Company: Actelion Pharmaceuticals UK Ltd.
Legal category: Prescription. High Tech. Sport permitted.
Active ingredient: Macitentan 10mg.
Description: Round, biconvex, white, film-coated tablets marked 10.
Presentation: 28, price available on request.
Indication: Long-term treatment of pulmonary arterial hypertension (WHO Functional Class II to III). As monotherapy or in combination.
Pharmacology: Macitentan is a potent endothelin receptor antagonist. It prevents endothelin-mediated activation of second messenger systems that result in vasoconstriction and smooth muscle cell proliferation.
Dosage: Adult: Swallow whole. 10mg once daily at about same time. For specialist use only. Elderly: Over 75 years, limited experience (caution). Children: Safety and efficacy not established.
Contraindications: Hypersensitivity to the active ingredient or to any of the excipients. Severe hepatic impairment, elevated hepatic aminotransferases (>3 × ULN). Pregnancy, lactation. Women must use contraception during treatment and for 1 month after.
Special precautions: WHO functional class I (benefit/risk ratio not established). Not recommended: Patients undergoing dialysis, moderate hepatic impairment, initiation in severe anaemia. Caution: Severe renal impairment. Renal impairment, consider monitoring blood pressure and haemoglobin. Prior to initiation measure haemoglobin concentrations (and as clinically indicated thereafter) and liver enzymes (monitor ALT and AST monthly). Monitor for hepatic injury. Discontinue if sustained, unexplained, aminotransferase elevations occur (or if accompanied by increased bilirubin (>2 × ULN) or liver injury symptoms); may consider reinitiation if levels return to normal (unless experienced liver injury). If signs of pulmonary oedema occur consider pulmonary veno-occlusive disease. Cases of anaemia requiring blood cell transfusion reported. Contains lactose, lecithin (soya). Driving/using machines. May affect male fertility.
Drug interactions: Avoid: Strong CYP3A4 inducers. Caution: Strong CYP3A4 inhibitors (including telithromycin). Drugs transported by breast cancer resistance protein. See appendix I.
Adverse drug reactions: Nasopharyngitis, bronchitis, pharyngitis, influenza, urinary tract infection, anaemia, headache, hypotension.
Full prescribing information and references available from Actelion Pharmaceuticals UK Ltd.
Telephone: 0044 (0)208 987 3333. E-mail: medinfo_uk@actelion.com