FUTURA-长城会分析.pptVIP

* 磺达肝癸钠通过AT间接起到抑制Xa因子，进而起到抗凝作用。 合成的简单的分子结构和药理学原理决定了一定剂量范围的磺达肝癸钠在有效抗凝的同时，不过度干扰生理止血的作用。 * * * OASIS 5 was a randomized, double-blind, double-dummy trial in 20,078 patients with UA/NSTEMI in 576 centers in 41 countries Patients were eligible if they presented to hospital with symptoms of UA or MI without persistent ST elevation and at least two of the following additional criteria: age 60 years, troponin T or I or CK-MB above the upper limit of normal or ECG changes compatible with ischemia (i.e., ST depression at least 1 mm in two contiguous leads or T-wave inversion 3 mm or any dynamic ST shift or transient ST elevation). Exclusion criteria were: Age 21 years Any contra-indication to enoxaparin Hemorragic stroke 12 months Creatinine 3 mg/dL or 265 μmol/L Fondaparinux was given for 8 days or until hospital discharge (if earlier), and enoxaparin was given for 2-8 days or until the patient was clinically stable, as per its current approval for use in UA and NSTEMI. The minimum duration of therapy was two days. However, catheterization and PCI could be scheduled earlier than this time if necessary. Blinded study drugs were continued through the PCI procedure. * Almost all categ或ies of 大出血 were reduced in the 磺达肝癸钠 group. * * There were no cases of catheter thrombosis with 磺达肝癸钠 when at least 1000 U of UFH was used (mean 5000 U). 相对危险性减少（relative risk reduction, RRR）： * * IQR（inter-quartile range）:四分位数间距. * 接受磺达肝癸钠治疗的ACS患者PCI中低剂量与标准剂量UFH的对比研究: FUTURA/OASIS 8 IIa II 纤维 蛋白原 纤维蛋白 凝块 外源性途径 内源性途径 AT Xa AT AT 抗凝血酶 (AT) Adapted from Turpie AGG et al. N Engl J Med. 2001;344:619. Prescribing Information for 磺达肝癸钠. 磺达肝癸钠通过与AT结合而间接抑制Xa因子 磺达肝癸钠作用机理磺达肝癸钠与AT结合作用于Xa因子，可循环利用 Xa 循环利用 磺达肝癸钠 Herbert et al. Cardiovasc Drug Rev 1997;15:1-26 van Boeckel et al. Angew Chem [Int Ed Engl] 1993;32: 1671-90 单一化学实体成份 无病菌污染危险 靶位高度选择性 一天一次 快速起效 (Cmax/2=25 min) 半衰期17小时 不经肝脏代谢，经肾脏清除 高度特异结合抗凝血酶 无药物间相互作用 没有 HIT 发生的报道 老年病人无需调整剂量 磺达肝癸钠--人工合成Xa因子抑制剂 安卓?的研发和应用历史 1982：戊糖被首次化学合成 (Toulouse, France