Generic Name

Aprocitentan

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Classification

FDA Approved Indications

• Treatment of resistant hypertension

Mechanism of Action

Aprocitentan is an endothelin receptor antagonist that blocks the action of endothelin-1, a potent vasoconstrictor, leading to vasodilation and blood pressure reduction.

Dosage and Administration

Adult: Initial dose: 12.5 mg once daily. Dose may be titrated up to 25 mg once daily based on response and tolerability.

Pediatric: Not established.

Geriatric: Use with caution; adjust dosage based on response and tolerability.

Renal Impairment: Adjustments not specified; monitor closely.

Hepatic Impairment: Use with caution; limited data available.

Pharmacokinetics

Absorption: Well absorbed orally.

Distribution: Protein binding approximately 97%.

Metabolism: Primarily hepatic metabolism via CYP3A4.

Excretion: Primarily fecal excretion, minimal renal excretion.

Half Life: Approximately 20-25 hours.

Contraindications

• Hypersensitivity to aprocitentan or any component of the formulation.

Precautions

• Use with caution in patients with hepatic impairment.
• Monitor blood pressure regularly.
• Assess for signs of hypotension.

Adverse Reactions - Common

• Headache (Common)
• Dizziness (Common)
• Peripheral edema (Common)
• Fatigue (Common)

Adverse Reactions - Serious

• Hypotension (Serious)
• Hepatotoxicity (Rare)
• Angioedema (Rare)

Drug-Drug Interactions

• CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase aprocitentan levels.
• Other antihypertensives may have additive effects.

Drug-Food Interactions

• No significant interactions reported.

Drug-Herb Interactions

• Potential interactions with St. John's Wort and other CYP3A4 inducers.

Nursing Implications

Patient/Family Teaching

• Take medication exactly as prescribed.
• Inform about potential side effects like dizziness and headache.
• Rise slowly from sitting or lying position.
• Report any signs of swelling, dizziness, or allergic reactions.

Special Considerations

Black Box Warnings:

• None currently issued.

Genetic Factors: No specific genetic markers identified for response.

Lab Test Interference: None noted.

Overdose Management

Signs/Symptoms: Severe hypotension, dizziness, fainting.

Treatment: Discontinue medication, provide supportive care, and monitor blood pressure. Consider vasopressor support if needed.

Storage and Handling

Storage: Store at room temperature, 20-25°C (68-77°F).

Stability: Stable under recommended storage conditions for the duration of the expiration date.