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Pharmacological action of Tracleer 62,5 mg:

It is a nonselective antagonist of ETA and ETV endothelin receptors. Endothelin 1 (ET1) – a powerful vasoconstrictor, which can bind with ETA and ETV receptors, located in the endothelium and vascular smooth muscle cells and thus, it induces fibrosis, cellular proliferation, hypertrophy and myocardial remodeling, exhibits proinflammatory activity. The concentration of ET1 in tissues and blood plasma increases in some cardiovascular diseases and connective tissue diseases, including pulmonary hypertension, scleroderma, acute and chronic CH, myocardial ischemia, hypertension and atherosclerosis.
Tracleer competitively blocks ЕТ1 receptors and is not bind with other receptors. It reduces the resistance of the systemic and pulmonary vessels that leads to increase of cardiac output without increasing heart rate.

Method of application and dosage

Tracleer 62,5 mg is taken in the morning and evening, regardless of meal. The initial dose of 62.5 mg is taken 2 times a day for 4 weeks, and then the dose is increased to the supportive one – 125 mg 2 times a day.
If you notice the clinical deterioration (with a decrease of walking distance during 6-minute test in at least 10% compared with the baseline), it is necessary to consider alternative ways of treatment despite the use of the drug for at least 8 weeks (at least 4 weeks with the recommended dose). Some patients, who have not had a therapeutic response after 8 weeks of reception, may observe the effect after additional 4-8 weeks. If you have made a decision to stop taking the drug, the dose is gradually canceled with the use of alternative therapy. If you notice clinical deterioration in a few months after the start of therapy, it is necessary to consider the feasibility of its continuation despite the use of the drug. In some patients who do not have a positive effect when taking 125 mg 2 times a day, tolerance to physical activity may improve with increasing doses up to 250 mg 2 times a day, but it is necessary to weigh the risk/benefit ratio for the patient taking into account the fact that hepatotoxicity is dose-dependent. If you want to avoid deterioration of the clinical condition due to the possible withdrawal syndrome, it is necessary to reduce the dose gradually, reducing it by half for 3-7 days, under the supervision of a doctor.
The initial dose for children weighing 10-20 kg is 31.25 mg 1 time a day for 4 weeks, supporting dose -31.25 mg 2 times a day; the initial dose in case of weight of 20-40 kg is 31.25 mg 2 times a day, supporting dose – 62.5 mg 2 times a day; the initial dose in case of weight over 40 kg is 62.5 mg 2 times a day, supporting dose – 125 mg 2 times a day.
Experience of reception in patients with low body weight (less than 40 kg) is limited.

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