Koplaviks

Коплавикс Drug photo

The description is actual on 23.12.2015

  • Latin name: Coplavix
  • ATH code: B01AC30
  • Active ingredient: Acetylsalicylic acid, Klopidogrel (Acetylsalicylic acid, Clopidogrel)
  • Producer: Sanofi-Winthrop Industrie (France)

Structure

Tablets of Koplaviks of 100 mg 75 mg contain 100 mg of acetylsalicylic acid and 97,8 mg of a klopidogrel of hydrosulphate (form II) that in terms of klopidogret makes 75 mg.

List of auxiliary connections

  • Are making kernels: 68,9 mg of Mannitolum, 34 mg of a macrogoal 6000, 144,7 mg of MKTs, 19,6 mg of the low-substituted hypro rod, 3,3 mg of the hydrogenated castor oil, 1,16 mg of stearic acid, 0,63 mg of colloid silicon dioxide, 11,1 mg of corn starch.
  • Pink Opadry are a part of a film cover: monohydrate of lactose, gipromelloz, titanium dioxide (E171), triacetin, and also 20 mg of dye of red iron oxide (E172) and trace amount of karnaubsky wax.

Release form

Tablets have film the covered in the form of a cover, oval biconvex form, light pink color and engravings of "C75" and "A100" from the different parties. Koplaviks No. 100 is issued in blisters according to 10 tab., besides there are packagings No. 7, 14, 28 where tablets are packed into cellular packagings on 7 pieces.

Pharmacological action

Anti-aggregation action is characteristic of drug.

Pharmacodynamics and pharmacokinetics

Biochemical effects and physiological action of a kopidogrel

Klopidogrel so-called pro-medicine as one of metabolites which turns by means of system of isoenzymes of P450 cytochrome and possesses the inhibiting properties in relation to aggregation of thrombocytes is active. The mechanism of action is based on the selection inhibition of ADF and irreversible linkng with ADF-receptors of thrombocytes, and also the subsequent activation of a complex of a glycoprotein of IIb/IIIa under the influence of ADF that also suppresses ADF-indutsiruyemuyu aggregation of thrombocytes. Thanks to irreversible communication normal function of thrombocytes is recovered with a speed which corresponds to the individual speed of updating of platelets.

Daily reception of a klopidogrel in a dose of 75 mg gives the essential suppression ADF-indutsirovannoy of aggregation of platelets (thrombocytes) increasing in 3–7 days from the 1st day. Achievement of an equilibrium state suppresses aggregation of thrombocytes steadily for 40–60%. The therapeutic effect disappears 5 days later after drug withdrawal.

Data on influence on a human body of acetylsalicylic acid (ASK)

Effect of acetylsalicylic acid differs from effects of a klopidogrel and supplements (but, does not change) its mechanism of antiagregantny influence due to irreversible suppression tsiklookigenazy-1, and as a result – decrease in secretion of A2 thromboxane — known as the inductor of vasoconstriction and aggregation of thrombocytes. It is established that klopidogret it is capable to strengthen influence of acetylsalicylic acid on collagen - the induced aggregation of thrombocytes.

The combination klopidogret with ASK

  • prevents development of an aterotromboz, including at such arrangement of the centers of atherosclerotic defeat as: cerebral, coronary or peripheral arteries;
  • decrease in risk of a myocardial infarction, stroke (mainly at patients with fibrillation of the auricles having risk factors of emergence of vascular complications);
  • decrease in total quantity of days of hospitalization in connection with cardiovascular pathology.

Pharmacokinetic characteristics

  • Process of absorption of 75 mg of a klopidogrel happens in intestines quickly enough – achievement of the maximum concentration in the amount of 2,2–2,5 ng/ml requires only 45 min. Absorption makes about 50%. While for achievement of the maximum concentration of ASK there have to pass not less than 1 hour as it gives in to hydrolysis and turns into salicylic acid and in 1,5–3 h Koplaviks in blood even in trace concentration it is not found.
  • The metabolism of a klopidogrel is intensive and occurs in a liver to an intermediate metabolite — 2-oxo-klopidogrela, and then transformation goes on 2 metabolic ways – 85% by means of esterases before education inactive derivative carboxyl acid, the others — by means of some isoenzymes of system of haemo proteins (Tsitokhromr450) give active tiolny derivative klopidogret. Salicylic acid mainly is exposed to conjugation in a liver to salitsilurovy acid, phenolic and acylic glucuronides and other minor metabolites.
  • Removal of a klopidogrel to last for 120 h – about 50% kidneys and 46% intestines. ASK elimination half-life in drug of Koplaviks makes about 2 h.

Indications to use

The prevention of aterotrombotichesky complications at patients with the acute coronary syndrome (ACS)

  • if on an ECG raising of the ST segment is not observed, unstable stenocardia is established, the myocardial infarction (the tooth of Q is absent) is postponed, was the stent at puncture coronary intervention is established;
  • if on an ECG there is a raising of the ST segment (at an acute myocardial infarction) and perhaps drug treatment and carrying out a thrombolysis.

The prevention of aterotrombotichesky or tromboembolic episodes (after a stroke, fibrillation of auricles, a ciliary arrhythmia)

  • appoint to patients with existence even of 1 risk factor of emergence of vascular complications;
  • low probability of development of bleedings and impossibility of use of indirect anticoagulants.

Contraindications

  • heavy degree of a liver failure — over 9 points on Chayld-Pyyu;
  • heavy degree of a renal failure with decrease in clearance of creatinine to 30 ml/min. and below;
  • acute bleedings, for example, intracraneal hemorrhage;
  • bronchial asthma or its syndrome induced by salicylates, NPVP;
  • syndrome of the rhinitis recuring a polypose of the nasal courses, okolonosovy bosoms;
  • mastocytosis;
  • disturbance of portability of a galactose, deficit of lactase, sprue of glucose and galactose;
  • pregnant women and the feeding patients;
  • safety and efficiency of use in pediatrics are not established;
  • hypersensitivity to any of the making drug substances, and also NPVP.

Appointment and use with care

  • liver failure of moderate degree — 7-9 points on Chayld-Pyyu;
  • easy and moderate severity of a renal failure;
  • predisposition to bleedings (the patients with a peptic ulcer of a stomach and a 12-perstny gut who had gastrointestinal bleeding, having manifestations of disturbances of work of upper parts of a gastrointestinal tract);
  • to the patients who had injuries, invasive cardiological procedures, surgical interventions (in 5-7 days klopidogret it is recommended to cancel);
  • passing disturbances of cerebral circulation, ischemic stroke;
  • therapy of NPVP, the selection TsOG-2 inhibitors, Warfarin, Heparin, inhibitors of a glycoprotein of IIb and IIIA, the selection inhibitors of the return capture of molecules of serotonin, thrombolytic drugs;
  • hyperuricemia;
  • gout;
  • to patients with genetically caused reduced activity of an isoenzyme of CYP2D9.

Side effects

  • From blood: decrease in quantity of thrombocytes, neutrophils in a peripheral blood-groove, heavy thrombocytopenia, a leukopenia, a granulocytopenia, a neutropenia, an eosinophilia, lengthening of bleedings, aplastic or hemolitic anemia, an agranulocytosis, a pancytopenia, a bitsitopeniya, the acquired hemophilia, a Werlhof's disease.
  • From peripheral and central NANOSECOND: headache, dizziness, paresthesia, vertigo, change of perception of taste.
  • From acoustic organs: noise or hearing loss.
  • From a gastrointestinal tract: gastric and intestinal bleedings, indigestion, abdominal pains, diarrhea, nausea, meteorism, gastritis, lock, vomiting, ulcer, colitis, gastritis, esophagitis, duodenitis, pancreatitis, stomatitis, ultseration or perforation of a gullet, gastralgia, perforation of intestines.
  • From a liver, zhelchevyvodyashchy ways: hepatitis, the acute hepatic unsufficiency raised activities of "hepatic" enzymes, hepatocellular damage of a liver.
  • From skin: rash, an itch, eczema, makulezno-papular, exfoliative, erythematic skin rash, the small tortoiseshell, violent dermatitis (a mnogoformny erythema, a toxic necrolysis of epidermis Stephens and Johnson's syndrome), acute exanthematous pustulez, flat deprive.
  • Immune response: anaphylactoid reactions, development of a serum disease, hypersensitivity cross-reactions with other thienopyridines (for example: Tiklopidin, Prazugrel), strengthening of food allergy, acute anaphylaxis.
  • Disturbances from mentality: confusion of consciousness and hallucination.
  • CCC: vasculitis, decrease in the ABP, purple Shenleyn-Genokh, Kounis's syndrome.
  • Bodies of respiratory system, mediastinum and thorax: bronchospasm, eosinophilic pneumonia, intersticial pneumonitis, development of not cardiogenic fluid lungs.
  • Musculoskeletal system: arthralgia, arthritises, mialgiya.
  • Kidneys and urinary tract: glomerulopatiya, glomerulonephritis, acute functional disorders, renal failure.
  • Reproductive system: gynecomastia.
  • Metabolism: hypoglycemia, gout.
  • The general: fever.

Koplaviks, application instruction (Way and dosage)

Take a pill of Koplaviks orally inside, once a day, regardless of a diet and a diet.

The scheme of treatment for adult and elderly patients with the normal level of activity of an isoenzyme CYP2C19

  • At the acute coronary syndrome (ACS) therapy is begun right after the first symptoms. At first use load doses of separate drugs — 300 mg of a klopidogrel and 75–325 mg of ASK.
  • To the elderly patients who had an acute myocardial infarction, having on an ECG raising of the ST segment therapy carry out without initial load dose of a klopidogrel and not less than 4 weeks carry out treatment by Koplaviks. In general, duration of treatment is defined individually, at most in clinical trials – 12 months.
  • At fibrillation of auricles separate load doses of a klopidogrel and ASK in the amount of 75 mg and 100 mg respectively, then therapy by Koplaviks – reception of tablets are recommended once a day.

The scheme of treatment of patients with the reduced level of activity of an isoenzyme CYP2C19

In connection with reduced antiagregantny influence of a klopidogrel to such patients appoint higher doses of a klopidogrel. Begin with load 600 mg of a klopidogrel, the daily dose in 150 mg is recommended further.

Attention! There are tests thanks to which it is possible to define a genotype of CYP2C19 and according to it to develop the most optimum therapeutic strategy.

Overdose

Clinical picture of reception of superdoses of a klopidogrel

Increase in a bleeding time and the subsequent complications in the form of higher probability of bleedings.

The undertaken measures: the antidote does not exist, transfusion of a platelet concentrate and other standard receptions when developing bleeding.

Clinical picture of reception of superdoses of ASK

At moderate extent of overdose (since plasma concentration over 300 mg/l) there is dizziness, a headache, in the ears dins, confusion of consciousness and dispeptic disturbances is observed. At children – the heavy hypoglycemia and potentially fatal poisoning is possible.

At heavy intoxication heavy deviations of acid-base balance are observed: at first there is a hyperventilation and a respiratory alkalosis, further — a respiratory acidosis as result of an inhibiting effect on a respiratory center of a respiratory alkalosis, and in blood — a metabolic acidosis. There are symptoms of a hyperthermia, plentiful sweating that conducts to dehydration, motive concern, spasms, hallucinations and a hypoglycemia. Owing to oppression of a nervous system development of a coma, a collapse and a full apnoea is possible.

The undertaken measures for treatment:

  • hospitalization;
  • induction of vomiting, in case of failure — a gastric lavage;
  • absorbent carbon or other adsorbents, and also salt laxatives;
  • for the forced alkalization of urine and the accelerated removal of salicylates appoint in/in kapelno 250 milimol bicarbonate sodium for 3 h with a constant control rn urine;
  • the hemodialysis or peritoneal dialysis is recommended to patients in a serious condition;
  • symptomatic treatment of other displays of intoxication.

Interaction

  • Simultaneous treatment with indirect anticoagulants (peroral) or Varfaron can increase probability of bleedings because of independent influence of each of drugs on a hemostasis therefore — similar combinations are undesirable.
  • Parallel treatment by Koplaviks and Naproxenum, and also NPVS, TsOG-2 inhibitors as it leads to increase in the hidden blood losses through a gastrointestinal tract is not recommended.
  • Systematic use of the Ibuprofen, conducts to inhibition of antiagregantny effect of ASK (in low doses) whereas irregular reception of the Ibuprofen – has no similar clinically significant effect.
  • With drugs of selective return capture of molecules of serotonin disturbance of activation of thrombocytes and increase in probability of bleedings is observed.
  • ASK is capable to suppress effect of the uricosuric drugs promoting removal from an organism of uric acid, for example: Benzbromarona, Probenetsida, Sulfinpyrazonum.
  • Simultaneous treatment by the Methotrexate in a dose from 20 mg/week leads to reduction of its renal clearance, and in turn — strengthens myelotoxic influence.
  • Metamizol reduces antiagregantny action of ASK.
  • Salicylates with Acetazoleamide apply with care as their combination increases probability of emergence of a metabolic acidosis.
  • The systematic use of etanolsoderzhashchy products, for example, the chronic use of large amounts of alcohol in a combination with ASK increases risk of bleedings.

Terms of sale

Attributing Koplaviks, the doctor has to issue the recipe.

Storage conditions

Temperature condition has to be sustained: to +25 ° Celsius.

Children and domestic animals should not have access to medical supplies.

Period of validity

It can be stored till 2 flyings.

Special instructions

The doctor has to notify the patient about increases in risk and duration of bleedings.

Before any surgical intervention, use of new medicines, visit of the stomatologist, patients have to inform on treatment by Koplaviks.

Koplaviks's analogs

  • tablets Lopirel (the producer Aktavis, Iceland, the average price of packaging No. 28 – 530-550 rubles);
  • tablets Listab (the producer Replekfarm, Macedonia, the average price of packaging No. 14 – 220-250 rubles);
  • tablets of Plaviks (the producer Sanofi-Aventis, France, the average price of packaging No. 28 – 2580-2700 rubles).

Zdravzona

  • Koplaviks 100 mg +75mg tablet No. 28
  • Koplaviks 100 mg +75mg tablet No. 14
  • Koplaviks 100 mg +75mg tablet No. 100

Drugstore of IFC

  • Koplaviks tbl p/pl/o 100 mg +75mg No. 28, Sanofi-Winthropfrantion
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Section: For blood
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Education: Graduated from the Nikolaev national university of V. A. Sukhomlinsky, gained the diploma of the specialist with honors as "An embryologist, a cytologist, a histologist". Also, the human physiology and animals, the teacher of biology" graduated from a magistracy majoring in ". The course on discipline "Pharmacology" is with honors passable.

Experience: Worked as the senior laboratory assistant of department of Physiology and biochemistry of the Nikolaev national university of V. A. Sukhomlinsky in 2010 - 2011.

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