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medicalmeds.eu Medicines Antitrombotichesky means. Inhibitors of aggregation of thrombocytes except heparin. Platogril

Platogril

Препарат Платогрил. ООО «Кусум Фарм» Украина


Producer: LLC Kusum Pharm Ukraine

Code of automatic telephone exchange: B01AC04

Release form: Firm dosage forms. Tablets.

Indications to use: Acute myocardial infarction. Ischemic stroke. Acute coronary syndrome. Unstable stenocardia.


General characteristics. Structure:

Active ingredient: clopidogrel; 1 tablet contains клопидогреля bisulphate in recalculation on клопидогрель 75 mg.

Excipients: povidone, attracts, cellulose microcrystallic, the hydroxypropyl cellulose low-replaced
hydrogenized castor oil, covering ferrous oxide red (Е 172), covering of Opadry Y-1-7000 white: gipromelloza,
polyethyleneglycol, titanium dioxide (Е 171).




Pharmacological properties:

Pharmacodynamics. Klopidogrel selectively oppresses linkng of adenosinediphosphate (ADF) with receptors on surfaces of thrombocytes and the following activation of the GPIIb/IIIa complex under the influence of ADF and thus oppresses aggregation of thrombocytes. Biotransformation клопидогреля is necessary for formation of active inhibitor of aggregation of thrombocytes. Klopidogrel also oppresses the aggregation of thrombocytes induced by other agonists, way of blocking of increase in activity of thrombocytes the released ADF. Klopidogrel it is irreversible modifies ADF-receptors of thrombocytes. So, thrombocytes which entered interaction with klopidogrely are damaged until the end of their life cycle. Normal function of thrombocytes is recovered with a speed which answers the speed of updating of thrombocytes.
From the first day of use in repeated daily doses of 75 mg essential delay ADF-indutsirovannoy of aggregation of thrombocytes comes to light. This action amplifies progressively and stabilized between 3 and 7 days. At a stable state the average level of oppression of aggregation under the influence of a daily dose of 75 mg makes from 40% to 60%. Aggregation of thrombocytes and duration of bleeding are returned to initial level on average in 5 days after the treatment termination.

Pharmacokinetics. After repeated oral administration of a dose of 75 mg a day клопидогрель it is quickly absorbed. However concentration of the main connection in a blood plasma very low and in 2 hours after reception does not reach a measurement limit (0,00025 mg/l). Absorption makes not less than 50%, proceeding from the level of metabolites клопидогреля which are removed with urine. 
Klopidogrel is quickly metabolized in a liver. Its main metabolite (derivative carboxylic acid) is inactive and makes 85% circulating in a connection blood plasma. The maximum concentration of this metabolite in plasma (about 3 mg/l after use of repeated peroral doses of 75 mg) is reached almost in an hour after reception.
Klopidogrel is a predecessor of active ingredient. Its active metabolite (thiol derivative) is formed by oxidation клопидогреля in 2-oxo-klopidogrel with further hydrolysis. Oxidizing reaction is regulated preferential by P450 cytochrome isoenzymes – 2B6 and 3A4 and to a lesser extent – 1A1, 1A2 and 2C19. An active thiol metabolite which was allocated to in vitro quickly and it is irreversible contacts receptors of thrombocytes, suppressing, thus, aggregation of thrombocytes. This metabolite in a blood plasma does not come to light.
Kinetics of the main circulating metabolite linear (increase in concentration in plasma is proportional to a dose) within doses from 50 to 150 mg клопидогреля.
Klopidogrel and the main circulating metabolite reversibly contact proteins of in vitro plasma (98% and 94% respectively). Binding is not sated with in vitro with the broad range of concentration.

After use of a peroral dose клопидогреля with a mark 14C about 50% also nearly 46% − with a stake for 120 hours after reception are allocated with urine. The elimination half-life of the main circulating metabolite makes 8 hours after one-time and repeated reception.
Concentration of the main circulating metabolite in a blood plasma at use of 75 mg клопидогреля in days was lower at patients with a serious illness of kidneys (clearance of creatinine from 5 to 15 ml/min.) in comparison with persons with a disease of moderately severe kidneys (clearance of creatinine from 30 to 60 ml/min.) and with levels which were observed in other researches at healthy volunteers. Though oppression ADF-indutsirovannoy of aggregation of thrombocytes was lower (for 25%), than healthy volunteers, had just the same lengthening of duration of bleeding, as at healthy volunteers who accepted 75 mg клопидогреля in days. Besides, all patients had a good clinical portability.


Indications to use:

Prevention of manifestations of an aterotromboz:
- at patients, who had a myocardial infarction (an initiation of treatment – in several days, but no later than in 35 days after emergence), an ischemic stroke (an initiation of treatment – in 7 days, but no later than in 6 months after emergence) or at patients for whom the disease of peripheral arteries is diagnosed;
- at patients with an acute coronary syndrome:
- without ST segment raising (unstable stenocardia or a myocardial infarction without Q tooth), including patients to whom the stent was established during performing transdermal coronary angioplasty, in a combination with acetylsalicylic acid (ASK);
- with an acute myocardial infarction with ST segment raising in a combination with ASK (at patients who receive standard drug treatment and to whom thrombolytic therapy is shown).


Route of administration and doses:

Platogril appoint the adult. Accept 75 mg of 1 times a day, irrespective of meal.
At patients with an acute coronary syndrome without ST segment raising (unstable stenocardia or a myocardial infarction without pathological tooth of Q on an ECG) treatment by drug begin 300 mg with a single load dose, and then continue by a dose 75 mg of 1 times a day with ASK in a dose of 75-325 mg/days). As use of higher doses of ASK increases risk of bleeding, it is not recommended to exceed ASK dose in 100 mg. The optimum duration of treatment is formally not established. There are data which testify in favor of use of drug up to 12 months, and the maximum effect was observed in 3 months of treatment.
At patients with an acute myocardial infarction with ST segment raising клопидогрель appoint 75 mg of 1 times a day, since a single load dose of 300 mg in a combination with ASK (from trombolitika or without them). Treatment of patients is more senior than 75 years begin without load dose клопидогреля. The combination therapy should be begun as soon as possible after identification of symptoms and to continue, at least, 4 weeks. The advantage of use клопидогреля with ASK at this disease was not studied over 4 weeks.

Children. Safety and efficiency of use of drug are not established to children
Renal failure. Therapeutic experience of use of drug to patients with a renal failure is limited (see the section "Features of Use").
Liver failure. Therapeutic experience of use of drug to patients with diseases of a moderately severe liver and possibility of hemorrhagic diathesis is limited (see the section "Features of Use").


Features of use:

Because of risk of development of bleeding and hematologic side effects it is necessary to carry out immediately developed blood test and/or other corresponding tests if during use of drug symptoms which testify to a possibility of bleeding are observed. As well as other antithrombocytic means, клопидогрель patients should apply with care with the increased risk of bleeding owing to injuries, surgical interventions or other morbid conditions, and also in case of use of ASK, heparin, inhibitors of a glycoprotein IIb/IIIa or non-steroidal anti-inflammatory drugs (NPVS), including TsOG-2 inhibitors. It is necessary to watch closely manifestations at sick symptoms of bleeding, the concealed hemorrhage, especially for the first weeks of treatment and/or after the invasive procedures on heart or surgical intervention. Simultaneous use клопидогреля with peroral anticoagulants is not recommended as it can increase intensity of bleedings (see the section "Features of Use").
In case of planned surgical intervention which does not need use of antithrombocytic means reception клопидогреля needs to be stopped in 7 days prior to operation. Klopidogrel extends the bleeding duration therefore it should be applied with care to patients with the increased risk of bleeding (especially gastrointestinal and intraocular).
Patients need to be warned that during treatment klopidogrely (separately or in a combination with ASK) bleeding can stop later, than usually and that they have to report to the doctor about any insignificant bleeding (in the place or duration). Before surgical intervention or before reception of any new drug patients have to inform doctors (including stomatologists) that they accept клопидогрель.
Cases of the trombotichesky Werlhof's disease (TWD) after use клопидогреля, sometimes even after its short-term use were very seldom observed. TTP is followed by thrombocytopenia and mikroangiopatichesky hemolitic anemia with neurologic manifestations, renal dysfunction or heat. TTP is potentially lethal state which needs immediate treatment, including a plasma exchange.
Because of insufficient data it is not recommended to appoint клопидогрель in the first 7 days after an acute ischemic stroke.
At patients with genetically reduced CYP2C19 function smaller concentration of an active metabolite клопидогреля in plasma and less expressed antithrombocytic effect is observed. They, as a rule, have cardiovascular complications after a myocardial infarction in comparison with patients with normal functioning of CYP2C19 much more often.
Therapeutic experience of use клопидогреля patients with a renal failure is limited therefore such patients need to appoint drug with care (see the section "Route of Administration and Doses").
Experience of use of drug to patients with diseases of a moderately severe liver and possibility of hemorrhagic diathesis is limited. Therefore such patients клопидогрель need to appoint with care (see the section "Route of Administration and Doses").

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Klopidogrel does not influence or has insignificant influence on speed of response at control of motor transport or work with other mechanisms (see the section "Side reactions").


Use during pregnancy or feeding by a breast.
Due to the lack of clinical data on use клопидогреля during pregnancy, it is undesirable to appoint клопидогрель to pregnant women.
Animal experiments did not find a direct or mediate negative impact on the course of pregnancy, development of an embryo/fruit, childbirth and post-natal development.
It is not known whether it is excreted клопидогрель in the woman's milk. In researches on animals it was shown that it is excreted in breast milk. Therefore during treatment by drug Platogril feeding by a breast should be stopped.

Children. Do not apply.


Side effects:

Bleeding is the most widespread side reaction, it most often arises in the first month of treatment.
Side reactions are distributed on system of bodies, the frequency of their emergence is determined as follows: extended (> 1/100, <1/10), not widespread (> 1/1000,     <1/100), seldom widespread (> 1/10 000, <1/1000), very seldom widespread (<1/10 000).
- From system of blood: not widespread – thrombocytopenia, a leykotsitopeniya, an eosinophilia; seldom widespread – a neutropenia, including a heavy neutropenia; very seldom widespread – the trombotichesky Werlhof's disease (TWD) (see the section "Features of Use"), aplastic anemia, a pancytopenia, an agranulocytosis, heavy thrombocytopenia, a granulocytopenia, anemia.
- From immune system: very seldom widespread – a serum disease, anaphylactoid reactions.
- From mentality: very seldom widespread – hallucinations, confusion of consciousness.
- From a nervous system: not widespread – intracranial bleedings (in certain cases – with a lethal outcome), a headache, paresthesia, dizziness; very seldom widespread – change of flavoring perception.
- From an organ of sight: not widespread – bleeding in an eye (conjunctive, ocular, retinal).
- From an acoustic organ: seldom widespread – dizziness.
- From cardiovascular system: extended – a hematoma; very seldom widespread – heavy bleeding, bleeding from an operational wound, a vasculitis, arterial hypotension.
- From respiratory system: extended – nasal bleeding; very seldom widespread – bleedings from respiratory ways (a pneumorrhagia, pulmonary bleedings), a bronchospasm, an intersticial pneumonitis.
- From a digestive tract: extended – gastrointestinal bleedings, diarrhea, abdominal pain, dyspepsia; not widespread – stomach ulcer and a duodenum, gastritis, vomiting, nausea, a lock, a meteorism; seldom widespread – retroperitoneal hemorrhage; very seldom widespread – gastrointestinal and retroperitoneal bleedings with a lethal outcome, pancreatitis, colitis (in particular ulcer or lymphocytic), stomatitis.
- From gepatobiliarny system: very seldom widespread – an acute liver failure, hepatitis, abnormal results of indicators of function of a liver.
- From skin: extended – hypodermic hemorrhage; not widespread – rashes, an itch, intradermal hemorrhages (purpura); very seldom widespread – violent dermatitis (a toxic epidermal necrolysis, Stephens-Johnson's syndrome, a multiformny erythema), a Quincke's disease, erythematic rashes, urticaria, eczema, flat deprive.
- From a musculoskeletal system: very seldom widespread – musculoskeletal hemorrhages (hemarthrosis), arthritis, an arthralgia, mialgiya.
- From an urinary system: not widespread – a hamaturia; very seldom widespread – a glomerulonephritis, increase in level of creatinine in blood.
- General disturbances: very seldom widespread – fever.
- Laboratory indicators: not widespread – lengthening of a bleeding time, decrease in quantity of neutrophils and thrombocytes.


Interaction with other medicines:

As клопидогрель turns into the active metabolite partially under the influence of CYP2C19, use of drugs which reduce activity of this enzyme, most likely, will lead to reduction of concentration of an active metabolite клопидогреля in plasma, and also to decrease in clinical performance. It is necessary to avoid simultaneous use of drugs which oppress activity of CYP2C19.
It is necessary to avoid simultaneous use of inhibitors of the proton pump, except for cases when it is extremely necessary. Proofs that other drugs which reduce products of acid in a stomach such as, for example, H2 locks or antacids, influence antithrombocytic activity клопидогреля no.
Belong to drugs which oppress activity of CYP2C19 омепразол, esomeprazole, флувоксамин, fluoxetine, моклобемид, вориконазол, флуконазол, тиклопидин, ciprofloxacin, Cimetidinum, carbamazepine, окскарбазепин and chloramphenicol.

Oral anticoagulants (warfarin). Simultaneous use of drug Platogril with oral anticoagulants is not recommended as it can increase intensity of bleeding (see the section "Features of Use").

IIb/IIIa glycoprotein inhibitors. Klopidogrel patients who receive the accompanying IIb/IIIa glycoprotein inhibitors should apply with care and therefore can have the increased risk of increase in bleeding caused by an injury, surgical intervention or other morbid conditions.

Acetylsalicylic acid (ASK). Acetylsalicylic acid does not change inhibitory action клопидогреля on ADF-indutsirovannuyu aggregation of thrombocytes, but клопидогрель strengthens action of ASK on the aggregation of thrombocytes induced by collagen. However simultaneous use of 500 mg of ASK twice a day for days essentially did not increase duration of the bleeding caused by reception клопидогреля. Pharmakodinamichesky interaction between klopidogrely and ASK is possible, at the same time it results in the increased risk of bleeding. Thus, it is necessary to be careful rather simultaneous use of these drugs.

Heparin. Klopidogrel does not cause need of change of a dose of heparin and does not modify influence of heparin on a blood coagulation. Simultaneous use of heparin does not influence the oppression of aggregation of thrombocytes caused klopidogrely. Between klopidogrely and heparin perhaps and it leads Pharmakodinamichesky interaction to growth of risk of bleeding. Thus, it is necessary to be careful at simultaneous use of these drugs.

Thrombolytic means. At patients with an acute myocardial infarction at simultaneous use клопидогреля, fibrinospetsifichesky or fibrinonespetsifichesky thrombolytic means and heparins the frequency of cases of clinically meaning bleedings is similar to that which is observed on condition of introduction of thrombolytic means and heparin along with ASK.

Non-steroidal anti-inflammatory drugs (NPVS). Simultaneous use клопидогреля and Naproxenum increases quantity of the concealed gastrointestinal hemorrhages. However because of insufficiency of researches of interaction with other NPVS it is still not found out whether the risk of gastrointestinal bleeding at use of NPVS increases. So, simultaneous use of NPVS, including TsOG-2 inhibitors, and клопидогреля has to be carried out with care.

Other accompanying therapy. Clinically meaning pharmakodinamichesky interaction was not observed if клопидогрель applied along with atenololy, nifedipine or with both drugs. Besides, pharmakodinamichesky activity клопидогреля remained almost not changed at simultaneous use of phenobarbital, Cimetidinum or estrogen.

The pharmacokinetics of digoxin and theophylline does not change at simultaneous use клопидогреля. Antacids do not influence extent of absorption клопидогреля.
Carboxyl metabolites клопидогреля can suppress activity of P4502C9 cytochrome. Potentially it can lead to increase in level in a blood plasma of such drugs as Phenytoinum and Tolbutamidum, and NPVS which are metabolized by P4502C9. Phenytoinum and Tolbutamidum can safely be applied along with klopidogrely.
Except for information concerning the interaction with specific medicines which is stated above клопидогреля with medicines which are usually appointed the patient with aterotrombozy were not conducted a research concerning interaction. However patients who used at the same time other drugs including diuretics, beta-blockers, inhibitors of an angiotensin-converting enzyme, antagonists of calcium, means which reduce cholesterol level, coronary vazodilatator, anti-diabetic means (including insulin), antiepileptic means, gormonozamestitelny therapy and antagonists of GPIIb/IIIa have no clinically meaning side effect.


Contraindications:

Hypersensitivity to active ingredient or to any component of drug. Heavy liver failure; acute bleeding (for example, round ulcer or intracraneal hemorrhage); hereditary intolerance of a galactose, deficit of lactase of Lapp or disturbance of malabsorption of glucose galactose. Pregnancy or period of feeding by a breast. Children's age.


Overdose:

At overdose клопидогреля lengthening of a bleeding time with the subsequent complications can be observed. In case of developing of bleeding the symptomatic treatment is recommended.
The antidote клопидогреля is unknown. In need of an immediate correcting of the extended bleeding time клопидогреля it can be terminated by transfusion of a platelet concentrate.


Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children.


Issue conditions:

According to the recipe


Packaging:

On 14 tablets in the blister; on 2 blisters in a cardboard box.



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