Amlodipine: instructions for use
ATX Code: C08CA01 (Amlodipine).
Release form: tablets.
Dosage form: biconvex tablets of a round form, white color. One side is smooth, on the other - engraving "AB 5".
Clinico-pharmacological group: a slow calcium channel blocker.
Pharmacotherapeutic group: antihypertensive, antianginal agent.
Active ingredient : amlodipine besylate.
Excipients: microcrystalline cellulose, anhydrous calcium phosphate, magnesium stearate, sodium carboxylmethyl starch (type A).
Amlodipine besylate, a derivative of dihydropyridine, has a blocking effect on calcium channels, reducing the transmembrane transition of calcium ions into smooth muscle vascular cells. Its ability to expand the coronary vessels is due to the expansion of the arteries and arterioles, a decrease in total peripheral vascular resistance. With the development of stenocardia, this drug reduces the severity of ischemia, increases the oxygen supply to the myocardium, reduces the load on the heart, prevents spasm of the coronary arteries, increases tolerance to physical activity, reduces the frequency of angina attacks.
The hypotensive effect of Amlodipine is caused by a direct vasodilator effect on vascular smooth muscle. In patients with arterial hypertension, when taking a single dose of the drug for 24 hours there is a clinically significant decrease in blood pressure. The development of orthostatic hypotension with the use of the drug is quite rare. Reduces the degree of left ventricular myocardial hypertrophy, does not affect cardiac contractility and conductivity, does not lead to a reflex increase in heart rate. Under the influence of Amlodipine, which has a weak natriuretic effect, the glomerular filtration rate increases, platelet aggregation is inhibited.
In patients with diabetic nephropathy, the severity of microalbuminuria does not increase. The drug does not affect the metabolic processes and the concentration of lipids in the blood plasma. Can be used in the treatment of patients with gout, diabetes and asthma.
With pathologies of the cardiovascular system (coronary atherosclerosis with a lesion of 1 to 3 arteries, after myocardial infarction, percutaneous transluminal angioplasty and stenocardia), Amlodipine prevents thickening of the intima-media of the carotid arteries, helps reduce the frequency of surgical interventions, reduce the number of surgical interventions, designed to, in reducing the frequency of surgical interventions, cartozoic arteries, helps to reduce the frequency of surgical interventions, reduce the number of surgical interventions, reduce the number of surgical interventions, designed to, and to reduce the frequency of surgical interventions, aimed at relief of intima-media of the carotid arteries, helps to reduce the frequency of surgical interventions, and to reduce the frequency of surgical interventions to the carotid arteries; , progression of chronic heart failure and the development of unstable angina.
In patients with chronic heart failure III-IV Art. non-ischemic etiology use of the drug may cause pulmonary edema
Amlodipine is slowly adsorbed from the gastrointestinal tract. The average absolute bioavailability - 64%, reaches the maximum concentration in serum after 6-9 hours after administration. To achieve an equilibrium concentration requires 7-8 days of use.
The drug is allowed to take, regardless of the time of the meal. Most of it is adsorbed in the tissue, the smaller remains in the blood. The average volume of distribution is 21 l / kg body weight. Slowly but actively disintegrates in the liver. Metabolites lack essential pharmacological activity.
The half-life after a single dose is 35-50 hours, with repeated - 45 hours. 10% of the drug is excreted by the kidneys unchanged, about 60% - in the form of metabolites, 20-25% - along with the bile, through the intestine. Total clearance - 0.116 ml / s / kg. The elimination half-life in elderly patients is 65 hours, but this difference is not critical. The drug is able to penetrate the blood-brain barrier, during hemodialysis is not removed.
Indications for use
- Arterial hypertension;
- Stable angina ;
- Vasospastic stenocardia (Prinzmetala).
Dosage and administration
In the treatment of the initial degree of angina and arterial hypertension - 5 mg once a day. Gradually, within 7-10 the dose of the drug is increased to 10 mg / day.
Maintenance dose in hypertension - 5 mg / day, once.
Vasospastic stenocardia and angina of exertion - 5-10 mg / day, once.
With the simultaneous use of ACE inhibitors, beta-blockers and thiazide diuretics, changing the dose of the drug is not required.
From the side of the central nervous system : dizziness, fatigue, headaches, drowsiness, general malaise, sleep disturbance, emotional lability, depression, increased anxiety, increased sweating. Migraine, ataxia, amnesia, seizures are quite rare;
Gastrointestinal tract : nausea, vomiting, abdominal pain, abnormal stool, flatulence, anorexia, thirst, drying of the oral mucosa. Very rarely - increased appetite, gingival hyperplasia, cholestatic jaundice, hepatitis, pancreatitis .
Lymphatic and hematopoietic systems : thrombocytopenia, thrombocytopenic purpura, leukopenia.
Cardiovascular system : heartbeat, flushing of the face, development of peripheral edema, excessive lowering of blood pressure, vasculitis , orthostatic hypotension, aggravation of chronic heart failure, shortness of breath, heart rhythm disturbances, fainting, chest pain, pulmonary edema, myocardial infarction.
Excretory system : painful urge to urinate, polyuria, dysuria, nocturia, pollakiuria.
Respiratory system : runny nose, shortness of breath, cough.
Reproductive system : impotence, gynecomastia.
Musculoskeletal system - arthralgia, myalgia, muscle cramps, back pain, myasthenia gravis, arthrosis.
Skin : itching, rash, urticaria , erythema multiforme, angioedema, alopecia.
Sense organs : visual disturbances, tinnitus, conjunctivitis , eye pain, parosmia.
Other : hyperglycemia, weight loss or increase, nosebleeds, chills, taste perversions.
Interaction with other drugs
With the simultaneous use of microsomal oxidation inhibitors, the concentration of Amlodipine increases, and when taking microsomal enzymes - decreases.
NSAIDs, alpha-adrenergic stimulants, sympathomimetics and estrogens weaken the hypotensive effect of the drug. Beta-blockers, diuretics, nitrates, antipsychotics, slow calcium channel blockers and ATP inhibitors increase the vasodilator and hypotensive effect.
Amlodipine pharmacokinetics are not affected by warfarin, digoxin, cimetidine.
With simultaneous use with lithium preparations, nausea, vomiting, abnormal stool, tinnitus, tremor, ataxia are possible.
The drug effect of Amlodipine can reduce potassium supplements.
Drugs that prolong the QT interval can increase the negative ionotropic effect.
- Hypersensitivity to the drug;
- Cardiogenic shock;
- Severe arterial hypotension;
- Unstable angina (with the exception of vasospastic);
- Pregnancy and lactation;
- Age up to 18 years.
During treatment, the patient should follow a special diet, constantly monitor body weight and sodium intake. To prevent the development of complications from the oral cavity requires frequent visits to the dentist and careful maintenance of dental hygiene.
For elderly patients, with increasing doses of the drug, requires constant medical supervision.
When discontinuing treatment, the dose should be reduced gradually.
When driving and working with different mechanisms, special precautions must be observed.
Terms of implementation
Amlodipine tablets are prescription drugs, i.e. prescription of a doctor.
Store in a dark, protected from light and moisture, out of the reach of children, at a temperature not exceeding 25 C.
The drug is usable for 3 years from the date of issue. Use of the product after the expiration date indicated on the package is prohibited.
Analogs of Amlodipine
- Amlovas (tablets);
- Vero-amlodipine (tablets);
- Normodipine (tablets);
- Norvask (tablets).
Amlodipine tablets 10 mg, 30 pcs. - from 27r.