Macitentan
ТаблеткиAn endothelin-1 receptor antagonist capable of binding to endothelin receptor types A and B. Endothelin-1 mediates a variety of effects including vasoconstriction, induction of fibrosis, cell proliferation, hypertrophy, and inflammation.
Indications
Macitentan, as monotherapy or as part of combination therapy, is indicated for the long-term treatment of pulmonary arterial hypertension (LAH) in adult patients with World Health Organisation (WHO) functional class (FC) II and III, including:
- idiopathic and hereditary LAH;
- LAH associated with connective tissue diseases;
- LAH associated with compensated simple congenital heart disease.
Contraindications
- Hypersensitivity to macitentan or to any of the excipients,
listed in section 6.1;
- Pregnancy;
- Breastfeeding;
- Use of the drug in women with preserved childbearing potential who do not use reliable contraceptive methods;
- Severe degree of hepatic insufficiency (10 points and higher on the Child-Pugh scale), both in case of diagnosed liver cirrhosis and without it;
- Initial increase in the activity of "hepatic" transaminases alanine aminotransferase (ALT) and/or aspartate aminotransferase (ACT) more than 3 times the upper limit of normal (ULN);
- Severe renal insufficiency (creatinine clearance <30 ml/min), including if dialysis is required. including if dialysis is required (no clinical data).
Usage
Inside. The film-coated tablet is not intended to be broken, it should be swallowed whole, drinking enough water. The drug Macitentan should be taken every day at the same time, regardless of the time of food intake.
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Drugs in the category Cardiology
Has contraindications. Needs specialist overview.