Amlodipine
Amlodipine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Reviews
- 17. Price in pharmacies
Latin name: Amlodipine
ATX code: C08CA01
Active ingredient: amlodipine (amlodipine)
Producer: Hemofarm (Serbia), Ozon, LLC (Russia), VERTEX (Russia), Kanonfarm production, CJSC (Russia)
Description and photo update: 2019-14-08
Prices in pharmacies: from 17 rubles.
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Amlodipine is an antihypertensive drug that lowers blood pressure due to its ability to relax vascular smooth muscle. The agent also has antianginal properties.
Release form and composition
Amlodipine is produced in tablets with the active substance (amlodipine in besylate form) of 2.5, 5 and 10 mg. The tablets of the drug are round, with beveled edges, white. One blister contains 10 pieces. There are 2 blisters in one carton box.
The composition of the preparation, in addition to the active component, includes silicate microcrystalline cellulose, magnesium stearate and pregelatinized starch.
Pharmacological properties
Pharmacodynamics
Amlodipine is a dihydropyridine derivative that has antihypertensive and antianginal effects on the body. This substance binds to the S6 segments of the III and IV domains of the alpha1-subunit of the L-type calcium channel and provides a blockade of calcium channels, reduces the transmembrane transition of calcium ions into the cell (mainly in vascular smooth muscle cells, to a lesser extent in cardiomyocytes). The antianginal effect after taking the substance is due to the expansion of arterioles, coronary and peripheral arteries.
With angina pectoris, amlodipine reduces the severity of myocardial ischemia. Promotes the expansion of peripheral arterioles, causes a decrease in total peripheral vascular resistance (decrease in afterload on the heart), without leading to a reflex increase in heart rate and, accordingly, contributing to a decrease in energy consumption. Reduces the need for myocardial oxygen supply. Expands arterioles and coronary arteries in the ischemic and unchanged areas of the myocardium, and also helps to increase the flow of oxygen to the myocardium in vasospastic angina. Prevents the development of coronary spasm (including smoking-related cases).
Taking a single daily dose of amlodipine in patients with angina pectoris increases the time to the first ischemic episode during exercise, prevents the occurrence of angina attacks and "ischemic" ST segment depression (by 1 mm) during exercise, and also helps to reduce the frequency of angina attacks and reduce the consumption of nitroglycerin and other nitrates.
The hypotensive effect of amlodipine is a direct vasodilating effect on the smooth muscle of the blood vessels. When taken, a long-term dose-dependent hypotensive effect is observed.
With arterial hypertension, taking a single daily dose of amlodipine leads to a clinically significant decrease in blood pressure within 1 day (in the position of the patient "standing" and "lying"). Does not lead to a sharp decrease in blood pressure, left ventricular ejection fraction. Does not affect the conductivity and contractility of the myocardium. Reduces the severity of left ventricular myocardial hypertrophy.
With ischemic heart disease (including coronary atherosclerosis with damage from one vessel to stenosis of three or more arteries or with atherosclerosis of the carotid arteries) in patients after myocardial infarction or percutaneous transluminal angioplasty of the coronary arteries, or in patients with angina pectoris, taking amlodipine prevents the development of thickening of the intima-media complex of the carotid artery, reduces mortality from stroke, myocardial infarction, transluminal angioplasty of the coronary arteries, coronary artery bypass grafting, reduces the number of hospitalizations due to unstable angina pectoris or chronic heart failure, and reduces the frequency of interventions to restore coronary blood flow.
Taking amlodipine during therapy with diuretics, angiotensin-converting enzyme inhibitors and digoxin does not increase the risk of death or the likelihood of complications leading to death in patients with chronic heart failure (NYHA functional class III – IV).
In chronic heart failure of non-ischemic etiology (NYHA functional class III – IV), amlodipine is likely to develop pulmonary edema.
Taking amlodipine does not adversely affect metabolism or plasma lipids. The active substance inhibits platelet aggregation, increases the glomerular filtration rate, and provides a weak natriuretic effect. Does not increase the severity of microalbuminuria in diabetic nephropathy.
The time of the onset of the effect is from 2 to 4 hours, the duration of the effect is 1 day.
Pharmacokinetics
When taken orally, amlodipine is well absorbed from the gastrointestinal tract. Food intake does not affect absorption. The time to reach the maximum concentration of the substance in the blood serum is 6–12 hours. Bioavailability - 60 to 65%. Plasma proteins bind 90–97%. The average volume of distribution is 21 l / kg body weight. Amlodipine crosses the blood-brain barrier.
In the liver, amlodipine is slowly metabolized (90%) to inactive metabolites, hepatic clearance is low. The half-life of amlodipine averages 35 hours (35-50 hours), which corresponds to its appointment 1 time per day. The value of the total clearance is 500 ml / min. After 7–8 days of therapy, a stable equilibrium concentration of the substance in the plasma is achieved. It is excreted by the kidneys (unchanged - 10%, in the form of metabolites - 60%), as well as in the form of metabolites through the intestines and with bile (from 20 to 25%). Not removed by hemodialysis.
In hepatic failure or severe chronic heart failure, as well as in elderly patients, the half-life is increased and is 60–65 hours. In case of impaired renal function, the half-life does not change.
Indications for use
According to the instructions, Amlodipine is prescribed for the treatment of the following diseases:
- Arterial hypertension (used both as part of complex treatment and as monotherapy);
- Exertional angina;
- Vasospastic angina pectoris;
- Ischemic heart disease (including in the chronic stage);
- Chronic heart failure;
- Bronchial asthma.
Contraindications
Amlodipine is not used for individual drug intolerance, cardiogenic shock, during pregnancy, breastfeeding, with arterial hypotension and collapse.
The drug is prescribed with caution in chronic heart failure, diabetes, lipid metabolism, liver function disorders, after a heart attack (especially in the first month), as well as in elderly patients and patients under 18 years of age.
Instructions for the use of Amlodipine: method and dosage
Amlodipine is prescribed in the following dosages:
- For hypertension, which is complicated by angina pectoris, ischemic disease, the drug is used 1 time per day, 5 mg;
- With arterial hypertension, which proceeds without complications, the drug is used once a day, 2.5 mg.
If necessary, the dosage can be increased to 10 mg, which is the maximum allowable daily dose.
Side effects
During treatment, side effects from the following body systems can be observed:
- Central nervous system: headache, fatigue, convulsions, paresthesia, dizziness, depression, disturbances in wakefulness and sleep, asthenia, nervousness, loss of consciousness, tremor, amnesia, apathy, anxiety;
- Cardiovascular system, hematopoiesis: leukopenia, extrasystole, cardiac arrhythmias, hypotension, flushing of the body and face, pain in the sternum, edema of the extremities, hyperglycemia, shortness of breath, thrombocytopenia;
- Gastrointestinal tract: vomiting, dry mouth, flatulence, gastritis, pain in the epigastric region, increased bilirubin, pancreatitis, nausea, stool disturbance, increased appetite, changes in the activity of liver enzymes.
The use of Amlodipine can also cause sexual dysfunction, joint pathology, urinary disorders, myasthenia gravis.
Cases of dermatitis, urticaria, pruritus, erythematous rash have been recorded.
The drug is also known to cause visual impairment, changes in body temperature, increased sweating, nosebleeds and ringing in the ears.
Overdose
Symptoms: a pronounced decrease in blood pressure with the possibility of developing reflex tachycardia, excessive peripheral vasodilation (the development of a persistent and pronounced decrease in blood pressure is possible, as a result of which shock and death may occur).
Treatment: gastric lavage (especially in the first 120 minutes after an overdose), taking activated charcoal, maintaining the function of the cardiovascular system, monitoring the function of the lungs and heart, monitoring the volume of circulating blood and urine output. The patient must be placed in a horizontal position with an elevated position of the legs. To restore vascular tone, vasoconstrictor drugs are prescribed (in the absence of contraindications to their use). The consequences of calcium channel blockade are eliminated by intravenous administration of calcium gluconate. Hemodialysis with an overdose of amlodipine is ineffective.
special instructions
During the period of treatment with Amlodipine, it is necessary to follow the diet and control sodium intake.
Before discontinuing the drug, a gradual dose reduction is recommended.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy. The safety and efficacy of amlodipine during this period have not been established.
There is no information regarding excretion in breast milk. If you need to use Amlodipine during lactation, you should stop breastfeeding.
Pediatric use
The drug is contraindicated for the treatment of patients under the age of 18 years.
With impaired renal function
No dose adjustment is required in renal failure.
For violations of liver function
If liver function is impaired, the drug should be used with caution.
Use in the elderly
When treating elderly patients, the drug should be used with caution.
Analogs
Amlodipine analogues are Amlovas, Norvask and Normodipin.
Terms and conditions of storage
Amlodipine must be stored in a dry and dark place, out of the reach of children, at a temperature of 15-25 ° C.
The shelf life is 3 years.
Reviews about Amlodipine
Reviews of Amlodipine from doctors indicate that this drug is effective in the treatment of heart disease and for the prevention of angina pectoris and heart attack. Only a doctor should determine the required dose of Amlodipine.
Amlodipine price in pharmacies
The approximate price for Amlodipine is: 90 tablets 5 mg - 140 rubles, 90 tablets 10 mg - 195 rubles.
Amlodipine: prices in online pharmacies
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Drug name Price Pharmacy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
