Ticlopidine Hydrochloride
Name: Ticlopidine Hydrochloride
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- Ticlopidine Hydrochloride mg
- Ticlopidine Hydrochloride dosage
- Ticlopidine Hydrochloride drug
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- Ticlopidine Hydrochloride tablet
Ticlopidine Hydrochloride Dosage and Administration
General
Prevention of Coronary Artery Stent Thrombosis
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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 Oral250 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 OralManufacturer 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
Tablets15–30°C1 or 20–25°C.71
Actions
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A thienopyridine-derivative P2Y12-receptor antagonist structurally and pharmacologically related to clopidogrel.1 2 52 71 82
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Time- and dose-dependent inhibition of platelet aggregation and release of platelet granule constituents; also prolongs bleeding time.1 71
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Inhibits ADP-induced platelet-fibrinogen binding and subsequent platelet-platelet interactions.1 71
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Platelet effects irreversible for the life of the platelet.1 71