Ticlopidine Hydrochloride

Name: Ticlopidine Hydrochloride

Ticlopidine Hydrochloride Dosage and Administration

General

Prevention of Coronary Artery Stent Thrombosis

  • Initiate therapy after successful stent implantation.1 46 71

Administration

Oral Administration

Administer orally with food to maximize GI absorption and tolerance.1 2 71

Dosage

Available as ticlopidine hydrochloride; dosage expressed in terms of the salt.1 71

Adults

Prevention of Thrombotic Stroke Oral

250 mg twice daily.1 71 Has been continued for at least up to 5.8 years in some patients.1 2 71

Prevention of Coronary Artery Stent Thrombosis Oral

Manufacturer recommends 250 mg twice daily, beginning after stent implantation and continuing for up to 30 days in conjunction with antiplatelet dosages of aspirin.1 46 71

If ticlopidine is used in combination with aspirin following drug-eluting stent (DES) implantation, combined therapy with ticlopidine and aspirin must be continued for ≥12 months to minimize the risk of potentially catastrophic stent thrombosis.70 (See Compliance with Therapy in Patients with Drug-eluting Stents under Cautions.)

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time;1 71 contraindicated in patients with severe hepatic impairment.1 71 (See Hepatic Impairment under Cautions.)

Renal Impairment

Reduce dosage or discontinue therapy if hemorrhagic or hematopoietic complications occur.1 71

Geriatric Patients

No specific dosage recommendations at this time.1 71

Interactions for Ticlopidine Hydrochloride

Drugs Metabolized by Hepatic Microsomal Enzymes

Possible increased plasma half-life of concomitantly administered drugs metabolized by hepatic microsomal enzymes; dosage adjustments may be required when initiating or discontinuing ticlopidine therapy.1 71

Specific Drugs

Drug

Interaction

Comments

Antacids

Decreased plasma ticlopidine concentrations1 71

Anticoagulants

Additive effects1 71

Manufacturer recommends discontinuing anticoagulant therapy prior to initiating ticlopidine1 71

Aspirin, other NSAIAs

Additive effect on platelet aggregation1 71

Use with caution in patients who have lesions with a propensity to bleed (e.g., peptic ulcers)1 71 (see Conditions Predisposing to Bleeding under Cautions)

Safety of concomitant use of ticlopidine and aspirin beyond 30 days not established;1 46 71 long-term concomitant use not recommended1

Digoxin

Slight decrease in plasma digoxin concentrations1 71

Little or no change in digoxin efficacy expected1 71

Phenobarbital

No inhibition of platelet aggregation effects of ticlopidine1 71

Phenytoin

Increased plasma phenytoin concentrations with associated somnolence and lethargy reported1 71

Cautious use recommended; monitor plasma phenytoin concentrations1 71

Propranolol

Potential for altered protein binding of propranolol1 71

Cautious use recommended1 71

Theophylline

Decreased elimination half-life and total plasma clearance of theophylline1 71

Thrombolytic agents

Additive effects1 71

Manufacturer recommends discontinuing of thrombolytic agents prior to initiating ticlopidine1 71

Ticlopidine Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed (>80%) following oral administration.1 Peak plasma concentrations at 2 hours.1 71

Food

Increases bioavailability by 20%.1 71

Distribution

Plasma Protein Binding

Binds reversibly (98%), mainly to serum albumin and lipoproteins.1 71

Elimination

Metabolism

Extensively metabolized by the liver.1 71

Elimination Route

Excreted in urine (60%) and feces (23%).1 71

Special Populations

Increased plasma concentrations in patients with advanced cirrhosis.1 71 Decreased plasma clearance in patients with mild to moderate renal impairment.1 71

Stability

Storage

Oral

Tablets

15–30°C1 or 20–25°C.71

Actions

  • A thienopyridine-derivative P2Y12-receptor antagonist structurally and pharmacologically related to clopidogrel.1 2 52 71 82

  • Time- and dose-dependent inhibition of platelet aggregation and release of platelet granule constituents; also prolongs bleeding time.1 71

  • Inhibits ADP-induced platelet-fibrinogen binding and subsequent platelet-platelet interactions.1 71

  • Platelet effects irreversible for the life of the platelet.1 71

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