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At a glance

Macitentan is used for the long-term treatment of pulmonary arterial hypertension (PAH). It acts as an endothelin receptor antagonist to reduce vasoconstriction and inflammation.

Indications
  • Pulmonary arterial hypertension (PAH) - WHO functional class II to III (idiopathic, heritable, connective tissue disease-associated, congenital heart disease-associated)
Pharmacology

Macitentan blocks ETA and ETB receptors to inhibit ET-1-mediated vasoconstriction, fibrosis, proliferation, hypertrophy, and inflammation.

Dosage

Adult Dose (Oral): 10 mg once daily

Side effects

Common Side Effects:

  • Nasopharyngitis (14%)
  • Headache (13.6%)
  • Anemia (13.2%)
Use in pregnancy

Use in Pregnancy: Contraindicated during pregnancy. Verify absence of pregnancy in women of childbearing potential before initiation; monthly pregnancy tests recommended.

Pregnancy Category: X — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Obtain liver enzyme tests prior to initiation
  • Not recommended in patients with severe anemia
  • Avoid concomitant use with strong CYP3A4 inducers
  • Caution with strong CYP3A4 inhibitors
  • Contraindicated in pregnancy and lactation
Overdose effects

Overdose may cause headache, nausea, and vomiting; dialysis is unlikely to be effective due to high protein binding.

Storage conditions

Store below 30°C, away from light and moisture; keep out of reach of children.

Macitentan — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.