Medical Information

Aprocitentan is a dual endothelin receptor antagonist primarily used to treat refractory hypertension. Its target population, limitations, and drug interactions must strictly follow clinical guidelines to ensure medication safety.

1. Applicable population

(1) Refractory hypertension patients: suitable for adult patients who have received at least three antihypertensive drugs (including diuretics) but still cannot control their blood pressure.

(2) Specific renal dysfunction patients: Patients with mild to moderate renal dysfunction need to adjust their dosage, while severe patients need to be carefully assessed for risk.

(3) Non pregnant adults: Women of childbearing age should take effective contraceptive measures to avoid exposing their fetuses to potential teratogenic risks.

2. Restrictive conditions

(1) Prohibited during pregnancy: Animal studies have shown embryotoxicity, and use by pregnant women may lead to fetal malformation or death.

(2) Liver dysfunction: Not recommended for patients with moderate to severe liver dysfunction (Child Pugh B/C grade), as it may worsen liver damage.

(3) Breastfeeding restriction: Medications may be secreted into breast milk, and breastfeeding should be suspended during treatment and for one month after discontinuation of medication.

3. Drug interactions

(1) Strong CYP3A4 inhibitors, such as clarithromycin and itraconazole, may increase the blood concentration of Apuxitan and should be avoided in combination or adjusted in dosage.

(2) Enhanced effect of antihypertensive drugs: Combined use with ACEI and ARB may increase the risk of hypotension, and close monitoring of blood pressure and renal function is necessary.

(3) Liver enzyme inducers: such as rifampicin, may reduce drug efficacy and dosage adjustments or alternative treatment options need to be considered.