Jeraygo (Aprocitentan)

Jeraygo, an endothelin receptor antagonist, is used in the management of resistant hypertension, a condition where blood pressure remains elevated despite multiple antihypertensive agents.

• Resistant hypertension: lowers systolic and diastolic blood pressure in patients whose hypertension is uncontrolled despite three or more antihypertensive drugs.

• Aprocitentan selectively blocks endothelin‑A (ETA) and endothelin‑B (ETB) receptors on vascular smooth‑muscle cells and renal tubular cells. By inhibiting these receptors, the drug reduces endothelin‑mediated vasoconstriction and sodium‑water retention, leading to decreased peripheral resistance and lower blood pressure.

Aprocitentan may cause a range of adverse reactions, most of which are mild to moderate in severity.

Common Side Effects

• Headache: mild to moderate intensity.
• Peripheral edema: swelling of the lower limbs.
• Flushing: transient warmth and redness of the skin.
• Dizziness or light‑headedness.
• Nasal congestion or sinus discomfort.
• Fatigue or general weakness.

Serious or Rare Side Effects

• Elevated liver enzymes: may indicate hepatic injury.
• Anemia: reduction in hemoglobin levels.
• Severe hypotension: marked drop in blood pressure requiring medical attention.
• Renal impairment: worsening kidney function.
• Pulmonary edema: fluid accumulation in the lungs.

Before initiating therapy, clinicians should assess patient suitability and monitor for potential complications.

• Blood pressure monitoring: check regularly to avoid excessive hypotension.
• Liver function tests: perform baseline and periodic assessments.
• Fluid status: evaluate for signs of edema or fluid overload.
• Renal function: monitor serum creatinine and eGFR.
• Contraindication in severe hepatic impairment: avoid use in patients with marked liver disease.
• Store at room temperature: keep in the original container, protect from moisture and direct sunlight.

Aprocitentan can interact with several drug classes, affecting its efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase plasma concentrations and risk of toxicity.
• Co‑administration with other endothelin receptor antagonists: additive vasodilatory effects can cause severe hypotension.

Moderate Interactions (Monitor Closely)

• Non‑steroidal anti‑inflammatory drugs (NSAIDs): may blunt antihypertensive response.
• ACE inhibitors or ARBs: combined use can enhance blood‑pressure lowering effect.
• Diuretics: may increase risk of electrolyte disturbances and hypotension.