2010/06/05

Abciximab

International name:
Abtsiksimab (Abciximab)

Group Affiliation:
Antiplatelet tool

Description of the active substance (INN):
Abtsiksimab

Dosage form:
intravenous

Mode of action:
Antiplatelet tool, is also fibrinolytic action. Connect to glycoprotein receptors (GP IIb / IIIa) platelet, inhibits their aggregation and subsequent formation of thrombus. It prevents the binding of fibrinogen, von Willebrand factor with receptor sites on activated platelets. Calling the conformational changes of receptors, reduces access to large molecules. Platelet function recovers within 48 h; in / bolus 0.15-0.3 mg / kg dose-dependent manner inhibits platelet function and increase bleeding time. After 2 h after a dose of 0.25-0.3 mg / kg blocks more than 80% receptor GP IIb / IIIa, with the bleeding time increased to 30 min. V / a bolus 0.25-0.3 mg / kg followed by continuous in / infusion at 10 micrograms / min for 12-96 h is stable blockade expressed GP IIb / IIIa receptors and inhibition of platelet function throughout the infusion. After graduating in / infusion partial blockade of GP IIb / IIIa retained for 10 days.

Indications:
Prevention of myocardial ischemia in patients with high-risk groups, which planned percutaneous coronary balloon angioplasty, stent implantation or atherectomy (consisting of combined therapy on the background of heparin and ASA). The state of the coronary arteries after angioplasty or atherectomy to prevent acute cardiac ischemic complications in patients with high risk of reocclusion of the operated vessel (the presence of intracoronary thrombus, extent of damage> 20 mm). A tendency to thrombosis, including acute myocardial infarction with Q Wave for 12 hours after it began, postinfarction angina. Unstable angina (patients with no effect on conventional therapy), if coronary angioplasty is planned within the next 24 hours

Contraindications:
Hypersensitivity; aneurysm of large vessels, malformations of the arteries, veins, internal bleeding, recent (within 6 weeks), clinically significant bleeding in the gastrointestinal tract or urinary system; ischemic attacks (in the history of the past 2 years), the residual effects of the cerebral circulation with neurological deficit, bleeding diathesis, hypertension (hypertensive crises within), intracranial neoplasm, extensive surgery or trauma (including recent - up to 6 weeks), thrombocytopenia (less than 100 thousand / ml), vasculitis, lactation, children vozrast.C caution. Diseases of the digestive tract (in history), receiving oral anticoagulants within the past 7 days with a decrease in prothrombin time 1.2 times more compared to baseline; in / dextran before the introduction of coronary angioplasty, pregnancy, body weight less than 75 kg, age over 65 years, percutaneous coronary intervention (not A successful, lasting more than 70 minutes, within 12 hours after the development of acute myocardial infarction).

Side effects:
From the side of hematopoiesis and hemostasis system: bleeding (in place of arterial access in the groin, gastrointestinal tract, urinary tract, retroperitoneal, intracranial), thrombocytopenia, anemia, leukopenia, petechiae. On the part of the SSA: lowering blood pressure, bradycardia, pulmonary edema, AV block III Art., supraventricular tachycardia, ventricular tachycardia, "intermittent" claudication, pericardial effusion, peripheral vascular thromboembolism, pulmonary embolism. On the part of the digestive system: nausea, vomiting, constipation, or diarrhea paralytic ileus. the nervous system: confusion, dizziness, insomnia, cerebral ischemia, hyperesthesia. On the part of the urinary system: kidney failure (worsening or development), urinary retention. Allergic reactions: itching, anaphylactic shock. Other: myopathy, myalgia, phlegmon, dysphonia, impairment, pleural effusion, pneumonia, leykotsitoz.Peredozirovka. Symptoms: profuse bleeding, vascular collapse, and thrombocytopenia. Treatment: removal of the drug, platelet transfusion.

Dosage and administration:
V / a bolus, 0.25 mg / kg for 10-60 min before coronary angioplasty (the duration of bolus injections - not less than 1 min) followed by continuous i / v infusion at 10 micrograms / min for 12 h (with a pump for continuous infusion with a built in sterile, apyrogenic weakly binding proteins by a filter with pores of 0.2 or 0.22 microns). Unstable angina in a similar bolus dose (followed by infusion for 12 h) starting 24 hours before planned angioplasty. The rules of preparation and administration solution for injection: for the introduction of a bolus recruit the required number abtsiksimaba (2 mg / ml) into a syringe through a sterile, pyrogen-free, low protein binding filter with pores of 0.2 or 0.22 microns for the preparation of infusion solution required for continuous infusion of abtsiksimaba injected into a sterile 0.9% NaCl solution or 5% dextrose. The prepared infusion solution can store up to 12 h at 2-8 grad.S. At the end of 12 h infusion of the unused portion of the solution destroyed.

Cautions:
Must be used only by doctors with sufficient diagnostic and therapeutic possibilities, and only in patients with high risk of acute coronary. Abtsiksimab should enter through a separate infusion system. During pregnancy and lactation are used only if the intended benefits to the mother outweigh the risks to the fetus and child. The risk of bleeding increased in patients weighing less than 75 kg, in patients older than 65 years, coronary angioplasty, which was conducted during 12 weeks after the onset of symptoms of acute myocardial infarction, coronary angioplasty during long (over 70 min), an unsuccessful coronary angioplasty. Before the introduction of the drug should be the definition of platelets, prothrombin time, APTT. Determination of Hb and hematocrit, and ECG done before the introduction, after 12 h and 24 h after a bolus injection. Blood pressure and heart rate monitor every hour during the first 4 h after bolus injection and then at 6, 12, 18, 24 h after it. In case of serious bleeding, which did not stop clamping, injection should be discontinued. Increases the likelihood of bleeding at the site of arterial access sheath femoral artery. For vascular access punktired only the front wall of an artery or vein. Using the method of cross-cutting approaches to determine the vascular structure is not recommended. Should be avoided without the need to puncture the arteries, veins, i / m injections, urinary catheterization, nazotrahealnoy intubation, the introduction of nasogastric tube, overlap cuff for automatic blood pressure measurement. Upon receipt of venous access should be avoided incompressible sites (subclavian or jugular vein). Vascular puncture site should be recorded and kept under observation. When removing the bandages to be especially cautious. In order to prevent spontaneous bleeding from the gastrointestinal tract - the appointment of H2-blockers, histamine receptors or liquid antacids, vomiting - antiemetic drugs.

Interaction:
Anticoagulants, thrombolytics, antiplatelet drugs (ASA, ticlopidine, dipyridamole, low molecular weight dextran) increases the risk of bleeding. The introduction of other monoclonal antibodies increases the risk of allergic reactions.