Amlodipine instructions for use, contraindications, side effects, reviews. Amlodipine: description, principle of action and distribution of the active components of the drug in the body


A drug Amlodipine- a calcium channel blocker of the group of dihydropyridine derivatives. One of the regulatory mechanisms in cells and tissues is a change in the concentration of Ca2+ ions in the cytoplasm and intercellular fluid. In this case, the exchange is carried out through special channels in cell membranes, they are of 6 types and are localized in various organs and tissues. Amlodipine is able to selectively block L-type channels located in the vascular wall and in the myocardium, in particular in the cells of the contractile and conduction systems of the heart muscle. By blocking the passage of calcium ions through the membrane, the drug prevents the increase in intracellular calcium concentration. As a result, the contractile activity of the cells of the vascular wall is inhibited, the vascular tone decreases, and blood pressure decreases. When taking the recommended doses of the drug, its effect on the vascular tone of the venous bed is not observed, thus, when taking therapeutic doses of the drug, the development of orthostatic hypotension is impossible.
Due to the gradual intake of Amlodipine to target cells and its long-term effect, reflex tachycardia does not develop during its use, since the decrease in vascular tone occurs gradually, due to this there are no fluctuations in blood pressure, which is typical for other drugs in this group. Under the action of the drug, not only arteries and arterioles expand, but also peripheral vessels, including coronary ones, thus, the intensity of manifestations of ischemia of the heart muscle decreases, and the course of angina pectoris is facilitated. By reducing vascular tone without increasing the heart rate, the load on the heart is reduced, which also helps to reduce the heart's need for oxygen.
A drug Amlodipine has a weak diuretic effect (accelerates glomerular filtration and excretion of sodium from the body). Promotes the production of nitric oxide, has antioxidant abilities.
The therapeutic effect occurs 2-4 hours after oral administration of the drug and lasts for a day (the effect persists at rest and in a state of physical activity).
Amlodipine slowly absorbed from the gastrointestinal tract, while the degree of adsorption does not depend on food intake. It has a high (more than 65%) bioavailability. The maximum plasma concentration is reached after oral administration after 6 hours, plasma protein binding is almost 98%. It penetrates well through the placental and blood-brain barriers, is excreted in breast milk. Metabolism of the drug occurs in the liver, excreted mainly by the kidneys, but some part is excreted in the feces. The half-life is 35 hours, in elderly patients and patients with insufficient liver function, the half-life is almost doubled.

Indications for use

A drug Amlodipine used to treat arterial hypertension in adults (both monotherapy with Amlodipine and its combination with other antihypertensive drugs are allowed); angina pectoris, Prinzmetal's angina pectoris (vasospastic angina pectoris), including therapy is indicated in cases where nitrates and B-blockers do not have the expected effect; ischemic heart disease, including chronic. The drug can be used in patients with chronic heart failure and bronchial asthma.

Mode of application

In the treatment of uncomplicated hypertension take 2.5 mg of the drug Amlodipine 1 time per day.
With hypertension complicated by coronary heart disease and angina, take 5 mg of the drug 1 time per day.
If necessary, the dose of the drug can be increased to 10 mg.
The maximum daily dose is 10 mg.
In complex therapy with other antihypertensive drugs, amlodipine does not require dose adjustment.
In patients with renal insufficiency and elderly patients, dose adjustment is not required.

Side effects

From the side of the cardiovascular system and the hematopoietic system: shortness of breath, swelling of the extremities, hyperemia of the upper face and body, chest pain, hypotension, migraine, extrasystole, possible heart rhythm disturbances. Thrombocytopenia, leukopenia, hyperglycemia.
From the side of the central nervous system: dizziness, fatigue, headache, disturbed sleep and wakefulness. Convulsions, tremor, asthenia, loss of consciousness, paresthesia, nervousness, depression, increased anxiety, apathy, amnesia.
From the gastrointestinal tract: pain in the epigastric region, nausea, vomiting. Changes in the activity of liver enzymes, increased levels of bilirubin, dry mouth, impaired stool, flatulence, increased appetite, gastritis, pancreatitis.
Others: violation of urination, violation of sexual function, the development of pathologies of the joints, myasthenia gravis is possible.

Dermatitis, pruritus, urticaria, erythematous rash.
Possible impaired visual function (including impaired accommodation, eye pain, diplopia, conjunctivitis), ringing in the ears, changes in body temperature, nosebleeds, increased sweating.

Contraindications

Contraindications to the use of the drug Amlodipine are: increased individual sensitivity to the components of the drug, arterial hypotension, cardiogenic shock, collapse, pregnancy and lactation.
The drug is prescribed with caution in patients with chronic heart failure, diabetes mellitus, impaired lipid metabolism, impaired liver function, elderly patients and persons under 18 years of age.
It is also prescribed with caution to patients who have had a myocardial infarction (especially the first month after an acute myocardial infarction).

Pregnancy

Studies regarding the safety of the drug Amlodipine during pregnancy were not carried out, therefore, taking the drug is possible only under the strict supervision of the attending physician, if the expected benefit to the mother is higher than the possible risks to the fetus.
If it is necessary to prescribe the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding for the period of treatment.

Interaction with other drugs

Ca2+ preparations may reduce the effect Amlodipine. Sympathomimetic drugs, estrogens, non-steroidal anti-inflammatory drugs also reduce the effectiveness of Amlodipine. Drugs that reduce the activity of liver enzymes can increase the toxic effect of Amlodipine and contribute to the manifestation of its side effects. Diuretics, B-blockers, ACE inhibitors, neuroleptics, nitrates and amiodarone can potentiate the action of Amlodipine. Amlodipine does not affect the intake of cardiac glycosides (including digoxin). Simultaneous administration with lithium preparations increases their toxicity and contributes to the manifestation and intensification of side effects.

Overdose

Overdose Amlodipine patients have hypotension, tachycardia, excessive expansion of peripheral vessels. In case of an overdose, gastric lavage, the use of adsorbing agents, symptomatic therapy, including the maintenance of the functions of the cardiovascular system, are indicated. It is recommended to constantly monitor blood pressure, change the position of the patient's body so that the limbs are at some elevation. Intravenous administration of calcium and dopamine preparations is also shown. Overdose Amlodipine hemodialysis has no effect.

Storage conditions

Amlodipine store in a dry place away from direct sunlight, at a temperature not exceeding 25 degrees Celsius. Shelf life - 2 years.

Release form

Tablets of 2.5; 5 or 10 mg of active ingredient, 10 pcs. in a blister, 1 or 3 blisters in a carton.
5 or 10 mg of the active substance, 100 pcs. in a bank of polymeric materials, in a cardboard box.

Compound

1 tablet of the drug Amlodipine contains:
Amlodipine besylate (in terms of amlodipine) - 2.5; 5 or 10 mg;
Excipients.

main parameters

Name: AMLODIPINE
ATX code: C08CA01 -

Amlodipine- a remedy from the group of calcium channel blockers, which is used to treat hypertension and stable angina pectoris. Amlodipine is a drug for continuous use, aimed at preventing angina attacks and the progression of arterial hypertension.

I recently started suffering from high blood pressure. Previously, even if it increased (I did not measure it), it did not bring me any discomfort at all.

I went to the doctor about this during the first hypertensive crisis, after which I was examined and treated.

Initially, I was prescribed, - a combination drug that includes two substances: an ACE inhibitor and a diuretic.

I took Noriprel A for a very short time, as I was faced with the appearance of new unpleasant symptoms. In particular, I periodically had dizziness, it got dark in my eyes. I even fainted a few times!

Naturally, I thought it was some kind of side effect of Noriprel and reported it to my doctor. It turned out that my body, for unknown reasons, reacts too strongly to the active ingredients of this drug, which was manifested by a sharp drop in pressure. BP was reduced much more than was necessary in the treatment of hypertension.

There was a question about changing the treatment, and I was prescribed amlodipine, a drug from another group ( it can also be used to prevent angina attacks). Against the background of taking Amlodipine, the pressure stabilized. Since then, for the treatment of hypertension, I drink only this medicine.

Hypotension was a rather serious complication, and, moreover, a dangerous complication! Amlodipine, of course, is also far from being an ideal drug, but it did not cause such side effects in me. After I started taking Amlodipine, I started to have swelling of the legs (then they disappeared) and periodic headache. But that doesn't seem scary to me at all.

By the way, in addition to these reactions , in the treatment of amlodipine may be observed also:

  • feeling of heartbeat;
  • feeling of "a rush of blood to the face";
  • drowsiness, dizziness;
  • nausea and abdominal pain;
  • skin rash;
  • pain in the limbs, a feeling of "running goosebumps" on the skin of the legs.

These side effects are quite common, but as you can see, they are not dangerous.

Also worth mentioning is how amlodipine interacts with other drugs.

For example, drugs for the treatment of atherosclerosis (statins, in particular) are not recommended to be taken together with many antihypertensive drugs, since their effect is significantly reduced. Amlodipine, according to my doctor, can be "mixed" with statins: I continue to take (rosuvastatin) calmly.

It turned out differently with another drug that I had previously taken. My knee joints periodically hurt (for many years already!), And in such a situation it always helped me - in ointment or in tablets. This is an anti-inflammatory agent, the active substance there is - diclofenac. Now I can't take this drug. because they are not compatible with Amlodipine. I even noticed the reason myself: I had never had such stomach pains from Diklak before.

Amlodipine is combined with almost all groups of drugs for the treatment of hypertension,- this is a rather rare and very useful feature of this remedy.

Here, to the information on how and with what you can combine Amlodipine, I will add a list contraindications:

  • acute myocardial infarction (within a month after it, Amlodipine should not be taken);
  • shock conditions;
  • unstable angina (rapidly progressive).

Especially Care must be taken when using Amlodipine people who suffer:

  • aortic stenosis;
  • heart failure;
  • liver diseases;

Children and pregnant women this drug should only be used if it is known for certain that the benefit of the treatment outweighs the potential harm.

Amlodipine is an anti-angial, antihypertensive, calcium channel blocker.

Release form and composition

Amlodipine is available as 5 mg or 10 mg tablets. There are 10 pieces in a blister pack, 100 pieces in a polymer jar. In a carton box - 1 can or 1, 2, 3, 4, 5 cell packs.

1 tablet 5 mg/10 mg contains:

Amlodipine besylate - 6.9 mg / 13.8 mg, which corresponds to 5 mg / 10 mg amlodipine;

  • Lactose monohydrate - 85.7 mg / 171.4 mg;
  • Povidone - 3.2 mg / 6.4 mg;
  • Crospovidone - 3.2 mg / 6.4 mg;
  • Calcium stearate - 1 mg / 2 mg.

Indications for use of Amlodipine

Indication for the use of Amlodipine is the presence of the following diseases:

  • Essential (primary) hypertension;
  • secondary hypertension;
  • Angina pectoris (angina pectoris);
  • Angina pectoris with documented spasm;
  • Chronic ischemic heart disease.

In arterial hypertension, the drug is used as an independent drug or in combination with other antihypertensive drugs. With stable or vasospastic angina pectoris, it is also used in patients who are resistant to therapy with beta-blockers or nitrates.

Contraindications

Amlodipine is contraindicated in case of hypersensitivity to any components of the drug or other dihydropyridines, as well as arterial hypotension (90 mm Hg and below), shock, acute myocardial infarction and within 1 month after it.

Method of application and dosage of Amlodipine

The drug is taken orally.

In the instructions for Amlodipine, the initial dosage in the treatment of angina pectoris and arterial hypertension is 5 mg 1 time per day. The maximum daily dose should not exceed 10 mg.

The maintenance dose for arterial hypertension is 2.5-5 mg per day. With vasospastic angina or exertional angina - 5-10 mg per day. For the prevention of angina attacks - 10 mg per day.

Patients with impaired liver function Amlodipine should be administered with caution. The initial dose as an antihypertensive agent is 2.5 mg, and antiangial - 5 mg.

In elderly patients, an increase in the half-life of the drug and a decrease in creatinine levels are possible. The dosage does not change, but medical supervision is necessary.

A dose change is not required for patients with renal insufficiency, as well as for the combination of Amlodipine with angiotensin-converting enzyme inhibitors, beta-blockers and thiazide diuretics.

Side effects of Amlodipine

Amlodipine may cause the following side effects:

  • On the part of the blood (hemostasis, hematopoiesis) and the cardiovascular system - flushing of the skin of the face, palpitations, bradycardia, ventricular tachycardia, atrial flutter, chest pain, hypotension (including orthostatic);
  • From the sensory organs and the nervous system - fatigue, headache, dizziness, drowsiness, fatigue, asthenia, visual disturbances, mood changes;
  • From the genitourinary system - peripheral edema of the feet and ankles, frequent urination, impotence;
  • From the organs of the gastrointestinal tract - nausea, abdominal pain, dyspepsia, change in the mode of defecation, jaundice;
  • From the respiratory system - shortness of breath;
  • From the musculoskeletal system - arthralgia, myalgia, paresthesia and pain in the extremities (with prolonged treatment);
  • On the part of the skin - itching, rashes, erythema multiforme;
  • Other side effects of Amlodipine are gingival hyperplasia, gynecomastia, increased levels of liver enzymes.

Exceeding the recommended doses of the drug provokes excessive peripheral vasodilation, a pronounced and prolonged decrease in blood pressure, tachycardia. In case of an overdose of Amlodipine, according to the instructions, it is necessary to wash the stomach and take activated charcoal. In the future, the doctor should monitor the performance of the lungs and heart, the volume of circulating blood and diuresis. Supportive or symptomatic therapy may be needed - intravenous fluids, dopamine, calcium gluconate, phenylephrine. Hemodialysis is ineffective.

special instructions

The use of Amlodipine is limited in unstable angina, severe aortic stenosis, heart failure, liver dysfunction.

Data on the safety and efficacy of the drug for patients under the age of 18 years are not enough.

Appointment during pregnancy is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Category of action on the fetus according to the FDA - C.

During the period of therapy, it is necessary to stop breastfeeding, as the drug is excreted in breast milk.

During work, caution should be observed by drivers of vehicles, as well as people whose professional activities are associated with increased concentration of attention, since drowsiness and dizziness are likely at the beginning of treatment.

Amlodipine is well combined with the main antihypertensive drugs - diuretics, angiotensin-converting enzyme inhibitors, beta-blockers, as well as with nitrates and hypoglycemic drugs. Amiodarone, quinidine and other calcium antagonists can enhance the action. Non-steroidal anti-inflammatory drugs, especially indomethacin, inhibit the synthesis of prostaglandins in the kidneys and natriuresis, thereby lowering the hypotensive effect.

Amlodipine's analogs

Analogues of Amlodipine are the following drugs:

  • Tenox;
  • Stamlo;
  • Omelar Cardio;
  • Normodipin;
  • Norvask;
  • Cordy Core;
  • Karmagip;
  • Corvadil;
  • Kalchek;
  • Cardilopin;
  • Vero-Amlodipine;
  • Amlorus;
  • Amlotop;
  • Amlonorm;
  • Acridipine;
  • Amlodac;
  • Amlocard-Sanovel;
  • Amlong;
  • Amlodipharm;
  • Amlovas;
  • Amlodigamma.

Replacement of the drug should be made strictly on the recommendation of a doctor.

Terms and conditions of storage

Store in a dry, dark place, at a temperature not exceeding 25 °C. Keep away from children.

Shelf life - 3 years.

Due to problems with blood vessels, malnutrition, stress and certain diseases, many people suffer from high blood pressure. To help maintain a normal state, you need to use effective medications. A popular remedy is the pressure drug Amlodipine, which effectively reduces high blood pressure.

What is Amlodipine

According to the classification, amlodipine tablets are included in the group of antihypertensive drugs that reduce pressure by relaxing the smooth muscles of the vessels. They are produced by Russian and foreign pharmaceutical companies. The drug acts due to the active substance of the same name. The antianginal effect of the drug lasts more than a day, which helps to keep pressure indicators under control.

pharmachologic effect

Amlodipine pressure tablets are second-generation slow calcium channel blockers. Their active substance belongs to dihydropyridine derivatives, has hypotensive and antianginal effects. The component binds to dihydropyridine receptors, reduces the transmembrane transition of calcium ions into the cell.

The antianginal effect of the drug is due to the expansion of peripheral and coronary arteries, arterioles. With angina pectoris, amlodipine reduces the severity of myocardial ischemia, preload on the heart, myocardial oxygen demand, and expands peripheral arterioles. The remedy can prevent the development of spasm of the coronary arteries, reduce the frequency of angina attacks and the need for nitroglycerin.

The drug has a long-term hypotensive effect, which is associated with a vasodilating effect on the smooth muscle tissue of the vessels. With the development of arterial hypertension, pressure decreases. The advantages of the drug include the fact that it does not provoke a sharp decrease in pressure, a decrease in exercise tolerance. The tool helps to stop the symptoms of left ventricular myocardial hypertrophy.

The drug does not provoke a reflex increase in the frequency of heart contractions, increases the glomerular filtration rate, and prevents platelet aggregation. In the presence of diabetic nephropathy, the drug Amlodipine does not lead to an increase in signs of microalbuminuria. The drug is not able to have a negative impact on metabolic processes, plasma lipids.

In case of arterial hypertension, a single daily dose of the drug reduces pressure for a day, reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects during ischemia. The drug does not affect the contractility and conductivity of the myocardium, inhibits platelet aggregation, and has a weak natriuretic effect. Its therapeutic effect occurs within three hours and lasts for 24 hours.

Amlodipine is slowly absorbed without dependence on food, has a 64% bioavailability, reaches a maximum concentration after 7.5 hours. The component binds to plasma proteins by 95%, penetrates the blood-brain barrier, undergoes metabolism in the liver with the formation of inactive metabolites. The remainder of the dose is excreted in 70 hours by the kidneys, intestines, and bile. Not subject to hemodialysis.

Indications for use

The drug Amlodipine is prescribed for the development of pathologies of the cardiovascular system. Indications for use are:

  • arterial hypertension (combination with other treatment or as monotherapy);
  • stable angina pectoris;
  • dilated cardiomyopathy;
  • Prinzmetal's angina;
  • chronic heart failure;
  • vasospastic angina;
  • cardiac ischemia;
  • bronchial asthma.

Compound

Amlodipine for pressure is available only in tablet format. Their composition, indicating the main and auxiliary substances:

How to take Amlodipine for high blood pressure

The drug is taken orally, regardless of the meal. Tablets should not be chewed or crushed, they must be washed down with water. In the treatment of arterial hypertension, for the prevention of attacks of angina pectoris and vasopathic type, an initial dose of 5 mg once / day is prescribed, if necessary, increased to a maximum of 10 mg. For violations of the liver, the initial dose is 2.5 mg, for antianginal treatment - 5 mg once / day.

With an infrequent increase in blood pressure, you can take a tablet a day, preferably in the morning. If improvement is not observed, the dosage can be increased to two tablets per day, taken at a time. Long-term use requires reducing the dose to half a tablet per day. With arterial hypertension, 0.5 tablets / day are prescribed for a supporting action. In heart disease, 1-2 tablets / day are recommended on an ongoing basis.

In renal insufficiency and in the elderly, dose adjustment is not required, but patients need careful monitoring. Special instructions for the safe use of Amlodipine for pressure:

  1. The dose of the drug does not change when combined with thiazide diuretics, monoamine oxidase inhibitors, beta-blockers.
  2. During drug therapy, the body weight of patients, the amount of sodium chloride they consume should be monitored, if necessary, prescribing a diet with salt restriction.
  3. To prevent soreness, hyperplasia and bleeding of the gums, it is necessary to monitor oral hygiene and visit the dentist regularly.
  4. Before stopping treatment with tablets, the dose is gradually reduced. Abrupt withdrawal may lead to deterioration (angina pectoris and hypertensive crisis).
  5. The drug does not affect the change in the concentration of potassium ions, triglycerides, uric acid, glucose, cholesterol, creatinine, low-density lipoproteins, urea nitrogen in the blood.
  6. The drug should not be used in hypertensive crisis. Dose changes may be required for low body weight, short stature of patients.
  7. The drug should be used with caution when driving vehicles and operating dangerous machinery, because it can cause drowsiness and dizziness.
  8. It is forbidden to combine with ethanol, alcohol and grapefruit juice.

High blood pressure in type 2 diabetes

Patients with type 2 diabetes often have hypertension. It is difficult to choose a drug for them that would not affect the deterioration of metabolism. Amlodipine refers to medicines that are allowed to drink from high blood pressure in diabetes mellitus. It can be combined with other drugs as part of complex therapy. The dosage is 5-10 mg per day. In diabetics, tablets reduce the risk of heart attacks, do not reduce glucose, cholesterol and triglycerides, do not worsen cell sensitivity to insulin and do not increase its plasma concentration.

Hypertension in the elderly

Compared to eprosartan, the blood pressure drug amlodipine is better at lowering blood pressure in the elderly. Doctors recommend combining it with Indapamide, a diuretic drug that differs from other diuretics in safety and the absence of side effects. In older people, there is a risk of a sharp drop in blood pressure when getting up from a sitting or lying position (orthostatic hypotension). The pressure medicine Amlodipine eliminates this problem, acting smoothly and evenly. The dosage is 2.5-5 mg / day.

Overdose

If you take an increased dose of the drug, it can cause an overdose. Its symptoms are a sharp decrease in pressure, the development of reflex tachycardia and peripheral vasodilation with the risk of shock, death. Treatment consists of gastric lavage, activated charcoal, transfer of the patient to the Trendelenburg position (lying on his back with the pelvis raised by 45 degrees). Vasoconstrictor drugs or intravenous administration of calcium gluconate may be prescribed.

Side effects

During therapy with Amlodipine, side effects from various body systems may occur. These include:

  • palpitations, peripheral edema, orthostatic hypotension, vasculitis, bradycardia, tachycardia, atrial fibrillation, myocardial infarction, migraine, chest pain;
  • headache, dizziness, fatigue, malaise, fainting, asthenia, paresthesia, hypesthesia, neuropathy, tremor, convulsions, apathy, amnesia, ataxia, agitation, depression;
  • blurred vision, diplopia, spasm of accommodation, conjunctivitis;
  • thrombocytopenia, purpura, leukopenia;
  • shortness of breath, rhinitis, cough;
  • nausea, abdominal pain, vomiting, flatulence, constipation, diarrhea, dyspepsia, anorexia, thirst, taste disturbances, dry mouth, gum hyperplasia, increased appetite, pancreatitis, gastritis, jaundice, hepatitis;
  • pollakiuria, painful urination, dysuria, nocturia, polyuria;
  • gynecomastia, impotence;
  • myasthenia gravis, back pain, arthralgia, myalgia, arthrosis, convulsions;
  • increased sweating, cold sweat, alopecia, xeroderma, impaired skin pigmentation, dermatitis;
  • allergy, rash, itching, urticaria, erythema, angioedema;
  • tinnitus;
  • chills;
  • weight gain;
  • nose bleed;
  • parosmia;
  • hyperglycemia.

Contraindications

Amlodipine at high pressure is prescribed with caution to patients with impaired liver function, severe bradycardia or tachycardia, chronic non-ischemic heart failure, aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction. Contraindications for the use of tablets are:

  • severe arterial hypotension;
  • collapse, cardiogenic shock;
  • unstable angina;
  • severe arterial stenosis;
  • lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
  • pregnancy, lactation (breastfeeding);
  • age up to 18 years;
  • hypersensitivity to the composition, derivatives of dihydropyridine.

drug interaction

Together with the drug, diuretics, ACE inhibitors (angiotensin-converting enzyme), beta-blockers, angiotensin receptor blockers can be prescribed. Other drug interactions:

  1. Inhibitors of microsomal oxidation with simultaneous use increase the concentration of amlodipine in the blood plasma, leading to an increase in side effects, and inducers of microsomal liver enzymes reduce its pharmacokinetic properties.
  2. Thiazide and loop diuretics, Verapamil, nitrates, Amiodarone, quinidine, alpha-blockers, antipsychotics, isoflurane, antiviral drugs (ritonavir) enhance the antiangial and hypotensive effects of the drug.
  3. Calcium preparations reduce the effect of the drug
  4. Lithium preparations increase neurotoxicity.
  5. No interaction was found with Digoxin, Warfarin, Cimetidine.

During pregnancy and lactation

According to animal studies, there was no teratogenic or inotropic effect of the active component of the tablet composition on the fetus. There is no experience of using the drug during pregnancy and lactation, therefore the drug is not prescribed to pregnant and lactating women. Also, you should not take pills for women of childbearing age who do not use reliable methods of contraception.

Amlodipine analogues with the least side effects

Drugs with minimal side effects, according to reviews, that do not cause swelling of the legs and do not impair metabolism, can replace the remedy. These include:

  • Duaktin - capsules help with hypertension, chronic heart palpitations, have a minimum number of contraindications.
  • Tenox - the drug is prescribed for severe hypertension and chronic angina pectoris, but is not suitable for acute heart failure.
  • Stamlo - capsules and tablets for arterial hypertension, are contraindicated in severe cases of the disease.
  • Normodipin - can normalize blood pressure in a short time, improve the functioning of the heart and blood vessels, is contraindicated in recent acute myocardial infarction.
  • Emlodin - an inexpensive analogue in the form of tablets, is prohibited in case of severe hypotension, impaired functioning of the left ventricle.

Price

The drug can only be bought with a prescription. The product is stored in a dry, dark place at temperatures up to 25 degrees for three years from the date of manufacture. The drug can be bought in the online store or ordered through the pharmacy catalog. The approximate cost of tablets in Moscow will be:

Type of packaging (number of tablets in a pack, concentration of the active substance)

Manufacturer

Internet price tag, rubles

Pharmacy cost, rubles

Hemofarm

Canonpharma

10 mg 30 pcs.

Canonpharma

10 mg 60 pcs.

Canonpharma

10 mg 90 pcs.

10 mg 20 pcs.

Hemofarm

Video

Formula: C20H25ClN2O5, chemical name: 2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridine dicarboxylic acid 3-ethyl 5-methyl ester (in form of besylate and maleate).
Pharmacological group: organotropic agents / cardiovascular agents / calcium channel blockers / dihydropyridine derivative - II generation calcium antagonist.
Pharmachologic effect: vasodilating, antianginal, hypotensive, antispasmodic.

Pharmacological properties

By binding to dihydropyridine receptors, amlodipine blocks calcium channels, inhibits the passage of calcium ions through the membrane into the cell (this mainly occurs in vascular smooth muscle cells, to a lesser extent in cardiomyocytes). It has a prolonged hypotensive effect (reduces blood pressure), the duration of which depends on the dose. The decrease in blood pressure occurs due to a direct relaxing effect on vascular smooth muscle, which leads to a decrease in total peripheral vascular resistance (OPVR). The severity of myocardial ischemia decreases, as peripheral arterioles expand, and OPSS decreases against the background of a slightly changing pulse rate. As a result of reducing the load on the heart, myocardial oxygen demand also decreases; the expansion of the coronary arteries and arterioles occurs in unchanged and ischemic areas of the heart, the supply of oxygen to the myocardium increases. Amlodipine has little effect on the sinoatrial and sinus node, slightly reduces AV conduction. Reduces platelet aggregation; increases the filtration rate in the renal glomeruli, sodium excretion and diuresis. These effects develop 1-2 hours after taking amlodipine and last about a day. Due to the fact that the action of amlodipine develops gradually, and the effect is prolonged, there is a gradual decrease in blood pressure and minimal reflex stimulation of the sympathetic nervous system. In hypertension, the degree of left ventricular myocardial hypertrophy also decreases; Amlodipine has a cardioprotective and antiatherosclerotic effect in ischemic disease. Amlodipine does not increase the risk of death in patients who suffer from heart failure (NYHA class III-IV) during treatment with digoxin, ACE inhibitors, diuretics. Absorption of amlodipine does not depend on food intake and occurs slowly, but almost completely. Bioavailability is 60-65% (due to the effect of "first pass" through the liver). The maximum concentration of amlodipine in the blood is reached after 6-12 hours. Plasma protein binding is 97–98%. With constant intake, the equilibrium concentration will be reached in 7-8 days. The volume of distribution is 20 l/kg. Amlodipine passes through the blood-brain barrier. In the liver it is biotransformed with the formation of inactive metabolites; elimination consists of 2 phases: the first phase is short, the second lasts 35–50 hours. The general clearance - 0,5 l/min. It is excreted in the urine (60% as metabolites, 10% unchanged), with bile (20-25% as metabolites) and in breast milk. The half-life in case of impaired liver function and in the elderly is extended, and in case of impaired renal function it does not change.

Indications

Amlodipine is used for arterial hypertension (as monotherapy, as well as in combination with other antihypertensive drugs); vasospastic (Prinzmetal) and stable angina, including can be used by patients who are resistant to treatment with beta-blockers or nitrates.

Dosing and Administration of Amlodipine

Amlodipine is taken orally, the initial dose is 2.5-5 mg 1 time per day, the usual dose is 5 mg per day, if necessary, the dose can be gradually increased to a maximum of 10 mg 1 time per day. Take after meals with a small amount of water.
If you miss the next dose of amlodipine, you must take the drug as you remember, the next dose should be taken in a day.
Carefully use amlodipine for stenosis of the aortic orifice, disorders of the liver and kidneys. Elderly patients do not require dose reduction. It is possible to use amlodipine in the treatment of patients with dilated (or non-ischemic) cardiomyopathy, which accompanies a severe form of chronic heart failure. Use with caution for drivers of vehicles and people whose professions are associated with increased concentration of attention (at the beginning of therapy, drowsiness and dizziness are possible).

Contraindications and restrictions for use

Hypersensitivity (also to other drugs of the dihydropyridine subgroup), hypotension (less than 90 mm Hg), acute myocardial infarction (also a period of 1 month after it), shock. Amlodipine should be limited in use for unstable angina, heart failure, severe aortic stenosis, impaired liver function, under the age of 18 years (efficacy and safety of use have not been determined).

Use during pregnancy and lactation

It is not recommended to use amlodipine during pregnancy, but it is possible in cases where the intended benefit of treatment outweighs the possible risk to the fetus. At the time of treatment with amlodipine stop breastfeeding.

Side effects of amlodipine

Circulatory system: palpitations, flushing of the skin of the face, rarely - arrhythmias (bradycardia, atrial flutter, ventricular tachycardia), hypotension (also orthostatic), chest pain; nervous system: fatigue, headache, drowsiness, dizziness, rarely - fatigue, mood changes, asthenia, visual disturbances;
urinary system: peripheral edema (swelling of the feet and ankles), rarely - impotence, increased frequency of urination;
digestive system: abdominal pain, nausea, rarely - a change in the mode of defecation, dyspepsia, jaundice;
respiratory system: rarely shortness of breath; system of support and movement: rarely - myalgia, arthralgia, pain and paresthesia in the limbs (with prolonged use);
leather: itching, rashes, rarely - erythema multiforme;
others: rarely - gynecomastia, gingival hyperplasia, increased levels of liver enzymes.

Interaction of amlodipine with other substances

With the simultaneous use of amlodipine and calcium channel blockers, agents for inhalation anesthesia, quinidine, amiodarone, an increase in the hypotensive effect is possible. With the simultaneous use of sympathomimetics, orlistat, indomethacin (and other non-steroidal anti-inflammatory drugs), estrogens, a decrease in the antihypertensive effect is possible. With the combined use of lithium carbonate, manifestations of neurotoxicity (nausea, vomiting, ataxia, diarrhea, noise and / or trembling in the ears) are possible. Amlodipine is compatible with the main groups of antihypertensive drugs (ACE inhibitors, diuretics, beta-blockers), hypoglycemic drugs and nitrates.

Overdose

With an overdose of amlodipine, a prolonged and pronounced decrease in blood pressure, excessive peripheral vasodilation, and tachycardia occur. It is necessary to wash the stomach, take activated charcoal, give the patient a horizontal position, raise the legs, monitor the performance of the lungs and heart, diuresis, blood volume, supportive and symptomatic treatment, intravenous infusion of dopamine, calcium gluconate, phenylephrine; hemodialysis is not effective.

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