Coplavix tabs 100mg + 75mg #100

Instruction for Coplavix

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Composition

Coplavix 100 mg 75 mg tablets contain 100 mg of acetylsalicylic acid and 97.8 mg of clopidogrel hydrogen sulfate (Form II), which, in terms of clopidogrel, is 75 mg.
List of auxiliary connections
    The constituents of the core are: 68.9 mg mannitol, 34 mg macrogol 6000, 144.7 mg MCC, 19.6 mg low-substituted giprolose, 3.3 mg hydrogenated castor oil, 1.16 mg stearic acid, 0.63 mg colloidal silicon dioxide , 11.1 mg of corn starch.
    The film shell of the pink Opadry includes lactose monohydrate, hypromellose, titanium dioxide (E171), triacetin, as well as 20 mg of red iron oxide (E172) and a trace amount of carnauba wax.

Form of issue

The tablets are film coated in the form of a shell, an oval biconvex form, light pink color and engraving "C75" and "A100" from different sides. Coplavix number 100 is produced in blisters for 10 tables, in addition there are packages No. 7, 14, 28, where the tablets are packed in cellular packs of 7 pcs.

pharmachologic effect

The drug is characterized by anti-aggregation effect.

Pharmacodynamics and pharmacokinetics

Biochemical effects and physiological effect of copyadogrel
Clopidogrel is a so-called prodrug, since one of the metabolites is active, which is converted by the cytochrome P450 isoenzyme system and has inhibitory properties with respect to platelet aggregation. The mechanism of action is based on selective inhibition of ADP and irreversible binding to ADP-receptors of platelets, as well as subsequent activation of the glycoprotein IIb / IIIa complex under the influence of ADP, which also suppresses ADP-induced platelet aggregation. Due to the irreversible connection, the normal function of platelets is restored at a rate that corresponds to the individual rate of platelet renewal.
Daily use of clopidogrel at a dose of 75 mg gives, from the first day, a significant suppression of ADP-induced aggregation of blood platelets (platelets), increasing after 3-7 days. Achieving the equilibrium state suppresses platelet aggregation stably by 40-60%. The therapeutic effect disappears after 5 days after drug discontinuation.
Data on the effect on the human body of acetylsalicylic acid (ASA)
The effect of acetylsalicylic acid differs from the effects of clopidogrel and supplements (but does not change) its mechanism of antiaggregant effect due to irreversible inhibition of cyclooquagenase-1, and as a consequence - a decrease in the secretion of thromboxane A2, known as an induction vasoconstriction and platelet aggregation. It was found that clopidogrel is able to enhance the effect of acetylsalicylic acid on collagen-induced platelet aggregation.
Combination of clopidogrel with ASA
    prevents the development of atherothrombosis, incl. with such an arrangement of foci of atherosclerotic lesion as: cerebral, coronary or peripheral arteries;
    reduction in the risk of myocardial infarction, stroke (mainly in patients with atrial fibrillation who have risk factors for vascular complications);
    decrease in the total number of days of hospitalization due to cardiovascular pathology.

Pharmacokinetic characteristics

    The process of absorption of 75 mg of clopidogrel takes place in the intestine quite quickly - to reach a maximum concentration of 2.2-2.5 ng / ml, only 45 minutes are needed. Absorption is approximately 50%. While to achieve the maximum concentration of ASA should pass at least 1 hour, as it lends itself to hydrolysis and turns into salicylic acid and after 1.5-3 h of Coplavix in the blood even in trace concentrations is not detected.
    The metabolism of clopidogrel is intense and occurs in the liver to the intermediate metabolite - 2-oxo-clopidogrel, and then the conversion takes place in 2 metabolic pathways - 85% with the help of esterases to the formation of an inactive carboxylic acid derivative, the rest - with some isoenzymes of the hemoprotein system (Cytochrome P450) active thiol clopidogrel derivative. Salicylic acid is mainly subjected to conjugation in the liver to salicyluric acid, phenolic and acyl glucuronides and other secondary metabolites.
    Excretion of clopidogrel lasts for 120 hours - approximately 50% by the kidneys and 46% by the intestine. The half-life of ASA in Coplavix is ​​about 2 hours.

Indications for use

Prevention of atherothrombotic complications in patients with acute coronary syndrome (ACS)
    if ECG elevation is not observed, unstable angina is established, myocardial infarction is transferred (Q tooth is absent), stent was established with puncture coronary intervention;
    if the ECG has a rise in the ST segment (with acute myocardial infarction) and possibly drug treatment and thrombolysis.
Prevention of atherothrombotic or thromboembolic complications (after stroke, atrial fibrillation, atrial fibrillation)
    prescribe to patients with the presence of even 1 risk factor for the occurrence of vascular complications;
    low probability of bleeding and the inability to use indirect anticoagulants.

Contraindications

    severe degree of hepatic insufficiency - over 9 points on Child-Pugh;
    severe renal failure with a decrease in creatinine clearance to 30 ml / min and below;
    acute bleeding, for example, intracranial hemorrhage;
    The bronchial asthma or its syndrome induced by salicylates, NSAIDs;
    syndrome of rhinitis, recurrent polyposis of nasal passages, paranasal sinuses;
    mastocytosis;
    violation of galactose tolerance, lactase deficiency, glucose malabsorption syndrome and galactose;
    pregnant and lactating patients;
    safety and efficacy in pediatrics have not been established;
    hypersensitivity to any of the constituent substances of the drug, as well as NSAIDs.

Intended use and use with caution

    hepatic failure of moderate degree - 7-9 points on Child-Pugh;
    light and moderate severity of renal failure;
    predisposition to bleeding (patients with peptic ulcer of stomach and duodenum, who underwent gastrointestinal bleeding, with manifestations of upper gastrointestinal disorders);
    patients who have suffered injuries, invasive cardiac procedures, surgical interventions (it is recommended to cancel clopidogrel 5-7 days);
    transient disorders of cerebral circulation, ischemic stroke;
    therapy with NSAIDs, selective COX-2 inhibitors, Warfarin, Heparin, glycoprotein IIb and IIIa inhibitors, selective serotonin reuptake inhibitors, thrombolytic agents;
    hyperuricemia;
    gout;
    patients with genetically determined reduced activity of the isoenzyme CYP2D9.

Side effects

    On the part of the blood: a decrease in the number of platelets, neutrophils in the peripheral blood stream, severe thrombocytopenia, leukopenia, granulocytopenia, neutropenia, eosinophilia, lengthening of bleeding, aplastic or hemolytic anemia, agranulocytosis, pancytopenia, bicitopenia, acquired hemophilia, thrombocytopenic purpura.
    From the side of the peripheral and central HC: headache, dizziness, paresthesia, vertigo, change in perception of taste.
    From the organs of hearing: noise or loss of hearing.
    Gastrointestinal: gastrointestinal and intestinal bleeding, indigestion, abdominal pain, diarrhea, nausea, flatulence, gastritis, constipation, vomiting, ulcer, colitis, gastritis, esophagitis, duodenitis, pancreatitis, stomatitis, ulceration or perforation of the esophagus, gastralgia, intestinal perforation.
    From the liver, bile ducts: hepatitis, acute liver failure, increased activity of "liver" enzymes, hepatocellular liver damage.
    Skin: rash, itching, eczema, maculopapular, exfoliative, erythematous skin rash, hives, bullous dermatitis (erythema multiforme, toxic epidermal necrosis of Stevens and Johnson syndrome,), acute exanthematous pustulosis, flat lichen.
    Immune response: anaphylactoid reactions, development of serum sickness, cross-reactivity of hypersensitivity with other thienopyridines (eg: Ticlopidine, prasugrel), increased food allergy, anaphylactic shock.
    Disorders from the psyche: confusion and hallucinations.
    CCC: vasculitis, a decrease in blood pressure, purple Shenlaine-Genocha, the syndrome of Kounis.
    Organs of the respiratory system, mediastinum and thorax: bronchospasm, eosinophilic pneumonia, interstitial pneumonitis, development of non-cardiogenic pulmonary edema.
    Musculoskeletal: arthralgia, arthritis, myalgia.
    Kidneys and urinary tract: glomerulopathy, glomerulonephritis, acute functional disorders, renal insufficiency.
    Sexual system: gynecomastia.
    Metabolism: hypoglycemia, gout.
    General: fever.

Coplavix, instructions for use (Method and dosage)

Take Coplavix tablets orally inwards, once a day, regardless of diet and diet.
Treatment regimen for adults and elderly patients with a normal level of activity of the isoenzyme CYP2C19
    In acute coronary syndrome (ACS), therapy is started immediately after the first symptoms. First, loading doses of individual drugs are used - 300 mg clopidogrel and 75-325 mg ASA.
    Elderly patients who underwent an acute myocardial infarction who had an ST-segment elevation on the ECG were treated without the initial loading dose of clopidogrel and treated with Coplavix at least 4 weeks. In general, the duration of treatment is determined individually, the maximum in clinical trials is 12 months.
    In atrial fibrillation, separate loading doses of clopidogrel and ASA are recommended in the amount of 75 mg and 100 mg respectively, then therapy with Coplavix - taking the tablets once a day.
Scheme of treatment of patients with a reduced level of activity of the isoenzyme CYP2C19
In connection with the decreased antiplatelet effect of clopidogrel, these patients are prescribed higher doses of clopidogrel. Begin with loading 600 mg clopidogrel, further recommended daily dose of 150 mg.
Attention! There are tests that help determine the genotype of CYP2C19 and, in accordance with this, develop the most optimal therapeutic strategy.

Overdose

Clinical picture of overdoses of clopidogrel
Increased bleeding time and subsequent complications in the form of a higher probability of bleeding.
Measures taken: antidote does not exist, transfusion of platelet mass and other standard methods in case of bleeding.
The clinical picture of overdoses of ASA
With a moderate degree of overdose (starting with a plasma concentration of more than 300 mg / l), dizziness, headache, ringing in the ears, confusion and dyspeptic disorders are observed. In children, severe hypoglycemia and potentially fatal poisoning are possible.
In severe intoxication severe abnormalities of the acid-base balance are observed: first there is hyperventilation and respiratory alkalosis, then - respiratory acidosis as a result of the inhibitory effect on the respiratory center of respiratory alkalosis, and in the blood - metabolic acidosis. There are symptoms of hyperthermia, profuse sweating, which leads to dehydration, motor anxiety, convulsions, hallucinations and hypoglycemia. Due to the oppression of the nervous system, the development of coma, collapse and complete stop of breathing.

Measures taken to treat:

    hospitalization;
    induce vomiting, in case of failure - gastric lavage;
    Activated carbon or other adsorbents, as well as salt laxatives;
    for forced urine alkalinization and accelerated salicylate elimination, 250 mM sodium bicarbonate is administered intravenously dropwise for 3 hours with a constant pH control of urine;
    patients in serious condition are recommended hemodialysis or peritoneal dialysis;
    symptomatic treatment of other manifestations of intoxication.

Interaction

    Simultaneous treatment with indirect anticoagulants (oral) or Warfaron may increase the chance of bleeding due to the independent effect of each drug on hemostasis, therefore - such combinations are undesirable.
    Parallel treatment with Coplavix and Naproxen, as well as NSAIDs, COX-2 inhibitors is not recommended, as this leads to an increase in latent blood loss through the gastrointestinal tract.
    Systematic use of ibuprofen leads to inhibition of the antiplatelet effect of ASA (in low doses), while irregular use of ibuprofen does not have a similar clinically significant effect.
    With preparations of selective re-uptake of molecules of serotonin, there is a violation of platelet activation and an increase in the probability of bleeding.
    ASA is able to suppress the effect of uricosuric drugs that promote the excretion of uric acid from the body, for example: Benzbromarone, Probenecid, Sulfinpyrazone.
    Simultaneous treatment with methotrexate at a dose of 20 mg / week leads to a decrease in its renal clearance, and in turn - increases myelotoxic effect.
    Metamizole reduces the antiplatelet effect of ASA.
    Salicylates with acetazolamide are used with caution, since their combination increases the likelihood of metabolic acidosis.
    The systematic use of ethanol-containing products, for example, chronic use of large amounts of alcohol in combination with ASA increases the risk of bleeding.

Storage conditions

The temperature regime should be maintained: up to +25 ° Celsius.
Children and pets should not have access to medicines.
Shelf life - 2 years.

special instructions

The doctor should notify the patient of the increased risk and duration of bleeding.
Before any surgical intervention, the use of new drugs, a visit to the dentist, patients should be informed of the treatment by Coplavix.

Reviews of Coplavix

Positive

    a convenient scheme of treatment and the possibility of prolonged use (up to 12 months), both in a hospital and at home;
    effectiveness.

Negative

    the effect does not come immediately, relief may appear after a month;
    complexity, if necessary, surgical interventions, dental procedures, the use of other drugs in connection with the prolongation of bleeding time, a list of adverse reactions and drug interactions.