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NDA 20-718/S-028 Page 4 Integrilin®(eptifibatide) INJECTION For Intravenous Administration DESCRIPTION Eptifibatide is a cyclic heptapeptide containing six amino acids and one mercaptopropionyl (des-amino cysteinyl) residue. An interchain disulfide bridge is formed between the cysteine amide and the mercaptopropionyl moieties. 6 2 Chemically it is N -(aminoiminomethyl)-N -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-�-aspartyl-L-tryptophyl-L­ prolyl-L-cysteinamide, cyclic (1→6)-disulfide. Eptifibatide binds to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets and inhibits platelet aggregation. The eptifibatide peptide is produced by solution-phase peptide synthesis, and is purified by preparative reverse- phase liquid chromatography and lyophilized. The structural formula is: Integrilin (eptifibatide) Injection is a clear, colorless, sterile, non-pyrogenic solution for intravenous (IV) use with an empirical formula of C H N O S and a molecular weight of 831.96. Each 10-mL vial contains 2 mg/mL of 35 49 11 9 2 eptifibatide and each 100-mL vial contains either 0.75 mg/mL of eptifibatide or 2 mg/mL of eptifibatide. Each vial of either size also contains 5.25 mg/mL citric acid and sodium hydroxide to adjust the pH to 5.35. CLINICAL PHARMACOLOGY Mechanism of Action Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands to GP IIb/IIIa. When administered intravenously, eptifibatide inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. Platelet aggregation inhibition is reversible following cessation of the eptifibatide infusion; this is thought to result from dissociation of eptifibatide from the platelet. Pharmacodynamics Infusion of eptifibatide into baboons caused a dose-dependent inh