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Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep
SIMPLE SUMMARY: Anthelmintic drugs are among those most widely used in veterinary practice. The development of resistance to these drugs is a widespread problem, especially in small ruminants, and represents a serious threat to animal production. Thus, new possibilities to use the available pharmaco...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8868263/ https://www.ncbi.nlm.nih.gov/pubmed/35203171 http://dx.doi.org/10.3390/ani12040463 |
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author | Diez, Raquel Diez, M. Jose Garcia, Juan J. Rodríguez, Jose M. Lopez, Cristina Fernandez, Nelida Sierra, Matilde Sahagun, Ana M. |
author_facet | Diez, Raquel Diez, M. Jose Garcia, Juan J. Rodríguez, Jose M. Lopez, Cristina Fernandez, Nelida Sierra, Matilde Sahagun, Ana M. |
author_sort | Diez, Raquel |
collection | PubMed |
description | SIMPLE SUMMARY: Anthelmintic drugs are among those most widely used in veterinary practice. The development of resistance to these drugs is a widespread problem, especially in small ruminants, and represents a serious threat to animal production. Thus, new possibilities to use the available pharmacological groups in a more efficient way should be explored. The objective of this study was to assess the pharmacokinetic interaction between a benzimidazole (albendazole, ABZ) and a choleretic drug (menbutone, MEN) in sheep, and it may result in greater effectivity of this drug against nematode parasites. Plasma concentrations of ABZSO (ABZ active metabolite) were higher when ABZ was administered with MEN. The proposed interaction is a simple, safe, and inexpensive way of increasing the effectivity of this anthelmintic widely used in livestock. ABSTRACT: The pharmacokinetic interaction between a benzimidazole (albendazole, ABZ) and a choleretic drug (menbutone, MEN) was evaluated in sheep. The plasma disposition of albendazole sulfoxide (ABZSO, active metabolite) and albendazole sulfone (ABZSO(2), inactive metabolite) was investigated following an oral administration of albendazole (ABZ) (5 mg/kg) alone or with menbutone (MEN) (intramuscular, 10 mg/kg). Blood samples were collected over 3 days post-treatment, and drug plasma concentrations were measured by high performance liquid chromatography (HPLC). ABZSO was measured from 0.5 to 48 h, and ABZSO(2) from 2 to 60 h. No parent drug was detected at any sampling time. Mean maximum plasma concentration (C(max)) and the area under the plasma concentration-time curve (AUC) were 12.8% and 21.5% higher for ABZSO when ABZ and MEN were administered together, which indicates a significant increase in the amount absorbed. The rate of absorption was not modified, with similar values for the time to reach C(max) (t(max)) (11.5 h with ABZ + MEN and 10.7 h with ABZ treatment), although no significant differences were observed for these latter pharmacokinetic parameters. Regarding ABZSO(2), C(max), AUC and t(max) values were similar after both treatments (ABZ or ABZ + MEN). The results obtained indicate that co-administration of ABZ and MEN may be an interesting and practical option to increase the efficacy of this anthelmintic. |
format | Online Article Text |
id | pubmed-8868263 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-88682632022-02-25 Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep Diez, Raquel Diez, M. Jose Garcia, Juan J. Rodríguez, Jose M. Lopez, Cristina Fernandez, Nelida Sierra, Matilde Sahagun, Ana M. Animals (Basel) Article SIMPLE SUMMARY: Anthelmintic drugs are among those most widely used in veterinary practice. The development of resistance to these drugs is a widespread problem, especially in small ruminants, and represents a serious threat to animal production. Thus, new possibilities to use the available pharmacological groups in a more efficient way should be explored. The objective of this study was to assess the pharmacokinetic interaction between a benzimidazole (albendazole, ABZ) and a choleretic drug (menbutone, MEN) in sheep, and it may result in greater effectivity of this drug against nematode parasites. Plasma concentrations of ABZSO (ABZ active metabolite) were higher when ABZ was administered with MEN. The proposed interaction is a simple, safe, and inexpensive way of increasing the effectivity of this anthelmintic widely used in livestock. ABSTRACT: The pharmacokinetic interaction between a benzimidazole (albendazole, ABZ) and a choleretic drug (menbutone, MEN) was evaluated in sheep. The plasma disposition of albendazole sulfoxide (ABZSO, active metabolite) and albendazole sulfone (ABZSO(2), inactive metabolite) was investigated following an oral administration of albendazole (ABZ) (5 mg/kg) alone or with menbutone (MEN) (intramuscular, 10 mg/kg). Blood samples were collected over 3 days post-treatment, and drug plasma concentrations were measured by high performance liquid chromatography (HPLC). ABZSO was measured from 0.5 to 48 h, and ABZSO(2) from 2 to 60 h. No parent drug was detected at any sampling time. Mean maximum plasma concentration (C(max)) and the area under the plasma concentration-time curve (AUC) were 12.8% and 21.5% higher for ABZSO when ABZ and MEN were administered together, which indicates a significant increase in the amount absorbed. The rate of absorption was not modified, with similar values for the time to reach C(max) (t(max)) (11.5 h with ABZ + MEN and 10.7 h with ABZ treatment), although no significant differences were observed for these latter pharmacokinetic parameters. Regarding ABZSO(2), C(max), AUC and t(max) values were similar after both treatments (ABZ or ABZ + MEN). The results obtained indicate that co-administration of ABZ and MEN may be an interesting and practical option to increase the efficacy of this anthelmintic. MDPI 2022-02-14 /pmc/articles/PMC8868263/ /pubmed/35203171 http://dx.doi.org/10.3390/ani12040463 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Diez, Raquel Diez, M. Jose Garcia, Juan J. Rodríguez, Jose M. Lopez, Cristina Fernandez, Nelida Sierra, Matilde Sahagun, Ana M. Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title | Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title_full | Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title_fullStr | Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title_full_unstemmed | Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title_short | Improvement of Albendazole Bioavailability with Menbutone Administration in Sheep |
title_sort | improvement of albendazole bioavailability with menbutone administration in sheep |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8868263/ https://www.ncbi.nlm.nih.gov/pubmed/35203171 http://dx.doi.org/10.3390/ani12040463 |
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