Acetylsalicylic acid cardio

General characteristics. Structure:

Active ingredient: 50 mg, 100 mg or 300 mg of acetylsalicylic acid in 1 tablet.

Excipients: cellulose microcrystallic, silicon dioxide colloid (aerosil); starch prezhelatinizirovanny; stearic acid.
 
Excipients for a cover: gidroksipropilmetiltsellyuloz (gipromelloz); methacrylic acid and ethyl acrylate copolymer (Kollikut MAY 100 P); propylene glycol; povidone (коллидон 30); talc; titanium dioxide; dye azoruby; dye blue brilliant (brilliant blue).

Analgetic and antiagregant. It is applied at a pain syndrome as anti-inflammatory drug, for prevention of thromboses and an embolism.

Pharmacological properties:

Pharmacodynamics. Acetylsalicylic acid (ASK) represents ester of salicylic acid, concerns to group of non-steroidal anti-inflammatory drugs (NPVP). The mechanism of action is based on an irreversible inactivation of enzyme of cyclooxygenase (TsOG-1) therefore synthesis of prostaglandins, prostacyclins and thromboxane is blocked. Reduces aggregation, adhesion of thrombocytes and a thrombogenesis due to suppression of synthesis of A2 thromboxane in thrombocytes.

Increases fibrinolitic activity of a blood plasma and vitamin of K-dependent factors of coagulation reduces concentration (II, VII, IX, X). The Antiagregantny effect is most expressed in thrombocytes as they are not capable to synthesize cyclooxygenase repeatedly. The Antiagregantny effect develops after use of small doses of drug and remains within 7 days after a single dose. These ASK properties are used in prevention and treatment of the myocardial infarction (MI), coronary heart disease (CHD), varicosis complications.

ASK renders also antiinflammatory, febrifugal and analgeziruyushchy action.

Pharmacokinetics. At intake of ASK it is soaked up quickly and completely from the digestive tract (DT). ASK is partially metabolized during absorption. In time and after absorption of ASK turns into the main metabolite – salicylic acid which is metabolized, mainly, in a liver under the influence of liver enzymes with formation of such metabolites as salol, a glucuronide salicylate and salitsilurovy acid, found in many fabrics and in urine. At women process of metabolism takes place more slowly (smaller activity of enzymes in blood serum).

ASK and salicylic acid highly contact proteins of a blood plasma (from 66 to 98% depending on a dose) and are quickly distributed in an organism. Salicylic acid gets through a placenta and is emitted with breast milk.

Elimination half-life (T?) ASK makes about 15-20 minutes of a blood plasma. Unlike other salicylates, at multiple dose of drug not hydrolyzed ASK does not collect in blood serum. Only 1% of ASK accepted inside is removed by kidneys in the form of not hydrolyzed ASK, other part is removed in the form of salicylates and their metabolites. At patients with normal function of kidneys of 80-100% of a single dose of drug it is removed by kidneys within 24-72 hours.

Indications to use:

- Prevention of an acute myocardial infarction with risk factors (for example, a diabetes mellitus, a lipidemia, the arterial hypertension (AH), obesity, smoking, advanced age) and a repeated myocardial infarction;

- unstable stenocardia;

- prevention of a stroke (including, at patients with passing disturbance of cerebral circulation);

- prevention of passing cerebral circulation;

- prevention of a thromboembolism after operations and invasive interventions on vessels (for example, aortocoronary shunting, endarterectomy of carotid arteries, angioplasty and stenting of coronary arteries);

- prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches (including, at a long immobilization as a result of extensive surgical intervention).

Route of administration and doses:

It is desirable to take a pill of the drug KARDIO Acetylsalicylic acid before food, washing down with a large amount of liquid. Drug is not accepted on an empty stomach! Drug is intended for prolonged use. Duration of therapy is defined by the doctor.

- Primary prevention acute to THEM with risk factors: 50 - 100 mg a day or 300 mg every other day.

- Prevention repeated to THEM, unstable stenocardia: 50 - 100 mg a day or 300 mg every other day.

- Prevention of a stroke and passing disturbance of cerebral circulation: 50-100 mg a day or 300 mg every other day.

- Prevention of a thromboembolism after operations and invasive interventions on vessels: 50 - 100 mg a day or 300 mg every other day.

- Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches: 100-200 mg a day.

Features of use:

Use at pregnancy. Use of high doses of salicylates in the first 3 months of pregnancy is associated with the increased frequency of defects of fetation (the split upper sky, heart diseases). Purpose of salicylates in the I trimester of pregnancy is contraindicated.

In the last trimester of pregnancy salicylates in a high dose (more than 300 mg/days) cause braking of patrimonial activity, premature closing of an arterial channel in a fruit, the raised bleeding in mother and a fruit, and appointment just before childbirth can cause intracraneal hemorrhages, especially in premature children. Purpose of salicylates in the last trimester of pregnancy is contraindicated.

In the II trimester of pregnancy it is possible to appoint salicylates only taking into account strict assessment of advantage for mother and risk for a fruit, not higher than 150 mg/days are preferable in doses and it is short.

Use during feeding by a breast. Salicylates and their metabolites in small amounts get into breast milk. Accidental reception of salicylates in the period of a lactation is not followed by development of side reactions in the child and does not demand the breastfeeding termination. However at prolonged use of drug or appointment it in a high dose feeding by a breast should be stopped immediately.

Data on possible influence of medicine for a medical use on ability to manage vehicles, mechanisms. During treatment it is necessary to be careful during the driving of vehicles and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions as use of the drug KARDIO Acetylsalicylic acid can cause dizziness.

Side effects:

From a digestive tract: nausea, heartburn, vomiting, pain in a stomach, stomach ulcer and a duodenum, including perforative, gastrointestinal bleedings, passing abnormal liver functions with increase in activity of "hepatic" transaminases.

From the central nervous system (CNS): dizziness, decrease in hearing, a sonitus that can be a drug overdose sign (see the section Overdose).

From system of a hemopoiesis: the increased frequency perioperatsionny (intra-and post-operating rooms) bleedings, hematomas, nasal bleedings, bleeding of gums, bleedings from urinogenital ways. There are messages on serious cases of bleedings to which gastrointestinal bleedings and hematencephalons (especially at the patients with arterial hypertension who did not reach target indicators of the arterial pressure (AP) and/or receiving the accompanying therapy by anticoagulating means) which in some cases can have life-threatening character belong. Bleedings can lead to development of an acute or chronic posthemorrhagic/iron deficiency anemia (for example, owing to the concealed hemorrhage) with the corresponding clinical laboratory symptoms (an adynamy, pallor, hypoperfusion).

Allergic reactions: skin rash, an itch, a small tortoiseshell, a Quincke's edema, rhinitis, hypostasis of a mucous membrane of a nasal cavity, rhinitis, a bronchospasm, a cardiorespiratory distress syndrome, and also heavy reactions, including an acute anaphylaxis.

Interaction with other medicines:

At simultaneous use of ASK strengthens action of some HP; in need of co-administration of ASK with the listed drugs it is necessary to consider a question of need of reduction of a dose of the specified means:

- a methotrexate, due to decrease in renal clearance and its replacement from communication with proteins of plasma;

- at simultaneous use with anticoagulants, thrombolytic and antiagregantny means (тиклопидин) increase in risk of bleedings as a result of a synergism of the main therapeutic effects of the used means is noted;

- at simultaneous use with the drugs possessing anticoagulating, thrombolytic or antiagregantny action strengthening of the damaging action on a mucous membrane of a GIT is noted;

- selective serotonin reuptake inhibitors that can lead to increase in risk of bleeding from upper parts of a GIT (a synergism with ASK);

- digoxin, owing to decrease in its renal excretion that can lead to overdose;

- hypoglycemic means for intake (sulphonylurea derivatives) and insulin due to hypoglycemic properties of the ASK in high doses and replacement of derivatives of sulphonylurea from communication with proteins of a blood plasma;

- at simultaneous use with valproic acid its toxicity due to its replacement from communication with proteins of a blood plasma increases;

- NPVP and derivatives of salicylic acid in high doses (increase in risk of ulcerogenic effect and bleeding from a GIT as a result of an action synergism); at simultaneous use with an ibuprofen antagonism concerning the irreversible oppression of thrombocytes caused by action of ASK that leads to decrease in cardioprotective effects of ASK is noted;

- ethanol (the risk of injury of a mucous membrane of a GIT and lengthening of a bleeding time as a result of mutual strengthening of effects of ASK and ethanol is increased).

Simultaneous use of ASK in high doses can weaken action of the listed below HP; in need of co-administration of ASK with the listed drugs it is necessary to consider a question of need of dose adjustment of the transferred funds:

- any diuretics (at combined use with ASK in high doses clinically significant reduction in the rate of glomerular filtering (SKF) as a result of decrease in synthesis of prostaglandins in kidneys is noted);

- inhibitors of an angiotensin-converting enzyme (APF) (dozozavisimy decrease in SKF as a result of inhibition of synthesis of prostaglandins possessing vasodilating action, respectively, weakening of hypotensive action is noted. Clinical decrease in SKF is noted at a daily dose of ASK more than 160 mg. Besides, decrease in positive cardioprotective effect of the APF inhibitors appointed to patients for therapy of HSN is noted. This effect is also shown at use together with ASK in high doses).

- drugs with uricosuric action – бензбромарон, пробенецид (decrease in uricosuric effect owing to competitive suppression of renal canalicular excretion of uric acid);

- at co-administration with system glucocorticosteroids (GKS) (except for the hydrocortisone applied to replacement therapy of a disease of Addison) strengthening of removal of salicylates and respectively weakening of their action is noted.

Contraindications:

- Hypersensitivity to ASK, excipients as a part of drug and other NPVP;

- GIT erosive cankers (in an aggravation phase);

- gastrointestinal bleeding;

- hemorrhagic diathesis;

- the bronchial asthma (BA) induced by reception of salicylates and other NPVP; a combination OH, the nose recuring a polypose and okolonosovy bosoms with portability of ASK;

- the combined use with a methotrexate in a dose of 15 mg a week and more;

- pregnancy (I and III trimester) and lactation period;

- age up to 18 years;

- the expressed renal failure (the clearance of creatinine (CC) less than 30 ml/min.);

- the expressed liver failure (a class B above on a scale of Chayld-Pyyu);

- the chronic heart failure (CHF) of the III-IV functional class on NYHA classification.

Overdose:

Can have serious consequences, first of all, at elderly patients and at children. The syndrome of a salitsilizm develops at reception of ASK in a dose more than 100 mg/kg/days for more than 2 days owing to use of toxic doses of drug within the wrong therapeutic use (chronic poisoning) or single accidental or intended dose of a toxic dose of drug by the adult or child (acute poisoning).

Overdose symptoms:

- at easy and moderate severity (a single dose less than 150 mg/kg): dizziness, a sonitus, decrease in hearing, the increased sweating, nausea and vomiting, a headache, confusion of consciousness, a tachypnea, a hyperventilation, a respiratory alkalosis.

Treatment: gastric lavage, multiple dose of absorbent carbon, the forced alkaline diuresis, recovery of water and electrolytic balance and an acid-base state.

- at average and heavy severity (a single dose of 150 - 300 mg/kg – moderate severity, more than 300 mg/kg – heavy degree of poisoning): respiratory alkalosis with a compensatory metabolic acidosis, a hyper pyrexia, a hyperventilation, not cardiogenic fluid lungs, respiratory depression, asphyxia; from cardiovascular system: disturbances of a heart rhythm, the expressed decrease in the ABP, oppression of cordial activity; from water and electrolytic balance: dehydration, the renal failure from an oliguria up to development of a renal failure which is characterized by a hypopotassemia, a hypernatremia, a hyponatremia; glucose metabolism disturbance: a hyperglycemia, a hypoglycemia (especially at children), ketoacidosis; sonitus, deafness; gastrointestinal bleedings; hematologic disturbances: from inhibition of aggregation of thrombocytes to a coagulopathy, lengthening of a prothrombin time, a prothrombinopenia; neurologic disturbances: toxic encephalopathy and oppression of the TsNS function (drowsiness, confusion of consciousness, lump, spasm).

Treatment: immediate hospitalization in specialized departments for performing the emergency therapy – gastric lavage, multiple dose of absorbent carbon, the forced alkaline diuresis, a hemodialysis, recovery of water and electrolytic balance and an acid-base state, symptomatic therapy.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity and the instruction on prohibition of use of medicine after a period of validity - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover of 50 mg, 100 mg and 300 mg. On 10 or 20 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4, 5 blister strip packagings together with the application instruction place in a pack from a cardboard.