medicalmeds.eu Medicines Antiagregantny means. Atsekardol

Atsekardol

Producer: JSC Sintez Russia

Code of automatic telephone exchange: N02BA01

Release form: Firm dosage forms. Tablets.

Indications to use: Acute myocardial infarction. Unstable stenocardia. Ischemic stroke. Prevention of a thromboembolism. Deep vein thrombosis.

General characteristics. Structure:

Active agent: acetylsalicylic acid – 50 mg, 100 mg, 300 mg;

Excipients: povidone low-molecular (polyvinylpirrolidone low-molecular medical 12600 + 2700), starch corn, cellulose microcrystallic, magnesium stearate, talc, lactoses monohydrate (sugar milk).

Excipients for receiving a covering: целлацефат (atsetilftaliltsellyuloz), titanium dioxide, castor oil.

Pharmacological properties:

Irreversible inhibition of cyclooxygenase (TsOG-1) therefore synthesis of A2 thromboxane is blocked is the cornerstone of the mechanism of antiagregantny effect of acetylsalicylic acid (ASK) and aggregation of thrombocytes is suppressed. The Antiagregantny effect develops even after use of small doses of drug and remains within 7 days after a single dose. It is considered that ASK has also other mechanisms of suppression of aggregation of thrombocytes.

In high doses of ASK (over 300 mg/) also has antiinflammatory, febrifugal and analgeziruyushchy effect.

Pharmacokinetics. Absorption

After intake of ASK it is quickly and completely soaked up from a GIT. 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 enzymes with formation of such metabolites as salol, salicylic acid a glucuronide 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).

Cmax of ASK in a blood plasma is reached in 10-20 min. after intake, Cmax of salicylic acid – in 0.3-2 h.

Because tablets are covered with an acid resisting cover, ASK is released not in a stomach (the cover effectively blocks dissolution of drug in a stomach), and in the alkaline environment of a duodenum. Thus, absorption of ASK in the form of the tablets covered with a kishechnorastvorimy cover is slowed down on 3-6 h in comparison with usual (without such cover) tablets.

Distribution

ASK and salicylic acid 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 into breast milk.

Removal

Removal of salicylic acid is dozozavisimy as her metabolism is limited by opportunities of enzymatic system. T1/2 makes of 2-3 h at use of ASK in low doses and to 15 h at use of drug in high doses (usual doses of ASK as analgeziruyushchy and an antipyretic). Unlike other salicylates, at multiple dose of drug not hydrolyzed ASK does not collect in blood serum. Salicylic acid and its metabolites are removed by kidneys. At patients with normal function of kidneys of 80-100% of a single dose of drug it is removed by kidneys during 24-72 h.

Indications to use:

— prevention of an acute myocardial infarction with risk factors (for example, a diabetes mellitus, a lipidemia, arterial hypertension, obesity, smoking, advanced age);

— prevention of a repeated myocardial infarction;

— unstable stenocardia;

— prevention of an ischemic stroke (including at patients with passing disturbance of cerebral circulation);

— prevention of a thromboembolism after operations and invasive interventions on vessels (for example, aortocoronary shunting, endarterectomy of carotid arteries, arteriovenous shunting, angioplasty and stenting of coronary arteries, angioplasty of carotid 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:

Pill should be taken before food, washing down with a large amount of liquid, 1 time/days of Atsekardol® is intended for prolonged use. Duration of therapy is defined by the doctor.

Prevention at suspicion of an acute myocardial infarction: 100 mg/days daily or 300 mg every other day (the first tablet needs to be chewed for more bystry absorption).

Prevention for the first time the arisen acute myocardial infarction with risk factors: 100 mg/days daily or 300 mg every other day.

Prevention of a repeated myocardial infarction and unstable stenocardia: 100-300 mg/days daily.

Prevention of an ischemic stroke and passing disturbance of cerebral circulation: 100-300 mg/days daily.

Prevention of a thromboembolism after operations and invasive interventions on vessels: 100-300 mg/days daily.

Prevention of a deep vein thrombosis and thromboembolism of a pulmonary artery and its branches: 100 mg/days or 300 mg every other day.

Features of use:

ASK can provoke a bronchospasm, and also cause attacks of bronchial asthma and other hypersensitivity reactions. Risk factors are existence of bronchial asthma in the anamnesis, hay fever, the polypose of a nose, chronic diseases of respiratory system, and also allergic reactions to other drugs (for example, skin reactions, an itch, urticaria).

The inhibiting effect of ASK on aggregation of thrombocytes remains within several days after reception in this connection increase in risk of bleedings is possible during an operative measure or in the postoperative period. In need of an absolute exception of bleeding during an operative measure it is necessary to refuse, whenever possible, completely use of ASK in the preoperative period.

ASK in low doses can provoke development of gout in the predisposed persons (having reduced excretion of uric acid).

At the combined use of GKS and salicylates it is necessary to remember that during treatment concentration of salicylates in blood is reduced, and after cancellation of GKS the overdose of salicylates is possible.

Exceeding of a dose of ASK is accompanied by risk of gastrointestinal bleeding.

Influence on ability to driving of motor transport and to control of mechanisms

During administration of drug of Atsekardol® it is necessary to be careful at control of vehicles, mechanisms and when performing other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: nausea, heartburn, vomiting, abdominal pains; ulcers of a mucous membrane of a stomach and duodenum; ruptured ulcers of a stomach and duodenum, gastrointestinal bleedings, passing abnormal liver functions with increase in activity of hepatic transaminases.

From system of a hemopoiesis: purpose of ASK is followed by the increased risk of bleedings owing to an inhibiting effect of ASK on aggregation of thrombocytes, anemia.

Allergic reactions: skin rash, a skin itch, a small tortoiseshell, a Quincke's edema, rhinitis, a rhinedema, a cardiorespiratory distress syndrome, and also heavy reactions, including an acute anaphylaxis.

From respiratory system: bronchospasm.

From TsNS: dizziness, decrease in hearing, headache, sonitus.

Interaction with other medicines:

ASK at simultaneous use strengthens effect of the following medicines:

— a methotrexate due to decrease in renal clearance and its replacement from communication with proteins of plasma; also the combination of acetylsalicylic acid to a methotrexate is followed by the increased frequency of development of side effects from bodies of a hemopoiesis;

— heparin and indirect anticoagulants due to dysfunction of thrombocytes and replacement of indirect anticoagulants from communication with proteins of plasma;

— thrombolytic means and antiagregant;

— digoxin owing to decrease in its renal excretion;

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

— valproic acid due to its replacement from communication with proteins of plasma.

ASK combination to anticoagulants, trombolitika and antiagregant is followed by the increased risk of development of bleeding.

At a concomitant use of ASK with alcohol strengthening of toxic effect of alcohol on the central nervous system is observed, the risk of injury of a mucous membrane of digestive tract and lengthening of a bleeding time increases.

ASK at simultaneous use weakens effect of the following medicines:

— uricosuric drugs - a benzbromaron (decrease in uricosuric effect owing to competitive suppression of renal canalicular excretion of uric acid);

— APF inhibitors (dozozavisimy reduction in the rate of glomerular filtering as a result of inhibition of prostaglandins possessing vasodilating action is noted and weakening of hypotensive action is respectively observed);

— diuretics (at combined use with ASK in high doses reduction in the rate of glomerular filtering as a result of decrease in synthesis of prostaglandins in kidneys is noted).

Strengthening elimination of salicylates, system GKS weaken their action.

Contraindications:

— GIT erosive cankers (in an aggravation phase);

— gastrointestinal bleeding;

— hemorrhagic diathesis;

— the bronchial asthma induced by reception of salicylates, a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of ASK;

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

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

— chronic heart failure (the III-IV functional class on NYHA classification);

— a concomitant use of a methotrexate in a dose of 15 mg/week and more;

— I and III trimesters of pregnancy;

— lactation period;

— children's age up to 18 years;

— deficit of lactase, lactose intolerance, glyukozo-galaktozny malabsorption;

— hypersensitivity to ASK.

With care at:

— to gout, a hyperuricemia since ASK in low doses reduces excretion of uric acid; it must be kept in mind that ASK in low doses can provoke development of gout in the predisposed patients (having reduced excretion of uric acid);

— a peptic ulcer of a stomach and a duodenum or gastrointestinal bleedings (in the anamnesis);

— an abnormal liver function (a class A on a scale of Chayld-Pyyu);

— renal failure (KK more than 30 ml/min.);

— bronchial asthma, chronic diseases of a respiratory organs, hay fever, polypose of a nose, medicinal allergy;

— a concomitant use of a methotrexate in a dose less than 15 mg/week;

— the accompanying therapy by anticoagulants;

— II trimester of pregnancy;

— estimated surgical intervention (including small, for example, extraction of tooth) since ASK can cause tendency to development of bleedings within several days after administration of drug.

Use of the drug ATSEKARDOL® at pregnancy and feeding by a breast

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

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

In the III trimester of pregnancy salicylates in a high dose (more than 300 mg/) cause weakening 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 III trimester of pregnancy is contraindicated.

Salicylates and their metabolites in small amounts get into breast milk therefore in the period of a lactation it is necessary to cancel breastfeeding.

Use at abnormal liver functions

It is contraindicated:

— the expressed liver failure (a class B and C on a scale of Chayld-Pyyu).

With care:

— an abnormal liver function (a class A on a scale of Chayld-Pyyu).

Use at renal failures

It is contraindicated:

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

With care:

— renal failure (KK more than 30 ml/min.).

Use for children

Contraindication: age up to 18 years.

Overdose:

The overdose is improbable owing to the low maintenance of ASK in drug. Exceeding of a dose of ASK is accompanied by risk of gastrointestinal bleeding. The overdose is especially dangerous at patients of advanced age.

Overdose symptoms from easy to moderate severity: dizziness, a sonitus, deterioration in hearing, the increased sweating (including profuse), nausea, 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.

Overdose symptoms from average to heavy degree:

— a respiratory alkalosis with a compensatory metabolic acidosis;

— hyper pyrexia (extremely high temperature of a body);

— breath disturbances: hyperventilation, not cardiogenic fluid lungs, respiratory depression, asphyxia;

— disturbances from cardiovascular system: disturbances of a heart rhythm, decrease in the ABP, oppression of cordial activity;

— disturbances of 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. When carrying out an alkaline diuresis it is necessary to achieve values рН between 7.5 and 8. The forced alkaline diuresis should be carried out when concentration of salicylates in plasma makes more than 500 mg/l (3.6 mmol/l) at adults and children have 300 mg/l (2.2 mmol/l).