Ticlopidine

Ticlopidine Uses, Dosage, Side Effects, Food Interaction and all others data.

When taken orally, Ticlopidine hydrochloride causes a time- and dose-dependent inhibition of both platelet aggregation and release of platelet granule constituents, as well as a prolongation of bleeding time. The intact drug has no significant in vitro activity at the concentrations attained in vivo; and, although analysis of urine and plasma indicates at least 20 metabolites, no metabolite which accounts for the activity of ticlopidine has been isolated.

Ticlopidine hydrochloride, after oral ingestion, interferes with platelet membrane function by inhibiting ADP-induced platelet-fibrinogen binding and subsequent platelet-platelet interactions. The effect on platelet function is irreversible for the life of the platelet, as shown both by persistent inhibition of fibrinogen binding after washing platelets ex vivo and by inhibition of platelet aggregation after resuspension of platelets in buffered medium.

Ticlopidine is a prodrug that is metabolised to an as yet undetermined metabolite that acts as a platelet aggregation inhibitor. Inhibition of platelet aggregation causes a prolongation of bleeding time. In its prodrug form, ticlopidine has no significant in vitro activity at the concentrations attained in vivo.

Trade Name Ticlopidine
Availability Prescription only
Generic Ticlopidine
Ticlopidine Other Names Ticlopidina, Ticlopidine, Ticlopidinum
Related Drugs Ticlid
Type Oral
Formula C14H14ClNS
Weight Average: 263.786
Monoisotopic: 263.05354785
Protein binding

Binds reversibly (98%) to plasma proteins, mainly to serum albumin and lipoproteins. The binding to albumin and lipoproteins is nonsaturable over a wide concentration range. Ticlopidine also binds to alpha-1 acid glycoprotein (about 15% or less).

Groups Approved
Therapeutic Class Anti-platelet drugs, Fibrinolytics (Thrombolytics)
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Ticlopidine
Ticlopidine

Uses

Ticlopidine is used to reduce the risk of thrombotic stroke (fatal or nonfatal) in patients who have experienced stroke precursors, and in patients who have had a completed thrombotic stroke. Because Ticlopidine is associated with a risk of life-threatening blood dyscrasias including thrombotic thrombocytopenic purpura (TTP), neutropenia/ agranulocytosis and aplastic anemia. Ticlopidine should be reserved for patients who are intolerant or allergic to aspirin therapy or who have failed aspirin therapy.

Ticlopidine is also used as an adjunctive therapy with aspirin to reduce the incidence of subacute stent thrombosis in patients undergoing successful coronary stent implantation

Ticlopidine is also used to associated treatment for these conditions: Stent Thrombosis, Stroke

How Ticlopidine works

The active metabolite of ticlopidine prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of ticlopidine.

Dosage

Ticlopidine dosage

Stroke:The recommended dose of Ticlopidine is 250 mg bid taken with food. Other doses have not been studied in controlled trials for these indications.

Coronary Artery Stenting:The recommended dose of Ticlopidine is 250 mg bid taken with food together with antiplatelet doses of aspirin for up to 30 days of therapy following successful stent implantation.

Side Effects

Diarrhoea, nausea, dyspepsia, bleeding, pupura, skin rash, increase in serum cholesterol concentration, elevation of LFTs, hepatitis, cholestatic jaundice.

Toxicity

Single oral doses of ticlopidine at 1600 mg/kg and 500 mg/kg were lethal to rats and mice, respectively. Symptoms of acute toxicity were GI hemorrhage, convulsions, hypothermia, dyspnea, loss of equilibrium and abnormal gait. The FDA label includes a black-box warning of neutropenia, aplastic anemia, thrombotic thrombocytopenia purpura, and agranulocytosis, so it is necessary to monitor patients' WBC and platelets when they are taking ticlopidine.

Precaution

Patients with increased risk of bleeding from trauma, surgery or pathological disorder. Moderate to severe renal impairment. May need to stop therapy 10-14 days before elective surgery. Full blood counts should be performed prior to therapy and every 2 wk during the first 3 mth of treatment. Pregnancy.

Interaction

Reduced clearance with cimetidine; corticosteroid may antagonise effects on bleeding time. Avoid concurrent use with clopidogrel.

Food Interaction

  • Take with a high fat meal. High fat meals will increase ticlopidine absorption.
  • Take with food. Food can help ticlopidine-induced stomach upset.

[Moderate] ADJUST DOSING INTERVAL: The bioavailability and gastrointestinal tolerance of ticlopidine is enhanced by food.br> br> MANAGEMENT: Patients may be advised to take ticlopidine with meals.

Ticlopidine Cholesterol interaction

[Moderate] Ticlopidine can induce increases in serum cholesterol and triglycerides.

Serum total cholesterol levels have increased 8% to 10% in some patients within 1 month of initiation of ticlopidine therapy and have persisted at those levels.

Clinical monitoring of lipid profiles is recommended during ticlopidine therapy in patients at risk for hyperlipidemia-associated adverse events.

Volume of Distribution

The volume of distribution was not quantified.

Elimination Route

Absorption is greater than 80%. Food increases absorption by approximately 20%.

Half Life

Half-life following a single 250-mg dose is approximately 7.9 hours in subjects 20 to 43 years of age and 12.6 hours in subjects 65 to 76 years of age. With repeated dosing (250 mg twice a day), half-life is about 4 days in subjects 20 to 43 years of age and about 5 days in subjects 65 to 76 years of age.

Clearance

Ticlopidine clearance was not quantified, but clearance decreases with age.

Elimination Route

Ticlopidine is eliminated mostly in the urine (60%) and somewhat in the feces (23%).

Pregnancy & Breastfeeding use

Pregnancy Category B. Teratology studies have been conducted in mice (doses up to 200 mg/kg/day), rats (doses up to 400 mg/kg/day) and rabbits (doses up to 200 mg/kg/day). Doses of 400 mg/kg in rats, 200 mg/kg/day in mice and 100 mg/kg in rabbits produced maternal toxicity, as well as fetal toxicity, but there was no evidence of a teratogenic potential of ticlopidine. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of a human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers: Studies in rats have shown ticlopidine is excreted in the milk. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from ticlopidine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

The use of Ticlopidine is contraindicated in the following conditions:

  • Hypersensitivity to the drug
  • Presence of hematopoietic disorders such as neutropenia and thrombocytopenia or a past history of either TTP or aplastic anemia
  • Presence of a hemostatic disorder or active pathological bleeding (such as bleeding peptic ulcer or intracranial bleeding)
  • Patients with severe liver impairment

Special Warning

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: Clearance of ticlopidine is somewhat lower in elderly patients and trough levels are increased. The major clinical trials with Ticlopidine in stroke patients were conducted in an elderly population with an average age of 64 years. Of the total number of patients in the therapeutic trials, 45% of patients were over 65 years old and 12% were over 75 years old. No overall differences in effectiveness or safety were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Renal Impairment: Dose reduction or discontinuance if haemorrhagic or haematopoietic complications occur.

Hepatic Impairment: Severe: contraindicated.

Acute Overdose

One case of deliberate overdosage with Ticlopidine has been reported by a foreign postmarketing surveillance program. A 38-year-old male took a single 6000-mg dose of Ticlopidine (equivalent to 24 standard 250-mg tablets). The only abnormalities reported were increased bleeding time and increased SGPT. No special therapy was instituted and the patient recovered without sequelae.

Single oral doses of ticlopidine at 1600 mg/kg and 500 mg/kg were lethal to rats and mice, respectively. Symptoms of acute toxicity were GI hemorrhage, convulsions, hypothermia, dyspnea, loss of equilibrium and abnormal gait.

Storage Condition

Store at 15° to 30° C

Innovators Monograph

You find simplified version here Ticlopidine

Ticlopidine contains Ticlopidine see full prescribing information from innovator Ticlopidine Monograph, Ticlopidine MSDS, Ticlopidine FDA label

FAQ

What is Ticlopidine used for?

Ticlopidine is used to reduce the risk of stroke in people who have had a stroke or have had warning signs of a stroke and who cannot be treated with aspirin.

What are side effects of Ticlopidine?

Common side effects of Ticlopidine include:

  • diarrhea,
  • stomach upset or pain,
  • nausea,
  • vomiting,
  • dizziness,
  • ringing in your ears, or.
  • itching.

What should be avoided when taking Ticlopidine?

You should not take Ticlopidine if you have any active bleeding such as a stomach ulcer or bleeding in the brain such as from a head injury, or a blood cell disorder such as anemia lack of red blood cells or low levels of platelets.

Is Ticlopidine safe during pregnancy?

There are no controlled data in human pregnancy. Ticlopidine should be given during pregnancy only when benefit outweighs the risk.

Is Ticlopidine safe during breastfeeding?

Due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Is Ticlopidine a blood thinner?

Ticlopidine is an oral drug that inhibits the ability of platelets to clump and form blood clots.

Is Ticlopidine an antiplatelet?

Ticlopidine is a new antiplatelet agent with a distinct mechanism of action.

What is the recommended of Ticlopidine?

The recommended Ticlopidine of  is 250 mg bid taken with food. Other doses have not been studied in controlled trials for these indications.

What foods interact with Ticlopidine?

The oral bioavailability of Ticlopidine is increased by 20% when taken after a meal. Administration of Ticlopidine with food is recommended to maximize gastrointestinal tolerance. In controlled trials in stroke patients, Ticlopidine was taken with meals.

When should I take Ticlopidine?

Take this medication by mouth with food or just after a meal as directed by your doctor, usually twice daily.

How to use Ticlopidine?

Take this medication with food or just after a meal, usually twice daily, or as directed by your doctor. Do not take this medication two hours before or after taking antacids.Duration of therapy is based on your medical condition.

Can I drive after taking Ticlopidine?

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely.

What happen If I missed Ticlopidine?

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Does Ticlopidine causes allergic reactions?

if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems.

Does Ticlopidine affect my liver?

liver or kidney problems, bleeding/blood clotting disorders, conditions that put you at risk of bleeding, high cholesterol or triglyceride levels.

*** Taking medicines without doctor's advice can cause long-term problems.
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