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PubMed1979

The metabolism of nitrophenolic and 5-arylazorhodanine anthelmintics by Ascaris suum, Moniezia expansa and by mouse- and sheep-liver enzymes.

1. The anthelmintics disophenol (2,6-diiodo-4-nitrophenol), nitroxynil (3-iodo-4-hydroxy-5-nitrobenzonitrile) and nitrodan (3-methyl-5-(4-nitrophenylazo)rhodanine) were reduced in vitro to the corresponding amines by intact Ascaris suum, Moniezia expansa, by enzymes prepared from these helminths, and by mouse- and sheep-liver homogenates. Helminth reductases required NADH2 and glutathione as cofactors and were inhibited about 50% by 2.0 x 10(-7) M allopurinol. Azo bonds of nitrodan and its analogues were not reduced by the helminths but were reduced by mouse- and sheep-liver enzymes. 2. Mouse- and sheep-liver enzymes, in addition to effecting nitro reduction, metabolized nitroxynil by hydrolysis to 3-iodo-4-hydroxy-5-nitrobenzamide and 3-iodo-4-hydroxy-5-nitrobenzoic acid. No hydroxylation products were found. Nitrodan was oxidized by the mammalian microsomal oxidation enzyme system to the thiazolidinedione derivative, but not by helminth enzymes.

Animals↗
PubMed2003

[Determination of benzimidazole anthelmintics in livestock foods by HPLC].

A simple and rapid liquid chromatographic method was developed for the simultaneous determination of twelve benzimidazole anthelmintics in livestock foods using reversed-phase high-performance liquid chromatography with photodiode array detection (PDA). A sample was homogenized with acetonitrile and n-hexane, and centrifuged. The acetonitrile phase was isolated and evaporated. The residue was dissolved in 0.1 mol/L carbonate buffer solution (pH = 9.1), sonicated, and then subjected to clean-up on a Bond Elut LRC-C18 cartridge. The benzimidazole compounds were separated isocratically on a Capcell Pak C18 UG 120 (5 microns, 150 x 4.6 mm i.d.) column and detected by PDA at 295 and 313 nm. Mixtures of acetonitrile and 0.05 mol/L ammonium acetate in mixing ratios of (20:80) and (40:60) were used as the mobile phase, and the flow-rate was 1.0 mL/min at 40 degrees C. The mean recoveries (n = 3) from 0.1-0.5 microgram/g added samples were 72.6-97.2% with coefficients of variation of 0.3-8.5%. The detection limits were 0.01-0.05 microgram/g.

Animals↗
PubMed2002

A questionnaire survey of the management and use of anthelmintics in cattle and antelope in mixed farming systems in Zimbabwe.

A survey of the management of mixed farming of cattle and antelope and use of anthelmintics was conducted on eleven farms between August and December 1999 by a self-administered questionnaire. Seventeen antelope species ranging from grey duikers (Sylvicapra grimmia) to eland (Taurotragus oryx) occurred on the farms. Impala (Aepyceros melampus) was the most abundant antelope on the farms. Seventy-five per cent of the antelope species on the farms were grazers and mixed feeders and shared grazing with cattle. Most farmers (n = 8) did not consider the stocking density for cattle and antelope as an important management factor. Fifty-four per cent of the farmers (n = 6) routinely dewormed both cattle and antelopes. Albendazole and fenbendazole were the most commonly used drugs for deworming cattle (72.7%) and antelope species (54.5%). The deworming of antelope was carried out during the dry season, using albendazole-, fenbendazole-and rafoxanide-medicated supplementary feed blocks. Doramectin injections were given to antelopes on two farms. Cattle were dewormed preventively and according to the general body condition of the animal. Few farmers (n = 4) followed the recommended deworming programme for cattle in Zimbabwe and only one farmer followed a specified dosing programme for game. However, results from the survey on the deworming of game indicate that farmers perceived helminth infections in antelope to be important.

Animals↗
PubMed2002

An introductory survey of helminth control practices in south africa and anthelmintic resistance on Thoroughbred stud farms in the Western Cape Province.

Fifty-one per cent of 110 questionnaires, designed for obtaining information on helminth control practices and management on Thoroughbred stud farms in South Africa, were completed by farmers during 2000. The number of horses per farm included in the questionnaire survey ranged from 15 to 410. Foals, yearlings and adult horses were treated with anthelmintics at a mean of 7.3 +/- 3.0, 6.6 +/- 2.7 and 5.3 +/- 2.3 times per year, respectively. An average of 3.4 different drugs were used annually, with ivermectin being used bymost farmers during 1997-2000. On 43% of farms the weights of horses were estimated by weigh band and 45% of farmers estimated visually, while both were used on 7% of farms and scales on the remaining 5%. Doses were based on average group weight on 50% ofthe farms and on individual weights on 46%. Forty-three per cent of farmers performed faecal egg count reduction tests (FECRT). Most farmers rotated horses between pastures and treated new horses at introduction. Faecal removal was practiced on 61% of farms and less than 50% of farmers used alternate grazing with ruminants. Faecal egg count reduction tests were done on 283 horses, using oxibendazole, ivermectin and moxidectin on 10,9 and 5 farms, respectively, in the Western Cape Province during 2001. While the efficacy of oxibendazole was estimated by FECRT to range from 0-88% and moxidectin from 99-100%, ivermectin resulted in a 100% reduction in egg counts. Only cyathostome larvae were recovered from post-treatment faecal cultures.

Animals↗
PubMed1981

Anthelmintic efficacy of amoscanate (C 9333-Go/CGP 4540) against various infections in rodents, dogs and monkeys.

The anthelmintic activity of Amoscanate (C 9333-GO/CGP 4540) has been studied in experimental infections with the human hookworm, Necator americanus, in hamsters; Nematospiroides dubius, Hymenolepsis nana and natural infections with Syphacia obvelata in mice; Ancylostoma caninum, A. ceylanicum in mongrel dogs; Oesophagostomum apiostumum and Strongyloides fuelleborni in rhesus monkeys. Single oral doses of 30-60 mg/kg eliminated 94 to 99% of the total Necator parasites in 37-day-old non-patent infection, while single oral doses of 25 mg/kg expelled the entire worm burden in patient infection in hamsters. When incorporated in feed at the 0.01% level and administered ad lib. to hamsters at 20, 27 and 34 days postexposure for 5 days, the worm burdens were reduced 88 to 94%. N. dubius was completely eradicated by a single oral dose of 200 mg/kg while S. obvelata and H. nana were expelled at doses of 12.6 mg/kg and 50 mg/kg, respectively. A dose of 25 mg/kg in dogs produced 100% fecal egg reduction in hookworm and 99% in ascarid infections. The drug at 3 x 2.5 mg/kg administered at 4-hour intervals produced similar effects in mixed A. caninum and A. ceylanicum infections. Against natural infections of S. fulleborni and Oe. apiostumum in rhesus monkeys the drug showed 100% efficacy at a dosage of 60 mg/kg administered thrice at 12-hour intervals.

Administration, Oral↗
PubMed1993

Synthesis and anthelmintic activity of 13-alkoxymilbemycin derivatives.

The synthesis of milbemycin derivatives having alkyloxy groups at the C-13 position was studied and a series of these analogs of milbemycin A4 and A3 was prepared by the reaction of 13-iodomilbemycin with a variety of alcohols. 13 beta-Phenethyloxy derivatives were found to possess excellent anthelmintic activity. Especially, the activities of derivatives with N-substituted 4-aminophenethyloxy groups were comparable to or superior to ivermectin against Nippostrongylus brasiliensis in rats.

Animals↗
PubMed2001

Cephaibols, new peptaibol antibiotics with anthelmintic properties from Acremonium tubakii DSM 12774.

Two groups of new peptaibol-type antibiotics termed cephaibols have been isolated from the fungus Acremonium tubakii, DSM 12774. These 16- or 17-unit straight-chain peptides, whose structures were characterized by amino acid analyses, 2-D NMR experiments, and by mass spectrometric sequencing, have a high content of the unusual amino acids aminoisobutyric acid and isovaline. The principal constituent of the novel peptaibol mixture is cephaibol A, which is formed in abundance in cultures of the wild strain. The striking biological property of cephaibol A is its pronounced anthelmintic action and activity against ectoparasites.

Acremonium↗
PubMed1989

Effect of selected anthelmintics on three common helminths in the brown pelican (Pelecanus occidentalis).

The effect of selected anthelmintics (albendazole, fenbendazole, piperazine dihydrochloride and clorsulon) against three major helminths (Contracaecum multipapillatum, Mesostephanus appendiculatoides, and Phagicola longus) were studied in 29 brown pelicans (Pelecanus occidentalis). Albendazole and fenbendazole were highly effective against all three parasites. Clorsulon had moderate effect against M. appendiculatoides and poor effect against C. multipapillatum and P. longus. Piperazine dihydrochloride had no effect against these helminths.

Albendazole↗
PubMedDate not supplied

Relationships between the anthelmintic activity of eight derivatives of benzimidazole carbamates against Trichinella spiralis and their chemical structures.

Efficacy of eight recently developed and used anthelmintics of the benzimidazole carbamates; mebendazole, flubendazole, oxfendazole, albendazole, oxibendazole, 790163 proflubendazole, 780118 "cyanide" benzimidazole and 780120 "selenium" benzimidazole was tested orally against the enteral immature larval and adult stages of Trichinella spiralis in mice. Six of these derivatives of methyl benzimidazole-2-carbamates have an aryl and two have an alkyl substituent at the 5'-position of the parent benzimidazole ring. The nature of these substituents was found to be related to the antitrichinellous activity of the compounds. Compounds with the 5'-substituent linked to the parent benzimidazole ring by either a carbon, sulfur or an oxygen atom are more potent than those bridged by selenium or by the carbon with an attached-CN group. The result clearly indicates that the benzimidazoles are invariably more potent against immature enteral phase than the adult worms. This finding would be of importance in a targeted synthesis of new, effective derivatives of benzimidazole, e.g., in the screening for more important tissue-dwelling nematodes like filarial worms.

Animals↗
PubMed1976

Uredofos: anthelmintic activity against nematodes and cestodes in dogs with naturally occurring infections.

A new broad-spectrum anthelmintic, uredofos, was tested in 146 dogs by single and multiple oral dosing. Single doses of 100 and 50 (but not 25) mg/kg were totally effective in removing Dipylidium caninum and Taenia spp from 46 dogs with infections of tapeworms. Among groups of 15 to 20 dogs, the average percentage efficacies against Toxocara canis for single soese of 100, 50, and 25 mg/kg were 98, 96, and 81%, respectively. The average percentage of efficacies against hookworm (Ancylostoma caninum) were greater than 96% in dogs treated with single doses of 100, 50, or 25 mg/kg and were 100% in the 35 dogs given 2 or 3 treatments (24-hour intervals) at dose levels of either 25 or 50 mg/kg. The whipworm, Trichuris vulpis, was not efficaciously eliminated by single doses of 25, 50, and 100 mg/kg (av percentage of efficacies of 30, 35, and 71%, respectively). Efficacy against T vulpis markedly improved when 2 doses were given at a 24-hour interval (av percentage of efficacies were 89% at dose level of 25 mg/kg and 99% at dose level of 50 mg/kg). At either dose (25 or 50 mg/kg), 3 daily treatments were no more efficacious against whipworms than were 2 doses. There was no evidence of drug toxicosis in any dogs tested. It was concluded that uredofos is highly effective against canine tapeworms, ascarids, and hookworms when given as a single dose of 50 mg/kg and against whipworm when given at dose level of 50 mg/kg/day for 2 days.

Ancylostomiasis↗
PubMed1999

In vitro studies on the effects of some anthelmintics on Cotylophoron cotylophorum (Digenea, Paramphistomidae): a structural analysis.

The effects of the anthelmintics praziquantel (PZQ), levamisole (LEV), mebendazole (MBZ), fenbendazole (FBZ) and albendazole (ABZ), on the morphology and the histology of a digenetic trematode, Cotylophoron cotylophorum, were studied. Scanning electron micrographs of the drug-treated worms revealed that PZQ was the most effective drug inducing surface damages to a great extent. The parasite exposed to PZQ for 6 h, showed smaller blebs on the oral sucker region as well as on the sensory papillae. These blebs enlarged in size after 24 h and ruptured after 30 h of exposure. The worms treated with LEV showed a few smaller blebs on the ventrolateral margin. In MBZ- and FBZ-treated worms the blebs appeared between the oral and genital sucker after 6 h of incubation. The changes were not apparent in the ABZ-treated worms.

Albendazole↗
PubMed1975

Anthelmintic treatment of subclinical parasitism of feedlot cattle in Georgia.

Forty heifer calves, 27 yearling heifers, and 64 yearling steers with naturally occurring infections of nematode parasites were treated with levamisole HCl or morantel tartrate or were not treated. Although heifer calves had much larger worm egg counts before treatment than yearling heifers, necropsies showed a smaller average number of nematodes in the calves. Both anthelmintics significantly reduced the egg counts. At the end of the experiments, 98 to 240 days after treatments, there was no significant difference among groups of cattle in respect to necropsy worm counts. An advantage of 5% in rate of gain in body weight was shown in each experiment or phase of an experiment in favor of the treated groups of cattle. Overall, an advantage of 6% in feed efficiency was calculated for the treated groups of cattle.

Animal Feed↗
PubMedDate not supplied

Screening of indigenous plants for anthelmintic action against human Ascaris lumbricoides: Part--II.

Alcoholic extracts of the rhizomes of Alpinia galanga, Andrographis paniculata, bark of Cinnamomum zeylanicum, rind of Citrus decumana, Desmodium triflorum, seeds of Hydnocarpus wightiana, rhizomes of Kaempfaria galanga, Lippia nodiflora, tender leaves of Morinda citrifolia, rhizomes of Pollia serzogonian, Tephrosia purpuria and rhizomes of Zingiber zerumbeth showed good in vitro anthelmintic activity against human Ascaris lumbricoides. While, the alcoholic extracts of the bark of Alibzzia lebbek, the bulb of Allium sativum, rhizomes of Alpinia calcaratta, rind of Citrus acida, rind of Citrus aromatium, rind of Citrus medica, rhizomes of Curcuma aromatica and rind of Punica granatum showed moderate invitro activity.

Animals↗
PubMed1975

Detection of activity for various anthelmintics against in vitro-produced Cooperia punctata.

The in vitro-grown parasitic stages of Cooperia punctata were used to evaluate 28 compounds with different kinds and degrees of in vivo activity. Using presumptive and confirmatory tests, it was possible to establish a group order of in vitro potency that compared favorably with an order based on established in vivo use of these compounds. The procedure lends itself to evaluating activity against a given parasitic growth stage and gives a quantitative estimate (range) of the concentration that produces 50% nematode kill. The system was most successful in detecting compounds with in vivo activity for C punctata, followed in order by compounds active against Cooperia spp, other gastrointestinal nematodes of ruminants, and other nematodes of non-bovine hosts. The procedure showed some differentiation between activity against nematodes versus that against cestodes, trematodes, and arthropods. The system permits considerable flexibility in experimental design, thus making possible the acquisition of the particular information desired. In addition to establishing lethal effects on the nematode, the procedure detected compounds with nematode-anesthetizing effects. The results indicate this in vitro system can be used with some expediency as a preliminary screening method in the search for new anthelmintic compounds.

Animals↗
PubMed2002

Determination of benzimidazole anthelmintics in animal-derived biological matrices.

This paper describes an easy multiresidue procedure for the determination of 8 benzimidazole anthelmintics (Albendazole, Albendazole sulphone, Albendazole sulphoxide, Ox-bendazole, Ossibendazole, p-OH-Fenbendazole, Fenbendazole, Flubendazole) in foodstuffs of animal origin for human consumption. According to the proposed procedure, 10 g of homogenised sample were extracted with acetonitrile in ultrasonic bath, the organic layer was evaporated to dryness and the residue dissolved in HCl 0.005 M. After an initial washing with hexane to remove fats, the aqueous layer was purified on SPE C2 column and the analytes were eluted with methanol, evaporated to dryness and reconstituted with phosphate buffer/acetonitrile (50/50). The solution obtained was analysed by HPLC with diode array detector (DAD); this detector provides useful information about the peaks present in routine samples, because it gains not only retention times of analytes, as well as their UV-spectra. Benzthiazuron was used as internal standard and the method was validated in the range 10-100 ppb, as requested by the imposed limits. The mean recoveries in spiked samples ranged between 70% and 95%, for 10 and 100 ppb respectively. The developed method resulted sensitive, simple and fast. It is particularly suitable for laboratories that execute screening analysis on a great number of samples, observing the EC regulations that establish the benzimidazole Maximum Residue Limits (MRLs) in food.

Animals↗
PubMed1992

[Study on toxicology of a new anthelmintic "85012"].

"85012", a new anthelmintic containing amidine synthesized in our laboratory, was experimentally effective against Nippostrongylus braziliensis and Ancylostoma caninum. In acute and subacute toxicity test, it was proved lowly toxic. There was no evidence that the drug induced any damages to main organs and tissues of animals. In order to evaluate its potential mutagenicity and teratogenicity, micronucleus test, bone marrow metaphase analysis, CHL cells chromosomal aberration assay, spermatic aberration test as well as teratogenicity test were performed. No mutagenic and teratogenic effects were observed.

Amidines↗
PubMed1992

[Treatment of soil-transmitted helminth infections by anthelmintics in current use].

The efficacy of broad-spectrum anthelmintics in current use was studied in Hengshan County, Hunan Province. The vermicides under study include albendazole (400mg, single dose), mebendazole composite (mebendazole 100 mg and levamisole 25mg bid x 3d), oxantel pyrantel pamoate composite (pyrantel pamoate 150 mg and oxantel pamoate 150 mg bid x 2d), and pyrantel pamoate composite (base 10 mg/kg, single dose). Therapeutic effect assessed 2 weeks after medication revealed Ascaris egg negative rates or cure rates (CR) of 97.5-100% for the former 3 regimens, and 80.9% for the latter one; while CR for hookworm infection were 95.4%, 78.6-100%, 96.7% and 83.3%, respectively. A follow-up survey pursued 4 weeks post treatment showed no significant difference in CR for the above regimens. Judging from CR in Trichuris trichiura infection, pyrantel pamoate composite was recommended as the drug of choice (89.3%), which was followed by mebendazole composite (64.6-83.8%) and albendazole (28.2-42.6%), whereas pyrantel pamoate was inefficacious. Obvious egg reduction rates were evidenced post application of the above drugs in trichuriasis treatment except pyrantel pamoate at single dose.

Albendazole↗
PubMed1978

Anthelmintic efficacy of albendazole against adult Dictyocaulus viviparus in experimentally infected calves.

Anthelmintic activity of albendazole against adult Dictyocaulus viviparus was evaluated in a controlled experiment. Calves were raised nematode-free to approximately 8 weeks of age and were each given 4,000 infective 3rd-stage larvae. Twenty calves with patent parasitisms were allotted to 2 groups of 10 calves each. Calves in group 1 were used as nonmedicated controls, and calves in group 2 were given albendazole in paste formulation at the dosage concentration of 7.5 mg/kg of body weight on the 30th day after administration of infective larvae. At necropsy, nonmedicated control calves had a total of 308 adult D viviparus, whereas the albendazole-treated calves had 11, for an average efficacy of 96.4%. These reductions were statistically highly significant (P less than 0.01). At necropsy, none of the treated calves was passing 1st-stage C viviparus larvae in their feces, whereas control calves were passing an average of 46 larvae/10 g of feces.

Animals↗