It promotes disaggregation. It inhibits aggregation of red blood cells and also enhances their ability to deform. Decreases in blood levels of factor IV and beta tromboglyukina. The action mechanism presumably due to aggregation of the fact that the drug interacts with the MP and glycoprotein II, inhibits the binding of fibrinogen to activated platelets. The mechanism of action of ticlopidine on platelets from different clenbuteral (e.g. acetylsalicylic acid), which is known to inhibit platelet aggregation induced by collagen II and stage of platelet aggregation. Ticlopidine bioavailability is 80-90%, the preparation postprandial increases bioavailability is 10-20%. Relationship to plasma proteins is 98% (bound to albumin, alpha 1-acid glycoprotein, and lipoproteins). Ticlopidine takes effect within 2 days from the beginning of the drug in 250 mg 2 times a day.
After cessation of bleeding time and other parameters of the drug blood platelets returned to normal values within two weeks. At therapeutic doses of ticlopidine has no other action except the action of the inhibitor of platelet function.
The drug is rapidly and almost completely absorbed from the gastrointestinal tract – the absorption of 80%, food intake improves the absorption of ticlopidine.
The time to reach peak serum concentration after taking the drug -. About 2 hours
Ticlopidine is metabolized primarily in the liver with the formation of four metabolites, one of which possesses pharmacological activity. In patients with impaired liver function in serum levels of ticlopidine increases.
The half Withdrawal after a single dose of 250 mg is 13 hours, against the backdrop of the regular use- 4 -5 days.
Equilibrium concentration (Css) achieved 2-3 week dosing. Upon receiving ticlopidine bleeding time can be increased twice.
Deduced through the bile path ticlopidine – 70% (unchanged), the kidney – 30% (mainly as metabolites). In urine, unchanged drug is not determined.
Prevention of thrombosis in ischemic clenbuteral stroke, thrombosis of cerebral vessels, coronary arteries. Thrombosis of peripheral vascular atherosclerosis of the arteries of the lower extremities. Prevention and reduction of platelet aggregation in patients prone to thrombotic complications in are on hemodialysis and extracorporeal circulation.
Confirmed hypersensitivity to ticlopidine. Hemorrhagic diathesis.
Disorders associated with an increased bleeding time. A hemorrhagic stroke, intracranial hemorrhage (including history). Peptic ulcer and / or duodenum in the acute phase, esophageal varices, liver failure.Hemodyscrasia history (neutropenia, thrombocytopenia, agranulocytosis).
There are no data on the safety of the drug in people younger than 18 years.
Be wary of the planned surgical interventions, trauma, severe renal insufficiency.
Dosage and administration
Adults: Dosage for the above indications is usually 250 mg (one tablet) twice a day. Due to the possibility of side effects from the gastrointestinal tract, the drug should always be taken during the main meal, for dividing the dose.
The maximum daily dose – 1 g (can be assigned only for a short period of time). In chronic renal failure dose reduction is necessary. When hemodialysis is assigned to 250-500 mg for a long period.
The most serious side effect of the drug – it is inhibition of bone marrow hematopoiesis, which manifests the change in blood counts – neutropenia, thrombocytopenia, agranulocytosis; often these changes occur in the first 3 months of treatment.
There may be such manifestations of disorders of the blood coagulation system, as local subcutaneous hematoma, epistaxis, hematuria, gastrointestinal bleeding or heavy bleeding after surgery.
During the first three months of treatment clenbuteral may cause violations the gastrointestinal tract (diarrhea, nausea, vomiting, etc.). Usually, these symptoms cease spontaneously within 2-3 weeks, and rarely cause discontinuation of treatment. Also available are: bloating, increased activity of “liver” transaminases. In rare cases, liver dysfunction (hepatitis, cholestatic jaundice).
Seldom hypersensitivity reactions (rash, pruritus, urticaria), usually in the first three months of treatment. The symptoms disappear within a few days after cessation of treatment.
Described isolated cases of severe allergic reactions such as angioneurotic edema, vasculitis; autoimmune reactions – lupus syndrome. Allergic and immunopathological reaction-Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.
Very rarely observed dizziness, abdominal pain, tinnitus.
There have been reports of rare cases of ticlopidine overdose.
An overdose manifest prolongation of bleeding time, and increased activity of alanine aminotransferase blood. These indicators have returned to normal on their own, without any additional treatment. In more serious cases of overdose you should immediately call a doctor and act in accordance with the instructions for poisoning and shock.