Introduction
Macipah Tablet 10 mg is an endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH). It works by blocking endothelin receptors on vascular smooth muscle and blood vessels, reducing vasoconstriction, vascular remodeling, inflammation, fibrosis, and cell proliferation, thereby improving pulmonary blood flow. Macipah Tablet 10 mg carries a high risk of embryo-fetal toxicity and is contraindicated during pregnancy, requiring strict pregnancy prevention measures in women of childbearing potential.
Uses
Macipah Tablet 10 mg is an endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.
Macipah Tablet 10 mg is indicated for patients with pulmonary arterial hypertension.
Associated Conditions
Pharmacodynamics
Macipah Tablet 10 mg blocks simulators of hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.
Mechanism of Action
Macipah Tablet 10 mg is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macipah Tablet 10 mg binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.
Absorption
Macipah Tablet 10 mg is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.
Volume of Distribution
Macipah Tablet 10 mg has a volume of distribution of 50L.
Protein Binding
Macipah Tablet 10 mg is >99% bound to plasma proteins, which are mainly albumin
Route of Elimination
Eliminated 50% through urine and 24% through feces.
Half Life
The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.
Clearance
Clearance data was not found.
Toxicity
Macipah Tablet 10 mg has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.
Food Interactions
- Take with or without food.
Dosage
Elderly: There is limited clinical data with Macipah Tablet 10 mg in patients over the age of 75 years, therefore Macipah Tablet 10 mg should be used with caution in this population.
Pediatric population: The safety of Macipah Tablet 10 mg in children and adolescents below 18 years has not yet been established.