ISSN: 0300-8932 Factor de impacto 2023 7,2
Vol. 11. Núm. A.
Páginas 3-7 (Febrero 2011)

Propiedades de los diferentes inhibidores de la glucoproteína IIb/IIIa: ¿se puede aceptar el efecto de clase?

Properties of Different Glycoprotein-IIb/IIIa Inhibitors: Do These Drugs Have a Class Effect?

Antonio Fernández-Ortiz¿Iván Núñez-GilBorja Ruiz-MateosBorja Ibáñez

Opciones

Resumen

Los tres agentes inhibidores de la glucoproteína IIb/IIIa actualmente en uso clínico, abciximab, eptifibatida y tirofibán, comparten como diana terapéutica el bloqueo de la vía final común de la agregación plaquetaria, pero difieren significativamente en su estructura química, en la forma de bloquear la integrina α2bβ3 plaquetaria y en la especificidad por el receptor. Como consecuencia de ello, el patrón de inhibición de cada uno de estos fármacos en la funcionalidad plaquetaria varía y la equivalencia de beneficio clínico para una misma indicación es cuestionable. Hoy por hoy, no se dispone de ensayos clínicos de equivalencia que nos permitan aceptar o excluir un efecto de clase para los inhibidores de la glucoproteína IIb/IIIa en una determinada indicación clínica. Los resultados de los metaanálisis realizados en las diversas indicaciones clínicas tampoco han sido concluyentes, ya que no siempre muestran beneficios clínicos similares en magnitud y dirección para cada uno de los inhibidores de la glucoproteína IIb/IIIa. Por lo tanto, no podemos recomendar el intercambio o sustitución de un inhibidor por otro más allá de la indicación particular para la que se lo haya estudiado y aprobado.

Abreviaturas

GPIIb/IIIa
ICP
SCA
SCACEST
SCASEST

Palabras clave

Síndrome coronario agudo
Antiplaquetarios
Inhibidores de la glucoproteína IIb/IIIa
Este artículo solo puede leerse en pdf
Bibliografía
[1.]
E.I. Peerschke.
The platelet fibrinogen receptor.
Semin Hematol, (1985), 22 pp. 241-259
[2.]
S. Shattil.
Signaling through platelet integrin αIIbβ3: inside-out, outside-in, and sideways.
Thromb Haemost, (1999), 82 pp. 318-325
[3.]
D.P. Chew, D.J. Moliterno.
A critical appraisal of platelet glycoprotein IIb/IIIa inhibition.
J Am Coll Cardiol, (2000), 36 pp. 2028-2035
[4.]
G. De Luca, H. Suryapranata, G.W. Stone, D. Antoniucci, J.E. Tcheng, F.J. Neumann, et al.
Abciximab as adjunctive therapy to reperfusion in acute ST-segment elevation myocardial infarction: a meta-analysis of randomized trials.
JAMA, (2005), 293 pp. 1759-1765
[5.]
J.J. Ferguson, D.J. Kereiakes, A.A. Adgey, K.A. Fox, W.B. Hillegass Jr., M. Pfisterer, et al.
Safe use of platelet GP IIb/IIIa inhibitors.
Eur Heart J, (1998), 19
[6.]
B.S. Coller, E.I. Peerschke, L.E. Scudder, C.A. Sullivan.
A murine monoclonal antibody that completely blocks the binding of fibrinogen to platelets produces a thrombasthenic-like state in normal platelets and binds to glycoproteins IIb and/or IIIa.
J Clin Invest, (1983), 72 pp. 325-338
[7.]
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), 330 pp. 956-961
[8.]
B.S. Coller.
Blockade of platelet GP IIb/IIIa receptors as an antithrombotic strategy.
Circulation, (1995), 92 pp. 2373-2380
[9.]
S.H. Tam, P.M. Sassoli, R.E. Jordan, M.T. Nakada.
Abciximab (ReoPro), chimeric 7E3 Fab demonstrates equivalent affinity and functional blockade of glycoprotein IIb/IIIa and αVβ3 integrins.
Circulation, (1998), 98 pp. 1085-1092
[10.]
D.R. Phillips, R.M. Scarborough.
Clinical pharmacology of eptifibatide.
Am J Cardiol, (1997), 80 pp. 11B-20B
[11.]
D.R. Phillips, W. Teng, A. Arfsten, L. Nannizzi-Alaimo, M.M. White, C. Longhurst, et al.
Effect of Ca2+ on GPIIb-IIIa interactions with integrilin: enhanced GPIIb-IIIa binding and inhibition of platelet aggregation by reductions in the concentration of ionized calcium in plasma anticoagulated with citrate.
Circulation, (1997), 96 pp. 1488-1498
[12.]
J.E. Tcheng, J.D. Talley, J.C. O'Shea, I.C. Gilchrist, N.S. Kleiman, C.L. Grines, et al.
Clinical pharmacology of higher dose eptifibatide in percutaneous coronary intervention (the PRIDE study).
Am J Cardiol, (2001), 88 pp. 1097-1102
[13.]
M.S. Egbertson, C.T. Chang, M.E. Duggan, R.J. Gould, W. Halczenko, G.D. Hartman, et al.
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for arg-gly-asp.
J Med Chem, (1994), 37 pp. 2537-2551
[14.]
J.J. Cook, B. Bednar, J.J. Lynch, R.J. Gould, M.S. Egbertson, W. Halczenko, et al.
Tirofiban (AggrastatTM).
Cardiovasc Drug Rev, (1999), 17 pp. 199-224
[15.]
Inhibition of the platelet glycoprotein IIb/IIIa receptor with tirofiban in unstable angina and non-Q-wave myocardial infarction.
Platelet Receptor Inhibition in Ischemic Syndrome Management in Patients Limited by Unstable Signs and Symptoms (PRISM-PLUS) Study Investigators.
N Engl J Med, (1998), 338 pp. 1488-1497
[16.]
C.P. Cannon, W.S. Weintraub, L.A. Demopoulos, R. Vicari, M.J. Frey, N. Lakkis, et al.
Comparison of early invasive and conservative strategies in patients with unstable coronary syndromes treated with the glycoprotein IIb/IIIa inhibitor tirofiban.
N Engl J Med, (2001), 344 pp. 1879-1887
[17.]
Effects of platelet glycoprotein IIb/IIIa blockade with tirofiban on adverse cardiac events in patients with unstable angina or acute myocardial infarction undergoing coronary angioplasty.
The RESTORE Investigators. Randomized Efficacy Study of Tirofiban for Outcomes and REstenosis.
Circulation, (1997), 96 pp. 1445-1453
[18.]
E.J. Topol, D.J. Moliterno, H.C. Herrmann, E.R. Powers, C.L. Grines, D.J. Cohen, TARGET Investigators, et al.
Do Tirofiban and ReoPro Give Similar Efficacy Trial. Comparison of two platelet glycoprotein IIb/IIIa inhibitors, tirofiban and abciximab, for the prevention of ischemic events with percutaneous coronary revascularization.
N Engl J Med, (2001), 344 pp. 1888-1894
[19.]
M. Valgimigli, G. Percoco, D. Barbieri, F. Ferrari, G. Guardigli, G. Parrinello, et al.
The additive value of tirofiban administered with the high-dose bolus in the prevention of ischemic complications during high-risk coronary angioplasty: the ADVANCE Trial.
J Am Coll Cardiol, (2004), 44 pp. 14-19
[20.]
M. Valgimigli, G. Campo, G. Percoco, L. Bolognese, C. Vassanelli, S. Colangelo, et al.
Multicentre Evaluation of Single High-Dose Bolus Tirofiban vs Abciximab With Sirolimus-Eluting Stent or Bare Metal Stent in Acute Myocardial Infarction Study (MULTISTRATEGY) Investigators. Comparison of angioplasty with infusion of tirofiban or abciximab and with implantation of sirolimus-eluting or uncoated stents for acute myocardial infarction: the MULTISTRATEGY randomized trial.
[21.]
I. Soares, A.V. Carneiro.
Drug class effects: definitions and practical applications.
Rev Port Cardiol, (2002), 21 pp. 1031-1042
[22.]
W.L. Greene, J. Concato, A.R. Feinstein.
Claims of equivalence in medical research: are they supported by the evidence?.
Ann Intern Med, (2000), 132 pp. 715-722
[23.]
A. Marzocchi, A. Manari, G. Piovaccari, C. Marrozzini, S. Marra, P. Magnavacchi, FATA Investigators, et al.
Randomized comparison between tirofiban and abciximab to promote complete ST-resolution in primary angioplasty: results of the facilitated angioplasty with tirofiban or abciximab (FATA) in ST-elevation myocardial infarction trial.
Eur Heart J, (2008), 29 pp. 2972-2980
[24.]
L. Bolognese, G. Falsini, F. Liistro, P. Angioli, K. Ducci, T. Taddei, et al.
Randomized comparison of upstream tirofiban versus downstream high bolus dose tirofiban or abciximab on tissue-level perfusion and troponin release in high-risk acute coronary syndromes treated with percutaneous coronary interventions: the EVEREST trial.
J Am Coll Cardiol, (2006), 47 pp. 522-528
[25.]
G.B. Danzi, M. Sesana, C. Capuano, L. Mauri, P. Berra Centurini, R. Baglini.
Comparison in patients having primary coronary angioplasty of abciximab versus tirofiban on recovery of left ventricular function.
Am J Cardiol, (2004), 94 pp. 35-39
[26.]
N.M. Ernst, H. Suryapranata, K. Miedema, R.J. Slingerland, J.P. Ottervanger, J.C. Hoorntje, et al.
Achieved platelet aggregation inhibition after different antiplatelet regimens during percutaneous coronary intervention for ST-segment elevation myocardial infarction.
J Am Coll Cardiol, (2004), 44 pp. 1187-1193
[27.]
U. Zeymer, A. Margenet, M. Haude, C. Bode, J.M. Lablanche, H. Heuer, et al.
Randomized comparison of eptifibatide versus abciximab in primary percutaneous coronary intervention in patients with acute ST-segment elevation myocardial infarction: results of the EVA-AMI Trial.
J Am Coll Cardiol, (2010), 56 pp. 463-469
[28.]
D.J. Moliterno, and the TENACITY Steering Committee and Investigators.
A randomized two-by-two comparison of high-dose bolus tirofiban versus abciximab and unfractionated heparin versus bivalirudin during percutaneous coronary revascularization and stent placement: The tirofiban evaluation of novel dosing versus abciximab with clopidogrel and inhibition of thrombin (TENACITY) study trial.
Catheter Cardiovasc Interv, (2010),
[29.]
E. Boersma, R.A. Harrington, D.J. Moliterno, H. White, P. Théroux, F. Van de Werf, et al.
Platelet glycoprotein IIb/IIIa inhibitors in acute coronary syndromes: a meta-analysis of all major randomised clinical trials.
[30.]
Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes.
The PURSUIT Trial Ivestigators. Platelet Glycoprotein IIb/IIIa in Unstable Angina: Receptor Suppression Using Integrilin Therapy.
N Engl J Med, (1998), 339 pp. 436-443
[31.]
M.L. Simoons, The GUSTO IV-ACS Investigators.
Effect of glycoprotein IIb/IIIa receptor blocker abciximab on outcome in patients with acute coronary syndromes without early coronary revascularisation: the GUSTO IV-ACS randomised trial.
Lancet, (2001), 357 pp. 1915-1924
[32.]
M.L. Simoons, M.J. De Boer, M.J. Van den Brand, A.J. Van Miltenburg, J.C. Hoorntje, G.R. Heyndrickx, et al.
Randomized trial of a GPIIb/IIIa platelet receptor blocker in refractory unstable angina. European Cooperative Study Group.
Circulation, (1994), 89 pp. 596-603
[33.]
S.R. Steinhubl, J.D. Talley, G.A. Braden, J.E. Tcheng, P.J. Casterella, D.J. Moliterno, et al.
Point-of-care measured platelet inhibition correlates with a reduced risk of an adverse cardiac event after percutaneous coronary intervention: results of the GOLD (AU-Assessing Ultegra) multicenter study.
Circulation, (2001), 103 pp. 2572-2578
[34.]
K.A. Ault, C.P. Cannon, J. Mitchell, J. McCahan, R.P. Tracy, W.F. Novotny, et al.
Platelet activation in patients after an acute coronary syndrome: results from the TIMI-12 trial. Thrombolysis in Myocardial Infarction.
J Am Coll Cardiol, (1999), 33 pp. 634-639
[35.]
G. Montalescot, D. Antoniucci, A. Kastrati, F.J. Neumann, M. Borentain, A. Migliorini, et al.
Abciximab in primary coronary stenting of ST-elevation myocardial infarction: a European meta-analysis on individual patients’ data with long-term follow-up.
Eur Heart J, (2007), 28 pp. 443-449
[36.]
G. De Luca, E. Navarese, P. Marino.
Risk profile and benefits from GP IIb-IIIa inhibitors among patients with ST-segment elevation myocardial infarction treated with primary angioplasty: a meta-regression analysis of randomized trials.
Eur Heart J, (2009), 30 pp. 2705-2713
[37.]
J.J. Smit, J.W. Van Werkum, J. Ten Berg, R. Slingerland, J.P. Ottervanger, T. Heestermans, et al.
Ongoing Tirofiban in Myocardial Infarction Evaluation (On-TIME) trial investigators. Prehospital triple antiplatelet therapy in patients with acute ST elevation myocardial infarction leads to better platelet aggregation inhibition and clinical outcome than dual antiplatelet therapy.
Heart, (2010), 96 pp. 1815-1820
[38.]
E.J. Topol, A.M. Lincoff, D.J. Kereiakes, N.S. Kleiman, E.A. Cohen, J.J. Ferguson, et al.
Multi-year follow-up of abciximab therapy in three randomized, placebo-controlled trials of percutaneous coronary revascularization.
Am J Med, (2002), 113 pp. 1-6
[39.]
M. Labinaz, C. Ho, S. Banerjee, J. Martin, S. Chen, S. Mensinkai.
Meta-analysis of clinical efficacy and bleeding risk with intravenous glycoprotein IIb/IIIa antagonists for percutaneous coronary intervention.
Can J Cardiol, (2007), 23 pp. 963-970
[40.]
M. Roffi, D.P. Chew, D. Mukherjee, D.L. Bhatt, J.A. White, C. Heeschen, et al.
Platelet glycoprotein IIb/IIIa inhibitors reduce mortality in diabetic patients with non-ST-segment-elevation acute coronary syndromes.
Circulation, (2001), 104 pp. 2767-2771
[41.]
W.B. Batchelor, T.R. Tolleson, Y. Huang, R.L. Larsen, R.M. Mantell, P. Dillard, et al.
Randomized COMparison of platelet inhibition with abciximab, tiRofiban and eptifibatide during percutaneous coronary intervention in acute coronary syndromes: the COMPARE trial. Comparison Of Measurements of Platelet aggregation with Aggrastat, Reopro, and Eptifibatide.
Circulation, (2002), 106 pp. 1470-1476
[42.]
J.W. Van Werkum, W.B. Gerritsen, J.C. Kelder, C.M. Hackeng, S.M. Ernst, V.H. Deneer, et al.
Inhibition of platelet function by abciximab or high-dose tirofiban in patients with STEMI undergoing primary PCI: a randomised trial.
Neth Heart J, (2007), 15 pp. 375-381
[43.]
D.J. Schneider, P.Q. Baumann, D.A. Whitaker, B.E. Sobel.
Variation in the ability of glycoprotein IIb-IIIa antagonists to exert and maintain their inhibitory effects on the binding of fibrinogen.
J Cardiovasc Pharmacol, (2005), 46 pp. 41-45
Copyright © 2011. Sociedad Española de Cardiología
¿Es usted profesional sanitario apto para prescribir o dispensar medicamentos?