Hypertension. Chronic, stable angina. The systolic Prinzmetal type angina pectoris.
Composition:
1 tabl contains 5 mg or 10 mg of Amlodipine in the form of besilate.
Action:
A drug from the group of Calcium antagonists, a dihydropyridine derivative. It selectively inhibits the inflow of calcium ions to the smooth muscle cells of the walls of the blood vessels and the heart muscle. Amlodipine reduces the total resistance of blood flow through the peripheral part of the circulatory system, the post-load loading of the heart without causing reflex tachycardia, thus reducing the heart's oxygen demand. Amlodipine also has been shown to prevent spasm and restore blood flow in the arteries and coronary arterioles. The dilation of the coronary arteries increases the blood supply to the heart muscle. These mechanisms cause the antianginal effect of amlodipine. In hypertensive patients, it causes vasodilatation, which reduces blood pressure in the standing and lying position. In patients with angina, amlodipine increases exercise tolerance, reduces the incidence of angina, and also reduces the dose of sublingually administered nitroglycerine. Amlodipine does not adversely affect the lipid profile. After oral administration, the maximum concentration in the blood occurs after 6-12 h. The bioavailability is 64-80% (food does not affect the bioavailability of the drug). It is extensively converted into inactive metabolites in the liver. It binds to plasma proteins in 97.5%. The elimination of the drug is two-phase, T0,5 is 35-50 h. The stationary blood concentration in the blood occurs after 7-8 days of administration of therapeutic doses. It is excreted in the urine (10% of the drug in unchanged form and 60% of metabolites). In elderly patients and patients with hepatic impairment, the elimination half-life of amlodipine increases.
Contraindications:
Hypersensitivity to Amlodipine, other dihydropyridine derivatives or other components of the preparation. Increased hypotension. Shock (including cardiogenic). Heart failure in the course of acute myocardial infarction (the first 28 days after myocardial infarction). High grade aortic stenosis.
Precautions:
Caution in patients with heart failure - risk of pulmonary edema. In patients with congestive heart failure, amlodipine increases the risk of cardiovascular events and death. Use with caution in liver failure. The safety and efficacy of use in the hypertensive crisis has not been established. There are no data on the use of the drug in children under 6 years of age.
Pregnancy and lactation:
The use of amlodipine in pregnancy is possible only when there is no other safer product, and when the disease is associated with a greater risk for the mother and fetus. It is not known whether amlodipine is excreted in breast milk. The decision to use amlodipine should be made after considering the risks and benefits for the mother and the child.
Side effects:
Common: drowsiness, dizziness and headache, palpitations, redness of the face, abdominal pain, nausea, swelling of the ankles, swelling, fatigue. Uncommon: insomnia, mood changes, anxiety, depression, tremor, disorder, taste, fainting, hypoaesthesia, hyperaesthesia, visual disturbances, tinnitus, hypotension, shortness of breath, rhinitis, vomiting, indigestion, diarrhea or constipation, dryness in the mouth, alopecia, purpura, skin discoloration, increased sweating, pruritus, rash, skin eruption, arthralgia and muscle pains, muscle spasms, back pain, disturbances of micturition, bedwetting, increased frequency of small amounts of urine, impotence, gynecomastia, chest pain, weakness, pain, malaise, weight gain or loss. Rare: confusion. Very rare: leukocytopenia, thrombocytopenia, hypersensitivity reactions, hyperglycemia, increased tension, peripheral neuropathy, myocardial infarction, bradycardia, ventricular tachycardia, atrial fibrillation, inflammation of the blood vessels, cough, pancreatitis, gastritis, gingival hypertrophy, hepatitis, jaundice , increased activity of liver enzymes (most often associated with cholestasis),angioneurotic edema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, Quinckie edema, hypersensitivity to light. In patients with circulatory insufficiency in the course of coronary disease, an increased incidence of pulmonary edema was observed.
Dosage:
Orally.Adults. Both in the treatment of hypertension and angina, the recommended starting dose is 5 mg once a day, preferably at the same time of the day. The maximum daily dose is 10 mg. No dose adjustment is required in patients with renal insufficiency or in the elderly. Dose adjustment may be necessary in patients with hepatic impairment.Children and adolescents with hypertension aged 6-17 years. The recommended starting dose is 2.5 mg once a day. It can be increased to 5 mg once a day if the desired blood pressure has not been reached after 4 weeks of use. Doses greater than 5 mg daily have not been studied in children and adolescents. The use of amlodipine 2.5 mg is not possible with this preparation.
(C)
