Ticklid

Ticlid contains the element ticlopidine, which slows down platelet aggregation. Given the portion size, the substance leads to suppression of the above process, release of individual platelet factors and prolongation of bleeding time.

Clinical trials have shown that the effect of ticlopidine is somewhat greater than that of aspirin when used for secondary prevention of thrombotic complications. This advantage can be considered in relation to the negative effects of ticlopidine. [ 1 ]

Indications Ticklid

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

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

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

Release form

The medicinal component is released in tablets - 10 pieces in a cell pack; there are 2 such packs in a box.

Pharmacodynamics

Ticlopidine blocks 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 (measured using the Ivy method) increases more than twice as compared to the initial level. The 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 bleeding time and other platelet function data 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 5th-8th day of therapy, in the case of taking 0.25 g of the drug 2 times a day.

In a therapeutic dose, ticlopidine inhibits ADP-associated (2.5 μmol/l) platelet aggregation by 50-70%. Small doses result in proportionally weaker suppression of this process.

Pharmacokinetics

When ingesting the 1st standard dose of the drug, rapid and almost complete absorption is observed. The substance reaches plasma Cmax values after 2 hours.

The optimal level of bioavailability of the drug is observed when it is taken after meals.

Stable plasma values are observed after 7-10 days of therapy with 2-time administration of a 0.25 g dose per day. The half-life of ticlopidine at stable values is approximately 30-50 hours. However, inhibition of platelet aggregation is not associated with plasma drug levels.

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

Dosing and administration

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

• Application for children

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

Use Ticklid during pregnancy

There is currently no information to determine the likelihood of developmental abnormalities or fetotoxic effects of ticlopidine when used in pregnant women. For this reason, Ticlid is not prescribed during this period.

Ticlopidine is excreted in breast milk, which is why it is not used during breastfeeding.

Contraindications

Main contraindications:

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

Side effects Ticklid

Among the possible side effects.

Hematological pathologies.

There are studies in which neutropenia was noted; in isolated cases, this disorder led to death.

Often, hematological disorders develop during the first 3 months of therapy and generally have no clinical manifestations. Because of this, it is necessary to constantly monitor hematological parameters. When disorders appear, a decrease in the number of myeloid precursors in the bone marrow is usually noted.

Other hematological disorders include:

Bone marrow aplasia or pancytopenia;

Isolated thrombocytopenia or combined with hemolytic anemia;

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

Hemorrhagic signs.

Hemorrhagic complications of varying severity may be observed throughout the entire period of therapy. They may last for approximately 10 days after the end of treatment and lead to pre- and postoperative bleeding.

Disorders associated with the gastrointestinal tract.

Among them are nausea and diarrhea. Usually such symptoms appear at the initial stage of therapy and pass after 7-14 days. But if such disorders are regular and have a strong expression, therapy is stopped.

Severe diarrhea accompanied by colitis (mainly lymphocytic form) is observed occasionally.

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

Usually, the rash appears during the first 7 days of therapy. These signs disappear after a few days from the moment of stopping the treatment. The rash may be generalized. Erythema multiforme is observed sporadically.

Allergy symptoms.

Rarely, disorders such as Quincke's edema, vasculitis, anaphylactic symptoms, allergic nephropathy, lupus-like syndrome, fever and allergic pneumopathy develop.

Liver dysfunction.

Rarely, cholestatic or cytolytic form of hepatitis is observed (during the first months of therapy). After stopping taking Ticlid, the course of the pathology has a positive prognosis. But occasionally there were fatal cases.

Biological (non-hematological) disorders.

Liver disorders.

Isolated or associated increase in transaminase, alkaline phosphatase and bilirubin levels during the first 4 months of therapy.

Blood lipids.

HDL-cholesterol, LDL-cholesterol, and serum triglycerides and VLDL-cholesterol may increase by 8-10% over a period of 1-4 months of therapy without subsequent progression with continuation of the course. Levels of the ratio of lipoprotein fractions (especially HDL/LDL) do not change.

Overdose

Information from animal studies indicates that severe gastrointestinal hypersensitivity may occur in cases of Ticlid poisoning.

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

Interactions with other drugs

Certain drugs may interact with the medication based on their antiplatelet activity. These include 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).

An increase in plasma theophylline values may be observed, there is a possibility of poisoning (decreased plasma clearance of theophylline). The patient should be clinically monitored and plasma theophylline values should be noted. If necessary, the dose of theophylline is changed during the use of ticlopidine and after completion of therapy with Ticlid.

Fosphenytoin with phenytoin.

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

Cyclosporine.

There is a decrease in the blood level of cyclosporine. It is necessary to increase the dosage of cyclosporine and monitor its blood values. After stopping the use of ticlopidine, the dosage can be reduced.

Storage conditions

Ticlid should be stored in a place inaccessible to children. Temperature values - maximum 25°C.

Shelf life

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

Analogues

Analogues of the drug are the drugs Vazotik and Aklotin with Ticlopidine, as well as Ipaton.