产地国家：英国

处方药：是

所属类别： 150毫克/片 28片/盒

包装规格： 150毫克/片 28片/盒

计价单位：盒

生产厂家英文名：AstraZeneca

原产地英文商品名：Casodex Tab 150mg/tab 28tabs/box

原产地英文药品名：Bicalutamide

中文参考商品译名：康士得薄膜片 150毫克/片 28片/盒

中文参考药品译名：比卡鲁胺

简介：

部份中文比卡鲁胺处方资料（仅供参参考）

英文药名: Casodex (Bicalutamide Tablets)

中文药名: 康士得(比卡鲁胺片)

生产厂家: AstraZeneca

药品英文名：Bicalutamide

药品别名：比卡鲁胺片

药物剂型：50mg。

贮法：低于30℃保存。

药理作用：本药属非甾体类抗雄激素药物，无其他激素的作用。通过与雄激素受体结合，使其无有效的基因表达，从而抑制雄激素的刺激，导致前列腺肿瘤萎缩。本药是消旋物，其抗雄激素作用仅出现在(R)-结构对应体上。药动学本药口服吸收良好，尚无证据表明食物对其生物利用度存在任何临床相关的影响。每天口服本药50mg，(R)-异构体的稳态血药浓度约为9μg/ml，稳态时有效(R)-异构体占循环内总药量的99%。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清除。(R)-异构体较(S)-异构体消除缓慢，其血浆半衰期为1周。在本药的每天用量下，(R)-异构体因其半衰期长，可在血浆中蓄积约10倍，因此适于一天服用1次。(R)-异构体的药代动力学不受年龄、肾功能损害或轻、中度肝功能损害的影响，但有证据表明在严重肝功能损害病例中，(R)-异构体血浆清除较慢。

适应证：1.与促性腺激素释放激素(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。2.国外尚用于多毛症(Hirsutism)的治疗。

禁忌证：(1)对本药过敏者。(2)妇女。(3)儿童。

注意事项：1.慎用 (1)中、重度肝功能损害者(因本药在肝脏广泛代谢，严重肝功能损害者药物清除减慢，可能发生药物蓄积)。(2)有氟他胺或尼鲁米特过敏史或严重不良反应病史的患者。2.药物对妊娠的影响 孕妇禁用。美国药品和食品管理局(FDA)对本药的妊娠安全性分级为X级。3.药物对哺乳的影响 本药是否经乳汁排泄尚不清楚，但本药禁用于女性，更不能用于哺乳妇女。4.用药前后及用药时应当检查或监测 用药期间应定期进行肝功能检查。(1)用药后如出现严重肝功能损害，应停止治疗。(2)本药对患者驾驶及操作机器的能力无影响。(3)尚无人类用药过量的经验。本药无特效解救药，用药过量时应对症和支持治疗(包括密切监测生命体征)。透析可能无效(因本药与血浆蛋白高度结合，且在尿液中以非原形排泄)。

不良反应：1.通常患者对本药的耐受性良好，少有因不良反应而停药的情况。2.由于本药的药理作用特点，可引起面色潮红、瘙痒、乳房触痛和男性乳房女性化等，这些反应可随睾丸切除而减轻。也可引起腹泻、恶心、呕吐、乏力和皮肤干燥。3.临床试验中观察到可致肝功能改变(如氨基转移酶升高、黄疸)，但少见严重变化，极少见肝功能衰竭。一般在治疗的最初6个月内出现，通常较短暂，继续治疗或随即终止治疗均可逐渐消退或改善。4.本药与LHRH类似物合用的临床研究中还观察到下列不良反应(临床试验者认为可能与药物相关且发生率大于1%)：(1)心血管系统：心力衰竭。(2)胃肠道：畏食、口干、消化不良、便秘、腹痛及胃肠胀气。(3)中枢神经系统：头晕、头痛、失眠、嗜睡。(4)呼吸系统：呼吸困难。(5)泌尿生殖系统：阳痿、性欲减低、夜尿增多。(6)血液：贫血。(7)代谢/内分泌系统：糖尿病、高血糖、周围性水肿、体重增加或减轻。(8)皮肤：脱发、皮疹、出汗、多毛。(9)其他：胸痛、骨盆痛、寒战。

用法用量：成人口服给药：成年男性(包括老年人)：一次50mg，一天1次。用本药治疗应与LHRH类似物或外科睾丸切除术治疗同时开始。1.肾功能不全时剂量：肾功能损害者无需调整剂量。2.肝功能不全剂量：轻度肝功能损害者无需调整剂量；中、重度肝功能损害者可能发生药物蓄积。

药物相应作用：1.本药与抑制药物氧化的其他药物(如西咪替丁和酮康唑)同用时应谨慎。理论上，两者合用可引起本药血药浓度增加，不良反应增加。2.本药与环孢素和钙通道阻滞药联合应用时应谨慎，尤其是出现药效增加或药物不良反应迹象时，可能需要减少这些药物的剂量。合用环孢素时，建议在本药治疗开始或结束后密切监测血药浓度和临床状况。3.本药能抑制细胞色素P450 CYP 3A4的活性，因此与主要由CYP 3A4代谢的药物联合应用时应谨慎。4.体外研究表明，本药可与香豆素类抗凝药(如华法林、双香豆素、苯丙香豆素等)竞争血浆蛋白结合点，两者合用可能增加出血的危险，应密切监测凝血酶原时间。5.本药不可与特非那定、阿司咪唑或西沙必利联合使用。6.本药与LHRH类似物之间无任何药效学或药动学方面的相互作用

英文版说明书：

CasodexPronunciationGeneric Name: bicalutamide (bye ka LOO ta mide)Brand Names: Casodex What is Casodex?Casodex (bicalutamide) 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 not listed in this medication guide.Important informationCasodex is used to treat prostate cancer. This medicine should never be taken by a woman or a child.Casodex can harm your liver. Call your doctor at once if you have nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).Before taking this medicineYou should not use Casodex if you are allergic to bicalutamide.Casodex should never be taken by a woman or a child.Although Casodex is not for use by women, this medicine can cause birth defects if a woman is exposed to it during pregnancy.To make sure Casodex is safe for you, tell your doctor if you have:•liver disease;•diabetes; or•if you also take a blood thinner (warfarin, Coumadin, Jantoven).How should I take Casodex?Take Casodex exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.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.Casodex is given as part of a combination prostate cancer treatment with another medicine called a luteinizing (LOO-tee-in-ize-ing) hormone-releasing hormone, or LHRH. These medicines prevent the testicles from producing testosterone.Treatment with Casodex and LHRH is usually started at the same time. Follow your doctor's instructions.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 stop using Casodex suddenly. Stopping suddenly may make your condition worse.While using Casodex, you may need frequent blood tests at your doctor's office.Store at room temperature away from moisture and heat.Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.Casodex dosing informationUsual Adult Dose for Prostate Cancer:50 mg orally once a day, given at the same time each day.What happens if I miss a dose?Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.Call your doctor for instructions if you miss an appointment for your LHRH injection.What happens if I overdose?Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.What should I avoid while taking Casodex?Casodex may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.Bicalutamide can pass into body fluids (including urine, feces, vomit, semen, vaginal fluid). Patients and caregivers should wear rubber gloves while cleaning up body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.Body fluids should not be handled by a woman who is pregnant or who may become pregnant. Use condoms during sexual activity to avoid exposure to body fluids.Casodex side effectsGet emergency medical help if you have any of these signs of an allergic reaction to Casodex: hives; difficult breathing; swelling of your face, lips, tongue, or throat.Call your doctor at once if you have:•breast pain or swelling;•blood in your urine;•fever, chills;•sudden chest pain or discomfort, wheezing, dry cough, feeling short of breath;•low red blood cells (anemia) - pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;•liver problems - nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or•high blood sugar - increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss.Common Casodex side effects may include:•hot flashes;•pain in your back, pelvis, or stomach;•swelling in your hands, ankles, or feet;•increased night-time urination;•weakness, dizziness; or•nausea, diarrhea, constipation.This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.See also: Side effects (in more detail)What other drugs will affect Casodex?Other drugs may interact with bicalutamide, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.