Lopyrel is an antiaggregant and is one of the most effective drugs to prevent the formation of thrombi in people with coronary syndrome in acute form.
The drug has a coronarodilating effect. The drug has proven itself in the fight against coronary heart disease and atherosclerosis.
Daily use of clopidogrel at a dose of 75 mg provides a significant suppression of ADP-induced platelet aggregation from the first day of admission. Gradually during 3-7 days the degree of suppression increases, reaching a constant level after reaching the equilibrium state. When taking a daily dose of 75 mg in an equilibrium state, platelet aggregation is inhibited by 40-60%.
For 5 days after discontinuation of the drug, bleeding time and platelet aggregation gradually return to the initial level.
Clinical and pharmacological group
Antiaggregant.
Conditions of leave from pharmacies
It is released on prescription.
Price list
How much does Lopirel cost? The average price in pharmacies is at the level of330 rublesfor 14 tablets in a package.
Form of issue and composition
The form of this drug is tablet, each unit is covered with a pink film shell and is marked with the symbol "I" on one side. The sale comes in cardboard packages (sometimes with a plastic bag), each of which contains 2, 4 or 9 blisters with 7 or 10 tablets in it.
- The active substance of Lopyrel is clopidogrel, as in the preparation with the appropriate name, in 1 tablet medication contains almost 98 mg of clopidogrel bisulfate, which is equivalent to 75 mg of clopidogrel.
- As an additional, the composition of the medicament includes anhydrous lactose and microcrystalline cellulose, as well as glyceryl, talc and crospovidone.
Pharmacological effect
Antiaggregant drug, a specific and active inhibitor of platelet aggregation. Has coronarodilating effect. Selectively reduces the binding of ADP to platelet receptors and the activation of GPI Ib / IIIa receptors by ADP, thereby reducing platelet aggregation. Reduces platelet aggregation, caused by other agonists, preventing their activation by released ADP, does not affect the activity of PDE. Irreversibly binds to ADP-receptor platelets, which remain immune to stimulation of ADP throughout the life cycle (about 7 days).
The inhibition of platelet aggregation is observed after 2 hours after administration (40% inhibition) of the initial dose of 400 mg. The maximum effect (60% suppression of aggregation) develops after 4-7 days of constant admission in a dose of 50-100 mg / day. Antiaggregant effect persists throughout the life span of platelets (7-10 days).
In the presence of atherosclerotic lesion of the vessel prevents the development of atherothrombosis, regardless of localization of the vascular process (cerebrovascular, cardiovascular or peripheral defeat).
Indications for use
Lopirel is prescribed in the following cases:
- Stenocardia of unstable type.
- With myocardial infarction (without a tooth "Q").
- After the transfer of myocardial infarction in acute form.
Other indications (for taking the drug as a prophylaxis):
- Atherothrombotic complications after myocardial infarction, stroke.
- Disease of peripheral arteries of occlusal type.
Contraindications
Contraindicated taking this medication to patients:
- with hyperfibrinolysis;
- with lung tumors;
- with colitis and tuberculosis;
- ladies during pregnancy and during brast-fiding;
- with increased sensitivity to components included in the composition of the product;
- with hemorrhagic syndrome,
- with acute bleeding, as well as intracranial hemorrhage;
- with severe renal failure;
- with ulcers of the stomach and duodenum at the stage of exacerbation;
- at the age of less than 18 years.
Use in pregnancy and lactation
It is not recommended during pregnancy due to the lack of clinical data on the use of pregnant women, although animals showed no direct or indirect adverse effects on the course of pregnancy, embryonic development, childbirth and postnatal development.
For the duration of treatment, breastfeeding should be discontinued. in studies on rats, it has been shown that clopidogrel and / or its metabolites are excreted into breast milk. Whether clopidogrel penetrates into human milk is unknown.
Dosage and route of administration
The instructions for use indicate that Lopirel is taken internally, regardless of food intake.
Adults and elderly people with normal activity of the isoenzyme CYP2C19
Myocardial infarction, ischemic stroke and diagnosed peripheral arterial occlusive disease
The drug is taken 75 mg once a day.
Acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q-wave)
Treatment with clopidogrel should be started with a single dose of 300 mg, then continued with a 75 mg dose once / day (in combination with acetylsalicylic acid in doses of 75-325 mg / day). Since the use of acetylsalicylic acid at higher doses is associated with an increased risk bleeding, recommended at this indication dose of acetylsalicylic acid should not exceed 100 mg. The optimal duration of treatment is not officially defined.
Clinical trials support the use of the drug for up to 12 months, the maximum favorable effect was observed by the third month of treatment.
Acute coronary syndrome with ST segment elevation (acute myocardial infarction with ST segment elevation)
Clopidogrel should be taken once 75 mg / day with the initial single dose loading dose Clopidogrel 300 mg in combination with acetylsalicylic acid in combination with thrombolytic or without combination with thrombolytics. Haveof patients older than 75 yearstreatment with clopidogrel should begin without taking its loading dose. Combination therapy is started as soon as possible after the onset of symptoms, and continues for at least 4 weeks. The efficacy of using a combination of clopidogrel and acetylsalicylic acid at this indication for more than 4 weeks has not been studied.
Atrial fibrillation (atrial fibrillation)
Clopidogrel should be taken in a dose of 75 mg 1 time / day. In combination with clopidogrel, you should start and then continue taking acetylsalicylic acid (75-100 mg / day).
Skipping the next dose
- If less than 12 hours have passed after missing the next dose, the missed dose of the drug should be taken immediately, and then the following doses should be taken at the usual time.
- If more than 12 hours have passed after missing the next dose, the patient should take the next dose at the usual time (do not take a double dose).
Patients with genetically determined reduced activity of the isoenzyme CYP2C19
The low activity of the isoenzyme CYP2C19 is associated with a decrease in the antiplatelet effect of clopidogrel. Mode of application in higher doses (loading dose - 600 mg, then 150 mg 1 time / day daily) In patients with low isozyme activity, CYP2C19 increases antiplatelet effect clopidogrel. However, at the moment, clinical trials that take into account clinical outcomes do not have an optimal regimen dosing of clopidogrel for patients with its reduced metabolism due to genetically determined low activity isoenzyme CYP2C19.
Special patient groups
In elderly volunteers over 75 years of age, when compared with young volunteers, there was no difference in platelet aggregation and bleeding time. Forelderly patientscorrection of the dose is not required.
Lopirel should not be used inchildren, t. there is no experience of its use in this group of patients.
After repeated use of clopidogrel at a dose of 75 mg / day inpatients with severe renal disease (SC from 5 to 15 ml / min)inhibition of ADP-induced platelet aggregation (25%) was lower than that of healthy volunteers, but the lengthening of bleeding time was similar to that of healthy volunteers who received clopidogrel at a dose of 75 mg / day. In addition, all patients had good tolerability of the drug.
After a daily intake of clopidogrel for 10 days at a daily dose of 75 mg ypatients with severe liver damageinhibition of ADP-induced platelet aggregation was similar to that of healthy volunteers. The mean bleeding time was also comparable in both groups.
The prevalence of the alleles of the CYP2C19 isoenzyme genes responsible for the intermediate and decreased metabolism of clopidogrel to its active metabolite differs inrepresentatives of different ethnic groups. There are only limited data for representatives of the Mongoloid race on the impact of the genotype of the isoenzyme CYP2C19 on clinical outcome events.
In a small study comparing the pharmacodynamic properties of clopidogrelmen and women, in women less inhibition of ADP-induced platelet aggregation was observed, but there was no difference in bleeding time elongation. In a large controlled study of CAPRIE (clopidogrel in comparison with acetylsalicylic acid in patients at risk of developing ischemic complications), the frequency of clinical outcomes, other side effects and deviations from the norm of clinical and laboratory indicators was the same for both men and women.
Side effects
Often there are cases of dyspepsia, pain in the digestive tract - organs, diarrhea, various bleeding.
Sometimes information is received on the occurrence of itching, rash, increased bleeding time, changes in clinical indicators of blood, vomiting, gastritis, ulcerative lesions of the gastrointestinal tract - organs, constipation, meteorism, paresthesias, dizziness, pain in the head.
Very rarely there are cases of febrile conditions, increased rates of creatinine, glomerulonephritis, arthritis, bronchospasm, arthralgia, arterial hypotension, vasculitis, anaphylaxis, rash, urticaria, depriving flat, thrombotic thrombocytopenic purpura, changes in blood, hepatitis, hallucinations, pancreatitis, confused consciousness, colitis, and taste sensory disturbances.
Overdose
When an overdose of drugs may increase the duration of bleeding and further deterioration of the condition.
- Treatment - according to the manifested symptoms.
The drug does not have a specific antidote. In extreme cases, it is possible to stop the drug by transfusing the affected platelet mass.
special instructions
Bleeding and hematologic disorders
In connection with the risk of bleeding and hematologic adverse effects in the event of the appearance during the treatment of clinical symptoms that are suspect for the onset bleeding, it is necessary to urgently do a clinical blood test, determine APTT, the number of platelets, indicators of the functional activity of platelets and carry out other necessary research.
Clopidogrel, as well as other antiplatelet drugs, should be used with caution in patients with an increased risk of bleeding associated with trauma, surgical interventions or other pathological conditions, as well as in patients receiving acetylsalicylic acid, other NSAIDs, including. inhibitors of COX-2, heparin, SSRIs or glycoprotein inhibitors IIb / IIIa.
In the treatment of clopidogrel, especially during the first weeks of treatment and / or after invasive cardiological procedures / surgical intervention, it is necessary to carefully monitor patients for the exclusion of signs bleeding, incl. hidden.
Joint use of clopidogrel with warfarin may increase the intensity of bleeding, therefore, with the exception of special rare clinical situations (such as the presence of a floating thrombus in the left ventricle, stenting in patients with atrial fibrillation) the combined use of clopidogrel and warfarin is not recommended.
If the patient is scheduled surgery, and there is no need for an antiplatelet effect, then 7 days before the operation, the use of clopidogrel should be discontinued.
Before any future operation and before starting any new drug, patients should inform the doctor (including the dentist) about taking clopidogrel.
Clopidogrel prolongs bleeding time, so the drug should be used with caution in patients with diseases predisposing to the development of bleeding (especially gastrointestinal and intraocular).
Patients should be warned that when taking clopidogrel (alone or in combination with acetylsalicylic acid) to stop bleeding may be required more time, and also that in case of occurrence at them unusual (on localization or duration) of a bleeding they should inform on it to the attending the doctor.
Recently suffered ischemic stroke
Taking Lopirel is not recommended for acute ischemic stroke with a duration of less than 7 days (because there is no data on its use in this condition).
In patients with recent ischemic stroke or transient ischemic attack and high risk of recurrent atherothrombotic events, combined therapy Clopidogrel and acetylsalicylic acid did not demonstrate a higher efficacy in comparison with monotherapy with clopidogrel, but may increase the risk of large bleeding.
Thrombotic thrombocytopenic purpura
Very rarely after the use of clopidogrel (sometimes even a short one) there have been cases of development of TTP, which is characterized by thrombocytopenia and microangiopathic hemolytic anemia, accompanied by neurological disorders, impaired renal function and fever. TTP is a potentially life-threatening condition requiring immediate treatment, including plasmapheresis.
Acquired hemophilia
With the use of clopidogrel, the acquired hemophilia was reported. In case of confirmation of prolongation of APTT with the development of bleeding or without it, the development of acquired hemophilia should be taken into account. If a diagnosis of acquired hemophilia is established, appropriate treatment should be started and the use of clopidogrel should be discontinued.
Cross reactions with thienopyridines
Since during the treatment with thienopyridines, cross-reactivity of hypersensitivity was reported before treatment it is necessary to clarify in the patient the presence of hypersensitivity reactions to thienopyridine in the history of the disease (clopidogrel, ticlopidine, prasugrel).
Tienopyridines can cause allergic reactions of varying severity, such as rash, angioedema, or haematological cross-reactions (thrombocytopenia and neutropenia). In patients who experienced allergic reactions and / or hematologic reactions in the previous treatment, one of the thienopyridine, the risk of developing similar reactions or reactions of another kind may be increased when another thienopyridine. It is recommended to control the symptoms of hypersensitivity in patients with allergic reactions to thienopyridines in the anamnesis.
Impaired renal function
The experience with clopidogrel in patients with impaired renal function is limited, so it should be used with caution in this group of patients.
Isozyme CYP2C19
Pharmacogenetics: in patients with delayed CYP2C19-mediated metabolism when taking clopidogrel in recommended doses, the active metabolite of clopidogrel is formed in smaller amounts and a weaker effect on aggregation thrombocytes. Tests are available to determine the genotype of the isoenzyme CYP2C19 in patients.
Since clopidogrel is metabolized to active metabolites in part with the participation of the CYP2C19 isoenzyme, drugs that inhibit the activity of this enzyme will lead to a decrease in the concentration of the active metabolite clopidogrel. The clinical significance of this interaction is unknown.
As a precaution, simultaneous administration of strong and moderate inhibitors of the CYP2C19 isoenzyme is not recommended.
Impaired liver function
The experience of using in patients with moderate violations of the liver, who have a risk of hemorrhagic diathesis, is limited. The drug Lopirel should be used with caution in this group of patients.
The content of lactose in the preparation
Lopirel should not be given to patients with rare hereditary intolerance to galactose, a deficiency of lactase, and a glucose-galactose malabsorption syndrome.
Impact on the ability to drive vehicles and manage mechanisms
Clopidogrel does not significantly affect the abilities necessary for driving or working with machinery.
Drug Interactions
When using the drug, it is necessary to take into account the interaction with other drugs:
- It is not recommended simultaneous administration of clopidogrel and warfarin in connection with an increased risk of bleeding.
- In view of the increased risk of bleeding, caution should be exercised while concomitant administration of clopidogrel and heparin or thrombolytic agents.
- Simultaneous administration of clopidogrel and NSAIDs increases the risk of ulcers of the gastrointestinal tract and ulcer bleeding. Therefore, care must be taken when they are assigned at the same time.
- There was no significant clinical interaction with simultaneous administration of clopidogrel and such drugs as atenolol, ACE inhibitors, cholesterol lowering agents, nifedipine, digoxin, phenobarbital, cimetidine, estrogens, theophylline.
- Clopidogrel inhibits the activity of the enzyme CYP2C19 of the cytochrome P450 system and, when combined with drugs, metabolized with the participation of this enzyme (phenytoin, tolbutamine), it is possible to increase their concentration in the plasma blood.
- Antacids do not affect the absorption of clopidogrel.
- Acetylsalicylic acid does not alter the ADP-induced platelet aggregation caused by clopidogrel. The periodic administration of acetylsalicylic acid, 500 mg twice a day, did not cause prolongation of bleeding time. Clopidogrel can potentiate the effect of acetylsalicylic acid on platelet aggregation, induced by collagen. Possible pharmacodynamic interaction of clopidogrel and acetylsalicylic acid increases the risk of bleeding, therefore joint use of them is possible not more than one year. The question of the joint application of these drugs should be comprehensively evaluated.
Reviews
By receiving Lopyrela today there are a lot of statistics and reviews. Patients write that after taking Lopirel, their clinical blood counts have improved significantly.
However, a stable good result can be achieved only after a long and regular intake of the drug. As inconvenience in use, many noted the need for daily intake, especially in the case of those people who often forgot to take a pill.
But the constant treatment after a while gives its effect. Reviews of real people about the drug Lopirel you can read below this article.
Analogues
It is difficult to say what is better, Clopidogrel or Lopirel, apply both the first and second medication equally. To the Russian and foreign analogues of Lopyrelya it is also possible to include medicinal preparations listed below:
- Atrogen,
- Zilt,
- Clopicore,
- Plavigrel,
- Tessiron,
- Gridoklyain and some others.
Before using analogues, consult your doctor.
Storage conditions and shelf life
Keep out of the reach of children at temperatures up to 30 ° C.
Shelf life - 3 years.
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