Abciximab

Abciximab, a glycoprotein IIb/IIIa receptor antagonist manufactured by Janssen Biologics BV and distributed by Eli Lilly under the trade name ReoPro, is a platelet aggregation inhibitor mainly used during and after coronary artery procedures like angioplasty to prevent platelets from sticking together and causing thrombus (blood clot) formation within the coronary artery. It is a glycoprotein IIb/IIIa inhibitor.[3]

Abciximab
Monoclonal antibody
TypeFab fragment
SourceChimeric (mouse/human)
TargetCD41 7E3
Clinical data
Trade namesReopro
Other namesAbcixifiban,[1] c7E3 Fab
AHFS/Drugs.comMonograph
License data
Routes of
administration		Intravenous (IV)
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC2101H3229N551O673S15
Molar mass47456.03 g·mol−1
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While abciximab has a short plasma half-life, due to its strong affinity for its receptor on the platelets, it may occupy some receptors for weeks. In practice, platelet aggregation gradually returns to normal about 96 to 120 hours after discontinuation of the drug. Abciximab is made from the Fab fragments of an immunoglobulin that targets the glycoprotein IIb/IIIa receptor on the platelet membrane.[4]

Indications for use

Abciximab is indicated for use in individuals undergoing percutaneous coronary intervention (angioplasty with or without stent placement). The use of abciximab in this setting is associated with a decreased incidence of ischemic complications due to the procedure[5] and a decreased need for repeated coronary artery revascularization in the first month following the procedure.[6]

Research also shows that this drug can be of use for patients with diabetes and chronic kidney disease. It is not the appropriate drug of choice if a patient is scheduled for an emergency surgery (i.e., heart surgery) because bleeding time may take about 12 hours to normalize. Pediatric uses include treatment of Kawasaki disease.

Pharmacokinetics

Abciximab has a plasma half-life of about ten minutes, with a second phase half-life of about 30 minutes. However, its effects on platelet function can be seen for up to 48 hours after the infusion has been terminated, and low levels of glycoprotein IIb/IIIa receptor blockade are present for up to 15 days after the infusion is terminated. Abciximab does not require dose adjustments for patients with kidney failure.[7]

Side-effects

Many of the side effects of abciximab are due to its anti-platelet effects which increase the risk of bleeding. The most common type of bleeding due to abciximab is gastrointestinal hemorrhage.

Thrombocytopenia is a rare but known serious risk characterized by a severe drop in platelets circulating in the blood. Abciximab induced thrombocytopenia is usually rapid occurring hours after administration but may occur up to 16 days later.[8] Transfusing platelets is the only known treatment for abciximab-induced thrombocytopenia, but this therapy may have limited effectiveness because the drug may bind and inhibit the receptors on the newly transfused platelets.

References
  1. Toronto Notes: Comprehensive medical reference and review for the Medical Council of Canada Qualifying Exam Part I and the United States Medical Licensing Exam Step 2 (32nd ed.). Toronto, Ontario, Canada.: Toronto Notes for Medical Students, Inc. ISBN 978-1-927363-26-3.
  2. "ReoPro Abciximab" (PDF). Janssen Pharmaceutical Companies. U.S. Food and Drug Administration. August 2019.
  3. "Abciximab". Drugs.com. Archived from the original on 20 April 2010. Retrieved 13 March 2010.
  4. "International Nonproprietary Names for Pharmaceutical Substances" (PDF). WHO Drug Information. 7 (4). 1993. Archived from the original (PDF) on June 27, 2004.
  5. EPIC Investigators (April 1994). "Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty". The New England Journal of Medicine. 330 (14): 956–61. doi:10.1056/NEJM199404073301402. PMID 8121459.
  6. Tcheng JE, Kandzari DE, Grines CL, Cox DA, Effron MB, Garcia E, et al. (September 2003). "Benefits and risks of abciximab use in primary angioplasty for acute myocardial infarction: the Controlled Abciximab and Device Investigation to Lower Late Angioplasty Complications (CADILLAC) trial". Circulation. 108 (11): 1316–23. doi:10.1161/01.CIR.0000087601.45803.86. PMID 12939213.
  7. Usta C, Turgut NT, Bedel A (November 2016). "How abciximab might be clinically useful". International Journal of Cardiology. 222: 1074–1078. doi:10.1016/j.ijcard.2016.07.213. PMID 27519521.
  8. Webb GJ, Swinburn JM, Grech H (2011). "Profound delayed thrombocytopenia presenting 16 days after Abciximab (Reopro) administration". Platelets. 22 (4): 302–4. doi:10.3109/09537104.2010.518324. PMID 21526887. S2CID 40372407.
  • "Abciximab". Drug Information Portal. U.S. National Library of Medicine.
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