Pharmacokinetic and pharmacodynamic modelling of intravenous, intramuscular and subcutaneous buprenorphine in conscious cats

Steagall, Paulo V.; Pelligand, Ludovic; Giordano, Tatiana; Auberger, Christophe; Sear, J.W.; Luna, Stélio Pacca Loureiro; Taylor, Polly

doi:10.1111/j.1467-2995.2012.00779.x

Cited by 62 publications

(125 citation statements)

References 30 publications

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“…In previous studies that tested thermal antinociception of buprenorphine in cats, antinociception was reported between 4 and 12 hours following 0.01 mg kg -1 IM buprenorphine [8]. Further investigation, including IV and OTM administration at doses of 0.01–0.02 mg kg -1 found shorter durations of antinociception (between 0.5 to 6 hours) [9, 12–14, 18, 22]. Additionally, it appeared that low dose buprenorphine administered SC was ineffective, with near undetectable plasma concentrations that did not provide thermal antinociception [18].…”

Section: Discussionmentioning

confidence: 99%

“…Prospective power analysis concluded that a sample size of six cats would be sufficient to detect mean temperature differences of > 3.2°C with a power of 0.8 and an alpha level set at 0.05 based on a previous study [18]. Statistical analyses were performed using a software (GraphPad Prism, GraphPad software Inc., California, USA).…”

Section: Methodsmentioning

confidence: 99%

“…The use of buprenorphine in this species has been recently reviewed in both experimental and clinical setting [1]. At standard clinical doses (0.02 mg kg -1 ) and concentrations (0.3 mg mL -1 ), buprenorphine is poorly absorbed and has limited antinociceptive effect after subcutaneous (SC) administration [2]. Further investigation showed that increased doses (> 1.2 mg kg -1 ) administered by this route of administration can provide prolonged antinociception and improved absorption compared with standard doses [3].…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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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“…Perhaps, the doses used herein were ineffective. Intravenous administration of 0.02 mg/kg of a similar formulation of buprenorphine resulted in thermal antinociception (Steagall and others 2013). The rationale of adding opioids to PNB is based on the presence of multiple opiate receptor sites on primary afferent nerve fibres (Fields and others 1980).…”

Section: Discussionmentioning

confidence: 99%

Sciatic and femoral nerve blockade using bupivacaine alone, or in combination with dexmedetomidine or buprenorphine in cats

et al. 2017

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The aim of this study was to determine the onset and offset of antinociception after sciatic (ScN) and femoral (FN) nerve blocks. Six healthy adult cats (4.8±1.3years; 4.3±0.4 kg) were included in a randomised, crossover, blinded and controlled study. Following sedation with dexmedetomidine (25 µg/kg, intramuscular), each ScN and FN injection was performed using 0.1 ml/kg of saline (CONTROL), bupivacaine (0.46 per cent, 0.46 mg/kg; BUPI), bupivacaine and dexmedetomidine (1 µg/kg; BUPI-DEX) or bupivacaine and buprenorphine (2.5 µg/kg; BUPI-BUPRE). Atipamezole (250 µg/kg) was administered after injections. Paw withdrawal thresholds (PWT) and motor blockade were evaluated before sedation and up to 24 hours. The PWT were significantly increased at half an hour in CONTROL, from two to four hours in BUPI and BUPI-DEX when compared with baseline. Motor blockade was observed between one and three hours in treatments using bupivacaine. Ability to walk was significantly impaired in BUPI at half an hour to two hours, BUPI-DEX at one to two hours and BUPI-BUPRE at two hours. Antinociception was observed in BUPI between one and eight hours, and in BUPI-DEX and BUPI-BUPRE between one and four hours. This study could not demonstrate a benefit of administering bupivacaine with dexmedetomidine or buprenorphine in cats. Results in BUPI-DEX may have been biased by the administration of atipamezole.

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“…Cats administered buprenorphine OTM or subcutaneously required more rescue analgesia than those administered buprenorphine via the intravenous or intramuscular routes. Other evidence indicates that OTM absorption might not be as high as originally thought (Pypendop and Ilkiw 2008) and that absorption after subcutaneous administration is erratic and unable to sustain plasma levels compatible with pain relief (Steagall and others 2013) .…”

Section: Pharmacology Of Analgesic Drugs In Catsmentioning

confidence: 99%

Controlling pain in cats

Drożdżyńska¹,

Pelligand²

2016

In Practice

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Pain should be assessed in cats as a part of triage and a validated pain scoring system should be used. A good understanding of pain physiology and pharmacology of analgesic agents is essential for choosing the most appropriate analgesic drug combination and reducing the risk of side effects. With diligent acute pain management, the risk of chronic pain development is reduced. This article summarises the physiology of adaptive and maladaptive pain, and provides an overview of currently available techniques and therapeutics used to assess and treat acute perioperative and chronic pain in cats.

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Pharmacokinetic and pharmacodynamic modelling of intravenous, intramuscular and subcutaneous buprenorphine in conscious cats

Cited by 62 publications

References 30 publications

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

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

Sciatic and femoral nerve blockade using bupivacaine alone, or in combination with dexmedetomidine or buprenorphine in cats

Controlling pain in cats

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