Ticlopidine

Chemical name

5-[2-Хлорфенил)метил]-4,5, 6,7-тетрагидротиено[3,2-c ]пиридин (and as hydrochloride)

Gross

C14-H14-Cl-N-S

Characteristics

White solid crystalline powder. Easily soluble in water, methanol, sparingly soluble in metilenhloride and ethanol, it is difficult soluble in acetone and nerastvorim buffer solutions with pH 6.3.

Of drugs

The drugs-antitromboticescoe, antiagregatine. Ingibiruet fosfolipazu C leads to the formation braking caused adenosinfosfatom, bonding with nine fibrinoguenom and consequently suppresses agregatia platelets. After intake of rapidly absorbed. C_max plasma is two hours; Bioavailability of 80 to 90% (an increase of 10-20% in the admission after eating). The plasma 98% relates to the protein (with albuminom, acid альфа_1-гликопротеино�� and lipoproteidami). Metabolised in the liver with the formation of four metabolites, one of whom has pharmacological activity. T_1/2 after receiving one (250 mg) is about 13 hours, with the regular-4-5 days. Equilibrium concentration in the blood is in 2-3 weeks. Excreted in the urine mainly in the form of metabolites. At 1 / 3 unchanged to be withdrawn from jelchew and faeces. Cl reduced in older patients. Impact agregatia platelets without changing activity gli and fosfodiesterzy. Hindered growth endotelialnah cells. Decreases viscosity of the blood and prolong bleeding time. Patients who are glomerulonefritom proteinuriu decreases and increases Cl creatinine. The effect begins in 24 to 48 hours after administration, reaches maximum at 3-6 day, and continues 4-10 days.

Indications

Acute myocardial infarction (early stages, and the rehabilitation period), the unstable stenocardia, simply think of the circulatory system (secondary prevention stroke), of the prosthetic heart valves, coronary bypass (with venoznam shuntom) and angioplastiki (bladder dilatation), a heavy man peripheral arteries peremejatayasa limp, chronic glomerulonefrit, sickle cell anaemia, mikroangiopatia diabetes.

Restrictions on the use of

Injuries planned surgery (removal of a 2 weeks); Child.

Contraindications

Hypersensitivity, acute pepticalkie stomach ulcers, the risk of bleeding, as the ulcers stomach and duodenal ulcers, intracranial bleeding (including the ill), bloody diates, neutropenia, thrombocytopenia, heavy human liver, acute haemorrhagic stroke, pregnancy, breast-feeding (optional waiver of breastfeeding).

Side-Effects

Gastrointestinal disorders (diarrhea, nausea, vomiting, decrease in appetite, pain in the abdomen, bloating), less frequently, bleeding, hemorrhagic skin, gematuria, thrombocytopenia, neutropenia (in the first 3 months), a heavy agranulozitos, pancitopenia, aplastic anemia (one case), dizziness, headache, uproar in the face, fatigue, increase in cholesterol and triglycerides in the serum, Enhancement transaminaz and alkaline phosphatase (in the first 1-4 months), holetsatical jaundice, rashes, itching of the skin.

Patient interaction

Increases ingibirutee of aspirin, etc. NPVS to kollageninducyruemuyu agregatia platelets and increases the risk of hemorrhage (including in the face of heparin and indirect anti). Antatsida by reducing the intake reduces concentration in plasma by 18%; Zimetidin by blocking mikrosomalnoe oxidation, Cl reduces by 50%. The 15% reduction in the level of digoxin in the blood, theofillina Cl. Increases concentration fenitoina plasma.

Overdosing

Haemorrhagic syndrome, convulsions, hypothermia, dizziness, vestibular violations. The postmarquetingovykh tests described one case of overdose (old man took one six grams without any major complications, an increase in bleeding time and the level of transaminaz).

Precautions

In the treatment desirable control of the cells of peripheral blood and the coagulation system.

Dosing and Administration

Inside, at the time of delivery on the 250 mg twice a day; With a good dose of endurance can be increased to 750 mg / sut. When kidney failure shows lower dosage.

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