Ticlopidine hydrochloride
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Classification: Platelet aggregation inhibitor Action/Kinetics: Irreversibly inhibits ADP-induced platelet-fibrinogen binding and subsequent platelet-platelet interactions. This results in inhibition of both platelet aggregation and release of platelet granule constituents as well as prolongation of bleeding time. Peak plasma levels: 2 hr. Maximum platelet inhibition: 8-11 days after 250 mg b.i.d. Steady-state plasma levels: 14-21 days. t 1/2, elimination: 4-5 days. After discontinuing therapy, bleeding time and other platelet function tests return to normal within 14 days. Rapidly absorbed; bioavailability is increased by food. Highly bound (98%) to plasma proteins. Extensively metabolized by the liver with approximately 60% excreted through the kidneys; 23% is excreted in the feces (with one-third excreted unchanged). Clearance of the drug decreases with age. Uses: To reduce the risk of fatal or nonfatal thrombotic stroke in clients who have manifested precursors of stroke or who have had a completed thrombotic stroke. Due to the risk of neutropenia or agranulocytosis, use should be reserved for clients who are intolerant to aspirin therapy. Investigational: Chronic arterial occlusion, coronary artery bypass grafts, intermittent claudication, open heart surgery, primary glomerulonephritis, subarachnoid hemorrhage, sickle cell disease, uremic clients with AV shunts or fistulas. Contraindications: Use in the presence of neutropenia and thrombocytopenia, hemostatic disorder, or active pathologic bleeding such as bleeding peptic ulcer or intracranial bleeding. Severe liver impairment. Lactation. Special Concerns: Use with caution in clients with ulcers (i.e., where there is a propensity for bleeding). Consider reduced dosage in impaired renal function. Geriatric clients may be more sensitive to the effects of the drug. Severe hematological side effects (including thrombotic thrombocytopenic purpura) may occur within a few days of the start of ticlopidine therapy. Safety and effectiveness have not been established in children less than 18 years of age. Side Effects: Hematologic: Neutropenia, agranulocytosis, thrombotic thrombocytopenia purpura, thrombocytopenia, pancytopenia, immune thrombocytopenia, hemolytic anemia with reticulocytosis. GI: Diarrhea, N&V;, GI pain, dyspepsia, flatulence, anorexia, GI fullness, peptic ulcer. Hepatic: Hepatitis, cholestatic jaundice, hepatocellular jauncide, hepatic necrosis. Bleeding complications: Ecchymosis, hematuria, epistaxis, conjunctival hemorrhage, GI bleeding perioperative bleeding, posttraumatic bleeding, intracerebral bleeding (rare). Dermatologic: Maculopapular or urticarial rash, pruritus, urticaria. Rarely, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome. CNS: Dizziness, headache. Neuromuscular: Asthenia, SLE, peripheral neuropathy, arthropathy, myositis. Miscellaneous: Tinnitus, pain, allergic pneumonitis, vasculitis, nephrotic syndrome, renal failure, angioedema, hyponatremia, serum sickness.
Laboratory Test Alterations:
Drug Interactions:
How Supplied: Tablet: 250 mg
Dosage
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Alkaline phosphatase, ALT, AST, serum cholesterol, and triglycerides. Abnormal LFTs.
Ticlopidine plasma levels
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