In what situations do doctors prescribe Clopidogrel? Instructions for use, analogues, release form, composition, side effects and indications for the use of this medication will be described in detail in this article. In addition, you will find out the cost of the drug and the opinion of patients about it.
Release form and composition
In what form can I buy Clopidogrel? The instruction informs that this medication is available in the form of tablets, which are coated with a film coating. One box contains 14 pieces, in a jar - 14 or 28, in a cardboard box - 1 or 2 plates with medicine. The main active ingredient is clopidogrel in the form of a hydrosulfate. The auxiliary components contained in the drug include anhydrous lactose, magnesium stearate, pregelatinized starch, hydrogenated castor oil, polyethylene glycol 6000 and microcrystalline cellulose. The film membrane on which the tablets are coated consists of titanium dioxide, hypromellose, aluminum varnish (based on Ponso 4 R dye) and polyethylene glycol 400 and 6000. The drug “Clopidogrel” is sold (the price will be indicated below) through a network of pharmacies, but only if available recipe.
Pharmacological characteristics
When treated with the drug, platelet aggregation caused by other agonists is reduced. The drug “Clopidogrel” is active (instructions for use, price, reviews and many other useful information are available on many medical portals and are presented in this article) for two hours, the maximum effectiveness is 4-7 days, with the constant intake of 50-100 mg per day. The antiplatelet effect lasts from 7 to 10 days throughout the life of the platelet.
Pharmacokinetics
After oral administration, the drug “Clopidogrel” (75 mg - standard dose) is rapidly absorbed from the gastrointestinal tract, while the concentration in the liquid part of the blood rises slightly, and after 2 hours it reaches a level that can be determined (0.025 μg / l).
Intensively metabolized in the liver. The main metabolite is an inactive derivative of a carboxylic acid (approximately 85% of the circulating starting material in the plasma). The average maximum concentration after repeated use of Clopidogrel is 3 mg / l, it can be observed one hour after administration.
The active substance and metabolite are irreversibly bound to plasma proteins. The bond remains unsaturated.
After oral administration of 14C-labeled “Clopidogrel”, almost half of the dose taken is excreted during urination, about 46% with feces for 120 hours. T1 / 2 of the main metabolite - 8 hours.
The saturation of the metabolite is many times greater in patients after reaching 75 years, while platelet aggregation and bleeding time do not change.
In plasma with severe kidney disease, the concentration of the metabolite is from 5 to 15 ml / min, while in diseases of moderate severity it is 30-60. Despite the fact that the inhibitory effect in patients on adenosine diphosphate - induced platelet aggregation decreased, the bleeding time increased as in healthy volunteers.
Indications
Are you aware of the purpose for which doctors prescribe a drug such as Clopidogrel to patients? Analogs and the medication itself are prescribed for the prevention of thrombotic complications in ischemic stroke, myocardial infarction and peripheral artery occlusion. The simultaneous use of acetylsalicylic acid and Clopidogrel is indicated as a prophylaxis for thrombotic complications caused by acute coronary syndrome.
Contraindications
"Klopidogrel" (the price in pharmacies of the Moscow region is about 510 rubles) is contraindicated in:
- hypersensitivity;
- acute bleeding;
- hemorrhagic syndrome ;
- severe liver failure;
- intracranial effusion and pathology predisposing to the development of bleeding (lung tumor, peptic ulcer exacerbation, hyperfibrinolysis, tuberculosis);
- lactose deficiency (for dosage forms containing milk sugar), hereditary galactose intolerance, glucose-galactose malabsorption syndrome .
"Clopidogrel": use and dosage
Tablets, according to the instructions, can be taken regardless of meals. To prevent thrombotic complications, patients with ischemic stroke or myocardial infarction are prescribed 75 mg Clopidogrel once a day. In acute disease, which is caused by the development of a focus of ischemic necrosis in the heart muscle, treatment should begin from the first days. The course of therapy using Clopidogrel - no more than 35 days. Patients with ischemic stroke can take this medication for six months. In case of thrombotic complications arising from ACS without raising the ST segment, treatment is started with a single dose of a loading dose (300 mg), and then no more than one tablet is taken per day. Maximum efficiency is observed after three months. The duration of therapy with the drug "Clopidogrel" (analogues and generics are presented below) should not exceed 1 year. Against the background of ACS with an ST segment elevation, 75 mg of the drug is most often prescribed daily with an initial single use of a loading dosage in combination with thrombolytics and acetylsalicylic acid. As soon as symptoms appear, you need to go to combination therapy. For patients over 75 years of age, treatment is prescribed without a loading dose.
Overdose
An increase in bleeding time with subsequent complications indicates the administration of the drug in doses exceeding the recommended ones. In such situations, appropriate therapy will be needed. In the case when a quick correction of increased bleeding time is needed, transfusion of TM is necessary. There is no specific antidote.
Interaction with other medicines
The concomitant use of Clopidogrel with warfarin leads to an increase in the intensity of bleeding, which is why this combination is extremely undesirable. The likelihood of bleeding increases with drug treatment in combination with non-steroidal anti-inflammatory drugs, acetylsalicylic acid, glycoprotein inhibitors and heparin.
Side effects
Treatment with the drug “Clopidogrel” (instructions, price, method of application and dose are described in detail in this material) can lead to undesirable consequences:
- Blood coagulation system: during the first month of therapy, bleeding often occurs, hematomas appear; less commonly, conjunctive bleeding; isolated cases - intracranial bleeding.
- Hematopoietic system: in rare cases, thrombocytopenic thrombohemolytic purpura, granulocytopenia, anemia, including pancytopenia and aplastic anemia.
- Nervous system: occasionally headaches, paresthesia, dizziness; infrequently - vertigo; isolated cases - confusion and hallucinations.
- Blood vessels and heart: hematomas often form; heavy bleeding, vasculitis sometimes occur, blood pressure decreases.
- Respiratory organs: epistaxis, bronchospasm, pulmonary hemorrhage, interstitial pneumonitis, hemoptysis.
- Digestive tract: diarrhea, dyspepsia, abdominal pain, gastrointestinal bleeding, gastritis and gastric ulcer, vomiting, flatulence, nausea, constipation, retroperitoneal bleeding, colitis, pancreatitis, stomatitis, acute liver failure, hepatitis, increased activity of liver enzymes.
- Musculoskeletal system: arthralgia, myalgia, arthritis.
- Skin: bullous rash (Stevens-Johnson and Lyell syndromes, erythema multiforme), eczema, erythematous rash, and lichen planus.
- Urinary system: hematuria, hypercreatininemia, glomerulonephritis.
- Allergic reactions: angioedema, serum sickness, urticaria, pseudo-allergic reactions.
During therapy with this drug, an increase in body temperature is rarely observed, which is perceived not as a result of taking the medication, but as a symptom of a cold.
special instructions
The medicine "Clopidogrel" is taken with extreme caution with a high probability of bleeding as a result of surgical interventions, impaired hemostasis. If surgery is necessary, and an antiplatelet effect is extremely undesirable, you should refuse to take the drug a week before the appointed time for surgery. Particularly carefully, the drug is prescribed for severe violations of the liver function, which can cause hemorrhagic diathesis. If there are signs of increased bleeding, a study of the hemostasis system will be required. In addition, it is necessary to constantly monitor indicators of the functional activity of the liver. Caution "Clopidogrel" is used with heparin, NSAIDs, warfarin. When conducting experimental studies did not reveal the carcinogenic and genotoxic effects of the drug, in addition, did not establish the effect on the ability to control transport.
"Clopidogrel": analogues and generics
Synonyms (analogues) of drugs are medicines that have the same effect or have the same composition. What medicines can replace the drug “clopidogrel”? The drug analogs for the active substance are as follows: “Cardutol”, “Detromb”, “Agregal”, “Trombeks”, “Klopilet”, “Troken”, “Plavix”, “Plagril”, “Plogrel”, “Targetek”, “Egithromb” , "Clopidogrel-Teva."
Each medication has different features, so the use is permissible only after consultation with your doctor.
Opinions about the medicine
What do people say about a drug like Clopidogrel? Reviews of patients who happened to suffer serious illnesses and surgical interventions are extremely positive. Patients note the high effective effect of the medication, however, it is not designed for use in self-medication. Analogues of drugs help patients to choose the best option for them in terms of price and quality, however, the appointment and control of effectiveness should be assigned to an experienced specialist.