Ticlopidine Hydrochloride

Trade Names: Ticlid - Tablets 250 mg

Pharmacology

Produces time- and dose-dependent inhibition of both platelet aggregation and release of platelet granule constituents as well as prolongation of bleeding time; interferes with platelet membrane function by inhibiting platelet-fibrinogen binding and subsequent platelet-platelet interactions.

Pharmacokinetics

Absorption

Ticlopidine is rapidly absorbed with peak levels (T _max ) occurring about 2 after dose. The drug is greater than 80% absorbed. Administration after meals results in a 20% increase in the AUC. Ticlopidine is 98% bound to plasma proteins.

Metabolism

Ticlopidine is metabolized extensively by the liver; only trace amounts are detected in urine.

Elimination

Ticlopidine t _½ is 4 to 5 days.

Special Populations

Average plasma concentration is slightly higher in cirrhosis.

Indications and Usage

Reduction of risk of thrombotic stroke in patients who have experienced stroke precursors and in patients who have had completed thrombotic stroke. Reserved for patients intolerant to aspirin because of greater risk of adverse reactions.

Unlabeled Uses

Improved walking distance in intermittent claudication; vascular improvement in chronic arterial occlusion; reduced incidence of neurologic deficit in subarachnoid hemorrhage; reduced incidence of vascular occlusion in uremic patients with arteriovenous shunts or fistulas; control of platelet count in open heart surgery; decreased graft occlusion in coronary artery bypass grafts; reduced degree of proteinuria and hematuria in primary glomerulonephritis; reduced incidence, duration, and severity of infarctive crises in sickle cell disease.

Contraindications

Presence of hematopoietic disorders (eg, neutropenia, thrombocytopenia); history of thrombotic thrombocytopenic purpura (TTP); presence of hemostatic disorder or active pathologic bleeding (eg, bleeding, peptic ulcer, intracranial bleeding, hemophilia, other coagulation defects); severe liver impairment.

Dosage and Administration

PO 250 mg twice daily with food.

Storage/Stability

Store at room temperature.