Bosentan
Bosentan is used to treat high blood pressure in a condition called pulmonary arterial
hypertension, which effects the lungs. PAH is a condition that is caused by increased levels
of an endothelin-1 in the body. It reduces the number of open wounds, especially on
fingertips and knuckles. Bosentan is a dual endothelin receptor antagonist, in that it
selectively inhibits the production of the substance Endothelin-1. The goal of Bosentan
therapy is to improve ability to exercise and slow the progression of the disease. Bosentan has
been shown effectiveness mostly in patients with symptoms that were rated as WHO
Functional Class II-III.
In the USA, the European Union and other countries, the license of owned by Actelion
Pharmaceuticals and sold under the trade name Tracleer.
Bosentan was approved for treatment for PAH in the US in 2001and in Europe in 2002.
Forms and Dosage
Bosentan is sold in film-coated tablets in strengths of 62.5 mg or 125 mg. It is also sold as
dispersible tablets for oral suspension of 32 mg. Bosentan is administered as a single dose of
2000 mg/day for 2 months.
Bosentan harms fetuses so pregnant women are not prescribed this medicine, moreover,
women taking Bosentan should not get pregnant. In the US, only doctors who follow an
FDA-mandated risk evaluation and mitigation strategy (REMS) with respect to risks to
fetuses and its risks of causing liver damage are allowed to prescribe it.
The wholesale cost of Bosentan
The average wholesale price is $49.50 per day for both 62.5 mg and 125 mg tablets and
$2,970 per month in the USA. The same dose will cost 1510 pounds in the UK.
The price of Bosentan is significantly lower in the developing world, with the leading Indian
brands costing only USD1 for 20 tablets of the same strength as sold in the USA or UK.
How does Bosentan work?
Bosentan is an antagonist of endothelin-1. When functioning normally, endothelin-1 causes the
pulmonary blood vessels to constrict. Endothelin also causes abnormal growth of the muscle
of the blood vessels in the lungs thus narrowing passages. This increases the pressure
required to push the blood through the lungs to get oxygen. Conversely, Endothelin-1 has
been associated with both vasodilation and vasoconstriction of vascular smooth muscle and
tissue. Bosentan blocks the receptors, causing a total decrease in pulmonary vascular
resistance.
Bosentan blocks off the effects of endothelin-1, which helps lower blood pressure in the
lungs, slow the worsening of symptoms from the disease. Because it can reduce the stress on
the lungs it also improves our ability to exercise and related research studies have verified
this improvement.
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