ticlopidine

Action and Spectrum

Actions and Spectrum:

ticlopidine is an anti-platelet drug that works by inhibiting the formation of blood clots. It belongs to a class of drugs called thienopyridines. The drug is used to reduce the risk of stroke or recurrent stroke in patients with cerebrovascular disease. ticlopidine is thought to work by inhibiting the activity of adenosine diphosphate (ADP), which is a substance involved in the process of blood clotting. By blocking ADP, ticlopidine helps to reduce the formation of clots that can cause strokes or other serious cardiovascular events.

Drug Interaction

Adverse Reaction

Frequency Defined 

1-10% 

Dyspepsia (7%)

Nausea (7%)

Rash (5%)

Elevated alkaline phosphatase (7.6%)

Elevated AST/SGOT (3.1%)

GI pain (3.7%)

Neutropenia (2.4%)

Vomiting (1.9%)

Purpura (2.2%)

Flatulence (1.5%)

Dizziness (1%)

Pruritus (1.3%)

>10% 

Diarrhea (12.5%)

Black Box Warning

Black Box Warning

The black box warning of ticlopidine states that the drug can cause serious and sometimes fatal blood disorders, including neutropenia, thrombotic thrombocytopenic purpura (TTP), and agranulocytosis.

Contraindication / Caution

Contraindication/Caution:

ticlopidine is contraindicated in individuals with a history of hypersensitivity reactions to the drug, such as severe skin reactions or blood disorders. It is also not recommended for use in patients with active peptic ulcer disease or severe liver or kidney dysfunction.

caution should be exercised in patients with a history of bleeding disorders, as ticlopidine can increase the risk of bleeding. Other potential side effects of the drug include nausea, diarrhea, and headache. It is important to inform the doctor of any medical conditions and medications being taken before starting ticlopidine treatment.

Pregnancy / Lactation

Pregnancy warnings:   

US FDA pregnancy category: B

Lactation:  

Excreted into human milk is unknown

Pregnancy Categories:        

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

ticlopidine is a medication that belongs to the class of drugs known as antiplatelet agents. It works by preventing the formation of blood clots by inhibiting platelet aggregation.

Pharmacodynamics: 

Mechanism of action: Ticlopidine works by inhibiting the activity of adenosine diphosphate (ADP), which is a substance that triggers platelet aggregation. By blocking the action of ADP, ticlopidine decreases the ability of platelets to stick together, reducing the risk of blood clots forming.

Pharmacokinetics:  

Absorption 

ticlopidine is absorbed from the gastrointestinal tract with an oral bioavailability of about 80%.

Distribution 

ticlopidine is distributed in the body and has a volume of distribution of approximately 200 L.

Metabolism 

ticlopidine is metabolized in the liver primarily by the cytochrome P450 enzyme system.

Elimination and Excretion 

ticlopidine is eliminated primarily in the urine as both unchanged drug and metabolites. The elimination half-life of ticlopidine is approximately 12 hours.

Adminstartion

Administration: 

Oral administration

ticlopidine is typically administered orally, in the form of a tablet, twice daily with or without food. The recommended starting dose is 250 mg twice daily, but this may vary depending on the patient’s condition and response to the medication. It is important to follow the dosing instructions provided by your healthcare provider and not to alter the dose without their approval.

Patient Information Leaflet

Patient information leaflet

Generic Name: ticlopidine

Why do we use ticlopidine?

ticlopidine is used to prevent blood clots and stroke in people who have already had a stroke or mini-stroke due to a blood clot. It works by preventing platelets in the blood from clumping together and forming clots, which can block blood flow to the brain and cause a stroke.

It may also be used to prevent blood clots in people with certain heart conditions, such as atrial fibrillation, and in those undergoing certain medical procedures