Abciximab

Abciximab (previously known as c7E3 Fab), manufactured by Centocor 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. Its mechanism of action is inhibition of glycoprotein IIb/IIIa.

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 24 to 48 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.

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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^[1] and a decreased need for repeated coronary artery revascularization in the first month following the procedure.^[2]

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.

Side effects

Many of the side effects of abciximab are due to its anti-platelet effects. This includes an increased risk of bleeding. The most common type of bleeding due to abciximab is gastrointestinal hemorrhage.

Thrombocytopenia is a rare but known serious risk. Abciximab-induced thrombocytopenia can typically be treated with transfusion of platelets. Abciximab induced thrombocytopenia can last for five days after initial drug administration. Transfusing platelets is the only known treatment and may have limited effectiveness as the drug may also bind to the new platelets. Platelet counts which should average 250,000-400,000 can effectively drop to zero^{[citation needed]}. This is not a particularly safe drug^{[citation needed]} and this rare but dangerous side effect is not as easily reversed as one would like.

References

1. ^ Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. The EPIC Investigation. N Engl J Med. 1994 Apr 7;330(14):956-61. PMID 8121459.
2. ^ Tcheng JE, Kandzari DE, Grines CL, Cox DA, Effron MB, Garcia E, Griffin JJ, Guagliumi G, Stuckey T, Turco M, Fahy M, Lansky AJ, Mehran R, Stone GW; CADILLAC Investigators. 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. 2003 Sep 16;108(11):1316-23. Epub 2003 Aug 25. PMID 12939213.