Atrogrel

General characteristics. Structure:

Active ingredient: clopidogrel; 1 tablet contains a klopidogrel in the form of a klopidogrel of bisulphate of 75 mg;
excipients: sodium of a kroskarmeloz, cellulose microcrystallic, lactoses monohydrate, magnesium stearate, plenochnoobrazuyushchy covering. Main physical and chemical properties:
Tablets of a round form with a biconvex surface, coated pink color. On cross section the kernel surrounded with a cover layer is visible.

Pharmacological properties:

Pharmacodynamics.
Klopidogrel selectively inhibits linkng of adenosinediphosphate (ADF) with his receptors on a surface of thrombocytes, blocks activation of thrombocytes and thus oppresses them aggregation. Inhibits also the aggregation of thrombocytes caused by other agonists. Braking of aggregation of thrombocytes is observed in 2 h after oral administration of a single dose of drug. At repeated use the effect amplifies, and the stable state is reached in 3–7 days of treatment (the average level of braking of aggregation makes 40-60%). Aggregation of thrombocytes and a bleeding time are returned to initial level on average in 7 days after drug phase-out, in process of updating of thrombocytes.

Pharmacokinetics.
After oral administration drug is quickly soaked up from digestive tract. Its concentration in a blood plasma insignificant and after use is not defined by 2 h (less than 0,025 mkg/l). It biotransformirutsya quickly in a liver. Its main metabolite (85% of the connection circulating in plasma) is inactive. An active tiolny metabolite quickly it is also irreversible contacts receptors of thrombocytes. In a blood plasma it is not found. Klopidogrel and the main circulating metabolite reversibly contact proteins of plasma.
After oral administration about 50% of the accepted dose are allocated with urine and 46% with a stake during 120 h after use. The elimination half-life of the main metabolite makes 8 h.
Concentration of the main metabolite in plasma at patients of advanced age (75 years are also more senior) much higher, however higher concentration in plasma are not followed by changes in aggregation of thrombocytes and a bleeding time.

Indications to use:

• Prevention of ischemic disturbances (a myocardial infarction, an ischemic stroke, sudden coronary death, thrombosis of peripheral arteries) at patients with atherosclerosis;
• prevention of a repeated myocardial infarction and ischemic stroke.

Route of administration and doses:

Drug is accepted orally on 1 tablet (75 mg) of 1 times a day irrespective of meal.
The patient with an acute coronary syndrome without ST segment elevation (unstable stenocardia or a myocardial infarction without pathological tooth of Q on an ECG) in the first day of treatment – 4 tablets (300 mg), in the next days – on 1 tablet of 1 times a day irrespective of meal.
Duration of treatment is determined by the doctor depending on a clinical picture of a disease.

Features of use:

With care appoint the patient with the increased risk of bleeding owing to an injury, operative measures, disturbance of system of a hemostasis. At the planned surgical interventions (if antiagregantny action is undesirable) the course of treatment drug should be stopped in 7 days prior to operation.
With care appoint the patient with heavy abnormal liver functions at which developing of hemorrhagic diathesis is possible.
Dose adjustment is not required for patients of advanced age, patients with a renal failure.
Patients should be warned that as the stop of the bleeding arising against the background of drug use demands bigger time, they have to report to the doctor about each case of unusual bleeding. Patients also have to inform the doctor on administration of drug if operative measures are coming them (surgery, stomatology, etc.) or if the doctor appoints medicine, new to the patient.
At emergence of symptoms of excessive bleeding (bleeding of gums, menorrhagias, a hamaturia) the research of system of a hemostasis (a bleeding time, quantity of thrombocytes, tests of functional activity of thrombocytes) is shown. Regular control of laboratory indicators of function of a liver is recommended.

Ability to influence speed of response at control of motor transport or other mechanisms.
Drug does not influence ability to manage motor transport and does not reduce the speed of psychomotor reactions.

Use during pregnancy or feeding by a breast.
Use of drug during pregnancy is contraindicated.
In need of use of drug during feeding by a breast feeding should be stopped.

Children.
Safety and efficiency of drug at persons aged up to 18 years are not established.

Side effects:

From system of blood: leukopenia, reduction of quantity of neutrophylic and eosinophilic granulocytes, lengthening of a bleeding time and decrease in quantity of thrombocytes. Very seldom: Werlhof's trombogemolitichesky disease, heavy thrombocytopenia, granulocytopenia, agranulocytosis, anemia and aplastic anemia / pancytopenia. Bleedings of various localization. The majority of cases of bleeding noted during 1 – го month of treatment.
From digestive tract: abdominal pains, dyspepsia, diarrhea; seldom – a lock, an exacerbation of stomach ulcer and a duodenum.
From a musculoskeletal system: very seldom – an arthralgia, arthritis.
From an urinary system: very seldom – a glomerulonephritis, increase in level of creatinine in blood serum.
From the central nervous system: headache, dizziness, parasthesias. Very seldom – confusion of consciousness, a hallucination, disturbance of flavoring feelings.
Allergic reactions: skin rashes, anaphylactoid reactions.
Others: very seldom - fever.

Interaction with other medicines:

Klopidogrel increases risk of developing of gastrointestinal bleedings against the background of use of non-steroidal anti-inflammatory drugs.
Combined use with warfarin is not recommended as strengthening of intensity of bleeding is possible.
Simultaneous use with acetylsalicylic acid or with heparin does not influence antiagregantny effect of drug, however safety of prolonged use of such combinations is not established yet therefore simultaneous use of these drugs demands care.
At combined use with Phenytoinum and Tolbutamidum increase in their level in a blood plasma is possible. However their combined use with klopidogrely is safe.
Clinically significant interaction of drug with diuretics is noted,
β-adrenoblockers, APF inhibitors, blockers of calcium channels, antacids, hypoglycemic, gipokholesterinemichesky and gormonozameshchayushchy drugs, antiepileptic means, phenobarbital, Cimetidinum, digoxin and theophylline.

Contraindications:

• Hypersensitivity to drug;
• serious illness of a liver;
• acute bleedings (intracraneal hemorrhages) and diseases contributing to their development (a peptic ulcer of a stomach and duodenum in aggravation stages, nonspecific ulcer colitis);
• age up to 18 years.

Overdose:

Symptoms. Lengthening of a bleeding time is possible.
Treatment: In need of bystry correction of rheological properties of blood pour a platelet concentrate.

Storage conditions:

To store in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 1 or on 3 blisters in a pack.