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 transport of Calcium ions 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. It reduces the hypoxia of the cardiac muscle through two mechanisms: it dilates the peripheral arterioles and thus decreases the peripheral resistance (afterload) - because the heart rate remains unchanged, it reduces energy consumption in the heart muscle and its oxygen demand; expands large arteries and coronary arterioles in both unchanged and altered areas due to ischaemia - thereby increasing the supply of oxygen to the heart muscle in patients with coronary spasm (Prinzmetal's angina). Amlodipine is well absorbed from the gastrointestinal tract, regardless of the presence of food (bioavailability 64-80%). About 97.5% is bound to plasma proteins. It is extensively metabolised in the liver to inactive metabolites. It is mainly excreted in the urine in the form of metabolites (60%) and unchanged (10%). T0,5 in the elimination phase it is about 35-50 h.
Contraindications:
Hypersensitivity to Amlodipine, other dihydropyridines or other components of the preparation. Severe hypotension. Shock (including cardiogenic shock). Haemodynamically unstable heart failure after acute myocardial infarction. Narrowing the outflow path from the left ventricle (eg aortic valve stenosis).
Precautions:
The safety and efficacy of amlodipine at hypertensive crisis has not been studied. Caution in patients with heart failure (patients with NYHA class III and IV heart failure have an increased incidence of pulmonary edema), congestive heart failure (increased risk of future cardiovascular events and death), 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; treatment should start at the lowest recommended dose. In patients with severe hepatic impairment, the dose should be slowly adjusted and adequate control should be provided. There are no data on the use of the preparation in children under 6 years.
Pregnancy and lactation:
The safety of amlodipine in pregnant women has not been established. Use during pregnancy is only recommended if it is not possible to administer another, safer medicine and if the underlying disease poses a greater risk to the mother and the fetus. It is unknown 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 antagonists, reversible biochemical changes in the sperm heads were observed.
Side effects:
Common: drowsiness, dizziness, headache (especially at the beginning of treatment), palpitations, flushing of the face with a feeling of heat, abdominal pain, nausea, swelling of the ankles, swelling, tiredness. Uncommon: insomnia, mood changes (including anxiety), depression, tremor, taste disturbances, fainting, hypoesthesia, paresthesia, visual disturbances (including double vision), tinnitus, hypotension, dyspnoea, rhinitis, vomiting, indigestion, intestinal dysfunction (including diarrhea and constipation), dry mouth, alopecia, purpura, skin discoloration, increased sweating, pruritus, rash, skin eruption, joint pain, muscle pain, muscle cramps, back pain, donor disorder urine, nocturia, frequent urination, impotence, gynecomastia, chest pain, weakness, pain, malaise, weight gain or loss. Rare: confusion.Very rare: leukopenia, thrombocytopenia, hypersensitivity reactions, hyperglycemia, hypertonia, peripheral neuropathy, myocardial infarction, arrhythmia (including tachycardia, ventricular tachycardia and atrial fibrillation), vasculitis, cough, pancreatitis, gastritis, hyperplasia gums, hepatitis, jaundice, increased liver enzymes (in most cases cholestasis), angioneurotic edema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke's edema, hypersensitivity to light. Exceptional cases of extrapyramidal syndrome have been reported.
Dosage:
Orally.Adults: initial dose both in the treatment of hypertension, which angina is 5 mg once a day; the dose can be increased up to a maximum of 10 mg daily, depending on the clinical response. In hypertensive patients, amlodipine is used concomitantly with thiazide diuretics, α- and β-blockers, and ACE inhibitors. In patients with angina pectoris, amlodipine can be used alone or in combination with other antianginal medications in patients with nitrate resistant angina or appropriate doses of β-blockers. The simultaneous use of thiazide diuretics, β-blockers and ACE inhibitors does not require modifying the dose of amlodipine.Children 6-17 years old: for the treatment of hypertension, the initial dose is 2.5 mg once a day, if the target blood pressure has not been reached after 4 weeks, the dose should be increased to 5 mg once a day. Amlodipine has not been studied in children and adolescents at doses> 5 mg / day.Special groups of patients. In patients with mild and moderate hepatic impairment, the dose should be carefully adjusted starting from the lowest recommended dose. Patients with severe hepatic impairment should be given amlodipine, starting with the lowest dose and slowly increasing it. No dose adjustment is required in patients with impaired renal function; amlodipine is not eliminated from the body during dialysis. Elderly patients are usually treated with the usual dose, but caution should be exercised when increasing the dose.
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