Plavix

Plavix is ​​an antiplatelet (antiplatelet) drug from the French pharmaceutical company Sanofi.

The active ingredient in it is clopidogrel. The drug is a prodrug, one of the metabolites of which has the ability to inhibit platelet aggregation (sticking). The mechanism of action of plavix is ​​to inhibit the binding of adenosine diphosphate to platelet receptors and the subsequent activation of glycoprotein IIb / IIIa complex, which leads to the suppression of platelet aggregation.

With regular intake of Plavix at a dose of 75 mg per day, the effect develops already on the first day, gradually increasing and reaching its maximum by 3-7 days of administration. At equilibrium, platelet aggregation is inhibited by an average of 40-60%.

Clinical and pharmacological group

Antiplatelet

Pharmacy sales terms

It is released on prescription.

Prices

How much does plavix cost in pharmacies? The average price in 2018 is at the level of 2000 rubles for 10 tablets.

Release form and composition

Plavix dosage form - film-coated tablets.

  • The basis of the drug is clopidogrel, its concentration in a single tablet is 75 mg. The auxiliary components of Plavix include: macrogol 6000, mannitol, microcrystalline cellulose (with low water content), low-substituted hyprolosis, hydrogenated castor oil.
  • Opadry pink and carnauba wax (trace amounts) are used to make the film shell.

The tablets are biconvex, round-shaped, their color is pink. The numbers "75" are engraved on one of the sides and the inscription "I I7I" on the other. Packaged in blisters of 7, 10 or 14 pieces, 1, 2 or 3 blisters in a cardboard box are sold.

Pharmacological effect

The drug is antiagregant. Plavix action according to the instructions leads to the suppression of platelet aggregation.

The use of the drug and Plavix analogues prevents the development of atherothrombosis in various locations of atherosclerotic vascular lesions, including those with peripheral, coronary, or cerebral arteries.

According to reviews, Plavix with daily intake of one pill causes suppression of ADP-induced platelet aggregation from the very first day, which increases over the next 3-7 days and subsequently goes to a constant level. In equilibrium, platelet aggregation is inhibited by approximately 40-60%. After discontinuation of Plavix, bleeding time and platelet aggregation return to baseline over five days.

Indications for use

What helps? Plavix is ​​used to prevent atherothrombotic complications in the following categories of patients:

  1. Persons with acute coronary syndrome.
  2. Persons diagnosed with occlusive peripheral arterial disease, ischemic stroke, with a prescription from 7 days to 6 months, and myocardial infarction, with a prescription from several days to 35 days.
  3. Persons with acute myocardial infarction with drug treatment, while maintaining the possibility of thrombolysis (acute coronary syndrome with ST-segment elevation), also in combination with acetylsalicylic acid.
  4. For individuals with myocardial infarction without a Q wave or unstable angina (acute coronary syndrome without ST-segment elevation), the drug is used in combination with acetylsalicylic acid.

The use of Plavix is ​​indicated for the prevention of thromboembolic and atherothrombotic conditions in atrial fibrillation (atrial fibrillation) and stroke.

Plavix can be prescribed to patients with at least one risk factor for the occurrence of vascular complications, who have a low risk of bleeding and cannot take indirect anticoagulants. In this case, the drug is used in combination with acetylsalicylic acid.

Contraindications

Absolute:

  • Age up to 18 years;
  • Period of pregnancy and lactation;
  • Acute bleeding (for example, intracranial hemorrhage or bleeding from a peptic ulcer);
  • Severe liver failure;
  • Galactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
  • Hypersensitivity to any component of the drug.

Relative:

  • The presence of risk factors for the development of bleeding (due to surgery, injury or pathological conditions) or the simultaneous use of drugs such as ASA and other NSAIDs, warfarin, heparin, glycoprotein IIb / IIIa inhibitors, selective serotonin reuptake inhibitors, selective COX-2 inhibitors;
  • Low activity of an isoenzyme CYP2C19;
  • Mild hepatic impairment with predisposition to bleeding;
  • Renal failure;
  • Diseases with the risk of bleeding (in particular, intraocular and gastrointestinal) or the simultaneous use of drugs that can damage the membrane of the gastrointestinal tract (nonsteroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid (ASA));
  • Anamnestic data on hematological or allergic reactions to thienopyridine (prasugrel, ticlopidine);
  • The period after a recent ischemic stroke or other cerebrovascular accident.

Use during pregnancy and lactation

The drug is contraindicated to take in specified periods.

Dosage and method of use

The instructions for use indicate that adults and elderly patients Plavix should be taken orally, regardless of the meal. The drug at a dose of 300 mg, is intended for use as a loading dose by patients with acute coronary syndrome.

Acute coronary syndrome with ST elevation (acute myocardial infarction with ST elevation):

  • Clopidogrel is administered once at a dose of 75 mg 1 time / day with an initial single dose of a loading dose of 300 mg in combination with acetylsalicylic acid and thrombolytics (or without thrombolytics). Combination therapy is started as soon as possible after the onset of symptoms and continues for at least 4 weeks. In patients older than 75 years, treatment with clopidogrel should be started without taking its loading dose. For a maintenance dose of clopidogrel (75 mg), Plavix 75 mg tablets are used.

Acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q wave):

  • Treatment with clopidogrel should begin with a single dose of a loading dose of 300 mg, and then continue with a dose of 75 mg 1 time / day (in combination with acetylsalicylic acid in doses of 75-325 mg / day). Since the use of acetylsalicylic acid in higher doses is associated with an increased risk of bleeding, the dose of acetylsalicylic acid recommended for this indication should not exceed 100 mg. The maximum beneficial effect is observed by the third month of treatment. The course of treatment is up to 1 year.

Patients with a genetically determined reduction in the function of the isoenzyme CYP2C19:

  • The status of a weak CYP2C19 metabolizer is associated with a decrease in the antiplatelet effect of clopidogrel. The regimen of high doses (600 mg — loading dose, then 150 mg 1 time / day, daily) in weak metabolisers increases the antiplatelet effect of clopidogrel. However, the optimal dosing regimen for patients with reduced metabolism using the CYP2C19 isoenzyme has not yet been established in clinical studies on clinical outcomes.

Side effects

Post-marketing experience with the drug:

  1. General frustration: unknown frequency - fever.
  2. Mental disorders: unknown frequency - confusion, hallucinations.
  3. On the part of the nervous system: unknown frequency - a violation of taste perception.
  4. Since the cardiovascular system: unknown frequency - vasculitis, lower blood pressure.
  5. On the part of the musculoskeletal system: unknown frequency - arthralgia, arthritis, myalgia.
  6. On the part of the urinary system: unknown frequency - glomerulonephritis.
  7. On the part of the reproductive system and the mammary gland: unknown frequency - gynecomastia.
  8. From the side of the hemopoietic system: unknown frequency - agranulocytosis, granulocytopenia, aplastic anemia / pancytopenia, thrombotic thrombocytopenic purpura (TTP), acquired hemophilia A.
  9. Allergic reactions: unknown frequency - anaphylactoid reactions, serum sickness; allergic and hematological cross-reactions with other thienopyridines (such as ticlopidine, prasagrel).
  10. On the part of the respiratory system: unknown frequency - bronchospasm, interstitial pneumonia, eosinophilic pneumonia.
  11. On the part of the digestive system: unknown frequency - colitis (including ulcerative colitis or lymphocytic colitis), pancreatitis, stomatitis, hepatitis (non-infectious), acute hepatic failure.
  12. Dermatological reactions: unknown frequency - maculopapular, erythematous or exfoliative rash, urticaria, pruritus, angioedema, bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), drug hypersensitivity syndrome, irritability, toxicity, toxicity necrolysis syndrome, idiopathic hypersensitivity syndrome, toxicity syndrome, toxicity syndrome, toxicity syndrome, acute hypersensitivity syndrome, idiopathic syndrome, toxic erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis; eosinophilia and systemic manifestations (DRESS syndrome), eczema, lichen planus.
  13. Hemorrhagic disorders: unknown frequency - cases of serious bleeding, mainly subcutaneous, musculoskeletal, eye hemorrhages (conjunctival, in the tissue and retina of the eye), bleeding from the respiratory tract (hemoptysis, pulmonary hemorrhage), nasal bleeding, hematuria and hemorrhage from post operative bleeding, nose bleeding, hematuria and bleeding from post operative bleeding cases of bleeding with a fatal outcome (especially intracranial hemorrhage, gastrointestinal bleeding and retroperitoneal hemorrhage).
  14. Laboratory and instrumental data: unknown frequency - deviation from the norm of laboratory parameters of the functional state of the liver, increasing the concentration of creatinine in the blood.

Overdose

In case of exceeding the recommended therapeutic dose of Plavix tablets, the risk of the development of intense bleeding of various localization increases significantly. Treatment of overdose is the cessation of the use of the drug, washing the stomach, intestines, taking intestinal sorbents (activated carbon), as well as medical supervision in a medical hospital.

With the development of bleeding, urgent measures are taken to stop it, including platelet transfusions or surgery. There is no specific antidote for the active ingredient of Plavix tablets.

Special instructions

When treating clopidogrel, especially during the first weeks of treatment and / or after invasive cardiac procedures / surgery, it is necessary to carefully monitor patients for signs of bleeding, including and hidden.

Due to the risk of bleeding and hematological undesirable effects, if clinical symptoms that are suspicious of bleeding occur during the treatment, a clinical blood test should be urgently performed, the APTT, platelet count, indicators of the functional activity of platelets and other necessary studies should be determined.

Clopidogrel, as well as other antiplatelet drugs, should be used with caution in patients with injuries, surgical interventions or other pathological conditions, because of the risk of increased bleeding, as well as in patients receiving acetylsalicylic acid, NSAIDs, including COX-2 inhibitors, heparin or glycoprotein IIb / IIIa inhibitors due to an increased risk of bleeding.

The combined use of clopidogrel with warfarin can increase the risk of bleeding, therefore, should be followed with caution when used together with clopidogrel and warfarin.

If the patient has a planned surgical operation, and there is no need for an antiplatelet effect, then clopidogrel should be discontinued 5-7 days before the operation.

Clopidogrel prolongs bleeding time and should be used with caution in patients with diseases that predispose to the development of bleeding (especially gastrointestinal and intraocular). Drugs that can cause damage to the gastrointestinal mucosa (such as ASA, NSAIDs) in patients taking clopidogrel should be taken with caution.

Patients should be warned that when taking clopidogrel (alone or in combination with acetylsalicylic acid), it may take longer to stop the bleeding, and that if they have unusual (by localization or duration) bleeding they should be reported about this to your doctor. Before any forthcoming operation and before the start of taking any new drug, patients should inform the doctor (including the dentist) about taking clopidogrel.

Very rarely after the use of clopidogrel (sometimes even briefly) there have been cases of thrombotic thrombocytopenic purpura (TTP), which is characterized by thrombocytopenia and microangiopathic hemolytic anemia, accompanied by neurological disorders, impaired kidney function and fever. TTP is a potentially life-threatening condition that requires immediate treatment, including plasmapheresis.

It has been shown that in patients with a recent transient cerebral circulation disorder or stroke with a high risk of recurring ischemic complications, the combination of ASA and clopidogrel increases the incidence of large bleeding. Therefore, such a combination therapy should be carried out with caution and only in the case of proven clinical benefit from its use.

It was reported about the development of acquired hemophilia while taking clopidogrel. With a confirmed isolated increase in APTT, accompanied or not accompanied by the development of bleeding, the possibility of developing acquired hemophilia should be considered. Patients with a confirmed diagnosis of acquired hemophilia should be monitored and treated by specialists for this disease and stop taking clopidogrel.

During the period of treatment, it is necessary to monitor the functional state of the liver. In severe liver damage, the risk of hemorrhagic diathesis should be kept in mind.

The use of clopidogrel is not recommended for acute stroke with a duration of less than 7 days (since there are no data on its use in this state).

In patients with low activity of the CYP2C19 isoenzyme with the use of clopidogrel in the recommended doses, less active clopidogrel metabolite is formed and its antiaggregant effect is less pronounced. Patients with acute coronary syndrome or undergoing percutaneous coronary intervention and being weak SUR2C19 metabolizers, receiving clopidogrel in recommended doses may have a higher incidence of cardiovascular complications than patients with normal CYP2C19 function. There are tests for genotyping the isoenzyme CYP2C19; These tests can be used to help determine therapeutic strategies.The issue of clopidogrel use in higher doses in patients with low CYP2C19 activity is being considered.

Patients should have a history of previous allergic and / or hematological reactions to other thienopyridines (such as ticlopidine, prasagrel), because Allergic and / or hematological reactions between thienopyridines have been reported.

Thienopyridines can cause moderate and severe allergic reactions (such as rash, angioedema) or hematological reactions (such as thrombocytopenia and neutropenia). Patients who have previously experienced allergic and / or hematological reactions to one of the drugs of the thienopyridine group may have an increased risk of developing similar reactions to another drug of the thienopyridine group. Monitoring of cross-allergic and / or hematological reactions is recommended.

Drug interactions

The simultaneous use of clopidogrel with warfarin, ASA or heparin may increase the risk of bleeding; with naproxen - possible hidden blood loss through the gastrointestinal tract.

Simultaneous administration of clopidogrel with proton pump inhibitors, which are moderate or strong inhibitors of the isoenzyme CYP2C19 (esomeprazole, omeprazole), is not recommended. If necessary, the use of such a combination should be applied proton pump inhibitors with the least inhibition of the isoenzyme CYP2C19 (lansoprazole, pantoprazole).

Clinically significant pharmacodynamic interaction between clopidogrels , atenolol was not detected.

The pharmacodynamics of clopidogrel does not change while taking estrogen, cimetidine and phenobarbital; its absorption does not decrease antacid agents. Clopidogrel does not affect the pharmacokinetic parameters of theophylline and digoxin; its use in combination with phenytoin and tolbutamide is safe.

Reviews

We picked up some reviews of people who used Plavix:

  1. Alexander. Excellent drug. Transfer operation stenting. Have helped. Drank them throughout the year. Feeling good.
  2. Igor Took more than 2 weeks, began to hurt the liver, a constant taste. Gastric irritation is exactly the aggravation of gastritis, the gums are sore, but it is connected with the drug or not, I find it difficult to answer.
  3. Julia. We have been prescribed this medication by a doctor for the pope, as he had a heart surgery due to a heart attack. The medicine must be taken as prescribed by a doctor, we were prescribed a course of 18 months, 1 tablet per day. Plavix is, of course, very expensive, but, as doctors say, very effective, especially for patients with acute coronary syndrome. The longer you take the drug, the lower the occurrence of a heart attack. Therefore, in any case, do not assign it to yourself, if you have heart problems. The annotation describes very dangerous side effects and contraindications!

Patient reviews and doctors' reviews of Plavix are similar and, in the overwhelming majority of cases, highly appreciate the therapeutic and prophylactic possibilities of this remedy. Reports of adverse reactions are quite rare. It should be remembered that the appointment of the drug and the selection of its dosage should be done exclusively by the attending physician.

Analogs

Structural analogues of the active substance:

  • Agregal;
  • Deplatt 75;
  • Detrombe;
  • Zilt;
  • Cardutol;
  • Klopigrant;
  • Clopidex;
  • Clopidogrel;
  • Clopidogrel hydrosulfate;
  • Clopidogrel bisulfate;
  • Klopilet;
  • Listab;
  • Lopirel;
  • Plagril;
  • Plogrel;
  • Targetk;
  • Troken;
  • Egitrombe.

Before using analogues consult your doctor.

Plavix or Zilt - which is better?

Zilt is a cheaper analogue of Plavix and has the same composition as the last. The choice between drugs should be carried out by the doctor, based on the clinic of the disease, individual characteristics and economic considerations.

Storage conditions and shelf life

Plavix tablets have a shelf life of 3 years from the time they were made. The drug should be stored in the original factory packaging, dark, dry, out of the reach of children at air temperature not higher than + 30 ° C.

Watch the video: Is Plavix a blood thinner? (December 2019).

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