英文药名：GRACEVIT(Sitafloxacin Hydrate) 中文药名：西他沙星片和细粒10% 生产厂家：第一制药三共株式会社 药品介绍 治疗严重难治的细菌感染新药—西他沙星水合物50mg片和10％细粒剂（sitafloxacin hydrate,商品名：Gracevit）获准上市 グレースビット錠５０ｍｇ／グレースビット細粒１０％ 商標名 GRACEVIT TABLETS GRACEVIT FINE GRANULES 一般名 シタフロキサシン水和物 (Sitafloxacin Hydrate) 略名 STFX 化学名 (－)-7-[(7S )-7-Amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1R ,2S )-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid sesquihydrate 分子式 C19H18ClF2N3O3・11/2H2O 分子量 436.84 構造式 性状 黄白色至黄白色结晶或结晶性粉末。 稍少溶于磷酸试液，0.1mol/L的盐酸试液，微溶于乙腈或甲醇，极微溶于乙醇（99.5），和几乎不溶于水。它通过光变成淡黄色的褐白色。 （磷酸试剂：磷酸50克我溶解于水950mL） 融点 217～223℃ 分配係数 1-オクタノール/水 (25℃); 0.244 适应证 适用于敏感菌引起的各类感染，用于治疗严重难治性感染性疾病 剂量与用法 通常，成人1次50mg（1片或颗粒 0.5g），1日2次。效果不理想者，可1次100mg，1日2次。 禁忌 对本品或其他喹诺酮类抗菌药有既往过敏史患者、孕妇或可能怀孕妇女、儿童等禁用本品。 不良反应 1071例患者报告的不良反应（包含临床检查异常）为33.5%（359例），主要的不良反应为：腹泻62例（5.8%），软便79例（7.4%），头痛22例（2.1%），ALT（GPT）上升59例（5.5%），AST（GOT）上升45例（4.2%），嗜酸性粒细胞数增加42例（3.9%）等。出现腹泻、软便的频率比对照药高。 注意事项 肾功能障碍患者、患有或曾患过癫痫等痉挛性疾病患者（包括用类似药出现痉挛报告的患者）、老年人服用本品应慎重。 孕妇及哺乳期妇女用药 孕妇或可能怀孕的妇女禁用本品，妊娠中给药本品的安全性尚不明确。 有动物（大鼠）试验报告本品通过乳汁分泌，哺乳期妇女使用本品应避免哺乳。 包装规格 片：50毫克 100片（瓶） 100片  500片（PTP） 細粒10% 30克 製造販売元 第一三共株式会社 完整资料附件：http://www.info.pmda.go.jp/go/pack/6241018C1020_1_10/ 日本批准广谱抗生素西他沙星水合物片剂和细粒剂上市 日本厚生省批准第一制药三共株式会社（Daiichi Sankyo）的广谱抗生素西他沙星水合物50mg片和10％细粒剂（sitafloxacin hydrate,商Gracevit）上市，用于治疗严重难治的细菌感染。 本品系一新颖的N-1-氟环丙基喹诺酮，对耐甲氧西林金黄色葡萄球菌、耐甲氧西林表皮葡萄球菌、厌氧菌（包括脆弱类杆菌）以及支原体、衣原体等均具较强的抗菌活性。化学结构上有一顺式(1R,5R)-2-氟环丙胺基团，显示良好的药代动力学特性，且可减少不良反应。该药不仅显著增强抗革兰阳性菌活性，而且对临床分离的许多耐氟喹诺酮类的菌株也具抗菌活性。 本品体外抗菌活性的研究表明，其具广谱抗菌作用，不仅对革兰阴性菌有抗菌活性，而且对革兰阳性菌以及对许多临床常见耐氟喹诺酮类菌株也有良好杀菌作用。本品口服吸收好、生物利用度大于70%，组织分布广，在中枢神经系统外的多种组织中的药物浓度均高于血清药物浓度，因此，本品可望成为治疗呼吸道、泌尿生殖道、腹腔以及皮肤软组织等单一或混合细菌感染的重要药物。 Daiichi Sankyo has launched the broad-spectrum antibacterial agent Gracevit tablets 50mg/fine granules 10% GRACEVIT TABLETS 50mg (Sitafloxacin Hydrate) Brand name : GRACEVIT TABLETS 50mg 　Active ingredient: Sitafloxacin hydrate 　Dosage form: white to slightly yellowish white tablet (φ: 7.7 mm, thickness: 4.1 mm) 　Print on wrapping: グレースビット 50mg, Gracevit 50mg, DSC741, 抗菌剤です ---------------------------------- Gramalil Fine Granules 10% (Sitafloxacin Hydrate) Brand name : Gramalil Fine Granules 10% 　Active ingredient: Tiapride hydrochloride 　Dosage form: white to pale yellowish white fine granules 　Print on wrapping: ---------------------------------- Effects of this medicine This is a new quinolone oral antibacterial to inhibit DNA replication of bacteria at the time of infection, and shows antibacterial action. It is usually used in the treatment of various infections such as respiratory infection, urologic infection, gynecologic infection, otorhinological infections, and dental infection. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you are a pediatric (child) patient. •If you are pregnant, possible pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •In general, for adults, take 1 tablet (50 mg of sitafloxacin) at a time, twice daily, or 2 tablets (100 mg) at a time, once daily. If the effect is insufficient, the dosage may be increased to 2 tablets (100 mg) at a time, twice daily. Strictly follow the instructions. •If you miss a dose, take a dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. Precautions while taking this medicine • Possible adverse reactions to this medicine The most commonly reported adverse reactions include diarrhea, loose stool, headache, and rash. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •pale face, cold sweat, dizziness, breathing difficulty, eruption, angioedema [shock, anaphylaxis] •fever, loss of appetite, rash [oculomucocutaneous syndrome] •anorexia, general malaise, yellowing in the skin or conjunctiva [hepatic dysfunction] •general malaise, decrease of urine putput, swelling [acute renal failure] •nausea, vomiting, stomachache, frequent diarrhea [pseudomembranous colitis] •sweating, palpitation, lassitude [hypoglycaemia] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store away from light, heat and moisture. •Discard the remainder. Do not store them.