英文药名: Casodex (Bicalutamide Tablets)

中文药名: 康士得(比卡鲁胺片)

生产品牌药厂家: AstraZeneca

药品名称和成分

通用名：比鲁卡胺片
商品名：康士得/Casodex
英文名：Bicalutamide tablet
康士得（比卡鲁胺片）是一种非类固醇的雄激素拮抗剂，与雄激素竟争雄激素受体，阻滞细胞对雄激素的摄取，抑制雄激素与靶器官的结合，本品与雄激素受体结合后形成受体复合物，并进入细胞核内，与核蛋白结合，从而抑制肿瘤细胞生长；可作为晚期前列腺癌姑息治疗的一线用药。
＊晚期前列腺癌姑息性治疗的一线用药；
＊全球销售量最大的抗雄激素类药物；
＊外科去势术后显示强大的药理优势；
＊耐受性好、副作用小、生物利用度高；
制造商 ：阿斯利康
【药理作用】 ：本药属于非甾体类抗雄激素药物，没有其它激素的作用，它与雄激素受体结合而使其无有效的基因表达，从而抑制了雄激素的刺激，导致前列腺肿瘤的萎缩。本药是消旋物，其抗雄激素作用仅仅出现在(R)-结构对应体上。
【药代动力学 】：本药经口服吸收良好。没有证据表明食物对其生物利用度存在任何临床相关的影响。(S)-异构体相对(R)-异构体消除较为迅速，后者的血浆半衰期为1周。在本药的每日用量下，R)-异构体因其半衰期长，在血浆中蓄积了约10倍，因此非常适合每日1次的日服。本药与血浆蛋白高度结合(96%)，并被广泛代谢(经氧化及葡萄糖醛酸化)，其代谢产物以几乎相同的比例经肾及胆消除。
【适应症 】：与黄体生成素释放激素（LHRH）类似物或外科睾丸切除术联合应用于晚期前列腺癌的治疗。
【用法用量 】
成人：成人男性包括老年人：一片（50 mg），每日1次，用本品治疗应与LHRH类似物或外科睾丸切除术治疗同时开始。
儿童：本品禁用于儿童
肾损害：对于肾损害的病人无需调整剂量。
肝损害：对于轻度肝损害的病人无需调整剂量，中重度肝操作的病人可能发生药物蓄积。
【不良反应】：面色潮红，瘙痒，乳房触痛和男性乳房女性化，腹泻、恶心、呕吐，乏力。暂时性肝功改变（转氨酶升高，黄疸）。本药与LHRH类似物联用，进行临床研究期间还观察到下列副作用(可能与药物相关且发生率大于1%)，这些副作用与药物的使用没有因果关系，有些是老年人日常固有的
心血管系统 ：心力衰竭。消化系统 ：厌食、口干、消化不良、便秘、腹痛、胃肠胀气。中枢神经系统 ：头晕、失眠、嗜睡、性欲减低。呼吸系统 ：呼吸困难。泌尿生殖系统 ：阳痿、夜尿增多。
血液系统 ：贫血。皮肤 ：脱发、皮疹、出汗、多毛。代谢及营养 ：糖尿病、高血糖、周围性水肿、体重增加或减轻。其他 ：胸痛、头痛、骨盆痛、寒战。
【禁忌症】 对本药过敏者，以及妇女、儿童。
【注意事项】 中、重度肝损伤病人可能发生药物蓄积，因此应慎用。
【药物相互作用】： 本药与黄体生成素释放激素（LHRH）类似物之间无任何药效学或药代动力学方面的相互作用。与常见的处方药合用未出现相互作用。在每天剂量高达150 mg时未发现酶诱导作用。体外研究表明，本药可以与双香豆素类抗凝剂，如华法令竞争其血浆蛋白结合点，因此建议在已经接受双香豆素类抗凝剂治疗的病人，如果开始服用本药，应密切监测凝血酶原时间。
药物过量： 没有人类过量的经验，没有特效的解药，应该对症治疗。透析可能无效，因为本药与血浆蛋白高度结合，且在尿液中以非原形排泄。但一般的支持疗法是需要的，这包括生命体征的密切监测。
新研究提示，放疗后每日比卡鲁胺(康士得，Casodex)治疗似乎可改善局部晚期前列腺癌男性的生存。然而，这种生存益处似乎与内科去雄疗法加入放疗的结果类似。
根据这些发现，作者相信抗雄激素药比卡鲁胺可能是去雄疗法的一种合适的、较好耐受的替代；去雄疗法对生活质量有不利影响。如同在8月的《癌症研究和临床肿瘤学杂志》（J Cancer Res Clin Oncol 2006;132:S7-S16.）上所报告的，美国Milwaukee医学院的William A. See博士及其同事评估了在放疗后被随机分配接受比卡鲁胺(150 mg)或安慰剂每日1次的1370例早期前列腺癌(T1-4, N any, M0)患者的生存结果。中位随访期为7.2年。
报告指出，比卡鲁胺治疗与无进展和总生存显著改善相关。与单用放疗比较，加用比卡鲁胺使客观进展风险降低44%。同样，这种药物治疗使总死亡风险降低35%。进一步分析显示，比卡鲁胺引起的总生存改善主要是由于其降低前列腺癌相关死亡的作用。与局部晚期疾病患者不同，有局灶性疾病的患者未从放疗加比卡鲁胺治疗中受益。
作者指出，这是非去雄疗法用于这类患者的总生存益处的首个证据。与去雄疗法比较，比卡鲁胺在维持性欲、体能和骨矿密度方面提供附加的生活质量益处。
【贮藏/有效期】 小心贮存30°C以下。五年。

【原产地英文商品名】CASODEX-50mg/Tablet 100Tablets
【原产地英文药品名】BICALUTAMIDE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·康士得-50毫克/片 100片/瓶
·康士得-50毫克/片 30片/瓶
【中文参考药品译名】比卡鲁胺
【生产厂家中文参考译名】阿斯利康
【生产厂家英文名】astrazeneca

Casodex is indicated for the treatment of prostate cancer in combination with LHRH analogue therapy or surgical castration.

What is Casodex?
Casodex is an anti-androgen. It works in the body by preventing the actions of androgens (male hormones).
Casodex is used together with another hormone to treat prostate cancer.
Casodex may also be used for purposes other than those listed in this medication guide.

Important information about Casodex.
Before taking Casodex, tell your doctor if you have liver disease, diabetes, or any other serious illness. Casodex is given as part of a combination prostate cancer treatment with another medication that prevents the testicles from producing testosterone. You should not start taking this medication until you have received the other medication prescribed as part of your treatment.
Your doctor may occasionally change your Casodex dose to make sure you get the best results from this medication. Do not stop taking Casodex without your doctor's advice. If you stop your treatment suddenly, your condition may become worse.
To be sure Casodex is helping your condition and is not causing harmful effects, your prostate and liver function will need to be checked with blood tests on a regular basis. Do not miss any scheduled appointments.
Call your doctor at once if you have a serious side effect such as chest pain, shortness of breath, swelling, blood in your urine, or stomach pain with loss of appetite, dark urine, and yellowing of your skin or eyes.
Casodex should never be taken by a woman or a child. Although Casodex is not for use by women, this medication can cause birth defects if a woman is exposed to it during pregnancy.

How should I take Casodex?
Take Casodex exactly as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended. Follow the directions on your prescription label.
Casodex is given as part of a combination prostate cancer treatment with another medication called a luteinizing (LOO-tee-in-ize-ing) hormone-releasing hormone, or LHRH. This medication prevents the testicles from producing testosterone.
Casodex is usually taken once per day in the morning or evening. You may take the medicine with or without food. Try to take the medication at the same time each day.
LHRH is given as an injection or a tiny implant injected through a needle under the skin around your navel. LHRH injections are given at intervals such as once every 4 weeks. Follow your doctor's instructions.
You should not start taking Casodex until you have received the LHRH injection prescribed as part of your treatment.
Your doctor may occasionally change your Casodex dose to make sure you get the best results from this medication. Do not stop taking this medication without your doctor's advice. If you stop your treatment suddenly, your condition may become worse.
To be sure this medication is helping your condition and is not causing harmful effects, your prostate and liver function will need to be checked with blood tests on a regular basis. Do not miss any scheduled appointments.
Store this medication at room temperature away from moisture and heat.

Casodex side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives;
difficulty breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have a serious side effect such as:

• chest pain, cough or trouble breathing;
• feeling short of breath, even with mild exertion;
• swelling in your hands or feet;
• fever, chills, body aches, flu symptoms;
• pale skin, easy bruising or bleeding;
• blood in your urine; or
• nausea, stomach pain, loss of appetite, itching, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Less serious Casodex side effects may include:

• hot flashes;
• breast pain or swelling;
• weakness, dizziness;
• back pain, pelvic pain, joint or muscle pain;
• increased nighttime urination;
• upset stomach, vomiting, diarrhea or constipation;
• weight changes;
• impotence, loss of interest in sex, or trouble having an orgasm;
• dizziness, headache; or
• sore throat, runny nose or other cold symptoms.

What other drugs will affect Casodex?
Before taking Casodex, tell your doctor if you are taking a blood thinner such as warfarin (Coumadin).
There may be other medicines that can interact with Casodex. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.