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PubMed2006

In vivo anthelmintic activity of Butea monosperma against Trichostrongylid nematodes in sheep.

Seeds of Butea monosperma administered as crude powder (CP) at doses of 1, 2 and 3 g/kg to sheep naturally infected with mixed species of gastrointestinal nematodes exhibited a dose and a time-dependent anthelmintic effect. The maximum reduction of 78.4% in eggs per gram of feces (EPG) was recorded on day 10 after treatment with 3 g/kg. Levamisole (7.5 mg/kg), a standard anthelmintic agent, exhibited 99.1% reduction in EPG.

Animals↗
PubMed2003

Quantitative chromatographic determination of several benzimidazole anthelmintic molecules in parasite material.

A specific, precise and accurate high-performance liquid chromatographic (HPLC) analytical method has been developed for the quantitative determination of different benzimidazole (BZD) anthelmintics in parasite material (Moniezia benedeni). Mebendazole (MBZ), oxibendazole (OBZ), flubendazole (FLBZ), albendazole (ABZ) ricobendazole (RBZ), albendazole sulphone (ABZSO(2)), fenbendazole (FBZ), oxfendazole (OFZ) and fenbendazole sulphone (FBZSO(2)) were measured simultaneously in M. benedeni, a sheep and cattle cestode parasite used as a model of the biological matrix. The recovery, linearity, precision, accuracy, limits of detection and quantification of the method were determined. Drug extraction from the parasite's tissue homogenate was performed using methanol (liquid phase extraction), and after solvent evaporation, the residual material was cleaned up by solid phase extraction prior to analysis by reversed-phase HPLC. The resolution of all the BZD molecules assayed was obtained on a C(18) reversed-phase (5 microm, 250 mm x 4.6 mm) column using acetonitrile and ammonium acetate as the mobile phase and ultraviolet (UV) detection at 292 nm. Regression analyses for all the BZD compounds assayed were linear at concentrations ranging from 1.61 to 64.21 nmol/100mg protein (triplicate determinations) showing correlation coefficients greater than 0.9922. The developed method is efficient for the simultaneous determination of several benzimidazole anthelmintic molecules in parasite material and useful for the ex vivo and in vivo characterisation of the kinetics of drug uptake/diffusion in target parasites, which seems to be relevant to optimise parasite control both in human and veterinary medicine.

Animals↗
PubMed2006

In vitro and in vivo anthelmintic activity of crude extracts of Coriandrum sativum against Haemonchus contortus.

In vitro anthelmintic activities of crude aqueous and hydro-alcoholic extracts of the seeds of Coriandrum sativum (Apiaceae) were investigated on the egg and adult nematode parasite Haemonchus contortus. The aqueous extract of Coriandrum sativum was also investigated for in vivo anthelmintic activity in sheep infected with Haemonchus contortus. Both extract types of Coriandrum sativum inhibited hatching of eggs completely at a concentration less than 0.5 mg/ml. ED(50) of aqueous extract of Coriandrum sativum was 0.12 mg/ml while that of hydro-alcoholic extract was 0.18 mg/ml. There was no statistically significant difference between aqueous and hydro-alcoholic extracts (p>0.05). The hydro-alcoholic extract showed better in vitro activity against adult parasites than the aqueous one. For the in vivo study, 24 sheep artificially infected with Haemonchus contortus were randomly divided into four groups of six animals each. The first two groups were treated with crude aqueous extract of Coriandrum sativum at 0.45 and 0.9 g/kg dose levels, the third group with albendazole at 3.8 mg/kg and the last group was left untreated. Efficacy was tested by faecal egg count reduction (FECR) and total worm count reduction (TWCR). On day 2 post treatment, significant FECR was detected in groups treated with higher dose of Coriandrum sativum (p<0.05) and albendazole (p<0.001). On days 7 and 14 post treatment, significant FECR was not detected for both doses of Coriandrum sativum (p>0.05). Significant (p<0.05) TWCR was detected only for higher dose of Coriandrum sativum compared to the untreated group. Reduction in male worms was higher than female worms. Treatment with both doses of Coriandrum sativum did not help the animals improve or maintain their PCV while those treated with albendazole showed significant increase in PCV (p<0.05).

Albendazole↗
PubMed2004

A meta-analysis of the milk-production response after anthelmintic treatment in naturally infected adult dairy cows.

Meta-analysis was used to estimate the effects of anthelmintic treatment on milk production in dairy cows. The literature search included peer-reviewed journals (both full articles and abstracts), conference proceedings and theses and included documents written in English, Spanish, French, Portuguese or Italian. The study outcome was defined as the difference in milk production (kg/cow per day) between treated and untreated cows. Random effect meta-analyses were performed on 75 trials published between 1972 and 2002. The combined estimate after controlling for publication bias and/or small-study effect was of 0.35 kg/cow per day. Significant variation among studies was detected and although several variables were associated with the study outcome, they did not significantly reduce the unexplained variability among trials. Trials reporting the use of endectocides had higher milk-production response compared with trials using older anthelmintics. Similarly, whole-herd treatment trials or trials which applied the treatment in mid-lactation or strategically throughout the year had higher response compared with calving or dry-period treatment trials. Trials reporting the results as total 305-day milk production had lower response compared with trials which measured production as daily milk weight. Primiparous cows trials had lower responses compared with multiparous cows trials.

Animals↗
PubMed2004

Veterinary anthelmintics: old and new.

Between 1960 and 1980, extraordinary success was achieved in anthelmintic development for animals. In these 20 years, drugs with diverse structure, novel activity and enviable safety were produced for a global livestock industry leading to the productivity gains needed to support a human population that grew by 1.5 billion during the same period. The following 20 years have been spent refining existing molecules with niche activity (parasite and host specificity), improving delivery systems and worrying about the inexorable spread of drug resistance. The challenge for the next 20 years will be to use the technologies available to design and produce new drugs and biological controls. Then, to use the lessons of the past to ensure that the new drugs enjoy a longer useful lifespan and contribute to an animal health industry (livestock and companion) which enriches the lives of a global population. Old and new veterinary anthelmintics comprise a very large field, which could not be comprehensively reviewed in a short article. The present mini-review focuses on major chemical discoveries, formulation developments, administration strategies and new products.

Adaptation, Physiological↗
PubMed2005

Anthelmintic resistance--looking to the future: a UK perspective.

The full extent of anthelmintic resistance in nematodes of farm animals is not known. Resistance can be detected with a faecal egg count reduction test and two in vitro tests, the egg hatch and larval development tests. The sensitivity of these two in vitro tests can be increased by using discriminating doses rather than calculating LD50 values. Only benzimidazole resistance can be detected with PCR based tests because the molecular mechanisms of resistance to levamisole and the macrocyclic lactones remain unknown. Resistance detection is important because it enables the appropriate management strategies to be put in place. The development of resistance is delayed by keeping sufficient parasites in refugia (not exposed to anthelmintic), but the necessary management details have not yet been validated in the field. It is probably too late to use combination products to delay the development of resistance, except in cattle but quarantining animals to prevent introduction of resistant helminths onto a farm is important. Dilution of resistant worms with susceptible ones is only at the preliminary research stage and the application of non-chemical methods of control to delay resistance is not yet a practical option. Extensive research is required to manage resistance, especially in the control of resistance in Fasciola hepatica.

Animals↗
PubMed2005

Modulation of porcine biotransformation enzymes by anthelmintic therapy with fenbendazole and flubendazole.

Fenbendazole (FEN) and flubendazole (FLU) are benzimidazole anthelmintics often used in pig management for the control of nematodoses. The in vivo study presented here was designed to test the influence of FLU and FEN on cytochrome P4501A and other cytochrome P450 (CYP) isoforms, UDP-glucuronosyl transferase and several carbonyl reducing enzymes. The results indicated that FEN (in a single therapeutic dose as well as in repeated therapeutic doses) caused significant induction of pig CYP1A, while FLU did not show an inductive effect towards this isoform. Some of the other hepatic and intestinal biotransformation enzymes that were assayed were moderately influenced by FEN or FLU. Strong CYP1A induction following FEN therapy in pigs may negatively affect the efficacy and pharmacokinetics of FEN itself or other simultaneously or consecutively administered drugs. From the perspective of biotransformation enzyme modulation, FLU would appear to be a more convenient anthelmintic therapy of pigs than FEN.

Alcohol Oxidoreductases↗
PubMed2005

In vitro anthelmintic, antibacterial and cytotoxic effects of extracts from plants used in South African ethnoveterinary medicine.

Many plants are used for ethnoveterinary purposes in South Africa, particularly in rural areas. Extracts of 17 plant species employed to treat infectious diseases were prepared using three solvents and the antibacterial activity of the extracts was determined against two Gram-positive and two Gram-negative bacteria. Anthelmintic activity was evaluated against the free-living nematode Caenorhabditis elegans and toxicity was determined using the brine shrimp larval mortality test. Most of the plant extracts demonstrated antibacterial activity, with the best minimum inhibitory concentration (MIC) being 0.1 mg mL(-1). More than a third of the extracts displayed anthelmintic activity. Toxic effects against brine shrimp larvae were shown by 30% of extracts, with the lowest LC(50) recorded as 0.6 mg mL(-1). The promising biological activity displayed by a number of plant extracts supports the ethnoveterinary use of these plants but in vivo tests are required to ascertain fully their medicinal properties and potential toxicity.

Animals↗
PubMed2006

Climatic influences on development and survival of free-living stages of equine strongyles: implications for worm control strategies and managing anthelmintic resistance.

Development of resistance to anthelmintic drugs by horse strongyles constitutes a growing threat to equine health because it is unknown when new drug classes can be expected on the market. Consequently, parasite control strategies should attempt to maintain drug efficacy for as long as possible. The proportion of a parasite population that is not exposed to anthelmintic treatment is described as being "in refugia" and although many factors affect the rate at which resistance develops, levels of refugia are considered the most important as these parasites are not selected by treatment and so provide a pool of sensitive genes in the population. Accordingly, treatment should be avoided when pasture refugia are small because such treatments will place significant selection pressure for resistance on worm populations. Given this new paradigm for parasite control, it has become important to identify seasons and circumstances wherein refugia are diminished. Free-living stages of equine strongyles are highly dependent on climatic influences, and this review summarises studies of strongyle development and survival under laboratory and field conditions in Northern (cool) temperate, Southern (warm) temperate and subtropical/tropical climates. In Northern temperate climates, refugia are smallest during the winter. In contrast, refugia are lowest during the summer in warm temperate and subtropical/tropical climates. Although adverse seasonal changes clearly have significant effects on the ability of free living stages of strongyle nematode parasites to survive and develop, available data suggest that climatic influences cannot effectively "clean" pastures from one grazing season to the next.

Animals↗
PubMed2004

Efficacy of benzimidazole anthelmintics in goats and sheep in the Philippines using a larval development assay.

The negative effects of nematodes in small ruminants can be reduced by use of dewormers but their effectiveness is increasingly limited by the emergence of anthelmintic resistance. The efficacy of benzimidazole (BZ) anthelmintics in the Philippines was estimated by an in vitro larval development assay using worm eggs recovered from faeces collected from goats and sheep. Two hundred and eighteen farms were selected to represent areas of the country with high goat and sheep populations and the full range of farm sizes, from smallholders with just a few animals to commercial and institutional farms with several hundred. Initial surveys of worm control advisers indicated that BZs have been in continuous widespread use for up to 20 years with little use of other chemical groups. A larval development assay (LDA: DrenchRite) was modified for use with BZs alone to allow up to five samples to be analysed on a single microtitre plate. The assay was validated by comparison with the faecal egg count reduction test (FECRT). The dominant nematode genera were Haemonchus and Trichostrongylus with small numbers of Oesophagostomum. The range of BZ efficacy estimated from the LDA results was 0-100% and the distribution of efficacy levels was continuous, with mean efficacy of 82 and 64% for goats and sheep, respectively. There were significant associations between efficacy and parameters measured to characterize the sampled farms: size of animal management group, FEC of sample, recent importation of stock and no access to common grazing were all correlated with decreased efficacy. Likewise, low efficacy was associated with reported frequency and number of years that BZ drenches had been used. The LDA was found to be highly suited to estimate efficacy in nematode populations from small farms where performance of a FECRT for even one chemical would be impractical. Using a larval development assay, we have demonstrated a wide efficacy range for BZs against nematodes from all sizes of goat and sheep farms in the tropics.

Animal Husbandry↗
PubMedDate not supplied

Novel sources of anthelmintics.

The G-series of naturally occurring compounds from Eucalyptus species contain representatives that are endoperoxides and Mannich bases. Mannich bases have been shown to be effective in killing protozoa in vitro. Previous studies of the role of cells of the immune system reveal that helminth parasites are susceptible to free radical attack. A 3-year research project studied the anthelmintic potential of endoperoxides and/or Mannich bases derived from G-compounds. Results from 1 series of synthetic analogues which show a positive relationship between chemical structure and anthelmintic activity are reported here. A G-Mannich base with an aromatic ring side chain as well as a long aliphatic side chain was the most active analogue in the series with an LD 50 < 0.1 mM in an in vitro larval motility assay. This work showed that Mannich bases are a potential source of compounds for parasite control. More work on formulation and pharmacokinetics is required to advance these compounds to the threshold of commercial production.

Animals↗
PubMedDate not supplied

Management of anthelmintic resistance: inheritance of resistance and selection with persistent drugs.

Resistance to the benzimidazole (BZ) anthelmintics is inherited as an incomplete dominant/ incomplete recessive trait and is now widespread in populations of gastrointestinal nematode parasites of sheep. Unlike benzimidazole resistance, which is common in Haemonchus contortus, Trichostrongylus colubriformis and Ostertagia circumcincta, resistance to levamisole is relatively rare in H. contortus, although common in the other 2 species. One explanation for the slow spread of resistance to levamisole in H. contortus is that it is inherited as an autosomal recessive trait, while in T. colubriformis levamisole resistance is inherited as a recessive sex-linked trait. With the introduction of the avermectin/milbemycin class resistance has developed to the relatively short-acting ivermectin, but this time it is inherited as a completely dominant trait. The potentially more serious situation of a persistent anthelmintic selecting a dominant resistance gene was investigated using a simulation model. Efficacy against incoming infective larvae (L3) was assumed to decline or remain high over the period of drug persistence (3 days to 4 weeks), thus allowing the estimation of the relative importance of selecting resistant L3s on the development of resistance in the worm population. These factors were also examined against a background of initial efficacy levels, against adults, and mode of inheritance. Persistence and initial efficacy were found to be far more important in determining the rate of selection for resistance than was selection of resistant L3 as drug efficacy declined.

Animals↗
PubMed2002

Development and validation of a liquid chromatographic-electrospray tandem mass spectrometric multiresidue method for anthelmintics in milk.

A liquid chromatographic-tandem mass spectrometric multiresidue method for the simultaneous quantitative determination of the tetrahydroimidazole, levamisole and the benzimidazoles thiabendazole, oxfendazole, oxibendazole, albendazole, fenbendazole, febantel and triclabendazole in milk has been developed and validated. The anthelmintic residues were extracted with ethyl acetate. The liquid chromatographic separation was performed on a reversed-phase C18 column with gradient elution. The analytes were detected by tandem quadrupole mass spectrometry after positive electrospray ionisation by multiple reaction monitoring. The confirmatory method is very sensitive and each component can be detected at a residue level lower than 1 microgram/l. The method is validated according to the revised European Union requirements and all parameters were found conform the criteria. The evaluated parameters were linearity, specificity, stability, recovery, precision (repeatability and within-laboratory reproducibility) and analytical limits (detection limit, decision limit and detection capability). This analytical method is applied in the Belgian monitoring programme for classical anthelmintic veterinary drugs in raw farm cow's milk.

Animals↗
PubMed2001

The anthelmintic pyrantel acts as a low efficacious agonist and an open-channel blocker of mammalian acetylcholine receptors.

Pyrantel is an anthelmintic which acts as an agonist of nicotinic receptors (AChRs) of nematodes and exerts its therapeutic effects by depolarizing their muscle membranes. Here we explore at the single-channel level the action of pyrantel at mammalian muscle AChR. AChR currents are elicited by pyrantel. However, openings do not appear in clearly identifiable clusters over a range of pyrantel concentrations (1-300 microM). The mean open time decreases as a function of concentration, indicating an additional open-channel block. Single-channel recordings in the presence of high ACh concentrations and pyrantel demonstrate that the anthelmintic acts as a high-affinity open-channel blocker. When analyzed in terms of a sequential blocking scheme, the calculated forward rate constant for the blocking process is 8x10(7) M(-1) x s(-1), the apparent dissociation constant is 8 microM at a membrane potential of -70 mV and the process is voltage dependent. Pyrantel displaces alpha-bungarotoxin binding but the concentration dependence of equilibrium binding is shifted towards higher concentrations with respect to that of ACh binding. Thus, by acting at the binding site pyrantel activates mammalian AChRs with low efficacy, and by sterical blockade of the pore, the activated channels are then rapidly inhibited.

Acetylcholine↗
PubMed1984

CNS, anthelmintic and antiinflammatory activities of some 1-[2/3-(2-phenyl benzimidazole)]2-methyl/phenyl-4-(3,4-disubstituted benzylidene)5-oxo-imidazoles.

Twelve title compounds were synthesised by condensing 2-(2/3 amino phenyl)benzimidazoles with appropriate 2-methyl/phenyl 4(3,4-disubstituted benzylidene)oxazolin 5-ones in dry pyridine and screened for toxicity gross CNS, anthelmintic and anti-inflammatory activities. In their lethal test, all the compounds were found to be non-toxic, and CNS depressants and hypothermic in their neuropharmacological testings. They showed valuable results against N. brasiliensis, whereas, were inactive against H. nana in their in vivo anthelmintic screening. Most of them showed remarkable anti-inflammatory activity against carrageenin induced oedema.

Animals↗
PubMed2001

Comparative efficacy, persistent effect, and treatment intervals of anthelmintic pastes in naturally infected horses.

Eighty horses were involved in a comparative, controlled, and randomised field study conducted in Australia and Brazil. This study was undertaken to address the duration of efficacy (by faecal egg count reduction) of four anthelmintic pastes and to measure the time required between treatments on horses naturally infected by gastrointestinal nematodes. The treatment interval was based on the egg reappearance period (ERP), defined as "the period after treatment when horses have reached a positive egg count equal or superior to 200 eggs per gram (epg) of faeces". Horses were ranked according to pre-treatment faecal egg counts and randomly allocated on Day 0 to one of the four treatment groups (n=16). Group A received a combination of ivermectin at 200 microg/kg and praziquantel at 1.5mg/kg, Group B received an ivermectin paste at 200 microg/kg, Group C received a reference product containing ivermectin at 200 microg/kg, Group D received a moxidectin paste at 400 microg/kg, and Group E received a placebo. Horses were individually faecal sampled at weekly interval from Days 0 to 70 after treatment and coprocultures were made on pooled samples at the pre-treatment time on D-7 in Brazil and D-6 in Australia. The nematode population was mainly composed of small strongyles (Cyathostominae, Gyalocephalus spp., Triodontophorus spp.). All products were efficient (>90% efficacy) until Day 42 with no statistical difference between groups. From Day 49 onwards, Group C reached the threshold, while Group B exceeded this threshold on Day 56. Groups A and D remained below 200 epg for the entire study period (70 days). The interval between two anthelmintic treatments can vary according to the threshold. The ERP was defined as the period after treatment while the output of eggs is negligible or considered as acceptable. The mean number of days calculated to recurrence of 200 epg and more was, respectively, 60 days for product A, 56 days for products B and C, and 64 days for product D. If treatments are combined with other methods of limiting exposure to infective larvae on pasture, the number of treatments required will be reduced even further.

Animals↗
PubMed2002

Evaluation of tests for anthelmintic resistance in cyathostomes.

Resistance, especially to the anthelmintic benzimidazoles (BZ), has been reported in horse cyathostomes world-wide. Diagnosis of resistance has traditionally been made by faecal egg count reduction (FECR) trials, however, this technique has limitations. Some of the shortcomings may be resolved by refining the test or by using an in vitro test. FECR tests and the larval development assay (LDA) were performed on adult horses held on 15 different horse properties across a wide geographical area of NSW, Australia. FECR were measured before and 10-14 after days treatment with oxibendazole (OBZ), morantel (MOR) or ivermectin (IVM) at recommended dose rates. Eight properties were rejected following low pre-treatment egg counts, leaving seven in the study. On these, the majority of larvae recovered from faecal cultures were cyathostomes. Using a definition of resistance as a FECR of <90%, resistance to OBZ was present on six properties and to MOR on two properties. Resistance to IVM was not detected. An alternative method of calculating FECR based on individual horse egg counts pre- and post-treatment was developed and results from the same properties compared with the results of the LDA. For example, for the BZ, correlation coefficients of values of lethal concentration to kill 50% of population (LC50) on LDA and FECR percentages were -0.536 before and -0.704 after OBZ treatment. We conclude that the LDA has the potential to be a single visit test for detection of anthelmintic resistance in horse cyathostomes but requires further investigation and standardisation.

Animals↗
PubMed1996

A survey of anthelmintic resistance in nematode parasites of goats in Denmark.

The occurrence of anthelmintic resistance in 15 goat herds in Denmark was investigated using the faecal egg count reduction test (FECRT), egg hatch assay (EHA) for thiabendazole (TBZ) and a microlarval development assay (LDA) for TBZ, levamisole (LEV) and ivermectin (IVM). Resistance to both benzimidazole (BZ) and levamisole (LEV) anthelmintics was detected on six farms, and to both BZs and IVM on one farm. Resistance to BZs was also detected on two farms and to LEV on two farms. Ivermectin resistance was present on one farm. Trichostrongylus and Ostertagia spp. were the predominant nematode species in both pre-treatment and post-treatment faecal cultures. In all nine instances where BZ resistance was detected in the FECRT, the LD50 values for TBZ in the EHA were higher than 0.5 microM TBZ (0.1 microgram TBZ/ml), indicating resistance. LD50 values for TBZ in the LDA were also higher than 0.5 microM where resistance to BZs was detected in the FECRT, except two farms where LD50 values of 0.21 and 0.29 microM TBZ were recorded. LD50 values in the LDA for isolates declared resistant to LEV ranged from 0.78 to 5.62 microM LEV. For IVM, the two resistant isolates had LD50 values of 25 and 68 nM IVM. There were disagreements in the declaration of resistance between methods of calculating faecal egg count reduction percentage (FECR%) based on the arithmetic mean and those where geometric mean EPG is used. Similarly, inclusion of pre-treatment EPG or control group EPG in the calculation of FECR% influenced declaration of resistance.

Animal Husbandry↗