Detection and pharmacokinetics of salbutamol in thoroughbred racehorses following inhaled administration

Wieder, M. E.; Paine, Stuart W.; Hincks, Pamela; Pearce, Clive M.; Scarth, James; Hillyer, Lynn

doi:10.1111/jvp.12150

Cited by 7 publications

(4 citation statements)

References 17 publications

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“…Total SAL concentration in urine was significantly higher than that in plasma ( p < 0.01), whether in pigs or goats. This is basically consistent with the reports of SAL in cattle, horses, and humans ( Wieder et al, 2015 ; Zhang et al, 2016 ; Zhang et al, 2017b ; Ye et al, 2019 ). Moreover, at the withdrawal time of 0.25 days, total SAL concentration in goat’s urine and plasma was 4 and 2 times that in pig’s urine and plasma, respectively, and the proportions of conjugated SAL in goat’s urine and plasma were also significantly higher than those in pigs.…”

Section: Discussionsupporting

confidence: 92%

Excretion and Residual Concentration Correlations of Salbutamol Between Edible Tissues and Living Samples in Pigs and Goats

et al. 2021

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Illegal use of salbutamol (SAL), a β-adrenergic leanness-enhancing agent, has posed potential threat to human health in China. The excretion and depletion of SAL in pigs and goats were investigated, and the concentration correlations between edible tissues and living samples were analyzed to find out a suitable living sample for pre-slaughter monitoring of SAL in pigs and goats. After a single oral dosage of 1.2 mg/kg SAL, approximately 70% of the dose was excreted by pigs and goats from their excreta. When pigs and goats were supplied feed containing SAL (20 mg/kg) for 14 consecutive days, high concentrations of SAL were observed in the liver and kidneys, and the longest persistence was observed in hair. Unlike pigs, SAL was presented primarily as conjugated SAL in goats. Excellent concentration correlations of SAL were observed between urine and edible tissues both in pigs and goats, and in addition, good correlations also were found between hair and edible tissues in pigs and between feces and edible tissues in goats. Hence, urine and hair could accurately predict SAL concentrations in edible tissues of pigs, whereas feces and urine were satisfactory for predicting SAL concentrations in edible tissues of goats. These data make it possible for pre-slaughter monitoring of SAL residues in the edible tissues of pigs and goats.

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Section: Discussionsupporting

confidence: 92%

Excretion and Residual Concentration Correlations of Salbutamol Between Edible Tissues and Living Samples in Pigs and Goats

et al. 2021

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“…23 This targeted action in the lungs is a relevant advantage, as it minimizes systemic adverse events and procures the therapeutic effect where it is required. Although salbutamol does enter systemic circulation, it is rapidly metabolized, [24][25][26] which can be a substantial consideration in equine competitions governed by drug use regulations. The intravenous route of administration of HBB could have contributed to its shorter duration of effect in the current study, as it directly enters the bloodstream and could be metabolized more rapidly.…”

Section: Discussionmentioning

confidence: 99%

Comparative study of the bronchodilator efficacy and adverse effects of salbutamol and hyoscine butylbromide in horses with severe asthma

Mozo Vives,

Mainguy‐Seers,

Lavoie

2024

Veterinary Internal Medicne

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BackgroundSalbutamol and hyoscine butylbromide (HBB) are commonly used bronchodilators in horses with severe asthma (SA).ObjectiveTo compare the bronchodilation potency, duration, and adverse effects of salbutamol and HBB in SA.AnimalsSix horses in exacerbation of SA.MethodsThe effects of inhaled salbutamol (1000 μg) and HBB (150 mg, IV) were compared in a randomized, blinded, crossover experiment. Lung function, intestinal borborygmi and heart rate were assessed before and sequentially until 180 minutes after drug administration, and analyzed with 2‐way repeated‐measures ANOVA and Dunnett's multiple comparison tests.ResultsBoth treatments caused a similar improvement in lung function. Pulmonary resistance and reactance returned to baseline values within 30 minutes after HBB administration, whereas salbutamol improved reactance until 180 minutes (mean improvement at 180 minutes of 0.040 Kpa/L/s, 95% CI = 0.004 to 0.076; P = .02 for salbutamol and of 0.009 Kpa/L/s, 95% CI = −0.028 to 0.045; P = .98 for HBB for the resistance at 3 Hz and of 0.040 Kpa/L/s, 95% CI = 0.007 to 0.074; P = .01 for salbutamol and of 0.009 Kpa/L/s, 95% CI = −0.024 to 0.042; P = .97 for HBB for the reactance at 7 Hz). From 5 to 30 minutes after HBB administration, the heart rate accelerated (mean increase of 3.3 beats per minute, 95% CI = −6.6 to 13.1; P = .92 for salbutamol, and of 13.0 beats per minute, 95% CI = 3.6 to 22.4; P = .002 for HBB at 30 minutes) and the gut sounds decreased (mean reduction of 1.3, 95% CI = −0.1 to 2.8; P = .09 for salbutamol and of 2.8 for the gastrointestinal auscultation score, 95% CI = 1.4 to 4.3; P < .0001 for HBB at 30 minutes).Conclusions and Clinical ImportanceBoth drugs have a similar bronchodilator potency but with a longer duration for salbutamol. Gastrointestinal and cardiovascular effects were noted only with HBB, suggesting the preferential use of salbutamol to relieve bronchoconstriction in horses with asthma.

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“…In association with the European Horserace Scientific Liaison Committee (EHSLC, ), the BHA develops advice in the form of DTs for commonly used therapeutic medications. A similar investigation into salbutamol was previously undertaken by Wieder and co‐workers (Wieder et al ., ). Average urinary concentrations at steady‐state were calculated to reach an effective urine concentration as a marker for the lung (9.6 ng/mL).…”

Section: Introductionmentioning

confidence: 99%

Detection and pharmacokinetics of salmeterol in thoroughbred horses following inhaled administration

Fenwick¹,

Hincks²,

Scarth³

et al. 2017

Vet Pharm & Therapeutics

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Salmeterol is a man-made beta-2-adrenergic receptor agonist used to relieve bronchospasm associated with inflammatory airway disease in horses. Whilst judicious use is appropriate in horses in training, they cannot race with clinically effective concentrations of medications under the British Horseracing Authority's Rules of Racing. Salmeterol must therefore be withdrawn prior to race day and pharmacokinetic (PK) studies used to establish formal detection time advice. Salmeterol xinafoate (Serevent Evohaler ) was administered (0.1 mg twice daily for 4.5 days) via inhalation to six horses. Urine and blood samples were taken up to 103 h postadministration. Hydrolysed samples were extracted using solid phase extraction. A sensitive Ultra high performance tandem mass spectrometry (UPLC-MS/MS) method was developed, with a Lower limit of quantification (LLOQ) for salmeterol of 10 pg/mL in both matrices. The majority of salmeterol plasma concentrations, postlast administration, were below the method LLOQ and so unusable for PK analysis. Urine PK analysis suggested a half-life consistent with duration of pharmacological effect. Average estimated urine concentration at steady-state was obtained via PK modelling and used to estimate a urine concentration of 59 ± 34 pg/mL as a marker of effective lung concentration. From this, potential detection times were calculated using a range of safety factors.

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Detection and pharmacokinetics of salbutamol in thoroughbred racehorses following inhaled administration

Cited by 7 publications

References 17 publications

Excretion and Residual Concentration Correlations of Salbutamol Between Edible Tissues and Living Samples in Pigs and Goats

Excretion and Residual Concentration Correlations of Salbutamol Between Edible Tissues and Living Samples in Pigs and Goats

Comparative study of the bronchodilator efficacy and adverse effects of salbutamol and hyoscine butylbromide in horses with severe asthma

Detection and pharmacokinetics of salmeterol in thoroughbred horses following inhaled administration

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