Oral Prophylaxis of subacute stent occlusion after intracoronary stenting
Adult: As an adjunct to aspirin: 250 mg bid, to be started before or on the day of the stent placement and continued for 4-6 weeks.
Oral Prophylaxis of thrombotic stroke
Adult: In patients with history of precursors of stroke or those who have had a completed stroke, who are intolerant or unresponsive to aspirin: 250 mg bid.
Dose reduction or discontinuation may be required if haemorrhagic or haematopoietic disorders occur.
Should be taken with food.
Haemostatic disorders, active pathological bleeding (e.g. peptic ulcer bleeding, intracranial bleeding), history of or current haematopoietic disorders (e.g. neutropenia, thrombocytopenia, agranulocytosis, thrombotic thrombocytopenic purpura, aplastic anaemia). Severe hepatic impairment.
Patients with increased risk of bleeding (e.g. peptic ulcer disease, surgery or trauma, other pathologic conditions); acute lower gastrointestinal bleeding, drug-eluting stents, previous hypersensitivity to thienopyridines (e.g. clopidogrel, prasugrel), pre-existing hypercholesterolaemia. Consider discontinuation of therapy 10-14 days prior to elective surgery if antiplatelet effect is not desirable. Moderate to severe renal and mild to moderate hepatic impairment. Pregnancy and lactation. Concomitant administration with anticoagulants and other antiplatelet agents.
Significant: Prolonged bleeding time, diarrhoea, thrombocytopenia; increased serum cholesterol, triglycerides, alkaline phosphatase, transaminases, and bilirubin levels. Ear and labyrinth disorders: Tinnitus. Eye disorders: Conjunctival haemorrhage. Gastrointestinal disorders: Dyspepsia, flatulence, nausea, vomiting, gastrointestinal pain. General disorders and administration site conditions: Weakness, pain. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Dizziness, headache, peripheral neuropathy. Rarely, intracranial haemorrhage. Renal and urinary disorders: Haematuria. Respiratory, thoracic and mediastinal disorders: Bronchiolitis obliterans-organising pneumonia, epistaxis. Skin and subcutaneous tissue disorders: Ecchymosis, pruritus, rash, urticaria, exfoliative dermatitis. Rarely, Stevens-Johnson syndrome. Potentially Fatal: Agranulocytosis, aplastic anaemia, neutropenia, pancytopenia, thrombotic thrombocytopenic purpura. Rarely, fulminant hepatitis, hepatic necrosis.
Obtain CBC with differential (including platelet count) at baseline prior to and every 2 weeks for the 1st 3 months; at least 2 weeks after stopping the therapy (if discontinued during the 1st 3 months). Monitor for signs of bleeding. Perform LFT (alkaline phosphatase, transaminases) for the 1st 4 months if liver dysfunction is suspected.
Increased risk of bleeding with anticoagulants, other antiplatelet agents (e.g. aspirin), thrombolytic agents, SSRIs, pentoxifylline, NSAIDs. Increased serum concentration of carbamazepine, phenytoin, theophylline, ketamine. Decreased serum concentration with antacids. Reduced clearance with cimetidine. Decreased serum concentration of digoxin and ciclosporin. May increase the plasma half-life of CYP450 substrates (e.g. phenazone).
May increase bioavailability with food.
Description: Ticlopidine, a thienopyridine antiplatelet agent, undergoes metabolism into unknown active metabolite which irreversibly antagonises the P2Y12 component of adenosine diphosphate (ADP) receptors by interfering with the binding of fibrinogen to the platelet membrane, which blocks the activation of GPIIb/IIIa receptor complex. This results in reduced platelet adhesion and platelet-platelet interactions. Onset: Approx 6 hours. Pharmacokinetics: Absorption: Readily and almost completely absorbed from the gastrointestinal tract. Food may increase the bioavailability by approx 20%. Time to peak plasma concentration: Approx 2 hours. Distribution: Plasma protein binding: Approx 98%, mainly to albumin and lipoproteins; ≤15%, to α1-acid glycoprotein. Metabolism: Extensively metabolised in the liver into at least 1 active metabolite. Excretion: Via urine (approx 60% as metabolites); faeces (23%, with low amounts as unchanged drug). Elimination half-life: Approx 13 hours.
B01AC05 - ticlopidine ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
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