Group: Drugs affecting the blood system and hematopoiesis
Active ingredient: acetylsalicylic acid
General characteristics
Composition of the medicinal product:
active ingredient: acetylsalicylic acid;
1 tablet contains acetylsalicylic acid 100 mg;
Excipients: powdered cellulose, corn starch, methacrylate copolymer dispersion, talc, triethyl citrate, polysorbate 80, sodium lauryl sulfate.
Dosage form.
Enteric-coated tablets.
Round, film-coated tablets, white or almost white in color, with a biconvex surface. When broken, a core surrounded by a single continuous layer is visible under a magnifying glass.
Name and location of the manufacturer. PrJSC "Technolog", Ukraine, 20300,
Cherkasy region, Uman city, Manuilsky str., 8.
Pharmacotherapeutic group.
Antithrombotic agents. Acetylsalicylic acid. ATC code B01A C06.
Pharmacodynamics. Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane A 2. The mechanism of its action is the irreversible inactivation of the cyclooxygenase enzyme (COX-1). This inhibitory effect is especially pronounced for platelets, since they are not capable of resynthesis of the specified enzyme. Acetylsalicylic acid also exhibits other inhibitory effects on platelets. Due to these effects, it is used in many vascular diseases.
Acetylsalicylic acid belongs to the group of nonsteroidal anti-inflammatory drugs (NSAIDs) with analgesic, antipyretic and anti-inflammatory properties. Orally in doses of 0.3 g and 1 g, the drug is used to relieve pain and in conditions accompanied by mild fever, such as colds and flu, to reduce fever and relieve pain in the joints and muscles.
After oral administration, acetylsalicylic acid is rapidly and completely absorbed from the gastrointestinal tract. During and after absorption, it is converted into the main active metabolite - salicylic acid. The maximum concentration of acetylsalicylic acid in the blood plasma is reached after 10-20 minutes, salicylates - after 20 - 120 minutes, respectively. Due to the enteric coating of Trombolic-Cardio tablets, the release of the active substance is carried out not in the stomach, but in the alkaline environment of the intestine. Therefore, the absorption of acetylsalicylic acid is slowed down to 3-6 hours after taking a tablet coated with an enteric coating, compared to a regular tablet. Acetylsalicylic and salicylic acids are completely bound to blood plasma proteins and are rapidly distributed in the body. Salicylic acid penetrates the placenta and also enters breast milk. Salicylic acid is metabolized in the liver. The metabolites of salicylic acid are salicyluric acid, salicylphenol glucuronide, salicylacyl glucuronide, gentisic acid and gentisinuric acid. The elimination kinetics of salicylic acid are dose-dependent, since metabolism is limited by the activity of liver enzymes. The half-life is dose-dependent and increases from 2-3 hours at low doses to 15 hours at high doses. Salicylic acid and its metabolites are excreted from the body mainly by the kidneys.
Indications for use.
To reduce risk:
Death in patients with suspected acute myocardial infarction; Death in patients who have had myocardial infarction; Transient ischemic attacks (TIA) and stroke in patients with TIA; Morbidity and death in stable and unstable angina.
For prevention:
thromboses and embolisms after vascular surgery (percutaneous transluminal catheter angioplasty (PTCA), carotid endarterectomy, coronary artery bypass grafting (CABG), arteriovenous bypass grafting); deep vein thrombosis and pulmonary embolism after prolonged immobilization (after surgery); myocardial infarction in patients with a high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and individuals with a multifactorial risk of cardiovascular diseases (hyperlipidemia, obesity, smoking, old age, etc.); stroke (secondary prevention).
Contraindication.
Hypersensitivity to acetylsalicylic acid, other salicylates or any component of the drug. Chronic asthma caused by the use of salicylates or NSAIDs in history. Acute peptic ulcers. Hemorrhagic diathesis. Severe renal failure. Severe hepatic failure. Severe heart failure.
Combination with methotrexate at a dosage of 15 mg/week or more (see “Interaction with other medicinal products and other types of interactions”).
III trimester of pregnancy. Children up to 16 years of age.
Special precautions.
Trombolic-Cardio is used with caution in: hypersensitivity to analgesics, anti-inflammatory, antirheumatic drugs, as well as in the presence of allergies to other substances; gastrointestinal ulcers, including chronic and recurrent peptic ulcers or a history of gastrointestinal bleeding; simultaneous use of anticoagulants; impaired renal and/or hepatic function.
In patients with allergic complications, including bronchial asthma, allergic rhinitis, urticaria, skin itching, swelling of the mucous membrane and nasal polyposis, as well as in combination with chronic respiratory tract infections and in patients with hypersensitivity to NSAIDs, the development of bronchospasm or an attack of bronchial asthma is possible during treatment with Trombolic-Cardio.
During surgical operations (including dental), the use of drugs containing acetylsalicylic acid may increase the likelihood of bleeding.
When using low doses of acetylsalicylic acid, uric acid excretion may be reduced. This may lead to the development of gout in patients with reduced uric acid excretion.
Do not use acetylsalicylic acid-containing drugs in children with acute respiratory viral infections (ARI), with or without fever, without consulting a doctor. With some viral diseases, especially influenza A, influenza B and chickenpox, there is a risk of developing Reye's syndrome, which is a very rare but life-threatening disease that requires urgent medical intervention. The risk may be increased if acetylsalicylic acid is used as a concomitant drug, but a causal relationship in this case has not been proven. If these conditions are accompanied by prolonged vomiting, this may be a sign of Reye's syndrome.
Use during pregnancy or breastfeeding.
Trombolic-Cardio can be used during pregnancy only if other medications are ineffective.
The use of salicylates in the first trimester of pregnancy in some retrospective epidemiological studies was associated with an increased risk of congenital malformations (palatoschisis ("wolf mouth"), heart defects). However, with prolonged use of the drug in therapeutic doses exceeding 150 mg/day, this risk is low: as a result of a study conducted on 32,000 mother-child pairs, no connection was found between the use of the drug Trombolic-Cardio and an increase in the number of congenital malformations.
Salicylates can be used in the first and second trimesters of pregnancy only after assessing the risk/benefit ratio. According to preliminary estimates, with long-term use of the drug Trombolic-Cardio, it is undesirable to take acetylsalicylic acid in a dose exceeding 150 mg/day.
In the third trimester of pregnancy, taking salicylates in high doses (more than 300 mg/day) can lead to miscarriage and decreased labor contractions, as well as cardiopulmonary toxicity (premature closure of the ductus arteriosus) in children.
The use of acetylsalicylic acid in large doses before delivery may lead to intracranial bleeding, especially in premature infants. Therefore, except in extremely special cases due to cardiological or obstetric medical indications with special monitoring, the use of acetylsalicylic acid during the last trimester of pregnancy is contraindicated.
Salicylates and their metabolites pass into breast milk in small amounts.
Since no adverse reactions in infants have been observed after accidental use of Trombolic-Cardio, it is usually not necessary to interrupt breastfeeding. With prolonged use of the drug or the use of acetylsalicylic acid at high doses, the question of stopping breastfeeding should be considered.
The ability to influence the reaction speed when driving or working with other mechanisms.
Does not affect.
children
For the above reasons, the use of the drug is contraindicated in children under 16 years of age without special indications (Kawasaki disease).
Method of administration and doses.
Trombolic-Cardio is prescribed for adults and children over 16 years of age. The drug is taken orally before meals, without chewing, with sufficient liquid.
To reduce the risk of death in patients with suspected acute myocardial infarction, the drug is used at a dose of 100 mg per day. A dosage of 300 mg per day can be used for a short time according to therapeutic indications. To achieve rapid absorption, the first tablet should be chewed.
To reduce the risk of death in patients who have had a myocardial infarction, 100 mg per day is used. A dosage of 300 mg per day may be used for short periods according to therapeutic indications.
For secondary prevention of stroke, it is used at a dose of 100 mg per day. A dosage of 300 mg per day can be used for a short time according to therapeutic indications.
To reduce the risk of TIA and stroke in patients with TIA, 100-200 mg per day is used. A dosage of 300 mg per day may be used for short-term therapeutic indications.
To reduce the risk of disease progression and death in patients with stable and unstable angina: from 100 mg per day. A dosage of 300 mg per day may be used for short periods according to therapeutic indications.
For the prevention of deep vein thrombosis and pulmonary embolism after prolonged immobilization (after surgery) - 100-200 mg per day or 300 mg per day every other day.
For the prevention of myocardial infarction in patients with a high risk of developing cardiovascular complications (diabetes mellitus, controlled arterial hypertension) and in individuals with a multifactorial risk of cardiovascular disease (hyperlipidemia, obesity, smoking, old age), 100 mg per day is used. A dosage of 300 mg per day can be used for a short time according to therapeutic indications.
warning:
The drug should be prescribed to children taking into account the information provided in the “Special Precautions” section of the Instructions.
Overdose.
Salicylate overdose is possible due to chronic intoxication resulting from long-term therapy (administration of more than 100 mg/kg/day for more than 2 days may cause toxic effects), as well as due to acute intoxication that is life-threatening (overdose), and the causes of which may be, for example, accidental use by children or unforeseen overdose.
Chronic salicylate poisoning can be insidious because its signs and symptoms are nonspecific. Moderate chronic salicylate intoxication, or salicylism, usually occurs only after repeated ingestion of large doses.
Symptoms: Dizziness, vertigo, tinnitus, deafness, increased sweating, nausea and vomiting, headache, confusion. These symptoms can be controlled by reducing the dose. Tinnitus may occur at plasma salicylate concentrations above 150-300 mcg/mL. More serious adverse reactions occur at plasma salicylate concentrations above 300 mcg/mL.
Acute intoxication is indicated by a pronounced change in the acid-base balance, which may vary depending on age and severity of intoxication. The most common indicator for children is metabolic acidosis. The severity of the condition cannot be assessed solely on the basis of the concentration of salicylates in the plasma. The absorption of acetylsalicylic acid may be slowed down due to delayed gastric emptying, the formation of concrements in the stomach or when the drug is taken in the form of tablets coated with an enteric coating.
Treatment. Treatment of intoxication caused by an overdose of acetylsalicylic acid is determined by the severity, clinical symptoms and is provided by standard methods used in poisoning. All measures taken should be aimed at accelerating the removal of the drug and restoring electrolyte and acid-base balance. Activated charcoal, forced alkaline diuresis are used. Depending on the state of acid-base balance and electrolyte balance, infusion of electrolyte solutions is carried out. In severe poisoning, hemodialysis is indicated.
Side effects.
Digestive tract: dyspepsia, epigastric pain and abdominal pain; in some cases - inflammation of the gastrointestinal tract, erosive-ulcerative lesions of the gastrointestinal tract, which can in isolated cases cause gastrointestinal hemorrhages and perforations with corresponding laboratory indicators and clinical manifestations. Central nervous system: dizziness and tinnitus have been observed, which may indicate an overdose. Hematopoietic system: due to its antiplatelet effect on platelets, acetylsalicylic acid may increase the risk of bleeding. Bleeding such as intraoperative hemorrhages, hematomas, bleeding from the genitourinary system, nosebleeds, bleeding from the gums have been observed; rarely or very rarely - serious bleeding, such as gastrointestinal bleeding, cerebral hemorrhage (especially in patients with uncontrolled arterial hypertension and / or with simultaneous use of antihemostatic agents), which in isolated cases could be potentially life-threatening. Hemorrhages can lead to acute and chronic post-hemorrhagic anemia / iron deficiency anemia (due to so-called hidden microbleeding) with corresponding laboratory manifestations and clinical symptoms, such as asthenia, pallor of the skin, hypoperfusion. Liver: rarely - transient liver failure with increased levels of liver transaminases. Allergic reactions: in patients with individual hypersensitivity to salicylates, allergic skin reactions may develop, including symptoms such as rash, urticaria, edema, itching. In patients with bronchial asthma, an increased frequency of bronchospasm may occur; allergic reactions of mild to moderate severity, potentially affecting the skin, respiratory tract, gastrointestinal tract and cardiovascular system. Severe reactions, including anaphylactic shock, have been observed very rarely.
Interaction with other drugs and other types of interactions.
Contraindications for interaction.
The use of methotrexate in doses of 15 mg/week or more increases the hematological toxicity of methotrexate (reduction in renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from plasma protein binding by salicylates).
When using this drug in doses less than 15 mg/week, the hematological toxicity of methotrexate increases (reduction in renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate from plasma protein binding by salicylates).
Concomitant use of ibuprofen prevents irreversible inhibition of platelets by acetylsalicylic acid. Treatment of patients at risk of cardiovascular disease with ibuprofen may limit the cardioprotective effect of acetylsalicylic acid.
The simultaneous use of the drug Trombolic-Cardio and anticoagulants increases the risk of bleeding.
The simultaneous use of high doses of salicylates with NSAIDs (due to a mutually reinforcing effect) increases the risk of ulcers and gastrointestinal bleeding.
Concomitant use with uricosuric agents such as benzobromarone, probenecid reduces the effect of uric acid excretion (due to competition for uric acid excretion by the renal tubules).
When used simultaneously with digoxin, the concentration of the latter in plasma increases due to reduced renal excretion.
With the simultaneous use of high doses of acetylsalicylic acid and oral antidiabetic drugs from the group of sulfonylurea derivatives or insulin, the hypoglycemic effect of the latter is enhanced due to the hypoglycemic effect of acetylsalicylic acid and the displacement of sulfonylurea bound to plasma proteins.
Diuretics in combination with high doses of acetylsalicylic acid reduce glomerular filtration by reducing prostaglandin synthesis in the kidneys.
Systemic glucocorticosteroids (excluding hydrocortisone), which are used for replacement therapy in Addison's disease, reduce the level of salicylates in the blood during corticosteroid treatment and increase the risk of overdose after the end of treatment.
When used with corticosteroids, the risk of gastrointestinal bleeding increases.
Angiotensin-converting enzymes (ACE) in combination with high doses of acetylsalicylic acid cause a decrease in glomerular filtration due to inhibition of vasodilator prostaglandins and a decrease in the antihypertensive effect.
When used simultaneously with valproic acid, acetylsalicylic acid displaces it from its connection with plasma proteins, increasing the toxicity of the latter.
Ethyl alcohol contributes to damage to the mucous membrane of the gastrointestinal tract and prolongs bleeding time due to the synergism of acetylsalicylic acid and alcohol.
Expiration date.
3 years.
Storage conditions.
Store at a temperature not exceeding 25 0 C.
Keep out of reach of children.
Packaging.
10 tablets with a dosage of 100 mg in blisters.
2 blisters in a cardboard pack.
Vacation category.
Without a prescription.
