头孢丙烯分散片

头孢丙烯分散片 核准日期:2006年10月16日 药品名称: 【通用名称】 头孢丙烯分散片 【商品名称】 银力舒 【英文名称】 Cefprozil Dispersible Tablets 【汉语拼音】 Tou Bao Bing Xi Fen San Pian 成份: 本品主要成份为头孢丙烯。 化学名称:6R，7R)-7-[(R)-2-氨基-2-(对羟基-苯基)乙酰氨基]-8-氧代-3-丙烯-5-硫杂-l-氮杂双环-(4，2，0)辛-2-烯-2-羧酸一水合物。 化学结构式: 分子式:C18H19N3O5S?H2O 分子量:407.45 所属类别: 化药及生物制品 >> 抗微生物药 >> 抗细菌药 >> 抗生素类 性状: 本品为类白色或淡黄色片。 适应症: 用于敏感菌所致的下列轻、中度感染。 上呼吸道感染:化脓性链球菌性咽炎/扁桃体炎。 注:通常治疗和预防链球菌感染(包括预防风湿热)应选择肌肉注射青霉素。虽然头孢丙烯一般可有效消除鼻咽部的化脓性链球菌，但目前尚无可供借鉴的头孢丙烯预防继发性风湿热的资料。 肺炎链球菌、流感嗜血杆菌(包括产β-内酰胺酶菌株)和卡他莫拉菌(包括产β-内酰胺酶菌株)性中耳炎。肺炎链球菌、嗜血流感杆菌(包括产β-内酰胺酶菌株)和卡他莫拉菌(包括产β-内酰胺酶菌株)性急性鼻窦炎。 下呼吸道感染:由肺炎链球菌、流感嗜血杆菌(包括产β内酰胺酶菌株)和卡他莫拉菌(包括产β内酰胺酶菌株)引起的急性支气管炎继发细菌感染和慢性支气管炎急性发作。 皮肤和皮肤软组织感染:金黄色葡萄球菌(包括产青霉素酶菌株)和化脓性链球菌引起的非复杂性皮肤和皮肤软组织感染，但脓肿通常需行外科引流排脓。 适当时应进行细菌培养和药敏试验以确定病原菌对头孢丙烯的敏感性。 administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6 规格: 0.25g(以头孢丙烯计) 用法用量: 口服。 成人(13岁和以上)上呼吸道感染，每次0.5g(2片)，每天1次;下呼吸道感染，每次0.5g(2片)，每天2次;皮肤或皮肤软组织感染，每天0.5g(2片)，分1次或2次;严重病例每次0.5g(2片)，每天2次。 2至12岁儿童上呼吸道感染，每次7.5mg,kg体重，每天2次;皮肤或皮肤软组织感染，每次20mg,kg体重，每天1次。 6个月婴儿至12岁儿童中耳炎，每次15mg,kg体重，每天2次;急性鼻窦炎，一般每次7.5mg,kg体重，每天2次;严重病例，每次15mg,kg体重，每天2次。 疗程一般7,14日，但β-溶血性链球菌所致急性扁桃体炎、咽炎的疗程至少10日。 肾功能不全 肾功能不全患者服用头孢丙烯应按下调整剂量: *血液透析可清除体内部分头孢丙烯，因此应在血液透析完毕后服用。 肝功能受损患者无需调整剂量。 不良反应: 1.头孢丙烯的不良反应与其他口服头孢菌素相似，主要为胃肠道反应，包括腹泻，恶心，呕吐和腹痛等。亦可发生过敏反应，常见为皮疹、荨麻疹。儿童发生过敏发应较成人多见，多在开始治疗后几天内出现，停药后几天内消失。 其他不良发应较少，包括:肝胆系统AST(谷草转氨酶)和ALT(谷丙转氨酶)升高。偶见碱性磷酸酶和胆红素升高。胆汁淤积性黄痕罕见。 中枢神经系统:眩晕、多动、头痛，精神紧张、失眠。偶见嗜睡。所有这些反应均呈可逆性。 血液系统:白细胞减少、嗜酸性粒细胞增多。 肾脏:血尿素氮增高，血肌酐增高。 其他:尿布皮炎样皮疹和二重感染，生殖器瘙痒和阴道炎。 administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6 下述不良事件，无论是否已明确与头孢丙烯的因果关系，在上市后监测中均少见。包括过敏、血管神经性水肿、结肠炎、(包括伪膜结肠炎)、多形性红斑、发热、血清病样反应、Stevens-Johnson综合征和血小板减少症。 2.头孢菌素类药物的不良反应 除上述所列使用头孢丙烯发生的不良反应外，头孢菌素类药物尚有以下的不良反应和实验室检查异常: 再生障碍性贫血、溶血性贫血、出血、肾功能不全、中毒性表皮坏死、中毒性肾病、凝血酶原时间延长、Coomb试验阳性、LDH增高、全血细胞减少、中性粒细胞减少、粒细胞缺乏症。 有几种头孢菌素药物与癫痫发作用关，特别是肾功能损伤患者未减少用药时(见“剂量和用法”)。如与药物治疗有关的癫痫发作，应停用药物，并根据临床表现进行抗惊厥治疗。 禁忌: 禁用于对头孢菌素类过敏患者。 注意事项: 使用本品治疗前，应仔细询问病人是否有头孢丙烯和其他头孢菌素类药物、青霉素类及其他药物的过敏史。有青霉素过敏患者服用本品应谨慎。凡以往有青霉素类药物所致过敏性休克史或其他严重过敏反应者不宜使用本品。如发生过敏反应，应停止用药。严重过敏反应需使用肾上腺素并采取其他紧急，包括给氧、静脉输液、静注抗组胺药、皮质激素、升压药和人工呼吸。 几乎所有抗菌药物包括头孢丙烯长期使用可引起非敏感性微生物的过度生长，改变肠道正常菌群，诱发二重感染，尤其是伪膜性肠炎。因此应仔细观察用药病人服药后的反应，特别注意对继发腹泻患者的诊断，如在治疗期间发生二重感染，应采取适当的措施。对伪膜性肠炎患者，轻度病例仅需停用药物，而中至重度病例，根据临床症状采取调节水和电解质平衡，补充蛋白，并用对耐药菌有效的抗菌药物治疗。 确诊或疑有肾功能损伤的病人(见剂量和用法)在本品治疗前和治疗时，应严密观察临床症状并进行适当的实验室检查，在这些病人常规剂量时血药浓度较高或,和排泄减慢，故应减少本品的每日用量。同时服用强利尿剂治疗的病人使用头孢菌素应谨慎，因此这些药物可能会对肾功能产生有害影响。 患有胃肠道疾病，尤其是肠炎病人应慎用头孢丙烯。 孕妇及哺乳期妇女用药: 家兔、小鼠和大鼠分别经口给予人用最大总剂量(1000mg)的0.8、8.5、18.5倍(以mg/m2计算)未发现对胎儿的影响。但尚未在妊娠妇女中进行充分和良好对照的研究。因为动物的生殖毒性研究不能完全预测人类的反应，故仅在确有需要时方可用于怀孕妇女。 哺乳妇女单次口服头孢丙烯1g，可在乳汁中发现发量药物(小于给药量的0.3%)。24小时后平均水平在0.25-3.3μg,mL范围。由于尚不清楚头孢丙烯对哺乳婴儿的影响，故哺乳妇女应慎用。 administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6 儿童用药: 尚无6个月以下小儿患者使用本品的安全性和疗效的资料。然而，已有有关其他头孢菌素类药物在新生儿体内蓄积(由于此年龄段小儿的药物半衰期延长)的报道。 老年用药: 健康老年志愿者(大于65岁)给予1g头孢丙烯，与20-40成人相比，AUC升高35,,60,，肾清除率下降40%。临床研究显示，当老年人接受和成人同样剂量时，安全有效性是可以接受的，且和非老年患者相当。 药物相互作用: 0. 已有氨基糖苷类抗生素和头孢菌素合用引起肾毒性的报道，与丙磺舒合用使头孢丙烯的AUC增加一倍。 药物/实验室试验相互作用 头孢菌素类抗生素可引起尿糖还原试[Benedict或Feling氏试剂或硫酸铜片状试剂(Clinitest片)]假阳性反应，但尿糖酶学试验(如Tes-Tape尿糖试纸)不产生假阳性。此类药物可引起假阴性血糖氰化反应，血液中头孢丙烯不干扰用碱性苦味酸盐法对血或尿中肌酐量的测定。 药物过量: 成年、断奶或新生大鼠以及成年小鼠单次口服总剂量达5000mg/kg未引起死亡或毒性症状，猴单次口服剂量达3000mg/kg引起腹泻和味觉丧失，但未见死亡。 头孢丙烯主要经肾脏清除，对严重过量，尤其是肾功能损伤患者，血液透析有助于头孢丙烯清除。 药理毒理: 本品为第二代头孢菌素类药物，具有广谱抗菌作用。该药的杀菌机制是通过与细菌细胞膜上的青霉素结合蛋白(PBPs)结合，阻碍细菌细胞壁合成，从而导致细菌的溶解死亡。 体外试验证明，头孢丙烯对革兰阳性需氧菌中的金黄色葡萄球菌(包括产β-内酰胺酶菌株)、肺炎链球菌、化脓性链球菌作用明显，对坚忍肠球菌、单核细胞增多性李斯特菌、表皮葡萄球菌、腐生葡萄球菌、Warnei葡萄球菌、无乳链球菌、链球菌C、D、F、G组和草绿色链球菌具抑制作用。对耐甲氧西林葡萄球菌和粪肠球菌无效。对革兰阴性需氧菌的流感嗜血杆菌(包括产β-内酰胺酶菌株)、卡他莫拉菌(包括产β-内酰胺酶菌株)高度敏感;可抑制Diversus枸橼酸菌、大肠杆菌、肺炎克雷伯菌、淋病奈瑟菌(包括产β-内酰胺酶菌株)、奇异变形杆菌、沙门菌属、志贺菌和弧菌的生长繁殖，对不动杆菌属、肠杆菌属、摩氏摩根菌属、普通变形杆菌、普罗威登菌属、假单孢菌属的多数菌株无抗菌作用。对厌氧菌中的黑色素类杆菌、艰难梭杆菌、产气荚膜杆菌、梭杆菌属、消化链球菌和痤疮丙酸杆菌具一定抑制作用，对多数脆弱杆菌株无抗菌作用。 毒理研究: 尚未进行长期致癌性研究。在沙门氏菌或大肠杆菌中进行的Ames试验和中国鼠卵巢细胞中进行的染色体畸变试验均未发现致突变作用。在鼠骨髓微核试验中口服给予剂量达人用量高剂量的30倍以上(以mg/?计算)未发现染色体畸变。 administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6 雄性或雌性大鼠经口给予头孢丙烯剂量达人用最高量18.5倍(以mg/?计算)未发现对生殖能力的损害。 药代动力学: 已有试验证明空腹口服头孢丙烯片剂、胶囊剂和混悬剂具生物等效。以下数据主要来自胶囊剂的研究资料。 受试者空腹口服头孢丙烯，约95,给药量可被吸收。空腹口服头孢丙烯250mg、500mg或1g后，服药后1.5小时达血药峰浓度，平均血药峰浓度分别为6.1、10.5和18.3μg/ml。 口服250mg、500mg和1g后最初4小时，尿中平均浓度分别为700μg/ml、1000μg/ml和2900μg/ml。尿回收率约为服药量的60,。 在健康受试者的平均血浆消除半衰期为1.3小时，稳态分布容积约0.23L/kg。总清除率和肾清除率分别为3m1/min,kg和2.3m1/min,kg左右。血浆蛋白结合率约为36,，当血药浓度在2,20μg/ml范围内，血浆蛋白结合率与血药浓度变化无关。 片剂或混悬剂与食物同服不影响头孢丙烯的吸收(AUC)和血药峰浓度，但达峰时间可延长0.25小时至0.75小时。 肾功能正常者口服头孢丙烯剂量达1000mg，每8小时一次，连续10天，未见有药物蓄积现象。 肾功能减退病人，根据肾功能损害程度不同，头孢丙烯血浆半衰期可延长至5.2小时;肾功能完全丧失患者，头孢丙烯的血浆半衰期可达5.9小时。血液透析时，半衰期缩短。肾功能明显不全患者的头孢丙烯排泄途径尚不明确(见注意事项与剂量和用法)。 头孢丙烯在肝功能损害病人的血浆半衰期可增至2小时左右，但这种改变并不说明肝功能损伤患者需调整剂量。 老年人(?65岁)平均AUC相对于年轻成人约增高35,,60,，女性AUC较男性AUC高15,,20,。但头孢丙烯药代动力学在年龄、性别间差异不足以说明有调整剂量的必要。 哺乳期妇女一次口服头孢丙烯1克，可在乳汁中测得少量的药物(,给药量的0.3,,。24小时平均浓度为0.25mg,L,3.3mg,L。由于尚不明确头孢丙烯对婴儿的影响，故哺乳期妇女服用本品应谨慎。 进行了儿童患者(6个月到12岁)和成人患者口服相应剂量后的比较研究。儿童给药后1,2小时可达到最高浓度，血浆消除半衰期约为1.5小时。一般，儿童患者给药剂量为7.5、15、30mg/?的达到的血浆浓度分别与成人服用250、500、1000mg剂量相当。 尚无有关头孢丙烯的脑脊液中药代动力学资料。 贮藏: 遮光，密封，在阴凉(不超过20?)干燥处保存。 包装: administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6 铝塑包装，每板6片，每袋1板，每小盒1袋; 铝塑包装，每板6片，每袋2板，每小盒1袋。 有效期: 24个月 administrative leadership of the criticism, resulting in serious consequences, the pursuit of leadership, along with 500-1000 punishment. (5) significant near miss should be attempted as the case of responsible for the accident and construction team injuries accident penalty provisions, mutatis mutandis. Eight, should perform in the construction standards and specifications, serial number a 1 GB3323-2005 steel fusion welded butt joints, welding engineering-Ray lighting and quality rating of 2 GB11345-89 steel welds manual methods of ultrasonic inspection and testing results for grade 3 GB50236-2002 industrial pipe welding engineering code for construction and acceptance of field equipment 4 HGJ222-92 technical specification for welding of aluminium and its alloys 5 low temperature steel welding procedure 6 SH3525-2004 petrochemical JB/ T4708-2000 of welding procedure qualification for steel pressure vessels 7 JB/4709-2000 8 JB4730-2005 pressure vessel welding procedures of steel pressure vessel NDT 9 JB/T4744-2000 steel pressure vessel products mechanical properties test of welded plate II, mechanical equipment installation engineering 1 GB150-98 2 GB50128-2005 vertical cylindrical steel pressure vessel steel welded tank code for construction and acceptance of 3 JB/ T4735-1997 steel welded atmospheric pressure vessel 4 GB50231-2009 mechanical equipment installation engineering construction and acceptance specification for 5 GB50275-98 compressor, fan and pump installation engineering construction and acceptance specification for lifting 6