MACITENTAN

It is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

Indications

Pulmonary Arterial Hypertension (WHO group1).

Dosage

Oral; 10mg once daily.

Contra-Indications

Pregnancy.

Special Precautions

Paediatric: Safety and efficacy in pediatric patients have not been established. Pregnancy: contraindicated, Female patients of reproductive potential must have a negative pregnancy test prior to starting treatment, monthly during treatment, and one month after discontinuation of treatment. Lactation: it is not known whether it is excreted into the human breast milk, advise women not to breastfeed during treatment Elderly: No overall differences in safety or effectiveness have been observed between elderly and other adult patients.

Side Effects

Anemia, Nasopharyngitis/pharyngitis, Bronchitis, Headache, Influenza, Urinary tract infection, hypersensitivity reactions (angioedema, pruritus and rash), nasal congestion, Elevations of liver aminotransferases (ALT, AST), edema/fluid retention, decrease in hemoglobin, decrease sperm count.

Drug Interactions

Strong CYP3A4 Inducers like rifampicin, Strong CYP3A4 Inhibitors like ketoconazole.