ASK-cardio (Acetylsalicylic acid) 100mg 30 tablets

Composition per 1 tablet: 

Active ingredient: 100 mg acetylsalicylic acid,

Excipients:

core: lactose monohydrate (milk sugar) 15.87 mg, povidone (polyvinylpyrrolidone), 0.16 mg, 3.57 mg of potato starch, talc, 0.2 mg, 0.2 mg of stearic acid,

sheath: methacrylic acid-ethacrylate copolymer [1: 1] (100 kolikoat MAE) 4.186 mg macrogol 6000 (high molecular polyethylene) 0.558 mg Talc 1.117 mg Titanium dioxide 0.139 mg.

Pharmacotherapeutic group: antiplatelet agent.

pharmacodynamics

Acetylsalicylic acid (ASA) is a salicylic acid ester, refers to the group of nonsteroidal anti-inflammatory drugs (NSAIDs). The mechanism of action is based on the irreversible inactivation of the enzyme cyclooxygenase (COX-1), resulting in the synthesis of prostaglandins is blocked, prostacyclin and thromboxane. Reduces aggregation, platelet adhesion and thrombus formation by inhibiting the synthesis of thromboxane A2 in platelets. Increases of plasma fibrinolytic activity and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Antiplatelet effect develops after applying small doses and stored for 7 days after a single dose. These properties of ASA used in the prevention and treatment of myocardial infarction, coronary heart disease, complications of varicose veins. ASA also has anti-inflammatory, antipyretic and analgesic effect.

Pharmacokinetics

After oral administration ASA is rapidly and completely absorbed from the gastrointestinal tract (GIT). ASA partially metabolized during absorption. During and after the suction head turns into ASA metabolite – salicylic acid, which is metabolized primarily in the liver by the enzymes to form metabolites such as phenyl salicylate, and salicylate glucuronide salitsilurovaya acid, found in many tissues and urine. In women, the process of metabolism is slower (lower activity in serum enzymes). The maximum concentration of ASA in the blood plasma achieved 10-20 minutes after ingestion, salicylic acid – after 0.3-2 hours. Because acid-coated tablet shell ASA is released not in the stomach (sheath effectively blocks the dissolution of the drug in the stomach) and in an alkaline environment of the duodenum. Thus, absorption of ASA in tablet form enteric-coated delayed for 3-6 hours as compared with conventional (without a shell) tablets.

Salicylic acid ASA and strongly bind to plasma proteins (66% to 98% depending on the dose) and rapidly distributed in the organism. Salicylic acid crosses the placenta and is secreted in breast milk.

Excretion of salicylic acid is dose-dependent, since its metabolism may limit enzyme system. half-life is 2-3 hours when applied at low doses of ASA and 15 hours when using the drug in high dose (usual dose of acetylsalicylic acid as an analgesic). Unlike other salicylates, when multiple dose ASA negidrolizirovannaya drug does not accumulate in the serum. Salicylic acid and its metabolites are excreted by the kidneys. In patients with normal renal function 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours.

Indications for use

• Unstable angina pectoris,
• Prevention of acute myocardial infarction in the presence of risk factors (eg, diabetes mellitus, hyperlipidemia, hypertension, obesity, smoking, older age) and reinfarction,
• Prevention of stroke (including patients with transient ischemic attack)
• Prevention of transient ischemic attacks,
• Prevention of thromboembolism after surgery and invasive procedures on vessels (eg, coronary artery bypass grafting, carotid endarterectomy, arterio-venous bypass, angioplasty of the carotid arteries)
• Prevention of deep vein thrombosis and pulmonary thromboembolism and its branches (for example, long-term immobilization due to surgery large).

Contraindications for use

• Hypersensitivity to acetylsalicylic acid (ASA), to excipients of the drug and other nonsteroidal anti-inflammatory drugs (NSAIDs)
• Gastrointestinal bleeding,
• Asthma induced by intake of salicylates and NSAIDs, a combination of asthma, recurrent nasal polyposis, and paranasal sinuses and intolerances ASA
• Hemorrhagic diathesis (hemophilia, von Willebrand disease, telangiectasia, hypoproteinemia, thrombocytopenia, thrombocytopenic purpura)
• The combined use with methotrexate 15 mg per week or more,
• Pregnancy (I and IIItrimestr) and lactation,
• The age of 18,
• Severe renal insufficiency (creatinine clearance (CC) of less than 30 ml / min)
• Severe hepatic impairment (class B or higher on the scale of Child-Pugh)
• Chronic heart failure III-IVfunktsionalnogo class NYHA classification,
• Lactose intolerance, lactase deficiency and glucose-galactose malabsorption.

Be wary appoint patsientams gout, hyperuricemia, with a history of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding, renal failure (creatinine clearance 30 mL / min), liver failure (below class B on a scale Child-Pugh), asthma , chronic respiratory disease, hay fever, nasal polyposis, drug allergy, including the group of NSAIDs (analgesics, anti-inflammatory, antirheumatic drugs), in IItrimestre pregnancy, vitamin K deficiency, in severe deficiency of glucose-6-phosphate dehydrogenase, assuming a surgical intervention (including minor, for example, tooth extraction), the combined use of the following drugs (methotrexate at a dose less than 15 mg per week, anticoagulant, thrombolytic and antiplatelet agents, NSAIDs, ibuprofen, salicylic acid derivatives in high doses, with digoxin with hypoglycemic agents for oral use (sulfonylurea derivatives) and insulin, valproic acid with alcohol, with selective serotonin reuptake inhibitors).

Use during pregnancy and breast-feeding

The use of high doses of salatsilatov in the first 3 months of pregnancy is associated with an increased rate of fetal defects (cleft palate, heart defects). In IItrimestre pregnancy salicylates can be given only on the basis of strict risk assessment and benefit.

In the last trimester of pregnancy salicylates in high doses (more than 300 mg / day) caused a weakening of labor, premature closure of the ductus arteriosus in the fetus, increased bleeding in the mother and the fetus, and the appointment just before birth may cause intracranial hemorrhage, especially in preterm infants. Appointment of salicylates in the last trimester is contraindicated.

Salicylates and their metabolites in small amounts into breast milk. Accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in children and does not require stopping breastfeeding. However, long-term use of the drug or to appoint him to a high dose of breast-feeding should be discontinued immediately.

dosing regimen, the route of administration

ASK cardio should be taken orally, after meals, without chewing, drinking plenty of fluids.

ASK cardio as an antiplatelet agent for long-term use. The duration of therapy is determined by the attending physician. It recommends the following dosing regimen of the absence of other appointments:

Prophylaxis in cases of suspected acute myocardial miokardanachalnaya dose of 100-300 mg (first tablet must be chewed for faster absorption) should be prinyatapatsientom as soon as possible after suspected in the development of acute myocardial infarction. In the following 30 days after myocardial infarction should be maintained dose of 200-300 mg / day.

Prevention of new-onset acute myocardial infarction in the presence of factors riska100 mg / day or 300 mg every other day.

Prophylaxis of recurrent myocardial infarction. Unstable angina. Prevention of stroke and transient ischemic attack. Prevention of thromboembolism after surgery and invasive issledovaniy100-300 mg / day.

Prevention of deep vein thrombosis and pulmonary embolism and its vetvey100-200 mg / day or 300 mg every other day.

Side effect

From the digestive system: most frequently reported nausea, heartburn, vomiting, pain in the abdomen, rarely – a stomach ulcer and duodenal ulcer, including perforated, gastrointestinal hemorrhage, transient liver function abnormalities with increased activity of “liver” transaminases.

Since the cardiovascular system: rarely – increased symptoms of chronic heart failure, lower limb edema.

From hemopoiesis system: an increased incidence of perioperative (intraoperative and postoperative) hemorrhage, bruising, nosebleeds, bleeding gums, bleeding from the urinary tract. There are reports of serious cases of bleeding, which include gastrointestinal bleeding and bleeding in the brain (especially in patients with hypertension who have not reached the target blood pressure (BP) and / or receiving concomitant therapy with anticoagulant drugs), which in some cases may be wear life-threatening. Bleeding can lead to acute or chronic post-hemorrhagic / iron-deficiency anemia (eg due to hidden bleeding) with relevant clinical and laboratory symptoms (fatigue, pallor, hypoperfusion).

There are reports of hemolysis and hemolytic anemia in patients with severe deficiency of glucose-6-phosphate dehydrogenase.

From the urinary system: there are reports of cases of renal dysfunction and acute renal failure.

On the part of the central nervous system: dizziness, hearing loss, tinnitus, that could be a sign of overdose (see Overdose section.).

Allergic reactions: hypersensitivity reactions with respective laboratory and clinical signs, such as asthmatic syndrome (bronchospasm), the reaction mild to moderate side of the skin, respiratory tract, gastrointestinal tract and the cardiovascular system, including symptoms such as skin rash , kozhnyyzud, urticaria, angioedema, rhinitis, swelling of nasal mucosa, cardio-respiratory distress syndrome, and severe reactions, including anaphylactic shock.

Overdose

It may have serious consequences, especially in the elderly and in children. salitsilizma syndrome develops when taking ASA in a dose of 100 mg / kg / day for 2 days due to the use of toxic doses of the drug within the wrong therapeutic use (chronic poisoning) or single accidental or intentional receiving toxic dose of an adult or a child of the drug (acute) .

Symptoms of overdose:

• For mild to moderate severity (a single dose of less than 150 mg / kg):

Vertigo, tinnitus, hearing loss, increased sweating, nausea and vomiting, headache, confusion, tachypnea, hyperventilation, respiratory alkalosis.

Treatment: gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, restoring fluid and electrolyte balance and acid-base status.

• In moderate and severe degrees of severity (single dose of 150 mg / kg, 300 mg / kg – moderate, more than 300 mg / kg – severe degree of poisoning)

Respiratory alkalosis with compensatory metabolic acidosis, hyperpyrexia, hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, apnea, from cardio – vascular system: cardiac arrhythmias, marked reduction in blood pressure, depression of cardiac activity, with the water-electrolyte balance: dehydration, impaired function kidneys from oliguria up to the development of renal failure, characterized by hypokalemia, hypernatremia, hyponatremia, impaired glucose metabolism: hyperglycemia, hypoglycemia (especially in children), ketoacidosis, tinnitus, deafness, gastrointestinal hemorrhage, hematologic disorders, from inhibition of platelet aggregation to a coagulopathy, prolonged 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 administration of activated charcoal, forced alkaline diuresis, hemodialysis, restoring fluid and electrolyte balance and acid-base status, symptomatic therapy.

Interaction with other drugs

With simultaneous use of ASA enhances the effect of the following medicines, if needed simultaneous use of ASA with transfer of funds should consider the need to reduce the dose of drugs:

• Methotrexate, due to reduction in renal clearance and displacement of its association with proteins,
• While the use of an anticoagulant, thrombolytic and antiplatelet agents (ticlopidine, clopidogrel), there is an increase risk of bleeding as a result of synergies major therapeutic effects of the means employed,
• While the use of drugs that possess anticoagulant, thrombolytic and antiplatelet effects, there is a growing damaging effect on the mucous membrane of the gastrointestinal tract,
• Selective serotonin reuptake inhibitors, which may lead to increased risk of bleeding from the upper gastrointestinal tract (synergism with ASA)
• Digoxin, as a result of decrease in its renal excretion, which can lead to overdose,
• Hypoglycemic agents for oral use (sulfonylurea derivatives) and insulin hypoglycemic properties by itself in high doses of ASA and sulfonylurea derivatives of displacement due to plasma proteins,
• While the use of valproic acid increases its toxicity due to displacement of its relation to plasma proteins,
• NSAIDs and derivatives of salicylic acid in high doses (increased risk ulcerogenic effects and bleeding from the gastrointestinal tract as a result of synergism of action), while the use of ibuprofen marked antagonism irreversible platelet inhibition caused by influence of ASA, which leads to a reduction cardioprotective effects ASA
• Ethanol (increased risk of damage to the mucosa of the gastrointestinal tract and prolongation of bleeding time as a result of mutual reinforcement effects of ASA and ethanol)

With simultaneous use of ASA at high doses reduces the effect of drugs listed below, if necessary, co-administration of ASA with the listed drugs should consider the need for dose adjustment of these funds:

• Any diuretics (when combined with ASA in high doses, there is a decrease in glomerular filtration rate (GFR) due to a decrease of prostaglandin synthesis in the kidneys)
•  Angiotensin-converting enzyme (ACE) inhibitors (marked dose-dependent decrease in GFR by inhibiting prostaglandins that have a vasodilatory effect, thus weakening the hypotensive action Clinical GFR decline observed at a daily dose of ASA 160 mg In addition, there is a decrease of positive cardioprotective effects of ACE inhibitors. patients designated for treatment of chronic heart failure. This effect is also apparent when used in conjunction with ASA in high doses)
• Drugs with uricosuric action – benzbromaron, probenecid (urikozuricheskogo reduction effect due to competitive suppression of renal tubular excretion of uric acid)
• While the use of systemic corticosteroids (except hydrocortisone used for replacement therapy in Addison’s disease) noted increased excretion of salicylates and thus weakening their actions.

special instructions

The drug should be used when prescribing physician.

ASA may provoke bronchospasm and induce asthma attacks or other hypersensitivity reactions. Risk factors are the presence of a history of asthma, hay fever, nasal polyposis, chronic respiratory diseases and allergic reactions to other drugs (eg, skin reactions, pruritus, urticaria).

ASA can cause bleeding of varying severity during and after surgery, so if you need the absolute exclusion of bleeding during surgery is necessary, if possible, to completely abandon the use of ASA in the preoperative period.

The combination of ASA with anticoagulant, thrombolytic and antiplatelet drugs is accompanied by an increased risk of bleeding.

ASA in low doses can trigger the development of gout in susceptible individuals (with a reduced excretion of uric acid).

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

High doses of ASA have a hypoglycemic effect, it must be borne in mind when assigning its patients with diabetes receiving hypoglycemic drugs for oral and insulin.

With the combination of glucocorticosteroids (GCS) and salicylates should be remembered that during treatment the level of salicylate in the blood is reduced, and after the abolition of GCS possible overdose of salicylates.

We do not recommend the combination of ASA with ibuprofen in patients with an increased risk of cardio – vascular diseases, as the latter reduces the positive impact on the life expectancy of ASA (ASA reduces the cardioprotective effect).

Exceeding the dose ASA carries a risk of gastrointestinal bleeding.

Overdose is especially dangerous in elderly patients.

With the combination of ASA with alcohol increased the risk of damage to the mucous membrane of the gastrointestinal tract and prolonged bleeding.

During the period of treatment must be careful when performing potentially hazardous activities that require high concentration and psychomotor speed reactions (driving vehicles, working with moving machinery, the work manager and operator, etc.) as well as the possible development of dizziness.

release Form

Pills, enteric-coated tablets, 100 mg.

10 tablets in blisters.

30, 50, 60 or 100 tablets per plastic cans.

Every bank or 1, 2, 3, 5, 6, 10 contour cell packages with instructions for use placed in a pile of cardboard.

Shelf life

4 years.

Do not use the drug after the expiry date stated on the package.

Storage conditions

In a dry place at temperatures no higher than 25 ° C.

Keep out of the reach of children