Bosentan Monohydrate

Generic Name

Bosentan Monohydrate

Other Names

• Bosentan Hydrate

Drug Class

• Endothelin Receptor Antagonist

Chemical Formula

C27H29N5O6S

Molecular Weight

551.619 g/mol

Mechanism of Action

• Blocks endothelin receptors ETA and ETB

Indications

• Pulmonary arterial hypertension

Common Dosage Forms

• Tablet

Typical Dosage

• 62.5 mg twice daily, up to 125 mg twice daily

Pediatric Dosage

• Not established

Geriatric Dosage

• Adjust dosing based on renal function

Side Effects

• Headache
• Flushing
• Edema
• Hepatotoxicity

Contraindications

• Hypersensitivity to bosentan
• Pregnancy

Pregnancy Category

• Category X

Lactation Safety

• Not recommended

Drug Interactions

• Cyclosporine
• Warfarin
• Sildenafil

Overdose Symptoms

• Hypotension
• Bradycardia
• Headache

Antidote for Overdose

• No specific antidote, manage symptoms

Storage Conditions

• Store at room temperature away from moisture and heat

Pharmacokinetics

• Absorption: Rapid and almost complete
• Distribution: Extensively bound to plasma proteins
• Metabolism: Primarily hepatic via CYP3A4
• Excretion: Mainly in feces

Precautions

• Monitor liver function tests regularly
• Use contraception during treatment

Warnings

• Risk of hepatotoxicity
• Risk of birth defects if used during pregnancy

Others

• Requires monthly liver function testing during treatment