Composition
Active ingredient:
acetylsalicylic acid 100 mg;
Auxiliary substances:
stearic acid;
corn starch;
lactose monohydrate (milk sugar);
hydrogenated castor oil;
povidone (plasdon K 90 or collidone 90F);
polysorbate (tween 80); MCC;
Film shell:
methacrylic acid and ethyl acrylate copolymer 1: 1 (collicutate 100 R);
macrogol and polyvinyl alcohol copolymer (collicutate IR);
copovidone (plasdon S630);
triethyl citrate;
talc;
titanium dioxide.
Pharmacological action
Cardi ASK – antiaggregational.
Pharmacodynamics
The mechanism of antiplatelet action of acetylsalicylic acid (ASA) is based on irreversible inhibition of COX-1, which blocks the synthesis of thromboxane a2 and suppresses platelet aggregation. The antiplatelet effect develops even after the use of small doses of the drug and persists for 7 days after a single dose. It is believed that ASA has other mechanisms for suppressing platelet aggregation, which expands the scope of its application in various vascular diseases. In high doses, ASA also has anti-inflammatory, antipyretic and analgesic effects.
Pharmacokinetics
After oral use, ASA is rapidly and completely absorbed from the gastrointestinal tract. ASA is partially metabolized during absorption. During and after absorption, ASA is converted to the main metabolite, salicylic acid, which is mainly metabolized in the liver under the influence of enzymes to form metabolites such as phenylsalicylate, salicylic acid glucuronide and salicyluric acid, which are found in many tissues and in the urine. In women, the metabolic process is slower (less activity of enzymes in the blood serum). Tmax ASA in blood plasma — 10-20 minutes after oral use, salicylic acid — 0.3–2 hours.
Due to the fact that the tablets are coated with an acid-resistant shell, ASA is released not in the stomach (the shell effectively blocks the dissolution of the drug in the stomach), but in the alkaline environment of the duodenum. Thus, the absorption of ASA in the form of enteric-coated tablets is slowed down by 3-6 hours compared to conventional (non-enteric-coated) tablets. ASA and salicylic acid bind to plasma proteins (from 66 to 93%, depending on the dose) and are rapidly distributed in the body. Salicylic acid passes through the placenta and into breast milk.
The elimination of salicylic acid is dose-dependent, since its metabolism is limited by the capabilities of the enzymatic system. T1/2 is from 2-3 hours when using ASA in low doses and up to 16 hours when using the drug in high doses (normal doses of acetylsalicylic acid as an analgesic). Unlike other salicylates, with repeated use of the drug, non-hydrolyzed ASA does not accumulate in the blood 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
- increased body temperature in various infectious and inflammatory diseases
- mild and moderate pain of various origins
- prevention of thrombosis and embolism (blockage of blood vessels)
- treatment of myocardial infarction and cerebral circulation disorders.
Contraindications
- ulcerative lesions of the gastrointestinal tract in the acute phase
- of bronchial asthma
- severe renal dysfunction
- hypersensitivity to the drug.
Side effects
Allergic reactions: Â urticaria, angioedema.
From the digestive tract: Â nausea, heartburn, vomiting, abdominal pain, ulcers of the gastric and duodenal mucosa, including perforating, gastrointestinal bleeding, increased activity of “liver” enzymes.
Respiratory system disorders: Â bronchospasm.
From the immune system: Â anaphylactic reactions.
From the hematopoietic system: Â anemia (rare), increased bleeding.
From the central nervous system: Â dizziness, tinnitus.
Interaction
When used together, Cardi ASK enhances the effects of methotrexate by reducing its renal clearance and displacing it from plasma protein bonds.
When used concomitantly, Cardi ASK enhances the effect of heparin and indirect anticoagulants by disrupting platelet function and displacing indirect anticoagulants from their plasma protein bonds.
Cardi ASK, when used in combination, enhances the effect of thrombolytic and antiplatelet drugs (including ticlopidine).
Cardi ASK increases the concentration of digoxin in blood plasma by reducing renal excretion and enhances its effects.
Cardi ASK enhances the effect of hypoglycemic drugs (insulin and sulfonylurea derivatives) due to the hypoglycemic effect of acetylsalicylic acid (in high doses) and the displacement of sulfonylurea derivatives from binding to plasma proteins.
Cardi ASC enhances the action of valproic acid by displacing the latter from binding to plasma proteins.
When used together, Cardi ASK weakens the effect of uricosuric drugs (benzbromarone) due to competitive tubular elimination of uric acid.
When used simultaneously, corticosteroids enhance the elimination of salicylates and weaken their effect.
When used concomitantly with ethanol, an additive effect is noted.
How to take, course of use and dosage
Cardi ASK should be taken orally, before meals, with plenty of fluids. Cardi ASK is intended for long-term use. The duration of therapy is determined by the attending physician.
Prevention of suspected acute myocardial infarction: Â 100-200 mg / day or 300 mg every other day (the first tablet should be chewed for faster absorption).
Prevention of first-time acute myocardial infarction in the presence of risk factors: Â 100 mg per day or 300 mg every other day. Prevention of recurrent myocardial infarction, unstable angina, prevention of stroke and transient cerebrovascular accident, prevention of thromboembolic complications after surgery or invasive research: Â 100-300 mg per dayprophylaxis of deep vein thrombosis and pulmonary embolism and its branches: Â 100-200 mg per day or 300 mg every other day.
Overdose
Moderate overdose symptoms: Â nausea, vomiting, tinnitus, hearing loss, dizziness, confusion. Treatment: Â reducing the dose of the drug.
Severe overdose symptoms: fever, hyperventilation, ketoacidosis, respiratory alkalosis, coma, cardiovascular and respiratory failure, severe hypoglycemia.
Treatment:  immediate hospitalization in specialized departments for emergency therapy — gastric lavage, determination of acid-base state, alkaline and forced alkaline diuresis, hemodialysis, use of solutions, activated charcoal, symptomatic therapy. When performing alkaline diuresis, it is necessary to achieve pH values between 7.5 and 8. Forced alkaline diuresis should be performed when the concentration of salicylates in blood plasma is more than 500 mg/l (3.6 mmol/l) in adults and 300 mg / l (2.2 mmol/l) in children.
Special instructions
Cardi ASK should be used after a doctor’s appointment.
ASA can provoke bronchospasm, as well as cause attacks of bronchial asthma 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).
ASA can cause bleeding of varying degrees of severity during and after surgery.
The combination of ASA with anticoagulants, thrombolytics and antiplatelet drugs is associated with an increased risk of bleeding.
ASA in low doses can provoke the development of gout in predisposed individuals (with reduced uric acid excretion). The combination of ASA with methotrexate is accompanied by an increased frequency of side effects from the hematopoietic system. High doses of ASA have a hypoglycemic effect, which should be taken into account when prescribing it to patients with diabetes mellitus receiving hypoglycemic drugs.
When prescribing corticosteroids and salicylates, it should be remembered that during treatment, the level of salicylates in the blood is reduced, and after the withdrawal of corticosteroids, an overdose of salicylates is possible.
The combination of ASA with ibuprofen is not recommended, as the latter worsens the beneficial effect of ASA on life expectancy. Excess of the ASA dose is associated with the risk of gastrointestinal bleeding. Overdose is especially dangerous in elderly patients. When ASA is combined with alcohol, the risk of damage to the gastrointestinal mucosa and prolongation of bleeding time is increased.
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
Pregnant women only in the second trimester as prescribed by a doctor, Adults
Indications
Prevention of acute myocardial infarction, Prevention of thrombosis, Prevention of heart attacks and strokes, Angina pectoris, Cerebral circulation disorders, Prevention of thromboembolism
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