ticlopidine (Ticlid)
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Introduction
Tradename: Ticlid.
Indications
- prevention of arterial thrombosis
- thromboembolic stroke (ischemic stroke) prophylaxis (aspirin failure*)
- also has beeb used for:
* No better than aspirin by Beers criteria
Contraindications
- active bleeding disorders
- neutropenia or thrombocytopenia
- severe liver disorder
- hemostatic disorder
Caution:
- gastric or duodenal ulcers
- patients with underlying hematologic disorders
- patients receiving oral anticoagulants
- concurrent use of NSAIDs including aspirin
- liver disease
- patients undergoing lumbar puncture
- patients udergoing surgical procedures: ticlopidine should be discontinued 14 days prior to surgery
Dosage
Tabs: 250 mg.
Pharmacokinetics
- about 80% absorbed from the GI tract
- 98% bound to plasma proteins
- metabolized by the liver
- peak effect after 3-5 days of oral therapy
- trace amounts of drug are found in the urine
- serum levels do NOT correlate with antiplatelet activity
- elimination 1/2life is 4-5 days after repeat dosing
elimination via liver
protein binding = 98 %
1/2life = 4-5 days
Monitor
- complete blood count (CBC) every 2 weeks for 1st 3 months, then every 6 months
- liver function tests every 6 months
Adverse effects
- not common (1-10%)
- rash, neutropenia (3%)
- uncommon (< 1%)
- ecchymosis, diarrhea, nausea/vomiting, GI pain, thrombocytopenia, epistaxis, abnormal liver function tests, tinnitus, hematuria
- other
- neutropenia
- most serious adverse effect
- generally occurs within 3 weeks to 3 months, but may occur later
- monitor CBC every 2 weeks for 1st 3 months
- reversible
- thrombocytopenia:
- fatal thrombotic thrombocytopenic purpura (TTP) (0.02-0.06%)[6] (more common than with clopidogrel)
- discontinue if platelet count drops below 80,000/mm3
- increased cholesterol & triglyceride levels
- neutropenia
Drug interactions
- cimetidine decreases clearance of Ticlid by 50%
- antacids (decreased absorption)
- glucocorticoids decrease effect of ticlopidine
- ticlopidine decreases effect of digoxin & cyclosporine
- ticlopidine increases effects/toxicity of
- drug interaction(s) of anti-platelet agents with SSRIs
- drug interaction(s) of antiplatelet agents with proton pump inhibitors
- drug interaction(s) of warfarin with antiplatelet agents
Test interactions
- increased serum cholesterol
- increased serum alkaline phosphatase
- increased serum transaminases
Mechanism of action
- platelet aggregation inhibitor
- ADP receptor antagonist
- suppresses platelet-derived growth factor (PDGF)
- may block von Willebrand factor
- effects irreversible for life of the platelet
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- ↑ Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 1022
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ 6.0 6.1 Ovbiagele B, In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
- ↑ 7.0 7.1 Deprecated Reference