Tiklid

Ticlide contains the element ticlopidine, which slows down platelet aggregation. Taking into account the size of the portion, the substance leads to the suppression of the above process, the release of certain platelet factors and the prolongation of the bleeding period.

Clinical tests revealed that the severity of the effect of ticlopidine slightly exceeds the effect of aspirin when used for the secondary prevention of thrombotic complications. This benefit can be seen in relation to the negative side effects of ticlopidine. [1]

Indications Tiklid

It is used to prevent the development of thrombotic complications in the arterial region ( myocardial infarction with stroke and death associated with vascular pathology) in persons whose first stroke developed due to atherosclerosis.

It is prescribed to prevent significant ischemic complications, especially of the coronary type, in people with an obliterating form of atherosclerosis (of a chronic nature), when the legs are affected and intermittent claudication is diagnosed.

It is used to prevent recurrent thrombosis in the area of arteriovenous fistulas during prolonged hemodialysis.

Release form

The release of the drug component is made in tablets - 10 pieces inside the cell pack; inside the box - 2 such packs.

Pharmacodynamics

Ticlopidine leads to a blockage of platelet aggregation - by slowing down the ADP-dependent synthesis of fibrinogen and platelet membranes. In addition, the component does not slow down the activity of COX, which distinguishes it from aspirin. Probably, platelet cAMP is not involved in the therapeutic effect of ticlopidine.

The bleeding period in the case of an intra-cuff pressure of 40 mm Hg. Art. (measured using the Eevee method) is more than doubled from the baseline. Prolongation of the bleeding period is less pronounced if it occurs without using a cuff to determine blood pressure values. [2]

In most patients, the term bleeding and other data on platelet function stabilize after 7 days from the moment of drug withdrawal. [3]

The development of the effect of inhibition of platelet aggregation is noted after 2 days from the start of taking ticlopidine 2 times a day. The substance reaches its maximum effect by the 5-8th day of therapy, in the case of the use of 0.25 g of drugs 2 times per day.

In a therapeutic portion, ticlopidine inhibits platelet aggregation associated with ADP (2.5 μmol / l) by 50-70%. Small dosages lead to proportionally weaker suppression of this process.

Pharmacokinetics

When the 1st standard portion of the medication is ingested, rapid and almost complete absorption is noted. The substance reaches the plasma Cmax after 2 hours.

The optimal level of bioavailability of the drug is observed when it is consumed after a meal.

Stable plasma values are observed after 7-10 days of therapy with 2-time use of a portion of 0.25 g per day. The half-life of ticlopidine at stable rates is approximately 30-50 hours. But the inhibition of platelet aggregation is not associated with the plasma level of the drug.

Most of ticlopidine is involved in intrahepatic metabolic processes. When a radioactive substance is ingested, about 50-60% of the radioactivity is recorded inside the urine, and another 23-30% - inside the feces.

Dosing and administration

The drug is taken orally for all indications - in the amount of 2 tablets per day, along with food. The duration of therapy is selected by the attending physician.

• Application for children

There is no information on the use of drugs in pediatrics.

Use Tiklid during pregnancy

At the moment, there is no information to determine the likelihood of developmental abnormalities or the occurrence of the fetotoxic effect of ticlopidine when used in pregnant women. Because of this, Tiklid is not appointed during the specified period.

Ticlopidine is excreted in mother's milk, which is why it is not used for breastfeeding.

Contraindications

The main contraindications:

• diathesis of hemorrhagic type;
• organic damage that causes bleeding: an active stage of a hemorrhagic stroke or an acute ulcer;
• blood diseases that cause prolongation of the bleeding period;
• a history of allergic manifestations associated with ticlopidine;
• a history of hematological disorders (thrombocyto- or leukopenia and agranulocytosis).

Side effects Tiklid

Among the possible side symptoms.

Hematological pathologies.

There are studies in which neutropenia was noted; singly, this violation led to death.

Often, hematological disorders develop during the first 3 months of therapy and generally do not have clinical manifestations. Because of this, hematological parameters must be constantly monitored. When disorders appear, there is usually a decrease in the number of myeloid precursors within the bone marrow.

Other hematological disorders include:

Bone marrow aplasia or pancytopenia;

Isolated thrombocytopenia or combined with hemolytic type anemia;

TTP with hemolytic anemia, thrombocytopenia, renal failure, neurological disorders, and fever.

Hemorrhagic signs.

Complications of the hemorrhagic type with varying severity may occur during the entire period of therapy. They can last about 10 days after stopping treatment and lead to pre- and postoperative bleeding.

Disorders associated with the work of the gastrointestinal tract.

Among them are nausea and diarrhea. Typically, such signs appear at the initial stage of therapy and passing after 7-14 days. But if such disorders are regular and severe, therapy is stopped.

Severe diarrhea, accompanied by colitis (mainly of the lymphocytic form), is occasionally noted.

Rash (urticarial or maculopapular, often accompanied by itching).

The rash usually appears during the first 7 days of therapy. These signs disappear after a few days from the date of stopping treatment. The rash may be generalized. Erythema polyformis is noted singly.

Allergy symptoms.

Disorders such as Quincke's edema, vasculitis, anaphylactic signs, allergic nephropathies, lupus-like syndrome, fever and allergic pneumopathy develop rarely.

Hepatic dysfunction.

Occasionally, there is a cholestatic or cytolytic form of hepatitis (during the first months of therapy). After stopping the intake of Tiklid, the course of the pathology has a positive prognosis. But occasionally there were also deaths.

Biological (non-hematological) disorders.

Hepatic disorders.

An isolated or associated increase in the values of transaminases, alkaline phosphatase and bilirubin during the first 4 months of therapy.

Blood lipids.

Indicators of cholesterol-HDL, cholesterol-LDL, as well as serum triglycerides and cholesterol-VLDL can increase by 8-10% over a period of 1-4 months of therapy without further progression with the continuation of the course. The levels of the ratio of lipoprotein fractions (especially HDL / LDL) do not change.

Overdose

Information from animal testing indicates that severe gastrointestinal hypersensitivity can occur with Tiklid poisoning.

If necessary, careful monitoring of the basic data of hemostasis and the state of the body is performed. In case of intoxication, vomiting must be induced. Symptomatic actions are performed.

Interactions with other drugs

Certain drugs are able to interact with medication in accordance with their antiplatelet activity. Among them: NSAIDs, tirofiban and aspirin with eptifibatide abciximab, as well as iloprost and clopidogrel.

The combination of several substances that slow down platelet aggregation and the use of drugs together with oral anticoagulants, heparin and thrombolytics can significantly increase the likelihood of bleeding, which is why constant biological and clinical monitoring of the patient's condition is performed.

Aminophylline and theophylline (salts and base).

There may be an increase in plasma theophylline values, there is a likelihood of poisoning (a decrease in plasma theophylline clearance). The patient should be clinically monitored and the plasma values of theophylline noted. If necessary, the dose of theophylline is changed during the use of ticlopidine and at the end of therapy with Tiklid.

Phosphenytoin with Phenytoin.

There may be an increase in the plasma index of phenytoin with manifestations of intoxication (inhibition of the metabolic processes of phenytoin). It is required to clinically monitor the patient's condition and the plasma level of phenytoin.

Cyclosporine.

There is a decrease in the blood level of cyclosporine. An increase in the dosage of cyclosporine and monitoring of its blood values is required. After stopping the use of ticlopidine, the dosage can be reduced.

Storage conditions

The tiklid must be kept out of the reach of children. Temperature values - maximum 25 ° С.

Shelf life

Tiklid can be used within a 36-month term from the date of manufacture of the therapeutic substance.

Analogs

Analogues of drugs are drugs Vasotik and Aklotin with Ticlopidine, as well as Ipaton.