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PubMedDate not supplied

A randomized controlled trial comparing mebendazole and albendazole against Ascaris, Trichuris and hookworm infections.

The efficacies and side effects of single dose treatments with 500 mg mebendazole (Janssen Pharmaceutica) and 400 mg albendazole (SmithKline Beecham) against intestinal nematodes were compared in a single-blind, randomized controlled trial among 2294 children aged 6 to 12 years on Pemba Island, Zanzibar, among whom infections with Ascaris, hookworms and Trichuris were highly prevalent. Both drugs were highly effective against Ascaris, with cure rates of over 97%. The cure rates for Trichuris were low, but mebendazole was significantly better than albendazole and produced a greater reduction in the geometric mean egg count. Mebendazole was inferior to albendazole in curing hookworm infections and in reducing the geometric mean egg count. There was no difference in the frequency of side effects reported by heavily infected children treated with either drug. In a trial on 402 children, 500 mg mebendazole (Janssen) was compared with a generic version of the drug, 500 mg mebendazole (Pharmamed). No difference was apparent in the efficacies of the 2 treatments against any of the 3 parasites studied.

Albendazole↗
PubMed1985

Anthelmintic effects of bithionol, paromomycin sulphate, flubendazole and mebendazole on mature and immature Hymenolepis nana in mice.

The anthelmintic effects of anti-tapeworm drugs, bithionol, paromomycin sulphate, flubendazole and mebendazole on immature and mature Hymenolepis nana in mice were compared. Immature worms were not affected by paromomycin sulphate or flubendazole administered for 12 consecutive days (days one to 12 after infection) at 100 mg/kg/day but 48% and 100% of H. nana were eliminated from mice by bithionol and mebendazole respectively, at the same dosage regimen. Bithionol, paromomycin sulphate, flubendazole and mebendazole given at 100 mg/kg/day for five consecutive days (days 12 to 16 after infection) eliminated 32%, 29%, 36% and 100% of mature worms respectively. 10 and 20 mg of mebendazole/kg/day for five consecutive days (days 12 to 16 after infection) had little effect on mature worms whereas 50 and 100 mg/kg/day for the same period eliminated 99% and 100% of mature worms, respectively. ED50 of mebendazole in the elimination of mature H. nana was 14 or 15 mg/kg/day for five days from the reduction in dry weight or in number of worms recovered respectively. The effects of mebendazole given 2 to 4 days, 8 to 10 days or 13 to 15 days after infection at 100 mg/kg/day were compared. Very low, if any, activity of the drug given 2 to 4 days after infection was seen, whereas the drug given 8 to 10 days or 13 to 15 days after infection eliminated 84% and 86% of H. nana respectively.

Animals↗
PubMed1985

The pharmacokinetics and bioavailability of a tracer dose of [3H]-mebendazole in man.

Five volunteers, whose ages ranged between 37 and 64 years, took part in a crossover study to determine the pharmacokinetics and bioavailability of mebendazole in man following intravenous and oral administration of a tracer dose of [3H]-mebendazole. Following intravenous administration, the average distribution half-life, elimination half-life and rate of clearance were 0.20 h, 1.12 h, and 1.063 min respectively. After oral administration of the solution, the average elimination half-life was 0.93 h, the apparent rate of clearance was 0.846 l/min, the average time to peak plasma concentration was 0.42 h, and the bioavailability of mebendazole was 22%. Comparison of metabolite area under the plasma concentration vs time data from each route of administration indicates that absorption of mebendazole from the gastrointestinal tract at this dose level is almost complete. The low bioavailability observed following oral administration at this dose level is postulated to be due to high first pass elimination. Approximately half of the administered dose of radioactivity following intravenous and oral administration was detected in the urine, and the major unconjugated metabolite of mebendazole was found to be 2-amino-5(6) [alpha-hydroxybenzyl]benzimidazole (IV), not 2-amino-5(6)benzoylbenzimidazole (II), as previously reported.

Absorption↗
PubMed2004

Toxic effects of mebendazole at high dose on the haematology of red-legged pademelons (Thylogale stigmatica).

OBJECTIVE: To investigate the effects of mebendazole at high dose on the haematology of macropods. Experimental. PROCEDURE: Five red-legged pademelons (Thylogale stigmatica) were dosed orally with mebendazole at 50 mg/kg/d for 5 to 6 days. Two control pademelons were dosed with water. Regular blood samples were taken for haematology over 20 days. RESULTS: All four treated pademelons sampled at 5 days developed severe leucopenia and neutropenia, moderate lymphopenia, thrombocytopenia, eosinopenia and monocytopenia, as well as bone marrow aplasia within 5 to 11 days after the first mebendazole dose. Four pademelons died unexpectedly or became ill and were euthanased 5 to 11 days after the first dose while the other animal recovered after 5 days of illness. Necropsy revealed systemic infection with opportunistic enteric bacteria, non-suppurative inflammation in tissues, haemorrhage and ulceration of the gastrointestinal tract. CONCLUSIONS: Red-legged pademelons rapidly develop bone-marrow aplasia and subsequent septicaemia after administration of high doses of mebendazole. Mebendazole at high doses should not be used for macropods.

Agranulocytosis↗
PubMed2006

A randomized, controlled, open-label trial of a single day of mebendazole versus a single dose of tinidazole in the treatment of giardiasis in children.

BACKGROUND: Giardia duodenalis is the most commonly detected parasite in the intestinal tract of humans and 5-nitroimidazole compounds, quinacrine and furazolidone have been used against giardiasis. However, cases refractory to treatment with these drugs are becoming more common worldwide. OBJECTIVE: To compare the efficacy and safety of mebendazole versus tinidazole in the treatment of giardiasis. RESEARCH DESIGN AND METHODS: 122 children (aged 5 to 15 years) of both sexes with confirmed Giardia duodenalis cysts or trophozoites in their stool samples were randomly separated into two groups of 61 individuals. Each group received either mebendazole 200 mg three times for 1 day or tinidazole 50 mg/kg in a single dose. The evaluation of the efficacy was based on parasitological response. Parents or legal guardians of each child were asked to provide three fecal samples on days 3, 5, and 7 after treatment completion. A child was considered to be cured if no Giardia trophozoites or cysts were found in any of the three post-treatment fecal specimens evaluated by direct wet mounts and/or after Ritchie concentration techniques. RESULTS: The frequency of cure was higher for tinidazole (81.97%) than for mebendazole (63.93%); the difference was statistically significant (p < 0.05). Transient abdominal pain was more common in children treated with mebendazole (p < 0.05), whereas loss of appetite, bitter taste, headache, vomiting, and nausea were more common in the tinidazole-treated group (p < 0.05). CONCLUSIONS: Three doses of mebendazole, in a single day, are inferior to a single dose tinidazole in the treatment of giardiasis.

Adolescent↗
PubMed2003

The effects of mebendazole on P4501A activity in rat hepatocytes and HepG2 cells. Comparison with tiabendazole and omeprazole.

Mebendazole is a benzimidazole anthelmintic widely used in veterinary and human therapy. Among benzimidazole derivatives, several drugs with inducing effect on cytochromes P450 can be found. However, the induction capacity of mebendazole on P450s has not been explored yet. In this study, the effects of mebendazole on P4501A activity was tested in primary cultures of rat hepatocytes and in human hepatoma HepG2 cell line. Two known P4501A inducers with benzimidazole structure, tiabendazole and omeprazole, were also included in the experiments with the aim of studying structure-induction relationships. After 24-, 48- and 72-h incubation of rat hepatocytes and HepG2 cells with drugs in various concentrations (0.1-100 microM), enzyme activity associated with P4501A1/2 (EROD, MROD) was measured. In addition, the P4501A1/2 protein levels in both in-vitro systems were determined by Western-blotting. Mebendazole provoked a significant increase in P4501A1/2 protein expression and P4501A activity in both in-vitro systems. Omeprazole caused a significant dose-dependent increase of P4501A activity only in HepG2 cells. Although tiabendazole treatment led to significant increase of P4501A protein level, no effect on P4501A activity was observed in either system. The results demonstrate that mebendazole possesses the ability to significantly induce P4501A. Thus, pharmacological and toxicological consequences of P4501A induction should be taken into account in human therapy. The structure-induction relationships and differences between in-vitro systems used are discussed.

Animals↗
PubMed1982

Strongyloides ratti and S. stercoralis: the effects of thiabendazole, mebendazole, and cambendazole in infected mice.

The effects of benzimidazole anthelmintics in murine strongyloidiasis were examined. Thiabendazole 50 mg/kg daily produced a 91% reduction in the numbers of Strongyloides ratti larvae in the feces. A similar suppression was seen when thiabendazole was given during the intestinal phase, but no effect was noted when the drug was administered during the phase of larval migration. Thiabendazole had no effect on larvae in the skin or lungs, did not inhibit maturation of worms, and did not expel adult worms from the gut, but did reduce fecundity of adult worms in the intestines by 84%. Mebendazole and cambendazole 50 mg/kg daily totally suppressed excretion of S. ratti in the feces. A similar suppression was seen when the two drugs were given during the phase of larval migration or during the intestinal phase. They had no effect on larvae in the skin, and the reduction in larval numbers in the lungs was not statistically significant. When given during the migratory phase and early intestinal phase, they reduced the numbers of fourth stage larvae recovered from the gut by 95%. Mebendazole and cambendazole totally eliminated intestinal adult worms. Dose response studies indicated that in terms of orally administered dose, cambendazole was 100-1,000 times more active than mebendazole. Thiabendazole and mebendazole had no significant effect on S. stercoralis larvae in the muscles. In contrast, cambendazole 50 mg/kg daily for 4 days eradicated S. stercoralis larvae from the muscles. It is concluded that cambendazole may have significant advantages over both thiabendazole and mebendazole in the treatment of strongyloidiasis.

Animals↗
PubMedDate not supplied

[Effectiveness and safety of mebendazole compared to nitazoxanide in the treatment of Giardia lamblia in children].

OBJECTIVE: Compare the effectiveness and safety of mebendazole versus nitazoxanide in the treatment of Giardia lamblia in children. Giardiasis is an intestinal protozoan of worldwide distribution which most frequently affects the infantile population. In Mexico we have, found a frequency of three to sixty percent. We have, used different medications in it's treatment, but the experience with mebendazole and nitazoxanide is scarce. METHOD: An experimental study as a clinical assay. We included children from the ages of 4 to 12 years old, which had a positive Giardia lamblia cysts in their feces. The children were divided into to two groups: A, were a administered 100 mg of mebendazole every 12 hours, for three days; B, were administered 100 mg of nitazoxanide every 12 hours, for three days; A feces control study was performed at three, five and seven days post treatment. At the end of the treatment we asked the parents if the children had presented any adverse events during the administration of the medication. For the statistical analysis we used Student's t and Chi squared. RESULTS: We studied 82 children, 41 (50%) for each group. In group A, the control feces studies were negative 33 resulting in a 80.4% effectiveness; in group B, 32 were negative resulting in a 78.0% effectiveness, without being statistically significant with a p = 0.8. We found adverse, events in 9 (22%) of the children in group A and 16 (39%) in group B, there was, statistically significant difference with p = 0.09. However, we discovered that the children who received nitazoxanide suffered from abdominal pain more frequently. CONCLUSIONS: We can conclude that both mebendazole and nitazoxanide are efficient for use against infection due to Giardia lamblia, however, the secondary reactions with nitazoxanide were more frequent than with mebendazol.

Animals↗
PubMed1989

[Comparative study of thiabendazole and mebendazole in strongyloidiasis].

Taking into consideration some statements about better efficacy and good tolerability of mebendazole and since thiabendazole has not been produced in our country the past few years we have conducted a study evaluating mebendazole, in comparison with thiabendazole in the treatment of patients with strongyloidiasis. Strongyloidiasis is a disease that should be treated with an effective and active drug since it can rapidly progress and be fatal in patients with disturbed immunocompetence. One hundred and ten patients with strongyloidiasis were treated with oral thiabendazole in a dosage of 50 mg/kg daily for two days; the other group of 41 patients was given mebendazole in a dosage of 10 mg/kg/day orally for five days. Clinical evaluations, parasitologic and hematologic tests were performed within three months after the therapy. Patients were considered to have been cured if parasitologic findings were negative and abnormal blood eosinophilia decreased below 0.09 (733/microliters). According to these criteria thiabendazole was effective in 96.4% of patients and mebendazole in 44% of patients only. We conclude that thiabendazole has still to be regarded the drug of choice in treating patients with strongyloidiasis. Mebendazole is far less effective in patients with this helminthiasis and very probably only suppresses the infection. The reports of other studies on the effect of some of the newer benzimidazole antihelmintics as cambendazole, albendazole and flubendazole have shown that they are toxic or less effective in the treatment of strongyloidiasis.

Humans↗
PubMed1987

[Experimental therapy in Chinese hamsters and rats infected with larval Echinococcus multilocularis by using mebendazole, albendazole and ivermectin with brief review of chemotherapy of human multilocular echinococcosis].

The effects of the mebendazole, albendazole and ivermectin on secondary multilocular echinococcosis in Chinese hamsters infected with intraperitoneal inoculation of protoscolices and in rats infected with transportal inoculation of protoscolices were investigated. A reduction in weight of the hydatids greater than 95% was recorded in Chinese hamsters intraperitoneally injected with mebendazole suspension. Oral administration of mebendazole moderately inhibited the development of the hydatids. Albendazole was less effective than mebendazole. Ivermectin was ineffective. The treatment with mebendazole of larval E. multilocularis inhibited the growth of the hydatids but it could not completely kill the parasite tissues. The present status of chemotherapy of the human multilocular echinococcosis was briefly discussed.

Albendazole↗
PubMed1985

[Mebendazole treatment of echinococcosis].

Forty patients with echinococcosis were treated with mebendazole (approximately 50 mg/kg body weight) and under observation for up to 8 years. In 8 patients, E. multilocularis-infection was diagnosed whereas 32 patients had liver (n = 19 lung, n = 7) or other infestations of E. granulosus. 23 patients had been treated with mebendazole alone. 20 further patients received the treatment pre- and post-operatively and in the remaining cases mebendazole was given pre- or post-operatively according to the patients' requirements. Besides the clinical and laboratory findings, morphological parameters of organ infestation due to the parasites were examined repeatedly by x-ray, ultra sound, Ct-scan or scintigram. In the course of treatment we noticed that mebendazole had a certain effect in the case of E. multilocularis-infection and in the case of lung infestation due to E. granulosus. Furthermore, patients who were treated with mebendazole and who were under observation for several years, showed improvement of the liver cyst. The analysis of all morphological data available from patients with liver cysts indicated that marked changes had already been observed in the period of one to thirty months after the beginning of therapy.

Echinococcosis↗
PubMed1993

A comparative study on the efficacy of albendazole and mebendazole in the treatment of ascariasis, hookworm infection and trichuriasis.

A comparative study of the efficacy of albendazole and mebendazole was carried out in Pattani Province in the southern part of Thailand. One hundred and ninety-six patients with single or multiple infections with Ascaris, hookworm, and Trichuris were randomized into 4 groups for different treatments. Stool examination by Kato-Katz technique were done before and on day 14 after treatment. Results of the study showed that (1) a single dose of 300 mg mebendazole (locally produced) resulted in cure rates of 50%, 0% and 0% and egg reduction rates of 87.3%, -15.3%, and 28.3%, for ascariasis, hookworm infection and Trichuris respectively; (2) a single dose of 300 mg mebendazole (original) resulted in cure rates of 100.0%, 9.1%, and 43.3%, and egg reduction rates of 100.0%, 72.0%, and 77.9%, for Ascaris, hookworm, and Trichuris respectively; (3) a single dose 500 mg mebendazole (original) resulted in cure rates of 100.0%, 30.2%, and 70.3%, and egg reduction rates of 100.0%, 70.4% and 89.9%, for Ascaris, hookworm, and Trichuris respectively and (4) a single dose of 400 mg albendazole (original) resulted in cure rates of 100.0%, 84.3%, and 67.4%, and egg reduction rates of 100.0%, 96.0% and 87.0%, for Ascaris, hookworm, and Trichuris respectively. Both mebendazole and albendazole are safe and no side effects were observed. The results of this study suggested that albendazole is the preferred benzimidazole derivative for mass treatment of multiple infections with Ascaris, hookworm, and Trichuris.

Adolescent↗
PubMed1998

A comparison of mebendazole and albendazole in treating children with Trichuris trichiura infection in Durban, South Africa.

OBJECTIVE: To compare the efficacy of mebendazole 500 mg and albendazole 400 mg single-dose treatments of Trichuris trichiura infection in children in the Durban area of KwaZuluNatal, South Africa. DESIGN: A single-blind randomised trial in children with a documented moderate infection of T. trichiura. Ova were counted in stool specimens before and 10 days after treatment by the formal-ether concentration method. SETTING: Two shelters for abandoned and orphaned children in Durban. PARTICIPANTS: Ninety-six children aged between 2 and 12 years. OUTCOME MEASURES: The number of children who showed reduced T. trichiura ova counts after the treatments, and reductions in ova counts, both expressed as percentages. Statistical analysis using the Wilcoxon 2-sample test and the chi-square test. RESULTS: Eighty-two children completed the trial; 42 received mebendazole and 40 albendazole. Of the mebendazole group 85% showed a reduction in T. trichiura ova count, compared with 75% of children who received albendazole. Mebendazole treatment was associated with a median percentage reduction in ova count of 72.2%, which significantly exceeded the 44.1% reduction after albendazole (P = 0.024). CONCLUSION: The mebendazole 500 mg single-dose therapy was more efficacious than the albendazole 400 mg single-dose therapy in treating T. trichiura infection in these children.

Albendazole↗
PubMed1976

[On the effect of mebendazole on metacestodes of Mesocestoides corti and Echinococcus multilocularis (author's transl)].

Mebendazole (5-benzoyl-2-methoxycarbonylaminobenzimidazole) was highly effective against tetrathydridia of Mesocestoides corti in the peritoneal cavity, liver and in the subcutis of mice when administered orally in the food (450 or 465 ppm) from days 7 or 40/50 post infectionem (p.i.) for 10 or 20 days in total doses of approximately 660-1660 mg/kg body weight (b.w.). All tetrathyridia were killed when treatment began at day 7 p.i., and only some survived when medication was started on days 40/50 p.i. A treatment of 5 days was only partially effective. In experiments with Echinococcus multilocularis laboratory animals were intraperitoneally infected with metacestode tissue transplants. Beginning on days 4-7 p.i. or on day 40 p.i. the animals were treated for 5, 10 or 20/21 days with mebendazole medicated food. In mice a treatment for 10 or 20/21 days with total mebendazole doses of approximately 660-2180 mg/kg b.w. caused an average reduction on metacestode weight of 61-89%. An average reduction between 58 and 84% was achieved in Meriones after a treatment for 20/21 days with total doses of approximately 650/530 mg/kg b.w. However, histological examinations and transplantation experiments revealed that in most of the treated animals metacestode tissue survived and retained its capability for budding. On the other hand, indications for a partial destruction of the parasite tissue were found in some of the treated animals. The oral mebendazole treatment was well tolerated. After intraperitoneal injection of 3 X 150 mg/kg b.w. mebendazole - as applied by Campbell et al. (1975) - all of 36 mice or Meriones died.

Animals↗
PubMed1983

Efficacy Of Mebendazole In Treatment And Control Of Trichuriasis In Korea.

Mebendazole was tested for its efficacy in individual treatment and mass control of Trichuris trichiura infection in Korea. The results were as follows: 1. The efficacy of mebendazole in 430 cases 3 weeks after treatment with mebendazole(100-1,200 mg) was not so satisfactory (15.0-64.0 and 24.6-95.2% in cure and egg reduction rates respectively). But it was observed that the higher the total dose of the drug the better the efficacy. 2. The egg positive rate of the inhabitants in mass control programme by 600 mg mebendazole decreased form 40.0 to 5.6 % during one year, May 1982-May 1983, by repeated blanket mass chemotherapy every 3 months (in conventional regimen), while the decrease was less marked or unrecognizable in 3-month (signle or two divided doses), 6-month, 12-month interval and placebo control groups. From the results, it was concluded that, although mebendazole was not highly effective in individual treatment of T. trichiura infection, it was fairly useful in mass cotrol, by repeated mass chemotherapy every 3 months.

Journal Article↗
PubMed1983

Severe, reversible neutropenia during high-dose mebendazole therapy for echinococcosis.

Two patients receiving oral high-dose mebendazole therapy for echinococcosis were found to have severe, reversible neutropenia, apparently due to marrow suppression; platelets and RBCs were also reversibly suppressed in one. High blood levels of mebendazole (239 ng/mL) in one patient may have resulted in the neutropenia and several toxic side effects, as well as a striking shrinkage of the patient's pulmonary and liver cysts. Neutropenia with high-dose mebendazole therapy may occur in up to 5% of patients and may be much more common than previously recognized. The WBC count should be monitored frequently during the first several weeks of therapy. Further experience will be needed to determine whether neutropenia is related to mebendazole levels.

Aged↗
PubMed1983

Preliminary observations on the biliary elimination of mebendazole and its metabolites in patients with echinococcosis.

The biliary excretion of mebendazole has been investigated in two patients to whom it was given for the treatment of echinococcosis, although it was found to be only partly effective. Oral mebendazole was extensively metabolized and the conjugated parent substance and its metabolites were excreted in the bile. One patient without cholestasis and with normal liver function had an apparent total biliary clearance (776 ml/min) which approached the hepatic plasma flow. The other patient with cholestasis and impairment of the hepatic drug metabolizing capacity showed a drastically reduced apparent total biliary clearance of 3.8 ml/min. The average plasma level of mebendazole was significantly lower in the former and higher in the latter patient (0.06 and 0.91 nmol/ml, respectively). The data suggest that impaired metabolism and/or biliary elimination can account for the higher plasma mebendazole level in patients with liver damage.

Adult↗
PubMed1984

Lack of effect of haemodialysis on mebendazole kinetics: studies in a patient with echinococcosis and renal failure.

The effect of haemodialysis on mebendazole kinetics has been studied in a patient receiving both mebendazole therapy and haemodialysis. The procedure of haemodialysis did not influence the plasma concentration-time profiles or the mean daily plasma levels. The arterio-venous difference in the dialyser was negligible and no mebendazole could be detected in the dialysate. Protein binding of mebendazole was 90% before dialysis and 88% during dialysis and not significantly different from the binding in patients without renal disease (91.4 +/- 1.9%, n = 22).

Adult↗