Amlodipine tablets: instructions, price, analogues and reviews. Amlodipine tablets: instructions for use General characteristics. Compound
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International Classification of Diseases (ICD-10)
I10 Essential [primary] hypertension I20 Angina pectoris [angina pectoris] I20.0 Unstable angina I20.1 Angina with documented spasmPharmacological group
Calcium channel blocker
pharmachologic effect
Selective class II calcium channel blocker. The antihypertensive effect is due to a direct relaxing effect on vascular smooth muscle. It is assumed that the antianginal effect of amlodipine is associated with its ability to dilate peripheral arterioles; this leads to a decrease in peripheral vascular resistance, and reflex tachycardia does not occur. As a result, there is a decrease in myocardial oxygen demand and energy consumption by the heart muscle. On the other hand, amlodipine appears to cause dilation of large-caliber coronary arteries and coronary arterioles in both intact and ischemic areas of the myocardium. This ensures the supply of oxygen to the myocardium during spasms of the coronary arteries.
Pharmacokinetics
When taken orally, it is absorbed from the gastrointestinal tract slowly and almost completely, Cmax in blood plasma is achieved within 6-9 hours. Protein binding is 95-98%. Subjects to minimal first-pass metabolism and slow but significant hepatic metabolism to metabolites with little pharmacological activity.
T1/2 averages 35 hours and with arterial hypertension can increase to an average of 48 hours, in elderly patients - up to 65 hours and in case of liver dysfunction - up to 60 hours. Excreted mainly in the form of metabolites: 59-62% - kidneys, 20-25% - through the intestines.
Arterial hypertension (as monotherapy or as part of combination therapy).
Stable angina, unstable angina, Prinzmetal's angina (as monotherapy or as part of combination therapy).
Severe arterial hypotension (systolic blood pressure less than 90 mmHg); left ventricular outflow tract obstruction (including severe aortic stenosis); hemodynamically unstable heart failure after myocardial infarction; children and adolescents under 18 years of age (efficacy and safety have not been established); hypersensitivity to amlodipine and other dihydropyridine derivatives.
From the cardiovascular system: peripheral edema, tachycardia, skin hyperemia; when used in high doses - arterial hypotension, arrhythmias, shortness of breath.
From the digestive system: nausea, abdominal pain; rarely - gum hyperplasia.
From the central nervous system and peripheral nervous system: headache, fatigue, drowsiness, dizziness; with prolonged use - paresthesia.
Allergic reactions: skin rash, itching.
Others: with prolonged use - pain in the limbs.
special instructions
Use with caution in patients with liver failure, chronic heart failure of non-ischemic etiology of functional class III-IV according to the NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after it), SSS (severe tachycardia, bradycardia), arterial hypotension, when used simultaneously with inhibitors or inducers of the CYP3A4 isoenzyme.
During the use of amlodipine in patients with chronic heart failure (class III and IV according to the NYHA classification) of non-ischemic origin, an increase in the incidence of pulmonary edema was observed, despite the absence of signs of worsening heart failure.
In elderly patients, T1/2 may increase and the clearance of amlodipine may decrease. No dose changes are required, but more careful monitoring of patients in this category is necessary.
The effectiveness and safety of amlodipine in hypertensive crisis has not been established.
Despite the absence of withdrawal syndrome with slow calcium channel blockers, it is advisable to discontinue treatment with amlodipine gradually.
There are no clinical data on the use of amlodipine in pediatrics.
For renal failure
Use with caution in case of impaired renal function.
In case of liver dysfunction
Use with caution in case of liver dysfunction.
Elderly
Elderly patients do not require dose reduction.
Use during pregnancy and breastfeeding
The safety of amlodipine during pregnancy has not been established, so use is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.
There are no data indicating the excretion of amlodipine in breast milk. However, other calcium channel blockers (dihydropyridine derivatives) are known to be excreted in breast milk. In this regard, if it is necessary to use amlodipine during lactation, the issue of stopping breastfeeding should be decided.
Drug interactions
It is possible to enhance the antianginal and antihypertensive effect of slow calcium channel blockers when used together with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their antihypertensive effect when used together with alpha 1-blockers, antipsychotics.
Although negative inotropic effects have not generally been observed in amlodipine studies, some calcium channel blockers may enhance the negative inotropic effects of antiarrhythmic drugs that cause QT prolongation (eg, amiodarone and quinidine).
Simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in the bioavailability of simvastatin by 77%. In such cases, the dose of simvastatin should be limited to 20 mg.
Antiviral drugs (for example, ritonavir) increase plasma concentrations of slow calcium channel blockers, incl. amlodipine.
With the simultaneous use of sympathomimetics and estrogens, the antihypertensive effect may be reduced due to sodium retention in the body.
Neuroleptics and isoflurane enhance the antihypertensive effect of dihydropyridine derivatives. With the simultaneous use of inhalation anesthesia, the hypotensive effect may be enhanced.
With simultaneous use of amiodarone, the antihypertensive effect may be enhanced.
With simultaneous use of lithium carbonate, manifestations of neurotoxicity (including nausea, vomiting, diarrhea, ataxia, tremors and/or tinnitus) are possible.
With simultaneous use, orlistat reduces the antihypertensive effect of amlodipine, which can lead to a significant increase in blood pressure and the development of a hypertensive crisis.
With the simultaneous use of indomethacin and other NSAIDs, the antihypertensive effect of amlodipine may be reduced due to inhibition of prostaglandin synthesis in the kidneys and fluid retention under the influence of NSAIDs.
With simultaneous use of quinidine, the antihypertensive effect may be enhanced.
Calcium supplements may reduce the effect of slow calcium channel blockers.
With simultaneous use of diltiazem (CYP3A4 isoenzyme inhibitor) at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (69 to 87 years) with arterial hypertension, an increase in the bioavailability of amlodipine by 57% was observed. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) does not lead to significant changes in amlodipine exposure (22% increase in AUC). Although the clinical significance of these effects is unclear, they may be more pronounced in older patients. Potent inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) may increase the plasma concentration of amlodipine to a greater extent than diltiazem. Amlodipine and inhibitors of the CYP3A4 isoenzyme should be used with caution.
There are no data on the effect of inducers of the CYP3A4 isoenzyme on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored while using amlodipine and inducers of the CYP3A4 isoenzyme.
For adults, when taken orally, the initial dose is 5 mg 1 time / day. If necessary, the dose can be increased.
Maximum dose: when taken orally - 10 mg/day.
- Instructions for use Amlodipine
- Composition of the drug Amlodipine
- Indications for the drug Amlodipine
- Storage conditions for the drug Amlodipine
- Shelf life of the drug Amlodipine
ATX code: Cardiovascular system (C) > Calcium channel blockers (C08) > Selective calcium channel blockers with a predominant effect on blood vessels (C08C) > Dihydropyridine derivatives (C08CA) > Amlodipine (C08CA01)
Release form, composition and packaging
tab. 10 mg: 30 pcs.Reg. No.: 7812/06/08/11 from 09/02/2011 - Expired
Pills round, biconvex, white or almost white with a notch on one side; without smell.
Excipients: calcium hydrogen phosphate (dihydrate), microcrystalline cellulose, sodium starch glycolate, magnesium stearate.
10 pieces. - blisters (3) - cardboard packaging.
Description of the drug AMLODIPINE tablets 10 mg created in 2012 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Update date: 05/07/2013
Slow calcium channel blocker, dihydropyridine derivative. By binding to dihydropyridine receptors, it blocks slow calcium channels, inhibits the transmembrane transition of calcium into the smooth muscle cells of the heart and blood vessels (to a greater extent into vascular smooth muscle cells than into cardiomyocytes). It has an antihypertensive and antianginal effect. The mechanism of the antihypertensive effect of amlodipine is due to a direct relaxing effect on vascular smooth muscle. Amlodipine reduces myocardial ischemia in two ways:
- dilates peripheral arterioles and thus reduces TPSS (afterload), while heart rate remains virtually unchanged, which leads to a decrease in energy consumption and myocardial oxygen demand;
- and also expands the coronary and peripheral arteries and arterioles in both normal and ischemic areas of the myocardium, which increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal angina) and prevents the development of coronary spasm. In patients with arterial hypertension, a single daily dose of Amlodipine provides a decrease in blood pressure for 24 hours both in the supine and standing positions. Due to its slow onset of action, amlodipine does not cause a sharp decrease in blood pressure. In patients with angina pectoris, a single daily dose of amlodipine increases the time of physical activity, delays the development of the next attack of angina and ST segment depression (by 1 mm) during exercise, reduces the frequency of angina attacks and the consumption of nitroglycerin tablets. In patients with cardiovascular diseases (including coronary atherosclerosis with damage to one vessel and up to stenosis of 3 or more arteries and atherosclerosis of the carotid arteries), who have had myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries (PCA) or suffering from angina, the use of Amlodipine prevents the development of intimal thickening - media of the carotid arteries, significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, TLP, coronary artery bypass surgery, leads to a decrease in the number of hospitalizations for unstable angina and progression of chronic heart failure, reduces the frequency of interventions aimed at restoring coronary blood flow. Amlodipine does not increase the risk of death or complications leading to death in patients with chronic heart failure (NYHA functional class III-IV) 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 possibility of pulmonary edema. Amlodipine does not have any adverse effects on metabolism and plasma lipid concentrations.
Suction and distribution
After oral administration in therapeutic doses, amlodipine is well absorbed, Cmax in the blood is reached 6-12 hours after administration. Absolute bioavailability is 64-80%. Food intake does not affect the absorption of amlodipine. Vd is approximately 21 l/kg. Plasma protein binding is approximately 97.5%. Amlodipine penetrates the BBB. Css in plasma is achieved after 7-8 days of continuous use of the drug.
Metabolism and excretion
Amlodipine is biotransformed in the liver to form inactive metabolites. T1/2 from plasma is about 35-50 hours, which corresponds to the administration of the drug 1 time / day. Total clearance - 0.43 l/h/kg. 10% of the unchanged active substance and 60% of the metabolites are excreted in the urine.
Pharmacokinetics in special clinical situations
In patients with liver failure and severe chronic heart failure, T1/2 increases to 56-60 hours. T1/2 from plasma in patients with renal failure increases to 60 hours. Changes in the concentration of amlodipine in plasma do not correlate with the degree of renal dysfunction. In older and younger people, the time required to achieve Cmax of amlodipine in blood plasma is almost the same. In elderly people with chronic heart failure, there is a tendency to decrease the clearance of amlodipine, which leads to an increase in AUC and T1/2 (up to 65 hours).
- arterial hypertension (both as monotherapy and in combination with other antihypertensive drugs);
- stable angina and angiospastic angina (Prinzmetal's angina) (both as monotherapy and in combination with other antianginal drugs).
For arterial hypertension and angina pectoris the average initial dose is 5 mg 1 time / day, depending on the individual response of the patient, it can be increased to a maximum dose of 10 mg. The tablets are taken orally 1 time/day with the required volume of water (up to 100 ml). It is not recommended to use Amlodipine, scored tablets 10 mg, if it is necessary to titrate the dose of amlodipine, starting from the minimum (2.5 mg), in the following cases:
- when prescribed to a patient for the first time;
- when prescribed to persons weighing less than 50 kg or with impaired liver function;
- in some cases, when selecting the dosage while being prescribed with thiazide diuretics, beta blockers, and ACE inhibitors.
From the cardiovascular system: often - peripheral edema (ankles and feet), palpitations;
From the musculoskeletal system: sometimes - arthralgia, muscle cramps, myalgia, back pain, arthrosis;
From the central nervous system and peripheral nervous system: often - a feeling of heat and “flushes” of blood to the skin of the face, increased fatigue, dizziness, headache, drowsiness;
From the digestive system: often - abdominal pain, nausea;
From the hematopoietic system: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.
From the side of metabolism: very rarely - hyperglycemia.
From the respiratory system: sometimes - shortness of breath, rhinitis;
From the urinary system: sometimes - frequent urination, painful urination, nocturia, impotence;
Allergic reactions: sometimes - skin itching, rash;
Others: sometimes - alopecia, tinnitus, gynecomastia, weight gain/loss, visual impairment, diplopia, accommodation disturbance, xerophthalmia, conjunctivitis, eye pain, taste perversion, chills, nosebleeds;
- cardiogenic shock;
- severe heart failure;
- severe aortic stenosis;
- acute myocardial infarction;
- acute unstable angina;
- hypotension;
- hypersensitivity to dihydropyridines, amlodipine or other components of the drug.
Carefully prescribe Amlodipine to patients with aortic stenosis who are at risk of developing hypotension. In patients with coronary atherosclerosis, at the beginning of use or with an increase in the dose of Amlodipine, the risk of worsening the course of angina pectoris and the development of acute myocardial infarction increases. Prescribing Amlodipine does not prevent beta blocker withdrawal syndrome.
Patients with severe liver failure should carefully select the dosage of Amlodipine.
Use during pregnancy and breastfeeding
The safety of Amlodipine during pregnancy and lactation (breastfeeding) has not been established. The use of Amlodipine during pregnancy is recommended only in cases where there is no safer alternative, and the risk associated with the disease itself outweighs the possible harm to the mother and fetus. If it is necessary to use Amlodipine during lactation, the issue of stopping breastfeeding should be decided.
The drug should be used with caution in patients with impaired liver function, chronic heart failure (III-IV functional class according to the NYHA classification) of non-ischemic etiology, aortic stenosis, acute myocardial infarction (and within 1 month after it). As when prescribing other calcium channel blockers, caution must be exercised when taking Amlodipine in patients with SSSU, mitral stenosis, hypertrophic obstructive cardiomyopathy, arterial hypotension. When treating arterial hypertension, Amlodipine can be used in combination with thiazide diuretics, alpha- and beta-blockers, inhibitors ACEs, long-acting nitrates, sublingual nitroglycerin, NGTG, antibiotics and oral hypoglycemic agents. As when prescribing other calcium channel blockers, caution must be exercised when taking Amlodipine in patients with CVS, mitral stenosis, hypertrophic obstructive cardiomyopathy, and arterial hypotension. For the treatment of angina pectoris, Amlodipine can be prescribed as monotherapy or in combination with other antianginal drugs, including. in patients refractory to treatment with nitrates and/or beta-blockers in adequate doses. Amlodipine does not have any adverse effects on metabolism and plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. Amlodipine can also be used in cases where the patient is predisposed to vascular spasm (vasoconstriction). Patients with low body weight, patients of short stature and patients with severe liver dysfunction may require a dose reduction. During treatment, weight control and dental supervision are necessary (to prevent pain, bleeding and gum hyperplasia).
Use in pediatrics
The drug should be prescribed with caution to children and adolescents under the age of 18, because the effectiveness and safety of its use in this group of patients have not been clearly established.
Impact on the ability to drive vehicles and operate machinery
Although no negative effect on the ability to drive a car or other technical means was observed while taking Amlodipine, however, due to a possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other side effects, you should be careful about the individual effect of the drug in these situations, especially at the beginning treatment and when changing the dosage regimen.
Symptoms: a pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (there is a possibility of severe and persistent arterial hypotension, including the development of shock and death).
Treatment: prescribing activated charcoal (especially in the first 2 hours after an overdose), gastric lavage (in some cases), giving an elevated position to the limbs, actively maintaining the function of the cardiovascular system, monitoring heart and lung performance, monitoring blood volume and diuresis. To restore vascular tone and blood pressure, if there are no contraindications, it is possible to use vasoconstrictor drugs. Use intravenous administration of calcium gluconate. Since amlodipine is highly bound to serum proteins, hemodialysis is not effective.
It can be expected that inhibitors of microsomal oxidation will increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes will reduce it.
With simultaneous use of Amlodipine with cimetidine, the pharmacokinetics of amlodipine does not change.
Unlike other calcium channel blockers, no significant interaction of Amlodipine was found when used together with NSAIDs, especially indomethacin.
It is possible to enhance the antianginal and hypotensive effects of calcium channel blockers when used together with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates; as well as an increase in their hypotensive effect when used together with alpha1-blockers and antipsychotics.
Although no negative inotropic effect was generally observed in studies with Amlodipine, some calcium channel blockers may enhance the negative inotropic effect of antiarrhythmic drugs that cause QT prolongation (for example, amiodarone and quinidine). When used together with lithium drugs, calcium channel blockers (no data for Amlodipine) may increase the manifestation of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not affect the degree of plasma protein binding of digoxin, phenytoin, warfarin and indomethacin in vitro.
A single dose of aluminum/magnesium-containing antacids does not have a significant effect on the pharmacokinetics of amlodipine.
A single dose of sildenafil in a dose of 100 mg in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.
Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin. When amlodipine was administered concomitantly with digoxin in healthy volunteers, serum levels and renal clearance of digoxin did not change.
With single and repeated use at a dose of 10 mg, amlodipine does not have a significant effect on the pharmacokinetics of ethanol.
Amlodipine does not affect changes in prothrombin time caused by warfarin. Amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine. A simultaneous single dose of 240 ml of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. Strong CYP3A4 inhibitors (eg ketoconazole, itraconazole, ritonavir) may increase plasma concentrations of amlodipine. Monitor for symptoms of hypotension and peripheral edema when amlodipine is coadministered with CYP3A4 inhibitors. There is currently no information on the quantitative effects of CYP3A4 inducers on the pharmacokinetics of amlodipine; however, it is necessary to carefully monitor blood pressure when amlodipine is co-administered with CYP3A4 inducers.
Detailed instructions for use are published on this page. Amlodipine. The available dosage forms of the drug (tablets 5 mg and 10 mg), as well as its analogues, are listed. Information is provided on the side effects that Amlodipine can cause and on interactions with other medications. In addition to information about the diseases for the treatment and prevention of which the drug is prescribed (reduction of high blood pressure, treatment of angina), the administration algorithms, possible dosages for adults and children are described in detail, the possibility of use during pregnancy and breastfeeding is clarified. The summary of Amlodipine is supplemented with reviews from patients and doctors.
Instructions for use and dosage regimen
Orally, the initial dose for the treatment of arterial hypertension and angina pectoris is 5 mg of the drug 1 time per day. The maximum daily dose is 10 mg once.
For arterial hypertension, the maintenance dose can be 2.5-5 mg (1/2 tablet of 5 mg - 1 tablet of 5 mg) per day
For exertional angina and vasospastic angina - 5-10 mg per day, once. To prevent angina attacks - 10 mg per day.
In patients with impaired liver function, Amlodipine is prescribed with caution as an antihypertensive agent, at an initial dose of 2.5 mg (1/2 tablet of 5 mg each), and as an antianginal agent - 5 mg.
No dose change is required when administered concomitantly with thiazide diuretics, beta-blockers and ACE inhibitors.
No dose changes are required in patients with renal failure.
Release forms
Tablets 5 mg and 10 mg. May be produced in combination with other dosage forms (combination drugs).
Amlodipine- dihydropyridine derivative - 2nd generation slow calcium channel blocker (SCBC), has antianginal and hypotensive effects. By binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes).
The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: in case of angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces peripheral vascular resistance, reduces preload on the heart, and reduces myocardial oxygen demand. Expands the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents the development of spasm of the coronary arteries (including those caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, slows down the development of angina and “ischemic” depression of the ST segment, reduces the frequency of angina attacks and the consumption of nitroglycerin and other nitrates.
It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over 24 hours (with the patient lying and standing). Orthostatic hypotension when prescribing amlodipine is quite rare.
Does not cause a decrease in exercise tolerance or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy, has an antiatherosclerotic and cardioprotective effect in ischemic heart disease. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect.
In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and plasma lipid concentrations and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout.
A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours. With long-term therapy, the maximum decrease in blood pressure occurs 6-12 hours after taking amlodipine orally. If amlodipine is discontinued after long-term treatment, the effective reduction in blood pressure persists for 48 hours after the last dose. Then blood pressure levels gradually return to the original level over 5-6 days.
Pharmacokinetics
After oral administration, Amlodipine is slowly absorbed from the gastrointestinal tract. Food intake does not affect the absorption of amlodipine. Most of the drug in the blood (95%) binds to blood plasma proteins. Amlodipine undergoes slow but active metabolism in the liver with no significant first-pass effect. Metabolites do not have significant pharmacological activity. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% unchanged, and 20-25% through the intestines, as well as with breast milk.
The drug penetrates the blood-brain barrier. It is not removed by hemodialysis.
In elderly patients (over 65 years of age), the elimination of amlodipine is slower than in younger patients, but this difference is not clinically significant.
Indications
- arterial hypertension (in monotherapy or in combination with other drugs);
- angina pectoris;
- vasospastic angina (Prinzmetal's angina).
Contraindications
- severe arterial hypotension (systolic blood pressure less than 90 mmHg);
- collapse, cardiogenic shock;
- unstable angina (with the exception of Prinzmetal angina);
- clinically significant aortic stenosis;
- pregnancy and lactation;
- age under 18 years (efficacy and safety have not been studied);
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- hypersensitivity to amlodipine, dihydropyridine derivatives and other components of the drug.
special instructions
During treatment with Amlodipine, it is necessary to monitor body weight and sodium intake, and prescribe an appropriate diet. It is necessary to maintain dental hygiene and follow-up with a dentist (to prevent pain, bleeding and gum hyperplasia).
Patients with low body weight, patients of short stature and patients with severe liver dysfunction may require a lower dose.
Despite the fact that discontinuation of Amlodipine is not accompanied by the development of withdrawal syndrome, it is advisable to discontinue treatment by gradually reducing the dose of the drug.
The effectiveness and safety of the drug in hypertensive crisis have not been established.
Impact on the ability to drive vehicles and operate machinery
There have been no reports of the effect of Amlodipine on driving or using machinery. However, some patients, mainly at the beginning of treatment, may experience drowsiness and dizziness. If they occur, the patient must take special precautions when driving a car and working with complex mechanisms.
Side effect
- heartbeat;
- peripheral edema (swelling of the ankles and feet);
- “flushes” of blood to the skin of the face;
- excessive decrease in blood pressure;
- dyspnea;
- vasculitis;
- orthostatic hypotension;
- development or worsening of heart failure;
- heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation);
- myocardial infarction;
- chest pain;
- headache;
- dizziness;
- increased fatigue;
- drowsiness;
- asthenia;
- paresthesia;
- insomnia;
- mood lability;
- unusual dreams;
- nervousness;
- depression;
- anxiety;
- migraine;
- increased sweating;
- nausea;
- stomach ache;
- vomit;
- constipation or diarrhea;
- flatulence;
- dyspepsia;
- anorexia;
- dry mouth;
- thirst;
- increased appetite;
- gastritis;
- thrombocytopenic purpura, leukopenia, thrombocytopenia;
- frequent urination;
- painful urination;
- impotence;
- gynecomastia;
- dyspnea;
- rhinitis;
- cough;
- dermatitis;
- skin pigmentation disorder;
- skin itching;
- rash (including erythematous, maculopapular rash, urticaria);
- angioedema;
- muscle cramps;
- backache;
- tinnitus;
- Pain in the eyes;
- chills;
- nose bleed.
Drug interactions
Amlodipine can be safely used for the treatment of hypertension together with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, long-acting nitrates, beta-blockers or short-acting nitrates.
Amlodipine can be used simultaneously with non-steroidal anti-inflammatory drugs (especially indomethacin), antibacterial agents and oral hypoglycemic agents.
It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when used together with alpha-blockers, antipsychotics.
Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that prolong the QT interval (eg, amiodarone and quinidine).
A single dose of 100 mg of sildenafil (Viagra) in patients with essential hypertension does not affect the pharmacokinetic parameters of amlodipine.
Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol (alcohol).
Antiviral agents (ritonavir) increase plasma concentrations of BMCC, incl. amlodipine.
Neuroleptics and isoflurane - enhance the hypotensive effect of dihydropyridine derivatives.
Calcium supplements may reduce the effect of BMCC.
When amlodipine is used together with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not change the pharmacokinetics of cyclosporine.
Does not affect the serum concentration of digoxin and its renal clearance.
Does not have a significant effect on the effect of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine.
Analogues of the drug Amlodipine
Structural analogues of the active substance:
- Acridipine;
- Amlovas;
- Amlodak;
- Amlodigamma;
- Amlodipine Zentiva;
- Amlodipine Cardio;
- Amlodipine Sandoz;
- Amlodipine Teva;
- Amlodifarm;
- Amlocard-Sanovel;
- Amlong;
- Amlonorm;
- Amlorus;
- Amlotop;
- Vero-Amlodipine;
- Kalchek;
- Cardilopin;
- Corvadil;
- Cordy Core;
- Norvasc;
- Normodipine;
- Omelar Cardio;
- Stamlo;
- Tenox.
Use in children
Contraindicated in children and adolescents under 18 years of age (efficacy and safety have not been studied).
Use during pregnancy and breastfeeding
Amlodipine was not found to be teratogenic in animal studies, but there is no clinical experience with its use during pregnancy and lactation. Therefore, amlodipine should not be prescribed to pregnant women and during lactation, as well as to women of childbearing age if they do not use reliable methods of contraception.
Amlodipine is a slow calcium channel blocker, which means it disrupts the transition of calcium into cellular structures.
The effect is mainly on the smooth muscles of the vascular walls. In addition, when taken, an antianginal effect is also manifested - an increase in the lumen of blood vessels in both the coronary and peripheral beds occurs. Additional blood pressure decreases. The main reason for prescribing this drug is hypertension and angina pectoris.
On this page you will find all the information about Amlodipine: complete instructions for use for this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Amlodipine. Would you like to leave your opinion? Please write in the comments.
Clinical and pharmacological group
Calcium channel blocker.
Conditions for dispensing from pharmacies
Dispensed with a doctor's prescription.
Prices
How much does Amlodipine cost? The average price in pharmacies is at the following level:
- Tablets 5 mg, 20 pieces – 51 – 109 rubles;
- Tablets 5 mg, 30 pieces – 34 – 209 rubles;
- Tablets 5 mg, 60 pieces – 83 – 124 rubles;
- Tablets 5 mg, 90 pieces – 113 – 174 rubles;
- Tablets 10 mg, 20 pieces – 71 – 167 rubles;
- Tablets 10 mg, 30 pieces – 60 – 281 rubles;
- Tablets 10 mg, 60 pieces – 113 – 128 rubles;
- Tablets 10 mg, 90 pieces – 184 – 226 rubles.
The cost of Amlodipine can vary significantly depending on the manufacturer of the drug. Thus, drugs produced by the Israeli corporation Teva or the Swiss Sandoz are quite expensive, while Amlodipine, produced by Russian pharmaceutical factories, on the contrary, is very cheap. Unfortunately, the quality and effectiveness of Amlodipine from different manufacturers also varies greatly. Therefore, if Amlodipine from any manufacturer turned out to be ineffective or caused side effects, then it makes sense to purchase a drug from another company, since it can be an excellent medicine.
Release form and composition
Available in tablets of 10, 20, 30, 40, 50 or 100 pieces. Active ingredient: 5 or 10 mg per tablet.
- Contains amlodipine besylate , in the equivalent of pure amlodipine, 5 and 10 mg.
- Additional substances are: crospovidone, lactose monohydrate, calcium stearate, povidone.
Pharmacological effect
Amlodipine helps with abnormalities in the heart, blocks calcium channels in the walls of blood vessels and heart muscle cells. As a result, the entry of calcium through cell membranes is prevented, which leads to relaxation of the myocardium and vascular muscle tone. Thus, vasodilation occurs, blood flow is facilitated, and as a result, blood pressure decreases.
Since in a relaxed state the heart muscle requires less oxygen for normal functioning, it acquires the ability to function in such conditions. This allows a patient suffering from angina to better tolerate stress and experience attacks of the disease less often. The antianginal effect of the drug lies in the reduced oxygen demand of the heart.
Antihypertensive properties are manifested by a decrease in blood pressure. These effects, as well as high safety, determine the popularity of the drug. Due to the lack of action aimed at quickly reducing blood pressure and preventing reflex heartbeat, Amlodipine tablets are prescribed to patients with diabetes, asthma, and gout.
Indications for use
In what cases can the medication in question be prescribed to a patient? Indications for taking this drug are the following conditions:
- stable;
- vasoconstriction or vasospasm;
- vasospastic angina;
- (as monotherapy and in combination with other drugs);
- dilated non-ischemic cardiomyopathy.
In what other cases can Amlodipine be recommended? What does this medicine help with? It is often prescribed along with antianginal medications, including in patients who are refractory to treatment with beta-blockers or nitrates.
Contraindications
Amlodipine is not used in case of individual intolerance to the drug, cardiogenic shock, during pregnancy, breastfeeding, arterial hypotension and collapse.
The drug is prescribed with caution in chronic heart failure, diabetes, disorders of lipid metabolism, liver function, after a heart attack (especially in the first month), as well as in elderly patients and patients under 18 years of age.
Use during pregnancy and lactation
No studies have been conducted showing that Amlodipine has a negative effect on the body of the mother and child. Amlodipine is used only in very extreme cases, when the beneficial effect of treatment far outweighs the possible harm. In cases of using Amlodipine during lactation, breastfeeding is stopped throughout the entire duration of treatment, until the drug and its components are completely eliminated from the body.
Instructions for use Amlodipine
The instructions for use indicate that Amlodipine is taken orally, regardless of food intake.
For treatment of arterial hypertension And prevention of attacks of angina pectoris and vasospastic angina The initial dose is 5 mg 1 time/day. If necessary, the daily dose can be increased to a maximum of 10 mg (1 time/day).
- In patients with impaired liver function, Amlodipine is prescribed with caution as an antihypertensive agent, at an initial dose of 2.5 mg (1/2 tablet of 5 mg each), and as an antianginal agent - 5 mg.
- No dose changes are required in patients with renal failure.
- In elderly patients, T1/2 may increase and CC may decrease. No dose change is required, but more careful monitoring of patients is necessary.
No dose change is required when administered concomitantly with thiazide diuretics, beta-blockers and ACE inhibitors.
Side effects
The following side effects are possible when using the drug:
| From the vascular system, heart and hematopoiesis | swelling of the extremities (especially the feet and ankles), shortness of breath, chest pain, migraine, hypotension, flushing of the face and body, heart rhythm disturbances, extrasystole, leukopenia, thrombocytopenia, hyperglycemia. |
| From the central nervous system (CNS) | excessive fatigue, dizziness, disturbance of wakefulness and sleep, headache, tremor, convulsions, asthenia, paresthesia, cases of loss of consciousness, depression, nervousness, amnesia, apathy, anxiety. |
| From the gastrointestinal tract (digestive system) | nausea, nagging pain in the epigastric region, increased bilirubin levels, bowel dysfunction, flatulence, dry mouth, increased appetite or anorexia, pancreatitis, gastritis. |
| Are common | dysfunction of sexual function, impaired urination, myasthenia gravis, development of pathologies in the joints, skin itching, erythematous rash, alopecia, urticaria, impaired vision (most often disturbance of accommodation), ringing in the ears, possible profuse nosebleeds, changes in body temperature, hyperhidrosis (increased sweating). |
Overdose
The maximum permissible dose for treatment is 10 mg per day. As a rule, the patient is prescribed 5 mg per day, and if necessary, the dose is adjusted by the attending physician. Failure to comply with or unauthorized increase in dosage may result in an overdose, resulting in the following symptoms:
- tachycardia;
- deterioration of perfusion of internal organs;
- hypotension.
In case of an overdose of Amlodipine, dialysis is not effective. The patient urgently needs to rinse the stomach and give activated carbon (or another adsorbent) to drink. The victim should be placed on a hard surface, making sure that the legs are slightly elevated. Continuous monitoring of the function of the respiratory and cardiovascular systems, general blood circulation, and diuresis is carried out. As a rule, treatment is prescribed symptomatically. The doctor may also prescribe maintenance treatment - intravenous administration of mezatone and dopamine.
special instructions
Before completely stopping the drug, experts recommend gradually reducing the dosage, that is, abrupt discontinuation of the drug is not recommended.
The pharmacological drug does not have a negative effect on blood plasma lipids, as well as metabolism. Taking the medicine does not affect the central nervous system in any way - it does not cause drowsiness or dizziness.
You should keep your blood pressure under control from the first days - if it drops sharply, complications such as weakness, dizziness and increased fatigue are possible. The drug can be used by people whose work requires increased concentration. If the patient notices a significant deterioration in the condition after starting to take the medicine, in this case it is necessary to contact the attending physician to determine the optimal dose of the medicine.
Drug interactions
- With the simultaneous use of microsomal oxidation inhibitors, the concentration of Amlodipine increases, and when taking microsomal enzymes, it decreases.
- NSAIDs, alpha-agonists, sympathomimetics and estrogens weaken the hypotensive effect of the drug. Beta blockers, diuretics, nitrates, antipsychotics, slow calcium channel blockers and ATP inhibitors enhance the vasodilator and hypotensive effect.
- The pharmacokinetics of Amlodipine are not affected by Warfarin, Digoxin, Cimetidine.
- When used simultaneously with lithium drugs, nausea, vomiting, stool disturbances, tinnitus, tremor, and ataxia are possible.
- The medicinal effect of Amlodipine can be reduced by potassium supplements.
- Drugs that prolong the QT interval can enhance the negative ionotropic effect.
Trade name of the drug: Amlodipine
International Nonproprietary Name (INN): Amlodipine
Dosage form:
pillsCompound:
one tablet 5 mg contains:active substance amlodipine besylate in terms of amlodipine - 5 mg;
Excipients: lactose (milk sugar) - 67.0 mg, potato starch - 6.5 mg, povidone (kollidon 25) - 2.85 mg, microcrystalline cellulose - 16.0 mg, magnesium stearate - 0.7 mg.
one tablet 10 mg contains:
active substance amlodipine besylate in terms of amlodipine - 10 mg;
Excipients: lactose (Milk sugar) - 134.0 mg, potato starch - 13.0 mg, povidone (kollidon 25) - 5.7 mg, microcrystalline cellulose - 32.0 mg, magnesium stearate - 1.4 mg.
Description: white or almost white tablets with a score on one side and a chamfer on both sides. Light marbling is allowed.
Pharmacotherapeutic group:
blocker of "slow" calcium channels.ATX code C08CA01
PHARMACOLOGICAL PROPERTIES
Pharmacodynamics
The dihydropyridine derivative is a second-generation blocker of “slow” calcium channels, has an antianginal and hypotensive effect. By binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes). The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: in case of angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces total peripheral vascular resistance, reduces preload on the heart, and reduces myocardial oxygen demand. By expanding the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including those caused by smoking). In patients with angina pectoris, a single daily dose increases the time of physical activity, slows down the development of angina and “ischemic” depression of the ST segment, reduces the frequency of angina attacks and nitroglycerin consumption.
It has a long-term dose-dependent hypotensive effect.
The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the patient’s “lying” and “standing” position). Does not cause a sharp decrease in blood pressure, exercise tolerance, or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy, has an antiatherosclerotic and cardioprotective effect in coronary heart disease (CHD). It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate (HR), inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. Does not have adverse effects on metabolism and blood plasma lipids. The onset of the effect is 2-4 hours, the duration of the effect is 24 hours.
Pharmacokinetics
After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64%, the maximum concentration in the blood serum is observed after 6-9 hours. A stable equilibrium concentration is achieved after 7 days of therapy. Food does not affect the absorption of amlodipine. The mean volume of distribution is 21 L/kg body weight, indicating that most of the drug is in the tissues and a relatively smaller portion is in the blood. Most of the drug in the blood (95%) binds to blood plasma proteins.
Amlodipine undergoes slow but extensive metabolism (90%) in the liver with the formation of inactive metabolites and has a “first pass” effect through the liver. Metabolites do not have significant pharmacological activity.
After a single oral dose, the half-life (T 1/2) varies from 31 to 48 hours; with repeated administration, T 1/2 is approximately 45 hours. About 60% of the dose taken orally is excreted in the urine, mainly in the form of metabolites, 10% unchanged, and 20-25% in feces, as well as in breast milk. The total clearance of amlodipine is 0.116 ml/s/kg (7 ml/min/kg, 0.42 l/h/kg).
In elderly patients (over 65 years of age), the elimination of amlodipine is slower (T 1/2 65 hours) compared to young patients, but this difference is not clinically significant. In patients with liver failure, a prolongation of T1/2 is expected, and with long-term administration, the accumulation of the drug in the body will be higher (T1/2 up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier. It is not removed by hemodialysis.
Indications for use
Arterial hypertension(monotherapy or in combination with other antihypertensive drugs).
Angina pectoris, vasospastic angina (Prinzmetal angina)
Contraindications
- hypersensitivity to amlodipine and other dihydropyridine derivatives;
- severe arterial hypotension;
- collapse, cardiogenic shock;
- unstable angina (with the exception of Prinzmetal angina)
- pregnancy and lactation period;
- age under 18 years (efficacy and safety have not been established).
Carefully: liver dysfunction, sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after) , diabetes mellitus, lipid profile disorders, old age.
Directions for use and doses
Orally, initial dose for treatment arterial hypertension and angina pectoris is 5 mg of the drug 1 time per day. The maximum dose can be increased to 10 mg once a day. For arterial hypertension, the maintenance dose can be 5 mg per day.
For angina pectoris and vasospastic angina- 5 - 10 mg per day, once. For thin patients, short patients, elderly patients, patients with impaired liver function, an initial dose of 2.5 mg is prescribed as an antihypertensive agent; as an antianginal agent - 5 mg.
No dose change is required when administered concomitantly with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors. No dose changes are required in patients with renal failure.
Side effect
From the cardiovascular system: palpitations, shortness of breath, marked decrease in blood pressure, fainting, vasculitis, edema (swelling of the ankles and feet), flushing of the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain, orthostatic hypotension, very rarely - development or worsening of heart failure, extrasystole, migraine.
From the central nervous system: headache, dizziness, fatigue, drowsiness, mood changes, convulsions, rarely - loss of consciousness, hypoesthesia, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams, very rarely - ataxia, apathy, agitation, amnesia .
From the digestive system: nausea, vomiting, epigastric pain, rarely - increased levels of liver transaminases and jaundice (caused by cholestasis), pancreatitis, dry mouth, flatulence, gum hyperplasia, constipation or diarrhea, very rarely - gastritis, increased appetite, anorexia, hyperbilirubinemia.
From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, sexual dysfunction (including decreased potency); very rarely - dysuria, polyuria.
From the skin: very rarely - xeroderma, alopecia, dermatitis, purpura, skin discoloration.
Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria), angioedema.
From the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with long-term use); very rarely - myasthenia.
Others: rarely - gynecomastia, polyuricemia, weight gain/loss, thrombocytopenia, leukopenia, hyperglycemia, blurred vision, diplopia, conjunctivitis, eye pain, tinnitus, back pain, dyspnea, nosebleeds, increased sweating, thirst; very rarely - cold sticky sweat, cough, rhinitis, parosmia, impaired taste, impaired accommodation, xerophthalmia.
Overdose
Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation..
Treatment: gastric lavage, administration of activated charcoal, maintaining the function of the cardiovascular system, monitoring indicators of heart and lung function, elevated position of the extremities, monitoring the volume of circulating blood and diuresis. To restore vascular tone, use vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of blockade of calcium channels - intravenous administration of calcium gluconate. Hemodialysis is not effective.
Interactions with other drugs
Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes reduce it.
The hypotensive effect is weakened by nonsteroidal anti-inflammatory drugs, especially indomethacin (sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenergic agonists, estrogens (sodium retention), and sympathomimetics.
Thiazide and loop diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates enhance the antianginal and hypotensive effects.
Amiodarone, quinidine, alpha 1-blockers, antipsychotic drugs (neuroleptics) and slow calcium channel blockers may enhance the hypotensive effect.
Does not affect the pharmacokinetic parameters of digoxin and warfarin.
Cimetidine does not affect the pharmacokinetics of amlodipine.
When used together with lithium drugs, it is possible to increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Calcium supplements may reduce the effect of slow calcium channel blockers.
Procainamide, quinidine, and other drugs known to prolong the QT interval enhance the negative inotropic effect and may increase the risk of significant QT prolongation.
Grapefruit juice may reduce the plasma concentration of amlodipine, but this decrease is so small that it does not significantly alter the effect of amlodipine.
special instructions
During the treatment period, it is necessary to monitor body weight and sodium intake, and prescribe an appropriate diet.
It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia). The dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.
Despite the absence of withdrawal syndrome with slow calcium channel blockers, a gradual dose reduction is recommended before stopping treatment.
Amlodipine does not affect plasma concentrations of K + , glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen.
Impact on the ability to drive a car and operate machinery
There have been no reports of the effect of amlodipine on driving or using machinery. However, some patients may experience drowsiness and dizziness, primarily at the beginning of treatment. If they occur, the patient must take special precautions when driving and operating machinery.
Release form
Tablets of 5 mg and 10 mg.
10, 30 tablets per blister pack.
10, 20, 30, 40, 50 or 100 tablets in a polymer container for medicines or a glass bottle with screw-on plastic caps.
One container (bottle) or 1, 2, 3, 4, 5, 6, 8 or 10 strip packaging along with instructions for use are placed in a cardboard pack.
5, 10 or 20 containers (bottles) or 20, 40, 60, 80 and 100 blister packs together with instructions for use are placed in a cardboard box for hospitals.
Storage conditions
List B. In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date indicated on the package.
Conditions for dispensing from pharmacies
On prescription.
Manufacturer
Ozon LLC
Legal address:
445351 Russia, Zhigulevsk, Samara region, st. Pesochnaya, 11.
Address for correspondence (actual address, including for receiving claims):
445351 Russia, Zhigulevsk, Samara region, st. Hydrostroiteley, 6.