Trombopol, pills 75 mg, 30 pcs.

Composition

1 tablet, coated with an enteric coating, contains:

Active ingredient:

acetylsalicylic acid 75 mg

. excipients:

corn starch,

microcrystalline cellulose,

sodium carboxymethyl starch.

shell composition:

hypromellose, Acryl-Aiz (tablet coating mixture): methacrylic acid copolymer type C, talc, titanium dioxide, triethyl citrate, red dye (Ponceau 4R), colloidal silicon dioxide, sodium bicarbonate, sodium lauryl sulfate.

Pharmacological action

Trombopol – NSAIDs, antiplatelet agent. The mechanism of action of acetylsalicylic acid is based on irreversible inhibition of COX-1, resulting in a blockage of thromboxane A2 synthesis and suppression of platelet aggregation. The antiplatelet effect develops even after using the drug in small doses and persists for 7 days after a single dose. Due to these properties, acetylsalicylic acid is used for the prevention and treatment of myocardial infarction, coronary heart disease, complications of varicose veins. Acetylsalicylic acid also has anti-inflammatory, analgesic, and antipyretic effects.

Trombopol tablets have an enteric coating, thanks to which they dissolve and secrete the Active ingredient in a more alkaline environment of the duodenum, reducing the irritating effect of acetylsalicylic acid on the gastric mucosa.

Pharmacokinetics

Suction

Absorption of acetylsalicylic acid from enteric coated tablets begins 3-4 hours after taking the drug, confirming that the shell effectively blocks the dissolution of the drug in the stomach. _Cmax in plasma is reached after approximately 2-3 hours and averages 12.7 mcg / ml for 150 mg tablets and 6.72 mcg / ml for 75 mg tablets. The presence of food in the gastrointestinal tract slows down the absorption of the drug.

The AUC is 56.42 mcg×h / ml for 75 mg tablets and 108.08 mcg×h/ml for 150 mg tablets.

Distribution

Acetylsalicylic acid quickly and largely penetrates most tissues and body fluids. The degree of binding of the drug to plasma proteins depends on the concentration; in healthy individuals, it decreases simultaneously with a decrease in this concentration.

The relative distribution is about 0.15-0.2 l / kg and increases simultaneously with an increase in the concentration of the drug in the blood serum.

Unlike other salicylates, with repeated administration of the drug, non-hydrolyzed acetylsalicylic acid does not accumulate in the blood serum.

Metabolism

Acetylsalicylic acid is partially metabolized during absorption. This process occurs under the influence of enzymes, mainly in the liver, with the formation of metabolites such as phenylsalicylate, glucuronide salicylate and salicyluric acid, found in many tissues and urine.

The elimination

of T_1/2 acetylsalicylic acid from the blood plasma is about 15-20 minutes.

Only 1% of the oral dose of acetylsalicylic acid is excreted by the kidneys as non-hydrolyzed acetylsalicylic acid, the rest is excreted as salicylates and their metabolites.

In patients with normal renal function,80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours

. Pharmacokinetics in special clinical cases

In renal failure, pregnancy, and newborns, salicylates can displace bilirubin from binding to albumin and contribute to the development of bilirubin encephalopathy.

In women, the metabolic process is slower (less activity of enzymes in the blood serum).

Indications

• Prevention of acute myocardial infarction in the presence of risk factors (for example, diabetes mellitus, hyperlipidemia, arterial hypertension, obesity, smoking, old age) and recurrent myocardial infarction.
• Unstable angina pectoris.
• Prevention of stroke (including in patients with transient cerebral circulatory disorders).
• Prevention of transient cerebral circulatory disorders.
• Prevention of thromboembolism after surgery and invasive vascular interventions (for example, coronary artery bypass grafting, carotid artery endarterectomy, arteriovenous bypass grafting, carotid artery angioplasty).
• Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches (including long-term immobilization as a result of extensive surgical intervention).

Use during pregnancy and lactation

The use of the drug Trombopol in the first and third trimesters of pregnancy and lactation is contraindicated. The use of salicylates in the first trimester of pregnancy leads to the development of cleavage of the upper palate, heart defects; in the third trimester, it causes inhibition of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in premature babies.

In the second trimester of pregnancy, salicylates can be prescribed only after a strict assessment of the expected benefit of therapy for the mother and the potential risk to the fetus. Salicylates and their metabolites are excreted in small amounts in breast milk. Accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in the child and does not require discontinuation of breastfeeding. However, if the drug is used for a long time or is prescribed in a high dose, breastfeeding should be stopped immediately.

Contraindications

• erosive and ulcerative lesions of the gastrointestinal tract in acute phase;
• gastrointestinal bleeding;
• bleeding diathesis;
• bronchial asthma induced by ingestion of salicylates and NSAIDs;
• the combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid;
• concomitant use with methotrexate at a dose of 15 mg per week or more;
• I and III trimester of pregnancy;
• lactation (breastfeeding);
• age to 18 years;
• hypersensitivity to the components of the drug Tromboon;
• hypersensitivity to other NSAIDs.

With caution, the drug should be used for gout, hyperuricemia, peptic ulcer of the stomach and duodenum or gastrointestinal bleeding (in the anamnesis), renal / hepatic insufficiency, bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergies, while taking methotrexate at a dose of less than 15 mg / week, concomitant therapy with anticoagulants, in the second trimester of pregnancy.

Side effects

From the digestive system: nausea, vomiting, heartburn, abdominal pain, diarrhea, ulcers of the gastric and duodenal mucosa, including perforated, gastrointestinal bleeding, increased activity of liver enzymes.

From the respiratory system: bronchospasm.

From the central nervous system: dizziness, tinnitus.

From the hematopoietic system: increased bleeding; rarely-anemia.

Allergic reactions: urticaria, angioedema.

Interaction

When used concomitantly, acetylsalicylic acid enhances the effect of methotrexate by reducing renal clearance and displacing it from protein binding; heparin and indirect anticoagulants by disrupting platelet function and displacing indirect anticoagulants from protein binding; thrombolytic drugs and platelet aggregation inhibitors (ticlopidine); digoxin, due to a decrease in its renal excretion; hypoglycemic agents (insulin and sulfonylurea derivatives) due to the hypoglycemic properties of acetylsalicylic acid itself in high doses and the displacement of sulfonylurea derivatives from the bond with proteins; valproic acid due to the displacement of its bond with proteins; NSAIDs; sulfonamides (including co-trimoxazole); barbiturates; lithium salts.

An additive effect is observed when taking acetylsalicylic acid with alcohol at the same time.

Acetylsalicylic acid reduces the effect of anti-gouty drugs that increase the excretion of uric acid (probenecid, sulfinpyrazone, benzbromarone), due to competitive tubular elimination of uric acid; antihypertensive agents, including ACE inhibitors; aldosterone antagonists (for example, spironolactone); “loop” diuretics (for example, furosemide).

Increasing the elimination of salicylates, corticosteroids for systemic use weaken their effect.

The combination of acetylsalicylic acid with anticoagulants, thrombolytic drugs and platelet aggregation inhibitors is associated with an increased risk of bleeding.

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

How to take it, course of administration and dosage

The drug is intended for long-term use. The duration of therapy is determined by the doctor. Tablets are taken orally, regardless of food intake, without chewing, with a small amount of water. For the purpose of prevention in case of suspected acute myocardial infarction: appoint 75 mg per day or 150 mg per day. In order to prevent the first acute myocardial infarction in the presence of risk factors: appoint 75 mg per day or 150 mg per day. For the prevention of recurrent myocardial infarction, unstable angina, for the prevention of stroke and transient cerebral circulatory disorders, for the prevention of thromboembolic complications after surgery or invasive research: 75 mg per day or 150 mg per day is prescribed.In order to prevent deep vein thrombosis and thromboembolism of the pulmonary artery and its branches: appoint 75 mg per day or 150 mg per day.

Overdose

Symptoms: The first symptoms are nausea, vomiting, tinnitus, and rapid breathing. Hearing loss, visual disturbances, headaches, motor agitation, drowsiness, seizures, and hyperthermia are also possible. With severe intoxication, it is possible to develop a violation of the acid-base and water-electrolyte balance (metabolic acidosis and dehydration). Symptoms of mild to moderate intoxication develop after the use of acetylsalicylic acid at a dose of 150-300 mg / kg. Symptoms of severe overdose develop at a dose of 300-500 mg / kg. The potentially lethal dose of acetylsalicylic acid is more than 500 mg / kg.

Treatment: induce vomiting and flush the stomach (to reduce absorption of the drug). Such actions give an effect within 3-4 hours after taking the drug, and in the case of taking it in an excessive dose-up to 10 hours. To reduce the absorption of acetylsalicylic acid, it is necessary to take activated carbon in the form of an aqueous suspension (dose for adults – 50-100 g, for children-30-60 g); it is necessary to carefully monitor the violation of the water-electrolyte balance and replenish it. In order to accelerate the elimination of acetylsalicylic acid by the kidneys and in the treatment of acidosis, it is necessary to inject sodium bicarbonate intravenously. It is necessary to maintain the pH in the range of 7.0-7.5. In case of very severe intoxication, hemodialysis or peritoneal dialysis should be performed. Due to the possibility of developing respiratory acidosis, it is forbidden to take drugs that depress the central nervous system, for example, barbiturates. Patients with respiratory disorders should be provided with airway patency and oxygen access. If necessary, perform an intratracheal intubation and provide mechanical ventilation. There is no specific antidote.

Special instructions

Acetylsalicylic acid can provoke bronchospasm, as well as cause asthma attacks and other hypersensitivity reactions. Risk factors include a history of bronchial asthma, hay fever, nasal polyposis, chronic respiratory diseases, and allergic reactions to other medications (for example, skin reactions, pruritus, and urticaria). Acetylsalicylic acid can cause bleeding of varying severity during and after surgery. The drug should be discontinued 5-7 days before the intended operation.

Acetylsalicylic acid in low doses can provoke the development of gout in predisposed individuals (with reduced uric acid excretion). Acetylsalicylic acid in high doses has a hypoglycemic effect, which should be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents.

It should be borne in mind that with the combined administration of corticosteroids and salicylates, the concentration of salicylates in the blood decreases, and after the withdrawal of corticosteroids, an overdose of salicylates is possible. It is not recommended to combine the drug Trombopol with ibuprofen, because the latter reduces the effectiveness of acetylsalicylic acid. Exceeding the dose of acetylsalicylic acid is associated with the risk of gastrointestinal bleeding. When acetylsalicylic acid is combined with ethanol, the risk of damage to the gastrointestinal mucosa and prolongation of bleeding time is increased.

Overdose is especially dangerous in the elderly. Patients over 65 years of age should be given lower doses of Thrombopol due to impaired renal function and more frequent occurrence of adverse reactions from the digestive system.

Influence on the ability to drive motor vehicles and manage mechanisms.

There are no data on the negative effects of the drug Trombopol on the ability to drive vehicles or work with mechanisms.

Form of production

Enteric coated tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Acetylsalicylic acid

Dosage form

Tablets

Purpose

For adults

Indications

Prevention of heart attacks and strokes, Prevention of thrombosis, Cerebrovascular

accident Weight

Weight: 16 gr.