What is the mechanism of action of bosentan?
What is the mechanism of action of bosentan?
The mechanism of action of bosentan is competitive inhibition of endothelin-1 receptors. Endothelin-1 is a potent vasoconstrictor, which also mediates cell proliferation, fibrosis and inflammation.
What is bosentan used for?
Bosentan is used to treat pulmonary arterial hypertension (PAH, high blood pressure in the vessels that carry blood to the lungs) in adults and children 3 years of age and older. Bosentan may improve the ability to exercise and slow the worsening of symptoms in patients with PAH.
Does bosentan cause hypotension?
Conclusions: An endothelin-receptor antagonist, bosentan, significantly lowered blood pressure in patients with essential hypertension, suggesting that endothelin may contribute to elevated blood pressure in such patients.
What is generic for Tracleer?
Teva’s generic of Tracleer® Tablets: Bosentan Tablets.
How much does Tracleer cost?
The cost for Tracleer oral tablet 62.5 mg is around $6,081 for a supply of 30, depending on the pharmacy you visit….Oral Tablet.
| Quantity | Per unit | Price |
|---|---|---|
| 30 (3 x 10 each) | $202.71 | $6,081.20 |
| 60 | $202.55 | $12,152.89 |
Is bosentan pulmonary hypertension?
Bosentan is an oral medication classified as an endothelin receptor antagonist (ERA) which is approved for the treatment of pulmonary arterial hypertension (PAH) in World Health Organization (WHO) Group 1 patients. The goal of this therapy is to improve exercise ability and slow progression of the disease.
What is the brand name of bosentan?
Bosentan From Wikipedia, the free encyclopedia Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH). Bosentan is available as film-coated tablets (62.5 mg or 125 mg) or as dispersable tablets for oral suspension (32 mg).
What is bosentan used to treat?
From Wikipedia, the free encyclopedia Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH). Bosentan is available as film-coated tablets (62.5 mg or 125 mg) or as dispersable tablets for oral suspension (32 mg).
What is bosentan a substrate of?
Bosentan is a substrate of CYP3A4 and CYP2C9. CYP2C19 may also play a role in its metabolism. It is also a substrate of the hepatic uptake transporter organic anion-transporting polypeptides ( OATPs) OATP1B1, OATP1B3, and OATP2B1. Elimination of bosentan is mostly hepatic, with minimal contribution from renal and fecal excretion.
What is the pathophysiology of bosentan elimination?
Elimination of bosentan is mostly hepatic, with minimal contribution from renal and fecal excretion. Use of bosentan with cyclosporine is contraindicated because cyclosporine A has been shown to markedly increase serum concentration of bosentan.