Dangerous Drug: Bosentan(bow sen’ tan)
Tracleer
PREGNANCY CATEGORY X
Drug Classes
Endothelin receptor antagonist
Pulmonary antihypertensive
Vasodilator
Therapeutic Actions
Specifically blocks receptor sites for endothelin ETA and ETB in the endothelium and vascular smooth muscles; these endothelins are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension.
Indications
Treatment of pulmonary arterial hypertension in patients with World Health Organization class II to class IV symptoms, to improve exercise ability and to decrease the rate of clinical worsening
Unlabeled uses: Prevention of Raynaud’s phenomenon; prevention of digital ulcers in systemic sclerosis
Contraindications and Cautions
Contraindicated with allergy to bosentan, severe liver impairment, pregnancy, lactation.
Use cautiously with hepatic impairment, anemia.
Available Forms
Tablets—62.5, 125 mg
Dosages
Adults and children older than 12 yr
62.5 mg PO bid for 4 wk. Then, for patients weighing 40 kg or more, maintenance dose is 125 mg PO bid. For patients weighing less than 40 kg, but older than 12 yr, maintenance dose is 62.5 mg PO bid. Administer in the morning and evening. Discontinue 36 hr before initiating ritonavir therapy; if patient has been on ritonavir for at least 10 days, initiate bosentan at 62.5 mg/day PO or once every other day.
Pediatric patients
Safety and efficacy not established.
Patients with hepatic impairment
Avoid use in moderate to severe hepatic impairment; reduce dosage and monitor patients closely with mild hepatic impairment. If ALT/AST is more than 3 to 5 or less times the upper limit of normal (ULN), reduce dose to 62.5 mg PO bid or interrupt treatment. Restart treatment only if liver enzyme levels return to pretreatment levels. Stop treatment if ALT/AST is more than 5 to 8 times ULN.
Pharmacokinetics
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