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Raltegravir oral

Updated 2 Feb 2023 | Other antiretrovirals


Oral preparations containing raltegravir (as potassium).

Drugs List

  • ISENTRESS 100mg chewable tablet
  • ISENTRESS 100mg granules for oral suspension
  • ISENTRESS 25mg chewable tablet
  • ISENTRESS 400mg tablets
  • ISENTRESS 600mg tablets
  • raltegravir 100mg chewable tablet
  • raltegravir 100mg granules for oral suspension
  • raltegravir 25mg chewable tablet
  • raltegravir 400mg tablets
  • raltegravir 600mg tablets
  • Therapeutic Indications


    HIV infection-combined with other antiretrovirals


    Different formulations are not bioequivalent.


    If raltegravir is co-administered with rifampicin in adults, doubling the dose of raltegravir may be considered.

    Raltegravir 600mg tablet
    1200mg once daily.

    Raltegravir 400mg tablet
    400mg twice daily.


    Children weighing at least 40kg
    Raltegravir 600mg tablet
    1200mg once daily.

    Children weighing at least 25kg
    Raltegravir 400mg tablet
    400mg twice daily.

    Raltegravir chewable tablets
    Body weight at least 40kg: 300mg twice daily.
    Body weight 28kg to less than 40kg: 200mg twice daily.
    Body weight 25kg to less than 28kg: 150mg twice daily.

    Children weighing 20kg to less than 25kg
    Raltegravir chewable tablets
    150mg twice daily.

    Children weighing 11kg to less than 20kg
    Raltegravir chewable tablets
    Body weight 14kg to less than 20kg: 100mg twice daily.
    Body weight 11kg to less than 14kg: 75mg twice daily.

    Raltegravir granules for oral suspension
    Patients at least 1 week old
    Body weight 14kg to less than 20kg: 10mL (100mg) twice daily.
    Body weight 11kg to less than 14kg: 8mL (80mg) twice daily.

    Children weighing 3kg to less than 11kg
    Raltegravir granules for oral suspension
    Patients at least 4 weeks old
    Body weight 8kg to less than 11kg: 6mL (60mg) twice daily.
    Body weight 6kg to less than 8kg: 4mL (40mg) twice daily.
    Body weight 4kg to less than 6kg: 3mL (30mg) twice daily.
    Body weight 3kg to less than 4kg: 2.5mL (25mg) twice daily.

    Patients at least 1 week old to 4 weeks old
    Body weight 2kg to less than 3kg: 0.8mL (8mg) twice a day.
    Body weight 3kg to less than 4kg: 1mL (10mg) twice a day.
    Body weight 4kg to less than 5kg: 1.5mL (15mg) twice a day.

    Patients from birth to 1 week old
    Body weight 2kg to less than 3kg: 0.4mL (4mg) once a day.
    Body weight 3kg to less than 4kg: 0.5mL (5mg) once a day.
    Body weight 4kg to less than 5kg: 0.7mL (7mg) once a day.


    Infants weighing less than 3kg
    Neonates under 1 month
    Hereditary fructose intolerance

    Precautions and Warnings

    Family history of hereditary muscular disorders
    Predisposition to rhabdomyolysis
    Glucose-galactose malabsorption syndrome
    Hepatitis B
    Hepatitis C
    History of depression
    History of myopathy
    History of non-traumatic rhabdomyolysis
    History of psychiatric disorder
    Lactose intolerance
    Severe hepatic impairment

    Some formulations contain aspartame - caution in phenylketonuria
    Treatment does not prevent risk of transmission of HIV
    Advise ability to drive/operate machinery may be affected by side effects
    HIV therapy: Must be used in combination with other antiretrovirals
    Not all available products are licensed for all age groups
    Treatment should be initiated by doctor experienced in HIV management
    Presentations with sorbitol unsuitable in hereditary fructose intolerance
    Some formulations contain fructose
    Some formulations contain lactose
    Some formulations contain sucrose
    Different formulations are not bioequivalent
    Autoimmune disorders can occur many months after initiation of treatment
    Monitor for signs of osteonecrosis
    Advise patient to seek medical advice if joint aches or pain occur
    Advise patient to seek medical advice if movement becomes difficult
    Inflammatory symptoms should be evaluated and treated appropriately
    Risk of developing opportunistic infections
    Discontinue if drug-related rash or other hypersensitivity reactions occur
    Discontinue if hepatic function deteriorates in pts with hepatic impairment
    Advise patient to avoid aluminium / magnesium hydroxide containing antacids

    When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and can cause serious clinical conditions or aggravation of symptoms. Such reactions are usually observed within the first few weeks or months after treatment initiation. Examples are cytomegalovirus retinitis, mycobacterial infections or Pneumocystis jiroveci pneumonia. Any inflammatory symptoms should be evaluated and treated appropriately.

    Severe, potentially life-threatening, and fatal skin reactions have been reported in patients taking raltegravir. These include cases of Stevens-Johnson syndrome and toxic epidermal necrolysis. Hypersensitivity reactions have also been reported and were characterized by rash, constitutional findings, and, organ dysfunction, including hepatic failure. Discontinue immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop. Clinical status including liver aminotransferases should be monitored and appropriate therapy initiated. Delay in stopping raltegravir treatment or other suspect agents after the onset of severe rash may result in a life-threatening reaction.

    Patients with pre-existing hepatic dysfunction, including chronic hepatitis, have an increased frequency of hepatic function abnormalities during combination anti-retroviral therapy. These patients should be closely monitored. If there is evidence of worsening hepatic disease in these patients, interruption or discontinuation of therapy should be considered.

    Patients with chronic hepatitis B or C who are treated with combination antiretroviral therapy have an increased risk of developing severe and potentially fatal hepatic adverse effects, and therefore should be closely monitored during treatment.

    Pregnancy and Lactation


    Raltegravir is contraindicated during pregnancy.

    There are no adequate data on the use of raltegravir during human pregnancy.

    Animal studies have shown reproductive toxicity. The potential risk for humans is not known. It is not known if raltegravir crosses the human placenta. The molecular weight (about 483), moderate plasma protein binding and the terminal half-life suggest that exposure of the embryo-foetus will occur. The low lipid solubility might mitigate the amount of exposure.

    Briggs (2015) suggests, if indicated, raltegravir should not be withheld because of pregnancy. Briggs (2015) recommends the use of zidovudine during the intrapartum period regardless of current regimen, as this may prevent vertical transmission of HIV to the newborn.

    Antiretroviral Pregnancy Registry
    A registry has been established to monitor maternal-foetal outcomes in patients inadvertently administered raltegravir while pregnant. Physicians are encouraged to register patients in this registry.

    The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( ) or if this is unavailable at the backup site ( ).


    Raltegravir is contraindicated during breastfeeding.

    It is recommend that HIV infected women do not breastfeed their infants under any circumstances in order to avoid transmission of HIV.

    It is not known if raltegravir is excreted into human milk.

    Studies in rats have demonstrated that raltegravir is excreted in milk. When a maternal dose of 600 mg/kg/day was administered, the mean substrate concentration in milk was approximately 3 times greater than in maternal plasma.

    Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
    Specialist advice is available from the UK Drugs in Lactation Advisory Service at

    Side Effects

    Attention disturbances
    Autoimmune hepatitis
    Carpal tunnel syndrome
    Changes in blood chemistry
    Chest discomfort
    Cognitive impairment
    Creatine phosphokinase increased
    Diabetes mellitus
    Disturbances of appetite
    Dry skin
    Elevated triglyceride levels
    Erectile dysfunction
    Facial wasting
    Gastro-intestinal symptoms
    Gastrointestinal disorder
    Graves' disease
    Hepatic failure
    Hepatobiliary disorders
    Herpes infections
    Hot flushes
    Hypersensitivity reactions
    Immune Reactivation/Reconstitution Syndrome
    Impaired memory
    Increase of liver transaminases
    Menopausal-like symptoms
    Molluscum contagiosum
    Mood changes
    Nasal congestion
    Peripheral neuropathy
    Reduced platelet count
    Renal cysts
    Renal impairment
    Skin papilloma
    Sleep disturbances
    Stevens-Johnson syndrome
    Suicidal tendencies
    Tendon inflammation
    Upper respiratory tract infection
    Ventricular extrasystoles
    Visual disturbances
    Weight gain


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last full review date: January 2018.

    Reference Sources

    Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

    Summary of Product Characteristics: Isentress 25mg and 100mg chewable tablets. Merck Sharp and Dohme Limited. Revised October 2018.
    Summary of Product Characteristics: Isentress 100mg granules for oral suspension. Merck Sharp and Dohme Limited. Revised October 2018.
    Summary of Product Characteristics: Isentress 400mg film-coated tablets. Merck Sharp and Dohme Limited. Revised October 2018.
    Summary of Product Characteristics: Isentress 600mg film-coated tablets. Merck Sharp and Dohme Limited. Revised October 2018.

    NICE Evidence Services Available at: Last accessed: 16 January 2018

    US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
    Available at:
    Raltegravir. Last revised: 10 March 2015
    Last accessed: 16 January 2018.

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