LongRange™ (eprinomectin 5%) extended-release injection parasiticide and the utility of extended-activity antiparasitics in cattle

Forbes, Andrew Benjamin

doi:10.1016/j.vetpar.2012.11.036

Cited by 19 publications

(20 citation statements)

References 42 publications

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“…In the context where EPR is widely used in lactating animals and in a longacting formulation (52) and is suggested to be an alternative to IVM for malaria parasite transmission control (53), these results have several important implications. Indeed, EPR efficacy may be limited in ML-resistant nematodes and could not be used as an alternative to IVM or MOX when IVM or MOX resistance occurs.…”

Section: Discussionmentioning

confidence: 99%

Acquired Tolerance to Ivermectin and Moxidectin after Drug Selection Pressure in the Nematode Caenorhabditis elegans

Ménez

Alberich

Kansoh

et al. 2016

Antimicrob Agents Chemother

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cIvermectin and moxidectin are the most widely administered anthelmintic macrocyclic lactones (MLs) to treat human and animal nematode infections. Their widespread and frequent use has led to a high level of resistance to these drugs. Although they have the same mode of action, differences in terms of selection for drug resistance have been reported. Our objective was to study and compare changes occurring upon ivermectin or moxidectin selection in the model nematode Caenorhabditis elegans. C. elegans worms were submitted to stepwise exposure to increasing doses of moxidectin. The sensitivity of moxidectin-selected worms to MLs was determined in a larval development assay and compared with those of wild-type and ivermectin-selected strains. Selection with either ivermectin or moxidectin led to acquired tolerance to ivermectin, moxidectin, and eprinomectin. Importantly, moxidectin was the most potent ML in both ivermectin-and moxidectin-selected strains. Interestingly, this order of potency was also observed in a resistant Haemonchus contortus isolate. In addition, ivermectin-and moxidectin-selected strains displayed constitutive overexpression of several genes involved in xenobiotic metabolism and transport. Moreover, verapamil potentiated sensitivity to ivermectin and moxidectin, demonstrating that ABC transporters play a role in ML sensitivity in ML-selected C. elegans strains. Finally, both ivermectin-and moxidectin-selected strains displayed a dye-filling-defective phenotype. Overall, this work demonstrated that selection with ivermectin or moxidectin led to cross-resistance to several MLs in nematodes and that the induction of detoxification systems and defects in the integrity of amphidial neurons are two mechanisms that appear to affect the responsiveness of worms to both ivermectin and moxidectin.T he broad-spectrum anthelmintic macrocyclic lactones (MLs) are most commonly used in veterinary medicine to treat diseases caused by gastrointestinal nematodes and external parasites in livestock (1, 2). Ivermectin (IVM) was the first ML approved for use in animals and remains today the sole ML registered for use in humans, mainly to treat onchocerciasis through mass chemotherapy. Another ML, moxidectin (MOX), was subsequently commercialized for the veterinary market and is currently being evaluated for possible use against human onchocerciasis (3). Inevitably, the intensive use of these compounds has led to the emergence of resistance in small ruminant, cattle, and some human nematode parasites (4-7). Discovering the mechanisms by which resistance to MLs occurs remains an important challenge today.There is consistent evidence that ATP-binding-cassette (ABC) transporters such as P-glycoproteins (Pgps) play an important role in multidrug resistance (MDR) in many organisms, including several nematode species. Gene expression levels of ABC transporters or allele frequencies were modified after ML selection (8-13), and they are involved in the tolerance of Caenorhabditis elegans (9, 14-16) and parasitic nematodes s...

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Section: Discussionmentioning

confidence: 99%

Acquired Tolerance to Ivermectin and Moxidectin after Drug Selection Pressure in the Nematode Caenorhabditis elegans

Ménez

Alberich

Kansoh

et al. 2016

Antimicrob Agents Chemother

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“…Both repeated use of shortacting anthelmintics and products providing prolonged control of parasites were demonstrated to be suitable measures in the management of parasites of grazing cattle (e.g., Shaw et al 1998;Stromberg and Gasbarre 2006;Sutherland and Scott 2010). In the cattle industry, long-acting products are widely accepted not only because they treat existing parasitic nematode infections and prevent new ones but also because of the substantial lower resources needed to treat the animals due to reduced frequency of administrations and associated livestock handling and restraint (labor and equipment) (Forbes 2013).…”

Section: Introductionmentioning

confidence: 99%

Activity of ivermectin long-acting injectable (IVOMEC® GOLD) in first-season grazing cattle exposed to natural challenge conditions in Germany

Rehbein¹,

Knaus²,

Visser³

et al. 2014

Parasitol Res

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The persistent activity of ivermectin long-acting injection (IVM LAI; IVOMEC® GOLD, Merial; 3.15% ivermectin w/v) against nematode infections of cattle was evaluated under natural challenge conditions. Seventy nematode-free Brown Swiss calves were blocked by pre-treatment bodyweight and allocated randomly to seven groups of 10 animals each: saline (control) at 1 mL/50 kg bodyweight once on day 0 or IVM LAI at 1 mL/50 kg bodyweight (630 mcg IVM/kg) on either days 0, 7, 14, 21, 28, or 35. After housing until day 35, calves were grazed as one herd on a naturally contaminated pasture for 42 days. Calves were then weighed and housed for 4 weeks before being necropsied for parasite counting. Treatment with IVM LAI prevented the establishment (>90%, p < 0.05) of Dictyocaulus viviparus (100%), Bunostomum phlebotomum (100 %), Haemonchus contortus (98.6%), Ostertagia ostertagi/lyrata (94.9%), and Oesophagostomum radiatum (93.3%) for at least 77 days; Ostertagia leptospicularis (99.1%) for 63 days; Cooperia punctata (97.7%), Trichostrongylus axei (96.5%), and Ostertagia spp. inhibited larvae 4 (93.3%) for 56 days; Cooperia oncophora/surnabada (96.9%), Trichuris discolor (93.6%), and Cooperia spp. inhibited larvae 4 (98.8%); and Nematodirus spp. inhibited larvae 4 (97.1%) for 42 days. Calves of groups treated with IVM LAI had significantly (p < 0.001) higher days 0 to 77 weight gains than the saline-treated controls (28.40-39.25 vs 2.60 kg); the weight gains of the IVM LAI-treated groups, however, were not different from one another (p > 0.3). This study demonstrated a very high efficacy of IVOMEC® GOLD in preventing the establishment of a wide range of bovine nematodes for extended periods of time which was associated with a significant benefit to productivity in terms of weight gain.

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“…bovis. (Forbes, ). Since the efficacy of subcutaneously administered EPM against R. microplus has not yet been reported, the results of the present experiment could not be compared with other data.…”

Section: Discussionmentioning

confidence: 99%

Injectable eprinomectin for cattle: Tick efficacy and pharmacokinetics

Nascimento

Bragaglia

Toma

et al. 2020

Vet Pharm & Therapeutics

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The aims of the present study were to evaluate the pharmacokinetic profile and efficacy of eprinomectin (EPM) against Rhipicephalus microplus in cattle of a new injectable form of EPM (Voss Performa®). The product was administered subcutaneously at a dose of 200 μg EPM/kg, in a single dose. The efficacy of EPM against R. microplus in cattle was evaluated through field and stall tests. Studies were performed to estimate the pharmacokinetic parameters of EPM with the purpose of better understanding the kinetics of the formulation. The formulation was effective in controlling R. microplus in both naturally and artificially infested cattle, providing efficacy greater than 95%. The results of pharmacokinetic study were Cmax of 47.15 ± 22.20 ng/ml, Tmax of 1.33 ± 0.492 days, T1/2 of 2.96 ± 1.212 days, AUC0–t of 228.08 ± 57.30 ng day ml−1, and AUC0‐∞ of 240.50 ± 58.44 ng day ml−1. Therefore, the new injectable EPM formulation becomes an important alternative for the control of cattle tick in Brazil.

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LongRange™ (eprinomectin 5%) extended-release injection parasiticide and the utility of extended-activity antiparasitics in cattle

Cited by 19 publications

References 42 publications

Acquired Tolerance to Ivermectin and Moxidectin after Drug Selection Pressure in the Nematode Caenorhabditis elegans

Acquired Tolerance to Ivermectin and Moxidectin after Drug Selection Pressure in the Nematode Caenorhabditis elegans

Activity of ivermectin long-acting injectable (IVOMEC® GOLD) in first-season grazing cattle exposed to natural challenge conditions in Germany

Injectable eprinomectin for cattle: Tick efficacy and pharmacokinetics

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