Avix - instructions for use of the drug, structure, Contraindications

Aviks – antithrombotic agent.

Aviks: indications and dosage

Avix appoint, when it is necessary to carry out the prevention of atherothrombotic manifestations:

• Patients, who have suffered a myocardial infarction (Avix is ​​prescribed immediately for several days and for thirty-five days), ischemic stroke (treatment is prescribed for a week and for six months), and also if the diagnostics showed, that peripheral arteries have disease;
• Patients, who have non-ST elevation acute coronary syndrome (Unstable angina or non-Q wave myocardial infarction). This includes patients, who have undergone stent placement during this procedure, like percutaneous coronary angioplasty, in combination with which was acetylsalicylic acid;
• Patients, who had an acute ST-segment elevation myocardial infarction (acetylsalicylic acid in combination) with standard medical treatment, if thrombolytic therapy is indicated.

The standard dose of Avix is 75 mg once daily. In non-ST elevation acute coronary syndrome (the presence of unstable angina or myocardial infarction without a Q wave on the ECG) the first single loading doses are 300 mg, further accept 75 mg once a day (in addition acetylsalicylic acid 75 – 325 mg per day). High doses of acetylsalicylic acid can lead to bleeding, therefore, it is not recommended to take it in volumes more than 100 mg. Treatment times vary on a case-by-case basis., no optimal solution has been found to date.. In medical practice, cases are common, when treatment with Avix lasts for a year, and the maximum effect is reached three months after the first dose of the drug. Sick, who have an acute ST-elevation myocardial infarction should take Avix at a dosage of 75 mg during the day, at the beginning - a single loading dose 300 mg together with acetylsalicylic acid (with or without thrombolytics). When the patient is over 75 years of age, then a loading dose of clopidogrel is not used. Combination therapy should be started as soon as possible, once the symptoms have been established, its period must be at least, than a month. If you combine clopidogrel with acetylsalicylic acid in this disease for more than a month, the effect of medical practice has not yet been studied.

Aviks: overdose

Since the main side effect of the drug Avix is ​​the occurrence of bleeding, drug overdose, and therefore its main active substance - clopidogrel - can cause the effect of increasing the duration of bleeding, and subsequent complications. If the drug has caused bleeding, appropriate measures must be taken to eliminate it.. To date, no antidote of clopidogrel is known to modern medical science.. In those situations, if you need to urgently eliminate prolonged bleeding, platelet transfusion can be performed, which will lead to, that the effect of clopidogrel will decrease.

Aviks: side effects

The most common side effect of Avix is ​​bleeding..

For, to classify side effects, introduce such categories: often (from once to 100 applications up to one in ten), sometimes (from one in a thousand receptions to one in a hundred), rarely (once in ten thousand receptions - once in a thousand), rarely (once for more than ten thousand receptions).

Side effects of Avix, classified by different organ systems.

Side effects of Avix on the blood and lymphatic system:

• rarely seen thrombocytopenia, leukopenia, eozinofilii;
• rare neutropenia, as well as severe neutropenia;
• very rarely - the presence of thrombotic thrombocytopenic purpura, aplastic anemia, pantsitopenii, agranulocytosis, severe thrombocytopenia, granoulozitopenia, anemia.

Side effects of Avix on the immune system:

• very rare cases of serum sickness, anaphylactoid reactions.

Adverse reactions of Avix may include psychiatric disorders.:

• very rarely hallucinations may occur, confusion.

Side effects of Avix on the nervous system:

• infrequently, the patient may experience intracranial bleeding due to taking the drug (in extremely rare cases, death is possible), headache , paresthesia, dizziness;
• very rarely, side effects of the drug can manifest themselves in a change in taste sensations.

Side effects of the drug Avix can manifest itself in eye pathologies:

• infrequently it is possible to meet bleeding in the area of ​​u200bu200bthe eyeballs (the presence of conjunctiva, ocular, retinal).

Side effects of Avix in pathologies of the ear and labyrinth:

• rare dizziness.

Side effects of Avix, that lead to vascular disorders:

• due to taking the drug, hematomas are frequent;
• very rare significant hemorrhage, bleeding from wounds, vasculitis, arterial hypotension.

Side effects of Avix – respiratory, thoracic and mediastinal disorders:

• frequent nosebleeds;
• in very rare cases, bleeding of the respiratory tract is possible (hemoptysis, pneumorrhagia), bronchospasm, interstitial pneumonitis.

Side effects of Avix, manifested in violations of the gastrointestinal tract:

• frequent gastrointestinal bleeding, diarrhea, stomach ache, dyspepsia
• in the "infrequently" category, gastric and duodenal ulcers are noted, gastritis, vomiting, nausea, constipation, flatulence, etc.;
• rarely – retroperitoneal hemorrhages;
• very rarely, gastrointestinal and retroperitoneal bleeding is possible (until death), pancreatitis, colitis (ulcerative or lymphocytic), stomatitis.

Side effects of Avix, affecting the hepatobiliary system:

• rarely – manifestations of acute liver failure, hepatitis, abnormal liver function test results

Side effects of Avix, affecting the skin and subcutaneous tissue:

• frequent subcutaneous hemorrhages;
• rare manifestations of a rash, itching, intradermal hemorrhages (purpura);
• Very rare bullous dermatitis (toxic epidermal necrolysis, Stevens syndrome- Johnson, erythema multiforme), angioedema, skin rash, krapivnicы, eczema, lichen planus.

Side effects of Avix, affecting the musculoskeletal system, connective and bone tissue:

• very rarely, musculoskeletal hemorrhage is possible (hemarthrosis), Arthritis, artralgii, mialgii.

Side effects of Avix, affecting the functioning of the kidneys and urinary system:

• infrequent manifestation of hematuria;
• very rare manifestations of glomerulonephritis, increased levels of creatinine in the circulatory system.

Side effects of Avix, manifested in the general state and reactions in the introduction mission:

• bleeding at the injection site is common;
• very rare in patients, host Avix, fever.

Side effects of Avix, having an impact on the conduct of laboratory research:

• in rare cases, an increase in time is possible, during which bleeding occurs, the number of neutrophils and platelets in the patient's body decreases.

Aviks: Contraindications

Contraindications to the use of the drug Avix is ​​the presence of:

• hypersensitivity to the components of the drug;
• severe hepatic insufficiency;
• acute bleeding (peptic ulcer, intracranial hemorrhage);
• hereditary galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption;
• period of childbearing and lactation;
• the drug is contraindicated in children.

Aviks: interactions with other drugs and alcohol

Clopidogrel has a property under the influence of CYP2C19 to turn into its active metabolite. Therefore, if drugs are used, which decrease the activity of this enzyme, the concentration of the active metabolite of clopidogrel in plasma will decrease, and correspondingly, the clinical efficacy of Avix will decrease.

If the drug leads to suppression of CYP2C19 activity, then you should not take it together with Avix.

Proton pump inhibitors should also not be used concomitantly with Avix., except for exceptional situations.

To date, no effect on the antiplatelet activity of clopidogrel drugs has been proven., reduce acid production in the gastrointestinal tract, for example, H2 blockers or antacids.

The action of omeprazole, èzomeprazola, fluvoxamine, fluoxetine, moclobemide, vorikonazola, flukonazola, ticlopidine, ciprofloxacin, cimetidine, karʙamazepina, oxcarbazepine and chloramphenicol is to suppress the activity of CYP2C19.

As for warfarin, together with it, it is not advised to use clopidogrel, because bleeding can become more intense due to this.

In the case of inhibitors IIb / IIIa, if patients receive them, the risk of bleeding, trauma-related, surgical interventions, or any of the other pathological conditions, increasing.

Acetylsalicylic acid does not modify clopidogrel-mediated inhibition of platelet aggregation, However, due to clopidogrel, there is an increase in the effect of acetylsalicylic acid on collagen-induced platelet aggregation. But when five hundred milligrams of Acetylsalicylic acid was simultaneously applied twice a day, there was no significant increase in bleeding time due to clopidogrel. Clopidogrel and acetylsalicylic acid may interact pharmacodynamically, in such a situation, acetylsalicylic acid may increase the risk of bleeding. Therefore, it is necessary to take these two drugs at the same time with extreme caution..

If clopidogrel is used together with heparin, then there is no need to change the dose of the latter, modification of the effect of heparin on the, how blood coagulates, not happening. Clopidogrel and heparin may interact pharmacodynamically, because of this, the risk of bleeding increases. Therefore, these two drugs must be taken at the same time, too, carefully..

When a patient has an acute myocardial infarction, then if you simultaneously use clopidogrel and fibrin-specific or fibrin-non-specific thrombolytic agents and heparin, clinically significant bleeding also occurs frequently, how and when thrombolytic agents and heparin are used together with acetylsalicylic acid.

If you use clopidogrel and naproxen at the same time, then hidden gastrointestinal bleeding may become more frequent. But the interactions of clopidogrel with other non-steroidal inflammatory drugs are not well understood., so it's not clear at the moment., whether the likelihood of gastrointestinal inflammation increases, when using non-steroidal anti-inflammatory drugs. Because the use of non-steroidal anti-inflammatory drugs, including COX -2, together with clopidogrel, should be done carefully.

Clinically significant pharmacodynamic interactions have not been recorded with the simultaneous use of clopidogrel with such drugs., as atenolol, nifedipine or both of them at once. Furthermore, pharmacodynamics of clopidogrel remained almost unchanged, even when phenobarbital was used concomitantly, cimetidine or estrogen. No change in pharmacokinetics, if clopidogrel is used together with digoxin and theophylline. No influence on, how is clopidogrel absorbed, from antacids. Suppression of cytochrome P4502C9 activity may be caused by carboxyl metabolites of clopidogrel. There is a potential, that increased plasma levels of phenytoin and tolbutamide, as well as non-steroidal anti-inflammatory drugs, metabolized P4502C9. Clopidogrel is safe to combine with phenytoin and tolbutamide.

Specific interactions of clopidogrel, part of Avix, we described. Other data on the interaction of clopidogrel with some other drugs, commonly prescribed for the treatment of patients with atherothrombotic disease, currently missing.

There have been quite a few cases, when patients were prescribed a variety of appropriate drug therapy with diuretics, beta-blockers, angiotensin-converting enzyme inhibitors, calcium antagonists, preparations, reducing cholesterol levels, coronary vasodilators, antidiabetic drugs (including insulin), antiepileptic drugs, hormone replacement therapy and glycoprotein IIb/IIIa antagonists, and there were no clinically significant adverse interactions.

Aviks: composition and properties

active substance: clopidogrel;

1 tablet, covered with a film shell, contains clopidogrel bisulfate 97,87 mg, equivalent to clopidogrel 75 mg;

excipients: microcrystalline cellulose, mannitol (E 421), hydroxypropylcellulose, polyethylene glycol 6000, croscarmellose sodium, sodium stearyl fumarate, iron oxide red (E 172), simethicone emulsion, paint white OY-7300 (hypromellose, polyethylene glycol, titanium dioxide (E 171)).

Product form: Avix is ​​available in the form of tablets., film-coated.

Aviks: pharmachologic effect:

Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADF) with its platelet receptor and subsequent ADP-mediated activation of the GPIIb/IIIa complex, which inhibits platelet aggregation. Clopidogrel biotransformation is required, to inhibit platelet aggregation.

Clopidogrel also contributes to the suppression of platelet aggregation., what other agonists do, by blocking increased platelet activation by released ADP.

Clopidogrel irreversibly modifies platelet ADP receptors. Because of this, platelets are forever changed (as long as the altered batch of platelets continues to exist). Normal platelet function is restored then, when they are fully updated. On repeated dose 75 mg per day from the first day there was a significant inhibition of platelet aggregation, which was caused by ADP. Results steadily increased and stabilized between three days and a week. The stable state was characterized by an average level of oppression, which was observed, when the dose was taken 75 mg per day, and amounted to 40% to 60%. The state of platelet aggregation and the duration of bleeding gradually acquired initial values, most often the period was five days after, How was the treatment cancelled?.

If repeated oral doses are taken up to 75 mg, clopidogrel is rapidly absorbed. But the parent compound exists in the blood plasma at very low concentrations., after 2:00 below the quantitation threshold (0,00025 mg / l). As shown by the results of the determination, How is clopidogrel excreted in the urine?, the body absorbs at least half of it. The liver extensively metabolizes clopidogrel.. In blood plasma, the circulation of the main metabolite is observed in the amount 85 % connections. This metabolite is a derivative of carboxylic acids, he is not active. Within one hour after taking the drug, a peak plasma level of this metabolite is observed.. The peak level is about 3 mg/l after, as oral dose 75 mg was administered). The active metabolite, thiol derivative, obtained after oxidation of clopidogrel to 2-oxo-clopidogrel followed by hydrolysis. The oxidation step is regulated mainly by isoenzymes 2B6 and 3A4 of cytochrome P450 and slightly less – 1A1, 1A2 and 2S19.

Storage conditions: Avix should be kept away from children., storage temperature 15-30 ºС.

Aviks: general information

• Sales form: on prescription
• Current in-about: Clopidogrel
• Manufacturer: Tabuk Pharmaceutical Manufacturing Co., Kingdom of Saudi Arabia
• Farm. Group: Antykoahulyantы