部份中文西他沙星水合物处方资料（仅供参考）
英文名：Sitafloxacin Hydrate
商品名：GRACEVIT TABLETS
中文名：西他沙星水合物
生产商：第一制药三共株式会社
药品介绍
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。
グレースビット錠50mg/グレースビット細粒10%
药物类别名称
广泛的口服抗菌制剂
批准日期：2008年4月
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
它是一种小黄白色晶体或结晶粉末。
在磷酸试验溶液中微微熔化的可能性较小,0.1mol/L盐酸试验溶液,几乎不溶于乙酰乙酸或甲醇,很难溶于乙醇(99.5),几乎不溶于水。它变成浅褐色白色由光。
(磷酸测试溶液:将50克磷酸盐溶解成950mL水)
8. 熔点
217 到 223
9. 分布系数
1-辛他醇/水(25°);0.244
药用药理学
1. 抗菌作用
Citafloxacin 具有广泛的抗菌光谱,适用于有氧或厌氧革正细菌和革兰氏阴性细菌、非典型细菌、金黄色葡萄球菌、肺炎球菌、肠球菌、莫拉西拉(Branhamela)猫科动物、大肠杆菌、西特罗巴塔, 克列布西耶拉, 肠杆菌, 塞拉蒂亚, 前列腺素, 摩根尼,流感, 伪多尼纳斯, 军团内嗜血杆菌, 肽类球菌, 普波泰莱塔, 波菲罗莫纳斯, 富索菌、曲霉素、沙眼衣原体、肺炎衣原体、肺炎衣原体、肺炎、支原体、支原体、支原体、肺炎等表现出较强的抗菌性能。特别是肺炎球菌(青霉素耐药性、大陆素耐药性和耐多药肺炎球菌)和肠球菌,针对伪多蒙多尼阿鲁吉诺萨和大肠杆菌(包括耐奎诺酮大肠杆菌),其他新的奎诺酮抗菌剂,它表现出很强的抗菌活性。
2. 对实验性感染的治疗作用
在小鼠脓毒症模型中,由革兰氏阳性细菌和革兰氏阴性细菌,西沙沙辛表现出感染防御效果,反映了体外抗菌能力。此外,在肺炎球菌的呼吸感染模型中,它表现出比其他新的奎诺酮抗菌剂控制良好的治疗效果。
3. 呼吸道感染的PK/PD分析
从呼吸道感染临床试验的PK/PD分析结果,随着AUC0-24hr/MIC或Cmax/MIC的增加,确认致因细菌的流失率增加。当AUC0-24hr/MIC超过100时,呼吸道感染的主要致病菌(包括22种肺炎球菌株)的流失率为96.3%(78/81),而当Cmax/MIC超过5时,损失率为96.3%(79/82)。此外,肺炎球菌在肺炎球菌呼吸道感染临床试验中的流失率,98.9%(89/90),当fAUC0-24hr/MIC转化血清环丙沙蛋白浓度超过30,fCpeak/麦克风是98.9%(89/90)时,它超过。
4. 作用机制
Citafloxacin表现出抑制活性对DNA茉莉花和托泊糖酶IV的细菌,作用是杀菌。 对该制剂的两种酶的抑制活性比其他新的奎诺酮抗菌素酶在控制中更强。 此外,该剂对奎诺酮耐药细菌衍生酶表现出很强的抑制活性。
适应症
[适应细菌]
金黄色葡萄球菌对该制剂的敏感性,链球菌,肺炎球菌,肠球菌,莫拉克塞拉(布兰查梅拉)卡塔利利,大肠杆菌,西托洛巴斯特,克莱布西耶拉,肠杆菌,塞拉蒂亚,普罗特乌斯,摩根内拉摩根尼, 流感细菌、假单体、血友病军团菌、胃肠球菌、前波氏菌、肺杆菌、气管炎(衣原体),肺炎衣原体。 肺炎衣原体),支原体(肺炎支原体)
[适应]
•咽喉炎,扁桃体炎(包括扁桃体炎,腹膜炎脓肿),急性支气管炎,肺炎,慢性呼吸道病变的继发性感染
膀胱炎, 肾上腺炎, 尿道炎
* 宫颈是
*耳炎介质,正新炎
* 牙周炎,牙周腹炎,端炎
用法与用量
临床表现
1. 按疾病分的有效率
在临床试验中,呼吸道感染、尿路感染、耳鼻喉科感染、牙科和口腔外科区域感染和性传播疾病,西塔氟辛50mg每天两次或100mg 如表1所示,每天施用1-2次不同疾病的有效率。
2. 细菌生长速率
呼吸感染、尿路感染、耳鼻喉科感染、从针对牙科和口腔手术区感染和性传播疾病患者的临床试验收集的致病微生物的细菌类型的细菌损失率如表2所示。
包装
片剂
50毫克
(塑料瓶)100 片(PTP) 100片
細粒10%
(塑料瓶) 30g
制造和销售
第一三共株式会社
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：http://www.info.pmda.go.jp/go/pack/6241018C1020_1_19/
GRACEVIT TABLETS 50mg：100tablets
Manufacturer：DAIICHI SANKYO
Brand：DAIICHI SANKYO
Description
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.
Presentation
100tablets
Feature
White to slightly yellowish white tablet
Active Ingredients
Sitafloxacin hydrate
Effect/Efficacy
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.
Usage/Dosage
〇 General dosage is as follows.
● 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.
〇 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.
〇 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.
Cautions
Contraindication
● The most commonly reported adverse reactions are following symptoms. If any of these symptoms occur, consult with your doctor or pharmacist.
-　diarrhea, loose stool, headache, and rash
● 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]
Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.