Cetrotide(注射用的cetrorelix acetate)是新一代促性腺荷爾蒙釋放激素(GnRH)拮抗劑，用以避免卵巢在進行輔助生育技術(ART)之前於接受刺激後提早排卵。 Cetrotide的治療可以在一個月內結束，因為這個藥物能夠發揮立即的效果。 Cetrotide的安全性相當理想。 GnRH在人體內的作用： 促性腺荷爾蒙釋放激素(GnRH)由大腦製造，可控制黃體激素(LH)的分泌，讓卵子順利成熟，從而排卵。過早排卵可能降低ART的效果，同時可能導致併發症(如卵子與胚胎品質不佳或不成熟，增加流產的可能性) Cetrotide是新一代GnRH拮抗劑，可對抗GnRH，避免垂體腺製造LH。病患使用可避免LH過早暴增導致提早排卵。 药品英文名 Cetrorelix 药品别名 醋酸西曲瑞克、Cetrotide 药物剂型 注射用醋酸西曲瑞克：0.25mg/支；3mg/支，配有注射用水作为溶剂。3mg包装，室温保存，避光，防潮，防热。0.25mg包装，2～8℃避光保存。 药理作用 本品是一种促性腺激素释放激素(GnRH)拮抗剂。GnRH与垂体细胞膜上的受体结合，刺激黄体生成素(LH)及促卵泡成熟激素(FSH)释放。本品与内源性GnRH竞争垂体细胞上的受体，从而抑制内源性LH及FSH的释放，推迟女性LH峰的出现，从而控制排卵。本品通过剂量依赖抑制脑垂体腺的黄体生成激素(LH)和卵泡刺激素(FSH)的分泌，抑制作用是直接的，并通过连续的治疗来维持，不引起黄体激素受体活性在初始时高涨随后下调。 药动学 单剂量注射本品后2h起效，每24h注射一次可以使抑制作用持续，本品血浆蛋白结合率为86%，消除半衰期为5h。 适应证 用于接受控制性促排卵辅助生殖治疗的妇女，防止过早出现LH峰及控制随后的排卵；子宫内膜异位。 禁忌证 1.对本品、外源性多肽激素及甘露醇过敏者禁用。 2.本品妊娠分类为X，对胎儿有影响，妊娠妇女禁用。3.尚无本品是否存在乳汁分泌资料，哺乳期妇女禁用。 4.严重的肝肾功能损害者禁用。 注意事项 药物用专用溶剂溶解后立即使用。 不良反应 不良反应包括过敏反应，如呼吸困难、咽喉阻塞、荨麻疹以及唇、舌、面部水肿。约3.5%的女性出现卵巢过度刺激综合征(OHSS)，表现为四肢肿大、腹部疼痛和肿大、气短、体重增加、恶心、呕吐。其他不良反应有头痛、注射部位发红、发痒或水肿。 用法用量 方案一：皮下注射，每天0.25mg，在促排卵的第5天或第6天(相当于开始促性腺素治疗后96～120h)，直至诱发排卵，注射时间可选择早上或晚上，如果选择在早上，则最后一支应在诱发排卵当天早上注射；如果选择在晚上，则最后一支应在诱发排卵前一天晚上注射。 方案二：皮下注射，在促排卵的第7天(相当于开始促性腺素治疗后132～144h)给予本品3mg，如果卵泡发育不同步，则在注射后的96h开始每天注射0.25mg直至诱发排卵。 药物相应作用 尚未发现药物相互作用。 Cetrotide Company: Asta Medica Approval Status: Approved August 2000 Treatment for: For the prevention of premature ovulation in women undergoing controlled ovarian stimulation Areas: Diabetes / Endocrinology; Pregnancy & Gynecology General Information Cetrotide has been developed to prevent premature ovulation in women undergoing controlled ovarian stimulation for assisted reproductive technologies (ART). Cetrotide blocks the effects of a natural hormone, called gonadotropin-releasing hormone (GnRH). GnRH controls the secretion of another hormone, called luteinizing hormone (LH), which induces ovulation during the menstrual cycle. During hormone treatment for ovarian stimulation, premature ovulation may lead to eggs that are not suitable for fertilization. Cetrotide blocks such undesirable premature ovulation. Clinical Results The effectiveness of Cetrotide has been examined in five clinical trials (two phase II and three phase III trials). Two dose regimens were investigated in these trials: either a single dose per treatment cycle or multiple dosing. In the phase II studies, a single dose of 3 mg was established as the minimal effective dose for the inhibition of premature LH surges with a protection period of at least four days. When Cetrotide is administered in a multidose regimen, 0.25 mg was established as the minimal effective dose. The extent and duration of LH-suppression was found to be dose dependent. In the phase III program, efficacy of the single 3 mg dose regimen and the multiple 0.25 mg dose regimen was established separately in two controlled studies utilizing active comparitors. A third non-comparative study evaluated only the multiple 0.25 mg dose regimen of Cetrotide. In the five phase II and phase III trials, 184 pregnancies have been reported out of a total of 732 patients (including 21 pregnancies following the replacement of frozen-thawed embryos). No drug related allergic reactions were reported from these clinical studies. (from FDA Label) Side Effects Adverse effects associated with Cetrotide include (but are not limited to) the following: Reddening, itching, or swelling at injection site Nausea Headache Additionally, Cetrotide should not be used by individuals who are or may be pregnant. Mechanism of Action GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrotide competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. The onset of LH suppression is approximately one hour with the 3 mg dose and two hours with the 0.25mg dose. This suppression is maintained by continuous treatment and there is a more pronounced effect on LH than on FSH. An initial release of endogenous gonadotropins has not been detected with Cetrotide, which is consistent with an antagonist effect. (from FDA Label) Additional Information For further information on Cetrotide, please visit the web site of Asta Medica --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: CETROTIDE EQ 0.25MG BASE/ML Injection Kit 原产地英文药品名: CETRORELIX 中文参考商品译名: 思哲凯EQ 0.25毫克/ML注射試劑盒 中文参考药品译名: 西曲瑞克 生产厂家中文参考译名: EMD SERONO 生产厂家英文名: EMD SERONO