英文药名: Vidaza (Azacitidine Injection) 中文药名: 维达扎(阿扎胞苷注射液) 药品介绍： 阿扎胞苷(Azacitidine) 英文名称：Azacitidine 英文别名：5-Azacytidine、Ladakamycin 其他名：5aza-C，拉达卡霉素(Ladakamycin),5-氮杂胞苷、5-氮杂胞嘧啶核苷、氮胞苷、氮杂胞苷。 作用机制：嘧啶类抗代谢药，干扰核苷酸的合成，以假嘧啶形式掺入DNA和RNA中，并与之结合。 主要适应证：急性非淋巴细胞性白血病。用于乳腺癌、肠癌、黑色素瘤等有一定疗效。 常用剂量及方案：100mg／m2，静脉推注，每8小时一次，连用5天，200mg／(m2·d)静脉持续滴注，连用5天。 注意事项：由于药物的稳定性差，因此应该在用药前配药，配药后立即使用，配药后8小时未用则应丢弃。静脉滴注应该用新鲜林格液配制，每8小时配制一次。 毒性反应： (1)骨髓抑制和其他血液学反应：所有的病人都会出现严重的骨髓抑制和其他血液学反应，表现为白细胞于第12~14天降至最低，偶见抑制持续超过几周。 (2)恶心呕吐和其他胃肠道反应：常见。静脉持续滴注可减轻恶心呕吐和其他胃肠道反应反应。 (3)皮肤粘膜反应：粘膜炎及皮肤红疹偶见 (4)其他反应： 1)腹泻：常见。 2)神经系统反应：肌肉疼痛、虚弱、嗜睡及昏迷，少见。 3)肝毒性：罕见，但可能严重。 暂时性发热：偶见。 Vidaza 24 February 2009, 9:58am For the treatment of intermediate-2 and high-risk myelodysplastic syndromes, chronic myelomonocytic leukaemia and acute myeloid leukaemia in patients not eligible for haematopoietic stem cell transplantation. Azacitidine is an antineoplastic agent believed to exert its effects by multiple mechanisms, including cytotoxicity on abnormal haematopoietic cells in the bone marrow and hypomethylation of DNA. The cytotoxic effects are thought to be as a result of DNA, RNA and protein synthesis inhibition as well as the activation of DNA damage pathways. It is recommended that patients be treated for a minimum of six cycles and treatment should be continued as long as the patient continues to benefit or until disease progression. Each cycle consists of 28 days and patients should be monitored for haematologic response/toxicity and renal toxicities. ------------------------------------------------------------------------------ Indication VIDAZA is indicated for treatment of patients with the following French-American-British (FAB) myelodysplastic syndrome subtypes: refractory anemia (RA) or refractory anemia with ringed sideroblasts (RARS) (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL). IMPORTANT SAFETY INFORMATION VIDAZA is contraindicated in patients with a known hypersensitivity to azacitidine or mannitol and in patients with advanced malignant hepatic tumors. In Studies 1 and 2, the most commonly occurring adverse reactions by SC route were nausea (70.5%), anemia (69.5%), thrombocytopenia (65.5%), vomiting (54.1%), pyrexia (51.8%), leukopenia (48.2%), diarrhea (36.4%), injection site erythema (35.0%), constipation (33.6%), neutropenia (32.3%), and ecchymosis (30.5%). Other adverse reactions included dizziness (18.6%), chest pain (16.4%), febrile neutropenia (16.4%), myalgia (15.9%), injection site reaction (13.6%), and malaise (10.9%). In Study 3, the most common adverse reactions by IV route also included petechiae (45.8%), weakness (35.4%), rigors (35.4%), and hypokalemia (31.3%). In Study 4, the most commonly occurring adverse reactions were thrombocytopenia (69.7%), neutropenia (65.7%), anemia (51.4%), constipation (50.3%), nausea (48.0%), injection site erythema (42.9%), and pyrexia (30.3%). The most commonly occurring Grade 3/4 adverse reactions were neutropenia (61.1%), thrombocytopenia (58.3%), leukopenia (14.9%), anemia (13.7%) and febrile neutropenia (12.6%). Because treatment with VIDAZA is associated with anemia, neutropenia and thrombocytopenia, complete blood counts should be performed as needed to monitor response and toxicity, but at a minimum, prior to each dosing cycle. Because azacitidine is potentially hepatotoxic in patients with severe preexisting hepatic impairment, caution is needed in patients with liver disease. In addition, azacitidine and its metabolites are substantially excreted by the kidneys and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, it may be useful to monitor renal function. VIDAZA may cause fetal harm when administered to a pregnant woman. Women of childbearing potential should be apprised of the potential hazard to the fetus. Men should be advised not to father a child while receiving VIDAZA. Nursing mothers should be advised to discontinue nursing or the drug, taking into consideration the importance of the drug to the mother. Please see full Prescribing Information. VIDAZA® is a registered trademark of and Celgene Patient Support™ is a trademark of Celgene Corporation. ©2010 Celgene Corporation. All rights reserved. ビダーザ注射用100mg 薬効分類名 骨髄異形成症候群治療剤 商標名 Vidaza for Injection 100mg 一般名 アザシチジン（Azacitidine）（JAN） 化学名 4-Amino-1-β-D-ribofuranosyl-1,3,5-triazin-2(1H)-one 分子式 C8H12N4O5 分子量 244.20 化学構造式 性状 白色～微灰色の固体。 本品はジメチルスルホキシドに溶けやすく、水又はN-メチルピロリドンにやや溶けにくく、エタノール（99.5）にほとんど溶けない。 融点 約227℃（分解） 承認条件 国内での治験症例が極めて限られていることから、製造販売後、一定数の症例に係るデータが集積されるまでの間は、全症例を対象に使用成績調査を実施することにより、本剤使用患者の背景情報を把握するとともに、本剤の安全性及び有効性に関するデータを早期に収集し、本剤の適正使用に必要な措置を講じること。 包装 ビダーザ注射用100 mg：1バイアル 製造販売元 日本新薬株式会社 www.info.pmda.go.jp/go/pack/4291419D1026_1_02/