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At least 19 recordsLinked to original sources
PubMed1997

Residue study of mebendazole and its metabolites hydroxy-mebendazole and amino-mebendazole in eel (Anguilla anguilla) after bath treatment.

Mebendazole (MBZ) is extensively used in eel culture for treatment of Pseudodactylogyrus spp. infections. This use may lead to residues of MBZ in eel tissues. Consequently, the residue profile of MBZ in eel after treatment with the drug is of special concern. Therefore, a residue study was performed in European eels (Anguilla anguilla), bath-treated with MBZ at a dose of 1 mg/liter for 24 hr and kept at a water temperature of 25 degrees C. Liver, kidney, fat, skin, and muscle tissues samples were collected at intervals during and after treatment and analyzed for MBZ and its metabolites, hydroxy-MBZ (MBZ-OH) and amino-MBZ (MBZ-NH2), by HPLC. Results showed that MBZ is extensively metabolized to MBZ-OH and MBZ-NH2. Liver and kidney were found to contain the highest levels of MBZ metabolites, and fat contained the highest levels of the parent compound. Skin contained higher residue levels for all three compounds, compared with muscle tissue. MBZ and its hydroxy metabolite were eliminated within 5 days from the edible parts (muscle and skin) of the eels, whereas MBZ-NH2 could be detected by the 14th day after the end of the treatment period. Consequently, although MBZ and MBZ-OH constitute the residues of toxicological concern, MBZ-NH2 should be taken as the compound of interest for estimating the withdrawal time for consumption of eel treated with MBZ.

Absorption↗
PubMed2003

Efficacy of mebendazole and levamisole alone or in combination against intestinal nematode infections after repeated targeted mebendazole treatment in Zanzibar.

OBJECTIVE: To evaluate the efficacy of and resistance to mebendazole (500 mg) and levamisole (40 or 80 mg), alone or in combination, for the treatment of Ascaris lumbricoides, Trichuris trichiura and hookworm infections on Pemba Island - an area exposed to periodic school-based mebendazole treatment since 1994. METHODS: A randomized, placebo-controlled trial was carried out in 914 children enrolled from the first and fifth grades of primary schools. Stool samples collected at baseline and 21 days after treatment were examined by the Kato-Katz technique to assess the prevalence and intensity of helminth infection. FINDINGS: Efficacies of mebendazole and levamisole as single treatments against intestinal nematode infections were comparable with those in previous trials, but mebendazole treatment of hookworm infections gave significantly lower cure (7.6%) and egg reduction (52.1%) rates than reported in a study undertaken before the beginning of periodic chemotherapy (cure rate, 22.4%; egg reduction rate, 82.4%). Combined treatment with mebendazole and levamisole had a significantly higher efficacy against hookworm infections (cure rate, 26.1%; egg reduction rate, 88.7%) than either drug given alone. No difference in mebendazole efficacy was found in children who had been treated repeatedly compared with those who had not been treated previously. CONCLUSION: The overall efficacy of mebendazole against hookworm infections after periodic chemotherapy is reduced. The efficacy of benzimidazoles in chemotherapy-based control programmes should be monitored closely. Combined treatment with mebendazole and levamisole may be useful as a tool to delay the development of benzimidazole resistance.

Antinematodal Agents↗
PubMed1986

Treatment of hydatid disease with high oral doses of mebendazole. Long-term follow-up of plasma mebendazole levels and drug interactions.

Plasma mebendazole levels were analysed retrospectively in patients treated for inoperable infections with Echinococcus multilocularis or granulosus. In 10 patients receiving mebendazole at 4 dose levels there was no relation between dose and plasma concentration. In 17 patients followed on the same dose for more than 18 months, the plasma levels varied with individual coefficients of variation ranging from 27 to 72%. The data reveal the limitations of single measurements of plasma mebendazole and emphasize the need for repeated monitoring. Coadministration of phenytoin and carbamazepine seemed to lower plasma levels, presumably as a result of enzyme induction. It was not possible appreciably to raise the mebendazole concentrations by inhibition of drug metabolizing enzymes with cimetidine.

Adult↗
PubMed1991

Treatment of experimental alveolar echinococcosis: comparative study of mebendazole, isoprinosine and a mebendazole isoprinosine association.

A comparative biochemical study of the effects of mebendazole and Isoprinosine used separately or associated was conducted in six-month old gerbils infected three months ago by Echinococcus multilocularis metacestodes. Mebendazole treatment induced a decrease of glucose (81%) whereas Isoprinosine increased the glucose uptake in the parasite. The combination of the two drugs led to a decrease of about 40% of the glucose concentration. The specific activities of alkaline and acid phosphatases were also modified. Isoprinosine seemed more effective when used alone than associated with mebendazole with the chosen procedure of treatment.

Acid Phosphatase↗
PubMed1994

A comparative study of the effectiveness of mebendazole (Janssen) and generically equivalent mebendazole (Nordia) in intestinal helminthiasis in Papua New Guinean children.

Papua New Guinean schoolchildren in the highlands were randomly assigned to treatment groups in order to verify the effectiveness of mebendazole (Nordia) and compare it with mebendazole (Janssen) in both extended and single-dose therapy in a double-blind controlled study. Only the Janssen product given twice daily for three days was of value in 'curing' hookworm. Single-dose treatment with the same product was highly effective in treating roundworm but not hookworm or whipworm. Observations suggest that drug particle size may be an important determinant of efficacy against hookworm. Based on this study, the use of the Janssen formulation of mebendazole would be preferable.

Adolescent↗
PubMed2003

Comparison of multivariate calibration methods to determine simultaneously mebendazole-cambendazole and mebendazole-thiabendazole in pharmaceutical preparations by UV-visible spectrophotometry.

Three multivariate calibration methods, Principal Component Regression (PCR), the K-matrix method and Q-mode factor analysis followed by varimax and Imbrie's oblique rotations were applied to the simultaneous spectrophotometric determinations of mebendazole (MBZ)-cambendazole (CBZ) and thiabendazole (TBZ)-mebendazole in commercial samples of Exelmin and Helmiben. The calibration set concentrations were selected to contain a +/-10% variation in the quantity of active ingredients as declared by the manufacturer. The Q-mode factor analysis provides superior results for the two pharmaceutical formulations. The K-matrix method proved to be totally inadequate for these determinations. Almost all Q-mode results have relative errors much smaller than 5% of the active ingredient contents. This investigation shows that PCR and Q-mode factor analysis can be used to determine MBZ-CBZ and TBZ-MBZ in commercial drugs.

Calibration↗
PubMed1982

The pharmacokinetics and bioavailability of mebendazole in man: a pilot study using [3H]-mebendazole.

Following the intravenous administration of a tracer dose (1.7 microgram) of [3H]-mebendazole to a man, an elimination half-life of 1.16 h was observed and the volume of distribution was calculated to be 2.03 l/kg. After oral administration of the same dose, an elimination half-life of 0.74 h was observed. The bioavailability of mebendazole from the solution was found to be 17%.

Benzimidazoles↗
PubMed1984

Studies on paragonimiasis: treatment with mebendazole, emetine with mebendazole and praziquantel.

One hundred cases of paragonimiasis from Saraburi province, Thailand were studied with respect to epidemiology, clinical manifestations, radiography and treatment. Highly endemic areas were Cha-om and Sum-pugpaew villages in Kang-koy district. The ratio of male to female was 48:52. Uncooked crabs and shrimps are the second intermediate hosts of Paragonimus. Hemoptysis and chronic cough were the main symptoms; with crepitations and rhonchi in both lungs. There was no specific changes in chest X-rays of the lungs, except in cases of hemoptysis where changes in pulmonary vessels were observed. Tomograms of the lungs provided 100% accuracy and confirmation of diagnosis of pulmonary paragonimiasis. Praziquantel 25 my/kg body weight three times a day for 2 days gave a cure rate of 90%, mebendazole plus emetine hydrochloride gave a cure rate of 70% and mebendazole alone was not effective.

Adolescent↗
PubMed1975

The lethal effect of mebendazole on secondary Echinococcus granulosus, cysticerci of Taenia pisiformis and tetrathyridia of Mesocestoides corti.

Oral administration of mebendazole at a rate of 1 g/kg feed (approximately 50 mg/kg body weight/day) for 14 days killed mature and immature cysticerci of Taenia pisiformis in rabbits, and multiplying tetrathyridia of Mesocestoides corti in mice. Progressive degrees of parasite damage caused by mebendazole treatment could be assessed by histological examination of calcereous corpuscles. A single subcutaneous injection of 10 percent mebendazole in carrier, at a rate of 100 mg/kg body weight, resulted in the death of all M. corti tetrathyridia in mice within 4 weeks, but the drug in saline was slowly mobilized and was relatively ineffective. Neither subcutaneous injections of mebendazole in saline or in carrier could kill cysticerci of T. pisiformis within 5 weeks, but the drug in carrier was effective after several months. Mebendazole in saline was effective when injected intraperitoneally, but adhesions often resulted from this route of administration. Echinococcus granulosus protoscoleces administered to mice by intraperitoneal injection were rapidly encapsulated by host lymphoid cells. The vesiculating protoscoleces were all contained within a fibrous capsule for more than 2 months after infection, but by 4 months almost all had grown free of the host reaction. Treatment of the encapsulated protoscoleces with mebendazole in feed for 14-21 days caused collapse of the outer cysts and death of the germinal membrane of all but the innermost protoscoleces. Six weeks later, however, cysts had regrown from surviving germinal tissue and a further treatment with mebendazole in feed for 14-21 days again did not destroy all germinal cells. Treatment of the 4-month-old scoleces with mebendazole in feed for 14 days caused all cysts to collapse and destroyed practically all E. granulosus germinal tissue. Three subcutaneous injections of mebendazole at fortnightly intervals, of drug in saline at 500 mg/kg body weight, or in carrier at 100 mg/dg body weight, were required in order apparently to kill all secondary cysts of E. granulosus. Host lymphoid cells were not able to traverse the laminated membrane of either untreated or collapsed cysts, and it has been shown that only a small amount of living germinative tissue is required to produce a new E. granulosus cyst. These factors could contribute to the relative ability of E. granulosus cysts to recover from mebendazole treatment, compared with cysticerci or tetrathyridia. The effectiveness of mebendazole thus seemed to depend on the formulation of the drug and its route of administration. Mebendazole is probably the first anthelmintic to have a lethal effect on larval cestodes. When applied orally there do not appear to be any adverse effects due to treatment.

Administration, Oral↗
PubMed1982

Clinical pharmacokinetics of high dose mebendazole in patients treated for cystic hydatid disease.

The plasma concentrations of mebendazole and its metabolites have been monitored in twelve patients after receiving a 10 mg/kg dose for cystic hydatid disease. The mebendazole plasma concentration-time profiles differed considerably between patients; elimination half-lives ranged from 2.8-9.0 h, time to peak plasma concentration after dosing ranged from 1.5-7.25 h and peak plasma concentrations ranged from 17.5 to 500 ng/ml. The mean peak plasma concentration of mebendazole after an initial dose (69.5 ng/ml) was lower than found in patients during chronic therapy (137.4 ng/ml). The plasma AUCTS for the major metabolites of mebendazole (methyl 5-(alpha-hydroxybenzyl)-2-benzimidazole carbamate and 2-amino-5 benzoylbenzimidazole) were about five times the plasma AUCT found for mebendazole in patients on chronic therapy. It is suggested that the slower clearance of these polar metabolites relative to mebendazole results from enterohepatic recycling. Since mebendazole is also highly plasma protein bound, caution should be observed in administering mebendazole to patients with liver disease. Concentrations of mebendazole found in the tissue and cyst material collected from two patients during surgery ranged from 59.5 to 206.6 ng/g wet weight.

Adult↗
PubMed1983

Safety studies evaluating the effect of mebendazole on liver function in dogs.

The effect of repeated and exaggerated mebendazole administration was evaluated in dogs with and without experimentally induced altered liver function. Irish Setters and Toy Poodles were dosed at 1, 3, and 5 times the therapeutic dose (22 mg/kg) of mebendazole for 17 days, without any effect on the liver. Mixed breed dogs that received increasing doses of mebendazole at 11 to 110 times the therapeutic dose for 2 months did not show adverse effects and remained in good health throughout the experiment. There was not substantial evidence that carbon tetrachloride-induced liver changes were exacerbated by subsequent repeated treatments with mebendazole at 15 times the therapeutic dose. Additionally, in dogs whose liver function was compromised experimentally by glutathione depletion and microsomal enzyme induction, administration of mebendazole at this same dosage for 30 days did not result in any hepatotoxic effect. When mebendazole was given at 15 times the therapeutic dose prior to an hypoxic episode in dogs pretreated with a barbiturate and high protein diet, there was no evidence of any adverse effect on liver function. These metabolic manipulations, in conjunction with mebendazole administration, failed to reveal any mechanism of hepatic dysfunction associated with mebendazole treatment. Unrecognized factors appear to be involved with the rare cases of hepatic dysfunction that have been reported after mebendazole administration. Only careful documentation of field cases and further laboratory research can identify these factors.

Animals↗
PubMed1999

Effect of mebendazole therapy during pregnancy on birth outcome.

BACKGROUND: In areas endemic for hookworm, routine antenatal mebendazole therapy could greatly reduce the prevalence of anaemia in pregnancy. At present, however, this is not a widely accepted control strategy because of a lack of data on the safety of the drug. We assessed the effect of mebendazole therapy during pregnancy on birth outcome. METHODS: A cross-sectional study was done in Sri Lanka, where prescription of mebendazole to women in the second trimester of pregnancy is recommended. Two hospitals were chosen for the study, and women who gave birth there between May, 1996, and March, 1997, were recruited. We compared the rates of major congenital defects, stillbirth, perinatal death, and low birthweight (< or = 1500 g) among babies of mothers who had taken mebendazole during pregnancy with those whose mothers had not taken an anthelmintic (controls). FINDINGS: The rate of major congenital defects was not significantly higher in the mebendazole group than in the control group (97 [1.8%] of 5275 vs 26 [1.5%] of 1737; odds ratio 1.24 [95% CI 0.8-1.91], p=0.39). Among 407 women who had taken mebendazole in the first trimester (contrary to medical advice), 10 (2.5%) had major congenital defects (odds ratio vs controls 1.66 [0.81-3.56], p=0.23). The proportions of stillbirths and perinatal deaths were significantly lower in the mebendazole group (1.9 vs 3.3%, 0.55 [95% CI 0.4-0.77]), as was the proportion of low-birthweight babies (1.1 vs 2.3%, 0.47 [95% CI 0.32-0.71]). INTERPRETATION: Mebendazole therapy during pregnancy is not associated with a significant increase in major congenital defects, but our results indicate that it should be avoided during the first trimester. This therapy could offer beneficial effects to pregnant women in developing countries, where intestinal helminthiases are endemic.

Abnormalities, Drug-Induced↗
PubMed2001

Development of colon targeted drug delivery systems for mebendazole.

The objective of the present study is to develop colon targeted drug delivery systems for mebendazole using guar gum as a carrier. Matrix tablets containing various proportions of guar gum were prepared by wet granulation technique using starch paste as a binder. The tablets were evaluated for drug content uniformity, and were subjected to in vitro drug release studies. The amount of mebendazole released from the matrix tablets at different time intervals was estimated by a high-performance liquid chromatography method. Guar gum matrix tablets released 8-15% of the mebendazole in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. When the dissolution study was continued in simulated colonic fluids the matrix tablets containing 20% of guar gum released another 83% of mebendazole after degradation into 2-3 pieces. The matrix tablets containing 30% of guar gum also released about 50% of mebendazole in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that matrix tablets containing either 20% or 30% of guar gum are most likely to provide targeting of mebendazole for local action in the colon. The mebendazole matrix tablets containing either 20% or 30% of guar gum showed no change either in physical appearance, drug content or dissolution pattern after storage at 45 degrees C/75% relative humidity for 3 months. Differential scanning calorimetry indicated no possibility of interaction between mebendazole and guar gum.

Animals↗
PubMed2005

Population-based case-control study of mebendazole in pregnant women for birth outcomes.

The objectives of the study was to check the embryotoxic-teratogenic and fetotoxic effect of mebendazole (Vermox; Richter, Budapest, Hungary) treatment during pregnancy. Mebendazole use during pregnancy was evaluated in mothers of babies born with congenital abnormalities and in matched control mothers of babies born without congenital abnormalities in the population-based data set of the Hungarian Case-Control Surveillance of Congenital Abnormalities between 1980 and 1996. Of 22,843 women who had newborns or fetuses with congenital abnormalities, 14 were found to have been treated with mebendazole for intestinal nematoda infections/diseases during pregnancy (crude POR: 1.8 with 95% CI: 0.7-4.2). Of 38,151 women who had newborns without any defects (controls), the same number (14) were found to have been treated with mebendazole during pregnancy. Six different congenital abnormality groups were evaluated and a higher prevalence of mebendazole use in these mothers throughout pregnancy was not found. Gestational age and birth weight were analyzed in control infants born to mothers with or without mebendazole treatment. The mean gestational age was somewhat longer and mean birth weight was larger in newborn infants born to mothers with mebendazole treatment. Thus, treatment with mebendazole during pregnancy did not indicate a teratogenic and fetotoxic risk to the embryo or fetus, though the numbers of treated cases and controls in this study were limited.

Abnormalities, Drug-Induced↗
PubMed1990

[Treatment of strongyloidiasis with mebendazole and its combination with thiabendazole].

Although Strongyloides stercoralis (S. stercoralis) infection rate in Okinawa Prefecture was less than 2% by the traditional method, it has been proven to be 6.2% by the new technique--agar plate method. Thiabendazole has strong activity to eradicate the organism, but it is well known that the rate of severe side effects is extremely high. Therefore, we attempted to evaluate the new treatment for the infection by mebendazole and its combination with thiabendazole. The reason for use of the drug is based on the reports of successful treatment of S. stercoralis infection in humans with the mild and infrequent side effects produced by the drug. Thirty three patients were orally given mebendazole 100 mg twice daily for 28 days. Twenty six patients were given thiabendazole 500 mg thrice daily for 5 days and after that, mebendazole 100 mg twice daily for 9 days. This combination therapy was repeated twice. The following results were obtained: 1) Out of a total of 59 patients, the cure rate was 83.3% (20/24) in single use of mebendazole and 100.0% (22/22) in the combination therapy. 2) Constipation (9.1%) and headache (9.1%) were of relatively high incidence in the mebendazole group, but they were mild. Nausea (19.2%) and headache (15.4%) were observed in the combination therapy group and the drug was discontinued in 2 patients. 3) The incidence of the elevation of S-GOT, S-GPT was noted in 71.4% (20/28) for the mebendazole group and 52.2% (12/23) for combination therapy group. All 13 patients of the mebendazole group were negative in lymphocyte stimulation test for mebendazole.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗