Drug Index

Bosentan

 
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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.


07/14/2019 19:36:16 Bosentan
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