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At least 19 recordsLinked to original sources

PubMed1979

The inheritance of thiabendazole resistance in Haemonchus contortus.

Haemonchus contortus worm populations isolated from naturally infected sheep at the Pastoral Research Laboratory, Armidale, N.S.W., were found to contain approximately 20% of worms resistant to a 50 mg/kg dose of thiabendazole. Following 3 generations of selection with 50 mg/kg thiabendazole the number of worms removed by the anthelmintic was too small to detect differences between treated and control groups. After more than 15 generations of selection, matings between males from the selected strain and non-resistant females produced resistant males and females in equal numbers. Thus, thiabendazole resistance does not appear to be sex-linked. A dose--response assay on the F2 adults indicated that worms from female resistant x male non-resistant crosses were more resistant than F2 adults of the reciprocal cross. An in vitro technique that identified thiabendazole-resistant eggs by their ability to hatch in a solution containing thiabendazole and 0.1% NaCl solution was also used to study the inheritance of resistance. F1 eggs had similar LC50's to the resistant parents. F2 and back-cross eggs from an original mating of thiabendazole-resistant females x non-resistant males had a higher LC50 than F2 and back-cross eggs from the reciprocal mating, indicating a degree of matroclinous inheritance of resistance. However, the resistant parents had tolerances to thiabendazole exceeding those of F2. F3 eggs had a resistance distribution that ranged from that of the resistant to the non-resistant parent. No significant deviation from linearity was observed in any of the dose--response lines. These results indicate that thiabendazole resistance in H. contortus worms is inherited as an autosomal and semi-dominant trait.

Animals↗

PubMed1979

Inhibition of thiabendazole metabolism in the rat.

1. A single oral dose of desmethylimipramine (80 mg/kg) administered to rats inhibited the hepatic microsomal hydroxylation of thiabendazole (45%), aniline (30%), biphenyl (30%) and ethylmorphine (15%) in vitro at 5 h after dosage; there was no decrease in cytochrome P-450 or b5. 2. A single oral dose of ethoxyquin (200 mg/kg) to rats inhibited the hepatic microsomal hydroxylation of thiabendazole (65%), aniline (40%) and biphenyl (40%) in vitro at 1 h after dosage; inhibition was less at 5 h. There were no changes in the contents of cytochromes P-450 and b5. 3. The max. plasma concn. of thiabendazole occurred 2--4 h after oral dosing (50--200 mg/kg) to rats. Thiabendazole (100 mg/kg) administered orally 30 min after oral ethoxyquin (400 mg/kg) or thiabendazole (200 mg/kg) administered orally 30 min after oral desmethylimipramine (80 mg/kg) delayed absorption of the thiabendazole and resulted in markedly markedly decreased plasma concentration of the anthelmintic. 4. Simultaneous administration of ethoxyquin (300 mg/kg) potentiated the anthelmintic effect of thiabendazole (750 mg/kg) on the helminth parasite, Nematospiroides dubius, in the mouse. Desmethylimipramine showed no similar potentiation.

Animals↗

PubMed1978

Interaction of thiabendazole with fungal tubulin.

Thiabendazole, 2-(4'-thiazolyl)benzimidazole, at 80 micrometer completely inhibits mitosis in hyphae of Aspergillus nidulans, growing in liquid culture. DNA and RNA synthesis and mycelial growth are only partially inhibited at this concentration. Binding studies with cell-free mycelial extracts from Penicillium expansum showed that thiabendazole competitively inhibits [14C]carbendazim binding to tubulin, which suggests that the antimitotic activity of thiabendazole is based on interference with microtubule assembly. Tubulin from a thiabendazole-resistant and carbendazim-highly sensitive mutant of P. expansum has a lower affinity to thiabendazole and a higher affinity to carbendazim than tubulin from a wide-type strain. This indicates that in this mutant the structure of the binding site is affected. The data presented suggest that several sites of both the tubulin and ligand molecule are involved in the binding of benzimidazole compounds to fungal tubulin.

Aspergillus nidulans↗

PubMed1979

Thiabendazole resistance in field populations of Haemonchus contortus.

Six populations of H. contortus were selected for a study of thiabendazole resistance from a collection of 40 populations made during a survey of the efficiency of thiabendazole on the Northern Tablelands of New South Wales. Based on survey results, 3 of these populations were considered susceptible and the remaining 3 were considered resistant. However, when these populations were compared with a known susceptible strain on the ability of their eggs to hatch in a solution containing thiabendazole and 0.1% NaCl all 6 had significantly greater LC50's. The resistance ratios of the LC50 for each of the 6 populations to that of the known susceptible strain were 5.1, 4.3, 3.2, 3.1, 2.3, and 1.6 respectively. Following dosing of their host with 44 mg/kg thiabendazole the resistance ratios of the survivors increased to 5.4, 5.1, 4.7, 4.4, 3.1 and 2.4. Eggs produced by the F1 generation of the worms surviving 44 mg/kg thiabendazole did not revert back to the lower LC50's of the unselected parents. Rather the LC50 remained at a level near that of a known highly resistant strain of H. contortus.

Animals↗

PubMed1977

The effect of route of administration on the anthelmintic efficacy of benzimidazole anthelmintics in sheep infected with strains of Haemonchus contortus and Trichostrongylus colubriformis resistant or susceptible to thiabendazole.

Observations of erratic anthelmintic activity of fenbendazole against known standardised thiabendazole-resistant strains of Haemonchus contortus and Trichostrongylus colubriformis in sheep were investigated. Fenbendazole at a dose rate of 10 mg/kg body weight was administered by oral, intra-ruminal or intra-abomasal routes, and was most effective against both resistant strains following intra-ruminal administration. In addition thiabendazole, oxibendazole, fenbendazole, parbendazole and mebendazole plus two unrelated compounds, levamisole and morantel tartrate, were used at one and a half times their suggested or recommended therapeutic dose rate against thiabendazole-resistant strains of H contortus and T colubriformis in sheep; each drug being administered by the intra-ruminal or intra-abomasal routes. Fenbendazole was more effective against both strains following intra-ruminal administration. Parbendazole was more effective against the resistant strain of T colubriformis following intra-ruminal administration. At the dose rate chosen for the other benzimidazoles used against these resistant strains, there was no difference in anthelmintic efficacy due to route of administration. Levamisole was highly effective against both resistant strains, irrespective of the route of administration. In the groups treated with morantel tartrate, the results obtained were difficult to interpret due to mortalities and a highly variable response in the surviving sheep. Fenbendazole, thiabendazole and mebendazole when used at their suggested or recommended therapeutic dose rate in sheep, were highly effective against known thiabendazole-susceptible strains of H contortus and T colubriformis following both intra-ruminal or intra-abomasal administration.

Abomasum↗

PubMed1979

Comparative study of the effect of thiabendazole and fungizone on Histoplasma capsulatum in macrophages.

The antifungal properties of Fungizone (amphotericin B intravenous solution) and thiabendazole on Histoplasma capsulatum within guinea pig macrophages were compared using the staining method and a newly developed plating method to determine the viability of intracellular H. capsulatum. The two methods were compared to determine the effectiveness of Fungizone and thiabendazole on H. capsulatum within macrophages. Fungizone was fungicidal for intracellular H. capsulatum, killing 99.9% of the yeasts at a concentration of 0.5 microgram/ml. There was some indication that non-viable intracellular yeasts were stained which could result in misinterpretation of the effectiveness of Fungizone using the staining method unless the yeasts are very closely examined for staining abnormalities. There was a good correlation between the two methods to demonstrate suppression of the multiplication of intracellular H. capsulatum in macrophages treated with 50 microgram/ml of thiabendazole. Thiabendazole was lethal for some intracellular H. capsulatum.

Amphotericin B↗

PubMed1976

The anthelmintic efficacy of fenbendazole against thiabendazole-resistant strains of Haemonchus contortus and Trichostrongylus colubriformis in sheep.

The anthelmintic efficacy of fenbendazole (methyl 5-(phenylthio)-2-benzimidazole carbamate) was tested in sheep against standardised strains of Hcaemonchus contortus and Trichostrongylus colubriformis, known to be resistant to thiabendazole (LD90 for thiabendazole against H ontortus was 200 mg/kg bodyweight and against T colubriformis was 150 mg/kg). Fenbendazole at dose rates of 5, 10 and 20 mg/kg per os reduced total worm counts in H contortus infected sheep by 66, 90 and 100 per cent respectively, with similar reductions recorded for worm egg outputs. For the thiabendazole resistant strain of T colubriformis, fenbendazole reduced total worm counts in infected sheep by 4, 44 (40-48), 79 (75-83), 96 and 100 per cent at dose rates of 5, 10, 20, 40 and 80 mg/kg per os. Significant suppression of worm-egg production by thiabendazole resistant T colubriformis was obtained with fenbendazole at dose levels of 5 mg/kg and above. The implications of these results are discussed in the light of the increasing occurrence of strains of trichostrongylid nematodes resistant to currently available benzimidazole anthelmintics.

Animals↗

PubMed1976

[Analysis of thiabendazole in citrus fruits and bananas].

With regard to routine analyses in market control, the authors recommend two methods (according to the expected amounts of active principle) for the determination of thiabendazole residues on citrus fruits and bananas. The ultraviolet spectrophotometric method is preferable in determining thiabendazole contents of more than 1 p.p.m., if the cleaning operations described are respected. For the detection of thiabendazole and for the determination of amounts of less than 1 p.p.m. (the tolerance limit being 0.2 p.p.m. for pomes, berries, stone fruits, kernel fruits and also for potatoes) the thin-layer chromatographic method seems likewise to be suited (also in considering that it is semi-quantitative by nature); especially since the spectrophotometric method yields values by 0.2 p.p.m. too high (due to the measurement of residual absorption of vegetable constituents). The authors are of opinion that such an error must be considered to be too high for contents lower than 1 p.p.m.

Chromatography, Thin Layer↗

PubMed1975

Anti-inflammatory activity of thiabendazole and its relation to parasitic disease.

In 6 differnet animal assays in the laboratory, thiabendazole had clear anti-inflammatory effect, though it was less potent than aspirin in all assays. These findings add support to clinical suggestions that the drug may have anti-inflammatory properties in man. Such properties may contribute to the clinical response observed following the use of thiabendazole in cases of trichinosis, cutaneous larva migrans, visceral larva migrans, dracunculosis and scabies. In parasitic infections in which corticosteroids are commonly used in clinical management, notably trichinosis, the fact that thiabendazole does not appear to have immunosuppressive activity may confer an added clinical advantage.

Animals↗

PubMed1979

Gas-liquid chromatographic determination of thiabendazole and methyl 2-benzimidazole carbamate in fruits and crops.

A method is described for the electron capture gas-liquid chromatographic determination of thiabendazole and methyl 2-benzimidazole carbamate (MBC) after derivatization with pentafluorobenzyl bromide (PFB-Br). The samples are extracted with ethyl acetate, and the residual thiabendazole, benomyl, and MBC are isolated by liquid-liquid extraction into dilute HCl. After neutralization and re-extraction with ethyl acetate, thiabendazole and MBC are reacted with PFB-Br to form the PFB derivatives. Alumina column chromatography was used to clean up extracts, and the derivatives could be detected as low as 5-10 pg. Recoveries were 95-98% from fruits fortified with 0.3-2.0 ppm thiabenzadole; recoveries were 91-97% when 0.05-1.0 ppm benomyl/MBC were added to fruits/crops. The PFB derivatives were identified by gas-liquid chromatography-mass spectrometry.

Benzimidazoles↗

PubMed1978

The dose response of several benzimidazole anthelmintics against resistant strains of Haemonchus contortus and Trichostrongylus colubriformis selected with thiabendazole.

Dose response lines for eight benzimidazole anthelmintics and thiophanate were determined, using standardised strains of thiabendazole selected and resistant Haemonchus contortus and Trichostrongylus colubriformis. Against H contortus, thiophanate, thiabendazole, parbendazole and oxibendazole were inactive. Mebendazole was inactive at dose rates of 6.26 and 12.5 mg/kg, although significant activity occurred at 25 mg/kg. Fenbendazole, cambendazole, oxfendazole and albendazole demonstrated significant activity at dose rates equal to or greater than the recommended therapeutic level. Thiophanate was inactive against resistant T colubriformis. The remaining compounds only showed significant activity when used at dose rates in excess of the recommended therapeutic level. These results show that a side resistance exists among the benzimidazole anthelmintics and suggests that changes in dose response lines could be expected to occur if resistant strains are selected with benzimidazoles other than thiabendazole.

Animals↗

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↗

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↗

PubMed1979

Sicca complex and cholangiostatic jaundice in two members of a family probably caused by thiabendazole.

An entire family (father, mother, and three daughters) were given thiabendazole because one of the children had acquired pinworm infestation. The mother and one daughter (non-infected) developed a sicca complex (keratoconjunctivitis sicca and xerostomia) accompanied by cholangiostatic jaundice. Sjögren's syndrome is an autoimmune disease and presents many immune mechanism aberrancies. An association between autoimmune liver disease and sicca complex has been reported. Labeled mitochondrial antibodies bound to the parotid duct have been noted in patients with autoimmune cholangiostatic jaundice and such antibodies may be similar to the antibody against salivary duct found in Sjögren's syndrome. It is suggested that in these two patients, thiabendazole may have acted as a hapten and by binding to the body protein induced the production of autoantibodies which may have acted against the biliary epithelium, the salivary duct epithelium, and the lacrimal gland ducts.

Adolescent↗

PubMed1979

Teratologic assessment of maleic hydrazide and daminozide, and formulations of ethoxyquin, thiabendazole and naled in rats.

Teratogenicity studies were conducted in rats treated orally from days 6-15 of gestation with single daily doses of 400-1600 mg/kg of maleic hydrazide, 300-1000 mg/kg daminozide, 125-500 mg/kg ethoxyquin or thiabendazole, or 25-100 mg/kg naled. Dams were killed on the 22nd day of gestation, and fetuses were evaluated by routine teratologic methods. No adverse effect was related to any treatment other than an increased incidence of anomalous fetuses at the highest dose (500 mg/kg) of thiabendazole.

Animals↗

PubMed1979

The incidence of thiabendazole resistance in field populations of Haemonchus contortus on the northern tablelands of New South Wales.

A survey was undertaken to assess the incidence of thiabendazole resistance in field populations of H. contortus in sheep flocks on 40 farms distributed throughout the sheep grazing area of the northern tablelands of New South Wales. Treatment with thiabendazole at 66 mg/kg reduced H. contortus ova output by 96-100% in 18 flocks while in the remaining 22 there was a range of responses down to levels where the anthelmintic was without apparent effect. Factors which may contribute to the high incidence of anthelmintic resistance are discussed and the possibility of widespread resistance occurring in other sheep raising areas is considered.

Animals↗

PubMedDate not supplied

The treatment of dracontiasis with thiabendazole.

400 cases of dracunculosis were treated with Thiabendazole and the results reported. Thiabendazole appears to be highly effective and its pleasant taste and lack of adverse effects account for its acceptability by the patients. The drug is cheap and can be recommended even for poor patients. The adverse reactions are minimal and do not necessitate stoppage of therapy. We conclude the Mintezol is highly efficacious and should prove a useful weapon against Guinea worm disease.

Adolescent↗

PubMed1979

Trichostrongylus colubriformis and Ostertagia circumcincta resistant to levamisole, morantel tartrate and thiabendazole: occurrence of field strains.

Field strains of Trichostrongylus colubriformis and Ostertagia circumcincta, designated PF4 and PF5 respectively, were recovered from a farm on which the sole use of levamisole over a preceding 12 year period led to the development of anthelmintic resistance. The results of field observations and preliminary critical trials in both Merino and crossbred sheep showed that both species have varying degrees of resistance to three major anthelmintics; levamisole, morantel tartrate and thiabendazole. Mean worm count reductions for adult T colubriformis (PF4) for therapeutic doses of morantel tartrate, thiabendazole and levamisole in crossbreds were 45.7 per cent, 97.3 per cent and zero respectively, and for Merinos 80.7 per cent, 88.3 per cent and 92.0 per cent respectively. Against O circumcincta the corresponding reductions for crossbreds were 51.4 percent, 95.4 per cent and 20.3 per cent and for Merinos, 52.5 per cent, 73.1 per cent and 29.8 per cent. There was no statistically significant difference in the responses of both parasite species to either levamisole or morantel. This result suggests that resistance to the two chemically unrelated drugs may be co-inherited.

Animals↗