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Integrase Inhibitors for HIV: What to Know

Medically Reviewed by Laura J. Martin, MD on April 15, 2022

People with human immunodeficiency virus (HIV) are living longer thanks to treatments like antiretroviral therapy, or ART. That’s a medication that lowers the amount of HIV in your body.

One class of ARTs, integrase inhibitors, has become a standard HIV treatment. Research shows they work well to keep the disease in check. Here’s what you need to know.

What are integrase inhibitors?

Integrase inhibitors are part of a class of drugs called antiretrovirals. The FDA approved the first integrase inhibitor in 2007. Today, there are five available to people living with HIV:

Integrase inhibitors are also part of some HIV drug combinations. These include two or more HIV medications from one drug class or multiple classes.

Integrase inhibitors come in pill form, which you swallow or chew. They also come as granules that dissolve in water. Depending on the specific medication, you’ll take an integrase inhibitor once or twice a day. Cabotegravir is also available as a shot you get once-a-month.

Why do doctors prescribe integrase inhibitors?

Doctors prescribe these drugs to treat HIV in some adults and children living with the condition. You may take an integrase inhibitor alone or with another HIV medication. Integrase inhibitors don’t cure HIV, but they lower your odds of the illness progressing to AIDS. Integrase inhibitors, along with a safe sex routine, can help stop the spread of HIV.

How do integrase inhibitors work?

HIV is a virus that attacks your body’s immune system, specifically white blood cells known as CD4 cells or T cells. Normally, these cells work together with your immune system to protect it from viruses and bacteria.

Once HIV invades your cells, it takes control of them by making integrase, a type of enzyme. When this happens, T cell DNA combines with the virus’s DNA, allowing HIV to take over. The virus then spreads by reproducing itself and taking control of other cells. Your T cells lose the power to communicate with your immune system to ward off infection.

Integrase inhibitors block HIV from making integrase, which stops the virus from copying itself and spreading to more cells.

How well do integrase inhibitors work?

Many people living with HIV take integrase inhibitors because they work well to treat the illness with few side effects. These drugs also continue to fight the virus over time, especially newer integrase inhibitors such as dolutegravir, bictegravir, and cabotegravir. Older integrase inhibitors, raltegravir and elvitegravir, have shown some resistance to HIV.

Which drugs interact with integrase inhibitors?

Some medicines you take for other health problems may interact with integrase inhibitors. The combination could be dangerous, so you’ll need to stop taking a certain medicine, change to a different one, or adjust your dosage. Tell your doctor if you take medication or supplements (especially St. John’s wort) to manage:

Who can take integrase inhibitors and who should avoid them?

Children. Depending on their age and weight, children with HIV can take integrase inhibitors. Some drugmakers suggest standard adult doses for children, while others tailor their dosage recommendations.

Older adults. People in this age group tend to have a higher chance of having liver, kidney, and heart problems.

Pregnant women. Health experts say pregnant women can take ART, including integrase inhibitors.

What are the possible side effects of integrase inhibitors?

Since integrase inhibitors fight HIV instead of infected cells, this type of drug comes with fewer side effects than other HIV medicines. Still, you could have these unwanted reactions while taking an integrase inhibitor:

  • Loose, watery stools
  • A sick feeling in your stomach
  • Extreme tiredness
  • Headache
  • Trouble falling or staying asleep
  • Problems concentrating
  • Anxiety
  • Mood changes
  • A change in dreams
  • Depression
  • Pain
  • Lightheadedness
  • Weight gain
  • Higher creatinine levels (a level that’s too high could mean kidney failure)

Less commonly, people taking integrase inhibitors have serious skin reactions and inflammation.

Some side effects from integrase inhibitors will last a few weeks, then go away. Tell your doctor if your side effects last longer or make you uncomfortable. But don’t stop taking it abruptly.

Show Sources

SOURCES:

IAPAC: “How Integrase Inhibitors Work,” “dolutegravir (Tivicay, Tivicay PD),” “raltegravir (Isentress, Isentress HD),” “elvitegravir (Vitekta),” “cabotegravir (Vocabria).”

Current Treatment Options in Infectious Diseases: “Update on Adverse Effects of HIV Integrase Inhibitors.”

Cleveland Clinic: “Creatinine Clearance Test.”

HIV.gov: “Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents Living with HIV.”

MedlinePlus: “Dolutegravir.”

Drugs: “HIV-1 Integrase Inhibitors: A Comparative Review of Efficacy and Safety.”

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