How does this medication work? What will it do for me?

Raltegravir belongs to the class of medications called antiretrovirals. It is used in combination with other antiretroviral medications to treat human immunodeficiency virus (HIV) infection when other antiretroviral medications have not kept the virus under control.

It works by blocking an enzyme, HIV integrase, which the virus needs to make more virus. When used with other antiretroviral medications, raltegravir helps the immune system by reducing the amount of HIV in the blood and increasing the number of CD4 or T-cells.

This medication does not cure HIV infection or AIDS and does not reduce the risk of passing HIV to others through sexual contact or blood contamination.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. As well, some forms of this medication may not be used for all of the conditions discussed here. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Each pink, oval-shaped, film-coated tablet, marked with "227" on one side contains 434.4 mg of raltegravir potassium (as salt) equivalent to 400 mg of raltegravir. Nonmedicinal ingredients: microcrystalline cellulose, lactose monohydrate, calcium phosphate dibasic anhydrous, hypromellose 2208, poloaxamer 407 (contains butylated hydroxytoluene as antioxidant), sodium stearyl fumarate, magnesium stearate, film-coating: polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350, talc, red iron oxide, and black iron oxide.

How should I use this medication?

The usual dose of raltegravir is 400 mg twice daily, taken with or without food.

Many things can affect the dose of a medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. The amount of HIV virus in your blood can increase if this medication is stopped for even a short period of time. Taking this medication exactly as prescribed will also decrease the chance of drug resistance (i.e., the medication stops working to fight HIV).

If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Raltegravir should not be taken by anyone who is allergic to raltegravir or to any of the ingredients of the medication.

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent. The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • abdominal pain
  • back pain
  • constipation
  • cough
  • decreased appetite
  • diarrhea
  • difficulty sleeping
  • dizziness
  • fatigue
  • fever
  • gas and bloating
  • headache
  • heartburn
  • muscle aches
  • nausea
  • rash
  • upset stomach
  • vomiting

Although most of these side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • increased blood pressure
  • persistent fatigue
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • signs of infection (e.g., fever, chills, sore throat, mouth ulcers, cough)
  • signs of liver problems (e.g., nausea, vomiting, loss of appetite, feeling unwell, fever, itching, yellowing of the skin or whites of eyes, dark urine)
  • unexplained muscle weakness, tenderness, or pain

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • severe chest pain
  • signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
  • signs of a severe skin reaction (e.g., blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort)
  • signs of kidney problems (e.g., nausea, loss of appetite, weakness, passing little or no urine, shortness of breath)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin taking a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should take this medication.

Immune reconstitution syndrome: This medication may cause immune reconstitution syndrome, where signs and symptoms of inflammation from previous infections appear. These symptoms occur soon after starting anti-HIV medication and can vary. They are thought to occur as a result of the immune system improving and being able to fight infections (e.g., pneumonia, herpes, or tuberculosis) that have been present without symptoms . Report any new symptoms to your doctor immediately.

Muscle pain: Occasionally, raltegravir causes breakdown of muscle tissues, which can be fatal. Report any symptoms of severe, unexplained muscle pain to your doctor as soon as possible.

Pregnancy: There are no studies evaluating the use of this medication by pregnant women. This medication is not recommended during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if this medication passes into breast milk. However, breast-feeding is not recommended for HIV-positive women since the virus can be passsed to the baby through breast milk.

Children: The safety and effectiveness of using this medication have not been established for children under 16 years old.

What other drugs could interact with this medication?

There may be an interaction between raltegravir and any of the following:

  • rifampin

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.