Ambrisan is indicated for the treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening.
Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide. Two receptor subtypes, ETA and ETB, mediate the effects of ET-1 in the vascular smooth muscle and endothelium. The primary actions of ETA are vasoconstriction and cell proliferation, while the predominant actions of ETB are vasodilation, antiproliferation, and ET-1 clearance.
Adult dose: Initial treatment is 5 mg once daily, and can be increased to 10 mg once daily if 5 mg is tolerated. Ambrisentan may be administered with or without food.
Pediatric patients: The safety and effectiveness of Ambrisentan in pediatric patients have not been established.
Multiple dose co-administration of Ambrisan and Cyclosporine resulted in an approximately 2-fold increase in Ambrisan exposure in healthy volunteers; therefore, limit the dose of Ambrisan to 5 mg once daily when co-administered with Cyclosporine.
Ambrisentan may cause fetal harm when administered to a pregnant woman. Ambrisentan is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.
Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with Ambrisan
Pregnancy Category X. It is not known whether Ambrisentan is excreted in human milk. Breastfeeding while receiving Ambrisentan is not recommended.
Anti-hypertensive, Endothelin receptor antagonist
Store in a cool and dry place, below 30°C. Protect from light and moisture.