1 tabl contains 2.5 mg, 5 mg or 10 mg of Amlodipine in the form of besilate.
Action:
Calcium antagonist from the group of dihydropyridine derivatives. Amlodipine inhibits the influx of Calcium ions across the cell membrane into the smooth muscle cells of blood vessels and cardiac muscle cells. It has antihypertensive effect by reducing vascular smooth muscle tone. In angina it has a bi-directional effect: it expands the peripheral arterioles and thus reduces the total peripheral resistance (afterload) and expands the main arteries and coronary arterioles. After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract, reaching Cmax within 6-12 h. Bioavailability is 64-80% (food does not affect bioavailability). It binds to plasma proteins in about 98%. To a large extent, it is metabolized in the liver to inactive metabolites. 10% of amlodipine is excreted in the urine unchanged and 60% in the form of metabolites. It is not removed by dialysis. T0,5 is 35-50 h. In patients with hepatic impairment and in the elderly, the half-life is prolonged and the AUC increased.
Contraindications:
Hypersensitivity to Amlodipine, other dihydropyridine derivatives or other components of the preparation. Severe hypotension. Shock (including cardiogenic shock). Narrowing the outflow path from the left ventricle (eg high grade aortic stenosis). Haemodynamically unstable heart failure after having acute myocardial infarction.
Precautions:
The safety and efficacy of amlodipine at hypertensive crisis has not been established. Caution in patients with heart failure (patients with NYHA class III and IV heart failure, an increase in pulmonary edema), congestive heart failure (increased risk of cardiovascular events and death), and in elderly patients when increasing the dose. Caution should be exercised in patients with impaired hepatic function, both during initiation of therapy and during dose escalation. There are no data on the efficacy and safety of the preparation in children under 6 years of age.
Pregnancy and lactation:
The safety of the medicine in pregnant women has not been established. It can only be used during pregnancy if another safe drug can not be used or if the disease is associated with a higher risk for the mother and the fetus. It is not known whether amlodipine is excreted in human milk; When deciding to continue or terminate breastfeeding or to continue or discontinue treatment with amlodipine, the benefits of breastfeeding for the child and the benefits of amlodipine treatment for the mother should be considered. In some patients treated with calcium channel antagonists, reversible biochemical changes were observed in the sperm heads.
Orally. Adults: the starting dose for both hypertension and ischemic heart disease is 5 mg once a day; the dose can be increased up to a maximum of 10 mg daily, depending on the clinical effect. In patients with hypertension, the preparation was used simultaneously with thiazide diuretics, α- and β-blockers and ACE inhibitors. In patients with angina pectoris, the product may be used alone or in combination with other anti-anginal medications in patients with nitrate resistant angina and / or appropriate doses of beta blocking drugs. The simultaneous use of thiazide diuretics, β-blockers and ACE inhibitors does not require modifying the dose of amlodipine. No dose adjustment is required in patients with impaired renal function. In patients with impaired liver function, the starting dose should be as low as possible of all available. In elderly patients, the usual dose is recommended; however, caution should be exercised when increasing the dose. Children 6-17 years: for the treatment of hypertension, the starting dose is 2.5 mg once a day, if you do not achieve the desired blood pressure after 4 weeks, it can be increased to 5 mg a day. Doses> 5 mg per day have not been studied in children and adolescents.
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