Included in the formulation
АТХ:B.01.A.C Inhibitors of platelet aggregation (excluding heparin)
B.01.A.C.16 Eptifibatid
Pharmacodynamics:Synthetic blocker of glycoprotein IIb/ IIIa receptors of platelet membranes, which leads to prevention of binding to fibrinogen receptors, von Willebrand factor and other adhesive ligands and reversible inhibition of platelet aggregation. Inhibition of platelet aggregation is reversible; 4 hours after stopping the infusion, the function of platelets is restored by more than 50%. Has no significant effect on prothrombin time, activated partial thromboplastin time.
Pharmacokinetics:In the bolus doses of 90-250 mkg / kg and infusion at a rate of 0.5-3.0 μg / kg per minute pharmacokinetics is linear and dose-dependent. When administered according to the recommended scheme (bolus, then infusion) maximum concentration is reached after 5 minutes, then the concentration slightly decreases and reaches an equilibrium level within 4-6 h. Binding to plasma proteins - about 25%. Half-life from the plasma - 2,5 h, ground clearance - 55-58 ml / kg / h, volume of distribution - 185-260 ml / kg. Metabolism occurs in the liver. In healthy people, the kidney clearance is 50% of the total clearance.It is excreted mainly with urine in unchanged form and in the form of metabolites.
Indications:Acute coronary syndrome (unstable angina, myocardial infarction), prevention of thrombotic occlusion of the affected artery and acute ischemic complications in percutaneous transluminal coronary angioplasty, including intracoronary stenting.
IX.I20-I25.I20.0 Unstable angina
IX.I20-I25.I22 Repeated myocardial infarction
IX.I20-I25.I21 Acute myocardial infarction
XXI.Z80-Z99.Z95.5 Presence of coronary angioplasty implant and graft
Contraindications:Hypersensitivity, haemorrhagic diathesis in history or severe bleeding in the previous 30 days, hemorrhagic stroke in the previous 30 days, severe arterial hypertension (systolic blood pressure above 200 mmHg or diastolic blood pressure above 110 mmHg) with antihypertensive therapy, extensive surgical interventions for the previous 6 weeks, simultaneous or planned use of another inhibitor IIb/IIIa-receptor platelets for parenteral administration, the need for hemodialysis in connection with renal failure, the period of breastfeeding, the age of 18 years.
Carefully:Blood clotting disorders, hyperuricemia.
Pregnancy and lactation:Recommendations for FDA - Category B. It is used in pregnancy in cases where the expected effect exceeds the risk to the fetus. Contraindicated during lactation.
Dosing and Administration:Intravenous bolus 180 μg / kg, then as a continuous infusion of 2 μg / kg per minute no more than 72 hours. The highest daily dose: 360 μg / kg.
Apply, as a rule, together with acetylsalicylic acid and heparin.
Side effects:The system of hematopoiesis: thrombocytopenia
The cardiovascular system: macrogemaria, hematemesis, gastrointestinal and pulmonary hemorrhages, hemorrhages in the brain.
Bleeding is more often observed with simultaneous application with heparin; more often - small bleeding (including macrohematuria), less often - large bleeding, extremely rarely - intracranial hemorrhage. In isolated cases - fatal bleeding. Thrombocytopenia is possible (the number of platelets is less than 100,000 in 1 μl or a decrease in their number by 50% or more from the baseline level).
Allergic reactions.
Overdose:Symptoms: bleeding.
Treatment: symptomatic, effective hemodialysis.
Interaction:Pharmaceutically incompatible with furosemide (can not be administered in the same system).
The risk of bleeding increases with simultaneous use with streptokinase.
Special instructions:The application is possible only in a hospital. All patients should be carefully screened to identify possible bleeding, especially patients with an increased risk of bleeding: women, elderly people, patients with low body weight. Required mmonitoring the amount of peripheral blood platelets, the level of hemoglobin and hematocrit within 6 hours after the initiation of therapy and then 1 time per day throughout the therapy (in the case of a decrease in indicators - more often).
It is recommended to cancel the drug 7 days before the scheduled operation.