A physiologically based model for tramadol pharmacokinetics in horses

Abbiati, R.; Cagnardi, P.; Ravasio, Giuliano; Villa, Roberto Edoardo; Manca, Davide

doi:10.1016/j.jtbi.2017.06.028

Cited by 4 publications

(4 citation statements)

References 26 publications

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“…Tramadol is an opioid analgesic that is widely prescribed by veterinarians [ 7 ]. It is routinely used to treat acute and chronic pain in animals [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

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Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys (Equus asinus)

Araújo-Silva,

de Macêdo,

Mouta

et al. 2024

Animals

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Our objective was to assess the pharmacokinetic characteristics of metamizole when administered together with tramadol in a single intravenous dose to donkeys. Ten male animals received 10 mg∙kg−1 of dipyrone associated with 2 mg∙kg−1 of tramadol (T2M10) and 25 mg∙kg−1 of dipyrone with 2 mg∙kg−1 of tramadol (T2M25). Venous blood samples were taken from groups to determine the pharmacokinetics after drug administration, using initial brief intervals that were followed by extended periods until 48 h. Restlessness and ataxia were observed in two animals in the T2M25 group. Analysis revealed prolonged detectability of tramadol, 4-methylamine antipyrine, 4-aminoantipyrine (up to 24 h), and O-desmethyltramadol (up to 12 h) after administration. Although metamizole and its metabolites showed no significant pharmacokinetic changes, tramadol and O-desmethyltramadol exhibited altered profiles, likely because of competition for the active sites of CYP450 enzymes. Importantly, the co-administration of metamizole increased the bioavailability of tramadol and O-desmethyltramadol in a dose-dependent manner, highlighting their potential interactions and emphasizing the need for further dose optimization in donkey analgesic therapies. In conclusion, metamizole co-administered with tramadol interferes with metabolism and this interference can change the frequency of drug administration and its analgesic efficacy.

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“…Tramadol is an opioid analgesic that is widely prescribed by veterinarians [ 7 ]. It is routinely used to treat acute and chronic pain in animals [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

“…Donkeys differ from horses in behavioral, physiological, and pharmacological aspects [ 16 ]. Therefore, knowledge of the pharmacokinetic properties of drugs is fundamental to guarantee effective and safe therapeutic administration [ 7 ].…”

Section: Introductionmentioning

confidence: 99%

Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys (Equus asinus)

Araújo-Silva,

de Macêdo,

Mouta

et al. 2024

Animals

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“…Tramadol is a synthetic opioid analgesic used for pain management [ 1 ] that acts on the µ-opioid receptor with a low risk of substance dependence [ 6 ]. Previous studies have investigated a physiologically based model for tramadol pharmacokinetics [ 1 ] and physiological responses to tramadol with xylazine [ 18 ] and detomidine [ 9 ] in horses. However, there has not been an evaluation of the clinical responses to a tramadol and medetomidine combination during an entire surgical procedure.…”

mentioning

confidence: 99%

“…There were no significant differences in the SS between groups (Fig 2A) Tramadol is an analgesic opioid that acts on µ-opioid receptor with a low risk of substance dependence [6]. There have been studies on the pharmacokinetics for optimal pharmacological treatment and analgesic effects of tramadol in horses [1,5]. Tramadol with detomidine has a longer analgesic effect than a single administration of detomidine or tramadol [9] and tramadol enhances the effects of xylazine [18].…”

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confidence: 99%

Comparison of intraoperative cardiorespiratory and behavioral responses to medetomidine combined with tramadol or butorphanol during standing laparoscopic ovariectomy in horses

et al. 2021

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The purpose of this study was to assess the cardiorespiratory and behavioral responses to the combination of medetomidine and tramadol (M-T) or butorphanol (M-B) in standing laparoscopic ovariectomy in horses. One ovary was removed under M-T and the contralateral ovary was removed under M-B with at least 4 weeks between operations at random. Horses were sedated using intravenous medetomidine (5 µg/kg) followed by tramadol (1 mg/kg) or butorphanol (10 µg/kg) after 5 min. Sedation was maintained through the repeated injection of medetomidine (1 µg/kg) and tramadol (0.4 mg/kg) or medetomidine (1 µg/kg) and butorphanol (4 µg/kg) every 15 min. Cardiorespiratory function and behavioral responses, including, sedation, ataxia, and analgesia, were assessed during the surgery. There were no significant differences in cardiorespiratory values and sedation and analgesia scores between M-T and M-B. Ataxia scores were significantly lower in M-T than in M-B. This result suggests that M-T could maintain smooth and stable standing surgery with minimal cardiorespiratory changes in horses.

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A history and recent efforts of selected physiologically based pharmacokinetic modeling topics

Lin

Fisher

2020

Physiologically Based Pharmacokinetic (PBPK) Modeling

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A physiologically based model for tramadol pharmacokinetics in horses

Cited by 4 publications

References 26 publications

Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys (Equus asinus)

Tramadol and M1 Bioavailability Induced by Metamizole Co-Administration in Donkeys (Equus asinus)

Comparison of intraoperative cardiorespiratory and behavioral responses to medetomidine combined with tramadol or butorphanol during standing laparoscopic ovariectomy in horses

A history and recent efforts of selected physiologically based pharmacokinetic modeling topics

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