Raltegravir
Raltegravir is an antiretroviral medicine in the HIV integrase inhibitor class. Raltegravir is used for HIV-1 infection in adults and HIV-1 infection in pediatric patients.
Pronunciation: Information unavailable in provided research notes.
- Generic name
- raltegravir
- Brand names
- ISENTRESS, ISENTRESS HD
- Drug class
- HIV integrase inhibitor
- Form
- Film-coated tablet (400 mg, 600 mg), chewable tablet (25 mg, 100 mg), granules for oral suspension (100 mg per packet)
- Route
- Oral
- Legal status
- Prescription-only medicine
Availability and supply rules vary by country
Trade names by country: United States
Australia: · Full directory
What raltegravir is and how it works
Raltegravir is an antiretroviral medicine in the HIV integrase inhibitor class. It works by decreasing the amount of HIV in the blood. Raltegravir is used in combination with other antiretrovirals to treat human immunodeficiency virus (HIV-1) infection in eligible adults and certain pediatric patients. (1) (2) (3)
Raltegravir does not cure HIV. Taking raltegravir and making lifestyle changes may decrease the risk of transmitting HIV to others. The exact product, dose, and schedule depend on age, weight, treatment history, and concomitant medicines.
Mechanism of action: how raltegravir works
Raltegravir is an HIV integrase inhibitor. It decreases the amount of HIV in the blood by blocking a viral enzyme necessary for replication. (1) (2)
What is Raltegravir used for?
HIV-1 infection in adults
Raltegravir, as ISENTRESS or ISENTRESS HD, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adult patients. The product choice and dosing regimen (once or twice daily) depend on whether the patient is treatment-naïve, virologically suppressed on an initial raltegravir regimen, or treatment-experienced. (2) (3)
HIV-1 infection in pediatric patients
ISENTRESS is indicated in combination with other antiretroviral agents for pediatric patients weighing at least 2 kg. ISENTRESS HD is indicated for pediatric patients weighing at least 40 kg. Specific age and weight criteria, product selection, and dosing are described in the prescribing information. (2) (3)
Before taking raltegravir
Do not take / not appropriate for
- No contraindications are listed in the US prescribing information. Do not take raltegravir if you have a known allergy to the medicine or any of its components unless the responsible specialist determines otherwise. (all products) (1) (2)
Tell your clinician about
- If you have ever had an allergic reaction to raltegravir, any part of this drug, or any other drugs, foods or substances.
- If you are being treated with dialysis or have a history of hepatitis, muscular disease, swelling of the muscles, or rhabdomyolysis.
- If you have phenylketonuria (PKU), because the chewable tablets contain aspartame.
- If you are pregnant, plan to become pregnant, or are breastfeeding.
- All prescription and non-prescription medicines, vitamins, and herbal products you take, especially antacids containing aluminum or magnesium.
Raltegravir dosage and how to take it
- Raltegravir is taken by mouth, with or without food, exactly as directed by your doctor.
- How often you take it depends on the form: the 400 mg tablet, chewable tablets, and granules for oral suspension are taken twice a day, while the HD tablets are taken once a day (the once-daily HD dose for adults and eligible children is 1,200 mg, taken as two 600 mg tablets). Take raltegravir at the same time(s) every day.
- The 400 mg and 600 mg film-coated tablets must be swallowed whole; do not split, chew, or crush them.
- If you are prescribed the chewable tablets, you may chew them or swallow them whole. For children who have difficulty chewing, the 25 mg chewable tablet can be crushed: place it in a clean cup with about 5 mL of liquid, wait up to 2 minutes for the tablet to absorb the liquid and fall apart, crush any remaining pieces, and administer immediately. If any of the medicine is left in the cup, add another teaspoonful (5 mL) of liquid, swirl, and take it right away so the full dose is given.
- If you are prescribed granules for oral suspension, read the manufacturer’s instructions. Empty the packet into the provided mixing cup with 10 mL of water. Gently swirl for 45 seconds; do not shake. Measure the prescribed volume using the provided syringe and administer within 30 minutes of mixing. Discard any unused suspension.
- Continue taking raltegravir even if you feel well. Do not stop taking raltegravir or your other anti-HIV medications without talking to your doctor. Skipping doses can lead to resistance.
Procedures and treatment changes
Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3)
Missed dose
Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take two doses at the same time to make up for a missed dose.
Overdose
There is no specific antidote information for raltegravir overdose. If you think someone has taken too much, contact a poison-information service or emergency department immediately; doctors use standard supportive measures and monitoring, which may include an electrocardiogram (ECG). (2) (3)
Raltegravir side effects
Clinical trials have evaluated raltegravir in treatment-naïve and treatment-experienced adults. Side effects can vary based on the concomitant antiretroviral regimen.
Nausea, headache, dizziness, tiredness, insomnia
What to notice: These were among the most commonly reported adverse reactions in clinical studies.
What to do: Tell your doctor if these symptoms are severe or do not go away. (1) (2)
Diarrhea, flatulence, asthenia, decreased appetite, abnormal dreams, depression, nightmare
What to notice: These were reported in clinical trials of raltegravir 400 mg twice daily in treatment-naïve adults.
What to do: Discuss any persistent or troublesome mood changes or physical symptoms with your doctor. (2)
Immune reconstitution syndrome
What to notice: New or worsening symptoms of an infection after starting raltegravir, as the immune system gets stronger and fights off previously hidden infections. Autoimmune disorders like Graves' disease have also been reported.
What to do: Contact your doctor promptly if you develop any new or worsening symptoms during treatment. (1) (2)
Muscle problems or rhabdomyolysis
What to notice: Muscle pain, tenderness, weakness, or dark/cola-colored urine.
Liver problems
What to notice: Extreme tiredness, nausea, vomiting, loss of appetite, pain in the upper right part of the stomach, yellowing of the skin or eyes, or pale stools.
What to do: Call your doctor immediately. (1)
Severe skin or hypersensitivity reactions
What to notice: Rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema.
What to do: These can be life-threatening. Seek emergency medical treatment and do not delay in stopping the medicine; management should be guided by a clinician. (1) (2)
Serious warnings
Severe skin and hypersensitivity reactions — emergency
Symptoms: Severe rash or rash with fever, general malaise, fatigue, muscle or joint aches, blisters, mouth lesions, red/itchy/swollen eyes, swelling of the eyes, face, lips, tongue, throat, hands, feet, ankles, or arms, difficulty breathing or swallowing.
Action: Seek emergency medical attention immediately if signs of a severe skin or hypersensitivity reaction develop. (1) (2)
Signs of a serious infection — urgent
Symptoms: Fever, sore throat, cough, chills, and other signs of infection.
Action: Call your doctor immediately if you experience new or worsening signs of infection. (1)
Interactions
| Medicine or test | Effect | Action |
|---|---|---|
| Antacids containing aluminum and/or magnesium | May interact with raltegravir; your doctor may need to adjust your medication or monitor you for side effects. | Tell your doctor and pharmacist if you are taking these before starting raltegravir. Do not start taking them while on raltegravir without discussing with your healthcare provider. (1) |
| Rifampin | When coadministered with rifampin, a dose adjustment of raltegravir to 800 mg twice daily is recommended for adults. | Your prescriber will adjust the dose; do not change your dose yourself. (2) |
| Other prescription/ nonprescription medicines, vitamins, and herbal products | May interact with raltegravir, requiring dose changes or monitoring. | Keep a written list of all medicines you take and bring it to every doctor's visit. (1) |
Special populations
Pregnancy and breastfeeding
Tell your doctor if you are pregnant or plan to become pregnant. Do not breastfeed without discussing risks with your doctor, as HIV and some of the medicine can pass into breast milk. (1)
People with phenylketonuria (PKU)
The chewable tablets contain aspartame, which forms phenylalanine. Each 25 mg tablet contains approximately 0.05 mg phenylalanine; each 100 mg tablet contains approximately 0.10 mg. This can be harmful to people with PKU. (1) (2)
People on dialysis
Because the extent to which raltegravir may be dialyzable is unknown, dosing before a dialysis session should be avoided. (2)
Pediatric patients
Eligibility and dosing depend on age, weight, and product formulation. ISENTRESS can be used from birth in full-term neonates weighing at least 2 kg; ISENTRESS HD is for patients weighing at least 40 kg. Specific dose tables are in the prescribing information. Data are unavailable for pre-term neonates. (2) (3)
Monitoring
Before starting
- Confirm the diagnosis of HIV-1 infection and eligibility for raltegravir as part of combination therapy.
- Review baseline liver function tests, especially if the patient has hepatitis B or C co-infection.
- Assess risk factors for myopathy or rhabdomyolysis, including history of elevated creatine kinase or concomitant medications.
- Note whether the patient has phenylketonuria before prescribing chewable tablets.
During treatment
- Keep all appointments with your doctor and the laboratory. Your doctor will order lab tests to check your body's response to raltegravir.
- Monitor for signs of severe skin or hypersensitivity reactions, muscle symptoms, and liver abnormalities.
- If co-infected with hepatitis B or C, closer monitoring of liver aminotransferases is required, as rates of AST and ALT abnormalities may be higher.
- Be alert to signs of immune reconstitution syndrome, including new or worsening symptoms of previous infections.
Storage
Keep raltegravir film-coated tablets and HD tablets in the original container, tightly closed, and out of reach of children. Store at room temperature away from excess heat and moisture (not in the bathroom). Do not remove the desiccant packet from the bottle. Dispose of unneeded medication through a medicine take-back program; do not flush down the toilet. Follow safe disposal guidelines to prevent accidental ingestion by children, pets, or others.
Professional information
Clinician-facing context only. Use the current local indication, dosing table, and formulation-specific instructions.
All regions
Indication: HIV-1 infection in adults
Dose summary: For treatment-naïve patients or those virologically suppressed on an initial 400 mg twice-daily regimen: 1200 mg (2 × 600 mg) once daily as ISENTRESS HD, or 400 mg twice daily as ISENTRESS. For treatment-experienced patients: 400 mg twice daily. When coadministered with rifampin: 800 mg (2 × 400 mg) twice daily.
Renal context: Dosing before a dialysis session should be avoided because dialyzability is unknown. No other renal impairment-specific dose adjustment is described in the provided notes. (2)
All regions
Indication: HIV-1 infection in pediatric patients
Dose summary: Formulation and dosing are weight-based and age-specific. See the product label for full-term neonates, patients aged 4 weeks and older, and patients weighing at least 25 kg or 40 kg. ISENTRESS for oral suspension is used for the youngest and lowest-weight patients; chewable tablets or film-coated tablets are used as weight increases. ISENTRESS HD is limited to patients ≥40 kg. (2)
Hepatic guidance
Use with caution in patients with co-existing hepatitis B and/or C; rates of AST and ALT abnormalities may be higher. No specific hepatic impairment dose adjustment is provided in the research notes.
Overdose note
No specific treatment information is available. Labels advise standard supportive measures (e.g., removal of unabsorbed material from the GI tract), clinical monitoring including an ECG, and supportive therapy as required; the extent to which raltegravir is dialysable is unknown. (1) (2)
Frequently asked questions
Can raltegravir cure my HIV?
No. Raltegravir does not cure HIV, but it may decrease your chance of developing AIDS and HIV-related illnesses when taken as part of a complete antiretroviral regimen. (1)
Can I switch between raltegravir tablets, chewable tablets, or the oral suspension?
No. The products have different pharmacokinetic profiles. You must take the exact formulation prescribed by your doctor. Do not substitute the chewable tablet or oral suspension for the film-coated tablet or HD tablet. (2)
Can I take raltegravir alone, without other HIV medicines?
Raltegravir is always used in combination with other antiretroviral agents. It is not approved for use as a single agent to treat HIV. (2)
What is the mechanism of action of raltegravir?
Raltegravir is an HIV integrase inhibitor. It decreases the amount of HIV in the blood by blocking a viral enzyme necessary for replication. (1) (2)
References
- Raltegravir: MedlinePlus Drug InformationMedlinePlus, U.S. National Library of Medicine · United States · accessed 2026-10-19 · source 1
- ISENTRESS and ISENTRESS HD (raltegravir) prescribing informationU.. Food and Drug Administration (Dailymed) · United States · accessed 2026-10-19 · source 2
- Isentress (raltegravir) EPAR Product Information, SmPC sections 4.1-4.9 (400 mg film-coated tablets)European Medicines Agency · European Union · accessed 2026-10-19 · source 3
Brand names by country
Single-ingredient raltegravir names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.
Priority countries
United States
- IsentressMerck Sharp & Dohme LLCregulator source
- Isentress HDMerck Sharp & Dohme LLCregulator source
View brands in additional countries.
European Union
Isentress