Abciximab
- CAS Number: 143653-53-6
Abciximab (also c7E3 Fab ) is a Fab fragment of a monoclonal antibody that binds to an inhibitory Glykoprotein-IIb/IIIa-Rezeptoren on the surface of platelets and as the drug is used. As an inhibitor of platelet aggregation, abciximab is used to prevent ischemic complications during operations on the heart and heart attack for short-term prophylaxis in patients with unstable angina pectoris. Abciximab was developed by the pharmaceutical company Centocor and is offered in cooperation with Eli Lilly under the trade name ReoPro ®.
- 2.1 pharmacodynamics ( mechanism of action )
- 2.2 pharmacokinetics
Clinical information
Indications ( application areas)
Abciximab is to prevent ischemic cardiac complications in patients undergoing percutaneous coronary intervention, such as balloon angioplasty, atherectomy and stent implantation undergo, admitted. In addition, a regulatory drug approval for short-term reduction in risk of myocardial infarction in patients with unstable angina who are refractory to standard therapy or for an above-mentioned percutaneous coronary intervention is planned. For these applications abciximab is used in combination with heparin and aspirin. However, a daily dose of aspirin of 300 mg should not be exceeded.
Contraindications (contraindications )
In a known hypersensitivity to abciximab or other murine antibody abciximab may not be applied. Since abciximab production reasons may contain traces of the enzyme papain, abciximab should not be used in patients with a known allergy to papain.
In addition, abciximab is contraindicated in diseases associated with an increased risk of bleeding. Likewise, do not abciximab in patients with brain tumors, not or difficult to control hypertension, hypertensive retinopathy, thrombocytopenia, vasculitis, or severe hepatic impairment are used. In patients with severe renal failure requiring hemodialysis Abciximab is also contraindicated due to lack of data.
When neuraxial anesthesia procedures ( spinal or epidural ) Abciximab should be discontinued 48 hours in advance and be given no earlier than four hours after the procedure.
Pregnancy and lactation
Animal reproduction studies have not been conducted with abciximab. Also, clinical data on the safety during pregnancy and lactation are lacking.
Interactions
The available data on possible interactions between abciximab and other drugs is limited. With simultaneous use of abciximab and thrombolytics the risk of bleeding is increased. However, the risk of bleeding should not be taken concomitantly with warfarin after abciximab and observations in a clinical study to be increased.
Side effects
Among the most significant side effects of abciximab are bleeding. Frequently also step out and thrombocytopenia, hypotension, bradycardia, back pain, nausea, vomiting, chest pain, fever, headache and pain at the puncture site. Rarely mostly alveolar pulmonary hemorrhage and shock lung was cardiac tamponade have been reported.
Pharmacology
Pharmacodynamics ( mechanism of action )
Abciximab binds to the Glycoprotein-GPIIb/IIIa-Rezeptor of platelets, which is primarily responsible for platelet aggregation. Through his connection abciximab blocks the binding sites for fibrinogen, von Willebrand factor, and other adhesion molecules. The blockade is a steric hindrance or an induced conformational change of the protein based. Moreover, Abciximab binds to the vitronectin receptor on epithelial cells and platelets, which is responsible inter alia for the coagulation of platelets and growth processes in the blood vessel wall. The ability to block both the GPIIb / IIIa receptor and the vitronectin receptor, results in a synergistic inhibition of the formation of thrombin.
Pharmacokinetics
Following intravenous administration, the concentration of free abciximab drops in blood plasma rapidly. For the rapid decrease following an at least bi-phasic kinetics substantially rapid binding of abciximab to its receptors on platelets is responsible. The plasma half -lives of both phases are 10 and 30 minutes. In platelet -bound abciximab form at least 15 days detectable. However, the normal platelet function occurs already within about 48 hours.
Trade names
Abciximab is available in Germany, Austria and Switzerland under the name ReoPro in trade.