Effects of transdermal lidocaine or lidocaine with prilocaine or tetracaine on mechanical superficial sensation and nociceptive thermal thresholds in horses

Söbbeler, F.; Kästner, Sabine

doi:10.1016/j.vaa.2017.10.003

Cited by 10 publications

(8 citation statements)

References 33 publications

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“…The number of horses selected was based on the thermal threshold. Power analysis, assuming a mean baseline thermal excursion of 71, a mean thermal excursion of 95 in each treatment group immediately after treatment and a mean thermal excursion of 85 in each treatment group 1-hour post treatment was conducted, as described in a previous study [ 36 ]. For paired t-tests, a standard deviation of 10 for the difference between baseline and treatment was used.…”

Section: Methodsmentioning

confidence: 99%

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Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses

et al. 2022

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Background In humans, codeine is a commonly prescribed analgesic that produces its therapeutic effect largely through metabolism to morphine. In some species, analgesic effects of morphine have also been attributed to the morphine-6-glucuronide (M6G) metabolite. Although an effective analgesic, administration of morphine to horses produces dose-dependent neuroexcitation at therapeutic doses. Oral administration of codeine at a dose of 0.6 mg/kg has been shown to generate morphine and M6G concentrations comparable to that observed following administration of clinically effective doses of morphine, without the concomitant adverse effects observed with morphine administration. Based on these results, it was hypothesized that codeine administration would provide effective analgesia with decreased adverse excitatory effects compared to morphine. Seven horses received a single oral dose of saline or 0.3, 0.6 or 1.2 mg/kg codeine or 0.2 mg/kg morphine IV (positive control) in a randomized balanced 5-way cross-over design. Blood samples were collected up to 72 hours post administration, codeine, codeine 6-glucuronide, norcodeine morphine, morphine 3-glucuronide and M6G concentrations determined by liquid chromatography- mass spectrometry and pharmacokinetic analysis performed. Pre- and post-drug related behavior, locomotor activity, heart rate and gastrointestinal borborygmi were recorded. Response to noxious stimuli was evaluated by determining thermal threshold latency. Results Morphine concentrations were highest in the morphine dose group at all times post administration, however, M6G concentrations were significantly higher in all the codeine dose groups compared to the morphine group starting at 1 hour post drug administration and up to 72-hours in the 1.2 mg/kg group. With the exception of one horse that exhibited signs of colic following administration of 0.3 and 0.6 mg/kg, codeine administration was well tolerated. Morphine administration, led to signs of agitation, tremors and excitation. There was not a significant effect on thermal nociception in any of the dose groups studied. Conclusions The current study describes the metabolic profile and pharmacokinetics of codeine in horses and provides information that can be utilized in the design of future studies to understand the anti-nociceptive and analgesic effects of opioids in this species with the goal of promoting judicious and safe use of this important class of drugs.

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Section: Methodsmentioning

confidence: 99%

“…A commercially available wireless device (Topcat Metrology, UK) was used, as described previously [ 36 , 38 – 41 ], for thermal threshold testing. Briefly, prior to the commencement of the study, an area on the outside of the metacarpus was shaved for application of the temperature probe.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses

et al. 2022

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“…The number of horses selected for this study was based on pharmacodynamic endpoints, specifically thermal threshold. A power analysis assuming a mean baseline thermal excursion of 71, a mean thermal excursion of 95 in each treatment group immediately after treatment, and a mean thermal excursion of 85 in each treatment group 1-hour post-treatment, using data from a related study [32] was conducted. For paired t-tests, a standard deviation of 10 for the difference between baseline and treatment was assumed.…”

Section: Horsesmentioning

confidence: 99%

“…Thermal threshold testing was conducted using a commercially available wireless device WTT2; TopCat Metrology, UK) as described previously [32]. Briefly, an area on the outside of the metacarpus was shaved at least one day prior to applying the temperature probe.…”

Section: Thermal Threshold Determinationmentioning

confidence: 99%

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Meperidine pharmacokinetics and effects on physiologic parameters and thermal threshold following intravenous administration of three doses to horses

et al. 2020

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Background Meperidine is a synthetic opioid that belongs to the phenylpiperidine class and is a weak mu receptor agonist. In horses there are a limited number of published studies describing the analgesic effects of systemically administered meperidine in horses. The objective of this study was to describe the pharmacokinetics, behavioral and physiologic effects and effect on thermal threshold of three doses of intravenously administered meperidine to horses. Eight University owned horses (four mares and four geldings, aged 3–8 years were studied using a randomized balanced 4-way cross-over design. Horses received a single intravenous dose of saline, 0.25, 0.5 and 1.0 mg/kg meperidine. Blood was collected before administration and at various time points until 96 hours post administration. Plasma and urine samples were analyzed for meperidine and normeperidine by liquid chromatography-mass spectrometry and plasma pharmacokinetics determined. Behavioral and physiologic data (continuous heart rate, step counts, packed cell volume, total plasma protein and gastrointestinal sounds) were collected at baseline through 6 hours post administration. The effect of meperidine administration on thermal nociception was determined and thermal excursion calculated. Results Meperidine was rapidly converted to the metabolite normeperidine. The volume of distribution at steady state and systemic clearance (mean ± SD) ranged from 0.829 ± 0.138–1.58 ± 0.280 L/kg and 18.0 ± 1.4–22.8 ± 3.60 mL/min/kg, respectively for 0.5–1.0 mg/kg doses. Adverse effects included increased dose-dependent central nervous excitation, heart rate and cutaneous reactions. Significant effects on thermal nociception were short lived (up to 45 minutes at 0.5 mg/kg and 15 minutes at 1.0 mg/kg). Conclusions Results of the current study do not support routine clinical use of IV meperidine at a dose of 1 mg/kg to horses. Administration of 0.5 mg/kg may provide short-term analgesia, however, the associated inconsistent and/or short-term adverse effects suggest that its use as a sole agent at this dose, at best, must be cautiously considered.

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Application of composite dissolving microneedles with high drug loading ratio for rapid local anesthesia

Zhan

Huang

et al. 2018

European Journal of Pharmaceutical Sciences

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Effects of transdermal lidocaine or lidocaine with prilocaine or tetracaine on mechanical superficial sensation and nociceptive thermal thresholds in horses

Cited by 10 publications

References 33 publications

Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses

Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses

Meperidine pharmacokinetics and effects on physiologic parameters and thermal threshold following intravenous administration of three doses to horses

Application of composite dissolving microneedles with high drug loading ratio for rapid local anesthesia

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