"Acecardol": indications for use, instructions, reviews, analogues

Among the means of antiplatelet therapy, which are used to prevent acute cardiovascular pathologies, acetylsalicylic acid (ASA) has been a key place for a long time. Synthesized in 1887, it is more than 125 years actively used in medical practice as an antiaggregant and antipyretic. And as an active medicinal substance, it is part of the drug "Acecardol", the indications for the use of which gradually expand as the pathogenetic mechanisms of vascular diseases are studied.

System characteristic of the medicinal product

The active substance of the drug according to the classification refers to the means that prevent aggregation. In this series, ASA is the most effective chemical compound, capable of completely ensuring the impossibility of aggregation of the entire pool of platelets. Evaluating the drug "Acecaradol", indications for use, analogs and its dosage form from the point of view of pharmacodynamics, the following is revealed:

• Its active substance - ASA, mediating the antithrombotic effect against arteries atherosclerosis;

• The drug is dosed optimally for the prevention of cardiovascular diseases;

• Its dosage form minimizes the gastro-toxic effect of ASA;

• The drug is most affordable at competing peers with identical efficacy.

The effect of preventing thrombosis of ASA is due to the blockade in the formation of prostanoids. Due to the inhibition of COX-1 - cyclooxygenase-1 platelets - the initiating factor of thrombus formation - aggregation of blood platelets is disturbed. There is a depression of the formation of thromboxane A2, which starts the process of attaching the platelet to the damaged site of the vascular wall.

Justification and characterization of gastotoxicity

Target indications for the use of "Acecardol" include prevention of thrombosis. However, in ASA, the active component of the drug, there is an undesirable effect associated with nonselectivity to cyclooxygenase. Also, the restoration of epithelial cells of the gastrointestinal tract is disturbed. Being under the aggressive influence of acidic gastric environment, they are damaged more strongly, which causes the development of chronic gastric inflammation. Occasionally (about 3.5% of all cases) this provokes bleeding in the digestive tract.

For the dosage form in which "Acecardardol" is used, the indications for use are wider because of its greater safety. It dissolves and is absorbed only in the duodenum, representing the enteric-soluble cardiac form of ASA. Her contact with the cells of the stomach is virtually excluded, thereby inhibiting its side effect of gastrotoxicity. The local damaging effect of "Acecardol" is minimized, because the drug is already considered as an enteric-soluble form already as a selective inhibitor of COX-1. Although inhibition of COX-2 also occurs in the intestine, which does not show significant disturbances.

An important effect of the dosage form of "Acecardol" is the immediate local decrease in gastrotoxicity. Due to the presence of an antacid substance in the form of magnesium hydroxide, the probability of damage to the stomach decreases even higher. And at the moment on the pharmacological market of the Russian Federation, "Acecardol" is one of three products with these properties. Remaining the most affordable among similar, it is successfully suited for permanent use.

Place "Acecardola" in antithrombotic therapy

ASA for the prevention of thrombotic events is used on the basis of a variety of clinical studies. They confirm its effectiveness in reducing the mortality of patients from vascular diseases. In particular:

• ASA reduces mortality by 16% among patients in the group of high cardiovascular risk by 16%

• 25% reduced the incidence of ischemic stroke;

• By 25% reduces the risk of thromboembolism of the pulmonary artery and its branches;

• By 29% reduces the likelihood of developing a manifest venous thrombosis of the pelvis or extremities;

• By 33% reduces the incidence of myocardial infarction.

These effects fully and provides the drug "Acecaradol", the indications for the use of which is slightly wider than that of gastric dissolving ASA. And today the strength of the antithrombotic effect of new antiplatelet agents is estimated only in comparison with it. Accordingly, "Acecaradol", as the safer, should take a central place in the prophylactic therapy of patients according to the indications.

A contingent of patients with indications for use

The drug "Acecaradol" indications for use, price, effectiveness and risks of use are optimally balanced. This makes it possible to take ASA in this dosage form by a wide range of patients who have occlusive risk factors. And the elimination of most side effects causes the drug in the following cases:

• (ACS) acute coronary syndromes with elevation, depression, or an intact ST interval on a cardiogram;

• With acute violations of cerebral (cerebral) circulation (ONMC);

• Transient (cerebral) ischemic attacks (TIA);

• When these diseases are transferred in order to prevent recurrent cases;

• With stable angina pectoris for prevention of ACS;

• With paroxysm or permanent forms of atrial fibrillation;

• With venous varicose disease.

Pathogenetic justification for the use of "Acecardol"

These indications for the use of "Acecardol" are due to the clinical effect of the drug. It is effectively used as a means of preventing thrombosis of the arteries at the location of concentric and marginal atherosclerotic plaques. At these sites, due to the narrowing of the arteries, blood flow is disturbed, with the formation of vortex blood flows. The mechanical pressure on the areas of the thinned endothelium leads to its tearing. The blood coagulation system recognizes this site as a violation of vascular integrity, which requires its mechanical closure by platelets with the formation of a thrombus.

Attachment of platelets is the stage of the initial thrombus formation, after which the skeleton for the future thrombus should form. Then, its size is increased by delaying the blood cells. Complete completion of hemostasis leads to a strong (more than 75% of the area) narrowing of the lumen of the vessel. Often this even blocks blood flow in the artery, and the areas that previously fed from it experience ischemia. This process underlies the ACS and ONMI, therefore the prevention of these phenomena is extremely important in order to reduce the mortality of people with atherosclerosis of the cardiac and brachiocephalic arteries.

Farmakodinamika antitromboticheskogo action "Acecardola"

Attached to the preparation "Acecaradol" instructions for use (description of the drug) does not reflect its pharmacodynamic effect, but characterizes it in terms of indications and reception characteristics. However, it does not describe the specific effect of ASA, thereby depriving the patient of important information about the mechanism of action. Its sequential algorithms look like this:

• Oppression of COX-1 and discontinuation of the synthesis of prostanoids;

• Irreversible blockade of thromboxane A2 production by platelets;

• An obstacle of platelet attachment to endothelial defects;

• Oppression of the processes of gluing together thrombocytes;

• The impossibility of forming a clotting arterial lumen of the thrombus.

"Accekarol" in acute conditions

Also, the instructions for use (summary, description) attached to the preparation "Acecardol" do not give information to the patient about the possibility of its use during developing acute circulatory disturbances in the heart or brain. In particular, with the development of a clinical syndrome characteristic of a myocardial or cerebral infarction, ASA can and should be applied.

Tablets of the drug must be chewed (in a dose of 150-300 mg), and not swallowed. If the patient has a drug at a dose of 50 mg, then at the time of acute condition it is required to simultaneously chew 3-6 tablets, if the dosage is 100 mg, then 2-3 tablets, if 300 mg, then 1 tablet. This is an emergency aid, which significantly reduces the likelihood of severe vascular thrombosis.

Contraindications to the use of "Acecardol"

The drug "Acecardol" (tablets) instruction on the application, expert reviews and pharmacological data confirm the balance of risk and benefits of use. However, contraindications due to concomitant diseases should be taken into account when taking the drug and consult with a specialist. Contraindications are divided into permanent (absolute) and temporary. Absolute are:

• Drug intolerance to ASA, development of bronchospasm;

• Intracranial hematoma of various localizations;

• Hemorrhagic vasculitis ;

• It is forbidden to use in adolescents and children due to the risk of development of Ray's syndrome ;

• It is forbidden to take women during lactation, in the first and third trimester of pregnancy.

Also, the temporary and relative contraindications are somewhat limited:

• Hepatic and renal failure;

• Presence of continuing bleeding, early postoperative period (temporary contraindication);

• Arterial hypertension at the time of crisis, uncontrolled hypertension;

• Ulcer of duodenum or stomach during exacerbation (temporary restriction).

Multiple Effects of Acecardol

In addition to the standard and well-studied effects caused by inhibition of COX, ACK also has another effect. It was revealed in several statistical studies in the US cancer and geriatric centers. In their course, the positive effect of the use of ASA for the prevention of malignant disease - colorectal cancer of various localizations - is proved.

Now a specific mechanism of the protective action of the drug substance is proved. The opinions of most researchers and clinicians agree on the predominance of the inhibitory effect of COX-2 in the lower intestine. Inhibiting the synthesis of prostaglandin E2, ASA allows artificially regulate the death and reproduction of cells. By the way, it is this cellular process that is the main one in the development of tumor neoplasms.

The conclusion on the basis of the proved facts is the following: the medicine "Acecaradol", the instruction, application, the experts feedback about which confirm its balanced effect, can be used and as a preventive agent for prevention of tumoral processes in the lower parts of the intestinal tract. During 5-12 years of administration, the risk of cancer mortality decreases, which naturally increases life expectancy. Nevertheless, ASA can not be used for treatment with already developed colorectal adenoma or intestinal carcinoma.

Analogs and alternative substances

Characteristics of the preparation "Acecardol": application, instruction, analogs, indications for antithrombotic treatment allow using it for treatment of a wide range of patients. However, in the series of antiplatelet agents, it is not the only remedy. In Russia, there are about 20 ASK generics, some of which are produced in a gastrointestinal form. They are on the security spectrum inferior to "Acecaradol".

The intestinal forms of ASA ("Cardiomagnum", "Polokard"), represented on the pharmacological market, are much higher in price. For the drug "Acecaradol" the price of a monthly treatment is 25 rubles. Completely identical analogues with the same security spectrum cost two-thirds more. Foreign drugs and do double or five times higher than the cost of budgetary treatment without visible benefits for the patient who takes "Acecaradol". Instructions for use, treatment, reviews, indications of analogues of this drug are also identical.

Conclusions about the benefits and risks of the analogues of "Acecardola"

Remaining the most affordable, the drug "Acecaradol" fully meets the requirements of clinicians. The risk of its use is balanced with the use of practical application as an antiplatelet agent. It effectively prevents repeated thrombosis of the vessels of the heart and brain, is used in atrial fibrillation, is used in varicose veins. And in comparison with regional analogues, the advantage of "Acecardola" is in price accessibility.

This fact significantly increases the importance of the drug "Acecaradol": the price of the drug is 20-odd rubles. This is significantly less than the cost of other antiplatelet agents. In this case among the drugs ASA, produced in the safest intestine-soluble form, at a price is precisely balanced "Acecaradol". It is natural that he is given preference in the treatment of the diseases mentioned above, and in their prevention. And the number of spheres of its application will gradually increase.