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Macitentan oral


Oral formulations of macitentan.

Drugs List

  • macitentan 10mg film coated tablets
  • OPSUMIT 10mg film coated tablets
  • Therapeutic Indications


    Pulmonary arterial hypertension: functional grades II and III

    Macitentan, as monotherapy or in combination, is indicated for the long term treatment of pulmonary arterial hypertension (PAH) in adult patients of WHO Functional Class (FC) II to III.

    Efficacy has been shown in a PAH population including idiopathic and heritable PAH, PAH associated with connective tissue disorders, and PAH associated with corrected simple congenital heart disease.



    The recommended dose is 10mg once daily.

    Additional Dosage Information

    Macitentan should be taken every day at the same time. If the patient misses a dose of macitentan, the patient should be told to take it as soon as possible and then take the next dose at the regularly scheduled time. The patient should be told not to take two doses at the same time if a dose has been missed.


    Children under 18 years
    Moderate hepatic impairment
    Renal dialysis
    Serum transaminases above 3 times upper limit of normal
    Severe anaemia
    Severe hepatic impairment

    Precautions and Warnings

    Females of childbearing potential
    Patients over 75 years
    Glucose-galactose malabsorption syndrome
    Lactose intolerance
    Pulmonary veno-occlusive disease
    Severe renal impairment

    Advise ability to drive/operate machinery may be affected by side effects
    Treatment to be initiated and supervised by a specialist
    Contains lactose
    Contains soya or soya derivative
    Ensure negative pregnancy test in week preceding initiation of treatment
    Monitor haemoglobin prior to initiating therapy and periodically thereafter
    Monitor hepatic function before initiating and at monthly intervals
    Ensure negative monthly pregnancy tests throughout treatment
    Monitor for signs of hepatic injury
    Renal impairment: Consider monitoring blood pressure
    Advise patients to seek medical advice if signs of hepatotoxicity occur
    Consider veno-occlusive disease if pulmonary oedema occurs
    Discontinue if AST or ALT level > 3x ULN and bilirubin > 2x ULN
    Advise patient not to take St John's wort concurrently
    Advise patient grapefruit products may increase plasma level
    May affect spermatogenesis
    Female: Contraception required during and for 1 month after treatment

    The benefit/risk balance of macitentan has not been established in patients with WHO class I functional status of pulmonary arterial hypertension.

    Reinitiation of macitentan may be considered following the return of hepatic enzyme levels to within the normal range in patients who have not experienced clinical symptoms of liver injury. The advice of a hepatologist is recommended.

    The development of testicular tubular atrophy in male animals was observed after treatment with macitentan. The relevance of this finding to humans is unknown, but a deterioration of spermatogenesis cannot be excluded.

    Pregnancy and Lactation


    Macitentan is contraindicated in pregnancy.

    At the time of writing there are no adequate data on the use of macitentan in pregnant women. Animal studies have shown reproductive toxicity. The potential risk for humans is still unknown. Macitentan is contraindicated during pregnancy and in women of childbearing potential who are not using reliable contraception.

    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 ( ).


    Macitentan is contraindicated in breastfeeding.

    It is not known whether macitentan is excreted into human breast milk. Studies in rats have shown macitentan and its metabolites are excreted into milk during lactation. A risk to the breastfeeding child cannot be excluded.

    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

    Decrease in haemoglobin
    Fluid retention
    Hypersensitivity reactions
    Increase in serum ALT/AST
    Nasal congestion
    Reduced platelet count
    Urinary tract infections


    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: September 2018

    Reference Sources

    Summary of Product Characteristics: Opsumit (macitentan) 10mg tablets. Actelion Pharmaceuticals UK Ltd. Revised August 2018.

    NICE Evidence Services Available at: Last accessed: 04 September 2018.

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    Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content

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    FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.