CardiASK (Acetylsalicylic acid) tablets

The composition and form of issue:

Tablets, covered kishechnorastvorima film-coated. 1 tablet contains active substance: 

acetylsalicylic acid 50 mg

100 mg

excipients: stearic acid corn starch lactose monohydrate (milk sugar) hydrogenated castor oil povidone (plasdone К90 or kollidon 90 F) Polysorbate (tween 80) MKC 

the shell of the enteric film: methacrylic acid and ethylacrylate copolymer (1:1) (collicut MAY 100R) macrogol vinyl alcohol copolymer (collicut IR) copovidone (plasdone es 630) triethylcitrate talc titanium dioxide 

in packing contour cell 10 or 30 PCs. in cardboard pack 1, 2 or 3 packages.

Description pharmaceutical form:

Tablets, film-coated white or almost white, round, lenticular. Slight roughness and a faint smell of acetic acid.

Pharmacokinetics:

After intake of ASA is rapidly and completely absorbed from the gastrointestinal tract. Ask partly metabolized during absorption. During and after absorption of ask becomes the major metabolite is salicylic acid, which is metabolized mostly in the liver under the influence of enzymes with the formation of metabolites such as phenyl salicylate, salicylic acid glucuronide and salitsilovaya acid, found in many tissues and urine. In women the metabolism process is slower (less enzyme activity in the blood serum). Cmax of ASA in the blood plasma is reached in 10-20 minutes after ingestion of salicylic acid through the 0.3–2 hours.

Due to the fact that the tablets coated with an acid resistant shell, ask released not in the stomach (shell effectively blocks the dissolution of the drug in the stomach), and in the alkaline environment of the duodenum. Thus, the absorption of ASA in the form of tablets, enteric coated, delayed by 3-6 hours compared to conventional (without shell) tablets.

ASA and salicylic acid to bind to proteins of blood plasma (from 66 to 98% depending on the dose) and rapidly distributed in the body. Salicylic acid crosses the placenta and in breast milk.

Deducing of salicylic acid is dose-dependent, since its metabolism is restricted by the enzyme system. T1/2 is 2-3 h with the use of ASA in low doses and up to 15 hours — in applying the drug in high doses (usual dose of ASA as analgesic). When multiple doses of the drug digitalisierung ask does not accumulate in the serum. Salicylic acid and its metabolites are excreted by the kidneys. In patients with normal renal function of 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours

Description pharmacological action:

The mechanism of antiplatelet action of acetylsalicylic acid (ASA) is an irreversible inhibition of COX-1, resulting in blocked synthesis ТхА2 and inhibits the aggregation of platelets. Antiplatelet effect occurs even after application of low doses of the drug and lasts for 7 days after a single dose. It is believed that the ASC has other mechanisms of suppression of platelet aggregation, that broadens the area of its application in various vascular diseases. In high doses, ASA also has anti-inflammatory, antipyretic and analgesic action.

Indications:

• primary prevention of acute myocardial infarction in the presence of risk factors (e.g. diabetes, hyperlipidemia, hypertension, obesity, Smoking, old age) and re-myocardial infarction
• unstable angina (including suspected acute myocardial infarction) and stable angina
• prevention of ischemic stroke (including patients with transient disorders of cerebral circulation)
• prevention of thromboembolism after surgery and invasive procedures on vessels (for example coronary artery bypass grafting, endarterectomy of the carotid arteries, arteriovenous bypass grafting, angioplasty and stenting of the coronary arteries, angioplasty of carotid arteries)
• prevention of deep vein thrombosis and thromboembolism pulmonary artery and its branches (including during prolonged immobilization after extensive surgery).

Contraindications:

• hypersensitivity to ASA, auxiliary substances in the composition of the drug and other NSAIDs
• bronchial asthma induced by ingestion of salicylates and other NSAIDs complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, intolerance to ASA and other NSAIDs
• erosivno-azwenne shock syndrome (in the acute stage)
• gastrointestinal bleeding
• hemorrhagic diathesis
• combined use with methotrexate dose 15 mg per week or more
• expressed kidney failure (Cl creatinine less than 30 ml/min)
• severe hepatic insufficiency (class and above of child-Pugh)
• chronic heart failure (III–IV functional class NYHA classification)
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption
• pregnancy (I and III trimester) and lactation
• children up to age 18 years.

With care: gout is hyperuricemia (because of ASA in low doses reduces the excretion of uric acid should be kept in mind that the ASA in low doses can trigger the development of gout in predisposed patients, with reduced excretion of uric acid) a history of: ulcers or gastrointestinal bleeding abnormal liver function (lower class of child-Pugh) impaired renal function (Cl creatinine more than 30 ml/min), bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug Allergy, including other NSAIDs II trimester of pregnancy in advance of surgery (including minor, for example, extraction of the tooth), as ASA may cause the tendency to develop bleeding for several days after taking the drug.

Application of pregnancy and breast-feeding:

The use of large doses of salicylates in the first trimester of pregnancy is associated with an increased rate of defects of fetus development (cleft palate, heart defects). The appointment of salicylates in the first trimester of pregnancy is contraindicated. In the second trimester of pregnancy salicylates can be assigned only subject to strict risk assessment to the fetus and benefits to the mother, preferably in doses no higher than 150 mg/day and short.

In the last trimester of pregnancy salicylates in high doses (over 300 mg/day) causes weakening of labor, premature closure of the ductus arteriosus in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in preterm infants. The appointment of salicylates in the last trimester of pregnancy is contraindicated.

Use during lactation. Salicylates and their metabolites in small amounts of infiltrating breast milk. Casual reception salicylates during lactation is not accompanied by the development of adverse reactions in children and do not require discontinuation of breastfeeding. However, prolonged use of the drug or appoint him to a high dose breast-feeding should be discontinued immediately.

Side effects:

From the digestive tract: the most frequent are nausea, heartburn, vomiting, abdominal pain, rarely ulcers of the gastric mucosa and duodenal ulcers very rare — perforated ulcer of the gastric mucosa and duodenal ulcers, gastrointestinal bleeding, transient liver function abnormalities with elevated liver transaminases.

With the hematopoietic system: the purpose of the ASC is accompanied by an increased risk of bleeding due to the inhibiting action of ASA on platelet aggregation rarely is anemia.

Allergic reactions: skin rash, pruritus, urticaria, angioedema, rhinitis, swelling of nasal mucosa, cardiorespiratory distress syndrome, and severe reactions, including anaphylactic shock.

CNS: dizziness, hearing loss, headache, tinnitus.

Drug interactions:

CardiASK, while the application increases the effects of the following drugs: methotrexate (due to decrease renal clearance and ousting him from the Association with plasma proteins, the combination of ASA and methotrexate is accompanied by increased incidence of side effects from the blood) heparin and indirect anticoagulants (due to dysfunction of platelets and displacing anticoagulants from plasma proteins) thrombolytic drugs, and antiplatelet agents (tiklopidin) digoxin (due to a decrease in its renal excretion) hypoglycemic agents — insulin and sulfonylureas derivatives (due to the hypoglycemic properties of ASA in high doses and displacement derived sulfonylureas from plasma proteins) valproic acid (due to displacement from its plasma proteins).

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

While receiving ask with alcohol there is an additive effect and increased risk of damage to the mucosa of the gastrointestinal tract and lengthening the bleeding time.

ASA reduces the effect of uricosuric drug benzbromarone (decrease uricosuric effect due to competitive suppression of the renal tubular excretion of uric acid), ACE inhibitors (marked dose-dependent decrease in glomerular filtration rate as a result of inhibition of PG, which has vasodilating effect, respectively the attenuation of the hypotensive effect), diuretics (combined with ASA in high doses there is a decrease in glomerular filtration rate due to the reduction of PG synthesis in the kidneys).

Enhancing the elimination of salicylates, systemic corticosteroids are weakening their action.

Method of application and dose:

Inside, before eating, squeezed more liquid. CardiASK tablets are taken 1 time per day. CardiASK designed for prolonged use. The duration of therapy determined by the treating physician.

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 is 50-100 mg/day.

Unstable angina (in cases of suspected acute myocardial infarction) — 50-100 mg/day.

Prevention of ischemic stroke and transient disorders of cerebral circulation is 50-100 mg/day.

Prevention of thromboembolism after surgery and invasive procedures on vessels — 50-100 mg/day.

Prevention of deep vein thrombosis and thromboembolism pulmonary artery and its branches is 50-100 mg/day.

Overdose:

Salicylate intoxication (develops while taking ASA in a dose of 100 mg/kg/day) may be the result of repeated use (for more than 2 days) toxic doses of the drug within the incorrect therapeutic use (chronic intoxication) or a single accidental or intentional ingestion of toxic doses of drugs to adults or child (acute intoxication).

Symptoms of acute intoxication: the main proyavlyaetsya a disorder of acid-base balance, the manifestations of which can vary depending on the patient’s age and severity of intoxication. In children, the most typical is the development of metabolic acidosis.

Treatment: performed in accordance with accepted standards and depends on the severity of intoxication and clinical picture and should be focused primarily on the rapid elimination of the drug and restoration of water and electrolyte balance and acid-base balance.

Symptoms of chronic intoxication derivatives of salicylic acid are nonspecific and are often diagnosed with difficulty. Intoxication mild usually develops only after repeated use of large doses of the drug and is manifested by dizziness, tinnitus, hearing loss, increased perspiration, nausea and vomiting, headache and confusion.

Treatment: the symptoms disappear after reduction of dosage. Tinnitus may appear when the concentration of ASA in blood plasma from 150 to 300 µg/ml. More severe symptoms occur when the concentration of ASA in the blood plasma is above 300 µg/ml.

Overdose is especially dangerous in elderly patients.

Overdose symptoms mild to moderate: dizziness, tinnitus, hearing loss, increased sweating, nausea, vomiting, headache, confusion, profuse sweating, tachypnea, hyperventilation, respiratory alkalosis.

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

Overdose symptoms are moderate to severe: respiratory alkalosis with compensatory metabolic acidosis or hyperpyrexia (extremely high fever), respiratory disorders (hyperventilation, necardiogenny pulmonary edema, respiratory depression, asphyxia) violations of the CCC (heart rhythm disturbances, reduction of pressure, depression of CardiASK activity) of violations of water-electrolyte balance (dehydration, impaired renal function oliguria from until the development of renal failure, characterized by hypokalemia, hypernatremia, hyponatremia) violation of glucose metabolism (hyperglycemia, hypoglycemia (especially in children), ketoacidosis) tinnitus, deafness, gastrointestinal bleeding hematologic disorders (inhibition of platelet aggregation to the elongation PV coagulopathy, hypoprothrombinemia) neurological disorders (toxic encephalopathy and Central nervous system depression (drowsiness, confusion, coma, convulsions).

Treatment: immediate hospitalization in specialized departments for carrying out emergency therapy — gastric lavage, repeated administration of activated charcoal, forced alkaline diuresis, hemodialysis, restoration of water and electrolyte balance and acid-base balance, symptomatic therapy.

Special instructions:

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

The inhibitory effect of ASA on platelet aggregation persists for several days after intake, in connection with which may increase the risk of bleeding during surgery or in the postoperative period. If necessary, exclusion of bleeding during surgical intervention should be possible to completely abandon the use of ASA in the preoperative period.

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

High-dose ASA have a hypoglycemic effect that you need to keep in mind when assigning its patients with diabetes, receiving gipoglikemicakie preparations.

With the combined use of SCS and salicylates should be remembered that during treatment the concentration of salicylates in the blood is reduced, and after the abolition of the SCS is possible overdose of salicylates.

Excess dose ASA is associated with risk of gastrointestinal bleeding.