Drug reference

Bosentan

Vasodilator · Pulmonary arterial hypertension agent

Also known as Bosentan monohydrate

VasodilatorPulmonary arterial hypertension agent

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Avoid (teratogenic in animal studies). Effective contraception required during administration (hormonal contraception not considered effective). Monthly pregnancy tests advised.

FDA category + note

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Mechanism

Bosentan is an endothelin antagonist. It binds to and blocks endothelin receptors, preventing the vasoconstrictive effects of endothelin-1. This leads to vasodilation and reduced pulmonary vascular resistance, used primarily in pulmonary arterial hypertension.

Indications

Pulmonary arterial hypertension (initiated under specialist supervision)Systemic sclerosis with ongoing digital ulcer disease (to reduce number of new digital ulcers)PAH with mild-to-severe functional impairment (functional classes II–IV)moderate PAH (functional class II–III)idiopathic or congenital PAH (pediatric population aged 3 years or older)

Dosing

Adult: Pulmonary arterial hypertension: Initially 62.5 mg twice daily by mouth for 4 weeks, then increased to 125 mg twice daily (max. per dose 250 mg). Systemic sclerosis with ongoing digital ulcer disease: Initially 62.5 mg twice daily by mouth for 4 weeks, then increased to 125 mg twice daily.
Hepatic adjustment: Manufacturer advises avoid in moderate-to-severe impairment or if baseline serum transaminases exceed 3 times the upper limit of normal.
Max dose: 500 mg per day (for pulmonary arterial hypertension)

Pharmacokinetics

Half-life

5 h

Metabolism

Metabolized by CYP2C9 and CYP3A4. Taken up in the liver by OATP1B1 and OATP1B3.

Excretion

Excretion of metabolites in the bile.

Contraindications

Acute porphyrias
Systemic systolic blood pressure below 85 mmHg
Pulmonary veno-occlusive disease
Moderate-to-severe hepatic impairment
Baseline serum transaminases exceeding 3 times the upper limit of normal
Pregnancy

Side effects

Common

AnaemiaDiarrhoeaFlushingGastrooesophageal reflux diseaseHeadacheNasal congestionPalpitationsSkin reactionsSyncopepulmonary edemaperipheral edemaanemianasal congestion/pharyngitisitchingedemarespiratory infections

Serious

Hepatic disorders
Leucopenia
Neutropenia
Thrombocytopenia
Angioedema
Vision blurred
embryo-fetal toxicity (potent teratogen, FDA-mandated REMS program)
increased liver transaminases (monitor closely)
testicular atrophy
infertility

Pregnancy & lactation

Pregnancy

Avoid (teratogenic in animal studies). Effective contraception required during administration (hormonal contraception not considered effective). Monthly pregnancy tests advised.

Lactation

Manufacturer advises avoid—no information available.