Index of drugs

Treatment to prevent myocardial infarction in patients with unstable coronary disease or myocardial infarction with no Q wave, with an episode of chest pain in the last 12 hours with ECG abnormalities and / or increased infarction index enzyme activity. The preparation is indicated in patients who are particularly prone to myocardial infarction within 3-4 days of the onset of symptoms of acute coronary heart disease, including those who are likely to undergo early PTCA.

1 ml of concentrate contains 250 μg of tirofiban in the form of a monohydrate hydrochloride.

Non-peptide antagonist of GP IIb / IIIa receptors - important surface platelet receptors involved in the aggregation process. Prevents fibrinogen from binding to GP IIb / IIIa receptors, blocking platelet aggregation and prolonging bleeding time. Platelet function returns to normal within 8 hours after discontinuation of the drug. The degree of inhibition of platelet function correlates with the plasma concentration of the drug. Tirofiban does not bind strongly to plasma proteins, and this binding does not depend on the drug concentration in the range of 0.01-25 μg / ml. The fraction not bound in plasma is 35%. It is metabolized to a small extent and excreted mainly in the urine and faeces. T_0,5 is about 1.5 hours.

Hypersensitivity to any of the ingredients. Thrombocytopenia after prior use of GP IIb / IIIa receptor antagonists. Do not use in patients with: stroke in the last 30 days or a history of hemorrhagic stroke; history of intracranial pathological process (eg cancerous growth, vascular anomalies, aneurysm); active or recent (up to 30 days) clinically significant bleeding; malignant hypertension; significant injury or major surgery in the last 6 weeks; thrombocytopenia (platelet count <100,000 / mm³), impaired platelet function; coagulation disorders; severe liver failure. The use of the preparation is not recommended without unfractionated Heparin (safety and efficacy in combination with small molecule heparins have not been studied). The use of the preparation is not recommended in the following cases: traumatic or prolonged cardiopulmonary resuscitation, organ biopsy or lithotripsy in the last 2 weeks; major surgery or severe trauma in the period of over 6 weeks, but less than 3 months; active peptic ulcer in the last 3 months; uncontrolled hypertension (> 180/110 mmHg); acute pericarditis; vasculitis (active or history); suspected aortic dissection; hemorrhagic retinopathy; the presence of latent blood in the stool or hematuria; thrombolytic therapy (up to date or started within 48 hours for drug administration); concomitant use of drugs that significantly increase the risk of bleeding (eg coumarin derivatives, other GP IIb / IIIa inhibitors used parenterally, dextran solutions). Use with particular caution in: recent, clinically significant bleeding (in the last year); severe, acute or chronic heart failure; cardiogenic shock; mild or moderate impairment of liver function; in the case of a puncture that can not be compressed within 24 hours before administration of the preparation; in the case of platelet counts <150,000 / mm³, coagulopathy or a history of thrombocytopenia or thrombocytopenia; hemoglobin below 11 g / dL or hematocrit <34%. Use cautiously in elderly patients, women, people with small age, and patients with impaired renal function. During pregnancy and breastfeeding, use only in cases of extreme necessity. There are no clinical data on the use of the preparation in children. There is insufficient data on the re-use of the preparation.

The most common is bleeding, usually referred to as mild. In addition, there are: nausea (1.7%), fever (1.5%), headache (1.1%).Changes in the results of laboratory tests concern bleeding: reduction of hemoglobin, hematocrit reduction, increased incidence of blood in urine and stool. Occasionally there are: sudden decrease in the number of platelets (reversible after discontinuation) or thrombocytopenia.

Intravenously in a loading infusion at an initial rate of 0.4 μg / kg / min for 30 min. The infusion should be continued at a maintenance dose of 0.1 μg / kg / min after the end of the infusion. The preparation should be administered with unfractionated heparin (usually as an intravenous bolus of 5,000 IU, administered simultaneously with the initiation of treatment with the preparation followed by a dose of approximately 1000 IU / hour based on APTT - which should be approximately doubled) and with Acetylsalicylic acid, if there are no contraindications to its use. No dose adjustment is required in the elderly. In patients with severe renal impairment (creatinine clearance below 30 ml / min), the dosage should be reduced by approximately 50%. It is best to start the treatment within 12 hours of the last angina pain, the recommended duration of treatment is at least 48 hours. The intravenous infusion of the formulation and unfractionated heparin can be continued during coronary angiography and should be maintained for at least 12 to a maximum of 24 hours after performing angioplasty or atherectomy. The total duration of treatment with the product should not exceed 108 hours. The preparation concentrate must be diluted with 0.9% NaCl solution or 5% Glucose solution before use.