1 tabl contains 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 effects by dilation of peripheral vessels, with a greater effect on smooth muscle cells in the walls of blood vessels. 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. This increases the supply of oxygen in the myocardium in patients with Prinzmetal angina attacks. After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract, reaching Cmax within 6-9 h. Bioavailability is 60-65% (food does not affect bioavailability). It binds to plasma proteins in over 95%. To a large extent, it is metabolized in the liver to inactive metabolites. It is excreted unchanged (up to 10% of the dose) and as metabolites in the urine (about 60% of the dose) and faeces (20-25% of the dose). It is not removed by dialysis. Renal insufficiency does not affect the pharmacokinetics of amlodipine. T0,5 is 35-45 h. In patients with hepatic impairment and in elderly patients, the half-life is prolonged and the AUC is increased.
Contraindications:
Hypersensitivity to Amlodipine, other dihydropyridines or other components of the preparation. Cardiogenic shock. Unstable angina with the exception of vasospastic form (Prinzmetal). Hypotension. Clinically significant aortic stenosis.
Precautions:
In patients with markedly increased organic changes in the coronary arteries, a worsening of coronary heart disease or a myocardial infarction was observed when initiating treatment or increasing the dose of amlodipine, however, it was not established whether this was causally related to the use of amlodipine. Caution should be exercised in patients with hepatic impairment, with aortic stenosis, severe cardiac insufficiency (NYHA class IV), and patients taking other antihypertensive agents. In clinical trials in patients with advanced heart failure (NYHA III and IV) with non-ischemic etiology, an increased risk of pulmonary edema has been observed, although there are no significant differences in the occurrence of exacerbation of heart failure. There are no data on the safety and efficacy of the medicine in children. The drug should not be sipped with grapefruit juice.
Pregnancy and lactation:
It must not be used during pregnancy unless clearly necessary. It is recommended to discontinue breast-feeding while using amlodipine.
Orally. Adults.Hypertension: the starting dose is usually 5 mg once a day. The maximum daily dose is 10 mg. Elderly patients and patients with hepatic impairment should be started with 2.5 mg once a day. After the initial dose, the dose should be increased gradually and not more often than every 1-2 weeks.In patients who are not normalizing the pressure using the monotherapy drug, it may be beneficial to attach a thiazide diuretic, a beta-blocker or an angiotensin-converting enzyme inhibitor.Stable angina, Prinzmetal anginaThe recommended dose is 5-10 mg once a day. Elderly patients and patients with hepatic impairment are advised to start treatment with 5 mg once a day. Amlodipine can be used in combination with thiazide diuretics, ACE inhibitors, β-blockers, long-acting nitrates, and sublingual nitroglycerine.
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