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Abciximab (previously known as c7E3 Fab), 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.^[1]

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.(Tanguay, J.F., Eur Heart J 1999; 1 (suppl E): E27-E35 Abciximab is made from the Fab fragments of an immunoglobulin that targets the glycoprotein IIb/IIIa receptor on the platelet membrane.^[2]

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^[3] and a decreased need for repeated coronary artery revascularization in the first month following the procedure.^[4] Research also shows that this drug can be of use for patients with diabetes and chronic renal insufficiency. 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.

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 renal dose adjustment.

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 is usually rapid occurring hours after administration but may occur up to 16 days later.^[5] 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 150,000-400,000, can effectively drop to zero.

References

^ "Abciximab". Drugs.com. Archived from the original on 20 April 2010. Retrieved 13 March 2010.
^ "International Nonproprietary Names for Pharmaceutiical Substances" (PDF). WHO Drug Information 7 (4). 1993.
^ "Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. The EPIC Investigation.". The New England Journal of Medicine 330 (14): 956–61. 1994. doi:10.1056/NEJM199404073301402. PMID 8121459.
^ Tcheng, J. E.; Kandzari, D. E.; Grines, C. L.; Cox, D. A.; Effron, M. B.; Garcia, E.; Griffin, J. J.; Guagliumi, G.; Stuckey, T.; Turco, M.; Fahy, M.; Lansky, A. J.; Mehran, R.; Stone, G. W.; Cadillac, I. (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): 1316–1323. doi:10.1161/01.CIR.0000087601.45803.86. PMID 12939213.
^ Profound delayed thrombocytopenia presenting 16 days after Abciximab (Reopro®) administration. Platelets. 2011;22(4):302-4. doi: 10.3109/09537104.2010.518324.

External links

Official website

UpToDate Contents

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1. 冠動脈疾患における血小板糖蛋白（GP）IIb/IIIa受容体拮抗薬に関する
初期臨床試験 early trials of platelet glycoprotein iib iiia receptor inhibitors in coronary heart disease
2. ST上昇型心筋梗塞における抗血小板剤 antiplatelet agents in acute st elevation myocardial infarction
3. 非ST上昇型急性冠症候群における抗血小板薬 antiplatelet agents in acute non st elevation acute coronary syndromes
4. 糖蛋白IIb / IIIa阻害剤による血小板減少症 thrombocytopenia induced by glycoprotein iib iiia inhibitors
5. 冠動脈ステント植え込みのための抗血栓療法：臨床試験 antithrombotic therapy for intracoronary stent implantation clinical trials

English Journal

Impact of abciximab on prognosis in diabetic patients undergoing primary percutaneous coronary intervention.

Perkan A, Vitrella G, Barbati G, De Monte A, D'Agata B, Merlo M, Giannini F, Grazia ED, Rakar S, Salvi A, Igidbashian D, Morgera T, Zalukar W, Sinagra G.SourceaStruttura Complessa di Cardiologia, Azienda Ospedaliero-Universitaria Ospedali Riuniti di Trieste, Trieste bIstituto di Sanità Pubblica e Microbiologia, Università degli Studi di Torino, Torino cTerza Divisione di Medicina, Azienda Ospedaliero-Universitaria Ospedali Riuniti di Trieste dStruttura Complessa di Pronto Soccorso - Azienda Ospedaliero-Universitaria Ospedali Riuniti di Trieste, Trieste eStruttura Complessa di Cardiologia, Ospedale di Gorizia, Gorizia fStruttura Complessa di Cardiologia, Ospedale di Monfalcone, Monfalcone, Italy.
Journal of cardiovascular medicine (Hagerstown, Md.).J Cardiovasc Med (Hagerstown).2013 Feb;14(2):127-135.
BACKGROUND: The impact of diabetes in patients with acute myocardial infarction (AMI) treated with primary percutaneous coronary intervention (PCI) is unclear. The benefit of abciximab in this subset of patients remains controversial.METHODS AND RESULTS: Three hundred and twenty-seven consecutive an
PMID 22343257

Synergistic effect of thrombus aspiration and abciximab in primary percutaneous coronary intervention.

Pyxaras SA, Mangiacapra F, Verhamme K, Serafino LD, De Vroey F, Toth G, Perkan A, Salvi A, Bartunek J, De Bruyne B, Wijns W, Sinagra G, Barbato E.SourceCardiovascular Center Aalst, OLV Clinic, Aalst, Belgium; Cardiovascular Department, University Hospital of Trieste, Trieste, Italy.
Catheterization and cardiovascular interventions : official journal of the Society for Cardiac Angiography & Interventions.Catheter Cardiovasc Interv.2013 Jan 29. doi: 10.1002/ccd.24837. [Epub ahead of print]
BACKGROUND.: Previous studies failed to assess the individual prognostic role of thrombus aspiration (TA) or abciximab in primary percutaneous coronary intervention (pPCI), due their prevalent combined use. METHODS AND RESULTS.: A total of 644 consecutive STEMI patients treated with pPCI were includ
PMID 23359568

Efficacy and safety of early versus late glycoprotein IIb/IIIa inhibitors for PCI.

Xu Q, Yin J, Si LY.SourceDepartment of Geriatrics, Southwest Hospital, The Third Military Medical University, Chongqing 400038, China.
International journal of cardiology.Int J Cardiol.2013 Jan 20;162(3):210-9. doi: 10.1016/j.ijcard.2012.06.001. Epub 2012 Jul 4.
BACKGROUND: Glycoprotein (Gp) IIb/IIIa inhibitors are beneficial for patients with ST-segment elevation myocardial infarction (STEMI) undergoing percutaneous coronary intervention (PCI). However, optimal drug timing remains inconclusive. Therefore, this study was to perform a meta-analysis of the cl
PMID 22769575

Japanese Journal

The Long-term Clinical Results of Platelet Glycoprotein IIb/IIIa Receptor Blocker (Abciximab : ReoPro) Coated Stent in Patients with Acute Myocardial Infarction(Acute Myocardial Infarction, Clinical (Diagnosis/Treatment) 7 (IHD), The 69th Annual Scientific Meeting of the Japanese Circulation Society)

Kim Weon,Jeong Myung Ho,Hong Young Joon,Kim Ju Han,Ahn Young Keun,Cho Jeong Gwan,Park Jong Chun,Cho Dong Lyun,Kim Hoon,Kang Jung Chaee
Circulation journal : official journal of the Japanese Circulation Society 69(Supplemnt_I), 239, 2005-03-01
NAID 110004052454

Effect of Combined Intracoronary Adenosine and Nicorandil on No-Reflow Phenomenon During Percutaneous Coronary Intervention

Lim Sang Yup,Bae Eun Hui,Jeong Myung Ho,Kang Dong Goo,Lee Yeon Sang,Kim Kye Hun,Lee Sang Hyun,Yoon Kyung Ho,Hong Seo Na,Park Hyung Wook,Hong Young Joon,Kim Ju Han,Kim Weon,Ahn Young Keun,Cho Jeong Gwan,Park Jong Chun,Kang Jung Chaee
Circulation journal : official journal of the Japanese Circulation Society 68(10), 928-932, 2004-09-20
… Incidence of thrombosis or dissection after balloon angioplasty, diameter and length of stent, and use of Reopro^[○!R] during PCI were not significantly different. …
NAID 110002692138

Abciximab readministration results of the ReoPro Readministration Registry

TCHENG JE
Circulation 104, 870-875, 2001
NAID 30029738693

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リンク元

「アブシキシマブ」

Abciximab
Monoclonal antibody
Type	Fab fragment
Source	Chimeric (mouse/human)
Target	CD41 7E3
Clinical data
Trade names	Reopro
AHFS/Drugs.com	monograph
Pregnancy; category	C (US);
Legal status	UK: POM (Prescription only);
Routes of; administration	IV
Pharmacokinetic data
Biological half-life	<10 min–30 min
Identifiers
CAS Number	143653-53-6
ATC code	B01AC13
DrugBank	DB00054
UNII	X85G7936GV
KEGG	D02778
ChEMBL	CHEMBL1201584
Chemical data
Formula	C2101H3229N551O673S15
Molecular mass	47455.4 g/mol
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英: abciximab
商: レオプロ ReoPro

血小板凝集抑制薬
GpIIb/IIIa受容体をブロックする。

参考

uptodate

. [charged] アブシキシマブ：医薬品情報 - uptodate [1]
. [charged] アブシキシマブ：患者向け医薬品情報 - uptodate [2]
. [charged] 冠動脈疾患における血小板糖蛋白IIb/IIIa受容体阻害剤に関する臨床試験：静脈内投与剤 - uptodate [3]
. [charged] 糖蛋白IIb / IIIa阻害剤による血小板減少症 - uptodate [4]

[1] "Abciximab". Drugs.com. Archived from the original on 20 April 2010. Retrieved 13 March 2010.

[INN-2] "International Nonproprietary Names for Pharmaceutiical Substances" (PDF). WHO Drug Information 7 (4). 1993.

[3] "Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty. The EPIC Investigation.". The New England Journal of Medicine 330 (14): 956–61. 1994. doi:10.1056/NEJM199404073301402. PMID 8121459.

[4] Tcheng, J. E.; Kandzari, D. E.; Grines, C. L.; Cox, D. A.; Effron, M. B.; Garcia, E.; Griffin, J. J.; Guagliumi, G.; Stuckey, T.; Turco, M.; Fahy, M.; Lansky, A. J.; Mehran, R.; Stone, G. W.; Cadillac, I. (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): 1316–1323. doi:10.1161/01.CIR.0000087601.45803.86. PMID 12939213.

[5] Profound delayed thrombocytopenia presenting 16 days after Abciximab (Reopro®) administration. Platelets. 2011;22(4):302-4. doi: 10.3109/09537104.2010.518324.

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