Cardiomagnyl forte film-coated tablets of 150 mg bottle of 30 pcs

Pharmacodynamics. acetylsalicylic acid is an analgesic, anti-inflammatory, antipyretic and antiplatelet agent. antiaggregation properties increase bleeding time.

The main pharmacological effect is inhibition of the formation of prostaglandins and thromboxanes. The analgesic effect is additional, which is due to the inhibition of the COX enzyme. The anti-inflammatory property is associated with a decrease in blood flow caused by inhibition of PGE _{2 synthesis.}

Acetylsalicylic acid irreversibly inhibits the synthesis of prostaglandins G / H, its effect on platelets is longer than being in the body. The effect of acetylsalicylic acid on the biosynthesis of thromboxane in platelets and on bleeding time continues for a long time after stopping treatment. The action stops only after the appearance of new platelets in the blood plasma.

Salicylic acid (an active metabolite of acetylsalicylic acid) has an anti-inflammatory effect, and also affects respiratory processes, the state of the acid-base balance, and the mucous membrane of the stomach. Salicylates stimulate respiration, mainly by directly affecting the bone marrow. Salicylates have an indirect effect on the gastric mucosa by inhibiting its vasodilatory and cytoprotective prostaglandins and increase the risk of ulcers.

Pharmacokinetics. Absorption. After ingestion, acetylsalicylic acid is rapidly absorbed from the gastrointestinal tract. After oral administration, absorption of the non-ionized form of acetylsalicylic acid occurs in the stomach and intestines. The rate of absorption decreases with food and in patients with migraine attacks, increases – in patients with achlorhydria or in patients taking polysorbates or antacids. C _max in blood serum is reached after 1-2 hours.

Distribution. Binding of acetylsalicylic acid to blood plasma proteins is 80-90%. The volume of distribution for adults is 170 ml/kg of body weight. When the concentration in the blood plasma is increased, the active centers of proteins are saturated, which leads to an increase in the volume of distribution. Salicylates extensively bind to blood plasma proteins and quickly spread throughout the body. Salicylates penetrate into breast milk and can penetrate the placental barrier.

Metabolism. Acetylsalicylic acid is hydrolyzed to the active metabolite – salicylic acid in the stomach wall. After absorption, acetylsalicylic acid is quickly converted into salicylic acid, but within the first 20 minutes after ingestion, it is dominant in the blood plasma.

Breeding. Salicylic acid undergoes metabolism mainly in the liver. Thus, the equilibrium concentration of salicylate in blood plasma increases disproportionately to the dose taken. At a dose of 325 mg, the elimination of acetylsalicylic acid occurs with the participation of first-order reaction kinetics. T _½ is 2-3 hours. With a high dose of acetylsalicylic acid, T _½ increases to 15-30 hours. Salicylic acid is also excreted unchanged in the urine. The excreted volume depends on the dose level and urine pH. About 30% of salicylic acid is excreted in the urine if the urine reaction is alkaline, only 2% – with an acidic reaction. Excretion by the kidneys occurs due to the processes of filtration, active secretion of renal tubules and passive tubular reabsorption.

Cardiomagnet

• Acute and chronic ischemic heart disease;
• prevention of repeated thrombus formation;
• primary prevention of thrombosis, cardiovascular diseases, such as acute coronary syndrome in patients over 50 years of age in the presence of risk factors for the development of cardiovascular system diseases: arterial hypertension, hypercholesterolemia, diabetes, obesity (body mass index 30), hereditary anamnesis (myocardial infarction in patients under the age of 55 in at least one parent or brother or sister);

Cardiomagnyl Forte

Acute and chronic ischemic heart disease.

Cardiomagnet

Acute and chronic ischemic heart disease: the recommended starting dose is 150 mg/day. The maintenance dose is 75 mg/day.

Acute myocardial infarction. Unstable angina: the recommended dose is 150-450 mg, used as soon as possible after the onset of symptoms.

Prevention of repeated thrombus formation: the recommended initial dose is 150 mg/day. The maintenance dose is 75 mg/day.

Primary prevention of thrombosis, cardiovascular diseases, such as acute coronary syndrome in patients with factors for the development of cardiovascular diseases. The recommended prophylactic dose is 75 mg/day.

Cardiomagnyl Forte. The recommended dose for adults is 150 mg (1 tablet) per day.

Tablets are swallowed whole with water. To ensure rapid absorption, the tablet can be chewed or dissolved in water.

Violation of liver function. The drug is not used in patients with severe liver function disorders. Dose adjustment may be necessary in patients with impaired liver function.

Impaired kidney function. The drug is not used to treat patients with severe renal insufficiency (glomerular filtration rate 0.2 ml/s (10 ml/min)). Dose adjustment may be necessary in patients with impaired renal function.

Hypersensitivity to acetylsalicylic acid, other salicylates or any component of the drug; asthma caused by the use of salicylates or substances with a similar effect, especially non-steroidal anti-inflammatory drugs in the anamnesis; acute ulcer; hemorrhagic diathesis; severe renal failure; severe liver failure; severe heart failure; combination with methotrexate at a dose of ≥15 mg/week (see interactions).

The given information on adverse reactions is based on spontaneous post-marketing reports of adverse reactions with the use of all dosage forms and dosages of acetylsalicylic acid (including oral use during a short and long course of treatment). despite this, the classification of adverse reactions by CIOMS iii frequency categories was not performed.

Gastrointestinal disorders: frequent manifestations and symptoms of dyspepsia, epigastric pain and abdominal pain; in some cases – inflammation of the gastrointestinal tract, erosive-ulcerative lesions of the gastrointestinal tract, which can in some cases lead to gastrointestinal hemorrhage and perforation with corresponding laboratory indicators and clinical manifestations.

As a result of its antiplatelet effect on platelets, acetylsalicylic acid may be associated with the risk of bleeding, prolongation of bleeding time. Bleedings such as PERIOPERATIVE hemorrhages, hematomas, bleeding from the organs of the genitourinary system, nosebleeds, bleeding from the gums were noted; rarely or very rarely – serious bleeding, such as hemorrhages in the gastrointestinal tract, cerebral hemorrhages (especially in patients with uncontrolled arterial hypertension and / or with the simultaneous use of antihemostatic agents), which in some cases could be potentially life-threatening. Hemorrhages can lead to acute and chronic posthemorrhagic anemia / iron-deficiency anemia (due to the so-called hidden microbleeding) with corresponding laboratory manifestations and clinical symptoms, such as asthenia, pallor of the skin, hypoperfusion.

In patients with severe forms of glucose-6-phosphate dehydrogenase deficiency, hemolysis and hemolytic anemia are noted.

Impaired kidney function and development of acute renal failure have been reported. Hypersensitivity reactions with corresponding laboratory and clinical manifestations, including asthmatic state, mild or moderate skin reactions, as well as from the respiratory tract, gastrointestinal tract and cardiovascular system, including symptoms such as rash, urticaria, edema , itching, rhinitis, nasal congestion, cardiorespiratory failure and very rarely – severe reactions, including anaphylactic shock.

Transient liver failure with increased levels of transaminases and serum LF has been reported very rarely.

Dizziness and ringing in the ears are noted, which may indicate an overdose.

The drug Cardiomagnil / Cardiomagnil forte is used with caution in the following situations:

• hypersensitivity to analgesic, anti-inflammatory, antirheumatic agents, as well as in the presence of allergies to other substances;
• ulcers of the gastrointestinal tract, including chronic and recurrent ulcer disease or gastrointestinal bleeding in the anamnesis;
• simultaneous use of anticoagulants;
• in patients with impaired renal function or patients with impaired blood circulation (for example, renal vascular pathology, congestive cardiovascular failure, hypovolemia, major operations, sepsis or severe bleeding), since acetylsalicylic acid may also increase the risk of impaired renal function and acute renal failure;
• in patients with severe deficiency of glucose-6-phosphate dehydrogenase, acetylsalicylic acid can cause hemolysis or hemolytic anemia. Especially in the presence of factors that can increase the risk of hemolysis, for example, high doses of the drug, fever or an acute infectious process;
• impaired liver function.

Ibuprofen can reduce the inhibitory effect of acetylsalicylic acid on platelet aggregation. In the case of using the drug Cardiomagnil / Cardiomagnil Forte, the patient must consult a doctor before starting to take ibuprofen as a pain reliever. Acetylsalicylic acid can cause the development of bronchospasm or asthma attacks or other hypersensitivity reactions. Risk factors include history of asthma, hay fever, nasal polyposis or chronic respiratory disease, history of allergic reactions (eg, skin reactions, pruritus, urticaria) to other substances.

Due to the inhibitory effect of acetylsalicylic acid on platelet aggregation, which persists for several days after administration, the use of preparations containing acetylsalicylic acid may increase the likelihood / intensify bleeding during surgical operations (including minor surgical interventions, such as tooth extraction).

When using acetylsalicylic acid in low doses, the excretion of uric acid may decrease. This can lead to a gout attack in predisposed patients. Medicines containing acetylsalicylic acid should not be used in children and adolescents with SARS, which is accompanied or not accompanied by an increase in body temperature, without consulting a doctor. With some viral diseases, especially influenza A, influenza B, and chicken pox, there is a risk of developing Reye’s syndrome, which is a very rare but life-threatening condition that requires immediate medical attention. The risk may be increased if acetylsalicylic acid is used as a concomitant medication, but a causal relationship in this case has not been proven. If these conditions are accompanied by constant vomiting, this may be a manifestation of Reye’s syndrome.

Use during pregnancy and breastfeeding. Suppression of the synthesis of prostaglandins can negatively affect pregnancy and / or embryonic / intrauterine development. Available data from epidemiological studies indicate a risk of miscarriage and fetal malformations after the use of prostaglandin synthesis inhibitors in early pregnancy. The risk increases depending on the dose and duration of therapy. According to the available data, the connection between taking acetylsalicylic acid and an increased risk of miscarriage has not been confirmed.

The available epidemiological data on the occurrence of malformations are not consistent, but an increased risk of gastroschisis cannot be excluded with the use of acetylsalicylic acid. The results of a prospective study of exposure in early pregnancy (1-4 months) involving approximately 14,800 woman-child pairs do not indicate any association with an increased risk of malformations. Animal studies indicate reproductive toxicity.

In the I and II trimesters of pregnancy, preparations containing acetylsalicylic acid should not be prescribed without a clear clinical need. In women who are likely to be pregnant, or in the I and II trimesters of pregnancy, the dose of drugs containing acetylsalicylic acid should be as low as possible, and the duration of treatment should be as short as possible.

In the III trimester of pregnancy, all prostaglandin synthesis inhibitors can affect the fetus as follows:

• cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);
• impaired kidney function with possible further development of renal failure with oligohydramnios.

Inhibitors of prostaglandin synthesis can affect a woman and a child at the end of pregnancy in the following way:

• the possibility of prolongation of bleeding time, antiplatelet effect, which can occur even after using the drug in very low doses;
• inhibition of uterine contractions, which can lead to a delay or increase in the duration of childbirth.

In view of this, acetylsalicylic acid is contraindicated in the III trimester of pregnancy.

Salicylates and their metabolites pass into breast milk in small amounts. Since no harmful effects of the drug on the baby have been found after taking it by women who are breastfeeding, it is usually not necessary to interrupt breastfeeding. However, in cases of regular use or when using the drug in high doses, breastfeeding should be stopped in the early stages.

Children. According to the evidence (see Method of use), the drug Cardiomagnil / Cardiomagnil Forte is not used in children.

The use of acetylsalicylic acid in children under the age of 15 can cause severe side effects (including Reye’s syndrome, one of the symptoms of which is constant vomiting).

The ability to influence the speed of reaction when driving vehicles or other mechanisms. Does not affect.

Contraindications for simultaneous use

Methotrexate. The use of acetylsalicylic acid and methotrexate in a dose of ≥15 mg/week increases the hematological toxicity of methotrexate (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from the connection with blood plasma proteins by salicylates).

ACE inhibitors in combination with acetylsalicylic acid in high doses cause a decrease in glomerular filtration due to inhibition of the vasodilatory effect of prostaglandins and a decrease in the antihypertensive effect.

Acetazolamide. A possible increase in the concentration of acetazolamide can lead to the penetration of salicylates from the blood plasma into the tissue and cause toxicity of acetazolamide (fatigue, lethargy, drowsiness, confusion of consciousness, hyperchloremic metabolic acidosis) and toxicity of salicylates (vomiting, tachycardia, hyperpnea, confusion of consciousness).

Probenecid, sulfinpyrazone. When using probenecid and salicylates in high doses (500 mg), the metabolism of each other is inhibited and the excretion of uric acid may decrease.

Combinations that should be used with caution

Methotrexate. When using acetylsalicylic acid and methotrexate in doses of 15 mg/week, hematological toxicity of methotrexate increases (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from the connection with blood plasma proteins by salicylates).

Clopidogrel, ticlopidine. The combined use of clopidogrel and acetylsalicylic acid has a synergistic effect. Such combined use is carried out with caution, as it increases the risk of bleeding.

Anticoagulants (warfarin, phenprocoumon). It is possible to reduce the production of thrombin, as a result of which there is an indirect effect on reducing the activity of platelets (antagonist of vitamin K) and the risk of bleeding increases.

Abciximab, tirofiban, eptifibatide. Possible inhibition of glycoprotein IIb / IIIa receptors on platelets, which leads to an increased risk of bleeding.

Heparin. It is possible to reduce the production of thrombin, as a result of which there is an indirect effect on reducing the activity of platelets, which leads to an increase in the risk of bleeding.

If two or more of the above substances are used together with acetylsalicylic acid, this can lead to a synergistic effect of increasing the inhibition of platelet activity and, as a result, to an increase in hemorrhagic diathesis.

NSAIDs and COX-2 inhibitors (celecoxib). Simultaneous use increases the risk of gastrointestinal disorders, which can lead to gastrointestinal bleeding.

Ibuprofen. Simultaneous use of ibuprofen inhibits irreversible platelet aggregation caused by the action of acetylsalicylic acid. Ibuprofen treatment in patients with an increased risk of exposure to the cardiovascular system may limit the cardioprotective effect of acetylsalicylic acid.

Patients taking once-daily acetylsalicylic acid for cardiovascular disease prevention and occasionally taking ibuprofen should take acetylsalicylic acid at least 2 hours before taking ibuprofen.

Furosemide. Possible inhibition of the proximal tubular elimination of furosemide, which leads to a decrease in the diuretic effect of furosemide.

Quinidine. An additive effect on platelets is possible, which leads to an increase in the duration of bleeding.

Spironolactone. A modified effect of renin is possible, which leads to a decrease in the effectiveness of spironolactone.

Selective serotonin reuptake inhibitors. Simultaneous use increases the risk of gastrointestinal disorders, which can lead to gastrointestinal bleeding.

Valproate. When used simultaneously with valproate, acetylsalicylic acid displaces it from binding to blood plasma proteins, increasing the latter’s toxicity (suppression of CNS function, disturbances from the gastrointestinal tract).

Systemic corticosteroids (except hydrocortisone, which is used for replacement therapy in Addison’s disease) reduce the level of salicylates in the blood and increase the risk of overdose after the end of treatment.

Antidiabetic drugs. Simultaneous use of acetylsalicylic acid and antidiabetic drugs increases the risk of hypoglycemia.

Antacids. An increase in renal clearance and a decrease in renal absorption (due to an increase in urine pH) are possible, which leads to a decrease in the effect of acetylsalicylic acid.

Chickenpox vaccine. Simultaneous use increases the risk of developing Reye’s syndrome.

Gingko biloba. Simultaneous use with ginkgo biloba prevents the aggregation of platelets, which leads to an increased risk of bleeding.

Digoxin. With simultaneous use with digoxin, the concentration of the latter in the blood plasma increases due to a decrease in renal excretion.

Alcohol promotes damage to the mucous membrane of the gastrointestinal tract and prolongs the bleeding time due to the synergism of acetylsalicylic acid and alcohol.

Toxicity.

A dangerous dose. Adults: 300 mg/kg of body weight.

Chronic salicylate poisoning may be latent, as its signs and symptoms are nonspecific. Moderate chronic intoxication caused by salicylates, or salicylism, is noted, as a rule, only after repeated administration of the drug in high doses. Symptoms of moderate chronic poisoning (result of long-term use of the drug in high doses): dizziness, vertigo, deafness, increased sweating, fever, rapid breathing, tinnitus, respiratory alkalosis, metabolic acidosis, lethargy, moderate dehydration, headache, confusion, nausea and vomiting. Acute intoxication is indicated by a pronounced change in the acid-base balance, which may differ depending on age and severity of intoxication. Its frequent manifestation in children is metabolic acidosis. The severity of the condition cannot be estimated only on the basis of the concentration of salicylates in the blood plasma. Absorption of acetylsalicylic acid can slow down due to delayed gastric release, formation of concretions in the stomach or in the case of taking the drug in the form of enteric-coated tablets. Symptoms of severe and acute poisoning (due to overdose): hypoglycemia (mainly in children), encephalopathy, coma, arterial hypotension, pulmonary edema, convulsions, coagulopathy, cerebral edema, heart rhythm disturbances.

A more pronounced toxic effect occurs in patients with chronic overdose or drug abuse, as well as in the elderly or children.

Treatment. In case of an acute overdose, it is necessary to wash the stomach and take activated charcoal. If a dose higher than 120 mg/kg of body weight is suspected, use activated charcoal again.

Serum salicylate levels should be measured at least every 2 hours after dosing until salicylate levels are consistently reduced and acid-base balance is restored.

Prothrombin time and/or international normalized index should be checked, particularly if bleeding is suspected.

It is necessary to restore the balance of fluid and electrolytes. Effective methods of removing salicylate from blood plasma are alkaline diuresis and hemodialysis. Hemodialysis should be used in case of severe intoxication, as this method significantly accelerates the removal of salicylates and restores the acid-alkaline and water-salt balance.

Given the complex pathophysiological effects of salicylate poisoning, manifestations/symptoms/test results may include:

At a temperature not higher than 25 °C.