Bosentan

Category: pharmacological

Aliases: Tracleer

Pharmacological Mechanism

Dual endothelin-A + B receptor antagonist — blocks vasoconstrictive + proliferative effects of endothelin-1 on pulmonary vasculature. Approved for pulmonary arterial hypertension. Hepatotoxicity (REMS program) + teratogenicity. Strong CYP3A4 inducer.

Half-Life (t½)

PO: 5h

Dosing Guidelines

• PO: Typical 125mg (Range: 62.5 - 125 mg)

Target Organ Systems

• cardiovascular
• respiratory
• digestive

Interactions

• Simvastatin
• Sildenafil
• Hormonal contraceptives