TICLOPIDINE

TICLOPIDINE
(ti-clo'pi-deen)
Ticlid
Classifications: anticoagulant; antiplatelet agent;
Therapeutic: antiplatelet
Prototype: Clopidogrel
Pregnancy Category: B

Availability

250 mg tablets

Action

Platelet aggregation inhibitor that interferes with platelet membrane functioning and therefore platelet interactions.

Therapeutic Effect

Prevents release of platelet constituents and prolongs bleeding time.

Uses

Reduction of the risk of thrombotic stroke in patients intolerant to aspirin.

Unlabeled Uses

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).

Contraindications

Hypersensitivity to ticlopidine; hematopoietic disease, coagulopathy; leukemia; pathologic bleeding; severe liver impairment; lactation.

Cautious Use

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

Stroke Prevention
Adult: PO 250 mg b.i.d. with food

Administration

Oral

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: Dizziness. GI: Nausea, vomiting, abdominal cramps; dyspepsia, flatulence, anorexia; abnormal liver function tests (few cases of hepatotoxicity reported). Hematologic: Neutropenia (resolves in 1–3 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 3–6 wk).

Diagnostic Test Interference

Increases total serum cholesterol by 8–10% within 4 wk of beginning therapy. Lipoprotein ratios remain unchanged. Elevates alkaline phosphatase and serum transaminases.

Interactions

Drug: antacids 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 levels. Food: Food may increase bioavailability of ticlopidine.

Pharmacokinetics

Absorption: 90% absorbed from GI tract; increased absorption when taken with food. Onset: Antiplatelet activity, 24–48 h; maximal effect at 3–5 d. Peak: Peak serum levels at 2 h. Duration: Bleeding times return to baseline within 4–10 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 4–5 d with repeated dosing.

Nursing Implications

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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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