Thrombital pills 75mg+15.2mg, 30pcs

Composition

Per tablet:

Active ingredients:  

acetylsalicylic acid – 75.00 mg,

magnesium hydroxide-15.20 mg.

Auxiliary substances:  

microcrystalline cellulose – 12.07 mg,

corn starch-9.50 mg,

potato starch-2.00 mg,

magnesium stearate-0.15 mg.

Shell:

hypromellose (hydroxypropylmethylcellulose 15 sPz) – 0.60 mg,

macrogol (polyglycol 4000) – 0.12 mg,

talc-0.36 mg

Pharmacological action

Pharmacodynamics

Reduces platelet aggregation, adhesion and thrombosis by suppressing the synthesis of thromboxane A2 in platelets. The antiplatelet effect persists for 7 days after a single dose (more pronounced in men than in women).

Acetylsalicylic acid reduces the mortality and risk of myocardial infarction in unstable angina, is effective in the primary prevention of diseases of the cardiovascular system, especially myocardial infarction in men over 40 years of age, and in the secondary prevention of myocardial infarction.

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

Acetylsalicylic acid in high doses also has anti-inflammatory, analgesic, and antipyretic effects.

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 mucous membrane and subsequent bleeding.

Magnesium hydroxide, which is part of the drug Trombital, protects the mucous membrane of the gastrointestinal tract from the effects of acetylsalicylic acid.

Pharmacokinetics

Acetylsalicylic acid is absorbed almost completely from the gastrointestinal tract. The elimination half-life of acetylsalicylic acid is about 15 minutes, because with the participation of enzymes, acetylsalicylic acid is rapidly hydrolyzed to salicylic acid in the intestine, liver and blood plasma.

The half-life of salicylic acid is about 3 hours, but it can significantly increase with the simultaneous use of large doses of acetylsalicylic acid (more than 3.0 g) as a result of saturation of enzyme systems.

The bioavailability of acetylsalicylic acid is 70%, but this value largely fluctuates, since acetylsalicylic acid undergoes presystemic hydrolysis (gastrointestinal mucosa, liver) to 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 mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old age).

Prevention of recurrent myocardial infarction and blood vessel thrombosis.

Prevention of thromboembolism after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty).

Unstable angina pectoris.

Use during pregnancy and lactation

Salicylic acid penetrates the placental barrier.

The drug Trombital is contraindicated for use in the first and third trimesters of pregnancy, because it has a teratogenic effect – when used in the first trimester of pregnancy, it leads to cleavage of the upper palate in the fetus, in the third trimester it causes inhibition of labor (suppression of prostaglandin synthesis), premature closure of the arterial duct in the fetus, pulmonary vascular hyperplasia and hypertension in the small circulatory circle.

Taking 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 pass into breast milk. Breast-feeding should be discontinued for the duration of treatment.

Contraindications

• Hypersensitivity to acetylsalicylic acid, auxiliary substances of the drug and other nonsteroidal anti-inflammatory drugs (NSAIDs);

• bleeding in the brain;

• a tendency to bleeding (vitamin K, thrombocytopenia, hemorrhagic diathesis);

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

• gastrointestinal bleeding;

• asthma induced by ingestion of salicylates and other NSAIDs;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses with intolerance to acetylsalicylic acid or other NSAIDs, including cyclooxygenase-2 inhibitors (including in the anamnesis);

• simultaneous reception of dose methotrexate 15 mg per week or more;

• pregnancy (I and III trimester);

• lactation;

• deficiency of glucose-6-phosphate dehydrogenase;

• severe renal insufficiency (creatinine clearance (CC) of less than 30 ml/min);

• severe liver failure (class b and C according to child-Pugh);

• chronic heart failure III and IV functional class NYHA classification;

• children up to age 18 years.

With caution

For gout, hyperuricemia, as acetylsalicylic acid in small doses reduces the excretion of uric acid.

If there is a history of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding.

In case of hepatic insufficiency (Child-Pugh class A).

In case of renal insufficiency (creatinine clearance more than 30 ml / min).

For bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, allergic conditions, drug allergies.

In the second trimester of pregnancy.

With diabetes mellitus.

In elderly patients.

If surgery is considered (including minor ones, such as tooth extraction), acetylsalicylic acid may cause a tendency to develop bleeding within a few days after taking the drug.

When taken concomitantly with the following medications (see section “Interaction with other medications”):

• with methotrexate at a dose of less than 15 mg per week;

• with anticoagulants, thrombolytic or antiplatelet drugs;

• NSAIDs and derivatives of salicylic acid in high doses;

• digoxin;

• with hypoglycemic agents for oral use (sulfonylureas) and insulin;

• with valproic acid,

• alcohol (alcohol in particular);

• with selective inhibitors of serotonin reuptake;

• with ibuprofen

• with lithium drugs,

• systemic corticosteroids,

• ethanol,

• narcotic analgesics,

• with sulfonamides,

• with the carbonic anhydrase inhibitors.

Side effects

Defining the categories of frequency of adverse events: very common (with a frequency of more than 1/10), common (with a frequency of at least 1/100, but less than 1/10), infrequent (with a frequency of at least 1/1000, but less than 1/100), rare (with a frequency of at least 1/10000, but less than 1/1000), very rare (with a frequency of less than 1/10000), including individual reports.

From the hematopoietic system:  very often-increased bleeding (hematomas, nosebleeds, bleeding gums, bleeding from the genitourinary tract); rarely-anemia; very rarely-hypoprothrombinemia, thrombocytopenia, neutropenia, aplastic anemia, eosinophilia, agranulocytosis; frequency unknown-leukopenia.

There are reports of serious cases of bleeding, which include gastrointestinal bleeding and brain hemorrhage (especially in patients with arterial hypertension who have not reached the target blood pressure values and/or are receiving concomitant therapy with anticoagulants), which in some cases can be life-threatening.

Bleeding can lead to the development of acute or chronic post-hemorrhagic / iron-deficient anemia (for example, due to latent bleeding) with appropriate clinical and laboratory signs and symptoms (asthenia, pallor, hypoperfusion). Hemolysis and hemolytic anemia have been reported in patients with severe glucose-6-phosphate dehydrogenase deficiency.

Allergic reactions:  often – urticaria, angioedema; infrequently – anaphylactic reactions, including angioedema; frequency unknown-skin rash, pruritus, rhinitis, nasal mucosal edema, cardio-respiratory distress syndrome, as well as severe reactions, including anaphylactic shock.

Nervous system disorders:  often – headache, insomnia; infrequently-dizziness, drowsiness; rarely-tinnitus, intracerebral hemorrhage; frequency unknown-hearing loss, which may be a sign of overdose of the drug (see the section “Overdose”).

Respiratory system disorders:  often – bronchospasm.

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

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

If the side effects mentioned above are observed, or they worsen, or any other side effects occur, the patient should inform the doctor.

Interaction

When used concomitantly, acetylsalicylic acid enhances the effect of the following medications::

– methotrexate by reducing renal clearance and ousting him from the blood, the combination of acetylsalicylic acid with methotrexate is accompanied by increased incidence of side effects from the digestive blood;

– narcotic analgesics, other NSAIDs;

– heparin and indirect anticoagulants due to dysfunction of platelets, and displacing anticoagulants from plasma proteins of the blood;

– thrombolytic, antiplatelet and anticoagulant drugs (ticlopidine);

digoxin due to a decrease in its renal excretion;

– hypoglycemic agents for oral use (sulfonylureas) and insulin due to the hypoglycemic properties of the acetylsalicylic acid in high doses and displacement of sulfonylureas from the blood plasma of the blood;

– valproic acid due to displacement from its Association 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, thrombolytics and antiplatelet agents is associated with an increased risk of bleeding.

Simultaneous use with acetylsalicylic acid increases the concentration of barbiturates and lithium salts in the blood plasma.

By increasing the elimination of salicylates, systemic corticosteroids weaken their effect.

CORTICOSTEROIDS, ethanol and ethanol-containing drugs increase the negative impact on the gastrointestinal mucosa and increase the risk of gastrointestinal bleeding.

The simultaneous use of acetylsalicylic acid with ethanol increased the toxic effect of ethanol on the Central nervous system.

Acetylsalicylic acid reduces the effect of uricosuric medicines benzbromarone, probenecid (decrease uricosuric effect due to competitive suppression of renal tubular excretion of uric acid), ACE inhibitors (marked dose-dependent decrease in glomerular filtration rate as a result of inhibition of prostaglandins, which has vasodilating effect, and, consequently, the attenuation of the hypotensive effect), diuretics (combined with acetylsalicylic acid in high doses there is a decrease in glomerular filtration rate due to the reduction of prostaglandin synthesis in the kidneys).

Antacids and colestyramine reduce the absorption of acetylsalicylic acid.

If the patient uses the above or other medications (including over-the-counter medications), you should consult your doctor before taking Trombital.

How to take, course of use and dosage

The drug is taken orally, once a day, with water. The tablet can be swallowed whole, chewed or pre-ground.

Primary prevention of cardiovascular diseases such as thrombosis and acute heart failure in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old age): Take 2 tablets of the drug Trombital on the first day, then 1 tablet 1 time a day.

Prevention of recurrent myocardial infarction and blood vessel thrombosis:1-2 tablets of the drug Trombital 1 time a day.

Prevention of thromboembolism after vascular surgery (coronary artery bypass grafting, percutaneous transluminal coronary angioplasty):1-2 tablets of the drug Trombital 1 time a day.

Unstable angina: 1-2 tablets of the drug Trombital 1 time a day.

The drug is intended for long-term use. The duration of treatment and the dose of Trombital is determined by the doctor.

Use the drug only according to the indications, the method of use and in the doses indicated in the instructions.

Overdose

It may occur after a single 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 mild,150-300 mg/kg – moderate, and with higher doses – severe.

Mild to moderate overdose symptoms: dizziness, tinnitus, hearing loss, visual impairment, increased sweating, nausea, vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

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

Moderate to severe overdose symptoms: 

· respiratory alkalosis with compensatory metabolic acidosis;

· or hyperpyrexia (extremely high body temperature);

· respiratory: hyperventilation, nicardipine pulmonary edema, respiratory depression, apnea;

· disorders of the cardiovascular system: arrhythmias, lowering blood pressure, depression of cardiac activity, collapse;

· violations of water-electrolyte balance: dehydration, impaired renal function taiguli until the development of renal failure, characterized by hypokalemia, with hypernatremia, hyponatremia;

· violation of the metabolism of glucose: hyperglycemia, hypoglycemia (especially in children), ketoacidosis;

· noise in the ears, deafness;

· gastrointestinal bleeding;

· hematologic disorders: from the inhibition of platelet aggregation to coagulopathy, prolongation of prothrombin time, hypoprothrombinemia;

· neurological disorders: toxic encephalopathy and inhibition of the function 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 (indicated at salicylate levels above 500 mg/l, provided by intravenous infusion of sodium bicarbonate – 88 meq in 1 liter of 5% glucose solution, at a rate of 10-15 ml/kg/h), restoration of circulating blood volume and induction of diuresis (achieved by use of sodium bicarbonate in the same dose and dilution, repeated 2-3 times); keep in mind that intensive fluid infusions in elderly patients can lead to pulmonary edema.

It is not recommended to use acetosolamide for alkalinization of urine (it can cause acidemia and increase the toxic effect of salicylates).

When performing alkaline diuresis, it is necessary to achieve pH values between 7.5 and 8. Hemodialysis is indicated if the level of salicylates in blood plasma is more than 1000 mg/l, and in patients with chronic poisoning-500 mg/l or lower if there are indications (refractory acidosis, progressive deterioration of the condition, severe damage to the central nervous system, pulmonary edema and renal failure).

With pulmonary edema, artificial ventilation of the lungs with a mixture enriched with oxygen is indicated in the positive pressure mode at the end of exhalation; hyperventilation and osmotic diuresis are used to treat brain edema.

The greatest risk of developing chronic intoxication is observed in the elderly when taking 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 content of salicylates in blood plasma.

Special instructions

The drug should be used as directed by a doctor.

Acetylsalicylic acid can provoke bronchospasm, as well as cause asthma attacks and other hypersensitivity reactions. Risk factors include a history of bronchial asthma, allergic conditions, hay fever, nasal polyposis, chronic respiratory diseases, and allergic reactions to other medications (for example, skin reactions, pruritus, urticaria).

Acetylsalicylic acid can cause bleeding of varying severity during and after surgery. A few days before the planned surgical intervention, the risk of bleeding should be evaluated in comparison with the risk of ischemic complications in patients taking low doses of acetylsalicylic acid.

If the risk of bleeding is significant, acetylsalicylic acid should be temporarily discontinued.

The combination of acetylsalicylic acid with anticoagulants, thrombolytics and antiplatelet drugs is associated with an increased risk of bleeding.

Acetylsalicylic acid in low doses can provoke the development of gout in predisposed patients (with reduced uric acid excretion).

Caution should be exercised when using the drug in patients with hepatic insufficiency (Child-Pugh class A), with renal insufficiency (creatinine clearance greater than 30 ml / min).

The combination of acetylsalicylic acid with methotrexate is accompanied by an increased frequency of side effects from the hematopoietic system.

High doses of acetylsalicylic acid have a hypoglycemic effect, which should be taken into account when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents for oral use (sulfonylureas) and insulin.

With the combined use of systemic glucocorticosteroids and salicylates, it should be remembered that during treatment, the concentration of salicylates in the blood is reduced, and after the withdrawal 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 diseases: when used simultaneously 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.

Caution should be exercised when concomitantly taking the drug with narcotic analgesics, NSAIDs and salicylic acid derivatives in large doses.

Increasing the dose of acetylsalicylic acid above therapeutic doses is associated with the risk of gastrointestinal bleeding.

Caution should be exercised when using the drug if there is a history of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding.

When taking long-term low-dose acetylsalicylic acid as antiplatelet therapy, caution should be exercised in elderly patients due to the risk of gastrointestinal bleeding.

Caution should be exercised when using the drug concomitantly with digoxin (due to a decrease in its renal excretion), valproic acid (due to its displacement from binding to plasma proteins), lithium preparations (due to an increase in their concentration in blood plasma), sulfonamides, carbonic anhydrase inhibitors, selective serotonin reuptake inhibitors.

Concomitant use of acetylsalicylic acid with alcohol increases the risk of damage to the gastrointestinal mucosa and prolongation of bleeding time.

With prolonged use of the drug, a general blood test and a fecal occult blood test should be performed periodically.

Influence on the ability to drive vehicles and mechanisms

During treatment with acetylsalicylic acid preparations, care should be taken when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets 75 mg +15.20 mg.

30 or 100 tablets in dark (amber) glass jars, sealed with a white screw-on lid (made of polyethylene) with a removable capsule with silica gel and a ring that provides control of the first opening.

1 jar of dark (amber) glass together with the instructions for use is placed in a pack of cardboard.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

: Acetylsalicylic acid, [Magnesium hydroxide]

Dosage form

Tablets

Purpose

For adults

Indications

Prevention of heart attacks and strokes, Prevention of thrombosis