英文药名: Casodex(Bicalutamide Filmcoated Tablets) 中文药名: 康士得(比卡鲁胺片) 生产厂家: 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 【治疗分类】内分泌治疗 【主要成份】比卡鲁胺 生产厂家: AstraZeneca(阿斯利康) 适应症 与促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。 用量用法 成人： 成年男性包括老年人：一片（50mg），一天一次，用康士得治疗应与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，中重度肝损伤的病人可能发生药物蓄积（见注意事项）。 如果您有任何疑问，请遵医嘱。 Casodex 50 mg Film-coated Tablets 1. Name of the medicinal product Casodex 50 mg Film-coated Tablets 2. Qualitative and quantitative composition Each tablet contains 50 mg bicalutamide (INN) Excipient(s) with known effect: Each tablet contains 61 mg lactose monohydrate. For the full list of excipients, see section 6.1. 3. Pharmaceutical form White film-coated tablet. 4. Clinical particulars 4.1 Therapeutic indications Treatment of advanced prostate cancer in combination with LHRH analogue therapy or surgical castration. 4.2 Posology and method of administration Posology Adult males including older people: one tablet (50 mg) once a day. Treatment with Casodex should be started at least 3 days before commencing treatment with an LHRH analogue, or at the same time as surgical castration. Renal impairment: no dosage adjustment is necessary for patients with renal impairment. Hepatic impairment: no dosage adjustment is necessary for patients with mild hepatic impairment. Increased accumulation may occur in patients with moderate to severe hepatic impairment (see section 4.4). Paediatric population: Casodex is contraindicated for use in children. 4.3 Contraindications Casodex is contraindicated in females and children (see section 4.6). Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. Co-administration of terfenadine, astemizole or cisapride with Casodex is contraindicated (see section 4.5). 4.4 Special warnings and precautions for use Initiation of treatment should be under the direct supervision of a specialist.Casodex is extensively metabolised in the liver. Data suggests that its elimination may be slower in subjects with severe hepatic impairment and this could lead to increased accumulation of Casodex. Therefore, Casodex should be used with caution in patients with moderate to severe hepatic impairment. Periodic liver function testing should be considered due to the possibility of hepatic changes. The majority of changes are expected to occur within the first 6 months of Casodex therapy. Severe hepatic changes and hepatic failure have been observed rarely with Casodex, and fatal outcomes have been reported (see section 4.8). Casodex therapy should be discontinued if changes are severe. A reduction in glucose tolerance has been observed in males receiving LHRH agonists. This may manifest as diabetes or loss of glycaemic control in those with pre-existing diabetes. Consideration should therefore be given to monitoring blood glucose in patients receiving Casodex in combination with LHRH agonists. Casodex has been shown to inhibit cytochrome P450 (CYP3A4), as such caution should be exercised when co-administered with drugs metabolised predominantly by CYP3A4 (see sections 4.3 and 4.5). Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. Androgen deprivation therapy may prolong the QT interval. In patients with a history of or risk factors for QT prolongation and in patients receiving concomitant medicinal products that might prolong the QT interval (see section 4.5) physicians should assess the benefit risk ratio including the potential for Torsade de pointes prior to initiating Casodex. 4.5 Interaction with other medicinal products and other forms of interaction There is no evidence of any pharmacodynamic or pharmacokinetic interactions between Casodex and LHRH analogues. In vitro studies have shown that R-bicalutamide is an inhibitor of CYP 3A4, with lesser inhibitory effects on CYP 2C9, 2C19 and 2D6 activity. Although clinical studies using antipyrine as a marker of cytochrome P450 (CYP) activity showed no evidence of a drug interaction potential with Casodex, mean midazolam exposure (AUC) was increased by up to 80%, after co-administration of Casodex for 28 days. For drugs with a narrow therapeutic index such an increase could be of relevance. As such, concomitant use of terfenadine, astemizole and cisapride is contraindicated (see section 4.3) and caution should be exercised with the co-administration of Casodex with compounds such as ciclosporin and calcium channel blockers. Dosage reduction may be required for these drugs particularly if there is evidence of enhanced or adverse drug effect. For ciclosporin, it is recommended that plasma concentrations and clinical condition are closely monitored following initiation or cessation of Casodex therapy. Caution should be exercised when prescribing Casodex with other drugs which may inhibit drug oxidation e.g. cimetidine and ketoconazole. In theory, this could result in increased plasma concentrations of Casodex which theoretically could lead to an increase in side effects. In vitro studies have shown that Casodex can displace the coumarin anticoagulant, warfarin, from its protein binding sites. It is therefore recommended that if Casodex is started in patients who are already receiving coumarin anticoagulants, prothrombin time should be closely monitored. Since androgen deprivation treatment may prolong the QT interval, the concomitant use of Casodex with medicinal products known to prolong the QT interval or medicinal products able to induce Torsade de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, moxifloxacin, antipsychotics, etc. should be carefully evaluated (see section 4.4). Paediatric population Interaction studies have only been performed in adults. 4.6 Fertility, pregnancy and lactation Casodex is contraindicated in females and must not be given to pregnant women or nursing mothers. 4.7 Effects on ability to drive and use machines Casodex is unlikely to impair the ability of patients to drive or operate machinery. However, it should be noted that occasionally somnolence may occur. Any affected patients should exercise caution. 4.8 Undesirable effects In this section, undesirable effects are defined as follows: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to ≤1/100); rare (≥1/10,000 to ≤1/1,000); very rare (≤1/10,000); not known (cannot be estimated from the available data). Table 1 Frequency of Adverse Reactions System Organ Class Frequency Event Blood and lymphatic system disorders Very common Anaemia Immune system disorders Uncommon Hypersensitivity, angioedema and urticaria Metabolism and nutrition disorders Common Decreased appetite Psychiatric disorders Common Decreased libido depression Nervous system disorders Very common Dizziness   Common Somnolence Cardiac disorders Common Myocardial infarction (fatal outcomes have been reported)4, Cardiac failure4   Not known QT prolongation (see sections 4.4 and 4.5). Vascular disorders Very common Hot flush Respiratory, thoracic and mediastinal disorders Uncommon Interstitial lung disease5 (fatal outcomes have been reported). Gastrointestinal disorders Very common Abdominal pain constipation nausea   Common Dyspepsia flatulence Hepatobiliary disorders Common Hepatotoxicity, jaundice, hypertransaminasaemia1   Rare Hepatic failure2 (fatal outcomes have been reported). Skin and subcutaneous tissue disorders Common Alopecia hirsutism/hair re-growth dry skin pruritus rash   Rare Photosensitivity reaction Renal and urinary disorders Very common Haematuria Reproductive system and breast disorders Very common Gynaecomastia and breast tenderness3   Common Erectile dysfunction General disorders and administration site conditions Very common Asthenia oedema   Common Chest pain Investigations Common Weight increased 1. Hepatic changes are rarely severe and were frequently transient, resolving or improving with continued therapy or following cessation of therapy. 2. Listed as an adverse drug reaction following review of post-marketed data. Frequency has been determined from the incidence of reported adverse events of hepatic failure in patients receiving treatment in the open-label Casodex arm of the 150 mg EPC studies. 3. May be reduced by concomitant castration. 4. Observed in a pharmaco-epidemiology study of LHRH agonists and anti-androgens used in the treatment of prostate cancer. The risk appeared to be increased when Casodex 50 mg was used in combination with LHRH agonists, but no increase in risk was evident when Casodex 150 mg was used as a monotherapy to treat prostate cancer. 5. Listed as an adverse drug reaction following review of post-marketed data. Frequency has been determined from the incidence of reported adverse events of interstitial pneumonia in the randomised treatment period of the 150 mg EPC studies. Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme.Website: www.mhra.gov.uk/yellowcard. 4.9 Overdose There is no human experience of overdosage. There is no specific antidote; treatment should be symptomatic. Dialysis may not be helpful, since Casodex is highly protein bound and is not recovered unchanged in the urine. General supportive care, including frequent monitoring of vital signs, is indicated. 5. Pharmacological properties 5.1 Pharmacodynamic properties Pharmacotherapeutic group: Anti-androgens, ATC code L02BB03 Casodex is a non-steroidal antiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition. Clinically, discontinuation of Casodex can result in antiandrogen withdrawal syndrome in a subset of patients. Casodex is a racemate with its antiandrogenic activity being almost exclusively in the (R)-enantiomer. 5.2 Pharmacokinetic properties Absorption Casodex is well absorbed following oral administration. There is no evidence of any clinically relevant effect of food on bioavailability. Distribution Casodex is highly protein bound (racemate 96% (R)-enantiomer >99%) and extensively metabolised (via oxidation and glucuronidation): Its metabolites are eliminated via the kidneys and bile in approximately equal proportions. Biotranformation The (S)-enantiomer is rapidly cleared relative to the (R)-enantiomer, the latter having a plasma elimination half-life of about 1 week. On daily administration of Casodex, the (R)-enantiomer accumulates about 10 fold in plasma as a consequence of its long half-life. Steady state plasma concentrations of the (R)-enantiomer of approximately 9 microgram/ml are observed during daily administration of 50 mg doses of Casodex. At steady state the predominantly active (R)-enantiomer accounts for 99% of the total circulating enantiomers. Elimination In a clinical study the mean concentration of R-bicalutamide in semen of men receiving Casodex 150 mg was 4.9 microgram/ml. The amount of bicalutamide potentially delivered to a female partner during intercourse is low and by extrapolation possibly equates to approximately 0.3 microgram/kg. This is below that required to induce changes in offspring of laboratory animals. Special Populations The pharmacokinetics of the (R)-enantiomer are unaffected by age, renal impairment or mild to moderate hepatic impairment. There is evidence that for subjects with severe hepatic impairment, the (R)-enantiomer is more slowly eliminated from plasma. 5.3 Preclinical safety data Casodex is a potent antiandrogen and a mixed function oxidase enzyme inducer in animals. Target organ changes, including tumour induction, in animals, are related to these activities. None of the findings in the preclinical testing is considered to have relevance to the treatment of advanced prostate cancer patients. 6. Pharmaceutical particulars 6.1 List of excipients Casodex includes the following excipients: Lactose Monohydrate Magnesium Stearate Hypromellose Macrogol 300 Povidone Sodium Starch Glycolate Titanium Dioxide (E171). 6.2 Incompatibilities None known. 6.3 Shelf life 5 years. 6.4 Special precautions for storage Do not store above 30°C. 6.5 Nature and contents of container PVC blister/aluminium foil packs. 6.6 Special precautions for disposal and other handling No special requirements. Any unused medicinal product or waste material should be disposed of in accordance with local requirements. 7. Marketing authorisation holder AstraZeneca UK Limited, 600 Capability Green, Luton, LU1 3LU, UK. 8. Marketing authorisation number(s) PL 17901/0005 9. Date of first authorisation/renewal of the authorisation 18th June 2000/19th January 2006 10. Date of revision of the text 2nd February 2015 附：Casodex 150 mg Film-coated Tablets.（https://www.medicines.org.uk/emc/medicine/2583） ----------------------------------------------------------------- 注：以下产品不同规格和不同价格，采购以咨询为准 ----------------------------------------------------------------- 产地国家：英国 原产地英文商品名: Casodex  -150mg/Tablet 28Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -150毫克/片 28片/盒 中文参考药品译名: 比卡鲁胺 生产厂家中文参考译名: 阿斯利康英国有限公司 生产厂家英文名: AstraZeneca UK Limited -------------------------------------------------------------------- 产地国家：英国 原产地英文商品名: Casodex -50mg/Tablet 28Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -50毫克/片 28片/盒 中文参考药品译名: 比卡鲁胺 生产厂家中文参考译名: 阿斯利康英国有限公司 生产厂家英文名: AstraZeneca UK Limited -------------------------------------------------------------------- 产地国家：加拿大 原产地英文商品名: Casodex -50mg/Tablet 30Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -50毫克/片 30片/盒 中文参考药品译名: 比卡鲁胺 生产厂家英文名: AstraZeneca -------------------------------------------------------------------- 产地国家：瑞士 原产地英文商品名: Casodex -150mg/Tablet 30Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -150毫克/片 30片/盒 中文参考药品译名: 比卡鲁胺 生产厂家英文名: AstraZeneca AG -------------------------------------------------------------------- 产地国家：瑞士 原产地英文商品名: Casodex -50mg/Tablet 30Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -50毫克/片 30片/盒 中文参考药品译名: 比卡鲁胺 生产厂家英文名: AstraZeneca AG -------------------------------------------------------------------- 产地国家：瑞士 原产地英文商品名: Casodex -150mg/Tablet 100Tablets 原产地英文药品名: BICALUTAMIDE 中文参考商品译名: Casodex -150毫克/片 100片/盒 中文参考药品译名: 比卡鲁胺 生产厂家英文名: AstraZeneca AG -------------------------------------------------------------------- 产地国家：瑞士 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: Casodex -50毫克/片 100片/盒 中文参考药品译名: 比卡鲁胺 生产厂家英文名: AstraZeneca AG