Agen

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

However, it should be remembered that severe heart failure requires a special approach, so it is necessary to consider the use of Agen as a secondary therapy in small doses. It is also necessary to carefully select doses, starting with the minimum, for people with liver failure, and in the age category after 70 years. In the note on the use of Agen, it is necessary to add the potentiation of the drug's effect by grapefruit or its juice due to the increase in the bioavailability of Agen.

Indications Agena

Indications for use of Agen are determined by the ability of amlodipine to affect muscle fibers in the walls of blood vessels. Contraction of any muscle fiber occurs due to calcium transport through the membrane, which ensures activation of the motor process. If calcium intake is blocked, then the muscles cannot contract and are in a relaxed state.

Due to this effect, the heart is relieved, since the peripheral vessels do not provide resistance with each cardiac output, while the coronary arteries that feed the heart muscle, relaxing, provide a sufficient supply of oxygen and loop substances.

Based on these facts, indications for the use of Agen include cardiovascular diseases caused by muscle spasm. These include arterial hypertension of 2-3 degrees of severity.

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

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Release form

The release form largely ensures the duration of the period when the drug begins to show its main properties. Thus, Agen is released in tablet form, so you should not expect an immediate therapeutic effect. It is necessary to take into account that the drug reaches its maximum concentration in the blood only after 6-12 hours after oral administration.

The form of the drug release provided for the use of not only fixed doses of amlodipine, but also minimal ones. Thus, each tablet, regardless of the dosage, has a dividing line in the middle. On one side of the tablet is the letter A, and next to it is the dose of the drug. This number indicates the content of the main active substance in this tablet.

The dividing line allows taking a half-sized dose of amlodipine than is contained in the entire tablet. Thus, therapy with Agen can be started with 2.5 mg of amlodipine, dividing the 5 mg tablet into two parts. As a result, the optimal dosage of Agen is correctly selected.

The tablet itself is white and oblong in shape.

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Pharmacodynamics

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

The pharmacodynamics of Agen are due to a direct relaxing effect on the smooth muscle fibers located in the wall of blood vessels. The exact mechanism of action of amlodipine in angina has not yet been clarified, but two possible pathways are identified.

The first method of eliminating pain in the heart area is based on the ability of amlodipine to dilate peripheral vessels, thereby reducing the resistance that the heart must fight with each contraction.

The second pathway is caused by relaxation of the muscles in the walls of the coronary arteries, causing them to expand and provide more oxygen and nutrients to the heart.

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

In angina pectoris, amlodipine prolongs the time until the next pain attack, thereby reducing the need for frequent use of nitrates.

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Pharmacokinetics

Pharmacokinetics of Agen includes gradual absorption of amlodipine in the blood after oral administration of the tablet. Parallel consumption of food together with the tablet does not cause side effects. Absolute bioavailability of amlodipine in unmetabolized form is approximately 60% to 80%. Maximum accumulation of the active substance in the blood occurs 6-12 hours after taking the tablet. The ability of amlodipine to bind to proteins reaches 97.5%.

The half-life of elimination from the bloodstream is about 30-50 hours. Constant plasma concentrations of the drug can only be achieved after regular administration of Agen for a week. Amlodipine is mainly metabolized to inactive metabolites. Amlodipine is 60% excreted by the kidneys, with 10% of the drug excreted unchanged.

The pharmacokinetics of Agen do not change in elderly people, so no dosage adjustment is required. The dose should be increased with caution if the effect is insufficient. In case of liver dysfunction, an increase in the duration of the breakdown and elimination of amlodipine should be taken into account.

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Dosing and administration

The method of administration and dosage are selected individually, taking into account the person’s health condition, 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 ingredient to control arterial hypertension and chest pain. The tablet is taken once a day, but if the therapeutic effect is insufficient, the dosage is increased to 10 mg.

The method of administration and dosage should be taken into account in a comprehensive approach to the treatment of hypertension. Thus, Agen can be combined with the use of thiazide diuretics, centrally acting 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 maintained for a month, after which the result should be assessed and, if necessary, correction should be made.

If the therapeutic effect is insufficient, the dose may be increased to 5 mg, but for children this is the maximum amount of amlodipine. The effect of higher doses has not been studied in this category of patients.

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Use Agena during pregnancy

Pregnant women, like no one else, 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 the development of complications.

The use of Agen during pregnancy has not been studied experimentally, therefore the use of the drug with the active substance amlodipine is recommended only in cases where it is impossible for the pregnant woman to choose another alternative drug to control blood pressure.

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

Since the possibility of amlodipine penetrating into the breast milk of a pregnant woman has not been studied, therefore, when deciding on the use of Agen, it is necessary to take into account the benefits of breastfeeding for the baby and the positive effect of using the drug for the pregnant woman.

Contraindications

Contraindications to the use of Agen include general recommendations for diseases and individual characteristics of the body. Thus, a low threshold of sensitivity 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 highlight a drop in blood pressure to low levels, up to the development of shock of various origins, including cardiac shock.

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

Contraindications also include unstable heart failure due to hemodynamic disturbances after the development of acute myocardial infarction. Amlodipine should not be taken during the first 8-10 days after the infarction.

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Side effects Agena

Side effects of Agen may be observed due to individual characteristics of the body when taking amlodipine, as well as if the recommendations for its use are not followed.

All side effects of Agen are divided by frequency of occurrence. The most common are the nervous system response with drowsiness, dizziness and headache. From the vascular system, there are "hot flashes" and swelling of the shins, and the digestive system can respond with pain in the abdomen and nausea.

Further, less frequently, there is insomnia, changes in the psycho-emotional state, fainting, visual impairment, ringing in the ears, increased heartbeat, hypotension, vomiting, digestive and intestinal disorders. From the musculoskeletal system, pain syndrome in the joints, muscles, lumbosacral spine is possible.

Quite rarely, changes in the blood picture, allergic reactions, conduction and rhythm disturbances of the heart, shortness of breath, cough, hepatitis, pancreatitis, nocturia, frequent urination and weight fluctuations are observed.

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Overdose

Overdose may occur when the daily dosage of amlodipine is exceeded, when inadequate doses of the drug are taken for a long time, or when there is concomitant liver or kidney disease, which results in a decrease in the rate of metabolism and excretion of amlodipine with its subsequent gradual accumulation.

Overdosing on Agen may result in excessive relaxation and dilation of peripheral vessels and possible reflex acceleration of the heart rate. When using the drug in high doses, cases of prolonged decrease in blood pressure have been reported, in some cases with the development of shock, which has led to death.

If symptoms of overdose occur, treatment should be started immediately. This includes cardiovascular support with continuous recording of the vital functions of the heart and respiratory system. The person should be in a supine position with the foot end of the bed raised. Mandatory criteria for assessing the condition are the volume of circulating blood and the amount of urine excreted (diuresis).

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

Calcium gluconate administered intravenously counteracts calcium channel blockade, thereby reducing the effect of amlodipine. The effect of gastric lavage can only be achieved if it is used within the first two hours after taking Agen.

Interactions with other drugs

Interaction of Agen with other drugs such as thiazide diuretics, centrally acting drugs, ACE inhibitors, alpha- and beta-blockers, long-acting nitrates, sublingual nitroglycerin, non-steroidal anti-inflammatory drugs, oral hypoglycemic drugs and antibiotics is possible.

Concomitant use of amlodipine with protease inhibitors, antifungals, macrolides, diltiazem or verapomil may increase the exposure of Agen. As a result, the clinical effect of the drug may exceed expectations and require dose adjustment.

Drugs such as rifampicin and St. John's wort can reduce the accumulation of amlodipine in the blood, as a result of which the therapeutic effect will not be achieved.

Infusion use of detrolen may provoke the development of hyperkalemia with subsequent ventricular fibrillation and vascular collapse.

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

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Storage conditions

Storage conditions for Agen include placing the drug in a place with a certain temperature and humidity conditions and without exposure to direct sunlight.

Thus, the storage temperature for amlodipine should not exceed 25 degrees. If the recommended requirements are not met, amlodipine may lose its medicinal properties prematurely.

In addition, the drug may disrupt its structure and acquire completely 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 package contains three blisters.

Storage conditions for Agen also imply keeping each tablet in its own cell without damaging its integrity. Once the tablet preparation has been removed from the cell, it should be taken as soon as possible. Storing tablets in an unprotected form is not allowed. The required storage conditions for each preparation must be observed throughout the entire period of the specified shelf life.

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Shelf life

The expiration date is the period from the date of manufacture of the drug to the date of its last use. The manufacturer indicates this information on the outer packaging for quick access to it. During this period, the pharmaceutical company that manufactured the drug guarantees the presence of a therapeutic effect after taking an amlodipine tablet.

These therapeutic effects have been studied and confirmed, so they are indicated in the instructions attached to the drug. The expiration date indicates the safety of the drug, provided that certain requirements for storing amlodipine are met, the outer packaging and each cell with a tablet are intact.

The shelf life of the antihypertensive drug Agen with the main active ingredient amlodipine is 3 years from the date of manufacture. After this period, its use is strictly prohibited, since the effects and side effects are unknown, which can develop after taking an amlodipine tablet.

Agen has proven its effectiveness both in monotherapy and in complex treatment of pathological conditions of the cardiovascular system. In addition, due to the tablet form and the presence of a dividing line, the drug is dosed quite well and the required dose of amlodipine is selected.