Thrombital Forte - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline - 24,15 mg, corn starch - 19,00 mg, potato starch - 4,00 mg, magnesium stearate - 0,30 mg. Sheath: hypromellose (hydroxypropylmethylcellulose 15 cps) - 1.20 mg, macrogol (polyglycol 4000) - 0.24 mg, talc - 0.72 mg.

Description:Round biconvex tablets coated with a white or almost white-colored film shell, on the transverse section a white or almost white core.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

N.02.B.A.51 Acetylsalicylic acid in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.Antiaggregant effect persists for 7 days after a single dose (more pronounced in men than in women). Acetylsalicylic acid reduces mortality and risk of myocardial infarction, unstable angina, is effective in primary prevention of diseases of the cardiovascular system, particularly myocardial infarction in men over 40 years, and for secondary prevention of myocardial infarction.

Suppresses the synthesis of prothrombin in the liver and increases prothrombin time. Increases fibrinolytic activity of blood plasma and reduces the concentration of vitamin-K-dependent clotting factors (II, VII, IX, X). Increases the risk of hemorrhagic complications during surgical interventions, increases the risk of bleeding during anticoagulant therapy.

Acetylsalicylic acid in high doses also has an anti-inflammatory, analgesic, antipyretic effect.

In high doses acetylsalicylic acid stimulates the excretion of uric acid (disrupts its reabsorption in the renal tubules).

Blockade of cyclooxygenase-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucosa and subsequent bleeding.

Magnesium hydroxide, which is part of the preparation Thrombital Forte, protects the mucous membrane of the gastrointestinal tract from the effects of acetylsalicylic acid.

Pharmacokinetics:

Acetylsalicylic acid is absorbed from the gastrointestinal tract almost completely. The half-life of acetylsalicylic acid is about 15 minutes. with the participation of enzymes acetylsalicylic acid quickly hydrolyzed into salicylic acid in the intestines, liver and blood plasma. Half-life of salicylic acid is about 3 hours, but it can significantly increase with the simultaneous administration of large doses of acetylsalicylic acid (more than 3.0 grams) as a result of saturation of enzyme systems.

Bioavailability of acetylsalicylic acid is 70%, but this value largely fluctuates, since acetylsalicylic acid is subjected to pre-systemic hydrolysis (gastrointestinal mucosa, liver) in salicylic acid under the action of enzymes. The bioavailability of salicylic acid is 80-100%.

The doses of magnesium hydroxide used do not affect the bioavailability of acetylsalicylic acid.

Indications:

Primary prevention of cardiovascular diseases, such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes, hyperlipidemia, hypertension, obesity, smoking, old age).

Prevention of cardiovascular diseases: repeated myocardial infarction, thrombosis of blood vessels.

Prevention of thromboembolism after surgical interventions on vessels (eg, aorto-coronary bypass, percutaneous transluminal coronary angioplasty, etc.).

Unstable angina (including suspected development of acute myocardial infarction).

Contraindications:

- Hypersensitivity to acetylsalicylic acid, drug auxiliaries and other non-steroidal anti-inflammatory drugs (NSAIDs);

- hemorrhage in the brain;

- propensity to bleed (insufficiency of vitamin K, thrombocytopenia, hemorrhagic diathesis);

- erosive-ulcerative lesion of the gastrointestinal tract (in the phase of exacerbation);

- gastrointestinal bleeding;

- The bronchial asthma, induced by the intake of salicylates and other NSAIDs;

- combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses with intolerance to acetylsalicylic acid;

- simultaneous reception of methotrexate in a dose of 15 mg per week or more;

- pregnancy (I and III trimesters);

- lactation period;

- deficiency of glucose-6-phosphate dehydrogenase;

- severe renal failure (creatinine clearance (CK) less than 30 ml / min);

- severe hepatic insufficiency (class B and C on the Child-Pugh scale);

- chronic heart failure III and IV functional class by classification NYHA;

- children's age till 18 years.

Carefully:

With gout, hyperuricemia, since acetylsalicylic acid in small doses reduces the excretion of uric acid.

In the presence of an anamnesis of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding.

With hepatic insufficiency (class A on the Child-Pugh scale).

With renal failure (QC more than 30 ml / min).

With bronchial asthma, chronic diseases of the respiratory system, hay fever, polyposis of the nose, allergic conditions, drug allergies.

With diabetes.

In elderly patients.

In the second trimester of pregnancy.

With the proposed surgical intervention (including minor, for example, tooth extraction), because acetylsalicylic acid may cause a tendency to develop bleeding within a few days after taking the drug.

At simultaneous reception with the following medicines (see the section "Interaction with other drugs"):

- with methotrexate in a dose of less than 15 mg per week;

- with anticoagulants, thrombolytic or antiplatelet agents;

- with NSAIDs and salicylic acid derivatives in large doses;

- with digoxin;

- with hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin;

- with valproic acid;

- with alcohol (alcoholic beverages in particular);

- with selective serotonin reuptake inhibitors;

- with ibuprofen,

- with narcotic analgesics,

- with sulfonamides (including co-trimoxazole),

- with inhibitors of carbonic anhydrase (acetazolamide),

- with lithium,

- with systemic glucocorticosteroids.

Pregnancy and lactation:

The drug Trombital Forte is contraindicated for use in the I and III trimesters of pregnancy, tk.has a teratogenic effect - when applied in the first trimester of pregnancy leads to the fetal splitting of the upper palate, in the third trimester - causes inhibition of labor (suppression of prostaglandin synthesis), premature closure of the arterial duct in the fetus, hyperplasia of pulmonary vessels and hypertension in the small circulation.

Reception of the drug in the second trimester is possible only if the potential benefit to the mother exceeds the risk to the fetus.

Acetylsalicylic acid and its metabolites penetrate into breast milk. For the duration of treatment, breast-feeding should be discontinued.

Dosing and Administration:

The drug is taken orally with water. The tablet can be swallowed whole, chewed or pre-grated.

The drug is intended for long-term use. The duration of treatment with Trombital Forte is determined by the doctor. In 1 tablet, Thrombital Forte contains 150 mg of acetylsalicylic acid. If necessary, according to the doctor's decision, it is possible to reduce the daily dose of acetylsalicylic acid to 75 mg (see section "Special instructions"). Primary prevention of cardiovascular diseases,such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age) - 1 tablet 1 time per day.

Prevention of cardiovascular diseases: repeated myocardial infarction, thrombosis of blood vessels - 1 tablet once a day.

Preventive maintenance of thromboembolism after surgical interventions on vessels (for example, aorto-coronary bypass, percutaneous transluminal coronary angioplasty, etc.) - 1 tablet once a day.

Unstable angina (including suspected development of acute myocardial infarction) - 1 tablet once a day.

With unstable angina pectoris with suspected development of acute myocardial infarction, the first tablet must be chewed for faster absorption.

Use the drug only according to the indications, that way of use and in those doses, which are specified in the instructions.

Side effects:

The undesirable phenomena listed below are distributed according to the frequency of occurrence in accordance with the following gradation: very often (with a frequency of more than 1/10),often (at a frequency of at least 1/100 but less than 1/10), infrequently (with a frequency of at least 1/1000 but less than 1/100), rarely (with a frequency of at least 1/10000 but less than 1/1000) , very rarely (with a frequency of less than 1/10000), including individual messages.

On the part of the blood and lymphatic system: very often - increased bleeding (hematomas, nasal bleeding, bleeding gums, bleeding from the genitourinary tract); rarely anemia; very rarely - hypoprothrombinemia, thrombocytopenia, neutropenia, aplastic anemia, eosinophilia, agranulocytosis; an unknown frequency is leukopenia. There are reports of serious bleeding events, which include gastrointestinal bleeding and cerebral hemorrhage (especially in patients with hypertension who have not reached the target figures for blood pressure and / or are receiving concomitant therapy with anticoagulant drugs), which in some cases may be life threatening character. Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (for example, due to latent bleeding) with appropriate clinical and laboratory signs and symptoms (asthenia, pallor, hypoperfusion).There are reports of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

Allergic reactions: often - urticaria, angioedema; infrequently - anaphylactic reactions, including angioedema; unknown frequency - skin rash, pruritus, rhinitis, swelling of the nasal mucosa, cardio-respiratory distress syndrome, and severe reactions, including anaphylactic shock.

From the nervous system: often - headache, insomnia; infrequently - dizziness, drowsiness; rarely - noise in the ears, intracerebral haemorrhage; unknown frequency - hearing loss, which may be a sign of drug overdose (see section "Overdose").

From the respiratory system, organs of the chest and mediastinum: often - bronchospasm.

From the gastrointestinal tract: very often heartburn; often - nausea, vomiting; rarely - pain in the abdomen, ulcers of the gastric mucosa and duodenal ulcers, including perforating (rare), gastrointestinal bleeding; rarely - increased activity of "liver" enzymes; very rarely - stomatitis,esophagitis, erosive lesions of the upper gastrointestinal tract, strictures, irritable bowel syndrome, colitis; unknown frequency - decreased appetite, diarrhea.

From the urinary system: unknown frequency - renal dysfunction and acute renal failure.

If you have side effects, specified in the instructions, or they are aggravated, or you notice any other side effects, not specified in the instructions, inform the doctor about it.

Overdose:

May occur after a single dose of a large dose or with prolonged use of the drug. If a single dose of acetylsalicylic acid is less than 150 mg / kg, acute poisoning is considered easy, 150-300 mg / kg is of moderate severity, and when used at higher doses, it is severe.

Symptoms of an overdose from mild to moderate severity: dizziness, tinnitus, hearing impairment, visual impairment, increased sweating, nausea, vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

Treatment: provocation of vomiting, repeated intake of activated carbon, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state.

Symptoms of an overdose from medium to severe:

- respiratory alkalosis with compensatory metabolic acidosis;

- hyperpyrexia (extremely high body temperature);

- breathing disorders: hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia;

- disorders of the cardiovascular system: heart rhythm disturbances, lowering of blood pressure, suppression of cardiac activity, collapse;

- disturbance of water-electrolyte balance: dehydration, disturbance of kidney function from oliguria up to the development of renal failure, characterized by hypokalemia, hypernatremia, hyponatremia;

- impaired glucose metabolism: hyperglycemia, hypoglycemia (especially in children), ketoacidosis;

- noise in the ears, deafness;

- gastrointestinal bleeding;

- hematological disorders: from inhibition of platelet aggregation to coagulopathy, prolongation of prothrombin time, hypoprothrombinemia;

- neurological disorders: toxic encephalopathy and depression of the central nervous system (drowsiness, confusion, coma, convulsions).

Treatment: Immediate hospitalization in specialized departments for emergency therapy - gastric lavage, repeated intake of activated charcoal and laxatives, alkalinization of urine (shown at a salicylate level above 500 mg / l, provided by intravenous infusion of sodium hydrogen carbonate - 88 meq per 1 liter of 5% glucose solution, at a rate of 10-15 ml / kg / h), recovery of circulating blood volume and induction of diuresis (achieved by the introduction of sodium bicarbonate in the same dose and dilution, repeated 2-3 times); it should be borne in mind that intensive infusion of fluid to elderly patients can lead to pulmonary edema. It is not recommended to use acetosolamide for urine alkalinization (can cause acidemia and enhance the toxic effect of salicylates). When carrying out alkaline diuresis, it is necessary to achieve pH values between 7.5 and 8. Hemodialysis is indicated with a salicylate level in the blood plasma of more than 1000 mg / l, and in patients with chronic poisoning - 500 mg / l and lower if there are indications (refractory acidosis, deterioration of the condition, severe central nervous system damage, pulmonary edema and renal failure).It is shown in pulmonary edema artificial ventilation with a mixture enriched in oxygen at a positive pressure mode at the end of the exhalation; To treat edema of the brain, hyperventilation and osmotic diuresis are used. The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism (nausea, vomiting, tinnitus, visual impairment, dizziness, headache, general malaise) are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood plasma.

Interaction:

With simultaneous application acetylsalicylic acid enhances the effect of the following drugs:

- methotrexate by reducing renal clearance and displacing it from the bond with proteins, the combination of acetylsalicylic acid with methotrexate is accompanied by an increased incidence of side effects on the part of the organs of hematopoiesis;

- narcotic analgesics, other NSAIDs;

- heparin and indirect anticoagulants due to disruption of platelet function and displacement of indirect anticoagulants from the connection with plasma proteins;

- thrombolytic, antiaggregant and anticoagulant drugs (ticlopidine);

- digoxin due to a decrease in its renal excretion;

- hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin due to hypoglycemic properties of acetylsalicylic acid itself in high doses and displacement of sulfonylurea derivatives from binding to plasma proteins;

- Valproic acid due to its displacement from the connection with blood plasma proteins. Simultaneous use of acetylsalicylic acid with ibuprofen leads to a decrease in the cardioprotective effects of acetylsalicylic acid.

The combination of acetylsalicylic acid with anticoagulants, thrombolytic agents and antiplatelet agents is accompanied by an increased risk of bleeding. Simultaneous reception with acetylsalicylic acid increases the concentration of barbiturates and lithium salts in blood plasma.

By enhancing the elimination of salicylates, systemic glucocorticosteroids weaken their action.

Glucocorticosteroids, ethanol and ethanol-containing drugs increase the negative effect on the mucous membrane of the gastrointestinal tract and increase the risk of developing gastrointestinal bleeding.

With the simultaneous administration of acetylsalicylic acid with ethanol, an increase in the toxic effect of ethanol on the central nervous system is observed. Acetylsalicylic acid uricosuric drugs - benzbromarone, probenicida (a decrease in the uricosuric effect due to competitive suppression of renal tubular excretion by uric acid), angiotensin converting enzyme inhibitors (a dose-dependent decrease in the glomerular filtration rate due to inhibition of prostaglandins with vasodilating action and, accordingly, weakening of the hypotensive effect) , diuretics (when combined with acetylsalicylic acid in a high dose x there is a decrease in the glomerular filtration rate as a result of a decrease in the synthesis of prostaglandins in the kidneys). Antacids and colestramine reduce the absorption of acetylsalicylic acid.

If you use the above or other medicines (including OTC drugs), consult your doctor before using Trombital Forte.

Special instructions:

The drug should be used as directed by a doctor.

Tablets of the drug Trombital Forte are film-coated, do not have risks and are not intended for division, so if a doctor recommends a reduction in the daily dose of acetylsalicylic acid to 75 mg, then a transition to another drug containing 75 mg of acetylsalicylic acid in 1 tablet is required. Acetylsalicylic acid can provoke bronchospasm, as well as cause seizures of bronchial asthma and other reactions of hypersensitivity. Risk factors are the availability of a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system as well as of allergic reactions to other drugs (e.g., skin reactions, pruritus, urticaria). Acetylsalicylic acid can cause bleeding of varying severity during and after surgical interventions. A few days before the planned surgical intervention, the risk of developing bleeding should be assessed compared with the risk of developing ischemic complications in patients taking low doses of acetylsalicylic acid.If the risk of bleeding is significant, the intake of acetylsalicylic acid should be temporarily discontinued. The combination of acetylsalicylic acid with anticoagulants, thrombolytics and antiplatelet drugs is accompanied by an increased risk of bleeding.

Acetylsalicylic acid in low doses can provoke the development of gout in predisposed patients (having decreased uric acid excretion). The combination of acetylsalicylic acid with methotrexate is accompanied by an increased incidence of side effects from the hematopoiesis.

High doses of acetylsalicylic acid have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents for ingestion and insulin.

When combined systemic glucocorticosteroids and salicylates should be remembered that during treatment, the concentration of salicylates in the blood is reduced, and after the abolition of systemic glucocorticosteroids, an overdose of salicylates is possible.

The combination of acetylsalicylic acid with ibuprofen is not recommended in patients with an increased risk of cardiovascular disease:simultaneous application with ibuprofen, there is a decrease in the antiplatelet effect of acetylsalicylic acid in doses up to 300 mg, which leads to a decrease in the cardioprotective effects of acetylsalicylic acid.

An increase in the dose of acetylsalicylic acid over therapeutic doses is associated with a risk of gastrointestinal bleeding.

With prolonged use of low doses of acetylsalicylic acid as antiplatelet therapy, caution should be exercised in elderly patients due to the risk of developing gastrointestinal bleeding.

With the simultaneous administration of acetylsalicylic acid with alcohol, the risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of bleeding time are increased.

With prolonged use of the drug should periodically make a general blood test and analysis of feces for latent blood.

Effect on the ability to drive transp. cf. and fur:

During the treatment with acetylsalicylic acid, caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 150 mg + 30.39 mg.

Packaging:

For 30 or 100 tablets in cans of dark (amber) glass, sealed with a screw cap of white color (from polyethylene) with a built-in removable capsule with silica gel and a ring that provides control of the first opening.

1 bank of dark (amber) glass, together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004144

Date of registration:13.02.2017

Expiration Date:13.02.2022

The owner of the registration certificate:OTISIFARM, OJSC OTISIFARM, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp25.03.2017

Illustrated instructions

Instructions

Thrombital Forte (Trombital Forte)