CardiASC pills 50mg, 30pcs

Composition

1 tablet coated with a film-like enteric coating contains:  

Active ingredients:

acetylsalicylic acid 50 mg and 100 mg;

Auxiliary substances:

stearic acid,

corn starch,

lactose monohydrate (milk sugar),

hydrogenated castor oil,

povidone (plasdon K-90 or collidone 90 F),

polysorbate (tween-80),

microcrystalline cellulose;

Excipients for obtaining enteric film coating:

methacrylic acid and ethyl acrylate copolymer (1: 1) (collicutate 100 R), macrogol and polyvinyl alcohol copolymer (collicutate IR), copovidone (plasdon Es-630), triethyl citrate, talc, titanium dioxide.

Pharmacological action

Pharmacotherapy group:

nonsteroidal anti-inflammatory drug (NSAID).

ATX code: B01 AC 06.

Pharmacological properties

Pharmacodynamics  The mechanism of antiplatelet action of acetylsalicylic acid (ASA) is based on irreversible inhibition of cyclooxygenase (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 (GIT). ASA is partially metabolized during absorption. During and after absorption, ASA is converted to the main metabolite, salicylic acid, which is metabolized mainly 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). The maximum concentration of ASA in blood plasma is reached in 10-20 minutes after ingestion, salicylic acid – in 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 98% 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. The elimination half-life is from 2-3 hours when using ASA in low doses and up to 15 hours when using the drug in high doses (usual 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

-Primary 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 (including suspected acute myocardial infarction) and stable angina.

– Prevention of ischemic stroke (including in patients with transient cerebrovascular accident).

– Prevention of thromboembolism after operations and invasive vascular interventions (for example, coronary artery bypass grafting, carotid artery endarterectomy, arteriovenous bypass grafting, angioplasty and stenting of the coronary arteries, 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 high doses of salicylates in the first 3 months of pregnancy is associated with an increased frequency of fetal defects (cleft palate, heart defects). The use of salicylates in the first trimester of pregnancy is contraindicated. In the second trimester of pregnancy, salicylates can be prescribed only taking into account a strict assessment of the risk to the fetus and the benefit to the mother, preferably in doses not exceeding 150 mg / day and for a short time.

In the last trimester of pregnancy, salicylates in a high dose (more than 300 mg/day) cause weakening of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and use immediately before childbirth can cause intracranial hemorrhages, especially in premature babies. The use of salicylates in the last trimester of pregnancy is contraindicated.

Salicylates and their metabolites pass into breast milk in small amounts. 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, breast-feeding should be stopped immediately.

Contraindications

-Hypersensitivity to acetylsalicylic acid, excipients in the drug and other non-steroidal anti-inflammatory drugs (NSAIDs). – Bronchial asthma induced by taking salicylates and other NSAIDs; complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, intolerance to ASA and other NSAIDs. – Erosive and ulcerative lesions of the gastrointestinal tract (in the acute stage). – Gastrointestinal bleeding. – Hemorrhagic diathesis. – Combined use with methotrexate at a dose of 15 mg per week or more. – Pregnancy (I and III trimester) and lactation. – Children under 18 years of age. – Severe renal insufficiency (creatinine clearance less than 30 ml / min). – Severe hepatic insufficiency (class B and higher on the Child-Pugh scale). – Chronic heart failure (NYHA functional class III-IV). – Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Use caution

in gout, hyperuricemia, because ASA in low doses reduces the excretion of uric acid; it should be borne in mind that ASA in low doses can provoke the development of gout in predisposed patients (with reduced uric acid excretion). – If there is a history of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding. – With impaired liver function (below class B on the Child-Pugh scale). – With impaired renal function (creatinine clearance more than 30 ml / min). – For bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergies, including NSAID groups (analgesics, anti-inflammatory drugs, antirheumatic drugs). – In the second trimester of pregnancy. – With the proposed surgical intervention (including minor ones, for example, tooth extraction), since ASA can cause a tendency to develop bleeding within a few days after taking the drug.

Side effects

From the digestive system:  The most common symptoms are nausea, heartburn, vomiting, abdominal pain; rarely-ulcers of the gastric and duodenal mucosa; very rarely-perforated ulcers of the gastric and duodenal mucosa, gastrointestinal bleeding, transient liver function disorders with increased activity of “liver” transaminases.

From the hematopoietic system: use of ASA is accompanied by an increased risk of bleeding due to the inhibitory effect of ASA on platelet aggregation, rarely – anemia.

Allergic reactions:  skin rash, pruritus, urticaria, Quincke’s edema, rhinitis, nasal mucosal edema, rhinitis, cardiorespiratory distress syndrome, and severe reactions, including anaphylactic shock.

From the central nervous system:  dizziness, hearing loss, headache, tinnitus.

Interaction

Cardi ASC®, when used concomitantly, enhances the effect of the following medications: :  

– methotrexate by reducing renal clearance and ousting him from Association with plasma proteins, the combination of acetylsalicylic acid with methotrexate is accompanied by increased incidence of side effects from the digestive blood;

– heparin and indirect anticoagulants due to dysfunction of platelets, and displacing anticoagulants from plasma proteins;

– thrombolytic and antiplatelet agents (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 plasma proteins;

– valproic acid due to its displacement from the bond with plasma proteins.

The combination of acetylsalicylic acid with anticoagulants, thrombolytics and antiplatelet agents is associated with an increased risk of bleeding. When taking acetylsalicylic acid with alcohol at the same time, an additive effect is observed and the risk of damage to the gastrointestinal mucosa and prolongation of bleeding time increases.

ACK reduces the effect of uricosuric medicines benzbromarone (decrease uricosuric effect due to competitive suppression of renal tubular excretion of uric acid), inhibitors of angiotensin converting enzyme (ACE) (marked, dose-dependent decrease in glomerular filtration rate as a result of inhibition of prostaglandins, which has vasodilating effect, respectively, the attenuation of the hypotensive effect), diuretics (in a joint application with ASA in high doses there is a decrease in glomerular filtration rate due to the reduction of prostaglandin synthesis in the kidneys). By increasing the elimination of salicylates, systemic glucocorticosteroids (corticosteroids) weaken their effect.

How to take, course of use and dosage

Tablets of the drug Cardi ASK should preferably be taken before meals, washed down with a large amount of liquid. Cardi ASK ® tablets are taken once a day. Cardi ASK® is intended for long-term use. The duration of therapy is determined by the doctor.

Primary prevention of acute myocardial infarction in the presence of risk factors: 50-100 mg / day.

Prevention of recurrent myocardial infarction, stable and unstable angina: 50-100 mg / day.

Unstable angina (if acute myocardial infarction is suspected): 50-100 mg / day.

Prevention of ischemic stroke and transient cerebrovascular accident: 50-100 mg / day.

Prevention of thromboembolism after surgery and invasive vascular interventions: 50-100 mg / day.

Prevention of deep vein thrombosis and pulmonary embolism and its branches: 50-100 mg / day.

Overdose

Salicylate intoxication (develops when taking ASA at a dose of more than 100 mg / kg / day for more than 2 days) may result from prolonged use of toxic doses of the drug as part of improper therapeutic use of the drug (chronic intoxication) or a single accidental or intentional intake of a toxic dose of the drug by an adult or child (acute intoxication).

Symptoms of chronic intoxication with salicylic acid derivatives are non-specific and often difficult to diagnose. Mild intoxication usually develops only after repeated use of large doses of the drug and is manifested by dizziness, tinnitus, hearing loss, increased sweating, nausea and vomiting, headache and confusion. These symptoms disappear after reducing the dose of the drug. Tinnitus can occur when the concentration of ASA in the blood plasma is from 150 to 300 mcg / ml.

More severe symptoms occur when the concentration of ASA in the blood plasma is higher than 300 mcg / ml. The main manifestation of acute intoxication is a severe violation of the acid-base state, the manifestations of which may vary depending on the age of the patient and the severity of intoxication. In children, the development of metabolic acidosis is most typical. Treatment of intoxication is carried out in accordance with accepted standards and depends on the severity of intoxication and the clinical picture and should be aimed mainly at accelerating the elimination of the drug and restoring the water-electrolyte balance and acid-base state.

Overdose is especially dangerous in elderly patients.

Mild to moderate overdose symptoms: 

Dizziness, tinnitus, hearing loss, increased sweating, nausea, vomiting, headache, confusion, profuse sweating, tachypnea, hyperventilation, respiratory alkalosis.

Treatment: gastric lavage, repeated use of activated charcoal, forced alkaline diuresis, restoration of water-electrolyte balance and acid-base state.

Moderate to severe overdose symptoms:

– respiratory alkalosis with compensatory metabolic acidosis; – or hyperpyrexia (extremely high body temperature); – respiratory: hyperventilation, nicardipine pulmonary edema, respiratory depression, apnea; – disorders of the cardiovascular system: arrhythmias, reduced pressure, depression of cardiac activity; – violations of water-electrolyte balance: dehydration (dehydration), impaired renal function from oliguria up to the development of renal failure, characterized by hypokalemia, with hypernatremia, hyponatremia; – violation of the metabolism of glucose: hyperglycemia, hypoglycemia (especially in children), ketoacidosis. noise in the ears, deafness; gastrointestinal bleeding; hematological disorders: from the inhibition of platelet aggregation to coagulopathy, prolongation of prothrombin time, hypoprothrombinemia; – neurologic disorders: toxic encephalopathy and Central nervous system depression (drowsiness, confusion, coma, convulsions).

Treatment:

Immediate hospitalization in specialized departments for emergency therapy – gastric lavage, repeated intake of activated charcoal, forced alkaline diuresis, hemodialysis, restoration of water-electrolyte balance and acid-base state, symptomatic therapy.

Special instructions

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).

The inhibitory effect of ASA on platelet aggregation persists for several days after use, and therefore, there may be an increased risk of bleeding during surgery or in the postoperative period. If it is necessary to absolutely exclude bleeding during surgery (it is necessary, if possible, to completely abandon the use of ASA in the preoperative period.

Acetylsalicylic acid in low doses can provoke the development of gout in Predisposed individuals (with reduced uric acid excretion). High doses of acetylsalicylic acid have a hypoglycemic effect, which should be taken into account when prescribing it to patients with diabetes mellitus receiving hypoglycemic drugs.

With the combined use of corticosteroids and salicylates, it should be remembered that during treatment, the concentration of salicylates in the blood is reduced, and after the withdrawal of corticosteroids, an overdose of salicylates is possible.

Exceeding the dose of acetylsalicylic acid is associated with the risk of gastrointestinal bleeding.

Form of production

film-coated tablets of white or almost white color, round, biconvex. Slight roughness and a faint smell of acetic acid are allowed.

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

Adults who are only pregnant in the second trimester as prescribed by a doctor

Indications

Cerebrovascular accident, Angina pectoris, Prevention of heart attacks and strokes, Prevention of acute myocardial infarction, Prevention of thromboembolism, Prevention of thrombosis