Ticlopidine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Anticoagulants

Included in the formulation

Tiklid®

pills inwards

Sanofi-Aventis France France

АТХ:

B.01.A. C.05 Ticlopidine

Pharmacodynamics:

The thienopyridine derivative inhibits platelet aggregation caused by ADP. Due to the formation of an active metabolite, irreversibly and selectively disturbs the interaction of ADP with receptors in the platelet membrane. Eliminates the stimulating effect of ADP on platelets and reduces the concentration of cytoplasmic Ca in them²⁺. As a result, binding to fibrinogen of platelets is broken without changing the conformation of glycoproteins Hb/ Sha in their membranes.

Pharmacokinetics:

After ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 2 hours. The connection with plasma proteins is 98%.

The therapeutic effect develops 24-48 hours after the beginning of the admission. Metabolism in the liver.

The elimination half-life is 24 hours. Elimination by the kidneys in the form of metabolites.

Indications:

It is used for the prevention of thrombosis in ischemic disorders caused by atherosclerotic changes in cerebral vessels and lower extremities, unstable angina, in the rehabilitation period after a previous myocardial infarction and subarachnoid hemorrhage, after shunting vessels, blood transfusions,when using artificial circulation, angiopathy in diabetes mellitus.

ICD-10

IX.I70-I79.I70 Atherosclerosis

IX.I60-I69.I67.2 Cerebral atherosclerosis

IX.I60-I69.I60.90 Subarachnoid haemorrhage, unspecified with hypertension

Contraindications:

Bleeding, severe hepatic insufficiency, individual intolerance.

Carefully:

Blood clotting disorders, hyperuricemia.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside for 250-500 mg.

The highest daily dose: 500 mg.

The highest single dose: 1 g.

Side effects:

Central and peripheral nervous system: headache, intracranial hemorrhage, confusion, paresthesia.

Respiratory system: shortness of breath, hemoptysis, nosebleed.

Digestive system: gingival, gastrointestinal, hemorrhoidal hemorrhages, diarrhea, constipation.

Musculoskeletal system: rarely - hemarthrosis.

Dermatological reactions: subcutaneous and dermal hemorrhages, bruising, itching.

Organs of the senses: conjunctival, intraocular, retinal hemorrhages, vertigo.

Reproductive system: metrorrhagia.

Urinary system: hematuria.

Local reactions: necrosis or bruising at the injection site.

Allergic reactions.

Overdose:

Bleeding.

Treatment is symptomatic.

Interaction:

The risk of bleeding increases with simultaneous use with salicylates, indirect coagulants, glucocorticoids, nonsteroidal anti-inflammatory drugs, antiaggregants.

Simultaneous use with CYP3A4 inhibitors (nefazodone, ketoconazole, clarithromycin, atazanavir and ritonavir) leads to an increase in exposure to ticagrelyl.

Simultaneous application with inductors CYP3A4 (dexamethasone, rifampicin, phenytoin, carbamazepine and phenobarbital) decreases the effectiveness of ticagrelyl.

Special instructions:

Monitoring the amount of peripheral blood platelets.

It is recommended to cancel the drug 7 days before the scheduled operation.

Instructions

Ticlopidine (Ticlopidinum)