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PubMed1977

The efficiency of levamisole, thiabendazole and fenbendazole against naturally acquired infections of Ostertagia ostertagi in cattle.

In two experiments, conducted in cattle with naturally acquired infections of Ostertagia ostertagi, comparative assessments were made of the anthelmintic efficiency of levamisole, thiabendazole and fenbendazole, each at 1.0, 1.5 and 2.0 times the recommended dose rate. Variable efficiencies of 81 and 49 per cent for levamisole, 86 and 56 per cent for thiabendazole were obtained against adult O ostertagi. Neither drug showed substantial activity against early fourth stage larvae. Efficiency of fenbendazole against adult O ostertagi was consistently high; 85 and 89 per cent in the two experiments respectively. In the first experiment in which cattle were slaughtered two to three days after treatment, only 22 per cent of inhibited early fourth stage larvae were removed whereas in the second experiment when slaughter took place 10--11 days after treatment, this efficiency was 89 per cent. There was no increased effect of increased dose rates on treatments with thiabendazole or fenbendazole. The activity of levamisole against adult worms and inhibited larvae was increased at twice the recommended dose rate.

Abomasum↗
PubMed1983

Intrahepatic cholestasis and sicca complex after thiabendazole. Report of a case and review of the literature.

Thiabendazole is a relatively safe and effective agent with a wide range of activity against nematodes infesting the gastrointestinal tract. A 55-yr-old man developed prolonged jaundice and sicca complex after a course of thiabendazole therapy. Endoscopic retrograde cholangiopancreatography demonstrated normal biliary tree and pancreatic ducts. Liver biopsy was consistent with a drug-induced intrahepatic cholestatic reaction. The patient recovered completely from his liver injury, but the sicca complex persisted 1 yr after the drug was given. The literature on thiabendazole-induced cholestasis and its association with sicca complex is reviewed.

Biopsy↗
PubMed1980

A comparison of the effect of albendazole, cambendazole, and thiabendazole on the larval development of three hymenolepidid cestodes.

Flour beetles (Tribolium confusum) parasitized either by Hymenolepis diminuta, H. nana, or H. microstoma were fed continuously on flour mixed either with thiabendazole, cambendazole, or albendazole (drug concentration was always 10%) from day 1 (24 hr) to day 10 postinfection when the experiments were terminated. All drugs markedly inhibited the development of H. diminuta and H. nana. Populations of these species recovered from beetles fed anthelmintics were composed mostly of under-developed forms, many of which still retained the size and appearance of newly hatched oncospheres, whereas all the parasites recovered from the control beetles (fed only flour) reached full development. Parasites inhibited by cambendazole and albendazole recovered and reached full development within 9 days after treatment was terminated. Also, results were obtained which implied that some parasites were able to continue their development at a reduced rate in the presence of the drugs. Hymenolepis microstoma differed from the other species in its response to the drugs. Albendazole and thiabendazole had no effect on its development and it was only slightly inhibited by cambendazole. Larvae recovered from beetles fed the latter drug had all developed beyond the oncosphere stage but 3 to 5% of them repeatedly failed to reach full development. The drugs varied in their effects on the flour beetles. An average of 63% and 33% of those fed thiabendazole and cambendazole, respectively, died before the 10th day of infection. Albendazole, on the other hand, had no effect on beetle survival.

Albendazole↗
PubMed1980

Trichostrongylus colubriformis and Ostertagia sp resistant to levamisole, morantel tartrate and thiabendazole: infectivity, pathogenicity and drug efficacy in two breeds of sheep.

Merino and Border Leicester cross Merino sheep, nine months old, were infected with 10,000 third stage larvae of both Trichostrongylus colubriformis (PF4) and Ostertagia circumcincta/O trifurcata (PF5), known to have varying degrees of resistance to levamisole, morantel tartrate and thiabendazole. Crossbred sheep carried heavier Ostertagia sp worm burdens but there was no difference in susceptibility between the two breeds of sheep to infection with T colubriformis. The anthelmintic efficacy of thiabendazole, at 50 mg/kg, against T colubriformis was 81.8 per cent and 92.4 per cent for Merinos and crossbreds respectively while levamisole, at 6.75 mg/kg, was 12.3 per cent and 18 per cent effective. Thiabendazole removed 92.3 per cent and 83.8 per cent of Ostertagia sp in Merinos and crossbreds respectively. However, worm burdens in levamisole treated sheep were not significantly different from controls. No significant breed differences were found in 24 h faecal egg outputs. It is suggested that breed differences previously described in four-month-old sheep may have been due to differences in the rate of development of immune responsiveness. This disparity was no longer detectable in the immunologically mature sheep used in this study.

Animals↗
PubMed2004

Determination of carbendazim, thiabendazole, and o-phenylphenol residues in lemons by HPLC following sample clean-up by ion-pairing.

An efficient analytical method is presented involving effective sample clean-up with solid-phase extraction and HPLC-UV analysis for the simultaneous determination of carbendazim, thiabendazole, and o-phenylphenol residues in lemons. Sample preparation involves extraction with acetonitrile acidified with trifluoroacetic acid and an ethyl acetate/petroleum ether mixture. Purification of the crude extract was carried out with liquid-liquid partitioning after addition of an aqueous ammonia solution. Final clean-up was performed on polymeric reversed-phase cartridges pretreated with sodium dodecyl sulfate. Chromatographic analysis was performed on a reversed-phase HPLC column isocratically eluted with an acetonitrile/water/ammonia mixture and UV detection at 254 nm. The chromatographic method is repeatable, reproducible, and sensitive. Fungicide recoveries from lemon samples fortified at levels of 5 and 1 mg kg(-1) were 81-85% for carbendazim, 96-98% for thiabendazole, and 81-106% for o-phenylphenol with coefficients of variation of 2.5-7.4%. Detection limits for carbendazim, thiabendazole, and o-phenylphenol in lemons were 0.21, 0.27, and 0.51 mg kg(-1), respectively.

Journal Article↗
PubMed2003

Persistence of the fungicides thiabendazole, carbendazim and prochloraz-Mn in mushroom casing soil.

The persistence of the fungicides thiabendazole, carbendazim and prochloraz-Mn in mushroom casing soil was determined following their application at rates commonly used in the UK mushroom industry. Following drench applications, the concentration of all active ingredients was always higher in the top half of the casing soil layer than in with the bottom half. When carbendazim and prochloraz-Mn were applied using half the recommended volume of water per unit area, there was a tendency for carbendazim concentrations to be even higher in the top half of the casing soil, compared with the standard treatment, while concentrations of prochloraz-Mn were similar, irrespective of the volume of water used. Carbendazim and prochloraz-Mn concentrations in the top half of the casing layer decreased to < or = 13 mg kg(-1) by day 28/29, following different applications, whereas the thiabendazole concentration was consistently high during the course of the crop, being < or = 83 mg kg(-1) at day 31. Fungicides that do not persist at high concentrations in mushroom casing soil for the duration of the crop may not give good control of mushroom pathogens, particularly if the fungicide concentration falls to a level which is close to the EC50 value.

Agaricales↗
PubMed1994

Fasciola hepatica: mebendazole and thiabendazole pharmacokinetics in sheep.

Pharmacokinetics of the two anthelmintic drugs mebendazole and thiabendazole were determined in sheep before and 4, 8, 13, 19, and 25 weeks after an infestation of animals by an oral administration of 150 metacercariae of Fasciola hepatica. The parasitic pathology was ascertained by the increase in plasma enzyme activities of glutamate dehydrogenase and gamma-glutamyltransferase. After oral administration of mebendazole (25 mg.kg-1), the parent drug and especially its reduced metabolite were present in plasma of animals. A significant 1.5- to 2.7-fold increase in the mean residence time occurred by Weeks 13 to 25 postinfection. This change was related to decreases in both the elimination from the pharmacokinetic compartment representing the reduced metabolite and the area under the curve of plasma metabolite concentration versus time. A 59% decrease in MBZ reduction was demonstrated in liver microsomes prepared from 12-week-infected sheep. This reductase activity was characterized by NADPH dependency and a pH peak activity of 6.0 and was competitively inhibited by daunomycin. In sheep receiving a 50 mg.kg-1 oral dose of thiabendazole, fascioliasis provoked only decreased plasma concentrations of the metabolite 5-hydroxythiabendazole by Weeks 4 to 25 postinfection. This change parallels an increase in urinary excretion of free metabolite but this is of minor significance in the general fate of the drug because of the prevalence of excretion as conjugates. In summary, fascioliasis appears to have more of an effect on the pharmacokinetics of mebendazole, a drug intensively metabolized by the liver into a metabolite present at high concentrations in the plasma of animals and humans.

Administration, Oral↗
PubMed1991

Determination of levamisole and thiabendazole in meat by HPLC and photodiode array detection.

An HPLC method for the analysis of levamisole and thiabendazole has been developed with recoveries varying over 63-75%. The two anthelmintics are extracted from meat with ethyl acetate, purified by liquid/liquid extraction and analyzed quantitatively on a mu Bondapak C18 column. The optimum detection is achieved by means of a photodiode array detector at 240 nm for levamisole and at 300 nm for thiabendazole. The detection limits for both compounds in meat are 25 micrograms/kg and 5 micrograms/kg, respectively.

Animals↗
PubMed1989

Micronodular cirrhosis after thiabendazole.

Hepatotoxicity secondary to the administration of thiabendazole has been rare since this drug was produced in 1964. In 14 of 15 patients reported previously in the literature, severe intrahepatic cholestasis resolved within seven months of the onset of illness. A recent report documented the progression to cirrhosis in a 15th patient. We report the second case of a patient with intrahepatic cholestasis that developed after treatment with thiabendazole and progressed to severe micronodular cirrhosis.

Biopsy↗
PubMed1979

Effect of thiabendazole and tincture of iodine on cattle ringworm caused by Trichophyton verrucosum.

Clinical trials were carried out on 3 groups of 30 Friesian cattle naturally infected with Trichophyton verrucosum. One group was treated with 3.75% thiabendazole in glycerine, another with 5% tincture of iodine and the last served as the control group without any treatment. Both the preparations were applied locally on the ringworm lesions at 3 day intervals with a total of 4 applications. The percentage of animals cured was 86.7 by thiabendazole and 46.7 by tincture of iodine. No recrudescence was observed during the subsequent 4 months period.

Animals↗
PubMed2001

Determination of imidacloprid, metalaxyl, myclobutanil, propham, and thiabendazole in fruits and vegetables by liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry.

Imidacloprid, metalaxyl, myclobutanil, propham, and thiabendazole have been simultaneously determined in strawberries, oranges, potatoes, pears, and melons by matrix solid-phase dispersion (MSPD) followed by liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry (LC-APCI-MS) in positive-ion mode. The samples were homogenized with C8 bonded silica as MSPD sorbent, placed in a glass column, and eluted with dichloromethane. Chromatographic separation of the compounds was achieved on a reversed-phase LC column using a methanol-ammonium formate (50 mmol L(-1)) gradient as a mobile phase. Samples were screened by monitoring the protonated molecular ion at m/z 256 for imidacloprid, 280 for metalaxyl, 289 for myclobutanil, and 202 for thiabendazole, and the main fragment at m/z 138 for propham. Positive samples were confirmed by multiple-ion monitoring. The repeatability (<20%) and recovery (>57%) of the method were good, and limits of detection (<0.05 mg kg(-1)) were adequate.

Antinematodal Agents↗
PubMed1982

Treatment of strongyloidiasis with thiabendazole: an analysis of toxicity and effectiveness.

The effects of therapy with thiabendazole were investigated in 43 men who had been infected with Strongyloides stercoralis for 35 years. Side effects of drug treatment were frequent and sometimes severe; nausea was the most common symptom. Six months later, approximately one third of patients had persistent diarrhoea, recurrent urticaria or considered that their general health had not improved. Parasites were found in 7% of persons six months after treatment. Blood eosinophil counts fell dramatically but the falls in serum IgE levels and serum Strongyloides antibody titres were less marked. Assessment of response to treatment is difficult because of the insensitivity of parasitological techniques and the ability of this parasite to replicate. It is concluded that thiabendazole cannot always be relied upon to eradicate infection.

Aged↗
PubMed1981

In vivo suppression of delayed hypersensitivity by thiabendazole and diethylcarbamazine.

Several anthelminthic agents, such as niridazole and metronidazole, have been demonstrated to have striking effects on the immune system, apparently independent of their antiparasitic activities. In the present study, we have examined the effect of thiabendazole and diethylcarbamazine on two parameters of delayed hypersensitivity, lung granuloma formation around Schistosoma mansoni eggs and delayed footpad edema in response to schistosome egg antigens. Both drugs caused significant reduction of lung granuloma size in unsensitized animals when given as daily doses for 8 days. Thiabendazole was the more potent suppressant, affecting granuloma size in unsensitized animals when given as single dose and in sensitized animals using a multiple dose regimen. Diethylcarbamazine was without effect on granuloma size in sensitized animals, but inhibited delayed footpad swelling when given daily for 6 days. Neither drug affected granulomas induced by non-antigenic plastic beads. These data support the hypothesis that some of the clinical activities of these drugs may be mediated by interference with host response to antigenic stimuli.

Animals↗
PubMed1986

Irreversible in vivo and in vitro binding of thiabendazole to tissue protein of pregnant mice.

In vivo experiments showed that [14C]thiabendazole is irreversibly bound to protein of the liver and embryo in pregnant mice, but not to DNA and RNA in these tissues. In experiments carried out in vitro, the binding of [14C]thiabendazole to microsomal protein of the liver was proportional to time and protein concentration, was dependent upon the presence of oxygen and NADPH and was inhibited by carbon monoxide or SKF-525A, indicating that it was mediated by the cytochrome P-450-dependent monooxygenase system. The binding capacity of microsomes in various tissues was examined, and that of the liver microsomes was found to be more pronounced than that of other tissues.

Animals↗
PubMed1990

Effect of thiabendazole and fenbendazole on glucose uptake and carbohydrate metabolism in Trichuris globulosa.

14C-glucose uptake by adult Trichuris globulosa was found to be a non-linear function of time and limiting substrate concentration. The uptake was a two component process, an initial rapid burst, followed by a lower steady state. Linear transformation of the substrate saturation kinetics by Eadie plot gave a Kt value of 5 X 10(3) microM and Jmax of 5 mumol mg-1 dry weight min-1. Presence of the benzimidazole drugs, thiabendazole and fenbendazole, markedly inhibited the uptake process at concentrations in which the motility of the parasites was not affected. T. globulosa was found to possess the full complement of enzyme systems of glycolysis, Krebs cycle, phosphatases, transaminases and other NAD- and NADP-dependent enzymes. Thiabendazole and fenbendazole lowered the Vmax of most of these enzymes and affected the substrate-affinity constant (Km) in some of them. The mode of action of these drugs was discussed in the light of the data obtained.

Animals↗
PubMed1996

Use of free living stages to study the effects of thiabendazole, levamisole, pyrantel and ivermectin on the fine structure of Haemonchus contortus and Heligmosomoides polygyrus.

Ultrastructural changes induced in vitro by thiabendazole, levamisole, pyrantel and ivermectin in the free living larval stages of two trichostrongyles (Heligmosomoides polygyrus and Haemonchus contortus) were analysed. The observed damage for each anthelmintic is related to the known mode of action and compared to the damage commonly described in adults. The advantage of using larvae to study the effects of anthelmintics on the fine structure of nematodes rather than adults is described. Thiabendazole induced alteration of the cellular organization especially epithelial cells of the digestive tract. Changes in mitochondria were also seen. Levamisole caused contraction of muscle fibres whereas no specific lesions were observed with pyrantel. Ivermectin caused an hypertrophy of muscular groups. The interest of such a technique in research on the modes of action of anthelmintics is emphasized.

Animals↗
PubMed2002

Analysis of thiabendazole and procymidone in fruits and vegetables by capillary electrophoresis-electrospray mass spectrometry.

A capillary electrophoresis-mass spectrometry method for determining procymidone and thiabendazole in apples, grapes, oranges, pears, strawberries and tomatoes is described. Separation is achieved using a buffer of formic acid-ammonium formate at pH 3.5 with 2% of methanol. Fungicide residues present in the sample are preconcentrated by both solid-phase extraction and injection of large sample volumes into the capillary by a stacking technique, to obtain lower detection limits. Ionization is performed at atmospheric pressure in an electrospray type source and detection is carried out using positive ionization and selected ion monitoring modes. The quantitation limits are 0.005 and 0.05 mg kg(-1), and the mean recoveries are 64 and 75% for thiabendazole and procymidone, respectively, with relative standard deviations below 12% (n=5). Real fruit and vegetable samples are analyzed by the proposed method showing that residues of both fungicides are frequently present.

Bridged Bicyclo Compounds↗