Comparative plasma disposition of fenbendazole, oxfendazole and albendazole in dogs

Gökbulut, Cengiz; Bilgili, Ali; Hanedan, Başak; McKellar, Quintin

doi:10.1016/j.vetpar.2007.06.028

Cited by 42 publications

(40 citation statements)

References 30 publications

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“…In our case, two alternative explanations can be reliable: first it is possible that (−) SOABZ is depleted faster from the nematode than their respective (+) antipode by means of an enantioselective excretion as occurred in the plasma of domestic animals (Cristofol et al 2000(Cristofol et al , 2001Goudah 2003;Gokbulut et al 2007). Thus, as pointed out by Alvarez et al (2000), if following uptake, the accumulation of SOABZ enantiomers within the parasite is a nonenantioselective process, only depending on the passive diffusion of both molecules (Capece et al 2009), a major contribution to the antiparasitic effect of (+) enantiomer may be expected since its (−) antipode is rapidly eliminated from the parasite body.…”

Section: Discussionmentioning

confidence: 74%

“…1), two SOABZ enantiomers have been identified in the plasma of several species including cattle, sheep, goats, dogs, rats, mice, horse and human after the administration of the pro-chiral ABZ (Benoit et al 1992;Delatour et al 1990b;1991a;García et al 1999;Gokbulut et al 2007;McKellar et al 2002). The pharmacokinetic behaviour of SOABZ enantiomers have been studied in several species including sheep, rats, dogs, human and mice (Delatour et al 1991a, b;García et al 1999;.…”

Section: Introductionmentioning

confidence: 99%

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Enantiomerical pharmacokinetic prevalence of (+) albendazole sulphoxide in Trichinella spiralis muscle larvae

et al. 2011

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In a previous work, it was demonstrated that (+) albendazole sulphoxide (SOABZ) has higher anthelmintic activity than (-) SOABZ (Bolás-Fernández et al. J Parasitol 90:407-409, 2004). In this work, the pharmacokinetics characteristics of SOABZ and its enantiomeric forms were studied in an ex vivo model system for Trichinella spiralis isolated muscle larvae. To this end, samples of either racemic or purified SOABZ enantiomers were added to the incubation medium. Quantification of either albendazole, racemic SOABZ or its enantiomers was performed by validated HPLC methods and the effect of different SOABZ concentrations in relation to time of contact with the larvae was also analysed. Obviously, higher concentration of SOABZ in the medium leads to higher concentrations of SOABZ inside the larvae which increased in an exponential mode, thus indicating a simple diffusion process. At least 18 h of contact with the drug was required to achieve anthelmintic effects. Besides, after this time, the concentration of (+) SOABZ inside the larvae was significantly higher than that of the (-) SOABZ. From these results, it can be concluded that the higher activity found in the previous work is clearly related to the pharmacokinetic prevalence of (+) enantiomer inside the larvae.

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Section: Discussionmentioning

confidence: 74%

Section: Introductionmentioning

confidence: 99%

Enantiomerical pharmacokinetic prevalence of (+) albendazole sulphoxide in Trichinella spiralis muscle larvae

et al. 2011

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“…However, this proposed mechanism requires further investigation. Additionally, compared with almost no uptake of fenbendazole 43 , the higher bioavailability of albendazole provides a plausible explanation for the higher efficacy of albendazole. The bioavailability of albendazole is higher than most benzimidazole derivatives, and the parent compound and the active metabolites undergo biliary excretion and accumulate in the gastrointestinal tube 44 .…”

Section: Anthelmintic Resistance To Benzimidazoles and Closantelmentioning

confidence: 99%

Anthelmintic resistance status of gastrointestinal nematodes of sheep to the single or combined administration of benzimidazoles and closantel in three localities in Mexico

et al. 2016

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Sheep production requires the constant assessment of parasitic burden and the efficacy of existing treatments for proper management. In this study, the administration of five different treatments was evaluated for the reduction of the percentage of eggs per gram of feces (EPG) shed by gastrointestinal nematodes (GIN) from sheep on three different sheep-breeding farms in Mexico (Texcoco, Estado de Mexico; Hueytamalco, Puebla; and Tlaltizapán de Zapata, Morelos). In these farms, ivermectin and benzimidazole derivatives had been routinely administered for two consecutive years. To determine whether drugs with different pharmacological properties decreased GIN fecal egg excretion, the treatments closantel (CLOS), albendazole (ABZ) and fenbendazole (FBZ) were administered alone and in combinations of CLOS + ABZ and CLOS + FBZ, to five groups of sheep, with an additional untreated control group on each farm (n = 28 per flock). Anthelmintic resistance was determined using Fecal Egg Count Reduction Tests (FECRT) as recommended in the guidelines of the World Association for the Advancement of Veterinary Parasitology. Fecal samples were collected 14 and 21 days after treatment. The anthelmintic resistance status was determined based on the reduction in the fecal egg count arithmetic mean and 95 % confidence limits. According to the FECRT, resistance developed to CLOS, ABZ, FBZ and CLOS + FBZ because the mean percentage of EPG reduction was ≤ 95 % with a lower confidence limit of ≤ 90 %. By contrast, nematode susceptibility was confirmed for the CLOS + ABZ combination, as it reduced the percentage of GIN fecal egg output by 96.46 ± 3.04 % (day 14) and 96.88 ± 3.04 % (day 21). Based on the morphometric identification of larvae, Haemonchus spp., Cooperia spp. and Teladorsagia spp. were the most abundant genera on all farms before the administration of these five treatments. In conclusion, the use of the anthelmintic combination of closantel plus albendazole may reduce the development of anthelmintic resistance in gastrointestinal nematodes.

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“…Intestinal parasitoses represent one of the major public health problems, particularly in developing countries, where they have a great economic impact 1 .Benzimidazole (BZD) and its derivatives are widely used in the treatment of intestinal helminths in animals and humans, with a large spectrum of activity and low toxicity 2 .However, this class of drugs have low solubility and as a result, they have variable and incomplete bioavailability [3][4][5] . Different strategies have been employed to increase the solubility of BZD, including the preparation of solid dispersions, the use of surfactants, liposomes and the development of inclusion complexes with cyclodextrins (CDs) 3,[6][7][8][9][10] .…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of the Rp-HPLC Method for Determination of Benzimidazole Carbamates in the Presence of Cyclodextrins

Rodrigues¹,

Reis²,

Katiki³

2017

Int. Res. J. Pharm.

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Liquid chromatography is the universal method to determine drugs in biological matrices and pharmaceutical products. Different strategies have been developed in order to improve the aqueous solubility and bioavailability of benzimidazoles, such as the complexation with cyclodextrins. Although extensive studies on cyclodextrins have been performed, studies on the impact of cyclodextrins on the chromatographic process are scarce. The objective of this study was to develop and validate a suitable HPLC method for the quantification of benzimidazoles carbamates (albendazole and fenbendazole) in the presence of cyclodextrins (β-cyclodextrin and hydroxypropyl-β-cyclodextrin). The retention time of the benzimidazoles and their metabolites decreases in the presence of cyclodextrins. The formation of inclusion complexes between drugs and cyclodextrins can explain the change in retention times. Hydroxypropyl-β-cyclodextrin decreased the retention time of the solute in a more pronounced way than β CD. This phenomenon can be attributed to the greater hydrophilicity of Hydroxypropyl-β-cyclodextrin, which promotes the formation of more soluble complexes and, therefore, with less affinity for the stationary phase.

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Comparative plasma disposition of fenbendazole, oxfendazole and albendazole in dogs

Cited by 42 publications

References 30 publications

Enantiomerical pharmacokinetic prevalence of (+) albendazole sulphoxide in Trichinella spiralis muscle larvae

Enantiomerical pharmacokinetic prevalence of (+) albendazole sulphoxide in Trichinella spiralis muscle larvae

Anthelmintic resistance status of gastrointestinal nematodes of sheep to the single or combined administration of benzimidazoles and closantel in three localities in Mexico

Development and Validation of the Rp-HPLC Method for Determination of Benzimidazole Carbamates in the Presence of Cyclodextrins

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