Care

 

The AIDS InfoNet is a project of the International Association of Providers of AIDS Care.
[email protected]

 

United States National Library of Medicine

Partially funded by the National Library of Medicine



Search Our Site
Newest Fact Sheets
Print This Fact Sheet
You can print this fact sheet on a single page in Microsoft Word (.doc) format or Adobe Acrobat (.pdf) format. Click on the links below to open the document in your browser and then print it.
 Adobe Acrobat PDF
 Microsoft Word

You can print directly from your browser using the link below. The printout will probably go onto a second page.
 Print Version (Web)

Monthly E-mail Updates

The InfoNet updates its Fact Sheets frequently. A listing of each month's changes is posted to several e-mail lists.

If you would like to receive this monthly update by personal e-mail, please click on the SUBMIT button.

SUBMIT