1 tabl powl. contains 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 direct relaxation effect on the smooth muscle of the vessels. In angina it has bi-directional effects: it expands the peripheral arterioles, which results in a reduction of peripheral resistance and post-traumatic load and extends the main arteries and coronary arterioles. Following oral administration, amlodipine is well absorbed from the gastrointestinal tract, reaching a maximum blood concentration within 6-12 h after administration. Bioavailability is 64-80%. Food does not affect the bioavailability of amlodipine. Amlodipine is approximately 98% bound to plasma proteins. Steady state is achieved after 7-8 days of treatment. Amlodipine is extensively metabolised in the liver to inactive metabolites. It is excreted in the urine in the form of metabolites (60%) and unchanged form (10%). Amlodipine can not be removed from the body by hemodialysis. T0,5 amlodipine is 35-50 h. In patients with impaired liver function and in elderly patients, the half-life is prolonged.
Contraindications:
Hypersensitivity to Amlodipine, other components of the preparation or other dihydropyridine derivatives. Severe hypotension. Shock. Narrowing the outflow pathway from the left ventricle (e.g., clinically significant narrowing of the aortic valve). Unstable angina. It should not be used in patients with heart failure after a recent myocardial infarction during the first 28 days.
Precautions:
Use with caution in patients with heart failure, impaired liver function, severe renal dysfunction undergoing dialysis, and low cardiac reserve. The safety and efficacy of the preparation at hypertensive crisis and in children has not been established.
Pregnancy and lactation:
The drug is contraindicated during pregnancy and breastfeeding. Women of childbearing age treated with amlodipine should use effective contraception.
Side effects:
Very common: swelling of the ankles. Common: drowsiness, pain and / or dizziness, fatigue, weakness, palpitations, flushing of the face with a feeling of heat, shortness of breath, stomach pain, nausea, indigestion. Uncommon: gynecomastia, sleep disturbances, irritability, depression, peripheral neuropathy, malaise, dysgeusia, dry mouth, fainting, hypoaesthesia, paresthesia, increased sweating, blurred vision, tinnitus, tachycardia, chest pain, worsening symptoms of angina (at the beginning of treatment), hypotension, vasculitis, cough, rhinitis, vomiting, diarrhea, constipation, gingival hypertrophy, alopecia, urticaria, skin discoloration, pruritus, rash, muscular and joint pain, muscle cramps, back pain, impaired urination, impotence, weight gain or loss. Rare: confusion, mood changes (including anxiety), hepatitis, jaundice, increased liver enzymes. Very rare: leukopenia, thrombocytopenia, hyperglycemia, tremor, pancreatitis, gastritis, angioneurotic edema. In single cases: myocardial infarction or arrhythmia (including additional spasms, tachycardia, atrial arrhythmias) in patients with coronary artery disease - no causal relationship has been established for these side effects with amlodipine, hypersensitivity reactions (including erythema multiforme, exfoliative inflammation) skin, angioneurotic edema). Severe pulmonary edema may occur in patients with severe heart failure (NYHA stage III and IV).
Dosage:
Orally. Adults: the usual starting dose for the treatment of hypertension and angina is 5 mg once a day (0.5 tabl).If the desired therapeutic effect does not occur within 2-4 weeks, the daily dose can be maximized up to 10 mg once a day. In hypertensive patients, amlodipine can be used on its own or in combination with thiazide diuretics, alpha-blockers, β-blockers or angiotensin converting enzyme inhibitors - in the case of combination therapy, dosage adjustment may be necessary for amlodipine; in the treatment of angina, amlodipine can be given as monotherapy or in combination with nitrates and / or beta blockers. Normally no dose adjustment is necessary for patients with impaired renal function. Elderly patients do not usually need to change their starting dose, but caution should be used when increasing the dose. There are no recommendations regarding the dosage of amlodipine in patients with impaired hepatic function. The tablets should be taken with or without a drink, with a glass of liquid.
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