Medical Information

Ambrisentan is a selective endothelin receptor antagonist mainly used for the treatment of pulmonary arterial hypertension, and special attention should be paid to liver function monitoring and pregnancy contraindications. The following provides a detailed explanation from two aspects: indications and medication precautions.

1. Indications

(1) Pulmonary arterial hypertension

Suitable for idiopathic or connective tissue disease-related pulmonary arterial hypertension with WHO functional classification II-III, it can improve exercise tolerance (an average increase of 50 meters in 6-minute walking distance) and delay clinical deterioration.

2. Medication precautions

(1) Liver function monitoring

Before treatment and monthly transaminase testing is required. If ALT/AST is greater than 3 times the normal value, medication should be suspended. If ALT/AST is greater than 5 times or accompanied by elevated bilirubin, medication should be permanently discontinued.

(2) Hematological impact

May cause a decrease in hemoglobin (average decrease of 0.8 g/dL), monitor blood routine every month during the initial stage of treatment, and evaluate iron metabolism in anemic patients.

(3) Pregnancy taboos

It has clear teratogenicity, and women of childbearing age need to confirm a negative pregnancy test before treatment. Dual contraception measures should be taken during treatment and one month after discontinuation of medication.

(4) Special populations

The starting dose for patients with moderate liver function impairment is halved, and severe use is prohibited; The elderly patients over 65 years old need to monitor the symptoms of fluid retention more frequently.

(5) Drug interactions

When combined with cyclosporine, the blood concentration of anlishentan increases by 50%, and the dosage needs to be adjusted; Avoid co administration with potent CYP3A4 inducers.