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PubMed1981

Effect of mebendazole against Echinococcus granulosus and Taenia 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 with Echinococcus granulosus and/or Taenia 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 on E. 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. No T. hydatigena cysts survived the 1- and 3-month treatments, but organisms from the 5-day treatment were infective to dogs. These results for E. granulosus in sheep suggest that long-term treatment with mebendazole may be required in hydatid disease in man. The results obtained for T. hydatigena in sheep are discussed in relation to the treatment of cysticercosis from T. solium in man. Mebendazole showed no untoward effect on the sheep or their lambs.

Animals↗
PubMed1988

[The long-term course of 60 patients with alveolar echinococcosis in continuous therapy with mebendazole (1976-85)].

Since 1976 60 patients with inoperable alveolar echinococcosis caused by Echinococcus multilocularis were treated with high doses of mebendazole and examined at regular intervals prospectively according to our protocol regarding clinical course, liver function, morphology, immunologically and plasma mebendazole levels. The average duration of disease was 8(1-19) years, the average duration of chemotherapy was 4.25 (0.75-9) years. The long term results showed a correlation of the clinical course with the mean plasma mebendazole levels and the duration of chemotherapy, respectively. Death (n = 5) or transient progression of the disease process (n = 14) was observed primarily in patients with low plasma mebendazole levels in the early course and within the first two years of chemotherapy. Only 9 patients showed a decrease of the parasite mass. Immundiagnosis (total serum IgE and serum antibodies against Echinococcus antigen) gave some information with regard to therapy results, but only in the long-term course. The cumulative survival of the patients under study was 96% at 5 years and 84% at 10 years, respectively which is markedly higher compared to historical control series with a letality of greater than 90% within 10 years.

Adult↗
PubMed2006

Pro-oxidant effects of Mebendazole in albino rats experimentally infected with Trichinella spiralis.

Trichinellosis treated with Mebendazole often leads to complications in the course of the disease in humans and animals as a result of intoxication and hyper-sensitization of an organism due to the massive destruction of parasites. This study was conducted to research Mebendazole incidence on lipid peroxidation processes (LPP) in rats' blood in Trichinella spiralis-infected and parasite-free albino rats. The research was conducted to evaluate erythrocyte superoxide dismutase (SOD) activity and malonic dialdehyde (MDA) concentration in blood serum. The parameters of the SOD-MDA system in infected albino rats, which were treated or untreated with Mebendazole were analyzed. It was concluded that Mebendazole amplifies the LPP in the blood of both infected and parasite-free animals: in a dose of 150 mg/kg anthelmintic causes disturbances of biochemical homeostasis in the SOD-MDA system, thus working as a pro-oxidant.

Animals↗
PubMed1985

Mebendazole and insulin secretion from isolated rat islets.

In a preliminary communication we reported that mebendazole, a vermicide, decreased plasma glucose and free fatty acid concentrations and increased plasma C peptide concentrations in both type II diabetic patients. Therefore, we suggested that mebendazole was an insulin secretagogue. However, these were uncontrolled studies, and improved metabolic control in these patients due to spontaneous remission rather than drug-induced insulin secretion was a possibility. To investigate the direct effect of mebendazole on insulin secretion we used intact islets isolated from normal rat pancreata. Mebendazole in concentrations as low as 10 to 20 mumol/L caused a twofold to threefold increase in acute-phase insulin release from isolated perifused rat islets. This heightened insulin release occurred in the presence of glucose-stimulated insulin secretion.

Animals↗
PubMed1994

Genotoxic activity of mebendazole in Aspergillus nidulans.

Mebendazole is an anthelmintic drug widely used in Cuba and in Mexico. Its interaction with tubulin interferes with the assemblage of the mitotic apparatus in the parasite cells, thus suggesting a possible genotoxic activity leading to chromosomal malsegregation. The heterozygous diploid strain D30 of Aspergillus nidulans was used to establish the ability of mebendazole to induce mitotic recombination and/or chromosomal non-disjunction, and the haploid strain FGSC #219 of A. nidulans was used to study the ability of mebendazole to induce point mutations in the methG suppressor system. Our results show that mebendazole can induce chromosomal non-disjunction but it fails to promote point mutations.

Analysis of Variance↗
PubMed1982

Studies on the experimental chemotherapy of Angiostrongylus malaysiensis infection in rats with mebendazole and levamisole.

The effect of levamisole hydrochloride and mebendazole on Angiostrongylus malaysiensis infection in albino rats was studied. Animals at different stages of infection were treated with various oral doses of levamisole and mebendazole with the aim of finding an effective treatment regime. Levamisole was most effective for treating rats seven days after infection but its efficacy dropped as infection progressed. Mebendazole given at a dose of 1 mg/kg for five days was more effective against early larval stages (97.39% efficacy). At 5 mg/kg for five days mebendazole was more effective than levamisole against all stages of the infection.

Angiostrongylus↗
PubMed2003

Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers.

The pharmacokinetic evaluation of guar gum-based colon-targeted tablets of mebendazole against an immediate release tablet was carried out in human volunteers. Six healthy volunteers participated in the study and a crossover design was followed. Mebendazole was administered at a dose of 50 mg both in immediate release tablet and colon-targeted tablets. On oral administration of colon-targeted tablets, mebendazole started appearing in the plasma at 5 h, and reached the peak concentration (C(max) of 25.7+/-2.6 ng/ml) at 9.4+/-1.7 h (T(max)) whereas the immediate release tablets produced peak plasma concentration (C(max) of 37.2+/-6.8 ng/ml) at 3.4+/-0.9 h (T(max)). Colon-targeted tablets showed delayed t(max) and absorption time, and decreased C(max) and absorption rate constant when compared to the immediate release tablets. The results of the study indicated that the guar gum-based colon-targeted tablets of mebendazole did not release the drug in stomach and small intestine, but delivered the drug to the colon resulting in a slow absorption of the drug and making the drug available for local action in the colon.

Adolescent↗
PubMed2003

Quality evaluation of generic drugs by dissolution test: changing the USP dissolution medium to distinguish between active and non-active mebendazole polymorphs.

Mebendazole is practically insoluble in water and studies of its polymorphism has led to the identification and characterization of three polymorphic forms (A, B, C) displaying solubility and therapeutic differences that show that polymorph C is therapeutically favored. The objective of this study was to adjust the USP dissolution test for mebendazole so that it was able to distinguish between the dissolution properties of three mebendazole polymorphs. This would provide generic manufacturers with one more test to ensure that the therapeutically active polymorph C is used. The results obtained in this study show that the USP dissolution test conditions were not able to distinguish between the dissolution properties of completely dispersed mebendazole polymorphs with comparable particle sizes. When sodium lauryl sulfate was removed from the dissolution medium, the percentage dissolved versus time profiles changed so that polymorph C dissolved faster (70% within 120 min) compared to polymorph B (37% within 120 min) and polymorph A (20% within 120 min).

Chemistry, Pharmaceutical↗
PubMed1987

In vitro effects of mebendazole on the carbohydrate metabolism of Avitellina lahorea (Cestoda).

Mebendazole (3.3 mumol), causes in vitro glycogen depletion and inhibits glucose uptake in Avitellina lahorea. Inhibition of non-specific phosphomonoesterases and adenosine triphosphatase by mebendazole discussed in the light of the role of phosphatases in uptake mechanisms. Mebendazole has no effect on hexokinase which has broad substrate specificity but influences the activities of some glycolytic enzymes such as phosphorylase, phosphoglucomutase and glucose-6-phosphatase. Thus, it appears that mebendazole also acts to disrupt certain enzymes of carbohydrate metabolism which may ultimately cause death of the parasite.

Acid Phosphatase↗
PubMed1988

Comparative efficacy of flubendazole and mebendazole on encysted larvae of Trichinella spiralis (USA strain) in the diaphragm of mice and rats.

Comparative efficacy of mebendazole and flubendazole, a p-fluor analogue of mebendazole against the encysted larvae of Trichinella spiralis (USA strain) in the diaphragm of mice and rats were studied in order to provide a better understanding of the structure-activity relationship within the benzimidazole series. Drugs given 10-100 mg/kg/day for 3 consecutive days (35-37 days post-infection) or at 300 mg/kg, 35 days post infection were significantly effective in decreasing early encysted larvae in mice. No significant differences in effectiveness against the early encysted larvae could be observed between the drugs under the present experimental conditions. Mebendazole was found to be more effective that flubendazole in decreasing old encysted larvae in mice treated 70-72 days post-infection based on a comparative study of their ED50 values. When rats were given the drugs at the dose of 10 mg/kg/day for 3 consecutive days, mebendazole was significantly effective against both early and old encysted larvae while flubendazole was not.

Animals↗
PubMed1998

Morphological changes of larval Echinococcus multilocularis in mice treated with albendazole or mebendazole.

Using DBA/2J mice, tissue homogenates of larval Echinococcus multilocularis were injected into the mesenteric veins to generate the liver infection. Mice were treated with either albendazole or mebendazole for prolonged periods to examine the morphological changes of the metacestode. Albendazole induced disorganization of both laminated and germinal layers and suppressed the maturation of vesicles. Amorphous but loosely laminated PAS-positive material was observed inside the damaged vesicles, although new vesicles slightly developed inside or outside of the damaged ones. Active proliferation of vesicles occurred after treatment with albendazole was terminated. Hydatid cysts were more severely damaged in mice treated with mebendazole and new vesicles did not develop around the damaged ones. Also, hydatid cysts reappeared after treatment with mebendazole was terminated. These results indicate that these drugs do not eliminate larval E. multilocularis in the long-term, but mebendazole has a higher suppressive effect on multivesiculation than albendazole.

Albendazole↗
PubMed2001

Comparative clinical trial of mebendazole and metronidazole in giardiasis of children.

Giardiasis and soil-transmitted helminthosis are prevalent in many parts of the world. Application of a single drug for treatment of both giardiasis and soil-transmitted helminthosis is highly desirable. One hundred children of both sexes, ranging from 7 to 12 years old with Giardia intestinalis cysts or trophozoites in their stool samples, were randomly separated into two groups of 50 individuals each. Each group received either mebendazole tablets 200 mg thrice daily for 5 days or metronidazole tablet 15 mg/kg/day in three divided doses, for 7 days. The results were evaluated by microscopic examination of stools on two successive occasions: 1 week and 2 weeks after treatment. Each occasion consisted of three stool examination on 3 successive days. The cure rate of mebendazole-treated children was 43 out of 50 (86 per cent), and for metronidazole it was 45 out of 50 (90 per cent) with no statistical difference between the two groups. No side-effects were observed in the mebendazole-treated group, whereas nausea, anorexia and metallic taste were observed in 4.9, 6 and 24 per cent of metronidazole-treated children, respectively. In conclusion, the use of mebendazole, which is less toxic with no side-effects, is available and effective on Giardia intestinalis as well as intestinal nematodes, is recommended especially in the areas where giardiasis and intestinal nematodiasis are prevalent and overlap.

Animals↗
PubMed1984

Liquid chromatography with electrochemical detection for monitoring mebendazole and hydroxymebendazole in echinococcosis patients.

A sensitive method is described for the simultaneous determination of mebendazole and hydroxymebendazole using flubendazole as an internal standard. The analytes were isolated with a single chloroform extraction from 1.0 ml of alkalinized plasma or cyst liquid samples. Separation and quantitation were performed with high-performance liquid chromatography with electrochemical detection. The limit of detection for mebendazole and hydroxymebendazole was approximately 5 and 2.5 ng/ml, respectively. The accuracy of the method was confirmed for mebendazole by a good correlation with an existing radioimmunoassay method. The method was applied for monitoring mebendazole therapy in echinococcosis patients. The results presented support the necessity of such monitoring, as most of the observed peak plasma concentrations did not reach the level regarded as minimal for therapeutic effect.

Benzimidazoles↗
PubMed1986

A correlation between serum mebendazole concentrations and the aminopyrine breath test. Implications in the treatment of hydatid disease.

In 25 patients an [14C]-aminopyrine breath test (ABT) was performed immediately before the oral administration of 1.5-2 g of mebendazole three times daily. The concentration of mebendazole in serum was measured 2 h after each drug intake. A significant correlation was found between the results of ABT and the serum drug concentrations obtained after the second and third intake, as well as the highest concentration value. The ABT was repeated in six patients during a continuous treatment with mebendazole. In all of them this test indicated an increase in 14CO2 production with continued treatment. The results support the view that mebendazole is metabolized by the liver monooxygenase activity and behaves as an enzyme inducer.

Adult↗
PubMed1996

Intracystic application of mebendazole solution in the treatment of liver hydatid disease. Preliminary report of two cases.

Mebendazole, a derivate of benzimidazole, is commonly used for the treatment of hydatid disease in patients at high operative risk and/or to prevent secondary hydatidosis. In this study, 2 cases of liver hydatid disease, in which mebendazole was used both orally and for intracystic application are presented. These cases have been treated by percutaneous drainage and videolaparoscopic methods. Mebendazole solution at a concentration of 2.4 micrograms/ml was injected into the cyst. For a period of 6 months 50 mg/kg/day oral treatment was given. At the end of a 6- to 9-month period, the total recovery was observed. This is the first report of mebendazole pair-treatment in the literature.

Adult↗
PubMed2002

Soil-transmitted nematode infections and mebendazole treatment in Mafia Island schoolchildren.

In August 2000, a cross-sectional study was performed to assess the prevalence and intensity of soil-transmitted nematode infections in schoolchildren on Mafia Island. Hookworm infection was widespread (72.5% prevalence) whereas Trichuris trichiura was less prevalent (39.7%) and Ascaris lumbricoides was present at a low prevalence (4.2%), mainly in urban areas. In a subsample of the study population, both Necator americanus and Ancylostoma duodenale were found, although N. americanus was more prevalent. This survey was followed by a parasitological evaluation of mebendazole treatment using a single, 500-mg dose. The data on outcome were used for comparison with those from recent studies of similar treatment regimens in the neighbouring island of Pemba, Zanzibar, where periodic chemotherapy with mebendazole to schoolchildren has been implemented as part of a helminth-control programme since 1994. A higher efficacy of mebendazole against hookworm infection was found in Mafia Island (where a cure 'rate' of 31.3% and an egg-reduction 'rate' of 78.1% were recorded) when compared with that observed in Pemba Island, possibly indicating that hookworms may be developing mebendazole resistance on Pemba Island as a result of intense exposure to the drug there.

Adolescent↗
PubMed1990

Theophylline and antiparasitic drug interactions. A case report and study of the influence of thiabendazole and mebendazole on theophylline pharmacokinetics in adults.

To determine a change in theophylline pharmacokinetics during concomitant thiabendazole or mebendazole therapy, we studied six normal, healthy male volunteers. Aminophylline was administered intravenously, followed by a 30-h blood sampling period. Subjects were randomized to receive thiabendazole or mebendazole, then crossed over to receive the other therapy. Theophylline concentrations were measured utilizing an HPLC technique and a one-compartment model was fit to the data. Theophylline pharmacokinetic parameters were significantly different during thiabendazole therapy. Mean theophylline half-life increased, clearance decreased and elimination rate constant decreased. Two subjects experienced severe nausea and vomiting during thiabendazole therapy. There were no significant differences in theophylline pharmacokinetic parameters during mebendazole therapy. Thiabendazole administration results in a significant decrease in theophylline clearance and beta elimination rate constant. The theophylline half-life increased significantly. Concomitant administration of theophylline and thiabendazole resulted in severe nausea and vomiting. Mebendazole administration did not seem to alter theophylline pharmacokinetics.

Adult↗
PubMed2001

A comparative study of different albendazole and mebendazole regimens for the treatment of intestinal infections in school children of Usigu Division, western Kenya.

A clinical trial to compare the effectiveness of 4- and 6-mo repeated treatment with albendazole 600 mg (Zentel, SmithKline Beecham) or mebendazole 600 mg (Vermox, Janssen) on geohelminth infections was carried out on children in 6 primary schools; the study included 1,186 children, ages 4 to 19 yr. Kato-Katz examination was performed on stool samples before and after treatment. Overall, albendazole produced better cure rates and egg reduction rates for geohelminths. The cure rates for albendazole were 92.4% for hookworm infection, 83.5% for Ascaris lumbricoides, and 67.8% for Trichuris trichiura. Mebendazole given either 2 or 3 times in a year had cure rates of 50 and 55.0% (respectively) for hookworm, 79.6 and 97.5% for A. lumbricoides, and 60.6 and 68.3% for T. trichiura infection. The geometric mean intensity of hookworm eggs per gram (epg) of stool decreased by 96.7% after albendazole treatment compared with 66.3 and 85.1%, respectively, for 2 or 3 doses of mebendazole (P < 0.05) over the same period. Reductions in epg for A. lumbricoides and T. trichiura were comparable for both drugs. Our results indicate that treatment with albendazole at a 6-mo interval was more effective than mebendazole regimens and may be the best choice for use in the control of the 3 geohelminths.

Adolescent↗