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Chinch 75 28’s 75 mg film-coated tablets

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Description

The instruction for medical use of KLOPI-75 medicine the Trade name of KLOPI-75 the International unlicensed name Klopidogrel Lekarstvennaya the Tablet form, film coated, 75 mg Structure One tablet contains active agent – klopidogret bisulphate of 99.875 mg (it is equivalent to a klopidogrel of 75.0 mg), excipients: lactoses monohydrate (Famatoz DCL 11), hydroxypropyl cellulose (LHPC-LH 21), silicon dioxide colloidal anhydrous (aerosil 200), castor oil hydrogenirovanny (HR Cutin), dimetikon 100cSt, structure of a film cover: Instacoat Universal Pink A05G30176 (gipromelloz (HPMC 2910), polyethyleneglycol 400, titan dioxide (E171), gland (III) oxide red (E172)). The description of the Tablet of rounded shape, biconvex, film coated, pink color, with an engraving of L II on the one hand Pharmacotherapeutic group Anticoagulants. Inhibitors of aggregation of thrombocytes, excepting heparin. Klopidogrel the ATX B01AC04 Code klopidogret the Pharmacological Pharmacokinetics Later properties of single and repeated oral administration in a dose of 75 mg a day quickly is soaked up. Average peak plasma concentration of not changed klopidogrel (about 2.2-2.5 ng/ml after single oral administration in a dose of 75 mg) were noted, approximately, in 45 minutes after reception. Judging by the metabolites of a klopidogrel allocated with urine, absorption of not less than 50%. Klopidogrel and his main (inactive) metabolite circulating in blood form reversible communication with proteins of plasma (98 and 94%, respectively). This communication is not saturable in the wide range of concentration. Klopidogrel is exposed to intensive metabolism in a liver. Klopidogrel is metabolized in two based ways: one is mediated by esterases and leads to hydrolysis with education inactive derivative carboxylic acid (85% of the metabolites which are in a blood-groove), another is mediated by various P450 cytochromes. At first klopidogret it is metabolized to an intermediate metabolite, 2-oxo-klopidogrela. The subsequent metabolism of an intermediate metabolite 2-oxo-klopidogrela leads to formation of an active metabolite, thiol derivative klopidogrel. This way of metabolism is mediated by CYP3A4, CYP2C19, CYP1A2 and CYP2B6. An active thiol metabolite quickly it is also irreversible contacts receptors of thrombocytes, suppressing thereby aggregation of thrombocytes. Cmax of an active metabolite increases twice, as after a single load dose of a klopidogrel of 300 mg, and after reception of a maintenance dose of 75 mg within 4 days. Cmax is observed approximately in 30-60 minutes after reception. After reception klopidogrelya, about, 50% also, about, 46% are allocated with urine – with stool within 120 hours. After reception of one tablet of 75 mg the elimination half-life klopidogrelya makes 6 hours. Elimination half-life of the main circulating (inactive) metabolite makes 8 hours after single and repeated receptions. The renal failure After repeated doses klopidogrelya on 75 mg a day at patients with a serious illness of kidneys (clearance of creatinine from 5 to 15 ml/min.) suppression of the aggregation of thrombocytes provoked by adenosinediphosphate (ADF) was lower (25%), than at healthy subjects, however, lengthening of a bleeding time was similar to that which it was observed at the healthy subjects receiving 75 mg of a klopidogrel a day. All patients had a good clinical tolerance. After repeated doses of a klopidogrel on 75 mg a day within 10 days the patients with heavy dysfunction baking suppression of the aggregation of thrombocytes provoked by ADF had a similar abnormal liver function to the suppression observed at healthy subjects. Average lengthening of a bleeding time in both groups was similar. KLOPI-75 pharmacodynamics – inhibitor of aggregation of thrombocytes. Klopidogrel is pro-medicine, one of metabolites of which is inhibitor of aggregation of thrombocytes. The active metabolite of a klopidogrel selectively inhibits linking of adenosinediphosphate (ADF) with his platelet receptor of P2Y12 and the subsequent, caused by ADF activation of the glycoprotein GPIIb/IIIa complex, interfering thereby aggregations of thrombocytes. Owing to irreversibility of binding the thrombocytes which were affected are damaged for all remained term of the life (approximately, 7-10 days), and restoration of normal function of thrombocytes is carried out with a speed corresponding to a platelet cycle. The aggregation of thrombocytes caused by agonists other than ADF is suppressed by blocking of strengthening of the activation of thrombocytes which is carried out under the influence of the released ADF too. As the active metabolite is formed by means of CYP450 enzymes, some of them are polymorphic or are suppressed with other medicinal connections, not at all patients the extent of oppression of thrombocytes is sufficient. Repeated doses on 75 mg a day from the first day led to considerable oppression of the aggregation of thrombocytes caused by ADF. The inhibiting effect amplified progressively and reached an equilibrium state in 3-7 days. In a stage of an equilibrium state the average level of inhibition observed at a dose of 75 mg a day was from 40% to 60%. Aggregation of thrombocytes and a bleeding time gradually returned to initial level, as a rule, in 5 days after treatment cancellation. Indications Prevention of aterotrombotichesky events – the adult patients having a myocardial infarction (from several days to less than 35 days), an ischemic stroke (from 7 days to less than 6 months), or patients with the diagnosed disease of peripheral arteries – the adult patients suffering from a syndrome of acute coronary insufficiency: – a syndrome of acute coronary insufficiency without raising of a segment of ST (unstable stenocardia or a myocardial infarction without tooth Q), including the patient, exposed to stenting during percutaneous coronary intervention, in a combination with acetylsalicylic acid (ASK), – an acute myocardial infarction with raising of a segment of ST in a combination with ASK at patients on drug treatment, suitable for performing thrombolytic therapy, Prevention of aterotrombotichesky and thromboembolic events in an atrial fibrillation – adult patients with an atrial fibrillation who have at least one risk factor of vascular events, patients with intolerance of the antagonists of vitamin K (AVK) and risk of bleeding, for which low, for prevention of aterotrombotichesky and thromboembolic events, including a brain stroke, in a combination with ASK. A route of administration and doses For intake. It is possible to accept regardless of meal. Adult and elderly patients of KLOPI-75 it is necessary to accept 75 mg in a single daily dose. At patients, the suffering syndrome of acute coronary insufficiency: – a syndrome of acute coronary insufficiency without raising of a segment of ST (unstable stenocardia or a myocardial infarction without tooth Q): treatment of KLOPI-75 has to be begun with a single load dose of 300 mg, and then is continued by a dose of 75 mg once a day (with acetylsalicylic acid in a dose of 75-325 mg a day). As higher doses of ASK were accompanied by the increased risk of bleeding, it is recommended that the dose of ASK did not exceed 100 mg. The maximum positive effect is observed after 3 months of treatment. – an acute myocardial infarction with raising of a segment of ST: KLOPI-75 should accept in a single daily dose 75 mg, since a load dose of 300 mg, in a combination with ASK and other thrombolytic means or without them. At patients 75 years are more senior treatment of KLOPI-75 should be begun without load dose. Combination therapy should be begun as soon as possible after emergence of symptoms and to continue, at least, within 4 weeks. Patients with an atrial fibrillation of KLOPI-75 should appoint 75 mg in the single daily dose equal. It is necessary to begin reception of ASK (75-100 mg a day) and to continue its use in a combination with klopidogrely. If the dose is passed: – there passed less than 12 hours after the usual planned drug intake time: patients should accept a dose immediately and after that to accept the following dose during the usual planned drug intake – there passed more than 12 hours: patients should accept the following dose during the usual planned drug intake, but it is impossible to accept a double dose. A renal failure Experience of treatment of patients with disturbance of renal function is limited (see. Special instructions). An abnormal liver function Experience of treatment of patients with a disease of a liver of moderate severity at whom hemorrhagic diathesis is possible is limited. Side effects Bleeding is the most frequent reaction registered both in clinical trials and in the post-marketing period. Often (≥1/100, 1/10) – a hematoma and a traumatic bruise – nasal bleeding – gastrointestinal bleeding, diarrhea, an abdominal pain, dyspepsia – bleeding in the place of a puncture Infrequently (≥1/1000, & lt, 1/100) – thrombocytopenia, a leukopenia, an eosinophilia – intracraneal hemorrhage (it was reported about several cases with a lethal outcome), a headache, paresthesia, dizziness – a hematopsia (conjunctival, ocular, retinal) – ulcer of stomach and duodenum, gastritis, vomiting, nausea, a constipation, a meteorism – rash, an itching, hemorrhage in skin (purple) – a hamaturia – lengthening of a bleeding time, decrease in number of neutrophils, decrease in number of thrombocytes Is rare (≥1/10000, & lt, 1/1000) – a neutropenia, including heavy – vertigo (vestibular dizziness) – retroperitoneal bleeding is Very rare (& lt, 1/10000) – the trombotichesky Werlhof’s disease (TWD), aplastic anemia, a pancytopenia, an agranulocytosis, heavy thrombocytopenia, the acquired hemophilia And, a granulocytopenia, anemia – a serum disease, anaphylactoid reactions – hallucinations, confusion of consciousness – disturbance of flavoring perception – heavy bleeding, bleeding from an operational wound, a vasculitis, hypotension – bleedings of a respiratory path (pneumorrhagia, pulmonary bleeding), a bronchospasm, an interstitial pneumonitis, eosinophilic pneumonia – gastrointestinal and retroperitoneal bleeding with a lethal outcome, pancreatitis, colitis (including ulcer or lymphocytic), stomatitis – an acute liver failure, hepatitis, pathological indicators of analyses of function of a liver – bullous dermatitis (a toxic epidermal necrolysis, a syndrome Stephens-Johnson, a mnogoformny erythema), the Quincke’s disease caused by drug intake a hypersensitivity syndrome, the medicinal rash which is followed by an eosinophilia and system manifestations (DRESS syndrome), erythematic or exfoliative rash, a small tortoiseshell, eczema and flat deprive – skeletal and muscular bleeding (hemarthrosis), arthritis, an arthralgia, myalgia – a glomerulonephritis, increase in level of creatinine in blood – fever Frequency is unknown – the hypersensitivity which developed as a result of cross-responsiveness to thienopyridinic drugs, such as tiklopidin and prasugret Contraindications – hypersensitivity to active ingredient or to any of medicine components – heavy abnormal liver functions – acute pathological bleeding, including, bleeding in a peptic ulcer of a stomach and a 12-perstny gut, ulcers of a gullet or intracraneal hemorrhage – pregnancy and the period of a lactation – intolerance of a galactose, deficiency of Lappa lactase or malabsorption of glucose galactose – children’s age up to 18 years Medicinal interactions Oral anticoagulants: simultaneous use of a klopidogrel with oral anticoagulants is not recommended as this combination can strengthen bleeding. In spite of the fact that reception of 75 mg of a klopidogrel a day did not change pharmacokinetics of S-warfarin and the international normalized relation (INR) at patients, is long accepting therapy by warfarin, the concomitant use of a klopidogrel with warfarin increases risk of bleeding because of independent effects on a hemostasis of both drugs. IIb/IIIa glycoprotein inhibitors: klopidogret it is necessary to apply with care at patients who at the same time receive IIb/IIIa glycoprotein inhibitors. Acetylsalicylic acid (ASK): ASK does not change the oppression of the aggregation of thrombocytes induced by ADF caused klopidogrely however klopidogret enhances effect of ASK on the aggregation of thrombocytes induced by collagen. Nevertheless, the concomitant use of ASK on 500 mg twice a day for day did not cause significant increase in the bleeding time caused by reception of a klopidogrel. Between klopidogrely and acetylsalicylic acid perhaps pharmakodinamichesky interaction which leads to the increased risk of bleeding. Therefore, simultaneous use of these drugs should be carried out with care. Nevertheless, klopidogret and ASK were appointed in common up to one year. Heparin: Simultaneous use of heparin did not influence oppression of the aggregation of thrombocytes caused klopidogrely. Between klopidogrely and heparin perhaps pharmakodinamichesky interaction which leads to the increased risk of bleeding. Therefore, simultaneous use of these drugs has to be carried out with care. Thrombolytic means: safety of combined use klopidogret with fibrinspetsifichesky and nefibrinspetsifichesky thrombolytic means and heparins was investigated on patients with an acute myocardial infarction. Frequency of clinically significant bleedings was similar to that that it was observed at use of thrombolytic means and heparin together with ASK. Non-steroidal anti-inflammatory drugs (NPVS): in the clinical trials conducted with participation of healthy volunteers, combined use of a klopidogrel and Naproxenum increased the hidden blood loss from digestive tract. However, owing to lack of sufficient clinical trials on interactions with other NPVS, it is not clear now whether the increased risk of gastrointestinal bleedings is characteristic of all NPVS. Therefore, simultaneous use of NPVS (including TsOG-2 inhibitors) and the klopidogrela demands care. Selective serotonin reuptake inhibitors (SIOZ): as SIOZ influence activation of thrombocytes and increase risk of bleedings, their joint appointment with klopidogrely demands care. Other at the same time carried out therapy: as klopidogret it is metabolized to the active metabolite partially by means of CYP2C19, it is expected that use of the medicines suppressing activity of this enzyme will lead to decrease in medicinal concentration of an active metabolite of a klopidogrel. The clinical importance of this interaction is not clear. For precaution, it is not necessary to approve simultaneous use of strong or moderate CYP2C19 of inhibitors. Omeprazolum and esomeprazole, fluvoksamin, fluoxetine, moklobemid, vorikonazol, flukonazol, tiklopidin, ciprofloxacin, Cimetidinum, carbamazepine, okskarbazepin and chloramphenicol belong to the medicines suppressing CYP2C19. Inhibitors of a Protonew Pomp (IPP): The omeprazolum in a dose of 80 mg once a day which was accepted either along with klopidogrely, or with observance of a 12-hour interval between intake of two medicines, reduced exposure of an active metabolite by 45% (load dose) and 40% (maintenance dose). Decrease was connected from 39% (load dose) and 21% (maintenance dose) with decrease in suppression of aggregation of thrombocytes. It is expected that the esomeprazole which was accepted along with klopidogrely will also lead to decrease in exposure of an active metabolite. Contradictory data on clinical value of this pharmacokinetic (FC) / the pharmakodinamichesky (FD) interaction expressed in important cardiovascular events were provided both to observant, and in clinical trials. As a precautionary measure it is not necessary along with klopidogrely to apply omeprazolum or esomeprazole. Less significant decrease in exposure of a metabolite were observed in case of a pantoprazol and a lansoprazol. Plasma concentration of an active metabolite were reduced by 20% (load dose) and for 14% (maintenance dose) during treatment pantoprazoly in a dose on 80 mg once a day. It sop
ovozhdatsya by decrease in average inhibition of aggregation of thrombocytes by 15% and 11% respectively. These results mean that klopidogret it is possible to apply together with pantoprazoly. Proofs that other medicines lowering acidity in a stomach such as H2 receptors blockers (except for Cimetidinum which is CYP2C19 inhibitor) or antacids, affect antithrombocytic activity of a klopidogrel no. Other medicines: Clinically important pharmakodinamichesky interactions were not observed when klopidogret it was applied together with atenolol or nifedipine or with these both substances. Simultaneous use of phenobarbital or estrogen had no significant effect on pharmakodinamichesky activity of a klopidogrel. The pharmacokinetics of digoxin and theophylline did not change at simultaneous use of a klopidogrel. Antiacid means did not change extent of absorption of a klopidogrel. Phenytoinum and tolbutamide which are metabolized by means of CYP2C9 can be applied with safety along with klopidogrely. Besides drugs mentioned above the researches of interaction of a klopidogrel with other medicines which are usually appointed to patients with aterotrombozy were not conducted. However for the patients accepting along with klopidogrely, the most various drugs, clinically significant undesirable interactions were not noted. Diuretics, beta blockers, inhibitors of angiotensin-converting enzyme (APF inhibitors), antagonists of calcium, drugs for decrease in level of cholesterol, coronary vazodilatator, antidiabetic drugs (including insulin), antiepileptic means and also blockers of GPIIb/IIIa-receptors are among the specified drugs. Special indications of Bleeding and hematologic disturbances Because of risk of bleeding and hematologic undesirable reactions during treatment at emergence of the clinical symptoms indicating bleeding it is necessary to make at once the general blood test and/or to carry out other corresponding analyses. Also as well as other antithrombocytic means, KLOPI-75 should be applied with care at patients who can be subject to the risk of the strengthened bleeding connected with an injury, surgical or other morbid conditions and also at the patients who are on treatment of ASK, heparin, inhibitors of a glycoprotein IIb/IIIa or non-steroidal anti-inflammatory drugs (NPVS) including TsOG-2 inhibitors or the selective serotonin reuptake inhibitors (SSRI). It is necessary to control carefully patients on presence of any symptoms of bleeding, including the concealed hemorrhage, especially, in the first weeks of treatment and/or after the invasive procedures on heart or surgical intervention. Simultaneous use of KLOPI-75 with oral anticoagulants as it can enhance intensity of bleeding is not recommended. If the patient has to transfer elective surgical intervention, and the antithrombocytic effect is temporarily undesirable, reception of a klopidogrel should be stopped in 7 days prior to operation. Before any planned operation and intake of any new medicine the patients have to warn doctors and stomatologists that they accept KLOPI-75. KLOPI-75 extends a bleeding time and has to be applied with care at patients with the pathological defeats contributing to bleeding (especially, gastrointestinal and intraocular). Patients should be informed that at reception of KLOPI-75 (one or in a combination with ASK) for a stop of bleeding more time, than usually can be required and that they should inform the attending physician if they have unusual (on localization or duration) a bleeding. The Trombotichesky Werlhof’s Disease (TWD) Very seldom, after use of KLOPI-75, and sometimes and after short exposure, cases of the trombotichesky Werlhof’s disease (TWD) were noted. It is characterized by thrombocytopenia and mikroangiopatichesky hemolytic anemia accompanied by neurologic changes, dysfunction of kidneys or fever. The TPP is potentially deadly state demanding immediate treatment including a plasma exchange. The acquired hemophilia It was reported that reception of KLOPI-75 leads to development of the acquired hemophilia. The possibility of development of the acquired hemophilia should be considered at the confirmed isolated increase in the activated partial tromboplastinovy time (APTT), with bleeding or without. With the confirmed diagnosis of the acquired hemophilia and tracking their state experts have to carry out treatment of patients, and reception of KLOPI-75 should be cancelled. The acute ischemic stroke In view of lack of data, cannot be recommended to KLOPI-75 in the first 7 days after an acute ischemic stroke. P450 2C19 cytochrome (CYP2C19) Pharmacogenetics: In a case to patients who are slow metabolizator of CYP2C19 at the recommended doses at a klopidogrel less active metabolites are formed, and it renders smaller effect on function of thrombocytes. There are tests for definition at patients of a genotype of CYP2C19. As KLOPI-75 is metabolized to the active metabolite partly thanks to CYP2C19, use of medicines which suppress activity of this enzyme will lead, as expected, to reduced levels of an active metabolite of a klopidogrel. The clinical importance of this interaction is at the moment not defined. As a precautionary measure, along with this drug use strong or average effect of CYP2C19 inhibitors is not recommended. Cross-reactions among thienopyridines In connection with the messages about development of cross-responsiveness among thienopyridines, patients it is necessary to survey on existence in the anamnesis of hypersensitivity to thienopyridines (for example, klopidogret, tiklopidin, prazugret). Thienopyridines can become the reason of development of allergic reactions from easy to heavy degree, such as rash, Quincke’s disease or hematologic cross-reactions as thrombocytopenia and a neutropenia. Patients at whom in the anamnesis the allergic reaction and/or hematologic reaction to one of thienopyridines was shown can have the increased risk of development of the same or other reaction to other thienopyridines. At patients with the known allergic reaction to thienopyridines it is recommended to conduct monitoring of signs of hypersensitivity. A renal failure Experience of treatment of KLOPI-75 of patients with a renal failure is limited. Therefore, in case of such patients of KLOPI-75 it is necessary to apply with care. An abnormal liver function Experience on drug use by patients with an abnormal liver function of moderate severity, inclined to hemorrhagic diathesis, is limited. In this regard, in this population of KLOPI-75 it has to be applied with care. Use in pediatrics Safety and efficiency of use of KLOPI-75 for children and teenagers is younger than 18 years are not established. The feature of influence of medicine on ability to run the vehicle or potentially dangerous KLOPI-75 mechanisms does not influence or has insignificant impact on ability to drive the car and working mechanisms. Overdose Symptoms: lengthening of a bleeding time with the subsequent complications of bleeding. Treatment: antidote of pharmacological activity klopidogrelya is not found. If fast correction of the extended bleeding time is necessary, transfusion of thrombocytes can stop effects of KLOPI-75. The form of release and packing On 14 tablets place in blister strip packaging from aluminum foil (Alu/Alu). On the 2nd blister strip packagings together with the instruction for medical use in the state and Russian languages place in a pack from cardboard. To Store storage conditions at a temperature not above 25o With to Store out of children’s reach! 2 years not to apply a period of storage after an expiration date. Prescription status According to the prescription the Name and the country of the Macleods Pharmaceuticals Limited 304, Atlanta Arcade, Marol Church Road, Andheri (East), Mumbai manufacturing organization – 400,059, India. The holder of the registration certificate of Macleods Pharmaceuticals Limited, India the Name and the country of the organization of the packer of Macleods Pharmaceuticals Limited, India the Address of the organization in the territory of the Republic of Kazakhstan, the accepting claim (offer) on quality of medicines from consumers and responsible for post-registration observation of safety of medicine: Branch KOO Macleods Pharmaceuticals Limited, Republic of Kazakhstan Almaty, Tulebayev St. 38/61, 5
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