Classifications: anticoagulant; antiplatelet agent; Therapeutic: antiplatelet
Pregnancy Category: B
250 mg tablets
Platelet aggregation inhibitor that interferes with platelet membrane functioning and therefore platelet interactions.
Prevents release of platelet constituents and prolongs bleeding time.
Reduction of the risk of thrombotic stroke in patients intolerant to aspirin.
Prevention of venous thromboembolic disorders; maintenance of bypass graft patency and of vascular access sites in hemodialysis
patients; improvement of exercise performance in patients with ischemic heart disease and intermittent claudication; prevention
of postoperative deep venous thrombosis (DVT).
Hypersensitivity to ticlopidine; hematopoietic disease, coagulopathy; leukemia; pathologic bleeding; severe liver impairment;
Hepatic function impairment, renal impairment; patients at risk for bleeding from trauma, surgery, or a bleeding disorder;
GI bleeding; pregnancy (category B). Safe use in children <18 y not established.
Route & Dosage
Adult: PO 250 mg b.i.d. with food
- Give with food or just after eating to minimize GI irritation.
- Discontinue anticoagulants or fibrinolytic drugs before ticlopidine administration.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)CNS:
Nausea, vomiting, abdominal cramps; dyspepsia, flatulence, anorexia; abnormal liver function tests (few cases of hepatotoxicity
Neutropenia (resolves in 13 wk), thrombocytopenia, leukopenia, agranulocytosis
(usually within first 3 mo), and pancytopenia
; hemorrhage (ecchymosis, epistaxis, menorrhagia, GI bleeding), thrombotic thrombocytopenia purpura
(usually within first month). Skin:
Urticaria, maculopapular rash, erythema nodosum (generally occur within the first 3 mo of therapy, with most occurring within
the first 36 wk).
Diagnostic Test Interference
Increases total serum cholesterol by 810% within 4 wk of beginning therapy. Lipoprotein ratios remain unchanged. Elevates alkaline phosphatase and serum transaminases.
decrease bioavailability of ticlopidine. anticoagulants
increase risk of bleeding. Cimetidine
decreases clearance of ticlopidine. corticosteroids
counteract increased bleeding time associated with ticlopidine. May decrease cyclosporine
levels (one case report). Increases theophylline
half-life by 42%, possibly increasing theophylline
serum levels. May increase phenytoin
Food may increase bioavailability of ticlopidine.
90% absorbed from GI tract; increased absorption when taken with food. Onset:
Antiplatelet activity, 2448 h; maximal effect at 35 d. Peak:
Peak serum levels at 2 h. Duration:
Bleeding times return to baseline within 410 d. Distribution:
90% bound to plasma proteins. Metabolism:
Rapidly and extensively metabolized in liver. Elimination:
Only 1% excreted unchanged; 60% of metabolites excreted in urine, 23% in feces. Half-Life:
12.6 h; terminal half-life is 45 d with repeated dosing.
Assessment & Drug Effects
- Lab tests: Monitor platelet count and bleeding time periodically. Monitor CBC with differentials q2wk from second week to
end of third month of therapy and thereafter if S&S of infection develop.
- Report promptly laboratory values indicative of neutropenia, thrombocytopenia, or agranulocytosis.
- Monitor for signs of bleeding (e.g., ecchymosis, epistaxis, hematuria, GI bleeding).
Patient & Family Education
- Report promptly to physician any of the following: Nausea, diarrhea, rash, sore throat, or other signs of infection, signs
of bleeding, or signs of cholestasis (e.g., yellow skin or sclera, dark urine or clay-colored stools).
- Understand risk of GI bleeding; do not take aspirin along with ticlopidine.
- Do not take antacids within 2 h of ticlopidine.
- Keep appointments for regularly scheduled blood tests.