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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. edit
^ 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. 待機的経皮的冠動脈インターベンションのための抗血栓療法：臨床研究 antithrombotic therapy for elective percutaneous coronary intervention clinical studies
5. ST上昇型心筋梗塞に対する血栓溶解後の経皮的冠動脈インターベンション percutaneous coronary intervention after fibrinolysis for acute st elevation myocardial infarction

English Journal

Abciximab as a bridging strategy to overcome morphine-prasugrel interaction in STEMI patients.

Siller-Matula JM1, Specht S1, Kubica J2, Alexopoulos D3, De Caterina R4, Hobl EL5, Jilma B5, Christ G6, Lang IM1.
British journal of clinical pharmacology.Br J Clin Pharmacol.2016 Jul 1. doi: 10.1111/bcp.13053. [Epub ahead of print]
OBJECTIVE: This study investigated whether the GPIIb/IIIa receptor blocker abciximab might be a successful bridging strategy to rapidly achieve sufficient levels of platelet inhibition in cases where prasugrel is used in morphine pre-treated ST-elevation myocardial infarction (STEMI) patients.METHOD
PMID 27366874

A randomized trial assessing the impact of three different glycoprotein IIb/IIIa antagonists on glycoprotein IIb/IIIa platelet receptor inhibition and clinical endpoints in patients with acute coronary syndromes.

Holmes LE1,2, Gupta R1,2, Rajendran S1,2, Luu J1,2, French JK1,2, Juergens CP1,2.
Cardiovascular therapeutics.Cardiovasc Ther.2016 Jun 21. doi: 10.1111/1755-5922.12203. [Epub ahead of print]
AIMS: To compare three glycoprotein IIb/IIIa receptor antagonists (GPIs) in terms of platelet inhibition and major adverse cardiac events (MACEs), and assess the rate of bleeding and MACEs between GPIs and co-administered P2Y12 agents.METHODS: Eighty-three ACS patients undergoing PCI with planned GP
PMID 27327862

Delayed severe abciximab-induced thrombocytopenia: A case report.

Piątek Ł1, Janion-Sadowska A2, Kurzawski J2, Grabowska U3, Janion M4.
Heart & lung : the journal of critical care.Heart Lung.2016 Jun 20. pii: S0147-9563(16)30100-5. doi: 10.1016/j.hrtlng.2016.06.003. [Epub ahead of print]
BACKGROUND: Thrombocytopenia is a possible side effect of routinely administered medical agents widely used in the management of patients with acute coronary syndromes (ACS). It is usually observed within 24 h after abciximab infusion. Differential diagnosis is challenging and the management controv
PMID 27340007

Japanese Journal

Effect of Abciximab Therapy in Patients Undergoing Coronary Angioplasty for Acute ST-Elevation Myocardial Infarction Complicated by Cardiogenic Shock

De Felice Francesco,Tomassini Francesco,Fiorilli Rosario [他]
Circulation journal : official journal of the Japanese Circulation Society 79(7), 1568-1574, 2015-07
NAID 40020502432

Effect of Abciximab Therapy in Patients Undergoing Coronary Angioplasty for Acute ST-Elevation Myocardial Infarction Complicated by Cardiogenic Shock

De Felice Francesco,Tomassini Francesco,Fiorilli Rosario,Gagnor Andrea,Parma Antonio,Cerrato Enrico,Musto Carmine,Nazzaro Marco Stefano,Varbella Ferdinando,Violini Roberto
Circulation Journal 79(7), 1568-1574, 2015
… Background:The effect of abciximab on survival in patients with ST-elevation myocardial infarction (STEMI) complicated by cardiogenic shock (CS) undergoing primary percutaneous coronary intervention (PCI) is not clear.Methods and Results:We evaluated outcome in 410 consecutive patients with STEMI and CS who underwent PCI treated without (n=123) or with (n=287) abciximab. … The groups with and without abciximab had similar survival at 1-year follow-up. …
NAID 130005083928

Effect of Abciximab Therapy in Patients Undergoing Coronary Angioplasty for Acute ST-Elevation Myocardial Infarction Complicated by Cardiogenic Shock

De Felice Francesco,Tomassini Francesco,Fiorilli Rosario,Gagnor Andrea,Parma Antonio,Cerrato Enrico,Musto Carmine,Nazzaro Marco Stefano,Varbella Ferdinando,Violini Roberto
Circulation Journal advpub(0), 2015
… Background:The effect of abciximab on survival in patients with ST-elevation myocardial infarction (STEMI) complicated by cardiogenic shock (CS) undergoing primary percutaneous coronary intervention (PCI) is not clear.Methods and Results:We evaluated outcome in 410 consecutive patients with STEMI and CS who underwent PCI treated without (n=123) or with (n=287) abciximab. … The groups with and without abciximab had similar survival at 1-year follow-up. …
NAID 130005066290

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★リンクテーブル★

リンク元	「mab」「アブシキシマブ」

「mab」

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);
Routes of; administration	IV
Pharmacokinetic data
Half-life	<10 min–30 min
Identifiers
CAS Registry 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
(what is this?) (verify)

　　[★]

関: モノクローナル抗体

mab

abciximab
adahmumab
adalimumab
afelimomab
alemtuzumab
apolizumab
arcitumomab
basiliximab
bevacizumab
cantuzumab
certolizumab
cetolizumab
cetuximab
clenoliximab
daclizumab
デノスマブ denosumab 抗RANKL抗体
eculizumab
edrecolomab
efalizumab
epratuzumab
galiximab
gemtuzumab
ibritumomab
インフリキシマブ infliximab 抗TNF-α抗体クローン病 Ph⁺ALL
inotuzumab
keliximab
natalizumab
nebacumab
omalilzumab
omalizumab
oregovomab
palivizumab
panitumumab
pertuzumab
pexelizumab
リツキシマブ rituximab：抗CD20抗体：慢性リンパ性白血病、B細胞リンパ腫

「アブシキシマブ」

　　[★]

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. edit

[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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abciximab