Deplatt-75

General characteristics. Structure:

Active ingredient: 75 mg of a klopidogrel.

Vspomogayushchy substances: a mannitol (Е 421), lactose anhydrous, a tselyulloza microcrystallic, кросповидон, polyethyleneglycol, silicon dioxide colloid anhydrous, talc, the oil ricinic hydrogenated magnesium stearate, a gidroksipropilmetiltselyulloz, titanium dioxide (Е 171), ferrous oxide red (Е 172).

Pharmacological properties:

Pharmacodynamics. Inhibitor of aggregation of thrombocytes. Selectively inhibits linkng of adenosinediphosphate (ADF) with receptors of thrombocytes and activation of the GPIIb/IIIa complex, oppressing, thus, aggregation of thrombocytes. Also inhibits the aggregation of thrombocytes caused by other agonists, way of blockade of increase in activity of thrombocytes the released ADF. Does not influence activity of FDE.

Klopidogrel it is irreversible changes ADF receptors on thrombocytes therefore thrombocytes remain nonfunctional throughout all "life", and recovery of normal function happens in process of their updating (approximately in 7 days).

Pharmacokinetics. After intake in a dose of 75 mg klopidogret quickly it is absorbed from a GIT. However concentration in a blood plasma increases slightly and in 2 h after reception does not reach the level which is giving in to definition (0.025 mkg/l).

It is intensively metabolized in a liver. The main metabolite is to inactive derivatives of carboxyl acid and makes about 85% of the initial substance circulating in plasma. Cmax of this metabolite in a blood plasma after repeated receptions of a klopidogrel makes about 3 mg/l and is observed approximately in 1 h after reception.

The pharmacokinetics of the main metabolite is characterized by linear dependence in the range of doses of a klopidogrel of 50-150 mg.

Klopidogrel and the main metabolite it is irreversible contact proteins of a blood plasma of in vitro (98% and 94% respectively). This communication remains to not saturable in vitro over a wide range of concentration.

After reception of a vnutr14s-mechenny klopidogrel about 50% of the accepted dose are allocated with urine and about 46% with a stake during the 120th p. T1/2 of the main metabolite make 8 h.

In comparison with healthy volunteers of young age concentration in a blood plasma of the main metabolite is much higher at elderly patients (at the age of 75 years and is more senior), at the same time changes of aggregation of thrombocytes and a bleeding time are not noted.

At a serious illness of kidneys (KK of 5-15 ml/min.) of concentration of the main metabolite in a blood plasma lower, than at diseases of moderately severe kidneys (KK of 30-60 ml/min.) and at healthy volunteers. Though the inhibiting effect on ADF-indutsirovannuyu aggregation of thrombocytes decreased in comparison with that at healthy volunteers, the bleeding time increased as much as at healthy volunteers.

Indications to use:

Prevention of trombotichesky complications at patients with a myocardial infarction, an ischemic stroke or occlusion of peripheral arteries. In a combination with acetylsalicylic acid for prevention of trombotichesky complications at an acute coronary syndrome: with raising of a segment of ST at a possibility of performing thrombolytic therapy; without raising of a segment of ST (unstable stenocardia, a myocardial infarction without Q tooth), including at the patients who are exposed to stenting.

Prevention of trombotichesky and tromboembolic episodes, including a stroke, at fibrillation of auricles (ciliary arrhythmia) with, at least, one risk factor of development of vascular complications, lack of a possibility of reception of indirect anticoagulants and existence of low risk of development of bleeding (in a combination with acetylsalicylic acid).

Route of administration and doses:

Accept in 1 times/days. An initial and maintenance dose - 75 mg/days. A load dose - 300 mg/days. The scheme of use depends on indications and a clinical situation.

Features of use:

Use at pregnancy and feeding by a breast. Adequate and strictly controlled clinical trials of safety of use of a klopidogrel at pregnancy were not conducted. Use is possible only in emergency cases.

It is unknown whether it is allocated klopidogret with breast milk at the person. In need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

In pilot studies on animals at use of a klopidogrel in doses of 300-500 mg/kg/days teratogenic action and negative influence on fertility and on fetation is not revealed. It is established that klopidogret and its metabolites are allocated with breast milk.

Use at abnormal liver functions. With care apply klopidogret at patients with heavy abnormal liver functions at which developing of hemorrhagic diathesis is possible.

Special instructions. With care apply klopidogret at the increased risk of bleedings owing to an injury, operative measures, disturbances of system of a hemostasis. At the planned surgical interventions (if antiagregantny action is undesirable) klopidogret it is necessary to cancel in 7 days prior to operation.

With care apply klopidogret at patients with heavy abnormal liver functions at which developing of hemorrhagic diathesis is possible.

At emergence of symptoms of excessive bleeding (bleeding of gums, menorrhagias, a hamaturia) the research of system of a hemostasis (a bleeding time, quantity of thrombocytes, tests of functional activity of thrombocytes) is shown. Regular control of laboratory indicators of functional activity of a liver is recommended.

With care to apply along with warfarin, heparin, NPVS, it is long - with acetylsalicylic acid since now safety of such use is not finalized.

In pilot studies cancerogenic and genotoksichesky action is not revealed.

Influence on ability to driving of motor transport and to control of mechanisms. Influence of a klopidogrel on ability to driving of motor transport and to control of mechanisms is not established.

Side effects:

From coagulant system of blood: often - bleedings; infrequently - increase in a bleeding time.

From the alimentary system: very often - gastrointestinal bleeding, diarrhea, abdominal pains, dyspepsia; infrequently - stomach ulcer and a duodenum, vomiting, nausea, a lock, abdominal distention; seldom - a retroperitoneal hemorrhage; very seldom - gastrointestinal bleeding and a retroperitoneal hemorrhage from the death, pancreatitis, colitis (including nonspecific ulcer colitis or lymphocytic colitis), stomatitis, an acute liver failure, hepatitis, an aberration of indicators of function of a liver.

From system of a hemopoiesis: infrequently - thrombocytopenia, a leukopenia, an eosinophilia; seldom - a neutropenia, including a heavy neutropenia; very seldom - a trombotichesky Werlhof's disease, aplastic anemia, a pancytopenia, an agranulocytosis, heavy thrombocytopenia, a granulocytopenia, anemia.

From a nervous system: infrequently - intracraneal hemorrhage (it was reported about several cases from the death), a headache, paresthesia, dizziness; very seldom - disturbances of flavoring perception, a hallucination, confusion of consciousness.

From sense bodys: infrequently - eye hemorrhages (conjunctival, in fabrics and a retina of an eye); seldom - вертиго.

From cardiovascular system: very seldom - a vasculitis, decrease in the ABP.

From respiratory system: often - nasal bleeding; very seldom - bleeding from respiratory tracts (a pneumorrhagia, pulmonary bleeding), a bronchospasm, intersticial pneumonia.

From immune system: very seldom - a serum disease, anaphylactoid reactions.

From skin and hypodermic fabrics: often - hypodermic bruises; infrequently - rash, an itch, a purpura (hypodermic hemorrhage); very seldom - violent dermatitis (a toxic epidermal necrolysis, Stephens-Johnson's syndrome, a mnogoformny erythema) a Quincke's disease, erythematic rash, a small tortoiseshell, eczema, flat deprive.

From a musculoskeletal system: very seldom - hemorrhages in muscles and joints, arthritis, an arthralgia, a mialgiya.

From an urinary system: infrequently - a hamaturia; very seldom - a glomerulonephritis, increase in concentration of creatine in blood.

Others: often - bleeding from the place of puncturation of vessels; very seldom - fever.

Interaction with other medicines:

At simultaneous use with NPVS (including Naproxenum) the risk of developing of gastrointestinal bleedings increases.

At simultaneous use with acetylsalicylic acid strengthening of antiagregantny action is possible.

As klopidogret can inhibit activity of an isoenzyme of CYP2C9, at simultaneous use with the drugs which are metabolized with the participation of this isoenzyme (including with Phenytoinum, tolbutaminy) it is impossible to exclude increase in their concentration in a blood plasma.

Contraindications:

Acute bleeding (including at a round ulcer or intracraneal hemorrhage), a heavy liver failure, pregnancy, the period of a lactation (breastfeeding), children's and teenage age up to 18 years, hypersensitivity to a klopidogrel.

Overdose:

At overdose lengthening of a bleeding time with the subsequent complications can be observed.

Symptomatic treatment. The specific antidote is unknown. In need of bystry correction of the extended bleeding time клопидогреля it can be terminated by transfusion of a platelet concentrate.

Storage conditions:

Period of validity - 3 years. To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

10 pieces - blisters (3) - packs cardboard.
10 pieces - blisters (10) - packs cardboard.