Opsumit

Generic name: macitentan

Drug class: Endothelin receptor antagonists

Dosage form: 10 mg film-coated tablets

Root of administration: Oral

Dose: 10 mg once daily

Mechanism of action: Macitentan is a dual endothelin receptor antagonist that blocks endothelin-1 from binding to both ETA and ETB receptors, leading to vasodilation and reduced pulmonary arterial pressure.

Drug usage cases:

• Treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce hospitalization risk.

Drug contraindications:

• Pregnancy
• Hypersensitivity to macitentan or any component of the product

Side effects:

• Headache
• Nasopharyngitis
• Anemia
• Urinary tract infection
• Bronchitis
• Flu-like symptoms
• Peripheral edema
• Elevated liver enzymes

Warnings:

• Embryo-fetal toxicity: Contraindicated during pregnancy; females of reproductive potential must use effective contraception during treatment and for one month after discontinuation.
• Hepatotoxicity: Monitor liver enzymes before and during treatment; discontinue if clinically relevant elevations occur.
• Fluid retention: Monitor for signs of edema; may require diuretic therapy or discontinuation.
• Decreased hemoglobin: Monitor hemoglobin levels; may require dose adjustment or discontinuation.
• Decreased sperm count: May affect male fertility; advise men of potential effects on fertility.

Use during pregnancy or breastfeeding: Macitentan is contraindicated during pregnancy due to potential fetal harm. Females of reproductive potential must exclude pregnancy before starting treatment, use effective contraception during treatment, and for one month after stopping treatment. Macitentan is not recommended during breastfeeding; consult a healthcare provider for guidance.