Agen

The drug Agen represents a group of calcium antagonists with the main active substance - amlodipine. The international name sounds like Amlodipine. Classification, which includes the drug, includes a common group, called agents that affect the cardiovascular system, as well as subgroups. Agen refers to calcium antagonists that act selectively. Their greatest activity is manifested in relation to the vessels. By origin, the preparation is a dihydropyridine derivative. Agen is widely used in cardiology, since its point of application is considered to be blood vessels. Thus, it is used in the form of monotherapy with increased arterial pressure, as well as in the combined treatment of cardiovascular pathologies.

However, it should be remembered that heart failure of severe form requires a special approach, so it is necessary to consider the use of Agen as a secondary therapy in small doses. Also, you need to carefully select the dose, starting with the minimum, for people with hepatic insufficiency, and in the age category after 70 years. In a note on the use of Agen, potentiation of the action of the drug with grapefruit or its juice should be added due to an increase in the bioavailability of Agen. 

Indications of the agen

Indications for the use of Agen are due to the ability of amlodipine to act on muscle fibers in the walls of blood vessels. Reduction of any muscle fiber is due to transport through the membrane of calcium, due to which the activation of the motor process is provided. If there is a blockage of calcium intake, then the muscles can not contract and are in a relaxed state.

Due to this effect, heart discharge is provided, since peripheral vessels do not resist at each cardiac output, while coronary arteries feeding the cardiac muscle while relaxing provide sufficient supply of oxygen and loop substances.

Based on these facts, indications for the use of Agen include diseases of the cardiovascular system, the cause of which is muscle spasm. These include hypertension 2-3 degrees of severity.

Agen is also used in ischemic heart disease with various manifestations of it, for example, stable angina pectoris or vasospastic angina. In addition, as an auxiliary drug is used for chronic heart failure.

[1], [2]

Release form

The form of release in many respects provides duration of the period when the preparation starts to show the basic properties. So, Agen is released in tablet form, so expect instant therapeutic effect is not worth it. It should be noted that the drug reaches its maximum concentration in the blood only after 6-12 hours after oral administration.

The form of the preparation provided for the use of not only fixed doses of amlodipine, but also minimal ones. So, each tablet, regardless of dosage, has a separating line in the middle. On one side of the pill is the letter A, and near it the dose of the drug. This figure indicates the content of the main active substance in this tablet.

Due to the dividing line, it is possible to take twice as little dose of amlodipine as is found in the whole tablet. Thus, therapy with Agen can be started with 2.5 mg of amlodipine, by dividing the tablet with a dosage of 5 mg into two parts. As a result, the correct selection of the optimal dosage of Agen is made.

The tablet itself has a white tinge and an elongated shape.

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Pharmacodynamics

Amlodipine is able to prevent the entry of calcium through slow channels and inhibits its accumulation in the fibers of the smooth muscles of the heart and vessels.

Pharmacodynamics Agen is caused by a direct relaxing effect on the smooth-muscle fibers located in the wall of blood vessels. Until now, the exact mechanism of amlodipine exposure to angina has not been clarified, but two possible ways are identified.

The first way to eliminate the pain syndrome in the heart area is based on the ability of amlodipine to expand the peripheral vessels, thereby reducing the resistance that the heart must fight with every contraction.

The second way is caused by the relaxation of the muscles in the walls of the coronary arteries, as a result of which they expand and provide a greater supply of oxygen and nutrients to the heart.

Pharmacodynamics Agen with arterial hypertension provides the necessary result - a decrease in blood pressure, throughout the day. Due to the gradual release of amlodipine, after the administration of Agen there is no sharp hypotension.

With angina, amlodipine prolongs the time until the next pain attack, which reduces the need for frequent intake of nitrates.

[4], [5], [6], [7], [8],

Pharmacokinetics

Pharmacokinetics Agen includes the gradual absorption of amlodipine in the blood after taking the tablet inside. The concurrent use of food in conjunction with the pill does not cause side effects. The absolute bioavailability of amlodipine in a non-metabolized form is approximately 60% to 80%. The maximum accumulation of active substance in the blood occurs 6-12 hours after taking the pill. The ability to bind amlodipine with proteins reaches 97.5%.

Half-life from the bloodstream is about 30-50 hours. Constant concentration of the drug in the plasma can be achieved only after a regular intake of Agen throughout the week. The transformation of amlodipine mainly occurs with the formation of inactive metabolites. The introduction of amlodipine is provided by 60% kidneys, with 10% of the drug being excreted unchanged.

Pharmacokinetics Agen does not change in elderly people, so dosage adjustment is not required. With care, it is necessary to increase the dose with insufficient effect. If the liver is disturbed, the increase in the duration of decay and elimination of amlodipine should be taken into account.  

[9], [10], [11], [12],

Dosing and administration

The method of application and dose are selected individually, taking into account the state of human health, the severity of the disease and the presence of concomitant pathology and contraindications.

In most cases, the starting dosage for an adult is 5 mg of the main active substance for the control of hypertension and chest pain. The tablet is taken once a day, but with insufficient therapeutic effect, the dosage is increased to 10 mg.

The method of administration and dose should be taken into account in an integrated approach to the treatment of hypertension. Thus, the Agen can be combined with the use of thiazide diuretics, central-action drugs and angiotensin-converting enzyme inhibitors.

In the treatment of angina, amlodipine is used in parallel with other antianginal drugs, such as nitrates or beta-blockers.

Agen is allowed to be used in children over 6 years of age if there are indications. The initial dose should not exceed 2.5 mg per day. This dosage should be kept for a month, after which you need to evaluate the result and, if necessary, carry out a correction.

With insufficient therapeutic effect, it is allowed to increase the dose to 5 mg, but for children this is the maximum amount of amlodipine. At high dosages, the effect was not investigated in this category of patients.

[18], [19], [20],

Use of the agen during pregnancy

Pregnant women, like no other, are subject to periodic increases in pressure in the presence of such a serious pathological condition as preeclampsia and eclampsia. It is the control of blood pressure indicators that helps prevent complications.

The use of Agen during pregnancy has not been studied with the help of experiments, so the use of the drug with the active substance amlodipine is recommended only in those cases when it is impossible for a pregnant woman to choose another alternative drug that controls blood pressure.

In addition, the use of Agen during pregnancy is permitted when the risk caused by the disease itself exceeds the occurrence of adverse reactions after taking amlodipine in the fetus and the woman.

Due to the fact that the possibility of amlodipine penetration into the breast milk of a pregnant woman has not been investigated, therefore, the use of breast-feeding for a baby and the positive effect of using the drug for a pregnant woman should be taken into consideration in order to decide on the use of Agen.

Contraindications

Contraindications to the use of Agen include general recommendations for diseases and individual characteristics of the body. Thus, a low sensitivity threshold to amlodipine, dihydropyridine or any other additional component that is part of the drug is one of the contraindications.

Among pathological conditions and diseases, it is necessary to single out the drop in arterial pressure to low figures, up to the development of shock of various origins, including cardiac shock.

Contraindications to the use of Agen are characterized by the presence of coronary heart disease with an unstable form of angina. In addition, attention should be paid to the condition of obstruction of the excretory blood vessel from the left heart, namely from the left ventricle. A similar condition is observed with severe aortic stenosis.

Also, one of the contraindications is the unstable form of heart failure due to hemodynamic disorders after the development of acute myocardial infarction. Amlodipine should not be taken during the first 8-10 days after a heart attack.

[13], [14], [15], [16],

Side effects of the agen

Side effects of Agen can be observed with individual characteristics of the body to receive amlodipine, as well as non-compliance with recommendations for its use.

All the side effects of Agen are divided according to the frequency of occurrence. Of the most frequent it is worth highlighting the response of the nervous system with the appearance of drowsiness, dizziness and headache. From the side of the vascular system, "hot flushes" and edema of the shins are observed, and the digestive system can respond with pain syndrome in the abdominal region and with nausea.

Then, insomnia, changes in the psycho-emotional state, fainting, visual impairment, "ringing" in the ears, increased heart rate, hypotension, vomiting, digestive disorders and bowel movements occur at a lower frequency. On the part of the musculoskeletal system, pain syndrome is possible in the joints, muscles, lumbar-cervical spine.

Changes in the blood picture, allergic reactions, conduction and rhythm disturbance of the heart, shortness of breath, cough, hepatitis, pancreatitis, nocturia, frequent urination and weight fluctuations are rarely noted.

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Overdose

Overdosage can occur when the daily dosage of amlodipine is used, the long-term administration of inadequate doses of the drug, as well as in the presence of concomitant liver or kidney pathology, resulting in a decrease in the metabolic rate and removal of amlodipine with subsequent gradual accumulation.

Overdose of Agen can lead to excessive relaxation and expansion of peripheral vessels and a possible reflex increase in heart rate. When using the drug in large doses, cases of a prolonged decrease in blood pressure were recorded, in some cases, with the development of shock, which led to a lethal outcome.

When symptoms of an overdose appear, you should immediately begin treatment. It includes cardiovascular support with a permanent recording of the vital functions of the heart and respiratory system. The position of the person should be lying with the raised foot of the bed. An obligatory criterion for assessing the condition is the volume of circulating blood and the amount of excreted urine (diuresis).

The use of vasoconstrictive drugs also has a positive effect, which is manifested by the restoration of vascular tone and blood pressure. Their use is recommended only in the absence of contraindications.

Calcium gluconate, injected intravenously, is counteracting blockade of calcium channels, thereby reducing the effect of amlodipine. The effect of gastric lavage can be achieved only when it is used in the first two hours after the administration of Agen.

Interactions with other drugs

It is possible to interact with other drugs such as thiazide diuretics, central mechanism of action, ACE inhibitors, alpha and beta blockers, prolonged-action nitrates, nitroglycerin with sublingual administration, nonsteroidal anti-inflammatory drugs, hypoglycemic oral drugs and antibiotics.

The simultaneous use of amlodipine with protease inhibitors, antifungal agents, macrolides, diltiazem or verapomil, then an increase in the exposure of Agen is possible. As a result, the clinical effect of the drug may exceed expectations and require dose adjustments.

Such drugs as rifampicin and St. John's wort can reduce the accumulation of amlodipine in the blood, so that the therapeutic effect will not be achieved.

Infusion use of detroven can provoke the development of hyperkalemia followed by ventricular fibrillation and vascular collapse.

Interaction of Agen with other drugs of hypotensive effect leads to potentiation of each other's actions. As for drugs that reduce cholesterol, digoxin, cyclosporine, alcohol and anticoagulants, then amlodipine has no effect on them.

[21], [22], [23], [24], [25], [26], [27], [28]

Storage conditions

Agen storage conditions include location of the preparation in a place with a certain temperature regime, humidity and without direct sunlight.

Thus, the temperature for storage of amlodipine should not exceed 25 degrees. If the recommended requirements are not met, premature loss of amlodipine may occur.

 In addition, the drug may break its structure and acquire absolutely unknown effects that may appear after taking the pill.

Agen is packaged in 10 tablets of 5 mg or 10 mg in one blister. One cardboard box contains three blisters.

Agen storage conditions also mean the content of each tablet in its cell without compromising its integrity. Once the tablet preparation has been extracted from the cell, it must be accepted soon. Do not store tablets in an unprotected form. The required storage conditions for each drug must be observed throughout the period of the indicated shelf life. 

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Shelf life

Shelf life is the period from the date of manufacture of the drug to the date of its last reception. The manufacturer specifies this information on the outer packaging for easy access to it. During this period, the pharmaceutical company that produced the medicinal product guarantees the therapeutic effect after taking amlodipine tablets.

These therapeutic effects have been investigated and confirmed, therefore they are indicated in the instructions accompanying the drug. Shelf life indicates the safety of the drug, subject to certain storage requirements for amlodipine, the integrity of the outer packaging and each cell with the tablet.

The juice of the antihypertensive drug Agen with the main active ingredient amlodipine is 3 years from the date of manufacture. After the expiration of this period, its use is strictly forbidden, since the effects and side effects are not known, which can develop after taking amlodipine tablets.

Agen has proven its effectiveness both in monotherapy and in the complex treatment of pathological conditions of the cardiovascular system. In addition, due to the shape of the tablet and the presence of the dividing line, the preparation is dosed well enough and the necessary dose of amlodipine is selected.