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小型猪专用复合麻醉剂麻醉后阿替美唑的颉颃效果及其体内药代动力学
Antagonistic Effect of Atipamezole and Its Pharmacokinetics Following Anaesthesia with the Combined Anaesthetic for Miniature Pigs in Minipigs

作  者: ; ; ; ; ;

机构地区: 东北农业大学动物医学学院

出  处: 《畜牧兽医学报》 2014年第12期2074-2080,共7页

摘  要: 旨在观察阿替美唑颉颃小型猪专用复合麻醉剂(XFM)的效果,探讨阿替美唑在小型猪体内的药代动力学。14头小型猪,随机均分为阿替美唑组和对照组,小型猪耳根部肌肉注射阿托品后再肌注XFM对小型猪进行全身麻醉。麻醉30min后阿替美唑组肌肉注射阿替美唑0.12mg·kg-1进行全麻催醒,对照组按同等剂量注射生理盐水。前腔静脉采集血样,并观察记录小型猪苏醒时间、心率和呼吸率变化,记录阿替美唑给药后小型猪镇痛、镇静、肌松、体位及听觉反射总得分,评价阿替美唑的催醒效果,同时用高效液相色谱法测定各采血时间点血浆药物浓度。结果表明,阿替美唑组小型猪苏醒时间显著短于对照组(P<0.05);阿替美唑给药后5~60min小型猪心率显著高于对照组(P<0.05);呼吸频率在10~15min显著高于对照组(P<0.05);小型猪镇痛、镇静、肌松、体位及听觉反射总得分在阿替美唑给药后10~90min显著低于对照组(P<0.05);阿替美唑在血浆中吸收相半衰期(T1/2α)为(11.056 9±3.093 4)min;消除相半衰期(T1/2β)为(875.421 8±159.375 3)min;药时曲线下面积(AUC)为(797 958.836 0±96 783.124 1)pg·(min·mL)-1;达峰时间(Tpeak)为(9.544 0±0.484 4)min;达峰浓度(Cmax)为(1 107.065 2±121.620 1)pg·mL-1。结果提示阿替美唑肌注小型猪后,其体内吸收迅速,分布广泛,在血浆中药物经时过程符合一级吸收二室开放模型,可迅速逆转XFM对小型猪的麻醉作用。 This study was conducted to investigate the antagonistic effect of atipamezole and following anaesthesia with the Combined Anaesthetic for Miniature Pigs(XFM)and its pharmacokinetics in minipigs.Fourteen pigs were randomly divided into control group and atipamezole group.All experiment pigs were anesthetised with XFM intramuscularly.Pigs in atipamezole group were administrated with atipamezole(0.12mg·kg-1)intramuscularly and pigs in control group were administrated with saline.Baseline physiological parameters of respiration and heart rate were recorded and blood sample were collected from cranial vena cava and detected by using high performance liquid chromatography(HPLC)for drug analysis in different phases.Results showed that the recovery time in the atipamezole group was significantly shorter than control group(P<0.05),values of HR were significantly higher than control group from 5to 60 min after administration of atipamezole(P<0.05),values of RR were significantly higher than control group from10 to 15min after administration of atipamezole(P<0.05),the total scores of analgesia,sedation,skelaxin,posture,and auditory response were significantly higher than control group from 10 to 15min after administration of atipamezole(P<0.05),and pharmacokinetic parameters were as follows:T1/2αwas 11.0569±3.0934 min,T1/2βwas 875.421 8±159.375 3 min,AUC was797 958.836 0±96 783.124 1pg·(min·mL)-1,Tpeakwas 9.544 0±0.484 4 min,Cmaxwas1 107.0652±121.620 1pg·mL-1.These results indicated that atipamezole is characterized by rapid drug action,slow metabolism,its best pharmacokinetic model was two-compartment open model,and atipamezole was effective for antagonizing the anaesthesia with XFM in minipigs.

关 键 词: 阿替美唑 催醒 小型猪复合麻醉剂 药代动力学 小型猪

领  域: [农业科学] [农业科学] [农业科学]

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