Pharm

Aprocitentan

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Aprocitentan, Tryvio

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