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CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › OTHER ANTIHYPERTENSIVES › Antihypertensives for pulmonary arterial hypertension
macitentan
C02KX04
Adult Dosing
- Pulmonary arterial hypertension (PAH): 10 mg orally once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of pulmonary arterial hypertension (PAH, WHO Group 1) to reduce morbidity and mortality
Mechanism of Action
- Dual endothelin receptor antagonist (ETA and ETB) that prevents endothelin-1-mediated vasoconstriction, cell proliferation, and fibrosis
Contraindications
- Pregnancy
- Hypersensitivity to macitentan or any component
- Initiation in patients with baseline aminotransferase levels greater than 3 times the upper limit of normal
Adverse Reactions
- Anemia
- Nasopharyngitis
- Headache
- Bronchitis
- Edema/fluid retention
- Elevated liver transaminases
- Hypotension
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole) may increase macitentan exposure; monitor for adverse effects
- Strong CYP3A4 inducers (e.g., rifampin) may significantly decrease macitentan efficacy; avoid coadministration
Curated Content: Needs Vetting Before Put to Clinical Use