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1.
使用不同剂量阿苯达唑对人工感染旋毛虫的小白鼠进行疗效试验,观察其不同剂量的杀虫效果.结果表明：应用阿苯达唑20 mg/（kg·d）×7治疗鼠旋毛虫病有很好的治疗效果,为阿苯达唑临床应用提供科学参考. 相似文献
2.
Capece BP Navarro M Arcalis T Castells G Toribio L Perez F Carretero A Ruberte J Arboix M Cristòfol C 《Veterinary journal (London, England : 1997)》2003,165(3):266-275
Three single oral doses (8.5, 10, and 14 mg/kg) of a racemic formulation of albendazole sulphoxide (ABZSO) were administered to pregnant rats on day 10 of gestation. Mother plasma and embryo concentrations of ABZSO enantiomers and albendazole sulphone (ABZSO(2)) were determined 9 h after administration. The (-)-ABZSO enantiomer showed higher peak concentrations in both maternal plasma and embryo than the (+) enantiomer. An increase in embryo concentrations of ABZSO enantiomers and ABZSO(2) was only observed when dose rose to 14 mg/kg. There was an increase in resorption when the dose increased, but significant differences were only found in the higher dose group when compared with the other groups. The incidence of external and skeletal malformations (mostly of the tail, vertebrae and ribs) rose significantly in the 10 mg/kg group, producing almost 20% and 90% of malformed fetuses, respectively, and gross external and skeletal abnormalities in the thoracic region and limbs were also found. 相似文献
3.
试验采用甲苯咪唑、丙硫苯咪唑单独给药及联合给药,以300ppm混入饲料连续饲喂的方式,对105只人工感染旋毛虫的大白鼠,在不同感染期采用长短不同的给药时间。结果表明:不同感染期的旋毛虫肌幼虫以甲苯咪唑(150ppm)与丙硫苯咪唑(150ppm)联合给药疗效最佳,其次为甲苯咪唑。较经济的给药时间为:感染期在40～90天之间,横纹肌感染量为2343条/克,给药10天;感染期在90～165天之间,横纹肌感染量为2080条/克,给药15天,感染165天以上,横纹肌感染量为2080条/克,给药20天。 相似文献
4.
Virkel G Lifschitz A Sallovitz J Inza G Lanusse C 《Veterinary journal (London, England : 1997)》2004,167(3):265-271
The benzimidazole (BZD) anthelmintics, netobimin (NTB) pro-drug and albendazole sulphoxide (ABZSO) are reduced to albendazole (ABZ) by ruminal microflora. The aim of the current work was to evaluate the influence of the ionophore monensin (MON) on the in vitro biotransformation of NTB and ABZSO by sheep ruminal fluid. Ruminal fluid, collected from Corriedale sheep, was preincubated (24 h) either without (control) or with known MON concentrations (0.5, 1.5 and 3.0 microg/mL) at 38 degrees C under a CO2 atmosphere. Afterwards, aliquots from both MON-pretreated and control ruminal fluid samples were incubated (30 and 60 min) with 2 microg/mL of either NTB or ABZSO. Incubated samples were chemically extracted and analysed by High Performance Liquid Chromatography to quantify the metabolites formed. The rate of ABZ production after 30 min of NTB incubation with control ruminal fluid was 0.023 microg/min. Conversely, the rates of ABZ formation were significantly (P<0.05) lower (0.009, 0.011 and 0.013 microg/min) when NTB was incubated with ruminal fluid pretreated with MON (at 0.5, 1.5 and 3.0 microg/mL, respectively). After both incubation periods, the reduction of ABZSO to ABZ was 22 to 70% lower when the ruminal fluid was preincubated with the different MON concentrations. The lower ABZ production observed in the presence of MON may result in a modified availability of this molecule in the gastrointestinal (GI) tract and hence, on its anthelmintic efficacy against GI nematodes. 相似文献
5.
Capece BP Afonso SM Lazáro R Harun M Godoy C Castells G Cristòfol C 《Research in veterinary science》2009,86(3):498-502
The kinetics of albendazole metabolites and albendazole sulphoxide enantiomers were studied in 2- and 14-month-old female and male goats, after a single oral dose administration (10 mg/kg) of an albendazole formulation. Blood samples from the jugular vein were collected at 0.5, 1, 2, 4, 6, 8, 10, 12, 16, 20, 24, 30, 36, 42, 48 and 54 h post-treatment and analyzed using a high performance liquid chromatography method. In all groups the area under the plasma concentration-time curve (AUC) and peak concentration (Cmax) values of (+)-ABZSO were significantly higher than those of (−)-ABZSO. The AUC and Cmax values obtained for (+)-ABZSO and (−)-ABZSO in adult animals were higher compared to the results in young animals, showing significant differences except for (+)-ABZSO in female animals. In young animals, independently of gender, the Cmax appeared earlier compared to adult animals. The mean residence time (MRT) values were shorter in young animals compared to adult animals for all compounds analyzed. No sex-related differences were found for any of the parameters calculated except for the (+)-ABZSO from adult animals. 相似文献
6.
Solana H Scarcella S Virkel G Ceriani C Rodríguez J Lanusse C 《Veterinary research communications》2009,33(2):163-173
Fascioliasis causes important economic losses in ruminant species all over the world. Its control is largely based on the
use of the flukicidal compound triclabendazole (TCBZ). However, its chemically related benzimidazole anthelmintic albendazole
(ABZ) is being successfully used to control TCBZ-resistance flukes. This research gains some insights into the comparative
molecular behaviour of both anthelmintics within the target fluke. The goals of the current work were: (i) to assess the competitive
binding of ABZ and TCBZ to cytosolic proteins of F. hepatica, and (ii) to evaluate the enantioselective biotransformation of ABZ in microsomal fractions obtained from TCBZ-susceptible
and TCBZ-resistant strains of the liver fluke. Cytosolic proteins from fluke specimens bound TCBZ with greater affinity (83%)
than ABZ (44%) and the fraction of TCBZ bound to cytosolic proteins was not displaced by ABZ. The microsomes from both -susceptible
and resistant flukes sulphoxidized ABZ into ABZ sulphoxide (ABZSO). However, this oxidative activity was 49% higher in microsomes
from TCBZ-resistant flukes (P < 0.001) with a predominant production of the (+) ABZSO enantiomer. As earlier shown for TCBZ,
the results reported here confirm an enhanced ability for ABZ oxidation in TCBZ-resistant flukes. While this enhanced oxidative
metabolism of ABZ may cooperate to the resistance phenomenon, other pharmacodynamic-based mechanisms may be involved, which
would explain why, although being chemically-related, ABZ remains efficacious against TCBZ resistant flukes under field conditions. 相似文献
7.
乌鲁木齐地区育肥羊消化道线虫对阿苯达唑的抗药性检测研究 总被引：2，自引：1，他引：1
临床上由于过于频繁的使用阿苯达唑(Albendazole),因此出现了抗药现象,其在推荐剂量5～15 mg/kg的基础上,有的养殖者已将其提高到使用剂量的5～10倍,但仍有效果不佳的报道,我国对消化道线虫抗药性的认识往往是通过驱虫效果来判断的,考虑到假冒伪劣药物的问题和人为因素,这种判断往往不真实,通过虫卵孵化试验(Egg Hatch Test,EHT)利用阿苯达唑分析纯试剂对乌鲁木齐地区两个育肥羊场饲养的羊体内寄生的消化道线虫的抗药性进行了检测,检测结果通过统计分析显示育肥羊感染的消化道寄生虫,特别是奥斯特线虫(Ostertagia.spp)对阿苯哒唑产生了相当严重的抗药性. 相似文献
8.
以阿苯达唑为原料,采用一锅合成法,通过氧化、酸化反应得到目标产物盐酸阿苯达唑亚砜。以丙酮为反应溶剂,当阿苯达唑和盐酸的投料比为30 g∶13 mL,阿苯达唑和双氧水的投料比为1∶1.01(n∶n),反应时间为30 min时,制备的盐酸阿苯达唑亚砜的收率为95.78%,通过IR、1H-NMR1、3C-NMR和ESI-MS分析对其产物结构进行了确证。 相似文献
9.
三种药物对猪棘头虫LDH同工酶的抑制试验 总被引：1，自引：0，他引：1
根据猪棘头虫与宿主（猪）血清的ＬＤＨ同工酶的差异，用０．１％硝硫氰醚、０．１％丙硫咪唑和０．１％吡喹酮分别对猪棘头虫雄虫、雌虫和猪血清的ＬＤＨ同工酶进行了抑制试验，结果除硝硫氰醚对蛭形巨吻棘头虫雄虫、雌虫的ＬＤＨ同工酶有抑制作用外，其余的试验组与对照组均无差异。硝硫氰醚对雄虫ＬＤＨ同工酶的第２、３、４带和雌虫ＬＤＨ同工酶的第２、３带有不同程度的抑制作用，特别是雌虫ＬＤＨ同工酶的第２带最敏感，在０．１％的浓度下，该酶带被完全抑制，即没显示出来，硝硫氰醚对雄虫和雌虫ＬＤＨ同工酶的极弱带（它们各自的第１带）均无抑制作用；临床实验也显示出硝硫氰醚对治疗猪棘头虫病有一定疗效，这些表明硝硫氰醚抑制蛭形巨吻棘头虫的ＬＤＨ同工酶活力可能是该药物对该虫体的作用机理之一。 相似文献
10.
测定丙硫唑和溴菌腈对芒果细菌性角斑病菌（Xanthomonas campestris pv. Mangiferaeindicae）的联合毒力及其田间防治效果。结果表明,丙硫唑与溴菌腈对芒果细菌性角斑病菌EC50值分别为2.869 μg/mL和0.206 μg/mL,当质量比为1:2混配时毒力增效作用最明显,增效系数为1.595,其EC50值为0.187 μg/mL;二者以75 g/hm2与150 g/hm2（有效成分质量比1:2）进行田间桶混处理15 d,防效达80%以上,显著高于单剂防效。 相似文献