Plaviks

Плавикс Drug photo

The description is actual on 18.04.2016

  • Latin name: Plavix
  • ATH code: B01AC04
  • Active ingredient: Klopidogrel (Clopidogrel)
  • Producer: Sanofi-Winthrop Industrie (France)

Structure

300 or 75 mg of a klopidogrel can be a part of one tablet of drug of Plaviks.

Additional substances: castor oil, a macrogoal 6000, opadray pink, Mannitolum, the low-substituted hypro rod, microcrystallic cellulose, wax.

Release form

Pink, coated tablets (300 mg) of oblong shape, with an engraving "300" on one surface and an engraving "1332" on other surface.

  • 10 pieces in the blister — 3 or 1 blisters in a paper pack.

Pink, coated tablets (75 mg) of oblong shape, with an engraving "75" on one surface and an engraving of "the I I7I" on other surface.

  • 7 pieces in the blister — 2, 1 or 3 blisters in a paper pack.
  • 10 pieces in the blister — 2, 1 or 3 blisters in a paper pack.
  • 14 pieces in the blister — 2, 1 or 3 blisters in a paper pack.

Pharmacological action

Anti-aggregation action.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Klopidogrel is pro-medicine, that is in itself he does not render effect, and one of its metabolites which blocks aggregation of thrombocytes is active. The specified active metabolite selektivno inhibits reaction of adenosinediphosphate with P2Y12 receptor on a surface of thrombocytes that causes the subsequent induction of glycoprotein IIb/IIIa of a complex. It provokes braking of aggregation of thrombocytes. Because the described binding is irreversible, thrombocytes during all the term of life (7-10 days) remain resistant to stimulation of ADF, and normalization of their function happens only after updating of thrombocytes.

The pasting of thrombocytes caused various to stimulators (not including ADF), is also slowed down due to blockade of activation of thrombocytes by molecules ADF.

The active metabolite is produced by means of P450 cytochrome isoenzymes which can possess polymorphism or be blocked by other drugs therefore not at all patients adequate oppression of aggregation of thrombocytes is guaranteed. At everyday reception on 75 mg of drug from the first day of treatment aggregation suppression which slowly increases for 3-7 days is noted and then becomes constant. Aggregation of thrombocytes in an equilibrium state is suppressed approximately for 40-60%. All listed above functions gradually return to norm within 5 days after phase-out of a klopidogrel.

Weaker ADF-indutsiruyemaya platelet aggregation is observed at women, however sexual distinctions in increase in a bleeding time are not observed.

Drug it is proved reduces risk of emergence of complications (including a lethal outcome) at persons with recently developed stroke, a heart attack and the revealed occlusal illness.

Pharmacokinetics

Active agent possesses ability to be soaked up quickly. The greatest concentration are reached approximately 1 hour later after reception. Klopidogrel and his main inactive metabolite contact plasma proteins for 96%.

It is intensively transformed in a liver by hydrolysis with formation of an inert metabolite of carboxyl acid and through a complex of P450 cytochrome under the influence of which klopidogret turns in 2-oksoklopidogret, and then and in a tiolny metabolite of a klopidogrel (active).

This metabolite quickly it is also irreversible reacts with receptors to surfaces of thrombocytes, inhibiting their aggregation.
5 days later after administration of drug by the person about 50% of substance are allocated with urine and 46% with a stake. Time of semi-removal of a klopidogrel comes by 6 o'clock. Time of semi-removal of the basic of inactive derivative makes about 8 hours.

Pharmacogenetics

Thanks to an isoenzyme of CYP2C19 it is produced active and intermediate metabolites. The pharmacokinetics and force of action of the main metabolite vary depending on genetically programmed like CYP2C19 enzyme. The patients having genes of loss of function of this enzyme are called weak metabolizator. Occurrence of weak metabolizator of an isoenzyme of CYP2C19 at the population of Caucasian race makes 2%, patients of negroid race have about 4%, and Chinese have about 14%.

Indications to Plaviks's use

Indications to Plaviks's use 75 mg

Prevention of aterotrombotichesky complications (in combination with Aspirin) at persons with an acute coronary syndrome regardless of existence of raising of a piece of ST on an ECG, including after stenting.

Indications to Plaviks's use 300 mg

Prevention of aterotrombotichesky complications:

  • at persons with a heart attack prescription to 35 days, with a stroke of ischemic type prescription of 7-28 weeks or with the revealed occlusion of peripheral arteries;
  • persons with an acute coronary syndrome regardless of existence of raising of a piece have ST on an ECG, including after stenting.

Prevention of tromboembolic and aterotrombotichesky episodes (including a stroke) at development of fibrillation of auricles:

  • at the persons suffering from fibrillation of auricles with risk factors of emergence of vascular complications which cannot accept anticoagulants of indirect type and have the lowered risk of bleeding (in combination with Aspirin).

Contraindications

  • Heavy insufficiency of function of a liver.
  • Acute bleeding (including intracraneal hemorrhage or ulcer bleeding).
  • Hereditary lack of lactase, intolerance of a galactose, glucose galactose absorption disturbance syndrome.
  • Pregnancy and lactation.
  • Age less than 18 years.
  • Hypersensitivity to any of means components.

Medicine is appointed with care at a liver failure of moderate severity with predisposition to bleeding; renal failure; at the diseases creating predisposition to emergence of bleedings; at simultaneous use of the drugs damaging mucous bodies of a digestive tract; at persons with the increased risk of bleedings (surgical interventions, injuries other states) or receiving Aspirin, Heparin, Warfarin, IIb/IIIa glycoprotein blockers, anti-inflammatory nonsteroid drugs, selective blockers of the return serotonin reuptake; at persons with low activity of CYP2C19 enzyme; at hematologic and allergic reactions to thienopyridines (Tiklopidin, Prazugrel); after recent temporary frustration of cerebral circulation or a stroke of ischemic type.

Side effects

  • Reactions from coagulation: increase in a bleeding time, purple, nasal bleeding, bruises, hamaturia, hematomas, eye hemorrhages, intracraneal and other hemorrhages.
  • Reactions from a hemopoiesis: an eosinophilia, a neutropenia, an agranulocytosis, a granulocytopenia, a leukopenia, aplastic anemia, hemophilia And the acquired type, thrombocytopenia.
  • Reactions from nervous activity: dizziness, change of flavoring perception, paresthesia, headache, vertigo.
  • Reactions from digestion: development of an ulcer, dyspepsia, diarrhea, gastritis, nausea, abdominal pains, lock, abdominal distention, vomiting, colitis, stomatitis, pancreatitis, hepatitis, liver failure of acute type.
  • Reactions from skin: flat deprive, eczema, violent dermatitis, a Quincke's disease, rash, the small tortoiseshell, an itch.
  • Allergic reactions: anaphylactoid phenomena, serum disease.
  • Reactions from mentality: confusion, hallucinations.
  • Reactions from blood circulation: vasculitis, hypotension.
  • Reactions from breath: intersticial pneumonia, bronchospasm, eosinophilic pneumonia.
  • Reactions from a musculoskeletal system: arthritis, arthralgia, mialgiya.
  • Reactions from secretory system: glomerulonephritis.
  • General and laboratory reactions: fever, change of indicators of a condition of function of a liver, increase in creatinine in blood.

Application instruction of Plaviks (Way and dosage)

Medicine is taken orally, regardless of meal.

Tablets on 300 mg are created for use as load dose to persons with an acute coronary syndrome.

Plaviks, application instruction

At treatment of a heart attack, ischemic stroke or occlusion of peripheral arteries of Plaviks appoint to accept 75 mg of times a day.

At treatment of an acute coronary syndrome without increase of a piece of ST (a heart attack without Q tooth on an ECG, unstable stenocardia) Plaviks it is necessary to begin to use equal 300 mg from the single use of a load dose. In the subsequent to continue reception of means in a dose of 75 mg of times a day together with Aspirin in a dose of 75-325 mg a day. The optimum duration of therapy is not determined, the greatest favorable effect comes to light by 3rd month of therapy.

At treatment of an acute coronary syndrome with increase of a piece of ST appoint to an ECG of 75 mg of drug to accept once a day with single use of a load dose together with Aspirin and trombolitika or without such combination. At persons 75 years therapy are more senior begin without load dose. Such treatment is begun as far as possible earlier after development of symptoms and continued for not less than 4 weeks.

At treatment of fibrillation of auricles appoint administration of drug on 75 mg once a day. Together with Plaviks it is necessary to take Aspirin in a dose of 75-100 mg a day.

Admission of reception of a dose

If after the admission of reception passed till 12 o'clock, then it is necessary to drink immediately passed dose, and to accept the subsequent doses as before, in usual time.

If after the admission of reception there passed over 12 hours, then the patient has to use the following dose in usual time.

Special groups of patients

Correction of dosages is not required to elderly patients.

Overdose

Overdose signs: prolongation of bleeding and complication in the form of emergence of bleedings of various localization.

Overdose treatment: at emergence of bleeding it is necessary to carry out the corresponding therapy including if necessary introduction of a platelet concentrate. The selective antidote does not exist.

Interaction

At persons, it is long accepting Warfarin, simultaneous use of a klopidogrel increases risk of bleeding in connection with additional independent influence of the last on processes of coagulability of blood. It is necessary to be careful at joint reception of the specified drugs.

Reception of blockers of receptors of GPIIb/IIIa together with klopidogrely also demands care from persons with existence of the increased risk of bleedings (operations, injuries or other states).

Between Aspirin and klopidogrely possibly farmakodinamichesky interaction leading to increase of risk of emergence of bleeding therefore at a similar combination it is necessary to observe extra care.

Sharing of a klopidogrel and Naproxenum raises the hidden losses of blood bodies of a digestive tract.

Selective blockers of the return serotonin reuptake break stimulation of thrombocytes and increase risk of bleeding, combined use of the specified means demands care.

As klopidogret it is transformed with formation of the main metabolite with the participation of CYP2C19 enzyme, administration of drugs, oppressing this isoenzyme (Esomeprazole, Omeprazol, Vorikonazol, Fluvoksamin, Moklobemid, Fluoxetine, Okskarbazepin, Ciprofloxacin, Tiklopidin, Flukonazol, Cimetidinum, Carbamazepine, Chloramphenicol) can lead to lowering of concentration of the main metabolite of a klopidogrel. Similar combinations should be avoided in spite of the fact that values of this effect it is not established.

Between Plaviks and Heparin the farmakodinamichesky interaction increasing risk of bleedings (at the specified combination care is necessary) is also not excluded.

It is necessary to avoid sharing of a klopidogrel and inhibitors of a pomp of the protons which are CYP2C19 isoenzyme blockers. If use inhibitors of a pomp of protons does not manage to be avoided, then it is necessary to use drug from this group (Pantoprazol, Lansoprazol) with the smallest effect of blocking of an isoenzyme of CYP2C19.

Terms of sale

According to the recipe.

Storage conditions

To protect from children. To store at a temperature up to 30 degrees.

Period of validity

Three years.

Special instructions

In the first weeks of treatment by drug or after carrying out invasive cardiological interventions it is necessary to conduct fixed supervision over patients for an exception of symptoms of bleeding which can be and hidden.

Because of risk of bleeding and undesirable hematologic effects in case of development during treatment of symptoms, suspicious on bleeding, it is necessary to make urgently blood test, a koagulogramma, to investigate number of thrombocytes, indicators of activity of thrombocytes and to make other necessary analyses.

Klopidogrel (as well as other antithrombocytic means) need to be applied with care at the persons having the increased probability of development of bleeding because of injuries, surgeries or other states and also at taking Aspirin, anti-inflammatory nonsteroid drugs, Heparin or blockers of a glycoprotein of IIb/IIIa.

At the planned surgical intervention, when there is no need of antithrombocytic therapy, reception of a klopidogrel should be stopped one week prior to operation.

Drug raises a bleeding time therefore it should be used with care at the persons having predisposition to bleedings. Klopidogret means which are capable to cause ulcerations of mucous bodies of a digestive tract in the patients receiving, it is also necessary to apply with care.

Before any planned operation and prior to use of any new drug patients have to report to the attending physician about use of a klopidogrel.

Extremely seldom after reception of a klopidogrel cases of Werlhof's trombotichesky disease (thrombocytopenia, hemolitic mikroangiopatichesky anemia, disturbances of work of kidneys, neurologic symptomatology, fever) which is a state, life-threatening and demanding carrying out urgent measures were revealed.

During treatment it is necessary to exercise control of work of a liver. At serious damages of a liver it is necessary to consider risk of hemorrhagic diathesis.

Use of a klopidogrel is not recommended at the acute stroke which is had less than 7 days ago.

Plaviks's analogs

Plaviks's analogs: Klapitaks, Klopigrant, Zilt, Agregal, Brilinta, Detromb, Deplatt-75, Kardogrel, Kardutol, Klopidogrel, Klopideks, Klopidogrel-Richter, Plogrel, Klopilet, Troken, Lirta, Egitromb, Klopidogrel-TAD, Lopirel, Klopidogrel-Teva, Plagril, Targetek, Klopidogrel-SZ, Trombexum, Tromborel.

Drug Plaviks and its analogs have broad dispersion of the prices, the last look on this background more favourably because of the moderate price. Drugs Co-Plaviks, Aspigrel and Klopiks Forte – good replacement to the combined treatment by Plaviks and Aspirin.

About Plaviks's analogs confirm lack of cardinal differences between their efficiency and efficiency of the described means.

Zdravzona

  • Koplaviks 100 mg +75mg tablet No. 28
  • Plaviks 75 mg No. 14 tabletkisanofi-Aventis
  • Plaviks 75 mg No. 28 tabletkisanofi-Aventis
  • Koplaviks 100 mg +75mg tablet No. 14
  • Koplaviks 100 mg +75mg tablet No. 100

Drugstore of IFC

  • Koplaviks tbl p/pl/o 100 mg +75mg No. 28, Sanofi-Winthropfrantion
  • Plaviks tbl p / about 75 mg No. 28, Sanofi-Winthropfrantion
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Apteka24

  • Plavikssanofi Winthrop Industrie (France)
  • Plavikssanofi Winthrop Industrie (France)
  • Plavikssanofi Winthrop Industrie (France)

BIOSPHERE

  • Co-Plaviks of 75 mg / 100 mg No. 28 tabl.p.p.o.sanofi-Winthrop Industrie (France)
  • Plaviks 75 mg No. 14 tabl.p.o.sanofi-Winthrop Industrie (France)
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Section: Cardiological Cardiovascular
in more detail

Education: Graduated from the Vitebsk state medical university majoring in "Surgery". At university headed Council of students' scientific society. Professional development in 2010 - in "Oncology" and in 2011 - in "A mammology, visual forms of oncology".

Experience: Work in an all-medical network 3 years the surgeon (The Vitebsk hospital of an emergency medical service, Lioznensky TsRB) and in combination the regional oncologist and the traumatologist. Work farm the representative within a year in the Rubicon company.

Provided 3 improvement suggestions on the subject "Optimization of an Antibioticotherapia depending on Species Composition of Microflora", 2 works took prizes in a republican competition review of student's scientific works (1 and 3 categories).
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