Ticlopidine

• 5 - (2 -chlorobenzyl ) - 4,5,6,7- tetrahydro thieno [3,2 -c] pyridine
• Latin: Ticlopidinum

• 55142-85-3
• 53885-35-1 (hydrochloride)

B01AC05

Antiplatelet

117-120 ° C ( 66.5 Pa)

Hydrochloride

Attention

1780 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Ticlopidine is a drug from the group of blood coagulation inhibitors ( platelet aggregation inhibitors).

Substance class

ADP inhibitor from the group of thienopyridine derivatives (see clopidogrel )

Operation

Thienopyridine derivatives bind irreversibly to the P2 receptor of platelets. This is the increase in activity of activated platelets and platelet activation is still inactive by ADP, which is released by activated platelets themselves inhibited. ADP- blocking effect, an indirect inhibition of the glycoprotein IIb / IIIa complex (see, GPIIb / IIIa antagonist is tirofiban ), which is responsible for the binding of fibrinogen, and therefore a reduction in the cross-linking of platelet thrombi on an intracellular mechanism. Emerging thrombi are under treatment with ticlopidine ( as clopidogrel ) is smaller and structurally looser, so that they can be easily dissolved and washed away by the blood stream. Observed thrombi under treatment were too small to lead to vascular occlusion can.

Ticlopidine and clopidogrel differ in their molecular structure, only one page group, ticlopidine can be understood as a precursor of clopidogrel, however, that significantly more deployments today.

Indication

Ticlopidine can be used for anticoagulation after myocardial infarction, with known CHD, after balloon dilation or stenting. Due to the availability of modern agents (eg clopidogrel, prasugrel, ticagrelor ) with a lower risk of side effects, the substance, however, lost much of its importance.

Side effects and limitations of use

Uncommon: blood dyscrasias (neutropenia, agranulocytosis ), dizziness, headache, weakness, loss of appetite, nausea, tinnitus, palpitations, insomnia, depressed mood

Rare: thrombocytopenia, pancytopenia, medullary aplasia, leukopenia (BB- control, bleeding tendency, susceptibility to infections! ) Diarrhea, nausea, allergic reactions, allergic vasculitis, lupus erythematosus, liver dysfunction, increases in cholesterol and triglycerides by about 10 %.

When neuraxial anesthesia procedures ( spinal or epidural ), ticlopidine should be discontinued ten days before, but may be given shortly after surgery.

Interactions

Concentration reduction in blood by antacids increase by cimetidine. Reduction of digoxin concomitantly with ticlopidine by 20-30%. Ticlopidine is metabolized by the cytochrome P450 system, thus influencing the half-lives of all those drugs that are metabolized by the same system (eg, sedatives, hypnotics, theophylline, phenytoin ).

Contraindications

Children, pregnancy and lactation, known blood dyscrasias, hemorrhagic diathesis, acute GI bleeding.

Trade names

Thrombodine (A), Tiklid (A), Tiklyd (D ), various generics (D)