Generic
Ambrisentan
2 brands available in the market
At a glance
Ambrisentan is indicated for the treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening.
Description
Selective endothelin A receptor antagonist used for managing pulmonary arterial hypertension and improving functional capacity.
Indications
Treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening.
Therapeutic class
Anti-hypertensive, Endothelin receptor antagonist
Pharmacological class
Selective ETA receptor antagonist
Pharmacology
High-affinity ETA receptor antagonist blocking vasoconstriction and cell proliferation mediated by Endothelin-1.
Mechanism of action
Competitive and selective antagonism of endothelin A receptors in vascular smooth muscle.
Dosage
Adult dose: Initial treatment is 5 mg once daily, can be increased to 10 mg once daily. Administered with or without food.
Administration
Oral administration with or without food.
Missed dose
Take as soon as remembered.
Side effects
Decreases in hemoglobin concentration, hematocrit, and peripheral edema.
Precautions & warnings
Monitor for fluid retention, pulmonary veno-occlusive disease, hematological changes; avoid in moderate/severe hepatic impairment.
Contraindications
Contraindicated in pregnancy (Category X) and patients with Idiopathic Pulmonary Fibrosis (IPF).
Drug interactions
Cyclosporine co-administration increases Ambrisentan exposure; limit dose to 5 mg daily.
Food interactions
Food does not affect its bioavailability.
Use in pregnancy
Pregnancy Category X. Contraindicated in pregnancy.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Breastfeeding while receiving Ambrisentan is not recommended.
Pediatric use
Safety and effectiveness in pediatric patients have not been established.
Geriatric use
Use as advised by physician.
Renal / hepatic impairment
Not recommended in moderate or severe hepatic impairment.
Overdose effects
Supportive care as needed.
Storage conditions
Store below 30°C, protected from light and moisture.
Chemical structure
Ambrisentan