Effect of mebendazole againstEchinococcus granulosus andTaenia hydatigena cysts in naturally infected sheep and relevance to larval tapeworm infections in man

The ability of three treatment schedules of mebendazole to kill well-established hydatid cysts was studied. Pregnant sheep, naturally infected withEchinococcus granulosus and/orTaenia hydatigena, were treated daily with mebendazole at a dose rate of 50 mg/kg body weight for either five days, one month, or three months.At autopsy, seven months after the commencement of treatment, no evidence was found that the 5-day treatment schedule had any damaging effect onE. granulosus cysts. The effects of the one month treatment were equivocal. There was evidence of a damaging effect from the 3-month treatment schedule and protoscoleces were not infective to dogs. NoT. hydatigena cysts survived the 1- and 3-month treatments, but organisms from the 5-day treatment were infective to dogs.These results forE. granulosus in sheep suggest that long-term treatment with mebendazole may be required in hydatid disease in man. The results obtained forT. hydatigena in sheep are discussed in relation to the treatment of cysticercosis fromT. solium in man. Mebendazole showed no untoward effect on the sheep or their lambs.     

甲苯咪唑微丸质量标准的研究

目的：建立对甲苯咪唑微丸进行定性鉴别和含量测定的方法。方法：采用薄层层析法进行定性鉴别,用紫外分光光度法进行含量测定。结果：含量测定方法平均回收率为１００．６％ , Ｒ Ｓ Ｄ＝ １．７２％ 。结论：所用方法简便可靠,可控制甲苯咪唑微丸的质量。     

5-Nitroimidazole refractory giardiasis is common in Matanzas,Cuba and effectively treated by secnidazole plus high-dose mebendazole or quinacrine: a prospective observational cohort study

ObjectiveTo evaluate the effectiveness and tolerability of secnidazole combined with high-dose mebendazole for treatment of 5-nitroimidazole-resistant giardiasis.MethodAdults with microscopically verified Giardia intestinalis monoinfection attending a secondary level hospital in Matanzas City, Cuba were prospectively included in a cohort. A recently introduced treatment ladder consisting of metronidazole as first-line treatment, followed by secnidazole, tinidazole, secnidazole plus mebendazole and quinacrine as second-to fifth-line treatments, respectively, was used. Adverse events and treatment success were determined by questioning and microscopy on concentrated stool samples, respectively on days 3, 5 and 7 after the end of treatment. If G. intestinalis was detected on day 3, 5 or 7, then the infection was classified as refractory and no further microscopy was performed.ResultsA total of 456 individuals were included. Metronidazole, 500 mg three times daily for 5 days, cured 248/456 (54%) patients. A single 2-g secnidazole dose as second-line treatment cured 50/208 (24%) patients. A single 2-g tinidazole dose as third-line treatment cured 43/158 (27%) patients. Three rounds of 5-nitroimidazole therapy therefore cured 341/456 (75%) patients. Secnidazole plus mebendazole (200 mg every 8 hours for 3 days) cured 100/115 (87%) of nitroimidazole refractory infections. Quinacrine cured the remaining 15 patients. All treatments were well tolerated.Conclusions5-Nitroimidazole refractory giardiasis was common, indicating that an alternative first-line treatment may be needed. Retreatment of metronidazole refractory giardiasis with an alternative 5-nitroimidazole was suboptimal, indicating cross-resistance. Mebendazole plus secnidazole were well tolerated and effective for the treatment of 5-nitroimidazole refractory G. intestinalis infection in this setting.     

Evaluation of in-vitro anthelmintic activity of Heliotropium indicum Linn. leaves in Indian adult earthworm

ObjectiveTo carry out an exhaustive study with a view to substantiate the therapeutic potential of the plant in terms of its anthelmintic activity against Pheretima posthuma using mebendazole as a reference standard.MethodsForty five worms were collected and were divided into nine groups and were washed in normal saline before they were released into 10 mL of respective drug solutions using distilled water as vehicle. Different concentrations (25 mg/mL, 50 mg/mL and 100 mg/mL) of the test (MEHI and AEHI) and standard solution were prepared before the commencement of the experiment. Time for paralysis and time for death were recorded for each group.ResultsCrude methanolic extract with concentrations of 25 mg/mL, 50 mg/mL, 100 mg/mL produced dose-dependent paralysis. Time of paralysis and death increased with concentration of 25 mg/mL, 50 mg/mL as compared with that of standard drug mebendazole. Methanolic extract of Heliotropium indicum Linn. (H. indicum) gave shorter paralysis and death time at 100 mg/mL as compared to aqueous extract H. indicum Linn. Results are expressed as mean±SEM (P<0.05) of 5 worms in each group.ConclusionsFrom the investigation, conclusion can be drawn that the methanolic extract of H. indicum (Boraginaceae) showed better activity than aqueous extract of the same to treat intestinal worm infections. In comparison with the standard drug mebendazole, methanolic extract of H. indicum showed significant anthelmintic efficacy.     

钩虫低感染人群目标化疗效果的初步观察

对钩虫低感染人群目标化疗效果进行了初步观察,结果对钩虫感染率较高的年龄组(>41岁)进行一次目标化疗一年后下降率42.16%,这与以前感染程度最高的村集体化疗一年后的下降率45.33%相当。因此,在肠线虫病防治后期,可以有针对性地结合当地肠线虫病流行特点,采取不同的目标化疗措施,可以合理使用药物和发挥更大的驱虫效果,减少实施过程中的工作量和药物耗量以及延缓药物抗性的产生,起到事半功倍的作用。     

Simultaneous quantitative analysis of mebendazole polymorphs A–C in powder mixtures by DRIFTS spectroscopy and ANN modeling

In the present study, a simple method, based on diffuse reflectance FTIR spectroscopy (DRIFTS) and artificial neural network (ANN) modeling is developed for the simultaneous quantitative analysis of mebendazole polymorphs A–C in powder mixtures. Spectral differences between the polymorphs are elucidated by computationally assisted band assignments on the basis of quantum chemical calculations, and subsequently, the spectra are preprocessed by calculation of 1st and 2nd derivatives. Then ANN models are fitted after PCA compression of the input space. Finally the predictive performance of the ANNs is compared with that of PLS regression. It was found that simultaneous quantitative analysis of forms A–C in powder mixtures is possible by fitting an ANN model to the 2nd derivative spectra even after PCA compression of the data (RMSEP of 1.75% for form A, 1.85% for B, and 1.65% for C), while PLS regression, applied for comparison purposes, results in acceptable predictions only within the 700–1750 cm⁻¹ spectral range and after direct orthogonal signal correction (DOSC), with RMSEP values of 2.69%, 2.68%, and 3.40% for forms A, B, and C, respectively. Application of the ANN to commercial samples of raw material and formulation (suspension) proved its suitability for the prediction of polymorphic content.     

甲苯达唑糖片驱除肠道线虫的效果观察

用甲苯达唑糖片以含药量１０Ｏｍｇ顿服驱除蛲虫，３００ｍｇ２ｄ分服驱除蛔虫，效果均很满意，排虫高峰分别于服药后的第２～３ｄ和第４～５ｄ，治毕３ｗｋ复查，虫卵阴转率分别为１００％和９８％～１００％。采用３００ｍｇ或４００ｍｇ２ｄ分服驱除钩虫和鞭虫，亦取得较好的疗效，排虫高峰分别于服药后的第２～４ｄ和第４～６ｄ，但从虫卵阴转率来看，药物剂量尚属偏低。该药糖片服用方便，效果确实，成本低廉，很受群众欢迎，儿童尤为喜欢，值得推广使用。     

吡喹酮、甲苯达唑及阿苯达唑对细粒棘球蚴作用的组织化学比较

本文比较了吡喹酮、甲苯达唑及阿苯达唑对NIH鼠体内细粒棘球蚴组织化学的影响。结果表明,三种药物治疗3～14天,均能迅速引起生发层内糖原、AKP、ACP及ATP酶的减少、减弱或消失,以甲苯达唑组的为最明显,阿苯达唑及吡喹酮的较轻,但对生发层内DNA、RNA、蚤白质结合的酪氨酸、色氨酸、组氨酸以及碱性蛋白质的影响仅见于7及14天。亦以甲苯达唑组的较为显著。停药后,上述变化的恢复时间,吡喹酮及阿苯达唑的分别为14～30及30天,而甲苯达唑组的则需90天。     

甲苯咪唑杀广州管圆线虫成虫的效果观察

目的观察甲苯咪唑对广州管圆线虫成虫的杀灭效果。方法用广州管圆线虫感染大鼠70d后，将其分为3组：1）甲苯咪唑组：用灌胃的方法给予甲苯咪唑50mg／kg，1次／d，连续2d；2）吡喹酮＋甲苯咪唑组：第1d灌服吡喹酮1次，剂量为300mg／kg；第4d和第5d灌服甲苯咪唑，给药剂量和次数同甲苯咪唑组；3）对照组：灌胃生理盐水。给药结束后第6d分别剖杀实验大鼠，分离、记数、观察广州管圃线虫成虫。结果甲苯咪唑组的减虫率为28．32％，虫荷数与对照组比较差异有显著性（P=0．0445）；吡喹酮＋甲苯咪唑组与甲苯咪唑组比较，减虫率差异无显著性（P=0．999）。结论甲苯咪唑对广州管圆线虫成虫有效，但杀灭效果较差。吡喹酮和甲苯咪唑联用对广州管圆线虫成虫无明显协同杀灭效应。     

Cytotoxicity of mebendazole against established cell lines from the human,rat, and mouse liver

The direct cytotoxicity of mebendazole (MBZ) was investigated by using cell lines derived from human, mouse and rat liver. It was demonstrated that Chang liver cells (derived from human liver) were more sensitive to the cytotoxic effects of MBZ than the other two cell lines. Longer incubation of the cells with MBZ resulted in stronger toxicity, and the cytotoxicity was dependent on the MBZ concentration above a certain threshold value (0.25–0.50 mg/l in a 42-h culture). Inhibition of the proliferation of Chang liver cells by MBZ was detected at a concentration of 0.008 mg/l, a lower concentration than that having a cytotoxic effect. The other two cell lines were less sensitive to the inhibitory effect of MBZ. Proliferation of human mononuclear cells following stimulation by phytohemagglutinin (PHA) was inhibited by MBZ, and this inhibition was more extensive than that of cells stimulated with whole formalin-treatedPseudomonas aeruginosa. It is suggested that dividing cells may be more sensitive to MBZ cytotoxicity. This anti-proliferative effect may be related to its clinically known side effects, such as hepatotoxicity and bone marrow suppression.