Valrubicin（商品名：VALSTAR）是蒽环类阿霉素的衍生物，已被美国食品和药物管理局（FDA）批准用于BCG难治性CIS的膀胱内治疗。
批准日期：1998年10月1日 公司：ENDO PHARMACEUTICALS VALERA IN
VALSTAR（戊柔比星[valrubicin]）溶液，用于膀胱内使用
初始美国批准：1981年
作用机制
Valrubicin是一种影响各种相互关联的生物功能的蒽环类药物，其中大多数涉及核酸代谢。 在细胞中，它抑制核苷结合到核酸中，引起染色体损伤，并阻止细胞周期进入G2。 尽管valrubicin不与DNA结合，但valrubicin代谢物会干扰DNA拓扑异构酶II的正常DNA断裂 - 再密封作用。
适应症和用法
Valstar是在患者膀胱为谁即时性膀胱切除术将具有不可接受的发病率或死亡率相关联的指示的用于原位（CIS）BCG-耐火癌的膀胱内治疗的蒽环类拓扑异构酶抑制剂。
剂量和用量
仅限膀胱内使用。
VALSTAR每周静脉注射一次，持续六周。
经尿道切除和/或电灼后至少两周延迟给药。
将VALSTAR缓慢升温至室温，但不要加热。
处理和准备VALSTAR解决方案时要小心。
剂量形式和强度
注射：一次性小瓶中200mg/5mL
禁忌症
穿孔膀胱或膀胱粘膜受损
对蒽环类抗生素或聚氧乙烯蓖麻油过敏。
并发尿路感染。
容量小的患者不能耐受75mL滴注。
警告和注意事项
延迟膀胱切除术可能导致转移性膀胱癌的发展，这是致命的。
不要给予给患者Valstar有穿孔的膀胱或那些在人膀胱粘膜的完整性就会受到损害。
在膀胱内灌注VALSTAR之前评估膀胱的状态。
对有严重膀胱过敏症状的患者慎用。
胚胎胎儿毒性：VALSTAR可导致胎儿伤害。建议的潜在风险胎儿的生殖潜力的女性，使用有效避孕。
不良反应
最常见的不良反应（> 5％）Valstar给药后有尿频，尿痛，尿急，膀胱痉挛，血尿，膀胱疼痛，尿失禁，膀胱炎，尿路感染，夜尿增多，局部灼热症状，腹痛，和恶心。
报告可疑的不良反应，请联系远藤制药公司在1-800-462-3636或FDA电话：1-800-FDA-1088或WWW.FDA.GOV/MEDWATCH。
用于特定人群
哺乳期：建议不要母乳喂养。
包装提供
VALSTAR是一种无菌，透明的红色溶液，用于聚乙二醇蓖麻油/脱水酒精USP，每毫升含有40毫克的valrubicin。 VALSTAR提供一次性透明玻璃瓶，单独包装，尺寸如下：
NDC 67979-001-01四箱200毫克/ 5毫升一次性小瓶
将样品瓶保存在2°-8°C（36°-46°F）的冷藏箱中。不要冻结。
完整说明资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e96f30a0-6662-11de-8f80-0002a5d5c51b
VALSTAR® (valrubicin) is a chemotherapy medicine that is put into the bladder with a flexible tube called a catheter. If your carcinoma in situ (CIS) bladder cancer did not respond to treatment with Bacillus Calmette-Guerin (BCG), and you can’t be considered for surgery, VALSTAR® may be an option for you.
WHAT IS VALSTAR®
VALSTAR® (valrubicin) is a liquid medicine put directly into the bladder with flexible tubing called a catheter. VALSTAR® is used for patients whose CIS bladder cancer did not respond to treatment with a drug called BCG or Bacillus Calmette-Guerin and who cannot have surgery right away to take out the bladder.
IMPORTANT SAFETY INFORMATION ABOUT VALSTAR®
You should not receive VALSTAR® if you are allergic to polyoxyl castor oil or to medicines called anthracyclines; if you have been told by a doctor you have a hole in your bladder or a weak bladder wall; if you have a urinary tract infection or if you have been told by a doctor that you have a small bladder.
Only about 1 in 5 patients no longer had CIS bladder cancer 6 months after treatment with VALSTAR®. If you do not respond to VALSTAR®, waiting to have your bladder taken out increases the chances that the bladder cancer can spread to other parts of your body which can lead to death. You should talk with your doctor about the risks of waiting for surgery to have your bladder taken out when you have CIS bladder cancer. If your CIS bladder cancer does not respond to VALSTAR® after 3 months or if your CIS bladder cancer comes back, you should talk with your doctor again about having surgery to take out your bladder.
To prevent VALSTAR® from entering other parts of your body, your doctor will check your bladder before treating you with VALSTAR®. If you have been told by a doctor you have a hole in your bladder, a weak bladder wall, or are having a certain type of surgery for your bladder, your doctor may choose to delay your treatment.
Tell your doctor if you have severe irritation in your bladder before receiving VALSTAR®. You may not be able to hold the VALSTAR® in your bladder for the whole time or it may leak out. You may have pain or irritation of your bladder during or shortly after getting VALSTAR®. For the first day after getting VALSTAR®, your urine may have a red color. This is normal. Tell your doctor right away if you have pain or if you have red-colored urine after the first day of getting VALSTAR®.
Women should not become pregnant and men should take measures to prevent their partner from getting pregnant during treatment with VALSTAR®. If you plan to be sexually active, talk with your doctor about possible risks and use the birth control method recommended by your doctor. Women should stop nursing before starting treatment with VALSTAR®. VALSTAR® may affect male reproductive fertility.
During or after getting VALSTAR®, common side effects included urinating often, difficulty urinating, a strong need to urinate right away, bladder spasm, burning and pain, blood in urine, not making it to the bathroom in time to urinate, bladder inflammation, urinary tract infection, need to urinate at night, stomach pain, and nausea. These are not all the side effects of VALSTAR®. For more information, ask your doctor or pharmacist. .
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