II. Indications
-
Hypertension
- Fourth-line agent in Refractory Hypertension not controlled on 3 other agents
- Requires REMS program (due to Teratogenicity)
III. Contraindications
- Pregnancy
- Stage 5 Chronic Kidney Disease (eGFR <15 ml/min) or Hemodialysis
- Advanced Congestive Heart Failure
- Liver Disease
IV. Mechanism
- Aprocitentan is a Endothelin Receptor Antagonist
- Endothelin is a vasonstrictor and Aldosterone mediator
- Endothelin Receptor Antagonists inhibit endothelin activity, resulting in vasodilation
V. Medications
- Aprocitentan (Tryvio) 12.5 mg tablets
VI. Dosing
- Take 12.5 mg orally once daily with or without food
VII. Adverse Effects
- Peripheral Edema
- Decreased male fertility
- Aprocitentan may decrease Sperm Count
- Liver Function Test Abnormalities
VIII. Safety
- Pregnancy Category X
- Must be enrolled in REMS program to prescribe Aprocitentan
- Women of childbearing age with a Uterus
- Contraception 1 month before, during and 1 month after
- Obtain monthly Pregnancy Test while taking Aprocitentan
- Monitoring
- Liver Function Tests (baseline and periodically)
- Serum Aminotransferase levels (AST, ALT)
- Serum Total Bilirubin
- Liver Function Tests (baseline and periodically)
IX. Resources
- Aprocitentan (DailyMed)