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.



Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Dose as in normal renal function

Dose in Patients undergoing Renal Replacement Therapies
CAPDNot dialysed. Dose as in normal renal function
HDNot dialysed. Dose as in normal renal function
HDF/High fluxNot dialysed. Dose as in normal renal function
CAV/VVHDNot dialysed. Dose as in normal renal function

Hepatic Dose :

Baseline:
Baseline AST/ALT > 3 times the upper limit of normal (ULN): Use is contraindicated.

On treatment:
AST/ALT > 3 to 5 times ULN: Reconfirm the results by repeating the test. Adults and Adolescents weighing > 40 kg: Reduce the dose to 62.5 mg twice daily or withhold treatment and monitor LFT once every 2 weeks. When levels return to baseline, restart treatment at 62.5 mg twice daily; reassess LFT within 3 days. In children: Withhold treatment. When levels return to baseline, reintroduce bosentan at the dose used prior to treatment interruption; reassess LFT within 3 days.
AST/ALT > 5 to 8 times ULN: Reconfirm the results by repeating the test. Discontinue treatment if confirmed. Monitor LFT once every 2 weeks. When levels return to baseline, restart treatment at 62.5 mg twice daily in adults and adolescents. In children, restart at the dose used prior to treatment interruption. Reassess LFTs within 3 days.
AST/ALT > 8 times ULN or clinical symptoms of hepatotoxicity or bilirubin increases > 2 times ULN: Discontinue treatment permanently.
05/25/2020 01:47:21 Bosentan
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