Eptifiʙatid
When ATH:
B01AC16
Pharmacological action.
Antiplatelet agent, a synthetic cyclic heptapeptide, comprising 6 amino acids and merkaptopropionilovy balance - dezaminotsisteinil. Inhibitor platelet aggregation, belonging to the class of RGD (arginine-glycine-aspartate)-stimulants: inhibits platelet aggregation, preventing the binding of fibrinogen, von Willebrand factor and other adhesive ligands to the glycoprotein IIb / IIIa platelet receptors. When on / in causing inhibition of platelet aggregation, the extent of which depends on the dose and drug concentration. Inhibition of platelet aggregation is reversible; through 4 hours after cessation of infusion platelet function recovers more than 50%. It does not have a noticeable effect on prothrombin time, and APTT.
Pharmacokinetics
Pharmacokinetics эptifibatida imeet lineynыy and dozozavisimыy character in struynom vvedenii in doze of 90 to 250 mg / kg and the infusion at a rate of 0.5 to 3 ug / kg / min. With the introduction of the drug on the recommended scheme (bole, zatem infusion) its plasma concentration quickly reaches the peak, then decreases slightly and comes to equilibrium within 4-6 no. Coronary angioplasty this decrease can be avoided by administration of the second dose bolus 180 mg / kg 10 minutes after the first. Plasma protein binding – 25%.
T1/2 is 2.5 no, clearance – 55-58 ml / kg / h, and Vd – 185-260 ml / kg. In healthy people, the share of total renal clearance is 50%; most of the excreted by the kidneys in an unchanged form and in the form of metabolites. In human plasma major metabolites are not found.
Testimony
Acute coronary syndrome (incl. unstable angina, acute myocardial infarction); prevention of thrombotic occlusion of the affected artery and acute ischemic complications of percutaneous transluminal coronary angioplasty (PTCA), including intracoronary stenting.
Dosage regimen
Used in conjunction with acetylsalicylic acid and heparin. Enter in / bolus and infusion. The dose depends on the indication, clinical situation, regimens, body weight.
Side effect
From the blood coagulation system: minor bleeding (incl. makrogematuriâ) often observed with the simultaneous use of heparin; less often – major bleeding; rarely – intracranial hemorrhage; in a few cases – fatal bleeding.
From the hematopoietic system: thrombocytopenia (the number of platelets<100 000 cells /, or reduce their number by 50% or more from baseline).
Contraindications
History of bleeding diathesis or severe abnormal bleeding in the past 30 days, severe hypertension (systolic blood pressure>200 mmHg. or diastolic blood pressure>110 mmHg.) against the background of antihypertensive therapy, extensive surgery during the previous 6 Sun., ischemic stroke in the previous 30 days or hemorrhagic stroke in history, simultaneous or planned use of another inhibitor IIb / IIIa receptor inhibitors for parenteral administration, the need for hemodialysis in renal failure due to, patients, which is required for clinical administration of thrombolytics (in acute transmural myocardial infarction with new pathological Q wave, ST-segment elevation or left bundle branch block on the ECG), lactation (breast-feeding), childhood and adolescence up 18 years, Hypersensitivity to eptifibaditu.
Pregnancy and lactation
When pregnancy is used with caution and only in those cases, when the expected therapeutic benefit outweighs the potential risk to the fetus.
Do not use this eptifibatide lactation (breast-feeding).
Cautions
Eptifibatide is intended for use only in a hospital. Before treatment, all patients must be carefully examined to identify potential bleeding, especially women, elderly patients, and patients with low body weight, as having the highest risk of bleeding complications. The risk of bleeding is greatest at the site of arterial access in patients, undergoing PTCA. It is necessary to closely monitor the possible bleeding sites (incl. place for catheterization); It should also be alert to possible bleeding from the gastrointestinal tract and urinary tract, retroperitoneal bleeding.
Caution must be exercised with concomitant use of other drugs, affecting hemostasis, including thrombolytics, antykoahulyantы, dextran, adenosine phosphate, NSAIDs, sulfinpirazon, antiagregantы.
If during treatment there is a need for emergency surgery, administration of the drug should be stopped immediately. Before the planned surgery administration of the drug was stopped early, to platelet function was restored to normal.
During the period of treatment is necessary to limit the number of arterial and venous punctures, to exclude the / m injection, as well as the use of urinary catheters, endotracheal tubes and nasogastric tubes. For I / O access, do not use a vein, not subject to compression (subclavian, jugular). In the event of serious bleeding, which can not be stopped by applying a pressure bandage, It should be stopped immediately, and administration of the drug heparin. The risk of bleeding is greatest at the site of the catheter into the femoral artery during PTCA. Use caution and make sure, Only that punctured the front wall of the femoral artery. System for the introduction of the femoral artery can be removed after the restore function to normal coagulation: APTT – less 45 sec, that usually occurs 3-4 hours after discontinuation of heparin. After removal system for injection should be carried out, followed by thorough hemostasis observation for at least 2-4 hours before discharge from the hospital.
By reducing the number of platelets less 100 000/l, introduction of eptifibatide and heparin should be discontinued and carry out the necessary remedial measures. If a history of thrombocytopenia have been cases when other parenteral glycoprotein IIb / IIIa receptor inhibitors, it should be particularly careful observation. There may be a reversible 5-fold increase in bleeding time. The bleeding time returns to the initial indicators for 2-6 h after cessation of eptifibatide.
Not recommended for use in conjunction with a low molecular weight heparin in the absence of clinical experience. The use of heparin is recommended in all cases (in the absence of contraindications to its use).
Before initiation of therapy to identify possible violations of hemostasis determination of prothrombin time is recommended, APTT, serum creatinine, platelet count, Hemoglobin, gematokrita. Latest 3 indicator should be continuously monitored for 6 hours after the start of therapy, then 1 time / day. throughout therapy (or more – in the case of decrease). When thrombocytopenia below 100 000 l should be retested to eliminate pseudothrombocytopenia; heparin should be discontinued.
Drug Interactions
In an application with streptokinase increased risk of bleeding.
