TICLID

Ticlopidine is an effective inhibitor of platelet aggregation.

It is a prodrug that is metabolised to an active form, which blocks the ADP receptor that is involved in GPIIb/IIIa receptor activation leading to platelet aggregation.

Ticlopidine is marketed under the brand name Ticlid and is indicated for patients who cannot take aspirin or in whom aspirin has not worked to prevent a thrombotic stroke.

FDA label includes a black-box warning of neutropenia, aplastic anemia, thrombotic thrombocytopenia purpura, and agranulocytosis, so it is necessary to monitor patients'WBC and platelets when they are taking ticlopidine.

Used in patients, who have had a stroke or stroke precursors and who cannot take aspirin or aspirin has not worked, to try to prevent another thrombotic stroke.

Ticlopidine is a prodrug that is metabolised to an as yet undetermined metabolite that acts as a platelet aggregation inhibitor.

Inhibition of platelet aggregation causes a prolongation of bleeding time.

In its prodrug form, ticlopidine has no significant in vitro activity at the concentrations attained in vivo.

is greater than 80%.

Food increases absorption by approximately 20%.

The volume of distribution was not quantified.

Ticlopidine is metabolized extensively by the liver with only trace amounts of intact drug detected.

At least 20 metabolites have been identified.

Hover over products below to view reaction partners Ticlopidine 2-Chloroticlopidine 2-Oxoticlopidine Active metabolite of Ticlopidine Thienodihydropyridinium Ticlopidine lactam analog (M8) Thienopyridinium Ticlopidine S-oxide Ticlopidine S-oxide dimer Dehydrogenated ticlopidine Ticlopidine N-oxide di-Hydroxyticlopidine 7-Hydroxyticlopidine.

Ticlopidine is eliminated mostly in the urine (60%) and somewhat in the feces (23%).

following a single 250-mg dose is approximately 7.9 hours in subjects 20-43 years of age and 12.6 hours in subjects 65-76 years of age.

With repeated dosing (250 mg twice a day), half-life is about 4 days in subjects 20-43 years of age and about 5 days in subjects 65-76 years of age.

Ticlopidine clearance was not quantified, but clearance decreases with age.

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Single oral doses of ticlopidine at 1600 mg/kg and 500 mg/kg were lethal to rats and mice, respectively.

Symptoms of acute toxicity were

GI hemorrhage, convulsions, hypothermia, dyspnea, loss of equilibrium and abnormal gait.

FDA label includes a black-box warning of neutropenia, aplastic anemia, thrombotic thrombocytopenia purpura, and agranulocytosis, so it is necessary to monitor patients'WBC and platelets when they are taking ticlopidine.