Aprocitentan is an endothelin receptor antagonist (ERA) used to treat hypertension, especially in combination with other antihypertensive drugs, to lower blood pressure in adult patients whose blood pressure has not been fully controlled after using other drugs.

1、 Drug name

1. Common name: Aprocentan

2. Product Name: TRYVIO ™

2、 Indications

Used to treat hypertension, it needs to be used in combination with other antihypertensive drugs and is suitable for adult patients to lower blood pressure when other drugs are poorly controlled. Lowering blood pressure can reduce the risk of fatal and non fatal cardiovascular events such as stroke and myocardial infarction.

3、 Specifications and characteristics

1. Specification: 12.5mg/tablet.

2. Appearance: Thin film coated sheet.

4、 Main components

1. Active ingredient: Apuxitan

2. Accessories: cross-linked carboxymethyl cellulose sodium, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, etc.

5、 Usage and dosage

1. Recommended dosage: 12.5mg orally once daily, can be taken with food or on an empty stomach.

2. Omission treatment: skip the missed dose and take the medication at the original time next time. Do not take double the dose on the same day.

6、 Dose adjustment

1. Population without dose adjustment: elderly people over 65 years old, mild to severe renal insufficiency (eGFR ≥ 15mL/min), mild liver injury (Child Pugh A grade).

2. Prohibited or cautious population: patients with renal failure (eGFR<15mL/min) or dialysis, moderate to severe liver injury (Child Pugh B/C grade).

7、 Medication precautions

1. Pregnancy contraindications: Pregnant women are prohibited from using the medication. Before taking the medication, it is necessary to confirm a negative pregnancy result. During the treatment period and one month after stopping the medication, pregnancy should be monitored monthly.

2. Contraceptive requirements: Patients of childbearing age must take effective contraceptive measures before, during, and within one month after discontinuing medication.

3. Dietary influence: not affected by food.

4. Vomiting treatment: If vomiting occurs after taking medication, there is no need to take it again. Follow the original plan for the next dose.

8、 Medication for special populations

1. Pregnant women: Absolute contraindication, may cause fetal malformation.

2. Breastfeeding period: It is recommended to stop taking medication or breastfeeding.

3. Children: Safety and efficacy have not been established.

4. Elderly: edema/fluid retention is more likely to occur, which needs close monitoring.

9、 Adverse reactions

1. Common (≥ 2%): edema/fluid retention (9.1%), anemia (3.7%).

2. Serious risks: hepatotoxicity, decreased hemoglobin, reduced sperm count.

10、 Contraindications

1. Pregnancy.

2. Allergic to Apuxitan or any excipients.

11、 Drug interactions

1. UGT inducers (such as rifampicin): may reduce the blood concentration of Apuxitan.

2. CYP3A4/CYP2C family inhibitors: caution should be exercised when using them in combination.

3. There is no significant interaction with midazolam (CYP3A4 substrate) and rosuvastatin (BCRP substrate).

12、 Storage method

Store at 20 ° C-25 ° C (allowing fluctuations of 15 ° C-30 ° C), keep the original packaging away from light and moisture, and retain the desiccant after opening.

Aprocitentaninformation