Acetylsalicylic acid Cardio - instructions for use, dose, side effects, contraindications

pellets of acetylsalicylic acid 30%	- 167 mg	- 333 mg
acetylsalicylic acid	- 50 mg	- 100 mg
Auxiliary substances:
sodium carboxymethyl starch	- 6.78 mg	- 13.56 mg
sucrose (sugar)	- 40.90 mg	- 80.80 mg
starch	- 31.28 mg	- 62.56 mg
dye sunset yellow	- 1.04 mg	- 2.08 mg
copovidone	- 5.28 mg	- 10.56 mg
Auxiliary substances for the pellet shell:
hypromellose	- 7.95 mg	- 15.90 mg
hypromellose phthalate	- 23.33 mg	- 46.66 mg
cetyl alcohol	- 0.44 mg	0.88 mg

Capsules hard gelatinous [body: gelatin -100%; cap: gelatin - up to 100%, dye azorubin - 0.0821%]

Description:

Dosage 50 mg: Hard gelatin capsules No. 2 with a clear, colorless body and cap transparent pink color. Contents of capsules are spherical pellets of orange color.

Dosage 100 mg: hard gelatin capsules No. 0 with a clear, colorless body and lid of a transparent pink color.The contents of the capsules are spherical pellets of orange color.

Pharmacotherapeutic group:Antiaggregant agent

ATX: & nbsp

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

Pharmacodynamics:

Acetylsalicylic acid (ASA) is an ester of salicylic acid, belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). The mechanism of action is based on the irreversible inactivation of the cyclooxygenase enzyme (COX-1), thereby blocking the synthesis of prostaglandins, prostacyclin and thromboxane. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.

Increases fibrinolytic activity of blood plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). The antiaggregant effect is most pronounced in platelets, since they are not able to re-synthesize cyclooxygenase. Antiaggregant effect develops after using small doses of acetylsalicylic acid (less than 300 mg per day) and persists for 7 days after a single dose. These properties of ASA are used in the prevention and treatment of acute myocardial infarction (MI), ischemic heart disease (IHD), complications of varicose veins.

Pharmacokinetics:

When administered orally, ASA is absorbed rapidly and completely from the gastrointestinal tract (GIT). ASA is partially metabolized during absorption. During and after absorption, ASA is converted into a major metabolite, salicylic acid, which is metabolized mainly in the liver under the influence of liver enzymes with formation of metabolites such as phenyl salicylate, glucuronide salicylate and salicyluric acid, found in many tissues and in urine. In women, the metabolic process is slower (less enzyme activity in the blood serum).

The maximum concentration of ASA in the blood plasma is reached after 10-20 minutes after ingestion, salicylic acid - after 0.3-2 hours. Due to the fact that the pellets inside the capsules are covered with an acid-resistant coating, ASA is not released in the stomach (the membrane effectively blocks the dissolution of the drug in the stomach), but in the alkaline medium of the duodenum, and the absorption of ASA is slowed down for 3-6 hours by compared with the usual (without such a shell) tablets.

ASA and salicylic acid are highly associated with blood plasma proteins (66 to 98% depending on the dose) and are rapidly distributed in the body. Salicylic acid penetrates the placenta and is excreted in breast milk.

The half-life of ASA from the blood plasma is about 15-20 minutes. Elimination of salicylic acid is dose-dependent, since its metabolism is limited by the possibilities of the enzymatic system. The half-life of salicylic acid is about 2-3 hours when using ASA in low doses. Unlike other salicylates, with repeated administration of the drug, unhydrolyzed ASA does not accumulate in the blood serum. Only 1% of the ingested ASA is excreted by the kidneys in the form of nonhydrolyzed ASA, the rest is excreted as salicylates and their metabolites. In patients with normal kidney function 80-100% of a single dose of the drug, - excreted by the kidneys within 24-72 hours.

Indications:

- prevention of acute myocardial infarction in the presence of risk factors (for example, diabetes mellitus, dyslipidemia, hypertension (AH), obesity, smoking, old age) and repeated myocardial infarction;

- unstable angina;

- prevention of stroke (including, in patients with transient impairment 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, angioplasty, and stenting of the coronary arteries);

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

Contraindications:

- increased sensitivity to acetylsalicylic acid, ancillary substances in the formulation and other non-steroidal anti-inflammatory drugs;

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

- gastrointestinal hemorrhage;

- hemorrhagic diathesis;

- bronchial asthma (BA), induced by the intake of salicylates and other NSAIDs; combination of asthma, recurrent nasal polyposis and paranasal sinuses with intolerance to ASA;

- simultaneous use with methotrexate in a dose of 15 mg per week or more;

- pregnancy (I and III trimester) and lactation;

- age to 18 years;

- severe renal failure (creatinine clearance (CK) less than 30 ml / min);

- severe hepatic impairment (class B and C on the Child-Pugh scale);

- chronic heart failure (CHF) III-IV functional class by classification NYHA.

Carefully:

With gout, hyperuricemia, peptic ulcer and duodenal ulcer or gastrointestinal hemorrhage (in the anamnesis), renal failure (QC more than 30 ml / min), liver failure (class A on the Child-Pugh scale), asthma, chronic diseases respiratory organs, hay fever, polyposis of the nose, drug allergies incl. to other NSAIDs (analgesics, anti-inflammatory and antirheumatic drugs);pregnancy (II trimester); with the proposed surgical intervention (including minor, for example, tooth extraction).

In severe forms of deficiency of glucose-6-phosphate dehydrogenase, ASA can cause hemolysis and hemolytic anemia. Risk factors for hemolysis are fever, acute infections and high doses of the drug.

At simultaneous reception with the following medicines (LS) (see.section Interactions with Other Drugs):

- methotrexate in a dose of less than 15 mg per week;

- with anticoagulants, thrombolytic or antiplatelet agents;

- with NSAIDs and salicylic acid derivatives in large doses;

- with digoxin;

- with hypoglycemic agents for oral administration (derivatives sulfonylureas) and insulin;

- with valproic acid;

- with alcohol (alcoholic beverages in particular);

- with selective serotonin reuptake inhibitors;

with ibuprofen.

Pregnancy and lactation:

The use of large doses of salicylates in the first 3 months of pregnancy is associated with an increased incidence of fetal developmental defects (split upper skies, heart defects). The appointment of salicylates in the first trimester of pregnancy is contraindicated.

In the last trimester of pregnancy salicylates in high dose (more than 300 mg / day) cause inhibition of labor, premature closure of the arterialduct the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in premature infants.The appointment of salicylates in the last trimester of pregnancy is contraindicated.

In the second trimester of pregnancy, salicylates can only be given taking into account a strict assessment of the benefits to the mother and the risk to the fetus, preferably at doses not exceeding 150 mg / day and for a short time.

Salicylates and their metabolites penetrate into breast milk in small amounts. Accidental reception 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:

Capsules-preparation Acetylsalicylic acid CARDIO it is desirable to take before eating, squeezed large amounts of liquid.

The drug is intended for long-term use. Duration of drug therapy Acetylsalicylic acid CARDIO capsules 50 mg and 100 mg is determined by a physician.

Primary prevention of acute MI in the presence of risk factors: 100 mg daily or 300 mg every other day.

Prevention of repeated myocardial infarction, unstable angina: 100-300 mg per day.

Prevention of stroke and transient impairment of cerebral circulation: 100-300 mg per day.

Prevention of thromboembolism after surgery and invasive vascular interventions: 100-300 mg per day.

Prevention of deep vein thrombosis and thromboembolism of the pulmonary artery and its branches: 100-200 mg per day or 300 mg every other day.

Side effects:

Allergic reactions: skin rash, itching, urticaria, Quincke's edema, rhinitis, mucous membrane swelling of the nasal cavity, rhinitis, bronchospasm, cardio-respiratory distress syndrome, and severe allergic reactions, including anaphylactic shock.

From the digestive system: nausea, heartburn, vomiting, abdominal pain, stomach and duodenum ulcers, including perforating, gastrointestinal bleeding, transient liver dysfunction with increased activity of "liver" transaminases.

From the central nervous system (CNS): dizziness, hearing loss, tinnitus, which may be a sign of drug overdose (see Overdose section).

From the hematopoiesis: increased frequency of perioperative (intra- and post-operative) bleeding, hematomas, nasal bleeding, bleeding gums, bleeding from the urogenital tract.There are reports of serious bleeding events, which include gastrointestinal bleeding and cerebral hemorrhage (especially in patients with hypertension who did not achieve blood pressure targets (BP) and / or who received concomitant therapy with anticoagulant drugs), which in some cases may have a life-threatening character. Bleeding can lead to the development of acute or chronic posthemorrhagic / iron deficiency anemia (eg, due to latent bleeding) with appropriate clinical and laboratory symptoms (asthenia, pallor, hypoperfusion). There are reports of hemolysis and hemolytic anemia in patients with severe forms of glucose-6-phosphate dehydrogenase deficiency.

From the urinary system: renal impairment and acute renal failure failure.

Overdose:

Overdose can have serious consequences, especially in elderly patients and children.

Overdose Symptoms mild severity: dizziness, tinnitus, hearing loss, sweating, nausea and vomiting, headache, confusion.Treatment: reduction of the dose of the drug.

Overdose Symptoms medium severity: in addition to the above - profuse sweating, rapid breathing, respiratory alkalosis. Treatment: reduction of the dose of the drug; gastric lavage, reception of activated carbon, forced alkaline diuresis, restoration of acid-base balance.

Overdose Symptoms severe: fever, hyperventilation, non-cardiogenic pulmonary edema, respiratory depression, asphyxia, respiratory alkalosis with compensatory metabolic acidosis, cardiac arrhythmias, arterial hypotension, cardiac depression, dehydration, renal dysfunction from oliguria to kidney failure, glucose metabolism disorder (hypo-, hyperglycemia), ketoacidosis, noise in the ears, hearing loss, gastrointestinal bleeding, thrombocytopenia, coagulopathy, toxic encephalopathy and CNS depression (drowsiness, confusion, coma, convulsive seizures). Treatment: immediate hospitalization in specialized departments for emergency therapy - gastric lavage, activated carbon reception, forced alkaline diuresis, hemodialysis, restoration of water-electrolyte balance and acid-base balance, symptomatic therapy.

Interaction:

With the simultaneous use of ASY enhances the effect of certain drugs; if it is necessary to simultaneously prescribe ASA with the listed drugs, consideration should be given to the need to reduce the dose of these drugs:

- methotrexate, by reducing renal clearance and displacing it from the bond with proteins plasma blood; the combination of ASA with methotrexate is accompanied by an increased incidence of side effects on the part of the hematopoiesis;

- with simultaneous use with anticoagulants, thrombolytic and antiplatelet agents (ticlopidine) there is an increased risk of bleeding as a result of synergism of the main therapeutic effects;

- with simultaneous use with drugs that have anticoagulant, thrombolytic or antiplatelet effect, increased damage to the mucosa of the gastrointestinal tract;

- selective serotonin reuptake inhibitors, which may lead to an increased risk of bleeding from the upper GI tract (synergy with ASA);

- digoxin, due to a decrease in its renal excretion, which can lead to an overdose;

- hypoglycemic agents for oral administration (sulfonylurea derivatives) and insulin due to hypoglycemic properties of the ASA itself at high doses and displacement of sulfonylurea derivatives from binding to plasma proteins;

- with simultaneous application with valproic acid, it increases toxicity due to its displacement from the connection with blood plasma proteins;

- NSAIDs and salicylic acid derivatives in high doses (increased risk ulcerogenic effect and bleeding from the gastrointestinal tract as a result of synergism of the action);

- ethanol (increased risk of damage to the mucous membrane of the gastrointestinal tract and prolonged bleeding time as a result of the mutual enhancement of the effects of ASA and ethanol).

Simultaneous use of ASA in high doses can weaken the effect of the following medicines; if it is necessary to simultaneously prescribe ASA with the listed drugs, consideration should be given to the need to correct the dose of the listed drugs:

- any diuretics (when combined with ASA in high doses, there is a clinically significant decrease in the glomerular filtration rate (GFR) as a result of a decrease in the synthesis of prostaglandins in the kidneys);

- Angiotensin converting enzyme (ACE) inhibitors (a dose-dependent decrease in GFR due to inhibition of the synthesis of prostaglandins with vasodilating action, respectively, weakening of the hypotensive effect.) A clinically significant decrease in GFR is observed with a daily dose of ASC greater than 160 mg. In addition, there is a decrease in the positive cardioprotective effect of inhibitors ACEs assigned to patients for CHF therapy, this effect also manifests when applied in conjunction with ASA in large doses).

- drugs with uricosuric action - benzbromarone, probenecid (decrease of uricosuric effect due to competitive suppression of renal tubular excretion of uric acid).

With simultaneous use with ibuprofen, antagonism is noted with respect to irreversible platelet suppression caused by the action of ASA, which leads to a decrease in the cardioprotective effects of ASA.

When used simultaneously with systemic glucocorticosteroids (GCS) (with the exception of hydrocortisone or another SCS used for the replacement therapy of Addison's disease), there is an increase in the elimination of salicylates and, accordingly, their weakeningactions.

Special instructions:

The drug should be used only as directed by a doctor.

The inhibitory effect of ASA on platelet aggregation persists for several days after admission, which may increase the risk of bleeding during surgery or in the postoperative period. If absolute elimination of bleeding is necessary in the course of surgical intervention, possibility to completely abandon the use of ASA in the preoperative period.

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

High doses of ASA have a hypoglycemic effect, which should be borne in mind when prescribing it to patients with sugar diabetes, receiving hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin.

When combined use of GCS and salicylates should be remembered that during treatment, the concentration of salicylates in blood is reduced, and after cancellation of SCS, an overdose of salicylates is possible.

It is not recommended to combine ASA with ibuprofen in patients with an increased risk of cardiovascular disease,since the latter reduces the positive effect of ASA on life expectancy (reduces the cardioprotective effect of ASA).

Excess dose of ASA is associated with a risk of gastrointestinal bleeding.

Overdose is especially dangerous in elderly patients.

With the combination of ASA and ethanol, the risk of damage to the gastrointestinal mucosa and the prolongation of bleeding time are increased.

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

During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions, since the use of the drug Acetylsalicylic acid CARDIO can rarely cause dizziness.

Form release / dosage:

Capsules 50 mg and 100 mg.

Packaging:

For 6 or 10 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1,2, 3, 4, 5 or 6 contour squares, together with the instructions for use, are placed in a pack of cardboard.

Storage conditions:

In dry, 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 expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-001735

Date of registration:02.07.2012

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp02.07.2012

Illustrated instructions

Instructions

Acetylsalicylic acid (Acetylsalicylic acid Cardio)