Abciximab
| Abciximab | ||
|---|---|---|
| Mass / length primary structure | 47.6 kDa | |
| Identifier | ||
| External IDs |
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| Drug information | ||
| ATC code | B01 AC13 | |
| DrugBank | BTD00041 | |
| Drug class | Antiplatelet drugs | |
Abciximab (also C7E3-Fab ) is a Fab fragment of a monoclonal antibody that inhibitively binds to the glycoprotein IIb / IIIa receptors on the surface of blood platelets and was used as a drug . As a platelet aggregation inhibitor , abciximab was used to prevent ischemic complications during heart surgery and for short-term heart attack prophylaxis in patients with unstable angina pectoris . Abciximab was developed by the pharmaceutical company Centocor and was approved under the trade name ReoPro ; it was distributed in cooperation with Eli Lilly and Jannsen-Cilag. After delivery bottlenecks from 2017 onwards, Janssen stopped selling the drug worldwide in December 2018.
Clinical information
application areas
Abciximab was approved for the prevention of ischemic cardiac complications in patients undergoing percutaneous coronary interventions such as balloon dilatation , atherectomy, and stenting . In addition, there was a drug approval for short-term risk reduction of a heart attack in patients with unstable angina pectoris who do not respond to standard therapy and for whom the above-mentioned percutaneous coronary intervention is intended. For these areas of application, abciximab was used in combination with heparin and acetylsalicylic acid . However, the daily dose of acetylsalicylic acid should not fall below 300 mg.
Contraindications and restrictions on use
Abciximab must not be used if there is a known hypersensitivity to abciximab or other mouse antibodies. Since abciximab may contain traces of the enzyme papain due to its manufacturing process , abciximab must not be used in patients with a known papain allergy . In addition, abciximab is contraindicated in diseases with an increased risk of bleeding. Abciximab must also not be used in patients with brain tumors , arterial hypertension that is difficult or impossible to control , hypertensive retinopathy, thrombocytopenia, vasculitis, or severe hepatic impairment. In patients with severe renal impairment requiring dialysis, abciximab is also contraindicated due to lack of data.
In the case of regional anesthesia procedures close to the spinal cord ( spinal anesthesia or epidural anesthesia ), the administration of abciximab must be discontinued 48 hours in advance and resumed no earlier than four hours after the procedure.
Animal reproduction studies with abciximab have not been performed. There is also a lack of clinical data on safety during pregnancy and breastfeeding.
Alternations and side effects
The data on possible interactions between abciximab and other drugs are limited. If abciximab and thrombolytic drugs are used at the same time , the risk of bleeding is increased. However, according to observations in a clinical study, the risk of bleeding should not be increased when abciximab and warfarin are taken at the same time .
One of the most significant side effects of abciximab is bleeding. Often beyond also were thrombocytopenia , hypotension , bradycardia , back pain, nausea , vomiting , chest pain, fever , headache and pain at the puncture site on. Pericardial tamponade , mostly alveolar pulmonary hemorrhage and shock lung have been reported rarely .
pharmacology
Pharmacodynamics (mechanism of action)
Abciximab binds to the glycoprotein GPIIb / IIIa receptor of platelets, which is mainly responsible for platelet aggregation. Through its binding, abciximab blocks the binding sites for fibrinogen , Von Willebrand factor and other adhesion molecules. The blockage is based on steric hindrance or an induced conformational change of the protein. Abciximab also binds to the vitronectin receptor of platelets and epithelial cells , which is partly responsible 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 leads to a synergistic inhibition of the formation of thrombin .
Pharmacokinetics
After intravenous administration, the concentration of free abciximab in the blood plasma falls rapidly. A rapid binding of abciximab to its receptors on platelets is essentially held responsible for the rapid decline, which follows at least biphasic kinetics. The plasma half-lives for both phases are 10 and 30 minutes. Abciximab is detectable in platelet-bound form for at least 15 days. However, platelet function returns to normal within about 48 hours.
See also
Monoclonal Antibody Nomenclature : Convention for naming antibodies
Web links
Individual evidence
- ↑ a b FDA label ReoPro August 2019.
- ↑ Jannsen-Cilag GmbH: Information letter: Voluntary discontinuation of sales of ReoPro® (Abciximab) in Germany on December 15, 2018. December 12, 2018, accessed September 19, 2019 .
- ↑ a b c d e f g Specialist information ReoPro. Centocor BV as of July 2007.
- ↑ Gogarten, Wiebke; Van Aken, Hugo K .: Perioperative thrombosis prophylaxis - platelet aggregation inhibitors - importance for anesthesia. AINS - Anaesthesiology · Intensive Care · Emergency Medicine · Pain Therapy, Edition 04, April 2012, pp. 242-254 doi : 10.1055 / s-002-23167 .
- ↑ SA Kozek-Langenecker, D. Fries, M. Gütl, N. Hofmann, P. Innerhofer, W. Kneifl, L. Neuner, P. Perger, T. Pernerstorfer, G. Pfanner, et al .: Locoregional anesthesia under anticoagulant medication. Recommendations of the Perioperative Coagulation Working Group (AGPG) of the Austrian Society for Anaesthesiology and Intensive Care Medicine (ÖGARI). DER ANESTHESIST Volume 54, Number 5 (2005), 476–484, doi : 10.1007 / s00101-005-0827-0 .
