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</li> <li> <br /> </li> <li> <span style="line-height:1.5;"><strong><u>吡喹?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> CAS?5268-74-1</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> 英文名:praziquantel</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> 分子式:C19H24N2O2 </u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>分子量:312.41</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> 含量?9%</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> 性状:本品为白色或类白色性粉末,</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> 用途:吡喹酮是较理想的新型广谱抗绦虫和抗血吸虫?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> </u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>USP30    25公斤纸板?  99% </u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> </u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u> </u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>性状】本品为白色或类白色结晶性粉末;味苦。本品在氯仿中易溶,在乙醇中溶解,?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>【药理?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>?)药数学吡喹酮是较理想的新型广谱抗绦虫和抗血吸虫药,目前广泛用于世界各国吡喹酮能使宿主体内血吸虫(包活日本分体血吸虫、曼氏分体血吸虫、埃及分体血吸虫)向肝脏移动,并在肝组织中死亡。此外,对大多数绦虫</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>成虫及未成熟虫体均有良效。加之,对动物毒性极小,是较理想的抗寄生虫药物?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>近有试验证实,吡喹酮能被绦虫和吸虫迅速吸收,首先使寄生虫发生瞬间的强直性收缩,然后使台胞体外皮迅速空泡形成,并逐渐扩大,最终表皮靡烂,终至溶解。当试管内药物浓度达到治疗血情浓浓度(??mg?/ml)?0s即发生上</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>述现象,但在体内则需l5min?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>皮层的空泡形成,绦虫仅发生于虫体前端部位,而吸虫则发生于全部体表外皮,空泡形成只发生于合胞体层,随?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>间延长而扩大病变范围。皮层破坏后,影响虫体吸收与排泄功能,更重要的是其体表抗原暴露,从而易擅受宿主免疫</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>攻击,促使虫体死亡?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>陈上述原发性变化外,吡喹酮还能引起继发性作用,使虫体表膜去极化,皮层碱性磷酸酶活性明显降低,以致葡萄糖的摄取受阻,内源性糖原耗竭。此外,吡喹酮尚可抑制虫体的核酸与蛋白质合成?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(2)药动?多种动物应用吡喹酮的研宄表明:内服后几乎全部迅速由梢化道吸收。血药峰值时间:小鼠?分钟,大鼠为l5?0分钟,犬?0?20分钟,绵羊约2h。吸收后药物广泛分布于所有组织器官,甚至能透过大鼠血一一脑屏障,且能进入犬的胆什。吡喹酮在动物组织器官内的广泛分布,奠定了对寄生于宿主各器官?肌肉、脑、腹膜腔、胆管和</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>小肠)的绦虫幼虫和成虫的有效杀灭作用的基础。吡喹酮主要在肝脏中迅速代谢灭活,如给大鼠?00mg/kg药量,肝门静脉药物浓度为21?mg/mL,而末梢血械为6?mg/mL,证明了吡喹酮在肝脏中迅速代谢灭活。以同样剂量肌肉或皮下注射,血浆中药物浓度维待时间更长,据大鼠、犬、恒河猴的试验表明,?4h内约?0?4C―标记的吡喹酮灭活代谢产物经屎排泄。对犬的排泄半衰期约3h,极少量犬、小鼠为0?%,绵羊??%原型药物经屎和粪便排性?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>【用途?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(1)?吡喹酮对绵羊、山羊大多数绦虫均有高效,l 0--1 5mg/kg剂量对扩展莫尼藏绦虫、贝氏莫尼藏绦虫、球点斯</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>豪绦虫和无卵黄腺绦虫均有i 00%驱杀效吊。对矛彤双腔吸虫、胰阔盘吸虫、绵羊绦虫需?0mg/kg量才能有效?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>对细颈囊尾蚴应以75mg/kg,连Ns天,杀灭效吊i 00%。吡喹酮对绵羊、山羊日本分体吸虫有高效?0mg/kg量灭</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>虫率接近100%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(2)牛lO--25mg/kg日量,连?天,或一次内50mg/kg,对牛细颈囊尾蚴有高效?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>据国内实践经验证明,吡喹酮对耕牛血吸虫病有高效,如人工感染尾蚴的水?25mg/kg),黄?30mg/kg)内服</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>吡喹酮后,灭虫率分别?9%%?5%~99%。有人试用第三胃注入15 mg/kg量,直至用药?0天,粪便转阴率,均为l00%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(3)犬、猫2?? mg/kg量内服或皮下注射,对大豆状带绦虫、犬复孔绦虫、猫肥颈带辱虫、乔伊绦?Joyeuxi e</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>lla pasqualei)几乎i00%有效;对细粒棘球绦虫、多房棘球绦虫需?--10mg/kg剂量,始能驱净虫体。对1?4日龄</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>幼虫应用更高剂量。对孟氏选宫绦虫、宽节裂头绦虫必须按25mg/kg日量,连?天?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>吡喹酮对犬卫氏肺吸虫亦有良效,一次应?0mg/kg或l OOmg/kg,有效率分别?7?-1 00%?0%--i 00%,但如按</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>25mg/kg连用3天,有效率几? 00%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(4)猪吡喹酮对猪细颈囊尾蚴有较好效吊,如以l Omg/kg量,连用l 4天,可杀灭大多数虫体;若?0mg/kg量,应用</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u><img src="/Common/KEditer/../../UploadFiles/KEditer/image/20160427/20160427143333_3601.jpg" alt="" />5天,则灭虫率?00%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>有人以人工感染血吸虫尾蚴的猪进行治疗试验,按30mg/kg量内服吡喹酮,其灭虫率接?0%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(5)?以l O--20mg/kg量一次内服,对鸡有轮赖利绦虫、漏斗带绦虫和节片戴文绦虫驱虫率接近l 00%。对鹅、鸭?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>彤剑带绦虫、斯氏双睾绦虫、片彤皱辱绦虫、细小匙掏绦虫、微细小体钩绦虫和冠状双盔绦虫亦有高效,l O--20mg/kg</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>量,药效接近l00%?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>【注意?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(1)本品毒性虽极低,但高剂量偶可使动物血情谷而转氨酶轻度升高现象。治疗血吸虫病时,个别牛会出现体温升</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>高,肌震颤和瘤胃膨胀等现象?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>(2)大剂量皮下注射时,有时会出现局部刺激反应。犬、猫出现的全身反?发生率为l 0?为疼痛、呕吐、下痢?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>梳涎、无力、昏睡等现象,但多能耐过?/u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>【用法与用量】内服一次量每lkg体重牛、羊、猪l O--35mg犬、猫2?--5mg</u></strong></span> </li> <li> <span style="line-height:1.5;"><strong><u>禽lO--200mg</u></strong></span> </li> 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