Ticlopidine inhibits platelet aggregation. It causes a dose-dependent inhibition of platelet aggregation and release of certain platelet factors, and prolongation of bleeding time.
The drug has no significant activity in vitro, but only in vivo. There was identified ticlopidine actively circulating metabolites.
Ticlopidine inhibits platelet aggregation by inhibiting what is anastrozole binding of fibrinogen to the platelet membrane. Unlike aspirin, it does not inhibit cyclooxygenase. Cyclic platelets apparently not play a role in the mechanism of action.
After discontinuation of therapy in most patients with bleeding time and other platelet function returns to normal within one week. Inhibition of platelet aggregation occurs within two days from the beginning of the use of ticlopidine twice a day.
The maximum effect is reached at 5-8 days of treatment at a dose of 250 mg twice a day. The therapeutic dose of ticlopidine inhibits . Lower doses cause proportionally less inhibition of platelet aggregation.
Following oral administration a unit dose disposable ticlopidine absorption occurs fast, with the achievement of the maximum plasma level after 2 hours after administration.
Absorption is almost complete. Appointment of ticlopidine after meals improves bioavailability.
Stable in plasma drug levels are achieved after 7-10 days of administration of 250 mg twice a day. The average what is anastrozole of ticlopidine at sustainable levels is approximately 30-50 hours. However, no inhibition of platelet aggregation depends on the concentration level of the drug in plasma.
Ticlopidine is metabolized in the liver. After oral administration of the drug, radiolabeled, 50-60% was found in the urine of 23-30% – in the feces.
The main clinical trials were conducted with the participation of a group of patients with mean age 64. Pharmacokinetics ticlopidine modified in elderly patients, but its pharmacological and therapeutic activity at a dose of 500 mg per day, regardless of the age.
– prevention of arterial thrombotic events (stroke, myocardial infarction, vascular death) in patients with ischemic stroke caused by cerebral atherosclerosis.
– Prevention of ischemic events, particularly coronary, in patients with coronary heart disease in patients with chronic diseases of the arteries of the lower extremities (intermittent claudication).
– Prevention of re-thrombosis in chronic hemodialysis.
– Allergy to ticlopidine in history.
– Haemorrhagic diathesis.
– Diseases with a tendency to bleeding (gastric ulcer or duodenal ulcer, hemorrhagic stroke).
– Diseases of the blood with prolongation of bleeding time.
– Hematologic abnormalities (leukopenia, thrombocytopenia or agranulocytosis in history) .
– Severe hepatic impairment.
– Pregnancy and lactation. The caution used in patients with impaired hepatic function (see “Special instructions”.) with renal insufficiency, surgical interventions, trauma and other pathological conditions with the risk of bleeding. Efficacy and safety of ticlopidine in children has not been established.
Dosage and administration
for adults only.
For oral administration.
For all indications drug administered in a dose of 250 mg 2 times a day, during or after meals. The maximum daily dose may be 1 gram (can be assigned only for a short period of time).
In chronic renal failure dose reduction is necessary
Side effects: From the side of hematopoiesis system leukopenia (neutropenia, agranulocytosis), pancytopenia, bone marrow aplasia (especially pronounced in elderly patients), hemolytic anemia, thrombocytopenia (isolated or conjugated with hemolytic anemia). Very rarely thrombotic thrombocytopenic purpura.
On the part of the hemostatic system
From the gastrointestinal tract
Nausea, diarrhea, pain in the stomach, rarely cytolytic and / or cholestatic hepatitis. Isolated or combined increased alkaline phosphatase, transaminases and bilirubin during the first 4 months of treatment.
With the skin side
polymorphic skin rash, often accompanied by itching. In very rare cases, there is erythema multiforme.
Very rarely observed various forms of immune-alllergicheskih reactions: very rarely – anaphylactic reaction, angioedema, arthralgia, vasculitis, lupus syndrome, allergic pneumonitis, and nephropathy. We describe an extremely rare case of high temperatures.
From the nervous system
Dizziness, headache, tinnitus, asthenia.
Within 1-4 months of treatment can be observed ticlopidine increase what is anastrozole and triglycerides in the serum 8-10%. With continued treatment further increase is observed. The proportion between the lipoprotein subfractions (especially between) remain unchanged. These clinical experiments have shown that this effect is not dependent on age, sex, or the presence of alcohol consumption, and diabetes does not affect the cardiovascular risk.