Effect of Ca2+ on GP IIb-IIIa interactions with integrilin : Enhanced GP IIb-IIIa binding and inhibition of platelet aggregation by reductions in the concentration of ionized calcium in plasma anticoagulated with citrate

Integrilin (eptifibatide), a potent inhibitor of the fibrinogen binding function of GP IIb-llla, has been shown to reduce the thrombotic complications of angioplasty and of acute coronary syndromes. The present study was designed to determine whether the reduced Ca2+ concentrations in plasma anticoa...

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Published in:Circulation (New York, N.Y.) N.Y.), 1997-09, Vol.96 (5), p.1488-1494
Main Authors: PHILLIPS, D. R, TENG, W, SCARBOROUGH, R. M, ARFSTEN, A, NANNIZZI-ALAIMO, L, WHITE, M. M, LONGHURST, C, SHATTIL, S. J, RANDOLPH, A, JAKUBOWSKI, J. A, JENNINGS, L. K
Format: Article
Language:English
Subjects:
Antibodies, Monoclonal
Anticoagulants - pharmacology
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Calcium - blood
Calcium - physiology
Citric Acid - pharmacology
Epitopes
Eptifibatide
Fibrinogen - metabolism
Humans
Medical sciences
Osmolar Concentration
Peptides - pharmacology
Pharmacology. Drug treatments
Plasma - drug effects
Platelet Aggregation Inhibitors - pharmacology
Platelet Glycoprotein GPIb-IX Complex - drug effects
Platelet Glycoprotein GPIb-IX Complex - immunology
Platelet Glycoprotein GPIb-IX Complex - metabolism
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Summary:Integrilin (eptifibatide), a potent inhibitor of the fibrinogen binding function of GP IIb-llla, has been shown to reduce the thrombotic complications of angioplasty and of acute coronary syndromes. The present study was designed to determine whether the reduced Ca2+ concentrations in plasma anticoagulated with citrate affect Integrilin binding to GP IIb-IIIa and the ex vivo pharmacodynamic measurements for this drug. Lower concentrations of Integrilin were found to inhibit platelet aggregation in plasma anticoagulated with citrate (for ADP, mean+/-SD IC(50)=140+/-40 nmol/L, n=6; Ca2+ =40 to 50 micromol/L) than with PPACK (IC(50)=570+/-70 nmol/L, P
ISSN:0009-7322
1524-4539
DOI:10.1161/01.CIR.96.5.1488