Thrombopol - instructions for use, doses, side effects, contraindications

Sheath: hypromellose, acryl-ayz (mixture to cover tablets): methacrylic acid copolymer type C, talc, titanium dioxide, triethyl citrate, dye crimson [Ponso 4R], silicon dioxide colloid, sodium hydrogen carbonate, sodium lauryl sulfate.

Description:

The tablets covered with an enteric coating, pink color, round, biconcave.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).

ATX: & nbsp

N.02.B.A Salicylic acid and its derivatives

Pharmacodynamics:

The mechanism of antiplatelet action of acetylsalicylic acid is irreversible inhibition of cyclooxygenase (COX-1), which blocks the synthesis of thromboxane A 2 and inhibits platelet aggregation.Antiaggregant effect develops even after application of small doses of the drug and persists for 7 days after a single dose. These properties of acetylsalicylic acid are used in the prevention and treatment of myocardial infarction, ischemic heart disease, complications of varicose veins.

Acetylsalicylic acid (ASA) also has anti-inflammatory, antipyretic and analgesic effects.

Tablets THROMBOPOL ® have an enteric coating, due to which they dissolve and release the active substance in a more alkaline medium of the duodenum, reducing the irritating effect of acetylsalicylic acid on the gastric mucosa.

Pharmacokinetics:

Absorption acetylsalicylic acid from tablets covered with an enteric-coated shell begins 3-4 hours after the administration of the drug, confirming that the membrane effectively blocks dissolution of the drug in the stomach.

The maximum concentration in plasma is observed after about 2-3 hours and averages 12.7 μg / ml for tablets of 150 mg and 6.72 μg / ml for tablets of 75 mg.

The presence of food in the gastrointestinal tract slows the absorption of the drug.

System Absorption Rate (AUC) is 56.42 μg x hour / ml for tablets 75 mg and 108.08 μg x hour / ml for tablets of 150 mg.

Distribution

Acetylsalicylic acid quickly and largely penetrates into most tissues and body fluids.

The relative distribution is about 0.15-0.2 l / kg and increases with the concentration of the drug in the blood serum. The degree of communication of the drug with plasma proteins depends on the concentration; in healthy individuals decreases simultaneously with a decrease in this concentration.

In renal failure, in pregnancy and in newborns, salicylates can displace bilirubin from bonding with albumin and promote the development of bilirubin encephalopathy.

Metabolism

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

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

Excretion

The half-life (T1 / 2) of acetylsalicylic acid from the blood plasma is about 15-20 minutes.

Unlike other salicylates, with repeated administration of the drug, unhydrolyzed acetylsalicylic acid does not accumulate in the blood serum. Only 1% of the ingested dose of acetylsalicylic acid is excreted by the kidneys in the form of unhydrolyzed acetylsalicylic acid, the rest is excreted as salicylates and their metabolites.

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

Indications:

- Prevention of acute myocardial infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, old age) and repeated myocardial infarction;

- unstable angina;

- prevention of stroke (including, in patients with transient impairment of cerebral circulation);

- prophylaxis of transient impairment of cerebral circulation;

- prevention of thromboembolism after surgery and invasive vascular interventions (eg, coronary artery bypass grafting, carotid endarterectomy, arteriovenous shunting, carotid angioplasty);

- prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches (including, with prolonged immobilization as a result of extensive surgical intervention).

Contraindications:

- Hypersensitivity to acetylsalicylic acid, excipients and other NSAIDs;

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

- gastrointestinal bleeding;

- hemorrhagic diathesis;

- The bronchial asthma, induced by the intake of salicylates and NSAIDs; a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and ASA intolerance;

- combined use with methotrexate at a dose of 15 mg per week or more;

- pregnancy (I and III trimester) and lactation;

- age to 18 years.

Carefully:With gout, hyperuricemia, peptic ulcer and duodenal ulcer or gastrointestinal hemorrhage (in the anamnesis), renal / hepatic insufficiency, bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergy, simultaneous taking of methotrexate in a dose less than 15 mg / week, concomitant anticoagulant therapy, pregnancy (II trimester).

Pregnancy and lactation:

Application in pregnancy

The use of salicylates in the first trimester of pregnancy leads to the development of cleavage of the upper palate, heart defects; in the III trimester 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 infants - the use of salicylates in these trimesters is contraindicated.

In the second trimester of pregnancy, salicylates can be administered only in the light of a strict assessment of the risk and benefit.

Application during lactation

Salicylates and their metabolites penetrate into breast milk in small amounts. The accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in the child and does not require the cessation of breastfeeding. However, with prolonged use of the drug or its administration in a high dose, breast-feeding should be stopped immediately.

Dosing and Administration:

Tablets should be taken regardless of food intake, without chewing, squeezed with a small amount of water.

The drug is intended for long-term use. The duration of therapy is determined by the doctor.

Preventive maintenance at suspicion of an acute myocardial infarction:

75 mg or 150 mg per day.

Prevention of the first acute acute myocardial infarction in the presence of risk factors:

75 mg or 150 mg per day.

Prevention of repeated myocardial infarction. Unstable angina. Prevention of stroke and transient disorders of cerebral circulation. Prevention of thromboembolic complications after surgery or invasive examinations:

75 mg or 150 mg per day.

Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches:

75 mg or 150 mg per day.

Side effects:

Gastrointestinal tract: nausea, heartburn, vomiting, abdominal pain, diarrhea, ulcers of the mucous membrane of the stomach and duodenum, including perforating, gastrointestinal bleeding, increased activity of "liver" enzymes.

Respiratory system: bronchospasm.

Central nervous system: dizziness, noise in the ears.

The system of hematopoiesis: increased bleeding, anemia (rarely).

Allergic reactions: urticaria, angioedema.

Overdose:

The first symptoms of an overdose of acetylsalicylic acid are: nausea, vomiting, tinnitus and rapid breathing.

Symptoms such as hearing loss, visual impairment, headaches, motor agitation, drowsiness, convulsions, hyperthermia can also be observed. In severe intoxication, an acid-base and water-electrolyte balance can be disturbed (metabolic acidosis and dehydration).

Symptoms of mild to moderate intoxication develop after the use of acetylsalicylic acid in a dose of 150-300 mg / kg. Symptoms of severe overdose develop at a dose of 300-500 mg / kg. The potentially fatal dose of ASA is more than 500 mg / kg.

Treatment: there is no specific antidote.

In case of an overdose of acetylsalicylic acid it is necessary:

-to induce vomiting and rinse the stomach (in order 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 a very large dose - up to 10 hours;

- To reduce the absorption of ASA, 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 closely monitor the violation of the water-electrolyte balance and replenish it;

-to accelerate the excretion of ASA through the kidneys and in the treatment of acidosis it is necessary to inject sodium bicarbonate intravenously. It is necessary to keep the pH between 7.0 and 7.5; -with very severe intoxication, hemodialysis or peritoneal dialysis is necessary;

- In connection with the possibility of developing respiratory acidosis, it is forbidden to take drugs that depress the central nervous system, for example, barbiturates;

Patients with respiratory failure should ensure airway patency and oxygen access. If necessary, perform intratracheal intubation and provide artificial ventilation.

Interaction:

With simultaneous application ASK enhances action following medicines:

- methotrexate, by reducing renal clearance and displacing it from the bond with proteins;

- heparin and indirect anticoagulants, due to disruption of platelet function and displacement of indirect anticoagulants from binding to proteins;

- thrombolytic agents and platelet aggregation inhibitors (ticlopidine);

- digoxin, due to a decrease in its renal excretion;

- hypoglycemic agents (insulin and sulfonylurea derivatives), due to hypoglycemic properties of ASA itself at high doses and displacement of sulfonylurea derivatives from binding to proteins;

- valproic acid, due to the displacement of its bond with proteins;

- NSAIDs;

- sulfonamides (including co-trimoxazole);

- barbiturates;

- lithium compounds.

Additive effect is observed with simultaneous reception of ASA with alcohol.

ASA weakens the effect:

- anti-gouty drugs that increase the secretion of uric acid (probenecid, sulfinpyrazone, benzbromarone), due to competitive tubular elimination of uric acid;

- antihypertensive agents, including angiotensin-converting enzyme inhibitors;

- antagonists of aldosterone (eg, spironolactone);

- "loop" diuretics (for example, furosemide);

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

Special instructions:

ASA 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).

ASA can cause bleeding of varying severity during and after surgical interventions. The drug should be discontinued 5-7 days before the proposed operation.

The combination of ASA with anticoagulants, thrombolytic drugs and inhibitors of platelet aggregation is accompanied by an increased risk of bleeding.

ASA in low doses can provoke the development of gout in predisposed individuals (having a decreased excretion of uric acid).

The combination of ASA with methotrexate is accompanied by an increased incidence of side effects from the hematopoiesis.

High doses of ASA have a hypoglycemic effect, which must be borne in mind when prescribing it to patients with diabetes mellitus receiving hypoglycemic agents.

When combined glucocorticosteroids (glucocorticosteroids) and salicylates should be remembered that during treatment, the level of salicylates in the blood is lowered, and after overtreatment of SCS, an overdose of salicylates is possible.

The combination of ASA with ibuprofen is not recommended, as it reduces the effectiveness of the THROMBOPOL® preparation and, as a result, can reduce life expectancy. Excess dose of ASA is associated with a risk of gastrointestinal bleeding.

When combined with ASA and ethanol, the risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of bleeding time are increased.

Overdose is especially dangerous in the elderly. Patients over 65 years of age due to decreased efficiency of the kidneys and more frequent occurrence of adverse reactions from the gastrointestinal tract should take ASA in smaller doses.

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

Data on the negative impact on the ability to drive a car or work with mechanisms there.

Form release / dosage:Tablets coated with enteric coating, 75 mg or 150 mg.

Packaging:Tablets of 75 mg: 10 or 25 tablets per blister of PVC / Al-foil. For 2 blisters (25 tablets) or 3, 5, 6 blisters (10 tablets) with instructions for medical use in a cardboard box.

Tablets of 150 mg: 10 tablets per blister of PVC / Al-foil. For 3, 5 or 6 blisters with instructions for medical use in a cardboard pack

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-006548/09

Date of registration:17.08.2009

The owner of the registration certificate:Pharmaceutical factory "POLFARMA" JSCPharmaceutical factory "POLFARMA" JSC Poland

Manufacturer: & nbsp

POLPHARMA, S.A. Poland

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp17.11.2019

Illustrated instructions

Instructions

Thrombopol® (Trombopol®)