Introduction:
Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension (PAH).
Mechanism of Action :
Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes constriction of the pulmonary blood vessels. By blocking this interaction, bosentan decreases pulmonary vascular resistance
Uses :
Bosentan is used to treat people with moderate pulmonary arterial hypertension and to reduce the number of digital ulcers — open wounds on especially on fingertips and less commonly the knuckles in people with systemic scleroderma.
It efficiently improves exercise tolerance and patients quality of life.
There is improved survival rate in PAH patients on long term treatment.
Also,progression of PAH is stopped effectively by use of Bosentan.
It improves functional class (QoL) on long term use.
It is available as 62.5 and 125 mg tablets.
Side Effects:
In addition to the risk of causing birth defects and of causing liver damage, bosentan has a high risk of causing edema, pulmonary veno-occlusive disease, decreasing sperm counts, and decreases in hemoglobin and hematocrit.
Very common adverse effects (occurring in more than 10% of people) include headache, elevated transaminases, and edema.
Common adverse effects (between 1% and 10% of people) include anemia, reduced hemoglobin, hypersensitivity reactions, skin inflammation, itchiness, rashes, red skin, flushing, fainting, heart palpitations, low blood pressure, nasal congestion, gastro-esophageal reflux disease, and diarrhea.
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