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PubMedDate not supplied

[The adenosinetriphosphatases of trematodes parasitizing cattle and the effect on them of anthelmintic preparations].

Activities and properties of adenosine triphosphatases in mitochondrial and microsomal fractions of trematodes Eurytrema pancreaticum and Calicophoron ijimai were studied. The highest ATPase activity was observed in mitochondrial fractions. The effect of anthelmintic preparations on activity of enzyme was investigated. Trichlorophene, bitionol, oxinide, G-937 and G-1028 turned out to be the most effective preparations.

Adenosine Triphosphatases↗
PubMed1993

Synthesis and potential anthelmintic activity of methyl-5-(4-salicyloyl-piperazin-1-yl)-benzimidazole-2-carbamates.

A series of methyl-5-(4-salicyloyl-piperazin-1-yl)-benzimidazole-2-carba mates (IX) has been prepared. 5-(4-Salicyloyl-piperazin-1-yl)-2-nitro anilines (VII) have been synthesized starting from 5-piperazino-2-nitro anilines and salicyloyl chlorides. Catalytic reduction of VII with Pd/C, followed by treatment with 1,3-dicarbomethoxy-S-methyl isothiourea, yielded the corresponding carbamates (IX), the anthelmintic activity of which was studied. Compound IXa significantly reduced the numbers of preadults, adults and encysted T. spiralis larvae in experimental mice.

Animals↗
PubMed1977

Critical evaluation of oxfendazole as a swine anthelmintic.

Sixty feeder pigs with mixed naturally acquired nematode infections were medicated with oxfendazole, a new benzimidazolecarbamate compound, at dose levels of 0, 3, 9, and 18 mg/kg of body weight. The dosage of 3.0 mg/kg administered once in the feed proved as efficacious as larger dosages and the same dosage administered 2 or 3 times in the removal of adult Ascaris suum, Oesophagostomum dentatum, and Metastrongylus pudendotectus. Trichuris suis adults were less susceptible. Anthelmintic efficacy was based upon comparative nematode egg counts, appearance of eggs, and recovered nematode burdens at necropsy. Signs of toxicosis were not seen in pigs given any one of the medicated feed schedules.

Animals↗
PubMed1995

[Anthelmintics resistance in gastrointestinal nematodes in domestic animals].

In Belgium benzimidazole resistance has been reported in 28% of the sheep farms and 29 to 50% of the studs. In several member states of the European Union the prevalence of anthelmintic resistance (AR) is even higher than in Belgium, although AR is nearly absent in some countries of Southern Europe. AR is particularly widespread in certain nematodes of sheep, goats and horses in Europe, whereas only sporadic cases of AR have been reported in helminths of cattle. In Belgium only one case of AR has been described in goat and one in cattle; no surveys for AR have been carried out in pigs. The main helminth species, in which AR has been observed, are Haemonchus contortus, Ostertagia circumcincta and Trichostrongylus spp. in small ruminants, the Cyathostominae in horses and Oesophagostomum spp. in pigs. Resistance has developed particularly against the benzimidazoles and to a lesser extent against the levamisole/morantel group. Up to now the prevalence of ivermectin resistance remains low, but the number of cases is increasing during recent years. Due to the low sensitivity of the currently used techniques for the detection of AR (egg count reduction test and in vitro egg hatch test) the available figures underestimate the prevalence of AR. Finally, possible control measures are discussed in order to avoid or to delay the development of resistance.

Animals↗
PubMed1995

[Resistance to anthelmintics in nematodes in sheep and goats].

The article offers a brief view on the most important theoretical knowledge of resistance of gastrointestinal nematodes to anthelmintic drugs in sheep and goats. Besides the definition and basic terms, factors of development and occurrence of resistance on farm are analyzed. Furthermore, methods for detection of resistant nematodes as well as complex of recommended preventive measures are given.

Animals↗
PubMed1977

Effect of three anthelmintics on weight gain of feedlot cattle.

Three groups of 50 heavy feedlot steers were treated with 1 of 3 anthelmintics (haloxon, tramisol, or thiabendazole). One group of 50 steers was not treated and served as a control. The initial degree of infection with gastrointestinal nematodes was light and decreased during the course of the study. There were no significant differences in weight gains among any of the groups at the end of a 113-day feeding period.

Animals↗
PubMedDate not supplied

[The results of micromorphological and histochemical studies of the musculocutaneous sac of nematodes in the suborder Oxyurata after anthelmintic exposure].

The paper presents the results of studies of the effects of anthelminthic agents on the in tegumentary tissues of nematodes from the Oxyurata suborder. All used anthelmintics causes varying structural changes in the integumentary tissues of Oxyurata. At the same time, there is swelling and loosening of the cuticle, its detachment from the subcuticular layer, vacuolization of the hypodermis and the plasma part of muscular cells, as well as irreversible changes in the cellular organoids of the hypodermis and muscular cells (destruction of canals of the endoplasmic network and the Golgi apparatus, mitochondrial membrane damage, nuclear pyknosis or lysis etc.)

Animals↗
PubMed1996

In vitro effects of anthelmintics on the histochemistry of Haemonchus contortus and Trichuris globulosa.

In vitro incubation of Haemonchus contortus (RUD., 1803) and Trichuris globulosa (v. LINSTOW, 1901) were proformed for 10-12 h in Tyrode's solution and 10 and 50 micrograms/ml concentrations each of albendazole (ABZ), fenbendazole (FBZ), thiophenate (TP), dl-tetramisole and oxyclozanide (TO), dl-tetramisole HCI (TMS) and levamisole HCI (LMS) to study morphological and histochemical alterations. The major structural changes observed after treatment with all the drugs were vacuolation in the intestine of H. contortus except with TP treatment and disruption of the epithelium in T. globulosa except with TMS treatment. The other major alteration in T. globulosa was the loss of muscle striations after TP, TO, TMS and LMS treatments. All the six anthelmintics reduced the quantity of neutral mucopolysaccharides in the intestine of H. contortus and T. globulosa except with TMS and LMS treatments in the latter. Acidic mucopolysaccharides detected in the microvilli of the intestine of H. contortus were lost after TO and ABZ treatments. The loss of lipids from the intestine was evident after TO, ABZ, FBZ and TP treatments in H. contortus and by all the drugs in T. globulosa. LMS treatment caused accumulation of very large lipid droplets in the intestine of H. contortus.

Animals↗
PubMed1996

[Helminth nervous system as a field for anthelmintic action].

In the review the results of the recent investigations and new ideas about the mode of action of neurotoxic anthelmintics are presented and discussed. Investigations of this group of drugs are very difficult, because our knowledge about neural system in helminths is still insufficient. However, some new perspectives have appeared recently. They concern such future targets of the drugs as acetylcholine transferase in filariae, a binding-site for ivermectin in Ascaris sp. or neuropeptides in nervous or neuromuscular system in Ascaris sp. The application of recombinant DNA techniques for cloning of parasite receptors, ion channels and protein involved in signal-transduction can be expected to lead to rapid progress in this field.

Animals↗
PubMed1977

Anthelmintic efficiency of oxfendazole in California lambs.

Oxfendazole, methyl 5(6)-phenylsulfinyl-2-benzimidazole carbamate, was given by oral drench (5 mg/kg) to California lambs harboring natural infections of gastrointestinal nematodes. Ninety-nine percent of adult Ostertagia circumcincta, Ostertagia trifurcata, Trichostrongylus axei, Trichostrongylus vitrinus, Trichostrongylus colubriformis, Nematodirus filicollis, and Nematodirus spathiger were removed by the anthelmintic.

Animals↗
PubMed1977

Anthelmintic activity of albendazole against gastrointestinal nematodes in calves.

Anthelmintic activities of albendazole were evaluated in a controlled experiment. Forty calves experimentally infected with gastrointestinal nematodes were allotted to 4 groups. Calves in group 1 were used as nonmedicated controls; calves in groups 2, 3, and 4 were given (by oral route) a suspension containing albendazole at dose concentrations of 2.5, 5.0, and 7.5 mg/kg of body weight on the 35th day after administration of infective nematode larvae. In groups 2, 3, and 4 calves, average overall reductions (based on geometric means) were 77.1, 93.6, and 98.1%, respectively. These reductions were highly significant (P less than 0.01) in calves given doses of 5.0 and 7.5 mg/kg, and were significant (P less than 0.05) in calves given the 2.5-mg/kg dose. Ostertagia ostertagi, Trichostrongylus axei, Cooperia onchophora, Cooperia punctata, and Oesophagostomum radiatum removals at the 5.0- and 7.5-mg/kg dose levels were all highly significant (P less than 0.01); whereas, removals of Haemonchus contortus were not significant, even at the 7.5-mg/kg dose level.

Animals↗
PubMedDate not supplied

[Isocitrate dehydrogenases of trematodes parasitizing cattle and the feasibility of inhibiting them using anthelmintic preparations].

Activities and properties of NADF-dependent isocitrate dehydrogenases in cytosol and mitochondrial fractions from trematodes Eurytrema pancreaticum and Calicophoron ijimai were examined. Cytosol and mitochondrial enzymes were activated by ions Mn2+ and Mg2+ and inhibited by ions of heavy metals and p-chloromercuribenzoate. The effect of anthelmintic preparations on activity of enzymes was investigated.

Animals↗
PubMed1998

The anthelmintic albendazole affects in vivo the dynamics and the detyrosination-tyrosination cycle of rat brain microtubules.

Albendazole (ABZ) is an anthelmintic benzimidazole drug widely used in human and veterinary medicine. ABZ has binding affinity to both mammalian and helminth parasite tubulin. In the current work, we have performed in vitro assays and in vivo experiments in which rats were given ABZ orally to better characterize the action of the drug on the polymerization of rat brain microtubules and on the detyrosination/tyrosination cycle that occurs on the COOH-terminal end of alpha-tubulin. The results showed that ABZ inhibits brain microtubule polymerization in vitro, and significantly delayed microtubule assembly in vivo. The tyrosination reaction cycle was not affected in vitro; however, in rats to which the drug was administered orally, the levels of in vitro tyrosination were reduced when compared to the controls with mock treatment. These results suggest that this apparent inhibition would be due to a decrease in the amount of substrate caused by the depolymerizing effect of ABZ and the subsequent tyrosination in the intact brain with endogenous tyrosine. In conclusion, ABZ strongly affects tubulin dynamics both in vivo and in vitro. The outcome of these experiments is a contribution to the understanding of the molecular mechanisms involved in the antimicrotubular action of benzimidazole compounds.

Albendazole↗
PubMed1987

Qualitative and quantitative analysis of the anthelmintic fenbendazole and its metabolites in biological matrices by direct exposure probe mass spectrometry.

Methodology for the qualitative and quantitative analysis of the anthelmintic fenbendazole and its metabolites in goat feces using electron impact (EI)/direct exposure probe (DEP)/mass spectrometric (MS) and tandem mass spectrometric (MS/MS) techniques is presented. Analyses were conducted on extracts from spiked feces and feces from animals treated per os with 5 mg fenbendazole/kg, with samples being collected at zero time and at twelve hour intervals for 144 h. The results of the EI/DEP/MS quantitation of these samples are compared to those for the same samples analysed by high pressure liquid chromatography (HPLC). Mass spectral data for fenbendazole and its metabolites are presented and the advantages of the use of EI/DEP/MS and/or DEP/MS/MS over HPLC are discussed. This methodology may be used as a confirmatory method for the HPLC analysis of fenbendazole and its metabolites or may be used as a method in its own right for the rapid qualitative and quantitative analysis of these compounds.

Animals↗
PubMedDate not supplied

Oral toxicity in weanling and adult rats and in vitro genotoxicity of the veterinary anthelmintic rafoxanide.

The oral toxicity of the veterinary anthelmintic Rafoxanide was evaluated in newborn rats exposed in utero and during lactation. In another group, 3 months of oral treatment started after weaning. Rafoxanide administration to dams (10 mg kg-1) decreased the number of pups per litter, induced high mortality (42%) and delayed the growth of offsprings before weaning. Histopathological examination of the central nervous system revealed vacuolation of the white matter. Vacuolation was particularly severe in the cerebellum of the 14-21-day-old rats. Rafoxanide induced, in some pups (35%), the formation of cataracts. These toxic effects seemed to be reversible and were no longer detectable after a further 3-month administration of Rafoxanide (10 mg kg-1) to rats born of treated dams. In adult rats treated orally for 3 months with 1, 5 or 25 mg kg-1 Rafoxanide, biochemical and haematological tests did not reveal dose-related effects. Rafoxanide had no mutagenic activity in the Ames and CHO/HGPRT tests.

Aging↗
PubMed1978

Mutagenicity studies with praziquantel, a new anthelmintic drug, in mammalian systems.

Praziquantel, a new anthelmintic drug with antischistosomal and anticestodal properties, was tested in comparison with a placebo control and a 'positive control' with cyclophosphamide in mammalian test system in vivo for potential mutagenic effects. The test systems used and the tested doses of Praziquantel were: (1) Dominant lethal test on male NMRI mice, 12 mating periods of 4 days each, 1 X 1200 mg/kg BW by mouth; (2) Dominant lethal test on female NMRI mice, treatment during pre-estrus, 1 X 1200 mg/kg BW by mouth; (3) Micronucleus test on male and female NMRI mice, two doses with a 24-h interval and preparation of the femoral marrow 6 h after the second dose, 2 X 300 mg/kg and 2 X 600 mg/kg BW by mouth; (4) Spermatogonial test on the Chinese hamster, two doses with a 24-h interval and preparation of the spermatogonia 48 h after the second dose, 2 X 600 mg/kg BW by mouth. The 1200 mg/kg BW dose corresponded to approximately 1/2 of the LD50 after oral application in the mouse and about 40 times the therapeutic dose (1 X 30 mg/kg BW). The cyclophosphamide doses in the test systems were 1 X 200 mg/kg or 2 X 200 mg/kg BW by mouth. No indication was found of any mutagenic potency of Praziquantel. This agrees with the results of point-mutation tests done by other authors.

Animals↗