Endobloc 5 And Endobloc 10 Tablet

ENDOBLOC 5 mg Tablets

Each film-coated tablet contains:

Ambrisentan IP ..................... 5 mg

COLOURS: Lake Ponceau 4R and Titanium Dioxide IP

ENDOBLOC 10 mg Tablets

Each film-coated tablet contains:

Ambrisentan IP ................... 10 mg

COLOURS: Lake Ponceau 4R and Titanium Dioxide IP

Ambrisentan is an orally active, propanoic acid-class, endothelin-receptor antagonist (ERA), selective for the endothelin A (ETA) receptor. Endothelin plays a significant role in the pathophysiology of pulmonary arterial hypertension (PAH). Ambrisentan is a potent (Ki 0.016 nM) and highly selective ETA antagonist (approximately 4,000-fold more selective for ETA as compared to ETB). Ambrisentan blocks the ETA receptor subtype, localized predominantly on vascular smooth muscle cells and cardiac myocytes. This prevents endothelin-mediated activation of second messenger systems that result in vasoconstriction and smooth muscle cell proliferation. The selectivity of ambrisentan for the ETA over the ETB receptor is expected to retain ETB receptor-mediated production of the vasodilators, nitric oxide and prostacyclin.