Characterization of Biochemical and Functional Effects of Antiplatelet Drugs as a Key to Their Clinical Development

Carlo Patrono; Paola Patrignani; Bianca Rocca; Raffele Landolfi

doi:10.1055/s-0038-1642710

Thrombosis and Haemostasis, Table of Contents

Thromb Haemost 1995; 74(01): 396-400
DOI: 10.1055/s-0038-1642710

Symposium

Antiplatelet Drugs

Schattauer GmbH Stuttgart

Characterization of Biochemical and Functional Effects of Antiplatelet Drugs as a Key to Their Clinical Development

Authors

Carlo Patrono

Department of Pharmacology, University of Chieti “G. D ‘Annunzio ” School of Medicine, Chieti; and Thrombosis & Haemostasis Research Center, Catholic University School of Medicine, Rome, Italy
Paola Patrignani

Department of Pharmacology, University of Chieti “G. D ‘Annunzio ” School of Medicine, Chieti; and Thrombosis & Haemostasis Research Center, Catholic University School of Medicine, Rome, Italy
Bianca Rocca

Department of Pharmacology, University of Chieti “G. D ‘Annunzio ” School of Medicine, Chieti; and Thrombosis & Haemostasis Research Center, Catholic University School of Medicine, Rome, Italy
Raffele Landolfi

Department of Pharmacology, University of Chieti “G. D ‘Annunzio ” School of Medicine, Chieti; and Thrombosis & Haemostasis Research Center, Catholic University School of Medicine, Rome, Italy

Abstract

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References

References
1 Bom GV R. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature 1962; 194: 927-929
2 Patrono C. Aspirin as an antiplatelet drug. N Engl J Med 1994; 330: 1287-1294
3 Patrono C, Ciabattoni G, Pinca E, Pugliese F, Castrucci G, De Salvo A, Satta MA, Peskar BA. Low dose aspirin and inhibition of thromboxane B₂production in healthy subjects. Thromb Res 1980; 17: 317-327
4 Patrono C, Ciabattoni G, Pugliese F, Pierucci A, Blair IA, FitzGerald GA. Estimated rate of thromboxane secretion into the circulation of normal humans. I Clin Invest 1986; 77: 590-594
5 Ciabattoni G, Pugliese F, Davi G, Pierucci A, Simonetti BM, Patrono C. Fractional conversion of thromboxane B₂to urinary 11-dehydro-thromboxane B2 in man. Biochim Biophys Acta 1989; 992: 66-70
6 Catella F, FitzGerald GA. Paired analysis of urinary thromboxane B₂metabolites in humans. Thromb Res 1987; 47: 647-656
7 Reilly IA G, FitzGerald GA. Inhibition of thromboxane formation in vivo and ex vivo: implications for therapy with platelet inhibitory drugs. Blood 1987; 69: 180-186
8 Born GV R, Hume M. Effects of numbers and sizes of platelet aggregates on optical density of plasma. Nature 1967; 215: 1027-1029
9 Latimer P, Born GV R, Michail F. Application of high-scattering theory to the optical effects associated with the morphology of blood platelets. Arch Biochem Biophys 1977; 180: 151-159
10 Thompson NT, Scrutton MC, Wallis RB. Particle volume changes associated with light transmittance changes in the platelet aggregometer: dependence upon aggregating agent and effectiveness of stimulus. Thromb Res 1986; 41: 615-626
11 Nichols AR, Bosmann HB. Platelet aggregation: newly quantified using non-empirical parameters. Thromb Haemostas 1979; 42: 679-693
12 Benner KU, Tamblyn CH, Swank RL, Seaman GV F. Platelet count ratio (PCR) as an additional parameter in the quantitation of platelet aggregation in vitro. Thromb Res 1980; 17: 801-808
13 Frojmovic MM, Milton JG, Gear AR L. Platelet aggregation measured in vitro by microscopic and electronic particle counting. Methods Enzymol 1989; 169: 134-149
14 Hause LL, Retzinger GS, Megan PA. Rapid determination of the rate constant of agonist-induced association of single platelets. Thromb Res 1991; 61: 105-112
15 Gear AR L. Rapid reactions of platelets studied by a quenched-flow approach: aggregation kinetics. J Lab Clin Med 1982; 100: 866-886
16 Frojmovic MM, Milton JG, Duchastel A. Microscopic measure-ments of platelet aggregation reveal a low ADP-dependent process distinct from turbidimetrically measured aggregation. J Lab Clin Med 1983; 101: 964-976
17 Leung LL K. Role of thrombospondin in platelet aggregation. J Clin Invest 1984; 74: 1764-1772
18 Pedvis LG, Wong T, Frojmovic MM. Differential inhibition of the platelet activation sequence: shape change, micro- and macro-aggregation, by stable prostacyclin analogue (Iloprost). Thromb Haemostas 1988; 59: 323-328
19 Rocca B, De Cristofaro R, Della Ventura M, Bizzi B, Landolfi R. Kinetics of free platelet decrease after ADP: effect of fibrinogen binding inhibitors. Platelets. 1995 in press
20 FitzGerald GA, Reilly IA G, Pedersen AK. he biochemical pharmacology of thromboxane synthetase inhibition in man. Circulation 1985; 72: 1194-1201
21 Gresele P, Deckmyn H, Arnout J, Nenci GG, Vermylen J. harac-terization of N,N'-bis(3-picolyl)-4-methoxy-isophthalamide (pico- tamide) as a dual thromboxane synthase inhibitor/thromboxane A₂receptor antagonist in human platelets. Thromb Haemostas 1989; 61: 479-484
22 Neri Serneri GG, Gensini GF, Poggesi L, Modesti PA, Rostagno C, Boddi M, Gori AM, Martini F, leri A, Margheri M, Abbate R. he role of extraplatelet thromboxane A₂in unstable angina investigated with a dual thromboxane A₂inhibitor: importance of activated monocytes. Coronary Artery Dis 1994; 5: 137-145
23 Minuz P, Lechi C, Arosio E, Guzzo P, Zannoni M, Lauciello C, Lechi A. ffect of picotamide on platelet aggregation and on throm-boxane A₂production in vivo. Thromb Haemostas 1991; 65: 312-316
24 Balsano F, Violi F. DEP group: Effect of picotamide on the clinical progression of peripheral vascular disease. Circulation 1993; 87: 1563-1569
25 Patrignani P, Filabozzi P, Patrono C. elective cumulative inhibition of platelet thromboxane production by low-dose aspirin in healthy subjects. J Clin Invest 1982; 69: 1366-1372
26 Patrono C, Ciabattoni G, Patrignani P, Filabozzi P, Catella F, Davi G, Forni L. linical pharmacology of platelet cyclooxygenase inhibition. Circulation 1985; 72: 1177-1183
27 FitzGerald GA, Oates JA, Hawiger J, Maas RL, Roberts LJ, Brash AR. ndogenous biosynthesis of prostacyclin and thromboxane and platelet function during chronic administration of aspirin in man. J Clin Invest 1983; 71: 676-688
28 De Caterina R, Giannessi D, Boem A, Bernini W, Battaglia D, Michelassi C, Dell'Amico F, L'Abbate A, Patrignani P, Patrono C. qual antiplatelet effects of aspirin 50 or 324 mg/day in patients after acute myocardial infarction. Thromb Haemostas 1985; 54: 528-532
29 Antiplatelet Trialists' Collaboration: Collaborative overview of randomised trials of antiplatelet treatment.. Part I: Prevention of death, myocardial infarction and stroke by prolonged antiplatelet therapy in various categories of patients. BMJ 1994; 308: 81-106
30 The RISC Group: Risk of myocardial infarction and death during treatment with low dose aspirin and intravenous heparin in men with unstable coronary artery disease.. Lancet 1990; 336: 827-830
31 Juul-Moller S, Edvardsson N, Jahnmatz B. or the Swedish Angina Pectoris Aspirin Trial (SAPAT) Group: Double-blind trial of aspirin in primary prevention of myocardial infarction in patients with stable chronic angina pectoris. Lancet 1992; 340: 1421-1425
32 The SALT Collaborative Group: Swedish aspirin low-dose trial (SALT) of 75 mg aspirin as secondary prophylaxis after cerebro-vascular ischaemic events.. Lancet 1991; 338: 1345-1349
33 Davi G, Catalano I, Averna M, Notarbartolo A, Strano A, Ciabattoni G, Patrono C. hromboxane biosynthesis and platelet function in type-II diabetes mellitus. N Engl J Med 1990; 322: 1769-1776
34 Davi G, Notarbartolo A, Catalano I, Averna M, Barbagallo C, Ciabattoni G, Patrono C. ncreased thromboxane biosynthesis in type Ha hypercholesterolemia. Circulation 1992; 85: 1792-1797
35 Koudstaal PJ, Ciabattoni G, Van Gijn I, Nieuwenhuis HK, De Groot P, Sixma JJ, Patrono C. Increased thromboxane biosynthesis in patients with acute cerebral ischemia. Stroke 1993; 24: 219-222
36 Vejar M, Fragasso G, Hackett D, Lipkin DP, Maseri A, Born GV R, Ciabattoni G, Patrono C. Dissociation of platelet activation and spontaneous myocardial ischemia in unstable angina. Thromb Haemostas 1990; 63: 163-168
37 Smith WL. rostanoid biosynthesis and mechanisms of action. Am I Physiol 1992; 263 F 181-191 F
38 Cipollone F, Patrignani P, Greco A, Cuccurullo F, Patrono C, Rebuzzi AG, Liuzzo G, Quaranta G, Maseri A. ifferential suppression of enhanced thromboxane biosynthesis in unstable angina by indobufen and aspirin. Eur Heart J. 1995 in press abstract
39 Patrignani P, Panara MR, Greco A, Fusco O, Natoii C, lacobelli S, Cipollone F, Ganci A, Creminon C, Maclouf J, Patrono C. iochemical and pharmacological characterization of the cyclooxy-genase activity of human blood prostaglandin endoperoxide synthases. J Pharmacol Exp Ther 1994; 271: 1705-1712
40 Davi G, Patrono C, Catalano I, Custro N, Giammarresi C, Ganci A, Cosentino F, Notarbartolo A. nhibition of thromboxane bio-synthesis and platelet function by indobufen in type II diabetes mellitus. Arterioscler Thromb 1993; 13: 1346-1349
41 ETDRS Investigators: Aspirin effects on mortality and morbidity in patients with diabetes mellitus.. Early treatment diabetic retinopathy study report 14. JAMA 1992; 268: 1292-1300
42 Landolfi R, Rocca B, Patrono C. leeding and thrombosis in myeloproliferative disorders: mechanisms and treatment. Crit Rev Oncol Hematol. 1995 in press
43 Landolfi R, Ciabattoni G, Patrignani P, Castellana MA L, Pogliani E, Bizzi B, Patrono C. ncreased thromboxane biosynthesis in patients with polycythemia vera: evidence for aspirin-suppressible platelet activation in vivo. Blood 1992; 80: 1965-1971
44 Landolfi R. ong-term safety of low-dose aspirin in polycythemia vera. J Investig Med. 1995 in press abstract
45 Van Kooten F, Ciabattoni G, Patrono C, Schmitz PI M, van Gijn J, Koudstaal PJ. vidence for episodic platelet activation in acute ischemic stroke. Stroke. 1994; 25: 278-281