Зилт

Зилт – antiagregantny means.

Form of release and structure

Dosage form – tablets, film coated: round, slightly biconvex form, pink color, the kernel of a tablet has white or almost white rough structure (on 7 pieces in blisters, in cardboard packs on 2, 4 or 12 blisters).

Active agent – klopidogret hydrosulphate, in 1 tablet – 97,875 mg, or klopidogret – 75 mg.

Auxiliary components: cellulose microcrystallic, lactose anhydrous, starch prezhelatinizirovanny, the castor oil hydrogenated a macrogoal 6000.

Structure of a film cover: propylene glycol, gipromelloz 6cp, talc, titanium dioxide (E171), dye ferrous oxide red (E172).

Indications to use

Zilt's use is shown for prevention of aterotrombotichesky complications at adult patients with cardiovascular pathologies:

• Myocardial infarction (the period from several to 35 days), an ischemic stroke (the period from 7 days to 6 months) or the diagnosed occlusal disease of peripheral arteries;
• Acute coronary syndrome without raising of a segment of ST (a myocardial infarction without formation of a tooth Q or unstable stenocardia), including patients with the carried-out stenting at transdermal coronary intervention, in combination with acetylsalicylic acid;
• Acute coronary syndrome with raising of a segment of ST (an acute myocardial infarction) in case of drug treatment and at a possibility of performing thrombolytic therapy in combination with acetylsalicylic acid.

Besides, drug is appointed for prevention of tromboembolic and aterotrombotichesky episodes (including a stroke) to adult patients with a ciliary arrhythmia (fibrillation of auricles) which cannot accept indirect anticoagulants and which have risk factor of development of vascular complications at insignificant probability of emergence of bleedings, including in a combination with acetylsalicylic acid.

Contraindications

• Heavy abnormal liver function;
• Syndrome of glyukozo-galaktozny malabsorption, lactose intolerance, deficit of lactase;
• Intracraneal hemorrhage, bleeding from a round ulcer and other types of acute bleedings;
• Period of pregnancy and breastfeeding;
• Age up to 18 years;
• Hypersensitivity to drug components.

With care use drug at patients: with a renal failure, moderate abnormal liver functions with predisposition to bleeding; at the injury, surgical intervention and states increasing risk of development of bleeding; with the gastrointestinal, intraocular and other diseases predisposed to development of bleedings; at a concomitant use of TsOG-2 inhibitors and other non-steroidal anti-inflammatory drugs (NPVS), warfarin, heparin or inhibitors of a glycoprotein IIb/IIIa; with low activity of an isoenzyme of CYP2C19 (because of increase in risk of cardiovascular complications); with hypersensitivity to a prazugrel, a tiklopidin and other thienopyridines.

Route of administration and dosage

Pill is taken inside, irrespective of meal.

The recommended dosing for patients with normal activity of an isoenzyme of CYP2C19, including patients of advanced age:

• Myocardial infarction, ischemic stroke or the diagnosed occlusal disease of peripheral arteries: on 75 mg of 1 times a day;
• Acute coronary syndrome without raising of a segment of ST (unstable stenocardia and a myocardial infarction without Q tooth): a load dose – once 300 mg, then on 75 mg of 1 times a day in a combination with acetylsalicylic acid in a dose of 75-325 mg a day. At appointment it is necessary to consider that doses of acetylsalicylic acid higher than 100 mg are accompanied by high risk of bleedings. The therapeutic effect occurs on the 3rd month of treatment, for optimum result it is reasonable to continue use of a klopidogrel up to 12 months;
• Acute myocardial infarction (an acute coronary syndrome with raising of a segment of ST): once load dose, then on 75 mg of 1 times a day in a combination with acetylsalicylic acid and trombolitikam (or without them). It is not recommended to use load doses at treatment of patients 75 years are more senior. Treatment should be begun at emergence of the first symptoms of a disease and to continue not less than 4 weeks;
• Fibrillation of auricles (ciliary arrhythmia): on 75 mg of 1 times a day in a combination with acetylsalicylic acid in a dose of 75-100 mg a day.

Pill is recommended to be taken at the same time, at delay it is less than 12 hours, it is necessary to accept the passed dose and following in usual time, at an interval between receptions more than 12 hours – the next dose without doubling is accepted.

At patients at Zilt's reception in the recommended doses formation of an active metabolite of a klopidogrel happens to genetically caused reduced activity of an isoenzyme of CYP2C19 less and its antiagregantny action is expressed more weakly. Optimum dosing for patients of this category is not established, usually, purpose of drug is made in the raised doses with a single dose of a load dose 600 mg and then on 150 mg of 1 times a day.

Dose adjustment is not required to patients of advanced age.

Side effects

• From cardiovascular system: often – a hematoma; very seldom – arterial hypotension, a vasculitis;
• From system of a hemopoiesis: infrequently – a leukopenia, thrombocytopenia, an eosinophilia; seldom – a neutropenia, including severe forms; very seldom – aplastic anemia, the trombotichesky Werlhof's disease (TWD), a pancytopenia, heavy thrombocytopenia, an agranulocytosis, anemia, a granulocytopenia;
• From the alimentary system: often – an abdominal pain, gastrointestinal bleeding, diarrhea, dyspepsia; infrequently – nausea, vomiting, a lock, gastritis, a meteorism, stomach ulcer and/or a duodenum; seldom – a retroperitoneal hemorrhage; very seldom – pancreatitis, retroperitoneal and gastrointestinal bleedings (including with a lethal outcome), colitis (including lymphocytic), an acute liver failure, hepatitis, functional disturbances of indicators of a liver, stomatitis;
• From a nervous system: infrequently – a headache, intracraneal hemorrhages (including with a lethal outcome), dizziness, paresthesias; very seldom – confusion of consciousness, a hallucination;
• From a musculoskeletal system: very seldom – a hemarthrosis, hemorrhages in muscles, arthritis, a mialgiya, an arthralgia;
• From respiratory system: often – nasal bleeding; very seldom – a bronchospasm, bleeding from respiratory tracts (pulmonary bleedings, a pneumorrhagia), an intersticial pneumonitis;
• From urinogenital system: infrequently – a hamaturia; very seldom – a glomerulonephritis, increase in level of concentration of creatinine in blood serum;
• From integuments: often – hypodermic hematomas; infrequently – a skin itch, rash, skin hemorrhages (purpura); very seldom – violent dermatitis (Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a mnogoformny erythema), urticaria, erythematic rash, flat deprive, eczema;
• From sense bodys: infrequently – retinal or conjunctival hemorrhages; seldom – вертиго; very seldom – flavoring pathologies;
• Laboratory indicators: often – reduction of quantity of thrombocytes and neutrophils, lengthening of the period of bleeding;
• Allergic reactions: very seldom – eczema, a Quincke's disease, anaphylactoid reactions, a serum disease; frequency is unknown – medicinal rash with system symptoms of DRESS syndrome and an eosinophilia, cross and reactive hypersensitivity to thienopyridines, a syndrome of the hypersensitivity induced by drugs;
• Others: often – vascular bleeding in the place of puncturation; very seldom – severe bleeding from an operational wound, fever.

Special instructions

Use of drug is connected with risk of development of bleedings and the undesirable hematologic phenomena therefore treatment needs to be accompanied with systematic control regarding symptoms of bleedings, especially at the beginning of reception of a klopidogrel, and also after surgical interventions or invasive cardiological procedures. In case of clinical signs of possible bleeding the patient should carry out blood test with determination of quantity and indicators of function of thrombocytes, the activated partial tromboplastinovy time (APTT) and some other necessary researches.

Purpose of drug is not recommended to patients with an acute ischemic stroke at prescription less than 7 days.

Drug extends time of bleedings, it needs to be considered at simultaneous use with acetylsalicylic acid, NPVS, IIb/IIIa glycoprotein inhibitors, heparin and warfarin.

Patients are recommended to be inspected regarding hypersensitivity to a tiklopidin, a prazugrel and other thienopyridines as cross and reactive hypersensitivity between drugs of this group is possible. At the instruction in the anamnesis of the patient on hypersensitivity to other thienopyridines it has to be observed carefully during therapy for the purpose of identification of symptoms of hypersensitivity to a klopidogrel.

By training the patient for planned surgery, Zilt's use needs to be cancelled in 5-7 days.

The patient has to be warned about a possibility of longer bleedings during treatment and about need to inform the attending physician of each case of bleeding. On reception at other doctors it is always necessary to report about reception of a klopidogrel, this information is important both at purpose of new medicines, and at a visit to the stomatologist.

Against the background of Zilt's use development of a trombotichesky Werlhof's disease of which the thrombocytopenia and mikroangiopatichesky hemolitic anemia associated with a renal failure, neurologic disturbances and fever are characteristic is possible. This state demands the emergency medical care, including a plasma exchange.

Treatment should be carried out at control of function of a liver as at heavy functional disturbances development of hemorrhagic diathesis is possible.

Content in drug of the castor oil hydrogenated can cause diarrhea and a gastric disturbance.

Drug does not influence ability of the patient to control of vehicles and mechanisms and performance of other potentially dangerous types of activity demanding the high speed of psychomotor reactions and concentration of attention.

Medicinal interaction

Due to the high risk of bleeding it is not recommended to appoint drug along with warfarin, and at a combination to heparin and other thrombolytic means it is necessary to observe extra care.

NPVS increase risk of development of ulcers and ulcer bleedings in digestive tract.

Clinically significant interaction it is not revealed at simultaneous use with atenololy, the inhibitors of an angiotensin-converting enzyme (APF), drugs reducing the content of cholesterol in blood, digoxin, nifedipine, phenobarbital, estrogen, Cimetidinum, theophylline.

Klopidogrel can increase effect of acetylsalicylic acid on the aggregation of thrombocytes induced by collagen. Pharmakodinamichesky interaction of drug with acetylsalicylic acid increases probability of bleeding therefore use of this combination is possible only during 1 year.

Antiacid means do not exert impact on absorption of a klopidogrel.

The combination to Tolbutamidum, Phenytoinum increases the level of their concentration in a blood plasma.

Terms and storage conditions

To store at a temperature up to 25 °C. To protect from children.

Period of validity – 3 years.