Opsumit (Macitentan)

Opsumit is used to target the endothelin pathway in pulmonary arterial hypertension, helping to improve exercise capacity and delay disease progression.

• Pulmonary arterial hypertension (PAH): Improves functional class and exercise capacity.
• WHO Group 1 PAH: Reduces risk of clinical worsening.
• Chronic thromboembolic pulmonary hypertension (CTEPH) after surgical evaluation: Supports long‑term management.

• Macitentan blocks both endothelin‑A and endothelin‑B receptors, preventing endothelin‑1 from binding and triggering vasoconstriction and smooth‑muscle proliferation in the pulmonary arteries. This dual antagonism leads to sustained vasodilation and reduced vascular remodeling, improving hemodynamic parameters in pulmonary arterial hypertension.

Common Side Effects

• Headache: mild to moderate intensity.
• Nasopharyngitis: typical upper‑respiratory infection symptoms.
• Peripheral edema: swelling of the lower limbs.
• Anemia: reduced hemoglobin levels.
• Fatigue: general tiredness.
• Nasal congestion: stuffy nose.

Serious or Rare Side Effects

• Liver injury: elevated transaminases or hepatitis.
• Severe anemia: marked drop in hemoglobin.
• Pulmonary edema: fluid accumulation in lungs.
• Hypotension: significant blood‑pressure reduction.
• Drug‑induced lupus‑like syndrome.
• Severe hypersensitivity reactions.

Patients should be monitored regularly for liver function, hemoglobin levels and signs of fluid retention.

• Liver monitoring: perform baseline and periodic liver enzyme tests.
• Hemoglobin checks: assess for anemia before and during therapy.
• Fluid retention: watch for peripheral edema or sudden weight gain.
• Pregnancy avoidance: contraindicated in pregnancy due to teratogenic risk.
• Drug interactions: review concomitant medications for CYP3A4 substrates.
• Store at ambient temperature: keep in original packaging, protect from moisture and direct sunlight.

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