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Trace determination of carbendazim, fuberidazole and thiabendazole in water by application of multivariate calibration to cross-sections of three-dimensional excitation-emission matrix fluorescence.

The simultaneous determination of carbendazim, fuberidazole and thiabendazole was accomplished by cross-section (CS) fluorimetry in combination with multivariate calibration algorithms. The total luminescence information of the compounds was used to optimise the linear trajectories of the CS. A comparison between principal component regression (PCR) and two partial least squares (PLS) algorithms, PLS-1 and PLS-2, with different pre-processing methodologies was made. The final model, which applied the PLS-1 method, built using pesticide standard and emission spectra, was successfully used for the determination of these compounds in synthetic mixtures. However, a different PLS-1 multivariate calibration model, based on CS through the total luminescence spectroscopic data, was necessary for determining the cited pesticides in water samples. Mean centring was the best pre-processing technique in both PLS-1 models. This later calibration model was built from ultra-pure water samples spiked with known carbendazim, fuberidazole and thiabendazole concentrations, after solid-phase extraction (SPE). The method, which had a precision better than 5%, was shown to be suitable for carbendazim, fuberidazole and thiabendazole monitoring in water samples at trace levels.

Benzimidazoles↗

Thiabendazole vs. albendazole in treatment of toxocariasis: a clinical trial.

Between 1986 and 1988, 34 patients (age range six to 83 years) with visceral or ocular larva migrans were randomly assigned to a five-day treatment with thiabendazole 2 x 25 mg kg-1 day-1 (15 patients) or albendazole 2 x 5 mg kg-1 day-1 (19 patients). On the fifth treatment day, six patients (40%) in the thiabendazole group and 11 patients (58%) in the albendazole group showed excellent or good drug tolerability. Efficacy of treatment was assessed after 30 weeks (range six to 56 weeks). In the thiabendazole group, median eosinophilia remained at 14% and four patients (27%) were clinically cured. In the albendazole group, the median eosinophilia decreased from 10 to 3.5% and six patients (32%) were clinically cured. We recommend albendazole for treatment of visceral and ocular larva migrans with a minimum dose of 10 mg kg-1 daily for five days.

Adolescent↗

Strongyloides stercoralis in chronic renal failure: safe therapy with thiabendazole.

The pharmacodynamics of thiabendazole (TBZ) and its metabolite, 5OH-thiabendazole (5OH-TBZ), were studied in an anephric patient with Strongyloides stercoralis pneumonitis. No toxic manifestations were noted in the patient, and serum TBZ and 5OH-TBZ levels were comparable to those in eunephric patients. We conclude that thiabendazole, in the usual recommended dose of 25 mg/kg twice daily, given to patients with compromised renal function is reasonable and safe.

Adult↗

[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↗

[New trial with thiabendazole for treatment of human strongyloidiasis].

Okinawa prefecture is well known as an endemic area of Strongyloides stercoralis infection, and its recent infection rate was reported 6.2%, which was investigated by a new technique to detect S. stercoralis, agar plate method. Traditional treatment with thiabendazole was temporarily effective for S. stercoralis, but the recurrence rate was extremely high. We tried the new treatment for the purpose of complete eradication of the parasite. The patients were divided into two groups, who were given 500 mg of thiabendazole three times daily for 5 days and not medicated for the following 9 days. The medication was repeated 3 times in group 1 which consisted of 92 patients and 4 times in group 2 which consisted of 70 patients. Obtained results were as follows: 1) Six months after treatment, the cure rate was 89.5% in the only one course treatment, and 100% in more than 2 course treatments. 2) Side effects such as nausea, vomiting, anorexia or general fatigue were noted in 67.5% of all the patients after initial treatment, and 45.1% of the patients were dropped out of this trial. The dose of the drug was reduced in 32.1% of the patients, and only 22.8% were treated with full course of the regimen. 3) The elevation of S-GPT was observed in 33.8% of all patients. After initial treatment the rate was only 8.1%, but after 3 or 4 repeated course of treatments the rate was elevated to 39.0% and 45.4%, respectively. The liver injury was closely related to the total dose of thiabendazole and the period of the medication.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

Possible thiabendazole-induced theophylline toxicity.

Strongyloidiasis in immunosuppressed patients often requires prolonged administration of the antihelminthic, thiabendazole. The case described herein represents the first report of theophylline toxicity induced by concurrent administration of thiabendazole. Preliminary studies suggest that interference with theophylline clearance by thiabendazole may be the mechanism involved in this drug interaction.

Aged↗

Efficacy and safety of ivermectin and thiabendazole in the treatment of strongyloidiasis.

Treatment of strongyloidiasis has been traditionally based on thiabendazole, despite its frequent gastrointestinal side effects and failure to achieve eradication of the parasite from faeces in approximately 30% of cases. Ivermectin has been shown to be more effective for treating chronic uncomplicated strongyloidiasis. The efficacy and tolerability of these drugs in a series of patients treated from 1999 to 2002 at the Oliva Health Centre, Valencia, Spain, are reported. A total of 88 patients diagnosed of strongyloidiasis were treated using the following regimens: thiabendazole 25 mg/kg/12 h for 3 consecutive days in 31 patients; ivermectin 200 mug/kg as a single dose in 22 patients; and ivermectin 200 mug/kg for 2 consecutive days in 35 patients. The efficacy and side effects were recorded. A total of 65 patients were male, and 23 female. The mean age was 64 +/- 12 years. Of the patients, 44 had worked barefoot in rice fields. Among the 31 patients treated with thiabendazole, 25 (78%) met the criteria for cure (the absence of parasite in faeces after examination of three samples collected on alternate days), and 5 (16%) experienced side effects (asthenia, epigastralgia and disorientation). Of the 22 patients treated with ivermectin on a single day, 17 (77%) met the criteria for cure, and 2 (9%) reported side effects (dizziness, dyspepsia). Among the 35 patients treated with ivermectin on 2 consecutive days, 100% met the criteria for cure, and 0% experienced side effects. In chronic uncomplicated strongyloidiasis, a treatment regimen consisting of ivermectin 200 mug/kg for 2 consecutive days provided the best results with regard to efficacy and tolerability. When the eosinophilia continued after treatment, we observed a high percentage of not-cure rate (7 of 9 patients, 77%).

Animals↗

Application of a mixed-mode solid-phase extraction and cleanup procedure for LC/MS determination of thiabendazole and carbendazim in apple juice.

Recently, a mixed-mode solid-phase extraction (SPE) procedure was developed for rapid extraction and cleanup for determination of the fungicides thiabendazole and carbendazim in various fruit juices. This paper reports the application of that sample preparation procedure to the liquid chromatographic/mass spectrometric determination of these fungicides in apple juice with detection by positive electrospray ionization mass spectrometry (ESI/MS). Response was linear for sample concentrations from 2 to 500 microg/L (ppb). Recoveries averaged 74% (9% RSD) for carbendazim and 93% (9% RSD) for thiabendazole. After SPE cleanup, no matrix supression was observed for the ESI+ response for either compound studied. The method was applied to the analysis of incurred residues in 4 store-bought apple juices; carbendazim levels ranged from 10 to 70 microg/L and thiabendazole levels ranged from less than 2 to 130 microg/L.

Benzimidazoles↗

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↗

Prodrugs of thiabendazole with increased water-solubility.

The poor peroral absorption of benzimidazole anthelmintics limits their usefulness for the treatment of systemic infections such as alveolar or cystic echinococcosis. The low bioavailability has mainly been attributed to the low aqueous solubility of the benzimidazoles. Using thiabendazole as a model compound the prodrug approach was investigated as a mean to obtain derivatives with improved water-solubilities. Bioreversible derivatization of thiabendazole was performed by N-acylation of the benzimidazole moiety with various chloroformates as well as by N-acyloxymethylation. Both the N-alkoxycarbonyl and the N-acyloxymethyl derivatives were readily hydrolyzed to thiabendazole in human plasma and in rat and pig liver homogenates. The pH-rate profiles for the hydrolysis of the derivatives were determined and the lipophilicity of the compounds was assessed by partition experiments. The water-solubility of the N-alkoxycarbonyl derivatives was up to 12 times higher than that of the parent drug. An N-(4-amino-methylbenzoyl)oxymethyl derivative possessed a 300-fold higher water-solubility. The improved aqueous solubility, adequate lipophilicity and chemical stability combined with a facile enzymatic hydrolysis make such derivatives promising prodrugs for benzimidazole anthelmintics with the aim of improving the peroral bioavailability.

Chromatography, High Pressure Liquid↗

Effects of thiabendazole in Mansonella perstans filariasis.

Mansonella perstans is a human filarial parasite distributed across the center of Africa and equatorial America. Although M. perstans infection is asymptomatic in most individuals, a variety of symptoms have been described, including angioedema, pruritus, fever, ocular involvement, and serous cavities pain. Eosinophilia is found in many cases. Treatment with diethyl-carbamazine or mebendazole is often ineffective. We present a study on the effects of thiabendazole in the treatment of symptomatic M. perstans filariasis. Twenty-five patients were treated with thiabendazole at a single dose of 50 mg/kg for children and 3 g for adults. Sixteen out of 25 subjects repeated a second dose a week later. Parasite density, eosinophilia, and symptoms were significantly reduced after both one and two-step therapy in most patients. This study shows that thiabendazole may be effective in M. perstans infection. More studies are needed to determine a more effective dosage, or a putative combination treatment.

Adolescent↗

[Miticidal efficacy of thiabendazole against Otodectes cynotis (Hering, 1838) in dogs].

The aim of the present study was to evaluate the efficacy of thiabendazole on the treatment of Otodectes cynotis infestations in dogs. Ten naturally infested beagle dogs were used. The mites were diagnosed through otoscopy. Dogs were examined three days before treatment (day -3) and on the treatment day (day 0). They were randomly divided into two groups, five animals for the control group and five for the treated. During seven days, was applied in both ears of the treated dogs 1ml of the thiabendazole 5% solution, which correspond to 50mg of the product. All animals were reexamined through otoscopy on days +1, +3, +7, +10, +17, +24 and +31. The dogs on the control group showed mites in both ears during the whole period of observation. On the treated group the efficacy varied from 20% on the left ear to 80% on the right ear, on the first day after treatment. On days +3, +7, +10, +17, +24 and +31 the medium efficacy was 100% on both ears. The thiabendazole was efficient on the elimination of O. cynotis in dogs when used on the dose of 50mg per ear during seven following days.

Animals↗

Resistance of population-B equine strongyles to thiabendazole, oxfendazole, and phenothiazine (1981 to 1987).

Critical tests were completed on foals (n = 15) naturally infected with benzimidazole (BZ)-resistant population-B strongyles during the period between 1981 and 1987. Thiabendazole at a dosage of 44 mg/kg was tested in 8 foals, oxfendazole at 10 mg/kg was tested in 4 foals, and phenothiazine at 55 mg/kg, cambendazole at 20 mg/kg, and fenbendazole at 5 mg/kg were tested in 1 foal each. Efficacies of thiabendazole, cambendazole, and fenbendazole against the 5 species of BZ-resistant small strongyles (Cyathostomum catinatum, Cyathostomum coronatum, Cylicocylus nassatus, Cylicostephanus goldi, and Cylicostephanus longibursatus) were partial. Removals in the aggregate averaged 48%, 52%, and 68%, respectively, indicating continued resistance of the 5 species of small strongyles to thiabendazole, cambendazole, and fenbendazole. In contrast, oxfendazole was efficacious, removing an aggregate average of 95% of the 5 BZ-resistant species of small strongyles in the 4 foals. This apparent reversion to susceptibility to oxfendazole may be attributable to paucity of reference data (1 test foal) done in 1976. All 5 species of the BZ-resistant small strongyles had cross resistance to phenothiazine (38% aggregate removal), whereas 9 of the BZ-susceptible species were effectively (99%) removed. This suggests a similar mode of action between phenothiaznie and the BZ compounds.

Animals↗

Enzyme-linked immunosorbent assay of benomyl and thiabendazole in some foods.

Enzyme-linked immunosorbent assays were developed for benomyl as its decomposition product, methyl 2-benzimidazole carbamate, and thiabendazole in foods. Immunogens consisting of human serum albumin coupled to 2-succinamidobenzimidazole or 2-(2'-succinamido-4'-thiazolyl)benzimidazole were used in rabbits to raise antisera that were specific for the respective fungicides. Lower limits of quantitation of 0.35 ppm for benomyl and 0.03 ppm for thiabendazole were established without cleanup of the ethyl acetate extract. Recoveries of benomyl from 3 crops spiked at 0.5 to 10 ppm averaged 89% (range 73-109%) and of thiabendazole from 5 crops spiked at 0.1 to 2.0 ppm were 93% (range 81-105%).

Animals↗

Monitoring residues of carbendazim (applied as benomyl) and thiabendazole in Wellspur apples.

Residues of benomyl (determined as carbendazim, widely accepted as MBC) and of thiabendazole in Wellspur apples were monitored after the apples were treated postharvest by immersion in a bath with each of the fungicides separately and stored under refrigeration. Whole fruit and pulp analyses were conducted over the period beginning 1 day after treatment and lasting up to 200 days afterwards. Under the conditions described, both benomyl (expressed as parts per million of carbendazim) and thiabendazole were found in the fruits in the following average amounts: 0.44 +/- 0.03 and 0.11 +/- 0.03 ppm benomyl (as carbendazim) in whole fruit and in pulp, respectively; 0.98 +/- 0.10 and 0.39 +/- 0.10 ppm thiabendazole in whole fruit and in pulp, respectively.

Benzimidazoles↗

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↗

Trichinosis: thiabendazole in the treatment of 11 cases.

We have studied 11 cases of acute human trichinosis; five of these patients were treated with thiabendazole. We have reviewed the laboratory data for these patients and described their course. This study has failed to show any definite effect of thiabendazole on the course of human trichinosis at the doses used. However, thiabendazole may have decreased the infectivity of the larvae which were embedded in the muscles of our patients.

Acute Disease↗

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↗