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CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › OTHER ANTIHYPERTENSIVES › Antihypertensives for pulmonary arterial hypertension
ambrisentan
C02KX02
Forms & Strengths
- Oral tablet: 5 mg
- Oral tablet: 10 mg
Adult Dosing
- Pulmonary Arterial Hypertension (PAH): Initial 5 mg once daily, with or without food
- May increase to 10 mg once daily based upon clinical response and tolerability
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening
Mechanism of Action
- Endothelin receptor antagonist (ERA) with high selectivity for the endothelin A (ETA) receptor, blocking vasoconstriction and smooth muscle proliferation
Contraindications
- Pregnancy (Category X; teratogenic)
- Idiopathic pulmonary fibrosis (IPF), with or without secondary pulmonary hypertension
- Known hypersensitivity to ambrisentan or any component of the product
Adverse Reactions
- Peripheral edema
- Nasal congestion
- Sinusitis
- Flushing
- Palpitations
- Anemia and decreased hemoglobin
- Constipation
Drug Interactions
- Cyclosporine: Coadministration increases ambrisentan exposure by approximately 2-fold; limit ambrisentan dose to 5 mg once daily
- Strong CYP3A and P-gp inhibitors: May increase exposure
- Strong CYP inducers: May decrease efficacy
Curated Content: Needs Vetting Before Put to Clinical Use