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A drug to lower blood pressure. Thanks to its mechanism of action, Amlodipine has a rapid and good effect. Popular among patients. Prescribed for adults only. Therapy usually involves taking the drug daily.
Amlodipine is available only in tablet form for oral administration at a dose of 5 or 10 mg. Round tablets white. The package may contain 10 or 30 tablets placed in a blister.
Amlodipine – medicinal product from the group of dihydropyridine derivatives. Its use allows for pronounced hypotensive effect, which occurs due to the entry of calcium ions into the cells of the myocardium and blood vessels. Extends medication intake peripheral vessels without disturbing the heart rate.
The instructions for the drug indicate that taking the medication reduces the load on the heart, reduces the need for the myocardium to receive large amounts of oxygen, and at the same time dilates the large coronary arteries. Thanks to this therapeutic effect of the drug, it can be used not only for high blood pressure, but also for the treatment of angina pectoris. Taking pills allows you to control the attack and increase the time of physical activity.
The active component of the drug is amlodipine besylate in an amount of 5 or 10 mg, as well as auxiliary components.
Amlodipine is a vasodilator drug. The active component of the drug has the property of lowering blood pressure and providing the heart muscle and blood vessels with the necessary amount of oxygen. The main therapeutic effect of the drug consists of antianginal and hypotensive effects. Amlodipine binds to dihydropyridine receptors, dilates coronary and peripheral arteries, thereby providing the following properties:
After taking the drug, blood pressure decreases gradually, which does not affect general health person. The drug has a pronounced cardioprotective, anti-atherosclerotic effect, inhibits platelet aggregation, and does not cause an increase in pulse and heart rate.
Thanks to this therapeutic effect of the drug, its use allows patients suffering from hypertension and angina to improve their quality of life, reduce the risk of complications, and normalize the functioning of the heart and blood vessels.
According to the instructions for use, Amlodipine is prescribed for patients with hypertension or angina pectoris. At what blood pressure levels you should take the drug is not easy to answer, since everything depends on the characteristics of the body. It is important to note that the drug should be taken daily, regardless of the indicators.
The main indications for taking the drug are:
Taking the drug can be combined with other medications prescribed by the doctor depending on the pathology of the cardiovascular system.
The drug is contraindicated for children, therefore there is no information about indications for children in the instructions.
No clinical trials have been conducted on taking the drug for pregnant and lactating mothers, so taking the medicine is prohibited.
Amlodipine tablets are used only as prescribed by a doctor, since they have a number of contraindications:
The dose of Amlodipine and the duration of its use are determined by the doctor individually for each patient. Basically, tablets are intended for long-term use. Admission therapy can take from several months to several years.
The tablets are intended for internal use. The initial dose of the drug for hypertension is 2.5 - 5 mg once a day. For angina pectoris, it is recommended to take ½ tablet of 5 mg per day. In more severe cases the dose can be increased to 10 mg. The daily dose of the drug should not exceed 10 mg.
If the patient’s medical history includes pathologies of the liver or kidneys, the daily dose should not exceed 2.5 – 5 mg per day.
The drug is contraindicated for children.
Amlodipine is not prescribed to pregnant and nursing mothers.
Amlodipine is well tolerated, but in some cases, after its use, symptoms may appear. adverse reactions organism, including:
If such symptoms occur, you should stop taking the drug and consult a doctor who can adjust the dose of the drug or prescribe another drug.
Analogues of Amlodipine include the following drugs:
Amlodipine can be used in combination with other medications, including those intended to treat hypertension. When taking alpha-blockers and neuroleptics, the effect of Amlodipine is enhanced. The drug is not compatible with alcohol.
Antihypertensive drugs, including Amlodipine, are intended for long-term use. Patients need to take the pills daily, do not miss the dose prescribed by the doctor, and in no case exceed the dose of the medicine.
While taking Amlodipine tablets, it is important to adhere to dietary nutrition, reduce the consumption of salt, spicy and fried foods.
The daily dose of tablets should not exceed 10 mg. If the dose was increased by mistake, symptoms of overdose may appear:
Such symptoms require medical intervention, so after they appear, you should seek medical help as soon as possible.
Store at a temperature not exceeding 25 degrees. The drug is an over-the-counter drug. The expiration date of the drug is indicated on the packaging and blister with the medicine.
The cost of Amlodipine is on average 115 rubles. Prices range from 10 to 307 rubles.
The most common disease - hypertension - is getting younger every year. If a couple of decades ago a third of the population of our country suffered from it, and these were mainly people aged 45 and above, now average age hypertension dropped to 35. Increasingly high blood pressure occurs in young people under 20 years of age.
What can I say! Even modern teenagers have indicators above 140 to 90. The disease is practically incurable. To support normal level blood pressure, you have to constantly take medications, of which there are a great many. Choosing the right one is the key to a full life with hypertension.
Amlodipine is one such drug. At a low cost, it has many advantages, especially when taken in combination.
Once in the human body, the drug blocks calcium channels, which lowers blood pressure and stops attacks of diseases such as angina pectoris and coronary artery disease. Having a cumulative effect that lasts throughout the day, the drug gradually lowers blood pressure, which has a beneficial effect on the well-being of patients.
According to the instructions for use, Amlodipine normalizes the walls of blood vessels and arteries without causing excitability of the middle muscular layer of the heart, scientifically the myocardium, has a mild diuretic effect and increases the body's endurance to moderate physical activity.
The medicine promotes vasodilation, supplying the heart and brain with the necessary amount of oxygen, thereby preventing hypoxia (oxygen starvation).
For patients suffering from angina pectoris, the drug is prescribed to reduce the number of attacks of the disease and their intensity.
Amlodipine has valuable properties: it normalizes blood pressure and replenishes the heart muscle with a sufficient amount of oxygen. Its hypertensive effect is achieved by dilating blood vessels and lasts for 24 hours when using a daily dose of the drug.
The contractions of the heart and the conductivity of the heart muscle do not change, but only the work of our motor is stimulated and the walls of its blood vessels are strengthened.
Why is Amlodipine prescribed and what does it help with? Indications for the use of the drug are quite extensive. It is prescribed for:
The drug is indispensable in maintaining normal blood pressure for patients suffering from hypertension of degrees 1, 2 and 3, and any form of angina. He lets them live full life with these far from pleasant diseases.
The medicine is sold in cardboard packages with three blisters containing 10 pieces of round, beveled pills of white or slightly yellowish color in everyone. Its dosage varies - 2.5; 5 and 10 mg.
The tablets contain the active component amlodipine, as well as auxiliary components, these are:
The drug is produced by several manufacturers. On the shelves of our pharmacies you can find medicines of the following names and manufacturers:
Also, the product of the same name is produced in Nizhny Novgorod, Perm and Moscow.
For hypertension not complicated by other diseases, a single dose of 2.5 mg is prescribed.
If there are complications such as ischemia and angina, the daily dose is 5 mg.
If necessary, the dosage is increased to 10 mg per day. This is the maximum dosage of the drug.
Patients suffering from hepatic and renal failure, you should take the medicine no more than 2.5 mg per day.
Children over the age of 6 years are prescribed 2.5 mg per day. If the desired effect does not manifest itself within four weeks, the dose is increased to 5 mg.
In old age, the dosage should be increased with caution.
Take the medicine in the morning, before meals, with a small amount of water. The dose is prescribed by the doctor. You should not self-medicate to avoid unpleasant consequences.
The instructions for use indicate that this remedy It is not recommended for pregnant women and nursing mothers to use it, however, in cases where the benefits of using Amlodipine are higher than the risk for the baby, it is prescribed, but only later pregnancy.
It is known that high levels are very dangerous both for expectant mother, and for her child. If you do not reduce blood pressure in a pregnant woman, this can lead to intrauterine death of the fetus due to hemorrhage in the brain, therefore, in order to avoid fatal consequences, women in pregnancy starting from 34 weeks are prescribed Amlodipine at a dose of 5 mg.
During breastfeeding, the drug is prescribed if the mother transfers her baby to artificial feeding.
Amlodipine is successfully used to lower blood pressure in patients diagnosed with - diabetes(SD). The medicine contains no substances that change the concentration of glucose in the blood, so it is not contraindicated in diabetes.
Also, its antianginal and antihypertensive effect has a beneficial effect on patients in this category, relaxing the vascular muscles and reducing the load on the myocardium, thereby reducing the number and weakening the intensity of angina attacks.
Like many medications, Amlodipine has some contraindications. It is prohibited to use if:
The use of the drug during pregnancy and breastfeeding is discussed above.
The drug is used with particular caution in case of kidney and liver diseases, as well as in the presence of pronounced tachycardia and bradycardia.
Amlodipine is well tolerated by patients, but sometimes, when using the drug, various deviations are possible, expressing themselves:
If, when taking the drug, at least one of the following occurs: listed symptoms, then taking the drug should be stopped immediately.
In case of an overdose of the drug, a sharp decrease in blood pressure is observed, accompanied by tachycardia, which is caused by excessive vasodilation. In case of drug poisoning, you should immediately call an ambulance.
If necessary, the doctor at the appointment will select medications that will go well with Amlodipine, however, it is worth remembering that:
Amlodipine itself is powerful vasodilator, lowering blood pressure, and its simultaneous use with alcoholic drinks will enhance this effect several times, which can lead to dire consequences.
The medicine is also processed in the liver, increasing the load on it. The same thing happens with ethanol. As a result of this, the liver may simply not withstand such a load, which can also end very badly for the patient.
And in general, alcohol negatively affects both the cardiovascular system and the central nervous system, so why carry out treatment if it is immediately canceled out by drinking alcohol?
When using the drug, it is worth remembering some subtleties of administration:
The pills do not cause drowsiness and do not depress the central nervous system unless this is a side effect, so they can be safely used by people involved in driving a car.
The price of the drug depends on the number of tablets in the package, dosage, and the manufacturer. For example, the cost of 30 tablets of 5 mg of domestic production ranges from 35-50 rubles, and imported ones are an order of magnitude higher, that is, about 200 rubles. 30 pills of 10 mg each cost: from our manufacturers - about 150 rubles, and imported ones - 250-300 rubles.
The most popular analogues of the drug are Normodipin, Cardilopin, Amlovas and Norvasc.
Many patients wonder which drug is better, Normodipine or Amlodipine? Experts will tell you that the first one is produced by the famous pharmaceutical company Gedeon Richter, and also does not have as many side effects, but it is an order of magnitude higher than the cheap Amlodipine.
But it does not eliminate the side effect of swelling of the feet, so if swelling occurs, it is worth replacing these drugs with others, for example, Lisinopril.
In any case, if the medicine needs to be changed to another, you do not need to do it yourself, but it would be best to seek advice from a specialist.
Most often, their choice is why and how it should be used, you will learn in our article.
The medication affects the body in two ways: antianginal and hypotensive.. Composition of the drug: amlodipine besylate, crospovidone, lactose monohydrate, povidone, calcium stearate. Available in the form of tablets of 5 and 10 mg.
Antianginal effect is the ability to stop and effectively prevent attacks by normalizing the functioning of the heart muscle and improving coronary blood flow. The hypotensive effect is a decrease with the help of relieving spasms, leading to their narrowing.
Amlodipine tablets 10 mg
The action of the drug is based on. Thanks to this, the transition of calcium ions into the structural elements of smooth muscle vessels is stimulated. With an increase in the total amount of calcium ions, the vascular muscles decrease in size, the passage for blood flow narrows, and accordingly, blood pressure increases.
The medication prevents the increase in vascular resistance and thickening of the walls of blood ducts, due to which blood pressure decreases. The hypotensive effect is due to the control of the condition of vascular smooth muscles.
The length of the cells of smooth muscle vessels increases, the lumen expands, and blood flows faster due to a decrease in ductal resistance. Blood pressure decreases, the effect lasts for at least a day.
The antianginal effect on the body occurs due to an increase in the patency of arteries and arterioles.
The load on the heart is reduced, the myocardium receives enough oxygen. This is especially important for angina and ischemia. The risk of coronary artery spasm is reduced. IHD requires special attention to blood pressure indicators. Amplodipine helps reduce the degree of myocardial hypertrophy, has a cardioprotective and antiatheresclerotic effect on blood vessels.
The cardioprotective effect on the myocardium is due to the effective delivery of oxygen and a decrease in the load on the heart. The effect of the drug alleviates the condition of patients not only with coronary artery disease, but also with its chronic form, and reduces the risk of blood clots in atherosclerosis.
When receiving a daily dose of Amlodipine, patients with vasospasmodic angina noted a decrease in the need for other nitrates and a decrease in the number of attacks.
Amlodipine has a wide and effective application if you have the following diseases:
When prescribing the drug, therapists focus on the chronic diseases of patients, clinical picture in general, age, weight.
Amlodipine for blood pressure and angina is prescribed in a dose of 5 mg. The amount of medication is increased depending on the patient’s condition and tolerance active substance, but no more than 4 times for a single use.
There are a few :
This medication is not allowed. He is accepted into for preventive purposes for chronic diseases of the cardiovascular system, therapeutic - in the detection of coronary artery disease, hypertension.
Separately, we should talk about drug overdose.
If you increase the dose on your own and take it several times a day, the patient will need to be hospitalized. Within the walls of the clinic, gastric lavage is carried out, with the help of calcium gluconate and Dopamine, the functioning of the heart and blood vessels is restored.
To eliminate dosage symptoms at home, use plenty of fluids, vomiting, and taking activated charcoal (1 tablet per 10 kg of weight). If the condition does not improve, call an ambulance.
Patients weighing less than 40 kg and short stature are prescribed daily dose Amlodipine no more than 2.5 mg.
Any medicine has. Amlodipine tablets are no exception.
Common side effects of taking medications for hypertension include:
If there are contraindications, Amlodipine is replaced with analogues. The drug in question should be used with caution for people engaged in dangerous work that requires concentration, working with technical devices and mechanisms, or driving a car. This is due to the fact that on initial stage Treatment in half of the patients, the medication causes drowsiness and lethargy.
The use of Amlodipine for type 2 diabetes has no effect on increasing blood glucose levels. Diabetics take it as usual.
Instructions for using the drug Amlodipine in the video:
According to the opinion, Amlodipine is the best remedy to normalize blood pressure. It has gained popularity among therapists and their patients due to its convenient administration - once a day, prolonged action - blood pressure does not increase for 20-24 hours, that is, until the next dose of the drug.
Thank you
Amlodipine represents vasodilator drug from the group of slow blockers calcium channels, which has the property of lowering blood pressure and reducing the need for oxygen in the heart muscle, thereby preventing angina attacks. Amlodipine is effective in relieving and preventing angina attacks in people who are not helped by nitrates (nitroglycerin, etc.). The drug is also effective for lowering blood pressure in people who are not helped by drugs from the group of beta-blockers (Atenolol, Acebutolol, Bisoprolol, Betaxolol, Metoprolol, Nadolol, Nebivolol, Propranolol, Sotalol, Timolol, etc.).
After the transition to a market economy and the privatization of enterprises, each pharmaceutical plant had the technology for producing Amlodipine, left over from the unified system of the USSR, but now it was necessary to make its drug unique, that is, branded. And for this, an abbreviation was added to the usual, old and well-recognized name “Amlodipine”, meaning the short name of the pharmaceutical plant. But, despite the “additive” in the name, the drug remains the same Amlodipine, since it is produced using old technology. That is why all varieties of Amlodipine, despite different but very similar names, are the same drug. The only difference between the varieties of Amlodipine may be in their quality: that is, the drugs from one plant are better than the other, since it better adheres to the standards of production technology, uses more raw materials High Quality etc. Otherwise, there are no differences between the varieties, so in the further text of the article we will combine them under one common name"Amlodipine".
All varieties of Amlodipine are available in a single dosage form – tablets for oral administration. As an active ingredient, the tablets contain amlodipine in three possible dosages– 2.5 mg, 5 mg or 10 mg. In this regard, tablets are in use various dosages often indicated by names "Amlodipine 5", "Amlodipine 10" or "Amlodipine 2.5", where the number corresponds to the dose of the active component.
However, in the instructions for use you can often find an indication that the tablets contain not 5 or 10 mg of amlodipine, but 6.9 and 13.8 mg amlodipine besilate respectively. This does not mean that the dosage active substance in such tablets is higher, since in fact it is 5 or 10 mg of amlodipine. The manufacturer simply indicates how much amlodipine besylate is contained in each tablet, which, of course, is slightly more, since its mass is higher. But if you recalculate how much amlodipine besylate contains pure amlodipine, you will get the same well-known figures - 5 mg and 10 mg, respectively.
As auxiliary components Amlodipine tablets from different manufacturers may contain different substances. Therefore, to clarify the composition of the auxiliary components, you should always carefully read the leaflet with instructions included in the package of tablets from each manufacturer. Most often The following substances are added to Amlodipine tablets as auxiliary components:
Amlodipine Teva mainly differs from Amlodipine in that it is produced in pharmaceutical factories in Hungary under the direction and technology of the Israeli corporation TEVA Pharmaceutical Industries, Ltd. Amlodipine is simply produced by Russian pharmaceutical factories. Accordingly, the production technology of the same drug is significantly different, which determines all the other differences between Amlodipine Teva and Amlodipine.
Firstly, the quality of Amlodipine Teva is often higher than that of Amlodipine produced by most Russian pharmaceutical factories, which is due to several factors. For the production of Amlodipine Teva, a purer active substance with a minimum amount of impurities is used. That is, before putting it into a tablet, the active component is first purified from impurities, tested according to various parameters, and only after that is allowed onto the production line. As a result, the active substance without impurities has a more pronounced therapeutic effect, causing excellent effectiveness of the drug and minimal quantity, severity and risk of side effects. That is, by purifying the active substance, TEVA Pharmaceutical Industries, Ltd. Achieved at the same time high efficiency and a small number of side effects of Amlodipine.
However, such purification and testing of the active substance is quite expensive and labor-intensive, and in addition, requires the availability of developed and tested technology. Therefore, at many Russian pharmaceutical plants, the active substance is not purified; it is immediately put into the technological cycle. And the active substances themselves, as a rule, are purchased from large chemical laboratories in India and China, which produce them in large quantities and, accordingly, of varying quality. The same active substance with different amounts of impurities will have different therapeutic effects. Moreover, a substance with fewer impurities has better therapeutic effect, and with greater, respectively, worse. Thus, the effectiveness of Amlodipine will depend entirely on how pure the active substance is in it. And since obtaining a substance well purified from impurities requires costs, then, accordingly, the more expensive Amlodipine will be of better quality compared to the cheaper one.
Thus, the main difference between Amlodipine Teva and Amlodipine is its best quality and, accordingly, higher cost. In addition, the instructions for Amlodipine Teva may indicate side effects that are not included in those for Amlodipine. However, this does not mean that Amlodipine does not cause the same side effects as Amlodipine Teva. On the contrary, it does, and even much more often. Simply TEVA Pharmaceutical Industries, Ltd. monitors the clinical use of Amlodipine Teva and records all side effects that occur, after which it supplements the instructions by adding them to the appropriate section. Russian manufacturers of Amlodipine do not monitor the occurrence of side effects and, in principle, have little interest in everything that happens to the drug during clinical application. Therefore, their instructions are written once and do not change long time. But this only reflects the fact that the manufacturer does not record the properties of its drug and does not make timely amendments to the instructions.
The dilation of myocardial vessels and a decrease in the tension of the muscle cells themselves leads to the fact that the heart muscle requires less oxygen for normal functioning. After all, relaxed muscles need less oxygen than tense muscles. Accordingly, the myocardium acquires the ability to function normally under conditions of a small amount of oxygen. And thus, a person suffering from angina pectoris can increase exercise tolerance and reduce the frequency and severity of angina attacks.
The effect of lowering blood pressure of Amlodipine is called antihypertensive (hypotensive), and reducing the myocardial oxygen demand is called antianginal. It is the hypotensive and antianginal effect that are the main effects of Amlodipine used in clinical practice.
Due to its high safety and the absence of reflex heartbeat or a sharp decrease in blood pressure, Amlodipine can be used to treat people suffering, in addition to angina, diabetes mellitus, gout or bronchial asthma.
The antianginal and hypotensive effects of Amlodipine provide the following action:
The primary effect of Amlodipine develops 2 to 4 hours after administration and persists for 24 hours.
Amlodipine can be taken regardless of food intake, since food does not affect the extent and speed of absorption of the drug into the bloodstream. Amlodipine, taken before, during or after a meal, is absorbed equally long - within 2 - 3 hours, as a result of which the therapeutic effect appears 2 - 4 hours after taking the tablet. The drug is taken once a day, and it is optimal to do this in the morning, so that you can monitor your own well-being, as well as evaluate the effectiveness and tolerability of Amlodipine.
For hypertension In order to reduce blood pressure, Amlodipine should be taken 5 mg (1 tablet) once a day. If blood pressure does not decrease to the required limits after 1 - 2 weeks of taking Amlodipine 5 mg 1 time per day, then, provided the drug is well tolerated, its dosage can be increased to 10 mg. Accordingly, Amlodipine should be taken 10 mg once a day. The drug at a dose of 10 mg once a day is taken until it is possible to achieve a stable decrease in blood pressure and keep it within normal limits without pronounced fluctuations during the day.
After this, they switch to taking Amlodipine in a maintenance dosage - 2.5 - 5 mg once a day. Moreover, first the dose is reduced to 5 mg and taken for a week. Then reduce the maintenance dose to 2.5 mg and monitor blood pressure readings. If they are normal, that is, blood pressure remains within normal limits and there are no fluctuations, then Amlodipine continues to be taken at a maintenance dosage of 2.5 mg continuously (for years). If the blood pressure begins to rise and fall sharply when taking 2.5 mg of Amlodipine per day, then you should return to the maintenance dosage of 5 mg per day and take the drug in this mode for a long time.
For arterial hypertension Amlodipine in maintenance dosages is taken continuously, without any breaks. The drug is discontinued by a doctor only if it has become ineffective or a course of treatment with other medications is necessary. In other cases, Amlodipine cannot be discontinued, since the drug should be taken constantly to maintain blood pressure levels within safe limits.
For any type of angina In order to prevent attacks and improve exercise tolerance, Amlodipine should be taken at a dose of 5 mg once a day for 2 to 3 weeks. Then, if necessary and against the background of normal tolerability, the dose of Amlodipine is increased to 10 mg per day and taken in this regimen for several months to prevent angina attacks.
For dilated cardiomyopathy , combined with severe heart failure, Amlodipine is started at 5 mg once a day for 1 to 3 weeks. After this, if the drug is well tolerated, the dosage is increased to 10 mg per day and taken for several months in a row. If Amlodipine 10 mg per day is poorly tolerated, then the dosage should be reduced and taken 5 mg once a day for several months.
In case of angina pectoris, the drug should be discontinued gradually to avoid sharp deterioration condition and course of the disease.
Amlodipine should not be used to relieve a hypertensive crisis or an attack of angina. Also, Amlodipine should not be used for therapy in the first days after myocardial infarction.
Women during the entire period of use of Amlodipine should use contraceptive methods, since the drug cannot be taken during pregnancy.
People weighing less than 40 kg should take Amlodipine in half dosages - 2.5 mg per day initial and 5 mg per day maintenance.
In principle, while using Amlodipine, it is recommended to use contraceptive methods to prevent pregnancy, which may be negatively affected by the drug.
It is unknown whether Amlodipine passes into breast milk. However, other drugs from the group of calcium channel blockers (for example, Nifedipine, Isradipine, Nimodipine, etc.) pass into breast milk. Therefore, if necessary, the use of Amlodipine should be discontinued. breastfeeding and transfer the child to artificial milk formula.
Calcium supplements reduce the severity of the therapeutic effect of Amlodipine.
Simultaneous administration of Amlodipine in a dosage of 10 mg and Simvastatin in an amount of 80 mg increases the degree of absorption of the latter drug by 77%. Therefore, in such cases, the dosage of Simvastatin should be reduced to 20 mg.
A single dose of 100 mg of Sildenafil (Viagra) or alcohol does not affect the therapeutic effects of Amlodipine in people suffering from arterial hypertension.
Antiviral drugs (Ritonavir, Tamiflu, Acyclovir, Ganciclovir, etc.) increase the concentration of Amlodipine in the blood plasma.
At simultaneous administration Amlodipine with lithium salts may cause nausea, vomiting, diarrhea, ataxia (impaired coordination of movements), tremors of the limbs and tinnitus.
1. The cardiovascular system:
Synonyms of Amlodipine include the following medications:
Negative reviews about Amlodipine are few and are due to two main factors - ineffectiveness in this particular case and poor tolerability due to the severe severity of side effects. Most often in negative reviews It is noted that Amlodipine causes drowsiness, lethargy and apathy, which are very poorly tolerated, since they do not allow a person to lead a normal lifestyle.
Amlodipine is a cellular calcium channel blocker. Calcium ions are active participants in a number of bioenergetic processes occurring in cells human body. However, their increased concentration is not a positive circumstance, rather the opposite: there is an excessive intensification of cellular metabolic processes that require excess oxygen. Such cell work “for wear and tear” can trigger a number of unwanted destructive changes. Amlodipine, preventing the penetration of calcium ions into the cell, is a kind of controller that maintains the biochemical balance in the extra- and intracellular space at the proper level.
One of the main advantages of amlodipine is its pronounced antianginal effect: it dilates coronary and peripheral blood vessels, which significantly unloads the heart muscle, reduces its need for oxygen, and reduces vascular resistance, which is especially important for angina and ischemia. Another advantage of amlodipine, widely used by cardiologists in relation to their patients, is its persistent hypotensive effect, due to the same vasodilating effect of the drug. For example, in people with arterial hypertension, even one-time appointment amlodipine provides a noticeable and at the same time smooth reduction in pressure for a period of up to 24 hours.
Amlodipine is taken at any time, regardless of the patient's diet. In order to prevent an attack of angina pectoris and for the treatment of hypertension, the initial dose of amlodipine is 5 mg per day, taken at a time. Depending on the observed effect, the dose can be doubled (but not more). Cardiologists advise establishing a clear schedule for taking amlodipine and then trying to stick to it, taking the drug at the same time. As part of combination pharmacotherapy while taking other cardiac medicines(ACE inhibitors, beta-blockers, etc.) no dose adjustment of amlodipine is required.
Patients with unimpressive dimensions, as well as those suffering from liver diseases, take smaller doses of the drug. But people suffering from renal failure or the elderly take amlodipine on a general basis. The withdrawal syndrome present in certain drugs of the cardiac group is not typical for amlodipine; however, before stopping the course of treatment, a gradual reduction in the dose of the drug is recommended. Patients suffering from diseases such as gout, bronchial asthma or diabetes mellitus can take amlodipine without any restrictions: it does not has a negative effect on blood lipids and does not affect metabolism.
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.
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.
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100 pieces. - polymer bottles (1) - cardboard packs.
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.
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 clinical significance These effects are not completely clear and may be more pronounced in older patients. Potent inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) may lead to increased plasma concentrations of amlodipine in 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.
From the cardiovascular system: peripheral edema, tachycardia, hyperemia skin; when used in high doses- arterial hypotension, arrhythmias, shortness of breath.
From the outside digestive system: nausea, abdominal pain; rarely - gum hyperplasia.
From the central nervous system and peripheral nervous system: headache, fatigue, drowsiness, dizziness; at long-term use- paresthesia.
Allergic reactions: skin rash, itching.
Other: with prolonged use - pain in the limbs.
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's and adolescence up to 18 years of age (efficacy and safety have not been established); increased sensitivity to amlodipine and other dihydropyridine derivatives.
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.
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 heart attack myocardium (and for 1 month after it), SSSU (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 not installed.
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.