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Bosentan

Published: July 26, 2026Updated: August 24, 2026

Bosentan Anhydrous is a dual endothelin receptor antagonist used primarily to treat pulmonary arterial hypertension (PAH) and to prevent new digital ulcers in patients with systemic sclerosis. It works by blocking the action of endothelin-1, a substance that causes blood vessels to narrow and contributes to the abnormal tissue growth seen in these conditions.

Quick summary

Endothelin receptor antagonist for pulmonary hypertension and systemic sclerosis-related ulcers.

Medically reviewed by WellAlly Editorial TeamLast reviewed August 24, 2026Editorial policy

Key facts at a glance

RxNorm
1468845
Generic
Bosentan Anhydrous
Class
pin-variant
Brands
—
Availability
rx
Lactation
unknown
Routes
—
Forms
—
Regions
US, EU, CN, JP
Monitoring
—

This page is for informational purposes only.

Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.

Dosage and administration

adult (standard)tablet
Usual dose
500mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
pediatric (standard)tablet
Usual dose
250mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
geriatric (standard)tablet
Usual dose
400mg daily
Maximum
consult physician
Frequency
once daily
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard

Overdose information

Important overdose information
Toxic dose: Single dose that may cause serious toxicity, significantly exceeding the maximum recommended daily dose of 250mg
Chronic overdose: Prolonged use exceeding recommended dosing leading to cumulative liver toxicity
Immediate actions
Gastric lavage within 1-2 hours if ingestion was recent, activate charcoal, provide supportive care, monitor liver function
Antidote
No specific antidote exists; treatment is supportive and symptomatic(Supportive care is the primary treatment approach)
Poison Control: 1-800-222-1222

Special Populations

9 groups
✗

pregnancy

first trimester
contraindicated
FDA Category
X
Dose Adjustment

avoid use completely

Key Recommendations

do not use during pregnancy - contraindicated due to teratogenic potential

Monitor

pre-pregnancy counseling required, discontinue before conception if possible

Use of this medication in this population requires careful consideration of risks and benefits.

✗

pregnancy

second trimester
contraindicated
FDA Category
X
Dose Adjustment

avoid use completely

Key Recommendations

discontinue immediately if pregnancy detected

Monitor

regular fetal ultrasound monitoring

Use of this medication in this population requires careful consideration of risks and benefits.

✗

pregnancy

third trimester
contraindicated
FDA Category
X
Dose Adjustment

avoid use completely

Key Recommendations

discontinue before delivery when possible

Monitor

fetal monitoring until delivery

Use of this medication in this population requires careful consideration of risks and benefits.

✗

lactation

breastfeeding
unsafe
FDA Category
X
Dose Adjustment

avoid breastfeeding

Key Recommendations

do not breastfeed during treatment - bosentan excreted in milk

Monitor

infant monitoring for potential adverse effects

Use of this medication in this population requires careful consideration of risks and benefits.

⚠

geriatric

elderly
caution
FDA Category
N
Dose Adjustment

start at lower end of dosing range

Key Recommendations

use with caution due to potential increased sensitivity in elderly

Monitor

monitor liver function and blood pressure regularly

Use with caution and monitor for adverse effects.

⚠

pediatric_age

children adolescents
caution
FDA Category
X
Dose Adjustment

weight-based dosing required

Key Recommendations

approved for use in pediatric patients with PAH; monitor growth and development

Monitor

regular liver function tests, hemoglobin monitoring, growth tracking

Use with caution and monitor for adverse effects.

✓

renal_impairment

mild to moderate
safe
FDA Category
N
Dose Adjustment

no significant adjustment needed

Key Recommendations

use standard dosing in mild to moderate renal impairment

Monitor

monitor renal function periodically

⚠

hepatic_impairment

mild
caution
FDA Category
X
Dose Adjustment

use with caution, monitor closely

Key Recommendations

use only if benefits outweigh risks in mild hepatic impairment

Monitor

frequent liver function monitoring required

Use with caution and monitor for adverse effects.

✗

hepatic_impairment

moderate to severe
contraindicated
FDA Category
X
Dose Adjustment

avoid use completely

Key Recommendations

contraindicated in moderate to severe hepatic impairment

Monitor

baseline and periodic liver function assessment

Use of this medication in this population requires careful consideration of risks and benefits.

Statistics and clinical data

drug_classWHO
2023

Drug class

Value:Endothelin receptor antagonist

Dual endothelin receptor antagonist (ERA)

prescribingFDA
2023

FDA approval year

Value:2001

FDA approval for pulmonary arterial hypertension

usageMedical guidelines
2023

Primary indications

Value:Pulmonary arterial hypertension, Systemic sclerosis

Main therapeutic indications

mechanismFDA
2023

Mechanism of action

Value:Dual endothelin-1 receptor antagonist

Blocks endothelin receptors ET-A and ET-B

Treatment of pulmonary arterial hypertension (WHO Group 1) to improve exercise capacity and delay clinical worsening; also used to reduce new digital ulcers in patients with systemic sclerosis (scleroderma).

Dual endothelin receptor antagonist that blocks both ETA and ETB receptors, preventing endothelin-1 from binding and causing vasoconstriction and smooth muscle proliferation in pulmonary arteries.

Requires monthly liver function monitoring due to hepatotoxicity risk. Contraindicated in pregnancy (teratogenic) and in patients with moderate-to-severe hepatic impairment. Must verify negative pregnancy status before and during treatment. May cause fluid retention and anemia.

Contraindications

Conditions and patient states where this medication should be avoided or used with caution.

Do not use (1)

ABSOLUTEhypersensitivity

Known allergy to this medication or its components

Use caution (1)

RELATIVEpregnancy

Consult healthcare provider for benefits vs risks assessment

Official drug label

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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.

Medical Disclaimer

This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.

If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.

Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy