部分中文亮丙瑞林处方资料（仅供参考）

FDA批准半年一次的Lupron Depot新剂型用于前列腺癌

Abbott公司表示美国FDA近日批准了公司的一种45mg规格、6个月一次的Lupron Depot (醋酸亮丙瑞林贮库型混悬剂)作为晚期前列腺癌的姑息治疗.

本品采用aleraPharmaceuticals公司的Hydron植入剂制备技术制成，可持续12个月释放合成的非肽类促黄体生成激素释放激素（LHRH）激动药组胺瑞林。LHRH激动药已成为局部治疗晚期和转移性前列腺癌的新药。

分类名称

一级分类：妇产科用药 二级分类：促性腺激素 三级分类：

药品英文名

Leuprorelin

药品别名

醋酸亮丙瑞林、亮脯瑞林、酰基辅氨酸、抑那通、利普安、Enantone、Leuprolide、LeuprorelinAcetate、Leuprorelinum

药物剂型

注射剂：1mg，3.75mg。

药理作用

本药是下丘脑产生的促性腺激素释放激素激动剂(GnRH-a)，是由9个氨基酸构成的肽类，能与垂体内的特异性受体结合，降低垂体反应性，从而抑制性腺系统。亮丙瑞林促进黄体生成素(LH)释放的活性约为GnRH的20倍，对垂体-性腺功能的抑制作用也较GnRH强。应用亮丙瑞林初期会出现短暂的尿促卵泡素(FSH)、黄体生成素(LH)、雌激素或雄激素升高的现象，随之由于垂体的反应性降低，FSH、LH和雌激素或雄激素的分泌受到抑制(选择性药物垂体切除和药物性卵巢或睾丸去势作用)，从而对性激素依赖性疾病如前列腺癌、子宫内膜异位症等起到治疗作用。本品属于戈那瑞林同类物，而且具有类似的作用。持续给药时，对前列腺癌、性早熟子宫内膜异位和子宫平滑肌瘤可起到抑制性激素的作用，而在短暂给药时，则可使男性的睾酮和二氢睾酮以及绝经后女性雌酮和雌二醇短暂增加。

药动学

本药醋酸盐口服无效，皮下或肌内注射吸收好。一次皮下注射醋酸亮丙瑞林3.75mg，1～2天达血药浓度峰值。用于子宫内膜异位症时，皮下注射醋酸亮丙瑞林3.75mg，每4周给药1次，共给药6次，血中原形药物的血药浓度约为0.2ng/ml。用于前列腺癌时，皮下给予醋酸亮丙瑞林3.75mg，每4周1次，共3次，血中稳态药物浓度在0.2～1.0ng/ml范围。醋酸亮丙瑞林在体内遇水分解，产生4种降解产物，通过泌尿系统排泄。皮下注射一次亮丙瑞林，28天后原形药物及代谢物的尿累积排泄率分别为2.9%和1.5%。

适应证

1.晚期前列腺癌。
2.绝经前乳腺癌，用于术后辅助治疗或复发、晚期患者，其效果与卵巢切除相似。
3.子宫内膜异位及子宫肌瘤。
4.治疗中枢性性早熟和其他与性激素有关的疾病，还可试用于某些胃肠道疾病如肠易激综合征。

禁忌证

1.对本药成分LH-RH及其衍生物有过敏史者。
2.有性质不明的阴道出血者。
3.孕妇及哺乳期妇女。

注意事项

1.慎用：
(1)伴有或可能发展为脊髓压迫、输尿管梗阻的前列腺癌患者；(2)充血性心力衰竭或有心血管病史者；
(3)需要限制钠盐摄入者；
(4)有血栓栓塞者；
(5)有骨质疏松史者；
(6)高龄患者。
2.用药初期由于高活性的LH-RH衍生物对垂体-性腺系统的刺激作用，使血中睾酮水平一过性增高，可使前列腺癌患者骨转移灶疼痛加剧，排尿困难或有脊髓压迫。故开始用药时应密切观察，出现症状时采取适当的措施。3.给药的第1周，应当住院并少活动。
4.可能出现反应能力改变，用药患者应避免上街或操作机械。

不良反应

1.内分泌系统：发热、热感，有时出现颜面潮红、发汗、性欲减退、阳痿、女性化乳房、睾丸萎缩、会阴部不适感。
2.肝脏毒性：LDH上升，有时AST、ALT、γ-GT、ALP上升。用药期间需密切观察。
3.肌肉骨骼系统：有时出现骨疼痛，肩、腰、四肢疼痛，步行困难等。4.泌尿系统：尿潴留、尿频、血尿。
5.循环系统：心电图异常、心胸比例增大等。
6.消化道反应：恶心、呕吐、食欲缺乏等。
7.过敏反应：皮疹、瘙痒等。
8.局部刺激：注射局部可出现硬结、疼痛、发红。
9.其他：有时出现水肿、胸部压迫感、发冷、疲倦、耳鸣、听力减退、头部多毛、三酰甘油上升、尿酸升高、BUN升高等。动物实验发现，长期注射本品致大白鼠垂体良性腺肿。

用法用量

1.治疗晚期前列腺癌，常每天1次皮下注射1mg。也可皮下注射储存制剂，在英国，每月皮下或肌内注射1次3.75mg，或每3个月皮下注射1次11.25mg。在美国，肌内注射此种储存制剂，每月给予7.5mg，或每3个月22.5mg，每4个月30mg。先给予几天的抗雄激素(如环丙孕酮)，然后开始使用本品至少连用3周，以避免疾病突发的危险。2.治疗子宫内膜异位症和子宫平滑肌瘤，每月可皮下或肌内注射1次储存制剂3.75mg，或每3个月肌内注射1次11.25mg，治疗应在月经周期头5天内开始，针对子宫内膜异位症可持续用药6个月，由于子宫平滑肌瘤持续伴有贫血，应同时补铁3个月。用于子宫手术，可于手术前5～6周1次肌内注射储存制剂3.75mg。3.治疗中枢性性早熟，每4周根据体重肌内注射1次储存制剂0.3mg/kg，然后根据效应调整。

药物相应作用

乙醇可加重本药的不良反应。

专家点评

研究证明注射亮丙瑞林3周后血中睾酮可降低至睾丸切除的水平(1.0ng/ml以下)，用药初期由于高活性LH-RH衍生物对垂体-性腺系统的刺激作用，使血中睾酮水平一过性增高，可使前列腺癌患者骨转移灶疼痛加剧，排尿困难或有脊髓压迫。故开始用药时应密切观察，出现症状时采取适当措施。

It’s not just cramps. Sometimes the pain is unbearable. It’s time to fight back and learn how Lupron Depot can help relieve your endometriosis pain. This site will provide you with information about endometriosis and treatment with Lupron Depot + Add-back*.

LUPRON DEPOT® (leuprolide acetate for depot suspension) 3.75 mg and – 3 Month 11.25 mg is used for the management of endometriosis, including pain relief and reduction of endometriotic lesions. LUPRON DEPOT with daily norethindrone acetate 5 mg is also indicated for initial management of endometriosis and for management of recurrence of symptoms. The recommended initial treatment is no more than 6 months. Repeat treatment for endometriosis should be limited to 6 months.

You should not receive LUPRON DEPOT if you are or may become pregnant, are breast-feeding or have undiagnosed vaginal bleeding. Increased endometriosis symptoms (i.e. pelvic pain or pressure and/or pain during intercourse) may occur for 1 or 2 weeks after starting this drug. Development or worsening of depression has occurred. Condoms, a diaphragm with contraceptive jelly, or an IUD is required to prevent pregnancy. Thinning of the bones, which may not be completely reversible, can occur during treatment with this drug. Norethindrone acetate used as add-back therapy with LUPRON DEPOT has additional serious risks and considerations.

Please see additional Important Safety Information you should know about Lupron Depot and discuss it with your doctor.

Please see the full Prescribing Information for Lupron Depot and discuss it with your doctor.

*Norethindrone acetate 5 mg daily

Important Safety Information and Use You Should Know About Lupron Depot®(leuprolide acetate for depot suspension)For prescription use only.

Important Safety Information

Do not take LUPRON DEPOT if you are or may become pregnant, are breast feeding, have undiagnosed vaginal bleeding, or if you have experienced any type of allergic reaction to LUPRON DEPOT, or similar drugs.

LUPRON DEPOT given with norethindrone acetate may lower your HDL-cholesterol level (the “good” cholesterol). You should not take norethindrone acetate with LUPRON DEPOT if you currently have or have previously had any clotting disorder, heart disease, stroke, liver disease or breast cancer.

Tell your health care provider before beginning treatment with norethindrone acetate if you currently have or have previously had high cholesterol, migraines, epilepsy, depression, or smoke.

During treatment with LUPRON DEPOT and norethindrone acetate, immediately tell your doctor if you have a sudden loss of vision, double vision, or if migraine headaches occur. You should notify your doctor if you experience fluid retention, epilepsy, asthma or worsening of asthmatic symptoms, heart or kidney problems.

Thinning of the bones may occur during therapy with LUPRON DEPOT alone, which may not be completely reversible in some patients. Since some conditions may increase the possibility of bone thinning, you should tell your doctor if you smoke, use alcohol in excess, have a family history of osteoporosis (thinning of the bones with fractures), or are taking other medications that can cause thinning of the bones. You should be aware that repeat treatment with LUPRON DEPOT alone is not advisable if you have these conditions.

After beginning LUPRON DEPOT, your estrogen levels will increase for 1 or 2 weeks. During this time, you may notice an increase in your current symptoms. You should notify your doctor if you develop any new or worsened symptoms after beginning LUPRON DEPOT treatment.

LUPRON DEPOT is not a method of birth control. Even though you may not have periods, unprotected intercourse could result in pregnancy. You should use non-hormonal birth control such as condoms, a diaphragm with contraceptive jelly, or an IUD to prevent pregnancy. If you think you have become pregnant while on LUPRON DEPOT, talk to your doctor immediately.

There is a possibility of the development or worsening of depression and/or the occurrence of forgetfulness.

Patients who have a history of depression should be carefully observed during treatment.

The most common side effects of LUPRON DEPOT include hot flashes, vaginal dryness, headaches, changes in mood, decreased interest in sex, depression and/or the occurrence of forgetfulness.

LUPRON DEPOT must be administered in your doctor’s office.

This is the most important information to know about LUPRON DEPOT. For more information, talk with your health care provider.

Use

LUPRON DEPOT® (leuprolide acetate for depot suspension) 3.75 mg and –3 Month 11.25 mg is used for the management of endometriosis, including pain relief and reduction of endometriotic lesions. LUPRON DEPOT with daily norethindrone acetate 5 mg is also indicated for initial management of endometriosis and for management of recurrence of symptoms. The recommended initial treatment is no more than 6 months. Repeat treatment for endometriosis should be limited to 6 months.

Reference: LUPRON DEPOT 3.75 mg and –3 Month 11.25 mg [package insert]. North Chicago, IL: Abbott Laboratories.

Please see the full Prescribing Information for Lupron Depot and discuss it with your doctor.

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产地国家: 美国

所属类别: 抗癌药物->治疗乳腺癌药物

处方药:处方药

包装规格: 45毫克/套

计价单位: 套

原产地英文商品名:

LUPRON DEPOT 45MG/KIT

原产地英文药品名:

LEUPROLIDE ACETATE

中文参考商品译名:

LUPRON DEPOT 45毫克/套

中文参考药品译名:

醋酸亮丙瑞林

原产地国家批准上市年份:

1995/12/22