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Mechanism of action.
Ambricentan is an active antagonist of endothelial class receptors of propanoic acid, selective for endothelin receptors of subtype A (ETL). Endothelin plays a significant role in the pathophysiology of pulmonary arterial hypertension (PAH).
The remedy blocks ETA receptors located mainly on the surface of smooth muscle cells of the vessel wall and cardiomyocytes. This allows to prevent endothelin-mediated activation of secondary messenger systems, and leads to vasoconstriction and proliferation of smooth muscle cells.
The selectivity of ambrisent for ETD receptors retains endothelial receptor-mediated subtype B mediated production of vasodilators (nitric oxide and prostacyclin). The using of ambrisental leads to a significant increase in the cardiac index in patients with PAH.
Protocol for the application of Letairis.
The remedy is taken orally, regardless of food intake. The initial dose for adult patients is 5 mg once a day. If the remedy is well tolerated, it is possible to increase the dose to 10 mg once a day.
The effectiveness of using Letairis.
An analysis of the results of placebo-controlled studies showed that when using ambrisental for 12 weeks, there was an improvement in the functional class according to WHO classification in correlation with a decrease in B-natriuretic peptide (BNP) concentration.
Contraindications of Letairis.
Letairis is not recommended for patients with severe impairment of liver function, as well as patients under the age of 18 years. Do not take the remedy during pregnancy and lactation.
Side effects of Letairis.
Common side effects include anemia, headache, increased palpitation, blood tides to the head and upper body, nasal congestion, sinusitis, rhinopharyngitis, abdominal pain, constipation, fluid retention and peripheral edema.
Interaction of Letairis with other remedies.
The dose of the remedy Letairis should be reduced to 5 mg once a day when combined with Cyclosporine due to an increase in the Cmax and AUC0-t values ambrisent against the background of repeated use of Cyclosporin A. Studies of the interaction of ambrisent with other remedies have not revealed any clinically significant results.