Opsumit

Monotherapy or in combination for long-term treatment of pulmonary arterial HTN (PAH) in adult patients of WHO functional class II-III.

Adult ≥40 kg 10 mg once daily.

May be taken with or without food: Take every day at about the same time. Swallow whole, do not break.

Hypersensitivity. Severe hepatic impairment (w/ or w/o cirrhosis). Baseline values of hepatic aminotransferase (AST &/or ALT) >3 x ULN. Women of childbearing potential who are not using effective contraception. Pregnancy & lactation.

Not to be used in patients w/ soya hypersensitivity. Liver function, discontinue use if unexplained clinically relevant aminotransferase elevations occur, or if elevations are accompanied by increased bilirubin >2 x ULN or by clinical symptoms of liver injury (eg, jaundice), obtain liver enzyme tests prior to initiation of treatment; not to be initiated in patients w/ elevated aminotransferases (>3 x ULN). Patient w/ WHO class I functional status of pulmonary arterial HTN. Hb conc, not recommended in patients w/ severe anemia, measure Hb conc prior to initiation & tests repeated during treatment as clinically indicated. Pulmonary veno-occlusive disease, monitor for signs of pulmonary oedema. Not to be taken by patients w/ galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. Avoid combination w/ strong CYP3A4 inducers. Concomitant use w/ strong CYP3A4, moderate dual CYP3A4 & CYP2C9, moderate CYP3A4 & CYP2C9 inhibitors. May affect ability to drive & use machines. Renal impairment, consider BP & Hb monitoring; not recommended in severe renal impairment. Women of childbearing potential should use effective contraception. Spermatogenesis in men. Not to be used during pregnancy & lactation. Childn & adolescents <18 yr.

Nasopharyngitis, bronchitis; anaemia, decreased Hb; headache; oedema, fluid retention. Pharyngitis, flu, UTI; leukopenia, thrombocytopenia; hypotension, flushing; nasal congestion; aminotransferase elevations; increased uterine bleeding.

Reduced efficacy w/ strong CYP3A4 inducers eg, rifampicin. Increased exposure w/ strong CYP3A4 (eg, ketoconazole), moderate dual CYP3A4 & CYP2C9 (eg, fluconazole, amiodarone) inhibitors. Caution w/ moderate CYP3A4 (eg, ciprofloxacin, cyclosporine, diltiazem, erythromycin, verapamil) & moderate CYP2C9 (eg, miconazole, piperine) inhibitors.

Other Antihypertensives

C02KX04 - macitentan ; Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.

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