两种药物治疗广州管圆线虫病的效果观察

目的　观察阿苯哒唑和甲苯咪唑治疗广州管圆线虫病的效果。　方法　以大白鼠为动物模型 ,用不同剂量和不同疗程的阿苯哒唑和甲苯咪唑进行治疗 ,然后解剖检虫、计数、观察 ,同时对广州管圆线虫病病人进行治疗。　结果　阿苯哒唑和甲苯咪唑总剂量达 12 0 mg/ kg时可杀死鼠体内的虫体 ;总剂量为 6 0 mg/ kg,疗程达 6 d时 ,也可杀灭虫体。但总剂量也为 6 0 mg/ kg而疗程只有 3d或总剂量 <6 0 mg/ kg时 ,部分虫体仍可存活 ,但虫体的发育受到严重影响 ,无法达到性成熟 ,不能产卵。对部分确诊的广州管圆线虫病病人进行治疗也收到很好的效果。　结论　阿苯哒唑和甲苯咪唑两种药物对广州管圆线虫病有显著的疗效。     

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。     

4种药物单用或联用治疗大鼠华支睾吸虫感染的实验研究

目的观察三苯双脒(TBD)、青蒿琥酯(AS)、阿苯达唑(ABZ)、甲苯咪唑(MBZ)单用或联用治疗感染华支睾吸虫大鼠的疗效。方法 140只大鼠各感染华支睾吸虫囊蚴100个,于感染后第5周开始分组治疗,均采用灌胃给药。感染大鼠随机分为药物治疗组同批感染对照组(每组5～10只),将TBD、AS、ABZ与MBZ分别按照高、低剂量单剂用药和两两配伍给药,顿服,观察疗效。治疗后10d处死大鼠,解剖,收集胆管和肝组织内的华支睾吸虫,计算平均虫数和减虫率,对相应组间的平均虫数进行单因素方差分析。结果感染华支睾吸虫大鼠用75mg/kg体重TBD、MBZ、ABZ单剂治疗后,平均减虫率分别为98.04%、100%和86.67%,30mg/kg体重AS治疗后减虫率为87.25%;当给药剂量均降低1/3时,上述各药物治疗组的平均减虫率分别降至78.3%、46.02%、31.94%和62.07%。50mg/kg体重TBD分别与50mg/kg体重MBZ、ABZ配伍用组平均减虫率为98.43%和100%,检虫数与75mg/kg体重TBD、MBZ、ABZ单用药组比较,差异有统计学意义(P<0.05)。20mg/kg体重AS分别与50mg/kg体重ABZ、50mg/kg体重MBZ配伍用,平均减虫率为89.22%和97.55%,检虫数与75mg/kg体重ABZ、MBZ,30mg/kg体重AS单用药组比较,差异有统计学意义(P<0.05)。结论联合用药可降低给药剂量,并具有增效作用,50mg/kg体重TBD分别与50mg/kg体重MBZ、ABI配伍用对治疗大鼠华支睾吸虫病疗效较好。     

甲苯达唑、阿苯达唑及其代谢物实验治疗小鼠继发性细粒棘球蚴病的研究

在疗程为10～14d时,甲苯达唑对小鼠继发性细粒棘球蚴病的最低有效剂量为25mg/kg/d,阿苯达唑的为100mg/kg/d。在所用的疗程下,甲苯达唑的剂量较阿笨达唑100～300mg/kg/d低3～11倍时,它们的疗效相仿,但甲苯达唑100mg/kg/d的疗效则优于剂量大l～2倍的阿苯达唑。甲苯达唑与阿苯达唑合并治疗未能明显提高疗效,但此2种药物并用吡喹酮治疗则疗效明显提高。实验证明阿苯达 唑亚砜的疗效优于阿苯达唑,而阿苯达唑用则无效。     

Comparison of albendazole, mebendazole and praziquantel chemotherapy of Echinococcus multilocularis in a gerbil model.

The efficacy of albendazole (50 mg/kg/d), mebendazole (50 mg/kg/d) and praziquantel (500 mg/kg/d) against established intraperitoneal infections of Echinococcus multilocularis in gerbils was compared by monitoring parasite weight and making ultrastructural observations on treated and untreated material. Praziquantel was the most active protoscolicidal agent, reducing protoscolex viability to less than 2%, although it did not inhibit cyst growth. Albendazole was the most effective agent in reducing cyst growth and was, when compared with other regimes significantly more effective than mebendazole (p less than 0.05), praziquantel (p less than 0.01) or untreated controls (p less than 0.01).     

吡喹酮、阿苯达唑和甲苯达唑对小鼠细粒棘球蚴生发膜超微结构的影响

小鼠感染的细粒棘球蚴囊经吡喹酮、阿苯达唑和甲苯达唑治疗后,其生发膜的超微结构均示有广泛的变化,主要是皮层基质变性、溶解和空泡变化;皮层细胞核周胞质的溶解、空泡形成,线粒体密集、变性、肿大,间质及肌束的广泛或局灶性溶解,以及囊腔面的溶解和脱落。甲苯达唑和阿苯达唑尚可引起角质层的损害及核染色质减少等。     

吡喹酮合并阿苯达唑治疗华支睾吸虫病的效果观察

采用吡喹酮１８０ｍｇ／ｋｇ、阿苯达唑９０ｍｇ／ｋｇ及吡喹酮９０ｍｇ／ｋｇ合并阿苯达唑４５ｍｇ／ｋｇ，３ｄ分服，每日３次，分别治疗华支睾吸虫病患者６６例、６２例和７４例，治后１个月粪检虫卵阴转率依次为９８．５％（６５／６６），６１．３％（３８／６２）和８７．８％（６５／７４）；未转阴者的虫卵减少率分别为９９．７％，６５．０％和９７．３％。吡喹酮合并阿苯达唑治疗组的疗效虽稍逊于吡喹酮治疗组，但其对轻、中度感染者的疗效仍较满意，且药物副反应少而轻，对合并感染钩虫、蛔虫和鞭虫等肠道线虫的患者亦有很好的疗效。     

甲苯达唑、阿苯达唑和吡喹酮实验治疗小鼠继发性细粒棘球蚴病的观察

小鼠于感染继发性细粒棘球蚴后用甲苯达唑口服治疗,剂量为12.5～100mg/kg/d×10时囊肿抑制率为49.2～77.5％,用阿苯达唑100～300mg/kg/d×10～14治疗的为61.3～72.1％,而用吡喹酮400mg/kg/d,或800mg/kg/d,2次均服,疗程为10d时则无效,但若给服500mg/kg/d×14,囊肿抑制率为63.4％。药物有效各组的每鼠平均囊数,除个别组外,均较相应对照组的为少。此外,甲苯达唑与吡喹酮合并服用,有一定的增效作用。     

A comparative trial of albendazole alone versus combination of albendazole and praziquantel for treatment of Trichuris trichiura infection

A randomized clinical trial was conducted to compare the effectiveness of albendazole alone and albendazole combined with praziquantel in the treatment of Trichuris trichiura infection. The drug regimens consisted of single dose of albendazole 400 mg (A1, n=34), 3 days of albendazole 400 mg daily (A3, n=34), 5 days of albendazole 400 mg daily (A5, n=35), single dose of albendazole 400 mg plus praziquantel 40 mg/kg (AIP1, n=34), and 3 days of albendazole 400 mg plus praziquantel 40 mg/kg daily (A3P3, n=36). It was found that treatment with 3 or more consecutive days of albendazole with or without praziquantel resulted in a significant reduction in density of Trichuris eggs in stools while a single dose of such drug did not. Praziquantel was not shown to have synergistic or antagonistic effects with albendazole. A regimen of 400 mg of albendazole daily for 3 days was found to be the most suitable therapy for Trichuris infection.     

三苯双脒、青蒿琥酯、蒿甲醚和吡喹酮单剂、多剂或联合用药治疗大鼠华支睾吸虫感染的实验研究

目的 观察三苯双脒、青蒿琥酯、蒿甲醚、或吡喹酮单剂、多剂给药,及其伍用治疗感染华支睾吸虫大鼠的疗效。 方法 147只SD大鼠各感染50个华支睾吸虫囊蚴,于感染后42～44 d分组治疗。各药物采用灌胃给药。①60只感染大鼠随机分为11组（每组4～5只）,分别为三苯双脒150 mg/kg（顿服）、75 mg/（kg·d）×2 d、50 mg/（kg·d）×3 d和25 mg/kg（tid）×2 d组;吡喹酮150 mg/kg（顿服）、75 mg/（kg·d）×2 d和25 mg/kg（tid）×2 d;青蒿琥酯或蒿甲醚75 mg/kg（顿服）和37.5 mg/（kg·d）×2 d组。②另87只感染大鼠随机分为15组（每组4～6只）,用青蒿琥酯或蒿甲醚（30 mg/kg）分别与吡喹酮（150 mg/kg）、三苯双脒（50 mg/kg和75 mg/kg）伍用组;三苯双脒（50 mg/kg）与吡喹酮（150 mg/kg）伍用组;三苯双脒（75 mg/kg）与吡喹酮（187.5 mg/kg）伍用组,及各药的单用组。并设同批感染未治疗对照组。受治鼠于治疗后2周剖杀,收集胆管和肝组织内的残留华支睾吸虫,计算各组的平均虫数和减虫率,用非参数统计方法（Mann-Whitney秩和检验）对相应组间的平均虫数进行分析。 结果 感染华支睾吸虫的大鼠口服单剂三苯双脒或吡喹酮（150 mg/kg）的减虫率分别为57.2%和63.8%。三苯双脒各小剂量多次给药组的减虫率稍高,达77.1%～79.4%,而吡喹酮小剂量多次给药组的减虫率则为50.6%～54.2%。但两种药物各组间的平均虫数的差异无统计学意义。青蒿琥酯和蒿甲醚各单剂给药组与小剂量多次给药组的减虫率均较高,分别为90.4%～98.5%和100%。三苯双脒小剂量（50或75 mg/kg）与吡喹酮（150 mg/kg 或187.5 mg/kg）伍用治疗,减虫率为74.9%～100%,高于其各单药组的减虫率（26.9%～79.6%）。青蒿琥酯或蒿甲醚小剂量（30 mg/kg）与吡喹酮（150 mg/kg）或三苯双脒（50或75 mg/kg）伍用治疗,减虫率为74.9%～97.9%,亦高于其各药组的减虫率（24.8%～79.6%）。 结论 青蒿琥酯、蒿甲醚、吡喹酮和三苯双脒均为有效的抗华支睾吸虫药物,各药物小剂量伍用具有增效作用。     

日本血吸虫病与肠线虫病联合化疗的效果

血吸虫病人合并感染肠线虫者(A组)采取;吡喹酮40mg/kg加阿苯达唑200mg和复方甲苯咪唑400mg(尚含左旋咪唑100mg)分2d顿服,1个半月后血吸虫阴转率88.0％,蛔虫、鞭虫和钩虫阴转率分别为77.4％、23.6％及100.0％。对不合并血吸虫病的肠线虫病患者采取两种联合化疗方案:B组—阿苯达唑200mg和复方甲苯咪唑200mg(尚含左旋咪唑50mg)顿服,蛔虫、鞭虫和钩虫的阴转率分别为66.7％、18.8％和62.5％,较A组结果稍低;C组—阿苯达唑100mg和噻嘧啶900mg顿服的驱虫效果差,蛔虫和鞭虫的阴转率分别为50.0％及11.1％。3种驱虫方案对血吸虫和蛔虫的减卵率可达97.0％～99.9％;对钩虫的减卵率达68.9％～100％;对鞭虫的效果差。相应增加药物的剂量及改进服法,当可提高疗效。     

Human fascioliasis successfully treated with triclabendazole

Fascioliasis, caused by the common liver fluke Fusciolu hepatica , is an endemic infection in sheep and cattle in many parts of Australia. Infections in humans in Australia have been reported infrequently and the most appropriate therapy for human fascioliasis remains to be determined. This case report describes a patient with the infection unsuccessfully treated with multiple high doses of praziquantel, mebendazole or albendazole. The infection was successfully eliminated by the administration of triclabendazole in two single doses of 900 mg (12 mg/kg) two days apart. No side effects were observed after the treatment. Based on our experience and that recently reported in the literature, triclabendazole may be regarded as the drug of choice for the treatment of human fascioliasis. (Aust NZ J Med 1992; 22: 45–47.)     

甲苯达唑、阿苯达唑和吡喹酮对继发性细粒棘球蚴囊液游离氨基酸含量的影响

对感染了继发性细粒棘球蚴的小鼠，于吡喹酮（Ｐｒａ）５００ｍｇ／ｋｇ／ｄ、甲苯达唑（Ｍｅｂ）２５ｍｇ／ｋｇ／ｄ或阿苯达唑（Ａｌｂ）３００ｍｙｋｇ／ｄ治疗１４天后，取包囊液测定了其中１８种游离氨基酸的含量，发现吡喹酮组小鼠囊液中有２种氨基酸的浓度高于对照组，有３种氨基酸的浓度低于对照组。而甲苯达唑组和阿苯达唑组囊液中的氨基酸浓度均低于对照组，其中各有１４种和１３种氨基酸含量明显低于对照组，表明甲苯达唑和阿苯达唑可干扰细粒棘球蚴囊的氨基酸代谢。     

Evaluation of the therapeutic effect of albendazole on experimental and human infections by Hymenolepis nana

With the objective of knowing adequately the spectrum of activity of albendazole against intestinal helminthiases, we made observations regarding hymenolepiasis caused by Hymenolepis nana. Two series of investigations were carried out: a) treatment of mice with single doses of either 25 or 50 mg/kg, repeated after ten days, using as controls animals treated with 25 mg/kg of praziquantel or not treated with any antiparasitic drugs; b) treatment of adults and children with 400 mg daily for three consecutive days, repeated after ten days.     

土源性线虫感染的化学治疗研究

在湖南省衡山县对常用驱虫药的疗效进行了研究。所用药物为阿苯达唑(400mg,单剂)、复方甲苯达唑(甲苯达唑100mg和左旋咪唑25mg bid×3d)、复方噻嘧啶(噻嘧啶与酚嘧啶各150mg,bid×2d)及噻嘧啶(10mg基质/kg,单剂)。给药后2wk的疗效显示前3种药物剂量组蛔虫感染者治愈率(CR)为97.5—100.0％,后者为80.9％;对钩虫感染者的CR分别为95.4％、78.6—100％、96.7％和83.3％,服药后4wk复查显示上述4个药物剂量组的CR无显著性差异。根据对鞭虫感染的CR来判断,以复方噻嘧啶为佳(89.3％),其次为复方甲苯达唑(64.6—83.8％),阿苯达唑再次之(28.2—42.6％),噻嘧啶无效。上述药物除噻嘧啶外,治疗鞭虫感染时虫卵减少率均显著。     

Pharmacokinetic investigation of albendazole and praziquantel in Thai children infected with Giardia intestinalis

The pharmacokinetics of albendazole/albendazole sulphoxide and praziquantel were investigated in Thai children with Giardia infection. Twenty school-age children were randomly allocated to receive either a single oral dose of albendazole (400 mg/child) or the same dose of albendazole given concurrently with a single oral dose of praziquantel (20 mg/kg). The concentrations of albendazole/albendazole sulphoxide and praziquantel in plasma samples, collected at intervals in the first 24 h post-treatment, were then quantified using HPLC with ultra-violet detection. No significant pharmacokinetic interaction between the albendazole and praziquantel was demonstrated. For albendazole sulphoxide, the active metabolite of albendazole, there was marked inter-individual variation in the maximum plasma concentration and the 'area under the curve'. The pharmacokinetics of albendazole sulphoxide were similar whether albendazole was given alone or in combination with praziquantel.     

Studies on taeniasis in Taiwan. V. Field trial on evaluation of therapeutic efficacy of mebendazole and praziquantel against taeniasis

Taeniasis is a major public health problem among the aboriginal populations on Taiwan, and is highly prevalent and wide spread in the mountain areas of 10 Counties. Over 27,000 cases of tapeworm infection are estimated influencing the health and economy in the endemic areas. A treatment of taeniasis with mebendazole and praziquantel followed by a re-treatment with atabrine has been done in the field trial, and confirmed that praziquantel is highly effective agent against tapeworm infection, but mebendazole is not. Based upon experiments reported here praziquantel in a single dose of 150 mg, and 450 mg are highly effective against taeniasis and hymenolepiasis respectively.     

Albendazole in the treatment of intestinal capillariasis

Albendazole or Zentel a benzimidazole derivative, was used to treat intestinal capillariasis in hospitalized patients seen in Northern Luzon in the Philippines. In initial studies, four patients responded satisfactorily to the drug in dosages of 400 mg/day in divided doses for 20 days. This is the same dosage used for mebendazole, which has been the drug of choice in treating the parasitosis. In further studies, 16 patients with Capillaria philippinensis, were treated with 400 mg/day of the drug for 10 days, and 15 were completely cured. The one treatment failure was found to be passing eggs of the parasite three months later, and was retreated with the standard mebendazole regimen of 400 mg/day for 20 days. Side effects attributed to albendazole were not reported in any of the patients. Albendazole, 400 mg/day in two divided doses, is now the recommended drug of choice in Northern Luzon in the Philippines.     

Benzimidazole treatment of cystic echinococcosis

Hydatidosis (cystic echinococcosis, CE) constitutes a serious public health problem worldwide. Total surgical removal of a hydatid cyst is still considered the gold standard treatment for CE. Percutaneous treatment (PAIR), using either hypertonic saline or alcohol as a larvacidal agent, appears to be an additional effective form of treatment. Benzimidazoles (albendazole, ABZ; mebendazole, MBZ), given either alone or combined with praziquantel (PZ) are currently used for the treatment of non-surgical cases and as a supplementary treatment prior and post-surgery. Combined chemotherapy was found to be more effective than either of the agents given alone. ABZ is easily absorbed and more effective than MBZ. ABZ (12-15 mg/kg/day) and MBZ (30-70 mg/kg/day) given for 14-20 days prior to surgery and continued for an additional 3-24 months in a cyclic monthly form were found effective against the disease. Either increased or decreased circulating antigen levels, which consequently cause changes in the humoral (IgG, IgG1, IgG4, IgE) immune responses, have a prognostic value in successfully treated CE cases. However, although the cellular immune response to echinococcal antigens decreased in improved or cured CE patients, it was not considered of practical use in determining treatment efficacy. In certain cases successful treatment was also followed by elevated eosinophilia and erythrocyte sedimentation rates. In the present article, the mechanism of drug activities as well as the development of resistance against the drugs available are further discussed.     

不同药物不同途径预防小鼠日本血吸虫感染的效果比较

目的　比较吡喹酮等药物不同途径预防小鼠日本血吸虫感染的效果。　方法　将吡喹酮、氯硝柳胺、丙硫咪唑和中药 W按一定剂量单独或配伍对小白鼠灌胃给药 ,进行 12 h预防日本血吸虫感染试验。同时进行含不同剂量不同透皮促进剂 (二甲亚砜、Azone、1,2 -丙二醇 )吡喹酮霜剂的小鼠 12 h或 2 4 h皮涂防护试验 ,并用环卵沉淀试验 (COPT)检测皮涂小鼠血清抗血吸虫抗体。　结果　皮涂各组减虫率均为 10 0 % ,可达 12 h或 2 4 h完全防护 ,透皮促进剂中 Azone用量少且无臭 ,COPT灵敏度和特异度均较高。灌胃各组比较 ,中药 W减虫效果明显 ,但毒性较大 ;吡喹酮单用及合用效果均好于氯硝柳胺 ,且吡喹酮与丙硫咪唑合用有一定增效作用 ,其中吡喹酮 14 0 m g/ kg合并丙硫咪唑 6 0 mg/ kg可达 12 h完全防护。　结论　皮涂吡喹酮霜剂效果好于口服预防 ,透皮剂中 Azone较理想 ,口服预防联合用药可降低剂量和毒性 ,提高防护效果。