Jeraygo (Aprocitentan)

Aprocitentan is used to manage conditions related to the endothelin pathway, primarily resistant hypertension.

• Resistant hypertension: lowers blood pressure when conventional antihypertensive regimens are insufficient.
• Uncontrolled hypertension: provides additional blood pressure reduction in patients with persistent elevated readings.
• Elevated endothelin activity: mitigates vascular constriction associated with high endothelin levels.

• Aprocitentan blocks both endothelin‑A (ETA) and endothelin‑B (ETB) receptors on vascular smooth‑muscle cells and the renal tubular epithelium. By antagonizing these receptors, it prevents endothelin‑mediated vasoconstriction and sodium‑water retention, leading to vasodilation, reduced peripheral resistance, and improved fluid balance, which collectively contribute to lower systemic blood pressure.

Aprocitentan may be associated with several adverse reactions, which are categorized by frequency and severity.

Common Side Effects

• Headache: mild to moderate intensity.
• Peripheral edema: swelling of ankles or lower limbs.
• Dizziness: sensation of light‑headedness.
• Nausea: occasional upset stomach.
• Fatigue: general tiredness.
• Nasal congestion: mild blockage of nasal passages.

Serious or Rare Side Effects

• Liver enzyme elevation: significant increase in ALT or AST.
• Severe hypotension: marked drop in blood pressure requiring medical attention.
• Pulmonary edema: fluid accumulation in the lungs.
• Anemia: reduction in red blood cell count.
• Renal impairment: worsening kidney function.
• Anaphylactic reaction: rare severe allergic response.

When prescribing Aprocitentan, clinicians should observe several precautionary measures to ensure patient safety.

• Blood pressure monitoring: check regularly to avoid excessive hypotension.
• Liver function assessment: evaluate baseline enzymes and repeat as needed.
• Renal function evaluation: monitor creatinine and eGFR, especially in patients with pre‑existing kidney disease.
• Electrolyte balance: watch for changes in sodium and potassium levels.
• Concomitant drug review: avoid combining with other endothelin antagonists or strong CYP3A4 inhibitors.
• Store at room temperature: keep below 25 °C in the original packaging, protect from moisture and direct sunlight.

Aprocitentan can interact with other medicines; some combinations should be avoided while others require careful monitoring.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase aprocitentan exposure.
• Dual endothelin receptor antagonists: additive vasodilatory effect can cause severe hypotension.
• Potassium‑sparing diuretics: risk of hyperkalaemia and fluid overload.

Moderate Interactions (Monitor Closely)

• ACE inhibitors or ARBs: combined effect on blood pressure may require dose adjustment.
• Calcium‑channel blockers: may enhance hypotensive response, necessitate monitoring.