- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Oral formulations of macitentan.
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
Serum transaminases above 3 times upper limit of normal
Severe hepatic impairment
Precautions and Warnings
Females of childbearing potential
Patients over 75 years
Glucose-galactose malabsorption syndrome
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 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 ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
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 https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Decrease in haemoglobin
Increase in serum ALT/AST
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 ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: September 2018
Summary of Product Characteristics: Opsumit (macitentan) 10mg tablets. Actelion Pharmaceuticals UK Ltd. Revised August 2018.
NICE Evidence Services Available at: www.nice.org.uk 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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