Kinetics and anthelmintic efficacy of topical eprinomectin when given orally to goats

Badie, C.; Lespine, Anne; Devos, J.; Sutra, J.F.; Chartier, Christophe

doi:10.1016/j.vetpar.2015.02.013

Cited by 13 publications

(7 citation statements)

References 21 publications

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“…Eprinomectin is another member of the avermectin class of anthelmintic compounds, commercially launched in the late 1990s as a novel avermectin. It is marketed as a pour-on formulation for use in cattle 41 . In addition to broad-spectrum activity, it exhibits interesting low elimination in milk and was licensed, in lactating cows only, as a pour-on formulation 42 .…”

Section: Introductionmentioning

confidence: 99%

The effects of some avermectins on bovine carbonic anhydrase enzyme

Köse

Gülçın

Özdemir

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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Avermectins are effective agricultural pesticides and antiparasitic agents that are widely employed in the agricultural, veterinary and medical fields. The aim of this study was to investigate the inhibitory effects of selected avermectins including abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin that are used as drugs against a wide variety of internal and external mammalian parasites, on the carbonic anhydrase enzyme (CA, EC 4.2.1.1.) purified from fresh bovine erythrocyte. CA catalyses the rapid interconversion of carbon dioxide (CO2) and water (H2O) to bicarbonate ([Formula: see text]) and protons (H(+)) and regulate the acidity of the local tissues. Bovine erythrocyte CA (bCA) enzyme was purified by Sepharose-4B affinity chromatography with a yield of 21.96% and 262.7-fold purification. The inhibition results obtained from this study showed Ki values of 9.73, 17.39, 20.43, 13.39, 16.44 and 17.73 nM for abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin, respectively. However, acetazolamide, well-known clinically established CA inhibitor, possessed a Ki value of 27.68 nM.

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Section: Introductionmentioning

confidence: 99%

The effects of some avermectins on bovine carbonic anhydrase enzyme

Köse

Gülçın

Özdemir

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…The elimination pattern of EPM in milk after oral administration was consistent with the plasma levels. The milk-to-plasma ratio values obtained from dairy goats were 0.36 and 0.33-fold after oral administration of EPM at 0.5 or 1.0 mg/kg, respectively [92]. These values were higher than those obtained from dairy goats at the same doses after pour-on treatment [81], and the percentage of total EPM dose excreted in milk was between 0.33% and 0.42% [92].…”

Section: Macrocyclic Lactonesmentioning

confidence: 81%

“…The relationship between the plasma and milk kinetic behaviors of EPM and using EPM as a topical formulation at twice the recommended dose (1.0 mg/kg) has been investigated in dairy goats [81] and dairy sheep [83]. Moreover, the plasma and milk kinetic behaviors of EPM after treatment by non-approved routes (sc and oral treatment) in dairy goats [91,92] and cattle [80,93,94] have been investigated (see Table 1). Some dates reported in dairy cattle (Chinese Holstein) have shown a similar bioavailability of EPM in plasma after pour-on (0.5 mg/kg) or oral (0.2 mg/kg) treatment.…”

Section: Macrocyclic Lactonesmentioning

confidence: 99%

“…It has become known that sc and oral routes of administration lead to higher drug concentrations in plasma and tissues and higher efficacy compared with topical administration [91,97]. Badie et al [92] have reported dates to characterize the EPM kinetics in plasma and milk after oral administration (0.5 or 1.0 mg/kg) of the topical formulation of EPM in lactating or non-lactating goats. A significantly higher systemic bioavailability has been reported for both doses after oral treatment compared with pouron administration [81].…”

Section: Macrocyclic Lactonesmentioning

confidence: 99%

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The Pattern of Blood–Milk Exchange for Antiparasitic Drugs in Dairy Ruminants

Imperiale

Lanusse

2021

Animals

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The prolonged persistence of milk residual concentration of different antiparasitic drugs in lactating dairy animals should be considered before recommending their use (label or extra-label) for parasite control in dairy animals. The partition blood-to-milk ratio for different antiparasitic compounds depends on their ability to diffuse across the mammary gland epithelium. The high lipophilicity of some of the most widely used antiparasitic drugs explains their high partition into milk and the extended persistence of high residual concentrations in milk after treatment. Most of the antiparasitic drug compounds studied were shown to be stable in various milk-related industrial processes. Thus, the levels of residues detected in raw milk can be directly applicable to estimating consumer exposure and dietary intake calculations when consuming heat-processed fluid milk. However, after milk is processed to obtain milk products such as cheese, yogurt, ricotta, and butter, the residues of lipophilic antiparasitic drugs are higher than those measured in the milk used for their elaboration. This review article contributes pharmacokinetics-based information, which is useful to understand the relevance of rational drug-based parasite control in lactating dairy ruminants to avoid undesirable consequences of residual drug concentrations in milk and derived products intended for human consumption.

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“…In cattle, rainfall, according to the SPC of the product, does not affect the absorbance of the drug when administered topically, but in sheep there is no relative data available ( Eprinex, UK SPC, 2018 ). In order to overcome the possible limitations from pour-on administration in sheep, the oral administration of eprinomectin has been investigated and found to be highly effective as well ( Badie et al, 2015 ). However, to the best of our knowledge, meat and milk residual analyses after the oral administration of eprinomectin in sheep are scarce.…”

Section: Discussionmentioning

confidence: 99%