Ticlopidine

What is Ticlopidine?

• Ticlopidine (Ticlid) is a platelet aggregation inhibitor, 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.
• It is also used along with aspirin to prevent blood clots from forming in coronary stents.

Ticlopidine

Ticlopidine ball-and-stick

What are the uses of this medicine?

Ticlopidine (Ticlid) 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.
• as adjunctive therapy with aspirin to reduce the incidence of subacute stent thrombosis in patients undergoing successful coronary stent implantation.

Limitations of use:

• 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.

Other uses:

• Ticlopidine also is used before open heart surgery and in the treatment of sickle cell disease, certain types of kidney disease (primary glomerulonephritis), and blocked arteries in the legs.

How does this medicine work?

• Ticlopidine (tye kloe' pi deen) is an inhibitor of adenosine diphosphate (ADP)-induced platelet aggregation and is used to decrease the risk of recurrence of stroke in patients who have documented previous cerebrovascular thrombosis, and as adjunctive therapy with aspirin to reduce the risk of coronary stent thrombosis.
• Ticlopidine is a thienopyridine and prodrug that requires activation in the liver by the cytochrome P450 system.
• Activated platelets release ADP which binds to purinergic platelet receptors causing platelets to adhere to each other and aggregate.
• Ticlopidine acts by inhibiting the binding of ADP to platelet receptors and triggering of the intracellular pathways that lead to activation of the glycoprotein IIb/IIIa complex, which causes a change in the shape of platelets and their aggregation.
• The aggregation of platelets plays an important role in the growth of atheromatous plaques which can lead to coronary, cerebral and peripheral arterial occlusions. In large clinical trials, ticlopidine therapy has been shown to decrease the frequency of recurrence of fatal and nonfatal stroke.

In Stroke Patients:

• A stroke occurs when a clot (or thrombus) forms in a blood vessel in the brain or forms in another part of the body and breaks off, then travels to the brain (an embolus).
• In both cases the blood supply to part of the brain is blocked and that part of the brain is damaged.
• Ticlopidine hydrochloride tablets work by making the blood less likely to clot, although not so much less that it causes you to become likely to bleed, unless you have a bleeding disorder or some injury (such as a bleeding ulcer of the stomach or intestine) that is especially likely to bleed.

In Stent Patients:

• A heart attack or [[]]angina (chest pain) can occur when fatty deposits block the arteries that carry oxygen and nutrient-rich blood to your heart.
• To decrease the chance of fatty deposits building up over time, your doctor may recommend the placement of a coronary stent.
• Ticlopidine hydrochloride tablets may be given to you with aspirin to make blood clots less likely to form inside the stent so that the artery remains open.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

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

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• antacids, anticoagulants ('blood thinners') such as warfarin (Coumadin), aspirin, cimetidine (Tagamet), clopidogrel (Plavix), digoxin (Lanoxin), and theophylline (Theo-Dur).

• If you also take antacids (Maalox, Mylanta) take them 1 hour before or 2 hours after taking ticlopidine.

Is this medicine FDA approved?

• Ticlopidine was approved for use in the United States in 1991, but it is currently rarely used, largely because of the risks of serious side effects including agranulocytosis, thrombotic thrombocytopenic purpura and aplastic anemia and the availability of clopidogrel, which has a similar mechanism of action and efficacy, but a lower rate of adverse events.

How should this medicine be used?

Recommended dosage: For Stroke:

• The recommended dose of ticlopidine hydrochloride is 250 mg bid taken with food.

For Coronary Artery Stenting:

• The recommended dose of ticlopidine hydrochloride is 250 mg bid taken with food together with antiplatelet doses of aspirin for up to 30 days of therapy following successful stent implantation.

Administration:

• Ticlopidine comes as a tablet to take by mouth.
• It usually is taken twice a day.
• Continue to take ticlopidine even if you feel well.
• Do not stop taking ticlopidine without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As tablet, for oral administration, contains 250 mg of ticlopidine hydrochloride

This medicine is available in fallowing brand namesː

• Ticlid

What side effects can this medication cause?

The most common side effects of this medicine include:

• Diarrhea
• Nausea
• Dyspepsia
• Rash
• GI Pain
• Neutropenia
• Purpura
• Vomiting
• Flatulence
• Pruritus
• Dizziness
• Anorexia
• Abnormal Liver Function Test

Less coomon side effects may include:

• Digestive System: GI fullness
• Skin and Appendages: urticaria
• Nervous System: headache
• Body as a Whole: asthenia, pain
• Hemostatic System: epistaxis
• Special Senses: tinnitus

Relatively serious and potentially fatal events associated with the use of ticlopidine may include:

• Hemolytic anemia with reticulocytosis, immune thrombocytopenia, hepatitis, hepatocellular jaundice, cholestatic jaundice, hepatic necrosis, hepatic failure, peptic ulcer, renal failure, nephrotic syndrome, hyponatremia, vasculitis, sepsis, allergic reactions (including angioedema, allergic pneumonitis, and anaphylaxis), systemic lupus (positive ANA), peripheral neuropathy, serum sickness, arthropathy and myositis.

What special precautions should I follow?

• Patients should be told that a decrease in the number of white blood cells (neutropenia) or platelets (thrombocytopenia) can occur with ticlopidine, especially during the first 3 months of treatment and that neutropenia, if it is severe, can result in an increased risk of infection. They should be told it is critically important to obtain the scheduled blood tests to detect neutropenia or thrombocytopenia.
• Patients should also be reminded to contact their physicians if they experience any indication of infection such as fever, chills, or sore throat, any of which might be a consequence of neutropenia.
• Thrombocytopenia may be part of a syndrome called TTP. Symptoms and signs of TTP, such as fever, weakness, difficulty speaking, seizures, yellowing of skin or eyes, dark or bloody urine, pallor or petechiae (pinpoint hemorrhagic spots on the skin), should be reported immediately.
• All patients should be told that it may take them longer than usual to stop bleeding when they take ticlopidine and that they should report any unusual bleeding to their physician. Patients should tell physicians and dentists that they are taking ticlopidine before any surgery is scheduled and before any new drug is prescribed.
• Patients should be told to promptly report side effects of ticlopidine such as severe or persistent diarrhea, skin rashes or subcutaneous bleeding or any signs of cholestasis, such as yellow skin or sclera, dark urine, or light-colored stools.
• Patients should be told to take ticlopidine with food or just after eating in order to minimize gastrointestinal discomfort.
• Ticlopidine should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery or pathological conditions.
• Ticlopidine prolongs template bleeding time. The drug should be used with caution in patients who have lesions with a propensity to bleed (such as ulcers).
• Ticlopidine therapy causes increased serum cholesterol and triglycerides.
• Rare cases of agranulocytosis, pancytopenia, or leukemia have been reported.
• It is not known whether this drug is excreted in human milk.
• Ticlopidine is associated with a low rate of serum enzyme elevations during treatment and has been linked to rare instances of idiosyncratic, clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Increased bleeding time and increased SGPT
• Symptoms of acute toxicity were GI hemorrhage, convulsions, hypothermia, dyspnea, loss of equilibrium and abnormal gait.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Pregnancy category B.
• 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.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• ticlopidine hydrochloride

Inactive ingredients:

• butylated hydroxyanisole, corn starch, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, povidone, stearic acid, and titanium dioxide.

Who manufactures and distributes this medicine?

Manufactured In Israel By:

• TEVA PHARMACEUTICAL IND. LTD.
• Jerusalem, Israel

Manufactured For:

• TEVA PHARMACEUTICALS USA
• Sellersville, PA

What should I know about storage and disposal of this medication?

• Keep this medication in the container it came in, tightly closed, and out of reach of children.
• Store it at room temperature and away from excess heat and moisture.

• Dailymed label info on Ticlopidine
• FDA Ticlopidine

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