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Active ingredients
Amlodipine
Release form
Pills
Composition
1 tab. Amlodipine (in the form of besylate) 5 mg. Excipients: lactose monohydrate - 63.
Pharmacological effect
A derivative of dihydropyridine is a blocker of slow calcium channels. It has antihypertensive and antianginal effect. Blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes). The antihypertensive effect is due to the direct vasodilating effect on vascular smooth muscle. It has a long dose-dependent antihypertensive effect. Amlodipine reduces myocardial ischemia (has antianginal effect) in two ways: 1) expands the peripheral arterioles and thus reduces congestive heart disease, reduces afterload on the heart, while the heart rate remains almost unchanged, which leads to a decrease in energy consumption and myocardial oxygen demand. 2) expands the coronary and peripheral arteries and arterioles in unchanged and ischemic areas of the myocardium, which increases the oxygen supply to the myocardium (especially for vasospastic angina), reduces the severity of myocardial ischemia and prevents the development of a spasm of the coronary arteries (including caused by smoking). In case of arterial hypertension, a single dose provides a clinically significant reduction in blood pressure for 24 hours (in the patient's position "lying" and "standing"). Due to the slow onset of action, amlodipine does not cause a sharp decrease in blood pressure. It does not reduce exercise tolerance and left ventricular ejection fraction. In patients with angina, a single daily dose of amlodipine increases exercise time, slows the development of angina and ischemic depression of the ST segment (by 1 mm), reduces the frequency of strokes and consumption of nitroglycerin and other nitrates. Reduces the degree of hypertrophy of the left ventricular myocardium, has anti-atherosclerotic and cardioprotective effect in IHD. In patients with coronary artery disease (including coronary atherosclerosis with a lesion of one vessel and up to stenosis of three or more arteries and atherosclerosis of the carotid arteries) who have suffered a myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (PLA), or suffering from angina pectorisamlodipine prevents the development of thickening intima-media carotid arteries significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, PTCA, coronary artery bypass surgery, reduces the number of hospitalizations for unstable angina and progression of chronic heart failure, reduces the frequency of interventions to restore coronary blood flow. Amlodipine does not increase the risk of death or the development of complications leading to death in patients with chronic heart failure (III-IV functional class according to the classification of the New York Heart Association (NYHA)) during therapy with digoxin, diuretics and ACE inhibitors. In patients with chronic heart failure (III-IV functional class according to the NYHA classification) of non-ischemic etiology when using amlodipine, there is a likelihood of pulmonary edema. Does not affect the contractility and conductivity of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. It does not adversely affect the metabolism and the concentration of lipids in the blood plasma and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. The onset of the effect of the drug - 2-4 hours, the duration of the effect - 24 hours. With long-term therapy, the maximum reduction in blood pressure occurs 6-12 hours after taking amlodipine inside. If, after long-term treatment, amlodipine is withdrawn, an effective reduction in blood pressure persists for 48 hours after the last dose. Then the blood pressure indicators gradually return to the initial level within 5-6 days.
Indications
- arterial hypertension (monotherapy or in combination with other antihypertensive drugs) - stable exertional angina, vasospastic angina (Prinzmetal's angina) (monotherapy or in combination with other antianginal drugs).
Contraindications
- severe hypotension (systolic blood pressure less than 90 mm Hg) - cardiogenic shock - acute myocardial infarction during the first 28 days - unstable angina (with the exception of Prinzmetal vasospastic / angina pectoris) - outflow tract obstructionleft ventricular (including clinically significant aortic stenosis) - age up to 18 years - lactose intolerance, lactase deficiency, glucose-galactose malabsorption - hypersensitivity to amlodipine, other derivatives of dihydropyridine and other components of the drug. With caution: abnormal liver function, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of functional class III-IV according to NYHA classification, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, elderly age.
Use during pregnancy and lactation
The safety of use of amlodipine during pregnancy has not been established, therefore, use during pregnancy is possible only when the use of the drug for the mother outweighs the potential risk to the fetus. There is no evidence of excretion of amlodipine in breast milk. However, it is known that other blockers of slow calcium channels, dihydropyridine derivatives, are excreted in breast milk. In this connection, if necessary, the appointment of the drug Amlorus. during lactation should decide on the termination of breastfeeding. Women of childbearing age should use reliable methods of contraception.
Side effects
The frequency of adverse reactions is understood: very often (& # 8805 .1 / 10). often (& # 8805 .1 / 100, less than 1/10). infrequently (& # 8805 .1 / 1000, less than 1/100). rarely (& # 8805 .1 / 10 000, less than 1/1000). very rarely (less than 1/10 000), including individual messages. Since the cardiovascular system: often - peripheral edema (ankles and feet), palpitations, sensation of heat and "tides" of blood to the skin of the face. infrequently - excessive decrease in blood pressure, orthostatic hypotension, vasculitis. rarely - the development or aggravation of the course of chronic heart failure. very rarely - cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain. From the side of the central nervous system: often - fatigue, dizziness, headache, drowsiness, migraine. infrequently - general malaise, fainting, increased sweating, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety. rarely - convulsions, apathy, agitation. very rarely - ataxia, amnesia.On the part of the senses: infrequently - ringing in the ears, visual disturbances, eye pain, diplopia, xerophthalmia, conjunctivitis, accommodation disturbance, taste perversion. very rarely - parosmia. On the part of the digestive system: often - abdominal pain, nausea. infrequently - vomiting, constipation, flatulence, dyspepsia, diarrhea, anorexia, dryness of the oral mucosa, thirst. rarely - gingival hyperplasia, increased appetite. very rarely - gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of hepatic transaminases, hepatitis. From the urinary system: infrequently - frequent urination, painful urination, nocturia, impotence. very rarely - dysuria, polyuria. On the part of the respiratory system: infrequently - shortness of breath, rhinitis, nosebleeds. very rarely - cough. On the part of the musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia, back pain, arthrosis. rarely - myasthenia. On the part of the skin: infrequently - alopecia. rarely - dermatitis. very rarely - a violation of skin pigmentation, xerodermia. From the side of blood-forming organs: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia. On the part of metabolism: very rarely - hyperglycemia. Allergic reactions: rarely - pruritus, rash. very rarely - angioedema, erythema multiforme, urticaria. Other: infrequent - gynecomastia, increase / decrease in body weight, chills. very rarely - cold sweat.
special instructions
The frequency of adverse reactions is understood: very often (& # 8805 .1 / 10). often (& # 8805 .1 / 100, less than 1/10). infrequently (& # 8805 .1 / 1000, less than 1/100). rarely (& # 8805 .1 / 10 000, less than 1/1000). very rarely (less than 1/10 000), including individual messages. Since the cardiovascular system: often - peripheral edema (ankles and feet), palpitations, sensation of heat and "tides" of blood to the skin of the face. infrequently - excessive decrease in blood pressure, orthostatic hypotension, vasculitis. rarely - the development or aggravation of the course of chronic heart failure. very rarely - cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain. From the side of the central nervous system: often - fatigue, dizziness, headache, drowsiness, migraine. infrequently - general malaise, fainting, increased sweating, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety. rarely - convulsions, apathy, agitation. very rarely - ataxia, amnesia.On the part of the senses: infrequently - ringing in the ears, visual disturbances, eye pain, diplopia, xerophthalmia, conjunctivitis, accommodation disturbance, taste perversion. very rarely - parosmia. On the part of the digestive system: often - abdominal pain, nausea. infrequently - vomiting, constipation, flatulence, dyspepsia, diarrhea, anorexia, dryness of the oral mucosa, thirst. rarely - gingival hyperplasia, increased appetite. very rarely - gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of hepatic transaminases, hepatitis. From the urinary system: infrequently - frequent urination, painful urination, nocturia, impotence. very rarely - dysuria, polyuria. On the part of the respiratory system: infrequently - shortness of breath, rhinitis, nosebleeds. very rarely - cough. On the part of the musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia, back pain, arthrosis. rarely - myasthenia. On the part of the skin: infrequently - alopecia. rarely - dermatitis. very rarely - a violation of skin pigmentation, xerodermia. From the side of blood-forming organs: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia. On the part of metabolism: very rarely - hyperglycemia. Allergic reactions: rarely - pruritus, rash. very rarely - angioedema, erythema multiforme, urticaria. Other: infrequent - gynecomastia, increase / decrease in body weight, chills. very rarely - cold sweat.