Thrombital (Acetylsalicylic acid + Magnesium hydroxide)

Instructions for Thrombital (Acetylsalicylic acid + Magnesium hydroxide)

Thrombital is an antiplatelet agent. 

Release form and composition:

The drug is produced in the form of film-coated tablets: biconvex, round, film shell and a core on a cross section of almost white or white [30 or 100 pcs. in a dark (amber) glass jar, sealed with a white polyethylene screw cap with a built-in removable capsule with silica gel and a ring providing control of the first opening; in a cardboard box 1 can and instructions for the use of Trombital].

1 tablet contains: active substances: acetylsalicylic acid - 75 mg, magnesium hydroxide - 15.2 mg; additional substances: potato starch, microcrystalline cellulose, corn starch, magnesium stearate; film shell: macrogol (polyglycol 4000), hypromellose (hydroxypropyl methylcellulose 15 cps), talc. Pharmacological properties 

Pharmacodynamics Thrombital:

Thrombital is a combined inhibitor of platelet aggregation.

The drug, as a result of suppression of thromboxane A 2 production in platelets, reduces aggregation, platelet adhesion and thrombus formation. After a single dose, the antiplatelet effect of the drug is observed for 7 days (in men, the effect is more pronounced than in women). Against the background of unstable angina pectoris, acetylsalicylic acid reduces mortality and the threat of myocardial infarction, it also demonstrates effectiveness in the primary prevention of cardiovascular lesions, mainly myocardial infarction in men after 40 years, and shows a good result in the secondary prevention of myocardial infarction. This active substance in the liver inhibits the production of prothrombin, contributes to an increase in prothrombin time, an increase in the fibrinolytic activity of blood plasma and a decrease in the level of vitamin K-dependent coagulation factors - II, VII, IX and X.

During surgical interventions, the active ingredient increases the risk of hemorrhagic complications, against the background of combined use with anticoagulants increases the likelihood of bleeding. When used in high doses, acetylsalicylic acid also exhibits anti-inflammatory, analgesic and antipyretic effects, activates the excretion of uric acid (disrupting the process of its reabsorption in the renal tubules). In the gastric mucosa, the blockade of cyclooxygenase-1 (COX-1) causes inhibition of gastroprotective prostaglandins, which can lead to ulceration of the mucous membrane and further development of bleeding. The magnesium hydroxide included in Trombital protects the mucous membrane of the gastrointestinal tract (GIT) from the negative effects of acetylsalicylic acid. 

Thrombital Pharmacokinetics:

Acetylsalicylic acid is almost completely absorbed from the gastrointestinal tract. The half-life (T ½ ) of the active substance is approximately 15 minutes, since under the action of enzymes it is rapidly hydrolyzed to salicylic acid in the blood plasma, liver and intestines. For salicylic acid, T ½ is approximately 3 hours, but can increase significantly with the simultaneous use of high doses (more than 3 g) of acetylsalicylic acid due to saturation of enzyme systems. The bioavailability of acetylsalicylic acid is 70%, but this value can fluctuate significantly, due to the fact that the active substance is metabolized by presystemic hydrolysis (liver, gastrointestinal mucosa) with the participation of enzymes into salicylic acid, the bioavailability of which is 80-100%. The applied doses of magnesium hydroxide do not affect the bioavailability of acetylsalicylic acid. 

Indications for use Thrombital:

primary prevention of cardiovascular lesions, including thrombosis and acute heart failure with existing risk factors (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking, obesity, old age);
prevention of blood vessel thrombosis and repeated myocardial infarction; prevention of thromboembolism after surgical interventions on the vessels, such as coronary artery bypass grafting, percutaneous transluminal coronary angioplasty; unstable angina. 

Thrombital Contraindications:

Absolute: gastrointestinal bleeding, erosive and ulcerative lesions of the gastrointestinal tract during an exacerbation; hemorrhage in the brain; chronic heart failure III – IV functional class according to NYHA classification (New York Association of Cardiologists); partial or complete combination of recurrent polyposis rhinosinusitis and bronchial asthma with intolerance to acetylsalicylic acid or any other non-steroidal anti-inflammatory drugs (NSAIDs), including cyclooxygenase-2 (COX-2) inhibitors, including indications in history; bronchial asthma due to the intake of salicylates and other NSAIDs; predisposition to bleeding (hemorrhagic diathesis, thrombocytopenia, vitamin K deficiency); renal failure of severe degree with creatinine clearance (CC) below 30 ml / min; severe hepatic impairment (Child-Pugh grades B and C); deficiency of glucose-6-phosphate dehydrogenase; I and III trimesters of pregnancy and lactation; concomitant use of methotrexate at a dose of 15 mg per week and above; age under 18; hypersensitivity to any of the constituents of the drug and other NSAIDs. Relative (take Trombital tablets with extreme caution): history of gastrointestinal bleeding or erosive and ulcerative gastrointestinal defects; impaired renal function (CC above 30 ml / min); liver failure (class A on the Child-Pugh scale); diabetes; chronic respiratory diseases, bronchial asthma, nasal polyposis, hay fever, allergic conditions, drug allergies, including in the form of skin reactions, itching, urticaria (since acetylsalicylic acid can lead to bronchospasm, as well as provoke attacks of bronchial asthma or development of other hypersensitivity reactions); gout, hyperuricemia, since acetylsalicylic acid, taken in small doses, reduces the excretion of uric acid; II trimester of pregnancy; the proposed surgical intervention (including such a minor one as tooth extraction), since Trombital can cause bleeding for several days after taking it; elderly age; combined administration with the following drugs: NSAIDs and salicylic acid derivatives in high doses, digoxin, valproic acid, anticoagulants, antiplatelet / thrombolytic agents, methotrexate at a dose below 15 mg per week, insulin and oral hypoglycemic agents (sulfonylurea derivatives), selective seizure of serotonin, ethanol (including ethanol-containing drinks), ibuprofen, systemic glucocorticosteroids (GCS), lithium preparations, carbonic anhydrase inhibitors, sulfonamides, narcotic analgesics.

method and dosage:

 Trombital tablets are taken orally with water, 1 time per day. If you find it difficult to swallow the whole tablet, you can chew it or crush it into powder beforehand. Recommended dosage regimen of Trombital: cardiovascular diseases, including thrombosis and acute heart failure with existing risk factors for primary prevention: on the first day - 2 tablets, then 1 tablet per day; thromboembolism after surgical interventions on the vessels, repeated myocardial infarction and blood vessel thrombosis for the purpose of prevention:
in a daily dose of 1-2 tablets; unstable angina pectoris: in a daily dose of 1-2 tablets; for faster absorption, it is recommended to chew the first tablet of the drug. Thrombital is intended for long-term use, the dose of the drug and the duration of therapy are determined by the attending physician. It is required to take the drug only in the above doses, in accordance with the indications.