MACITENTAN

-Macitentan is a medication belonging to the class of endothelin receptor antagonists. It is primarily used in the treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and delay disease progression. -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

-Macitentan is indicated for the treatment of pulmonary arterial hypertension (PAH) to reduce the risk of disease progression and hospitalization for PAH. -Pulmonary Arterial Hypertension (WHO group1).

Dosage

-The recommended dosage of macitentan is typically 10 mg taken orally once daily, with or without food. Dosage adjustments may be necessary based on individual patient factors. -Oral; 10mg once daily.

Contra-Indications

Macitentan is contraindicated in patients with a known hypersensitivity to the drug. It is also contraindicated in pregnancy due to potential harm to the fetus.

Special Precautions

Pregnancy: Macitentan can cause fetal harm, and therefore, reliable contraception is essential during treatment and for a period after stopping the drug. Liver Function: Regular monitoring of liver function is recommended, as macitentan may cause liver enzyme elevations. 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

-Common side effects of macitentan include headache, nasopharyngitis, anemia, and peripheral edema. Serious side effects may include liver enzyme elevations and fluid retention. -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

-Macitentan may interact with certain drugs, such as cyclosporine and rifampin, affecting their levels in the body. Close monitoring and dosage adjustments may be required when used concomitantly. -Strong CYP3A4 Inducers like rifampicin, Strong CYP3A4 Inhibitors like ketoconazole.