Intravenous and sublingual buprenorphine in horses: pharmacokinetics and influence of sampling site

Messenger, Kristen M.; Davis, Jennifer L.; LaFevers, D. Heath; Barlow, Beth M.; Posner, Lysa P.

doi:10.1111/j.1467-2995.2011.00613.x

Cited by 39 publications

(67 citation statements)

References 26 publications

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“…Almost all buprenorphine treated horses showed increased locomotor activity and signs of excitation for approximately 5 hours like it was described in previous studies [9,24-26]. Locomotor activity became evident when acepromazine effects declined, which might interfere with the detection of behavioural responses to thermal stimulation [3].…”

Section: Discussionmentioning

confidence: 55%

“…Elimination half-life for buprenorphine was 6.4 hours in the current study, which might even be underestimated as serum concentrations did not fall below the limit of quantification in the terminal phase. However, the determined terminal half-life is comparable to 5.79 hours determined with a slightly lower dose of buprenorphine (0.006 mg/kg, IV) [24]. At a buprenorphine dose of 0.005 mg/kg buprenorphine IV elimination half-life was shorter with 3.58 hours [25] suggesting a dose dependent effect, differences in sensitivity of the buprenorphine analysis or an influence of acepromazine co-medication.…”

Section: Discussionmentioning

confidence: 74%

“…In other studies gastrointestinal borborygmi also decreased following buprenorphine which was attenuated when buprenorphine was given sublingually [9,24,26]. When hay was withdrawn 12 hours before intravenous buprenorphine, there were no signs of abdominal discomfort observed [9].…”

Section: Discussionmentioning

confidence: 88%

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Nociceptive thermal threshold testing in horses – effect of neuroleptic sedation and neuroleptanalgesia at different stimulation sites

et al. 2013

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BackgroundAim of the study was to compare the effect of neuroleptic sedation with acepromazine and neuroleptanalgesia with acepromazine and buprenorphine on thermal thresholds (TT) obtained at the nostrils and at the withers. The study was carried out as a randomized, blinded, controlled trial with cross-over design. Thermal thresholds were determined by incremental contact heat applied to the skin above the nostril (N) or the withers (W). Eleven horses were treated with saline (S), acepromazine (0.05 mg/kg) (ACE) or acepromazine and buprenorphine (0.0075 mg/kg) (AB) intravenously (IV). Single stimulations were performed 15 minutes prior and 15, 45, 75, 105, 165, 225, 285, 405 and 525 minutes after treatment. Sedation score, gastrointestinal auscultation score and occurrence of skin lesions were recorded. Data were analysed with analysis of variance for repeated measurements.ResultsThere were no significant differences in TT between N and W with all treatments. The TT remained constant after S and there was no difference in TT between S and ACE. After AB there was a significant increase above baseline in TT until 405 minutes after treatment. Restlessness occurred 30–90 minutes after AB in 7 horses. All horses had reduced to absent borborygmi after AB administration for 165 to 495 minutes.ConclusionThermal stimulation at both described body areas gives comparable results in the assessment of cutaneous anti-nociception in horses. There is no differential influence of neuroleptic sedation or neuroleptanalgesia on TTs obtained at N or W. Buprenorphine combined with acepromazine has a long lasting anti-nociceptive effect associated with the typical opioid induced side effects in horses.

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Section: Discussionmentioning

confidence: 55%

Section: Discussionmentioning

confidence: 74%

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Nociceptive thermal threshold testing in horses – effect of neuroleptic sedation and neuroleptanalgesia at different stimulation sites

et al. 2013

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“…There are two studies in particular in which this overestimation has been documented. One study found an F of 116% and the other 139% in cats [9] and horses [27], respectively. When carotid arterial, jugular venous and saphenous sampling sites were simultaneously compared in cats, F was reported as 32%, 47% and 23% respectively [26].…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic modelling after subcutaneous, intravenous and buccal administration of a high-concentration formulation of buprenorphine in conscious cats

et al. 2017

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BackgroundThe aim of this study was to describe the joint pharmacokinetic-pharmacodynamic model and evaluate thermal antinociception of a high-concentration formulation of buprenorphine (Simbadol™) in cats.MethodsSix healthy cats (4.9 ± 0.7 kg) were included in a prospective, randomized, blinded, crossover study. Simbadol™ (1.8 mg mL-1) was administered by the subcutaneous (SC; 0.24 mg kg-1), intravenous (IV; 0.12 mg kg-1) or buccal (OTM; 0.12 mg kg-1) route of administration and thermal thresholds (TT) were compared with a saline group (SAL). Thermal threshold testing and blood sampling were performed at predetermined time points up to 72 hours including a placebo group. Plasma buprenorphine and norbuprenorphine concentrations were measured using liquid chromatography mass spectrometry. A bespoke bicompartmental pharmacokinetic model simultaneously fitted data from two analytes/three routes of administration. Temporal changes in TT were analyzed using one-way ANOVA followed by Dunnett’s test and treatment comparisons using two-way ANOVA with Bonferroni’s correction (P < 0.05).ResultsThermal thresholds were significantly increased after SC, IV and OTM from 1–24 hours (except 2 hours), 0.5–8 hours (except 6 hours), and 1–8 hours (except 6 hours), respectively, when compared with baseline. Thermal thresholds were significantly increased after SC (1–30 hours), IV (1–8 hours) and OTM (1–12 hours) when compared with SAL, but not different among buprenorphine-treated cats. The absolute buprenorphine clearance was 0.98 L kg-1 hour-1, volume of distribution at steady state was 7.9 L kg-1 and the elimination-half-life was 12.3 hours. Bioavailability for SC and OTM was 94% and 24%, respectively. Subcutaneous absorption was biphasic. An initial peak (0.08 hours) was followed by a slow (half-life 11.2 hours) and progressive (peak acceleration at 2.8 hours) uptake.ConclusionThe SC administration of Simbadol™ was characterized by prolonged absorption half-life and sustained plasma concentrations yielding long-lasting antinociception (≥ 24 hours) when compared with the IV and OTM routes.

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“…Lately, as an alternative to butorphanol, buprenorphine is gaining interest as an analgesic for horses (Messenger et al 2011, Taylor et al 2014, Love et al 2015. As no data were available for treatment of foals, the antinociceptive efficacy of buprenorphine in foals was investigated using the NWR model.…”

Section: Opioidsmentioning

confidence: 99%

The model of the Nociceptive Withdrawal Reflex in horses

Spadavecchia¹,

Rohrbach²,

Levionnois³

et al. 2016

PHK

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Summary: In equine pain research, the Nociceptive Withdrawal Reflex (NWR) model has been proposed as an alternative to classical thermal, mechanical and electrical models to investigate the physiology of nociception. This model does not only allow a more reliable definition of the nociceptive threshold through neurophysiological characterization of the elicited response , but also consents plotting a stimulus-response curve as well as the evaluation of temporal summation mechanisms. Aim of this report is to summarize the experience and results obtained using the NWR model in horses over the last 15 years, firstly with the purpose of describing its physiological characteristics and secondly with the aim of evaluating its pharmacological modulation through analgesic and anaesthetic compounds. The NWR can be elicited in horses through electrical transcutaneous stimulation of a peripheral sensory nerve and is recorded through electromyographic electrodes from the muscles involved in the withdrawal reaction. As the non-nociceptive fibres have lower threshold to electrical stimuli than the nociceptive one, it is impossible to differentiate between the two groups on the stimulus side. So, the only guidance to assess the quality of the stimulus and the recruitment of nociceptive afferents should rely on the characteristics of the electromyographic response, most of all on the timing of its various components. A reflex response can be considered to be a true NWR only if it appears within a time epoch compatible with the conduction velocity of the A fibers. Furthermore a clearly recognizable EMG burst in the epoch of interest has to be accompanied by a consistent aversive behavioural reaction, thus allowing the definition of a reliable NWR threshold. Responses to stimulation intensities below and above thresholds can be quantified to draw a stimulus response curve. Furthermore, through repeated stimulation at subthreshold intensities, it is possible to elicit the phenomenon of temporal summation, considered to be the early phase of the wind up phenomenon and of relevant interest to study central integrative mechanisms of pain processing. Alpha-2 agonists, opioids, systemic lidocaine, ketamine and inhalation anaesthetics have been investigated using the NWR model in horses. Drug-specific modulation of NWR threshold, stimulus-response curves and temporal summation are summarized for each tested compound.

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Intravenous and sublingual buprenorphine in horses: pharmacokinetics and influence of sampling site

Cited by 39 publications

References 26 publications

Nociceptive thermal threshold testing in horses – effect of neuroleptic sedation and neuroleptanalgesia at different stimulation sites

Nociceptive thermal threshold testing in horses – effect of neuroleptic sedation and neuroleptanalgesia at different stimulation sites

Pharmacokinetic and pharmacodynamic modelling after subcutaneous, intravenous and buccal administration of a high-concentration formulation of buprenorphine in conscious cats

The model of the Nociceptive Withdrawal Reflex in horses

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