Plasma and milk kinetics of eprinomectin following topical or oral administration to lactating Chinese Holstein cows

Wen, Huiqiang; Pan, Baoliang; Wang, Yuwan; Wang, Fangfei; Yang, Zhenzhong; Wang, Ming

doi:10.1016/j.vetpar.2010.08.017

Cited by 18 publications

(6 citation statements)

References 23 publications

(30 reference statements)

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“…1 ) despite the pour-on being administered at 2.5 times the dose rate of the oral. However, this is in contrast with other studies comparing oral and pour-on administration of ML products to cattle, which showed significantly higher levels in plasma following oral administration ( Wen et al, 2010 ; Leathwick and Miller, 2013 ; Leathwick et al, 2016 ). A similar pattern has also been shown in other host species ( Gokbulut et al, 2010 ; Mackintosh et al, 2014 ).…”

Section: Discussioncontrasting

confidence: 98%

Route of administration influences the concentration of ivermectin reaching nematode parasites in the gastrointestinal tract of cattle

Leathwick

Miller

Waghorn

et al. 2020

International Journal for Parasitology: Drugs and Drug Resistan

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An animal trial was conducted to measure the concentrations of ivermectin occurring in abomasal and small intestinal contents and mucosa, and in the target parasites ( Ostertagia ostertagi and Cooperia oncophora ) following administration by subcutaneous, oral and pour-on routes. Twenty-five steers were infected with ivermectin-resistant isolates of O . ostertagi and C . oncophora and following patency randomly allocated to 3 treatment groups of 7 and 1 untreated control group of four. On day 0, animals in the treatment groups were administered ivermectin via the oral, injectable or pour-on routes. On days 1, 2, 3, 4, 5, 6 and 8, blood samples were collected from all live animals, one animal from each treatment group was euthanised and the abomasum and small intestine recovered. Control animals were euthanised on each of days 4, 5, 6 and 8. Samples of gastrointestinal tract organs, their contents, mucosa and parasites were collected and assayed for ivermectin concentration using HPLC. The highest plasma concentrations occurred following subcutaneous administration. In the gastrointestinal contents the highest levels occurred following oral administration, although one high value occurred following pour-on administration, which was attributed to self-licking by the treated animal. The lowest GI content levels followed subcutaneous injection. Ivermectin concentrations in the gastrointestinal mucosa were highest following subcutaneous injection. Drug levels in the abomasal parasite O . ostertagi were most closely correlated with levels in the abomasal mucosa whereas levels in the intestinal C . oncophora were most closely correlated with those in the intestinal contents. Thus, the maximun levels of drug reached C . oncophora in the small intestine following oral administration. In contrast, the highest levels of ivermectin in O . ostertagi followed subcutaneous injection. Therefore, route of administration is likely to influence the exposure to ivermectin for different parasite species.

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Section: Discussioncontrasting

confidence: 98%

Route of administration influences the concentration of ivermectin reaching nematode parasites in the gastrointestinal tract of cattle

Leathwick

Miller

Waghorn

et al. 2020

International Journal for Parasitology: Drugs and Drug Resistan

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“…The plasma and milk kinetic behaviors of EPM as a topical formulation have been investigated in dairy cattle [60,79,80], goats [81], and sheep [82,83]. The results about EPM excretion in different species indicate that the milk excretion is not an important route of elimination for EPM unlike other endectocide drugs such as IVM and, particularly, MXD.…”

Section: Macrocyclic Lactonesmentioning

confidence: 99%

“…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%

“…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. The maximum concentration values of EPM in milk after topical and oral treatment [80] were lower than those obtained after sc treatment (0.2 mg/kg) [94]. The milk-to-plasma ratio values obtained from Chinese Holstein after topical (0.124-fold) and oral (0.104-fold) treatment were similar to the value obtained from dairy cattle after topical (0.5 mg/kg) (0.102-fold) treatment [79].…”

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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“…The pharmacokinetics of eprinomectin have been described in several bovine species or breeds, including the Prim Holstein (Alvinerie et al ., ), Chinese Holstein (Wen et al ., ), Braunvieh (Rehbein et al ., ), Indian Zebu cattle (Bengone‐Ndong et al ., ), and water buffaloes (Dupuy et al ., ), it has not been reported in lactating yaks. These reports show that the pharmacokinetics of eprinomectin could be quite different in different bovine species or breeds.…”

Section: Introductionmentioning

confidence: 99%

Plasma kinetics, excretion in milk of eprinomectin, and its efficacy against Hypoderma spp. following topical administration in yaks

Shi

Cai³

et al. 2015

Vet Pharm & Therapeutics

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The plasma pharmacokinetics and mammary excretion of eprinomectin were determined in dairy yaks following topical administration at a dose of 0.5 mg/kg. The kinetics of plasma and milk concentrations were analyzed using a noncompartmental model. Plasma and milk concentrations of eprinomectin increased to reach maximal concentrations of 5.45 ± 2.84 and 2.29 ± 0.90 ng/mL at a Tmax of 1.79 ± 0.57 and 2.00 ± 0.82 days, respectively. The concentration of eprinomectin in plasma was remained >0.5 ng/mL for more than 30 days after administration. The mean residence times of eprinomectin in plasma and milk were 14.73 ± 6.22 and 9.37 ± 2.81 days, respectively. The AUC value in plasma (55.89 ± 18.16 ng day/mL) was threefold greater than that in milk (18.02 ± 6.48 ng day/mL). The AUC milk/plasma ratio was 0.33 ± 0.08. The systemic availability of eprinomectin in yaks was lower than that observed value in other domestic bovines. The low level of eprinomectin excretion in milk suggests that eprinomectin can be used in yaks with zero milk-withdrawal time. The efficacy of eprinomectin against naturally acquired larvae of Hypoderma spp. was also determined in yaks. Topically administrated eprinomectin at a dose of 0.5 mg/kg was 100% efficacious against larvae of Hypoderma bovis, H. lineatum, and H. sinense.

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Plasma and milk kinetics of eprinomectin following topical or oral administration to lactating Chinese Holstein cows

Cited by 18 publications

References 23 publications

Route of administration influences the concentration of ivermectin reaching nematode parasites in the gastrointestinal tract of cattle

Route of administration influences the concentration of ivermectin reaching nematode parasites in the gastrointestinal tract of cattle

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

Plasma kinetics, excretion in milk of eprinomectin, and its efficacy against Hypoderma spp. following topical administration in yaks

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