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, thus reducing the total 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 ischemia - this action increases the oxygen supply in patients with coronary spasm (Prinzmetal angina). Amlodipine is well absorbed from the gastrointestinal tract, regardless of the presence of food (bioavailability 64-80%), reaching Cmax during 6-12 h. In about 97.5% it is associated with 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 is about 35-50 h. Patients with hepatic impairment have a reduced clearance of amlodipine.
Contraindications:
Hypersensitivity to Amlodipine, other dihydropyridine derivatives or any of the excipients. Severe hypotension. Shock, including cardiogenic shock. Narrowing of the outflow path from the left heart of the left ventricle (eg severe aortic stenosis). Haemodynamically unstable heart failure after acute myocardial infarction.
Precautions:
The safety and efficacy of amlodipine at hypertensive crisis has not been established. Use with caution: in patients with heart failure (there is an increased risk of cardiovascular events and death in patients with congestive heart failure, and an increase in pulmonary edema has been reported in patients with heart failure in the third and fourth year of NYHA); in elderly patients when increasing the dose; in patients with impaired hepatic function, both during initiation of therapy and during dose escalation (increased amlodipine AUC, prolonged T0,5). There are no data on the efficacy and safety of the preparation in children <6 years.
Pregnancy and lactation:
The safety of amlodipine in pregnant women has not been established. It can only be used during pregnancy if another safer medicine can not be used and the disease is associated with a higher risk for 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 channel antagonists, reversible biochemical changes were observed in the sperm heads.
Side effects:
Common: drowsiness, dizziness, headache (especially at the beginning of treatment), palpitations, redness, abdominal pain, nausea, swelling of the ankles, swelling, fatigue. Uncommon: insomnia, mood disorders (including anxiety), depression, tremor, taste disturbances, fainting, hypoesthesia, paresthesia, visual disturbances (including double vision), tinnitus, hypotension, dyspnea, rhinitis, vomiting, indigestion, intestinal dysfunction (including diarrhea and constipation), dry mouth, alopecia, purpura, hyperpigmentation, increased sweating, pruritus, rash, rash, joint pain, muscle pain, muscle cramps, back pain, urinary disorder , bedwetting, more frequent urination, impotence, gynecomastia, chest pain, asthenia, pain, malaise, weight gain or loss. Rare: confusion.Very rare: leukopenia, thrombocytopenia, hypersensitivity reactions, hyperglycemia, hypertension, peripheral neuropathy, myocardial infarction, arrhythmia (including tachycardia, ventricular tachycardia and atrial fibrillation), vasculitis, cough, pancreatitis, gastritis, hypertrophy gums, hepatitis, jaundice, increased liver enzymes (usually corresponding to stagnation of bile), angioneurotic edema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke's edema, hypersensitivity to light. Isolated 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 patient's individual response. In patients with hypertension, the preparation was used simultaneously with thiazide diuretics, α- and β-blockers and ACE inhibitors. In patients with angina, the product may be used alone or in combination with other anti-angina medicines. 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 starting dose is 2.5 mg once a day, if the target blood pressure has not been reached after 4 weeks, it can be increased to 5 mg once a day. Amlodipine has not been studied in children and adolescents at doses above 5 mg daily.Special groups of patients. No dose adjustment is required in patients with impaired renal function; amlodipine is not eliminated from the body during dialysis. In patients with impaired liver function, the starting dose should be as low as possible of all available. Elderly patients are usually treated with the usual dose, but caution should be exercised when increasing the dose.
(C)
