药品信息:
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About FASLODEX FASLODEX, a type of hormonal treatment known as an antiestrogen, is for hormone receptor-positive in postmenopausal women whose breast cancer has recurred or progressed following antiestrogen therapy, such as tamoxifen. FASLODEX is a hormonal therapy, not a cytotoxic chemotherapy.
In clinical trials, FASLODEX was found to be effective in women whose breast cancer recurred or progressed following other antiestrogen therapy such as tamoxifen. FASLODEX is given by intramuscular (IM) injection once a month.
The hormones estrogen and progesterone play an important role in the growth, development and function of the breasts. These hormones are naturally produced by organs in the body. To receive the signals from these hormones, normal healthy breast cells have estrogen receptors and progesterone receptors inside them. The hormones attach to these hormone receptors.
The breast cancer cells of many women diagnosed with breast cancer will have receptors for estrogen and/or progesterone. When they do, the breast cancer is said to be hormone receptor positive. When breast cancers are estrogen receptor positive, estrogen may contribute to the growth and spread of the cancer.
FASLODEX is a hormonal therapy that works by binding to estrogen receptors. In doing so, FASLODEX can block the effect estrogen has on the cancer cells. FASLODEX causes the estrogen receptor to change shape and not work as well. In addition, FASLODEX causes a decrease (downregulation) in the number of estrogen receptors.
【药物别名】Faslodex 【制剂规格】5、2.5ml 【药理毒理】本品是一类新的ER抑制剂-ER下调剂类乳腺癌治疗药物。由于在许多乳腺癌患者中均发现有ER,且这些肿瘤的生长受到雌激素的刺激,因此目前治疗乳腺癌的主要方法是减少雌激素的浓度。本品可与ER竞争性结合,其亲和力可与雌二醇相比。本品还可阻断ER,抑制其与雌激素的结合,并激发受体发生形态改变,降低ER浓度从而使肿瘤细胞受到损害。这种通过ER的作用与Ki67的减少有关,而后者是一种细胞增生标志物。 【药动学】静注后本品在体内进行广泛而快速的分布,稳态时表现分布容积约为3~5L/kg,并快速清除。本品单次肌注后血浆浓度约在7天后达峰值,并维持至少1个月,谷浓度约为峰浓度的1/3,半衰期约为40天。一月1次肌注本品250mg,血浆浓度约在3~6次剂量后达稳态,多次剂量后的AUC是单次剂量的2.5倍,谷浓度与单次剂量的峰浓度相当。本品与血浆蛋白结合率高达99%,主要与极低密度脂蛋白(VLDL)、低密度脂蛋白(LDL)和高密度脂蛋白(HDL)结合。本品肌注或静注后在体内进行与内源性甾体激素相似的多种途径的生物转化,包括氧化、芳香化、羟化等,在已确定的代谢物中大多数无活性或与母体活性相似,并主要从粪便中排泄,经肾清除者不到1%,主要的代谢酶为CYP3A4。 【适应证】抗雌激素疗法治疗无效、病情进展、雌激素受体(ER)呈阳性的绝经后转移性晚期乳腺癌治疗。 【不良反应】最常见的为胃肠道反应(恶心、呕吐、便秘、腹泻和腹痛),头痛、背痛、潮红和咽炎,注射部位反应多为轻微及一过性疼痛和炎症。其他报道的与剂量有关的反应还有血栓栓塞、肌痛、眩晕和白细胞减少,但发生率不到1%。另外,在治疗的头6周里,从激素治疗转为本品治疗者可能出现阴道出血。 【用法用量】肌注一月一次,每次250mg,可单次注射(1次5ml)或分2次注射(1次2.5ml),应缓慢注射。 【注意事项】 孕妇禁用。由于本品对绝经前妇女未进行研究,因此不推荐本品用于该类人群。儿童不宜使用本品。轻度肝、肾功能受损者无需调整剂量,对肝功能中、重度受损及肾功能严重受损者未进行评价。服药前应排除怀孕的可能,服药期间应采取有效的避孕措施。因本品对胎儿有毒性作用,致畸危险性属D类。本品不能用于出血素质、血小板减少或进行抗凝治疗者。目前未发现有药物相互作用,但未进行与强的CYP3A4抑制剂之间相互作用的研究。
该药属于冷藏药品(2-8摄氏度)
于2010-12-13更新 |