Among the means of antiplatelet therapy, which are used for the prevention of acute cardiovascular pathologies, acetylsalicylic acid (ASA) has been the key for a long time. Synthesized in 1887, it has been actively used in medical practice for more than 125 years as an antiplatelet agent and antipyretic. And as an active drug substance, it is part of the drug āAcecardol,ā the indications for the use of which are gradually expanding as we study the pathogenetic mechanisms of vascular diseases.
Systemic characteristics of the drug
The active substance of the drug according to the classification refers to agents that prevent aggregation. In this series, ASA is the most effective chemical composition that can fully ensure the impossibility of aggregation of the entire platelet pool. Evaluating the drug "Acecardol", indications for use, analogues and its dosage form in terms of pharmacodynamics, the following is revealed:
its active substance is ASA, which mediates the antithrombotic effect against arterial atherosclerosis;
the drug is dosed optimally for the prevention of cardiovascular disease;
its dosage form minimizes the gastrotoxic effect of ASA;
the drug is most affordable at a price among competing analogues with identical efficacy.
The effect of preventing ASA thrombosis is explained by the blockade of the formation of prostanoids. Due to the inhibition of COX-1 - platelet cyclooxygenase-1 - the initiating factor in the formation of a thrombus, aggregation of blood plates, is disturbed. The formation of thromboxane A2 is inhibited, triggering the process of platelet attachment to the damaged area of āāthe vascular wall.
Justification and characterization of gastrotoxicity
Targeted indications for the use of Acekardol include the prevention of thrombosis. However, ASA, the active component of the drug, has an undesirable effect associated with non-selectivity to cyclooxygenase. The restoration of gastric epithelial cells is also impaired. Being under the aggressive influence of an acidic gastric environment, they are damaged more, 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 "Acekardol" is used, the indications for use are wider because of its greater safety. It dissolves and is absorbed only in the duodenum 12, representing the enteric ASF cardioform. Her contact with the cells of the stomach is virtually eliminated, thereby inhibiting its side effect of gastrotoxicity. The local damaging effect of "Acecardol" is minimized, because the drug is considered in enteric form as a selective COX-1 inhibitor. Although inhibition of COX-2 also occurs in the intestine, which is not manifested by significant disorders.
An important effect of the Acecardol dosage form is a direct local reduction in gastrotoxicity. Due to the presence of an antacid substance in the form of magnesium hydroxide, the probability of damage to the stomach is reduced even higher. Moreover, at the moment on the pharmacological market of the Russian Federation, āAcecardolā is one of three agents with these properties. Remaining the most affordable among similar ones, it is well suited for continuous use.
Place āAcecardolā in antithrombotic therapy
ASA for the prevention of thrombotic events is used on the basis of many clinical studies. They confirm its effectiveness in reducing the mortality of patients from vascular diseases. In particular:
ASA reduces death by 16% among patients at high cardiovascular risk:
25% reduces the incidence of ischemic stroke;
25% reduces the risk of thromboembolism of the pulmonary artery and its branches;
by 29% reduces the likelihood of manifest venous thrombosis of the pelvis or limbs;
by 33% reduces the incidence of myocardial infarction.
These effects are fully ensured by the drug Acekardol, the indications for use of which are slightly wider than that of gastric soluble ASA. Moreover, today the strength of the antithrombotic action of new antiplatelet drugs is evaluated only in comparison with it. Accordingly, āAcecardolā, as a safer one, should occupy a central place in the preventive treatment of patients according to indications.
Contingent of patients with indications for use
The drug "Acekardol" indications for use, price, effectiveness and risks of use are optimally balanced. This allows you to take ASA in this dosage form for a wide range of patients with occlusal risk factors. Moreover, the elimination of most side effects causes the drug to be taken in the following cases:
(ACS) acute coronary syndromes with elevation, depression or intact ST interval on the cardiogram;
in acute disorders of cerebral (cerebral) blood circulation (stroke);
transient (cerebral) ischemic attacks (TIA);
with the above diseases, in order to prevent repeated cases;
with stable angina pectoris for the prevention of ACS;
with paroxysm or persistent forms of atrial fibrillation;
with venous varicose veins.
Pathogenetic rationale 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 arterial thrombosis at the location of concentric and regional atherosclerotic plaques. In these areas, due to narrowing of the arteries, blood flow is disturbed with the formation of vortex blood flows. Mechanical pressure on the areas of the thinned endothelium leads to its tear. 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 blood clot.
Platelet attachment is the initial stage of thrombus formation, at the end of which a framework for the future thrombus should form. Then its size increases due to the delay of blood cells. The 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 the blood flow in the artery, and areas that previously fed on it experience ischemia. This process underlies ACS and stroke, therefore, the prevention of these phenomena is extremely important in order to reduce the mortality of people with atherosclerosis of the heart and brachiocephalic arteries.
Pharmacodynamics of the antithrombotic action of āAcecardolā
The instructions for use (description of the drug) attached to the drug āAcekardolā do not reflect its pharmacodynamic effect, but characterize it in terms of indications and characteristics of the administration. 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 are as follows:
inhibition of COX-1 and termination of the synthesis of prostanoids;
irreversible blockade of thromboxane A2 production by platelets;
obstruction of platelet attachment to endothelial defects;
inhibition of platelet gluing processes;
the impossibility of the formation of a clot clogging the arterial lumen.
"Acecardol" in acute conditions
Also, the instructions for use (abstract, description) attached to the drug āAcekardolā do not provide information to the patient about the possibility of its use during developing acute circulatory disorders in the heart or brain. In particular, in the development of a clinical syndrome characteristic of myocardial or cerebral infarction, ASA can and should be used.
The tablets of the drug should be chewed (at a dose of 150-300 mg), and not swallowed. If the patient has a drug in a dose of 50 mg, then at the time of an acute condition it is required to chew 3-6 tablets simultaneously, if the dosage is 100 mg, then 2-3 tablets, if 300 mg, then 1 tablet. This is an emergency aid by which the likelihood of severe vascular thrombosis is significantly reduced.
Contraindications to the use of "Acekardol"
The preparation āAcekardolā (tablets) contains instructions for use, reviews of specialists and data from pharmacological studies confirm the balance of risk and benefits of use. However, contraindications due to concomitant diseases must be taken into account when taking the drug and consult a specialist. Contraindications are divided into permanent (absolute) and temporary. Absolute are:
drug intolerance to ASA, the development of bronchospasm;
intracranial hematoma of various locations;
hemorrhagic vasculitis;
it is forbidden to use in adolescents and children due to the risk of Reye's syndrome ;
it is forbidden to take women during lactation, in the I and III trimester of pregnancy.
Also, temporary and relative contraindications somewhat limit the intake:
hepatocellular and renal failure;
the presence of ongoing bleeding, an early postoperative period (temporary contraindication);
arterial hypertension at the time of crisis, uncontrolled hypertension;
an ulcer of the duodenum or stomach during exacerbation (temporary restriction).
Multiple Effects of Acecardol
In addition to standard and well-studied effects caused by inhibition of COX, ASA also has another effect. It has been identified in several statistical studies at cancer and geriatric centers in the United States. In their course, the positive effect of the use of ASA for the prevention of a malignant disease - colorectal cancer of various localizations is proved.
Now the specific mechanism of the protective effect of the drug substance is being 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 you to artificially regulate cell death and reproduction. By the way, this particular cellular process is the main one in the development of tumor neoplasms.
The conclusion on the basis of the proven facts is the following: the medicine āAcecardolā, instructions, use, reviews of specialists about which confirm its balanced effect, can also be used as a prophylactic to prevent tumor processes in the lower intestinal tract. During the 5-12-year intake, the risk of cancer mortality is reduced, which naturally increases the life expectancy. However, ASA cannot be used to treat already developed colorectal adenoma or intestinal carcinoma.
Analogues of the drug and alternative substances
Characterization of the drug "Acecardol": use, instructions, analogues, indications for antithrombotic treatment allow it to be used to treat a wide range of patients. However, in the series of antiplatelet agents, it is not the only means. In Russia, there are about 20 generic ASA, some of which are produced in gastric soluble form. They are inferior to Acecardol in the safety spectrum.
Enteric-soluble forms of ASA (Cardiomagnyl, Polokard), presented on the pharmacological market, are much higher in price. For the drug "Acecardol" the price of a monthly treatment is 25 rubles. Completely identical counterparts with the same safety spectrum cost two-thirds more. Foreign drugs do double or five times the cost of budgetary treatment without visible benefits for a patient taking Acecardol. Instructions for use, treatment, reviews, indications from analogues of this drug are also identical.
Conclusions on the benefits and risks of Acecardol analogues
Remaining the most affordable, the drug āAcecardolā fully complies with the requirements of clinicians. The risk of its use is balanced with the benefits of practical use as an antiplatelet agent. It effectively prevents repeated thrombosis of the vessels of the heart and brain, is used for atrial fibrillation, and is used for varicose veins. And in comparison with regional analogues, the advantage of Acecardol is in affordability.
This fact significantly increases the importance of the drug āAcekardolā: the price of the drug is more than 20 rubles. This is significantly less than the cost of other antiplatelet agents. At the same time, among the ASA preparations produced in the safest enteric form, āAcecardolā is balanced at a price. Naturally, he is given preference in the treatment of the diseases indicated above, and in their prevention. And the number of areas of its application will gradually increase.