Trade Names:Ticlid- Tablets 250 mgApo-Ticlopidine (Canada)Gen-Ticlopidine (Canada)Nu-Ticlopidine (Canada)Sandoz Ticlopidine (Canada)
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.
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.
Ticlopidine is metabolized extensively by the liver; only trace amounts are detected in urine.
Ticlopidine t ½ is 4 to 5 days.
Average plasma concentration is slightly higher in cirrhosis.
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.
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.
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.
PO 250 mg twice daily with food.
Store at room temperature.
May reduce ticlopidine absorption.Aspirin
Increased effect of aspirin on collagen-induced platelet aggregation.Cimetidine
Elevated ticlopidine levels with possible increase in therapeutic and toxic effects.Theophylline
Elevated serum theophylline concentrations, increasing risk of toxicity.Phenytoin
Elevated phenytoin plasma levels with associated somnolence and lethargy have been reported. Exercise caution when administering with ticlopidine.
None well documented.
Headache; peripheral neuropathy; dizziness.
Maculopapular or urticarial rash; rash; pruritus.
Diarrhea; nausea; fullness; dyspepsia; GI pain; purpura; vomiting; flatulence; anorexia.
Prolonged bleeding time; bleeding complications (ecchymosis, epistaxis, hematuria, conjunctival hemorrhage, GI bleeding, perioperative bleeding); neutropenia; pancytopenia; hemolytic anemia; serum sickness; immune thrombocytopenia; abnormal LFTs; TTP; agranulocytosis; eosinophilia; bone marrow depression.
Hepatitis; cholestatic jaundice; increased alkaline phosphatase, serum transaminases, and bilirubin.
Increased cholesterol and triglycerides.
Weakness; pain; allergic pneumonitis; systemic lupus erythematosus; arthropathy; myositis; hyponatremia; aplastic anemia; hepatic necrosis; peptic ulcer; renal failure; sepsis; angioedema; hepatocellular jaundice.
Life-threatening events including neutropenia, agranulocytosis, thrombotic thrombocytopenic purpura (TTP), and aplastic anemia. Severe hematological problems may occur within a few days after the start of therapy. Thus, monitor hematologically and clinically. Immediately discontinue therapy at any evidence of neutropenia or TTP. TTP incidence peaks at 3 to 4 wk posttherapy initiation. Neutropenia risk peaks at 4 to 6 wk posttherapy initiation. Aplastic anemia risk peaks at 4 to 8 wk posttherapy initiation. Perform CBC with ANC, platelet count, and appearance of the peripheral smear at baseline and every 2 wk during therapy for the first 3 mo.
Category B .
Safety and efficacy in children under 18 yr not established.
Require dosage reduction.
Reactions range from minor to life-threatening.
Dosage reduction or discontinuation of therapy may be required if hemorrhagic or hematopoietic complications occur.
Use not recommended because patient may have preexisting bleeding diathesis.
May cause increased serum cholesterol and triglycerides.
Use with caution in patients who have lesions with a propensity to bleed.
Fatal reactions (eg, pancytopenia) have occurred.
Use with caution in patients who may be at risk of increased bleeding from trauma, surgery, or pathological conditions.
Increased bleeding time, increased ALT.
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