Drug Index



Mechanism :

It is competitive antagonist of endothelin-1; blocks endothelin receptors on vascular endothelium and smooth muscle resulting in inhibition of vasoconstriction.

Indication :

• Pulmonary arterial hypertension in patients with WHO class III or IV symptoms.

Contraindications :

Hypersensitivity to bosentan or any of the components, concurrent use of cyclosporine or glyburide.

Dosing :

Persistent pulmonary hypertension of the newborn (PPHN):

≥34 weeks gestational age: Oral: Initial 1 mg/kg/dose twice daily; may increase to 2 mg/kg/dose twice daily.

Children 3 years-12 years:

4 to 8 kg: Oral: 16 mg twice daily

>8 to 16 kg: Oral: 32 mg twice daily

>16 to 24 kg: Oral: 48 mg twice daily

>24 to 40 kg: Oral: 64 mg twice daily

Children ≥12 years and Adolescents:

>20 to 40 kg: Initial: 31.25 mg twice daily; increase to a target dose of 62.5 mg twice daily.

>40 kg: Initial: 62.5 mg twice daily; increase to a target dose of 125 mg twice daily.

Adverse Effect :

Elevations in aminotransferases, elevated bilirubin, decrease in hematocrit and hemoglobin, thrombocytopenia. (Monitor hemoglobin initially after a month and then every 3 monthly). Other adverse effects: Flushing, edema, fatigue, hypotension, palpitations, diarrhea, dyspepsia, rash, angioneurotic edema, pruritus, headache, dizziness.

Interaction :

Cyclosporine: Significantly increases serum levels of bosentan.
Glyburide: Concurrent use is contraindicated since it results in an increased risk of serum transaminase elevations.
CYP3A4 Inhibitors (clarithromycin and erythromycin): May increase serum concentrations or effects of bosentan.
CYP2C8/9 inducers (Carbamazepine, Phenytoin, Rifampin) and isoenzyme CYP3A4 inducers (Carbamazepine, Nevirapine): May decrease bosentan serum concentrations or effects.
St. John Wort: The herbal medicine may potentially decrease serum concentrations of bosentan and is not recommended for concurrent use.
Oral Contraceptives: Bosentan significantly decreases the serum concentrations of oral contraceptives.

03/13/2020 19:59:21 Bosentan
ask a doctor
Ask a Doctor
Disclaimer: The information given by www.pediatriconcall.com is provided by medical and paramedical & Health providers voluntarily for display & is meant only for informational purpose. The site does not guarantee the accuracy or authenticity of the information. Use of any information is solely at the user's own risk. The appearance of advertisement or product information in the various section in the website does not constitute an endorsement or approval by Pediatric Oncall of the quality or value of the said product or of claims made by its manufacturer.
0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0