Clopidogrel
Clopidogrel: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Drug interactions
- 10. Analogs
- 11. Terms and conditions of storage
- 12. Terms of dispensing from pharmacies
- 13. Reviews
- 14. Price in pharmacies
Latin name: Clopidogrel
ATX code: B01AC04
Active ingredient: clopidogrel (clopidogrel)
Producer: ZAO Biocom, ZAO Kanonfarma Production, OOO Izvarino Pharma, OOO Nanolek, Severnaya Zvezda, Rafarma, Russia
Description and photo update: 2019-13-08
Prices in pharmacies: from 100 rubles.
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Clopidogrel is an antiplatelet drug.
Release form and composition
Clopidogrel is produced in the form of film-coated tablets: round, biconvex, pink (in blisters of 7, 10, 14, 15, 30 pcs., 1-4, 6, 8, 10 packs in a cardboard box; in cans of 7, 10, 14, 20, 28, 30, 50, 56, 60, 100 pcs., 1 can in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: clopidogrel - 75 mg (in the form of clopidogrel hydrosulfite - 97.875 mg);
- Auxiliary components: pregelatinized starch - 27 mg, anhydrous lactose (anhydrous milk sugar) - 63.125 mg, magnesium stearate - 1 mg, polyethylene glycol 6000 (macrogol) - 8 mg, microcrystalline cellulose - 40 mg, hydrogenated castor oil - 3 mg;
- Sheath: Opadry II pink - 9 mg (hydroxypropyl methylcellulose (hypromellose) - 2.52 mg, lactose monohydrate - 3.6 mg, triacetin - 0.72 mg, titanium dioxide - 2.0484 mg, indigo carmine dye - 0.0036 mg, dye red charming - 0.108 mg).
Pharmacological properties
Pharmacodynamics
Clopidogrel inhibits platelet aggregation and selectively inhibits the binding of adenosine diphosphate to receptors localized on the platelet walls and the induction of the GPIIb / IIIa complex, thus preventing platelet adhesion. The substance also blocks platelet aggregation, which is caused by other agonists, by stopping the stimulation of platelets by the released adenosine diphosphate. Clopidogrel does not alter the activity of phosphodiesterase, and also provides for the irreversible transformation of adenosine diphosphate receptors on platelets, as a result of which they lose their functionality until the moment of their natural death. The restoration of physiological function occurs in the process of their regeneration, which takes about a week.
Pharmacokinetics
Clopidogrel is absorbed from the intestines rather quickly, and its content in the blood increases slightly. The substance is actively involved in the metabolic processes taking place in the liver. The main metabolite has no pharmacological activity and accounts for up to 85% of the dose of clopidogrel taken.
The compound binds to plasma proteins by about 94-98%. 50% of the dose taken is excreted through the kidneys, and approximately 46% of the administered clopidogrel through the intestines. The half-life is about 8 hours.
Indications for use
- Prevention of the development of atherothrombotic events (in combination with acetylsalicylic acid) in patients with acute coronary syndrome: with ST-segment elevation (acute myocardial infarction) with the possibility of thrombolysis and drug treatment; without ST-segment elevation (non-Q wave myocardial infarction or unstable angina pectoris), including patients who underwent stenting during percutaneous coronary intervention;
- Prevention of atherothrombotic events in patients with ischemic stroke, myocardial infarction, or diagnosed peripheral arterial occlusive disease.
Contraindications
- Liver failure (severe);
- Active bleeding (including intracranial hemorrhage or bleeding from a peptic ulcer);
- Lactase deficiency, lactose intolerance, galactose / glucose malabsorption syndrome;
- Pregnancy and the period of breastfeeding (the safety and effectiveness of the use of Clopidogrel for this group of patients have not been established);
- Age up to 18 years (the safety and efficacy of taking the drug for this age group of patients have not been established);
- Hypersensitivity to drug components.
According to the instructions, Clopidogrel should be taken with caution in the following diseases / conditions:
- Chronic renal failure
- Moderate hepatic impairment;
- Pathological conditions that increase the risk of bleeding, including trauma and surgery;
- Hereditary decrease in the activity of the isoenzyme CYP2C19;
- Concomitant use with warfarin, acetylsalicylic acid, heparin, non-steroidal anti-inflammatory drugs (including COX-2 inhibitors), glycoprotein IIb / IIIa inhibitors.
Instructions for the use of Clopidogrel: method and dosage
Clopidogrel is taken orally, regardless of food intake.
For adults and elderly patients, the drug is prescribed in a daily dose of 75 mg in 1 dose.
Therapy should be started: after myocardial infarction - from 1 to 35 days; after ischemic stroke - in the period from 7 days to 6 months.
The dosage regimen is determined by the indications:
- Acute coronary syndrome without ST-segment elevation (unstable angina pectoris or myocardial infarction without Q wave): therapy begins with a single loading dose of 300 mg, then 75 mg per day is used simultaneously with taking acetylsalicylic acid (75-325 mg per day). The recommended dose of acetylsalicylic acid is up to 100 mg per day, as higher doses increase the risk of bleeding. The maximum beneficial effect develops after 3 months. The duration of the treatment course is up to 1 year;
- Acute coronary syndrome with ST segment elevation (acute myocardial infarction with ST segment elevation): 75 mg per day with an initial loading dose (once) simultaneously with acetylsalicylic acid and thrombolytics (or without them).
In patients with a genetically determined decrease in the activity of the isoenzyme CYP2C19, the effect of Clopidogrel may be reduced. For these patients, the optimal dosing regimen has not been established.
For patients over 75 years of age, Clopidogrel is prescribed without using a loading dose. Combination treatment should be started as early as possible after symptoms develop and continued for at least 1 month.
The experience of use in patients with moderate hepatic failure or chronic renal failure is limited.
Side effects
During the use of Clopidogrel, the following side effects may develop (≥1 / 10 - very often; from ≥1 / 100 to <1/10 - often; from ≥1 / 1000 to <1/100 - infrequently; from ≥1 / 10,000 up to <1/1000 - rarely; <1/10 000 (including individual messages) - very rare):
- Nervous system: infrequently - headache, paresthesia and dizziness, intracranial hemorrhage; rarely - systemic dizziness; very rarely - hallucinations, confusion, taste disorders;
- Digestive system: often - dyspepsia, diarrhea, gastrointestinal bleeding, abdominal pain; infrequently - gastritis, nausea, stomach and duodenal ulcers, constipation, vomiting, flatulence; rarely - retroperitoneal hematoma; very rarely - pancreatitis, stomatitis, colitis (including ulcerative or lymphocytic), hepatitis, acute liver failure, severe gastrointestinal bleeding with a fatal outcome;
- Cardiovascular system: often - hematoma; very rarely - vasculitis, bleeding from the surgical wound, severe bleeding, lowering blood pressure;
- Urinary system: infrequently - hematuria; very rarely - glomerulonephritis;
- Musculoskeletal system: very rarely - hemarthrosis, arthralgia, arthritis, myalgia;
- Hematopoietic system: infrequently - leukopenia, thrombocytopenia, eosinophilia; rarely - neutropenia, including severe; very rarely - thrombotic thrombocytopenic purpura, agranulocytosis, severe thrombocytopenia (with platelet count ≤30 × 10 9 / L), granulocytopenia, pancytopenia, anemia, including aplastic;
- Respiratory organs: very often - nosebleeds; very rarely - interstitial pneumonitis, bronchospasm, hemoptysis, pulmonary hemorrhage;
- Sense organs: infrequently - hemorrhages in the retina, conjunctiva;
- Skin and subcutaneous tissue: often - subcutaneous hemorrhage; infrequently, purpura;
- Laboratory indicators: very rarely - an increase in the concentration of creatinine in the blood, impaired liver function tests, prolonged bleeding time;
- Allergic reactions: infrequently - itching, rash; very rarely - erythema multiforme, angioedema, Stevens-Johnson syndrome, urticaria, erythematous rash, toxic epidermal necrolysis, anaphylactic reactions, serum sickness;
- Others: often - bleeding at the injection site; very rarely - an increase in temperature.
Overdose
An overdose of Clopidogrel can provoke hemorrhagic complications and prolonged bleeding time. If bleeding occurs, appropriate therapy should be initiated. Antidotes that level the specific activity of clopidogrel have not been found. If urgent correction of a prolonged bleeding time is required, platelet transfusion should be used.
special instructions
During therapy, it is necessary to monitor the indicators of the hemostasis system, including the number of platelets, activated partial thromboplastin time, tests of the functional activity of platelets, and also regularly examine the functional activity of the liver.
To identify any signs of bleeding, including latent ones, the patient's condition should be carefully monitored, especially during the first weeks of using Clopidogrel and / or after surgery or invasive procedures on the heart.
The drug must be used with caution in patients with an increased risk of bleeding during surgery, trauma, other pathological conditions, in the presence of diseases that predispose to the development of bleeding (especially eye and gastrointestinal), as well as in patients receiving acetylsalicylic acid, nonsteroidal anti-inflammatory drugs (including COX-2 inhibitors), glycoprotein IIb / IIIa inhibitors, or heparin.
Concomitant use with warfarin is not recommended, as it may increase the intensity of bleeding (except in special rare clinical situations).
During surgical interventions, if the antiplatelet effect is undesirable, the intake of Clopidogrel should be interrupted 7 days before the operation.
The drug lengthens the bleeding time, therefore it is prescribed with caution to patients with diseases that predispose to the development of bleeding (especially intraocular and gastrointestinal).
In very rare cases, after taking Clopidogrel (including its short-term use), thrombotic thrombocytopenic purpura has occurred, characterized by microangiopathic hemolytic anemia and thrombocytopenia in combination with neurological symptoms, functional renal impairment or fever. Thrombotic thrombocytopenic purpura is a potentially life-threatening disease that requires immediate treatment, incl. using plasmapheresis.
In the presence of severe functional disorders of the liver, the risk of hemorrhagic diathesis should be taken into account. The experience of using Clopidogrel in patients with moderate liver dysfunction is limited, as a result of which the drug is prescribed to such patients with caution.
Due to the existing possibility of dizziness, during therapy, it is recommended to be careful when driving vehicles and performing other potentially hazardous work that requires a high concentration of attention and fast psychomotor reactions.
Drug interactions
In patients with an increased risk of bleeding (during surgery, trauma or other pathological conditions), the simultaneous administration of Clopidogrel with IIb / IIIa receptor blockers requires caution.
With the simultaneous use of Clopidogrel with certain drugs, undesirable effects may occur:
- Acetylsalicylic acid: potentiation of its effect on collagen-induced platelet aggregation (care must be taken);
- Warfarin: an increase in the intensity of bleeding (the use of this combination is not recommended);
- Heparin: increased risk of bleeding (care must be taken).
Analogs
Clopidogrel analogs are: Aggregal, Detromb, Deplatt-75, Clopidogrel-SZ, Clopidogrel-Richter, Clopidogrel-Teva, Clopidogrel-TAD, Clopidogrel-LEXVM, Clopidogrel-Clopilet, Cardogrel, Kardogrel, Leksutol, Clopidopilt Plavix, Plagril, Plogrel, Trombex, Tromborel, Troken, Targetek, Egithromb.
Terms and conditions of storage
Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Clopidogrel
There are numerous reviews about Clopidogrel from patients who have undergone serious illnesses and surgical operations (for example, stenting) and highly appreciate the effectiveness of the drug. But in no case can it be used for self-medication, the appointment of a therapy regimen and control of the effectiveness of treatment should be carried out by a specialist.
Price for Clopidogrel in pharmacies
The price for Clopidogrel varies in the range of 259–373 rubles. (for a package containing 14 tablets) or 471–655 rubles. (per pack containing 28 tablets) depending on the manufacturer.
Clopidogrel: prices in online pharmacies
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Drug name Price Pharmacy |
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Clopidogrel 75 mg film-coated tablets 14 pcs. RUB 100 Buy |
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Clopidogrel 75 mg film-coated tablets 14 pcs. 111 RUB Buy |
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Clopidogrel 75 mg film-coated tablets 14 pcs. 152 RUB Buy |
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Clopidogrel tablets p.p. 75mg 14 Pcs. 217 r Buy |
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Clopidogrel 75 mg film-coated tablets 28 pcs. 219 r Buy |
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Clopidogrel 75 mg film-coated tablets 28 pcs. RUB 300 Buy |
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Clopidogrel 75 mg film-coated tablets 28 pcs. 339 r Buy |
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Clopidogrel 75 mg film-coated tablets 28 pcs. 429 r Buy |
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Clopidogrel tablets p.p. 75mg 28 Pcs. Canonpharm 452 RUB Buy |
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Clopidogrel tablets p.p. 75mg 30 pcs RUB 671 Buy |
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Clopidogrel 75 mg film-coated tablets 30 pcs. RUB 671 Buy |
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Clopidogrel 75 mg film-coated tablets 90 pcs. 893 r Buy |
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Clopidogrel 75 mg film-coated tablets 90 pcs. 981 RUB Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
