Prasugrel

Číslo: 1 / 2011 (Obsah)
Rubrika: Nová léčiva / Nové indikace
Obor: Kardiologie
Autoři: Doc. MUDr. Zuzana Moťovská, Ph.D.
Autoři - působiště: III. interní kardiologická klinika 3. LF UK a FNKV, Praha
Klíčová slova: inhibice aktivace destiček, prasugrel, clopidogrel
Citace: 1 Husted S, van Giezen JJ. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc Ther 2009;27(4): 259–74. 2 Farid NA, Smith RL, Gillespie TA, et al. The disposition of prasugrel, a novel thienopyridine, in humans. Drug Metab Dispos 2007;35:1096–104. 3 Jakubowski JA, Winters KJ, Naganuma H, et al. A Novel Thienopyridine Antiplatelet Agent. Cardiovascular Drug Reviews 2007;25(4):357–74. 4 Clarke TA, Waskell LA. The metabolism of clopidogrel is catalyzed by human cytochrome P450 3A and is inhibited by atorvastatin. Drug Metab Dispos 2003;31:53–9. 5 Brandt JT, Payne CD, Wiviott SD, et al. A comparison of prasugrel and clopidogrel loading doses on platelet function: Magnitude of platelet inhibition is related to active metabolite formation. Am Heart J 2007;153: e9–e16. 6 Wiviott SD, Trenk D, Frelinger AL, et al. Prasugrel compared with high loading- and maintenance-dose clopidogrel in patients with planned percutaneous coronary intervention: the Prasugrel in Comparison to Clopidogrel for Inhibition of Platelet Activation and Aggregation-Thrombolysis in Myocardial Infarction 44 trial. Circulation 2007;116:2923–32. 7 Sugidachi A, Ogawa T, Kurihara A, et al. The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel’s active metabolite. J Thromb Haemost 2007;5:1545–51. 8 Wallentin L, Varenhorst C, James S, et al. Prasugrel achieves greater and faster P2Y12 receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease. Eur Heart J 2008;29:21–30. 9 Muller I, Besta F, Schulz C, et al. Prevalence of clopidogrel non-responders among patients with stable angina pectoris scheduled for elective coronary stent placement. Thromb Haemost 2003;89:783–7. 10 Lev EI, Patel RT, Maresh KJ, et al. Aspirin and clopidogrel drug response in patients undergoing percutaneous coronary intervention: the role of dual drug resistance. J Am Coll Cardiol 2006;47(1):27–33. 11 Matetzky S, Shenkman B, Guetta V, et al. Clopidogrel resistance is associated with increased risk of recurrent atherothrombotic events in patients with acute myocardial infarction. Circulation 2004;109:3171–5. 12 Jernberg T, Payne CD, Winters KJ, et al. Prasugrel achieves greater inhibition of platelet aggregation and a lower rate of non-responders compared with clopidogrel in aspirin-treated patients with stable coronary artery disease. Eur Heart J 2006;27:1166–73. 13 Motovska Z, Kala P. Benefits and risks of clopidogrel use in patients with coronary artery disease: Evidence from randomized studies and registries. Clin Ther 2008;30P2:2191–202. 14 Wiviott SD, Braunwald E, McCabe CH, et al. TRITON-TIMI 38 Investigators. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Eng J Med 2007;357:2001–15. 15 Montalescot G, Wiviott SD, Braunwald E, et al; TRITON-TIMI 38 investigators. Prasugrel compared with clopidogrel in patients undergoing percutaneous coronary intervention for ST-elevation myocardial infarction (TRITON-TIMI 38): double-blind, randomised controlled trial. Lancet 2009;373(9665):723–31. 16 A comparison of prasugrel and clopidogrel in acute coronary syndrome subjects (TRILOGY ACS). http://www.clinicaltrials.gov/ct2/ show/NCT00699998?term=NCT00699998&rank=1. 17 Wiviott SD, Braunwald E, McCabe CH, et al. Intensive oral antiplatelet therapy for reduction of ischaemic events including stent thrombosis in patients with acute coronary syndromes treated with percutaneous coronary intervention and stenting in the TRITON-TIMI 38 trial: a subanalysis of a randomised trial. Lancet 2008;371(9621):1353–63. 18 Donahoe SM, Stewart GC, McCabe CH, et al. Diabetes and mortality following acute coronary syndromes. JAMA 2007;298:765–75. 19 Yusuf S, Zhao F, Mehta SR, Chrolavicius S, et al. Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 2001;345:494–502. 20 Motovska Z, Widimsky P, Petr R, et al.; on behalf of the PRAGUE-8 Study Investigators. Factors Influencing Clopidogrel Efficacy in Patients With Stable Coronary Artery Disease Undergoing Elective Percutaneous Coronary Intervention: Statin's Advantage and the Smoking "Paradox". J Cardiovasc Pharmacol 2009;53(5):368–72. 21 Angiolillo DJ, Showmaker SB, Desai B, et al. Randomized comparison of a high clopidogrel maintenance dose in patients with diabetes mellitus and coronary artery disease: results of the optimizing antiplatelet therapy in diabetes mellitus (OPTIMUS) study. Circulation 2007;115:1–9. 22 Angiolillo DJ, Bernardo E, Sabate M, et al. Impact of platelet reactivity on cardiovascular outcomes in patients with type 2 diabetes mellitus and coronary artery disease J Am Coll Cardiol 2007;50:1541–7. 23 Erlinge D, Varenhorst C, Braun OÖ, et al. Patients with poor responsiveness to thienopyridine treatment or with diabetes have lower levels of circulating active metabolite, but their platelets respond normally to active metabolite added ex vivo. J Am Coll Cardiol 2008;52:1968–77. 24 Wiviott SD, Braunwald E, Angiolillo DJ, et al. Greater clinical benefit of more intensive oral antiplatelet therapy with prasugrel in patients with diabetes mellitus in TRITON-TIMI 38. Circulation 2008;118:1626–36. 25 Simon T, Verstuyft C, Mary-Krause M, et al. Genetic determinants of response to clopidogrel and cardiovascular events. N Engl J Med 2009;360:363–75. 26 Mega JL, Close SL, Wiviott SD, et al. Cytochrome P-450 polymorphisms and response to clopidogrel. N Engl J Med 2009;360:354–62.

Souhrn

Duální protidestičková léčba, kyselina acetylsalicylová a thienopyridin, potlačuje aktivaci trombocytů v míře, která umožňuje implantaci intrakoronárního stentu s akceptovatelným rizikem trombózy stentu i krvácaní. Prasugrel, thienopyridin 3. generace, má rychlejší nástup účinku a receptory P2Y12 inhibuje efektivněji ve srovnání s clopidogrelem, thienopyridinem 2. generace. Protidestičkový účinek prasugrelu je stabilní, bez významné interindividuální variability. Laboratorní přednosti prasu-grelu se transformovali i do klinických výsledků. Cílovou populací pro tento lék jsou pacienti s vysokým rizikem aterotrombotických příhod: pacienti podstupující PCI pro infarkt myokardu s elevacemi ST, diabetici s akutním koronárním syndromem, kteří podstupují PCI, pacienti s rizikem trombózy stentu nebo po trombóze stentu a pacienti s genetickou mutací, která vede k významně snížené metabolizaci clopidogrelu na jeho aktivní formu. „

Literatura

1 Husted S, van Giezen JJ. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc Ther 2009;27(4): 259–74. 2 Farid NA, Smith RL, Gillespie TA, et al. The disposition of prasugrel, a novel thienopyridine, in humans. Drug Metab Dispos 2007;35:1096–104. 3 Jakubowski JA, Winters KJ, Naganuma H, et al. A Novel Thienopyridine Antiplatelet Agent. Cardiovascular Drug Reviews 2007;25(4):357–74. 4 Clarke TA, Waskell LA. The metabolism of clopidogrel is catalyzed by human cytochrome P450 3A and is inhibited by atorvastatin. Drug Metab Dispos 2003;31:53–9. 5 Brandt JT, Payne CD, Wiviott SD, et al. A comparison of prasugrel and clopidogrel loading doses on platelet function: Magnitude of platelet inhibition is related to active metabolite formation. Am Heart J 2007;153: e9–e16. 6 Wiviott SD, Trenk D, Frelinger AL, et al. Prasugrel compared with high loading- and maintenance-dose clopidogrel in patients with planned percutaneous coronary intervention: the Prasugrel in Comparison to Clopidogrel for Inhibition of Platelet Activation and Aggregation-Thrombolysis in Myocardial Infarction 44 trial. Circulation 2007;116:2923–32. 7 Sugidachi A, Ogawa T, Kurihara A, et al. The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel’s active metabolite. J Thromb Haemost 2007;5:1545–51. 8 Wallentin L, Varenhorst C, James S, et al. Prasugrel achieves greater and faster P2Y12 receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease. Eur Heart J 2008;29:21–30. 9 Muller I, Besta F, Schulz C, et al. Prevalence of clopidogrel non-responders among patients with stable angina pectoris scheduled for elective coronary stent placement. Thromb Haemost 2003;89:783–7.
10
Lev EI, Patel RT, Maresh KJ, et al. Aspirin and clopidogrel drug response in patients undergoing percutaneous coronary intervention: the role of dual drug resistance. J Am Coll Cardiol 2006;47(1):27–33.
11
Matetzky S, Shenkman B, Guetta V, et al. Clopidogrel resistance is associated with increased risk of recurrent atherothrombotic events in patients with acute myocardial infarction. Circulation 2004;109:3171–5.
12
Jernberg T, Payne CD, Winters KJ, et al. Prasugrel achieves greater inhibition of platelet aggregation and a lower rate of non-responders compared with clopidogrel in aspirin-treated patients with stable coronary artery disease. Eur Heart J 2006;27:1166–73.
13
Motovska Z, Kala P. Benefits and risks of clopidogrel use in patients with coronary artery disease: Evidence from randomized studies and registries. Clin Ther 2008;30P2:2191–202.
14
Wiviott SD, Braunwald E, McCabe CH, et al. TRITON-TIMI 38 Investigators. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Eng J Med 2007;357:2001–15.
15
Montalescot G, Wiviott SD, Braunwald E, et al; TRITON-TIMI 38 investigators. Prasugrel compared with clopidogrel in patients undergoing percutaneous coronary intervention for ST-elevation myocardial infarction (TRITON-TIMI 38): double-blind, randomised controlled trial. Lancet 2009;373(9665):723–31.
16
A comparison of prasugrel and clopidogrel in acute coronary syndrome subjects (TRILOGY ACS). http://www.clinicaltrials.gov/ct2/ show/NCT00699998?term=NCT00699998&rank=1.
17
Wiviott SD, Braunwald E, McCabe CH, et al. Intensive oral antiplatelet therapy for reduction of ischaemic events including stent thrombosis in patients with acute coronary syndromes treated with percutaneous coronary intervention and stenting in the TRITON-TIMI 38 trial: a subanalysis of a randomised trial. Lancet 2008;371(9621):1353–63.
18
Donahoe SM, Stewart GC, McCabe CH, et al. Diabetes and mortality following acute coronary syndromes. JAMA 2007;298:765–75.
19
Yusuf S, Zhao F, Mehta SR, Chrolavicius S, et al. Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 2001;345:494–502.
20
Motovska Z, Widimsky P, Petr R, et al.; on behalf of the PRAGUE-8 Study Investigators. Factors Influencing Clopidogrel Efficacy in Patients With Stable Coronary Artery Disease Undergoing Elective Percutaneous Coronary Intervention: Statin's Advantage and the Smoking "Paradox". J Cardiovasc Pharmacol 2009;53(5):368–72.
21
Angiolillo DJ, Showmaker SB, Desai B, et al. Randomized comparison of a high clopidogrel maintenance dose in patients with diabetes mellitus and coronary artery disease: results of the optimizing antiplatelet therapy in diabetes mellitus (OPTIMUS) study. Circulation 2007;115:1–9.
22
Angiolillo DJ, Bernardo E, Sabate M, et al. Impact of platelet reactivity on cardiovascular outcomes in patients with type 2 diabetes mellitus and coronary artery disease J Am Coll Cardiol 2007;50:1541–7.
23
Erlinge D, Varenhorst C, Braun OÖ, et al. Patients with poor responsiveness to thienopyridine treatment or with diabetes have lower levels of circulating active metabolite, but their platelets respond normally to active metabolite added ex vivo. J Am Coll Cardiol 2008;52:1968–77.
24
Wiviott SD, Braunwald E, Angiolillo DJ, et al. Greater clinical benefit of more intensive oral antiplatelet therapy with prasugrel in patients with diabetes mellitus in TRITON-TIMI 38. Circulation 2008;118:1626–36.
25
Simon T, Verstuyft C, Mary-Krause M, et al. Genetic determinants of response to clopidogrel and cardiovascular events. N Engl J Med 2009;360:363–75.
26
Mega JL, Close SL, Wiviott SD, et al. Cytochrome P-450 polymorphisms and response to clopidogrel. N Engl J Med 2009;360:354–62.

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