Maxititan

Special attention must be paid to embryo-fetal toxicity during the use of macitentan. Women of childbearing age must rule out pregnancy before treatment and take effective contraceptive measures during treatment and for at least one month after discontinuation of treatment.

1. Drug name

1. Generic name: Macitentan;

2. Trade name: Opsumit®.

2. Indications

Macitentan is an endothelin receptor antagonist (ERA), used to treat pulmonary arterial hypertension (PAH, WHO Class I) to delay disease progression.

3. Specifications and properties

1. Specifications: 10mg

2. Properties: Tablets

4. Main ingredients

Active ingredient: Macitentan (chemical name: N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfonamide).

5. Usage and Dosage

1. Recommended dose: 10 mg orally, once a day.

2. How to take the medicine: Swallow the whole tablet before or after meals.

3. Treatment of missed doses: If you remember to take a missed dose on the same day, you can take it again at the original time the next day.

VI. Dose adjustment

1. Abnormal liver function: Pause when ALT/AST>3 times the upper limit, and consider reducing the dosage after recovery.

2. Decreased hemoglobin: Use with caution in patients with severe anemia (Hb<10g/dL).

7. Medication Precautions

1. Pregnancy risk : Women need to take a pregnancy test before treatment, every month during treatment and 1 month after stopping the drug, and take two kinds of contraceptive measures.

2. Monitoring requirements : Baseline and regular checks of liver function and hemoglobin.

3. Vomiting treatment : If you vomit after taking the medicine, there is no need to take more.

8. Medication for special groups

1. Pregnant women : Contraindicated, it may cause fetal malformation.

2. During lactation : Discontinue medication or stop breastfeeding.

3. Children and the elderly : The safety and effectiveness are not clear; elderly patients do not need to adjust the dose.

9. Adverse reactions

1. Common (≥3%): Anemia (13%), nasopharyngitis (20%), bronchitis (12%), headache (14%), influenza (6%), urinary tract infection (9%).

2. Serious reactions: Hepatotoxicity, pulmonary edema (PVOD), and sperm count.

10. Contraindications

Contraindicated for pregnant women.

11. Drug interactions

1. Strong CYP3A4 inducers (such as rifampin) : Significantly reduce macitentan exposure and avoid combined use.

2. Strong CYP3A4 inhibitors (such as ketoconazole, ritonavir) : Increase macitentan exposure and avoid combined use.

12. Storage method

1. Storage temperature: 20-25°C (68-77°F), 15-30°C (59-86°F) allowed for short periods.

2. Keep the original packaging and avoid moisture and light.