Bosentan
Administration
- Type: Endothelin receptor antagonists
- Dosage Forms: tablet, tablet for oral suspension
- Dosage Strengths: tablet: 62.5, 125 mg; tablet for oral suspension: 32mg
- Routes of Administration: PO
- Common Trade Names: Tracleer
Adult Dosing
- 62.5-125mg PO BID
Pediatric Dosing
Safety/efficacy not established
Special Populations
- Pregnancy Rating: X
- Lactation risk: Infant risk cannot be ruled out
- Renal dosing:
- Hepatic dosing: avoid in moderate-severe disease
Contraindications
- Allergy to class/drug
- Concomitant administration with cyclosporine A or glyburide
- Pregnancy or potential pregnancy
Adverse Reactions
Serious
- Anemia
- Cirrhosis, liver failure
- Oligozoospermia
- Edema, fluid retention
Common
- Anemia
- Respiratory tract infection
Pharmacology
- Half-life: 5h
- Metabolism: Hepatic: via CYP3A4 and CYP2C9
- Excretion: Biliary, renal
Mechanism of Action
- Dual endothelin receptor antagonist, inhibits vasoconstriction → vasodilation