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Novel holistic pharmacokinetic model applied to plasma and urine concentrations of 2,5‐dihydroxybenzene sulphonate following administrations of calcium dobesilate and etamsylate to exercised horses (2023)
Journal Article
Paine, S. W., Harding, C., Waller, C. C., Zemenova, J., Viljanto, M., Habershon Butcher, J., & Hincks, P. R. (2023). Novel holistic pharmacokinetic model applied to plasma and urine concentrations of 2,5‐dihydroxybenzene sulphonate following administrations of calcium dobesilate and etamsylate to exercised horses. Journal of Veterinary Pharmacology and Therapeutics, 46(6), 365-374. https://doi.org/10.1111/jvp.13387

AbstractCalcium dobesilate (CD) is a synthetic venoactive drug used in veterinary medicine to treat equine navicular disease. Etamsylate is a haemostatic agent used in horses for the treatment of exercise‐induced pulmonary haemorrhage. Both etamsylat... Read More about Novel holistic pharmacokinetic model applied to plasma and urine concentrations of 2,5‐dihydroxybenzene sulphonate following administrations of calcium dobesilate and etamsylate to exercised horses.

Pharmacokinetics of paracetamol in the Thoroughbred horse following an oral multi-dose administration (2021)
Journal Article
Pesko, B., Habershon-Butcher, J., Muir, T., Gray, B., Taylor, P., Fenwick, S., …Paine, S. (2022). Pharmacokinetics of paracetamol in the Thoroughbred horse following an oral multi-dose administration. Journal of Veterinary Pharmacology and Therapeutics, 45(1), 54-62. https://doi.org/10.1111/jvp.13024

Paracetamol is a widely used, non-opioid analgesic and antipyretic drug. Scientific evidence suggests that it is an effective pain treatment in equine medicine. However, there is very little published information about the pharmacokinetics of the dru... Read More about Pharmacokinetics of paracetamol in the Thoroughbred horse following an oral multi-dose administration.

Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses (2021)
Journal Article
Paine, S. W., Aldurdunji, M., Garth-Greeves, A., Muir, T., & Hincks, P. R. (2022). Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses. Journal of Veterinary Pharmacology and Therapeutics, 45(1), 46-53. https://doi.org/10.1111/jvp.13010

Hydroxyzine and cetirizine are first- and second-generation oral antihistamine drugs, respectively, used to treat allergic reactions in horses. Cetirizine is also a metabolite of hydroxyzine, which may lead to complexities in regulating their use in... Read More about Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses.

Plasma and urine pharmacokinetics of two formulations of dexamethasone in greyhound dogs (2021)
Journal Article
Morris, T., Paine, S. W., Zahra, P., Li, E., Colgan, S., & Karamatic, S. (2021). Plasma and urine pharmacokinetics of two formulations of dexamethasone in greyhound dogs. Journal of Veterinary Pharmacology and Therapeutics, 44(5), 689-695. https://doi.org/10.1111/jvp.12970

Dexamethasone, formulated as sodium phosphate and as phenylpropionate combined with sodium phosphate, was administered subcutaneously to six greyhounds. Plasma and urine were collected for up to 240h and analysed with a limit of quantification (LOQ)... Read More about Plasma and urine pharmacokinetics of two formulations of dexamethasone in greyhound dogs.

Pharmacokinetics of carprofen and firocoxib for medication control in racing greyhounds (2020)
Journal Article
Morris, T. H., Paine, S. W., Zahra, P. W., Li, E. C., Colgan, S. .., & Karamatic, S. L. (2020). Pharmacokinetics of carprofen and firocoxib for medication control in racing greyhounds. Australian Veterinary Journal, 98(12), 578-585. https://doi.org/10.1111/avj.13014

Animals used in sport should be treated as required to ensure animal welfare but any such use of medication should also be controlled to ensure integrity. Pharmacokinetic studies on groups of six greyhounds were performed to measure plasma and urine... Read More about Pharmacokinetics of carprofen and firocoxib for medication control in racing greyhounds.

Prediction of Pharmacokinetic Clearance and Potential Drug-Drug Interactions for Omeprazole in the Horse using in vitro Systems (2020)
Journal Article
Shibany, K. A., Pratt, S. L., Aldurdunji, M., Totemeyer, S., & Paine, S. W. (2020). Prediction of Pharmacokinetic Clearance and Potential Drug-Drug Interactions for Omeprazole in the Horse using in vitro Systems. Xenobiotica, 50(10), 1220-1227. https://doi.org/10.1080/00498254.2020.1764131

Horses are exposed to various kinds of medication, however, there are limited determinations of plasma clearance (CLp) for the drugs used due to the high cost of equine in vivo studies. Many of the CLp values generated come from the equine sports ind... Read More about Prediction of Pharmacokinetic Clearance and Potential Drug-Drug Interactions for Omeprazole in the Horse using in vitro Systems.

Hydrostatic pressure regulates CYP1A2 expression in human hepatocytes via a mechanosensitive aryl hydrocarbon receptor-dependent pathway (2020)
Journal Article
Burton, L., Scaife, P., Paine, S. W., Mellor, H. R., Abernethy, L., Littlewood, P., & Rauch, C. (2020). Hydrostatic pressure regulates CYP1A2 expression in human hepatocytes via a mechanosensitive aryl hydrocarbon receptor-dependent pathway. American Journal of Physiology - Cell Physiology, 318(5), C889-C902. https://doi.org/10.1152/ajpcell.00472.2019

Approximately 75% of xenobiotics are primarily eliminated through metabolism; thus the accurate scaling of metabolic clearance is vital to successful drug development. Yet, when data is scaled from in vitro to in vivo, hepatic metabolic clearance, th... Read More about Hydrostatic pressure regulates CYP1A2 expression in human hepatocytes via a mechanosensitive aryl hydrocarbon receptor-dependent pathway.

The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses (2020)
Journal Article
Paine, S. W., Bright, J., Scarth, J. P., Hincks, P. R., Pearce, C. M., Hannan, C., …Hillyer, L. (2020). The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses. Journal of Veterinary Pharmacology and Therapeutics, 43(2), 162-170. https://doi.org/10.1111/jvp.12838

In equine and racing practice, detomidine and butorphanol are commonly used in combination for their sedative properties. The aim of the study was to produce detection times to better inform European veterinary surgeons, so that both drugs can be use... Read More about The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses.

Re-evaluation of the pharmacokinetics of xylazine administered to Thoroughbred horses (2019)
Journal Article
Habershon‐Butcher, J., Cutler, C., Viljanto, M., Hincks, P. R., Biddle, S., & Paine, S. W. (2020). Re-evaluation of the pharmacokinetics of xylazine administered to Thoroughbred horses. Journal of Veterinary Pharmacology and Therapeutics, 43(1), 6-12. https://doi.org/10.1111/jvp.12820

© 2019 John Wiley & Sons Ltd Xylazine is widely used worldwide as a short-acting sedative in general equine and racing practice. In the UK, although it has a legitimate use during training, equine anti-doping rules state it is a prohibited substanc... Read More about Re-evaluation of the pharmacokinetics of xylazine administered to Thoroughbred horses.

Copper physiology in ruminants: trafficking of systemic copper, adaptations to variation in nutritional supply and thiomolybdate challenge (2019)
Journal Article
Clarkson, A., Paine, S., Martín-Tereso, J., & Kendall, N. (2020). Copper physiology in ruminants: trafficking of systemic copper, adaptations to variation in nutritional supply and thiomolybdate challenge. Nutrition Research Reviews, 33(1), 43-49. https://doi.org/10.1017/S0954422419000180

Ruminants are recognised to suffer from Cu-responsive disorders. Present understanding of Cu transport and metabolism is limited and inconsistent across vets and veterinary professionals. There has been much progress from the studies of the 1980s and... Read More about Copper physiology in ruminants: trafficking of systemic copper, adaptations to variation in nutritional supply and thiomolybdate challenge.

Plasma and urine pharmacokinetics of intravenously administered flunixin in greyhound dogs (2019)
Journal Article
Morris, T., Paine, S. W., Zahra, P., Li, E., Colgan, S., & Karamatic, S. (2019). Plasma and urine pharmacokinetics of intravenously administered flunixin in greyhound dogs. Journal of Veterinary Pharmacology and Therapeutics, 42(5), 505-510. https://doi.org/10.1111/jvp.12775

© 2019 John Wiley & Sons Ltd Medication control in greyhound racing requires information from administration studies that measure drug levels in the urine as well as plasma, with time points that extend into the terminal phase of excretion. To char... Read More about Plasma and urine pharmacokinetics of intravenously administered flunixin in greyhound dogs.

The effects of aging on hepatic microsomal scaling factor and hepatocellularity number in the horse (2018)
Journal Article
Shibany, K. A., Tötemeyer, S., Pratt, S. L., & Paine, S. W. (2018). The effects of aging on hepatic microsomal scaling factor and hepatocellularity number in the horse. Xenobiotica, 48(12), 1237-1244. https://doi.org/10.1080/00498254.2017.1413263

Scaling factor values for the in vitro-in vivo extrapolation of hepatic metabolic clearance for xenobiotics have not yet been determined in horses. Scaling factors were determined by comparing the total protein and or CYP P450 content in microsomes a... Read More about The effects of aging on hepatic microsomal scaling factor and hepatocellularity number in the horse.

The pharmacokinetics of orally administered butylscopolamine in greyhound dogs (2018)
Journal Article
Morris, T., Paine, S. W., Viljanto, M., Hudson, S., Gower, S., Pittorino, M., & Colgan, S. (2018). The pharmacokinetics of orally administered butylscopolamine in greyhound dogs. Journal of Veterinary Pharmacology and Therapeutics, 41(6), 790-794. https://doi.org/10.1111/jvp.12701

The oral tablet formulation of butylscopolamine, which is available without prescription, is commonly used by trainers of racing greyhounds to treat functional urethral obstruction. As medication control of butylscopolamine is therefore required for... Read More about The pharmacokinetics of orally administered butylscopolamine in greyhound dogs.

Re-evaluation of the regulation of omeprazole in racehorses: an evidence-based approach (2018)
Journal Article
Viljanto, M., Hillyer, L., Hincks, P., Pearce, C., & Paine, S. (2018). Re-evaluation of the regulation of omeprazole in racehorses: an evidence-based approach. Journal of Veterinary Pharmacology and Therapeutics, 41(3), 469-475. https://doi.org/10.1111/jvp.12491

Medication and doping control has been established in horseracing to ensure the integrity of the sport and the welfare of the horses. This ensures that horses do not compete under the influence of any drugs, including omeprazole, a therapeutic medica... Read More about Re-evaluation of the regulation of omeprazole in racehorses: an evidence-based approach.

Pharmacokinetics of inorganic cobalt and a vitamin B12 supplement in the thoroughbred horse: differentiating cobalt abuse from supplementation (2017)
Journal Article
Hillyer, L., Ridd, Z., Fenwick, S., Hincks, P., & Paine, S. (2018). Pharmacokinetics of inorganic cobalt and a vitamin B12 supplement in the thoroughbred horse: differentiating cobalt abuse from supplementation. Equine Veterinary Journal, 50(3), 343-349. https://doi.org/10.1111/evj.12774

Background

While cobalt is an essential micronutrient for vitamin B12 synthesis in the horse, at supraphysiological concentrations, it has been shown to enhance performance in human subjects and rats, and there is evidence that its administration... Read More about Pharmacokinetics of inorganic cobalt and a vitamin B12 supplement in the thoroughbred horse: differentiating cobalt abuse from supplementation.

A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions (2017)
Journal Article
Cherkaoui-Rbati, M., Paine, S., Littlewood, P., & Rauch, C. (2017). A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions. PLoS ONE, 12(9), Article e0183794. https://doi.org/10.1371/journal.pone.0183794

All pharmaceutical companies are required to assess pharmacokinetic drug-drug interactions (DDIs) of new chemical entities (NCEs) and mathematical prediction helps to select the best NCE candidate with regard to adverse effects resulting from a DDI b... Read More about A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions.

A clinical evaluation of the pharmacokinetics and pharmacodynamics of intravenous alfaxalone in cyclodextrin in male and female rats following a loading dose and constant rate infusion (2017)
Journal Article
White, K. L., Paine, S., & Harris, J. (2017). A clinical evaluation of the pharmacokinetics and pharmacodynamics of intravenous alfaxalone in cyclodextrin in male and female rats following a loading dose and constant rate infusion. Veterinary Anaesthesia and Analgesia, 44(4), https://doi.org/10.1016/j.vaa.2017.01.001

Objective: To characterise, as a clinical study, the pharmacokinetics and pharmacodynamics and describe the hypnotic effect of the neurosteroid alfaxalone (3α-hydroxy-5 α-pregnane-11, 20-dione) formulated with 2-hydroxypropyl-β-cyclodextrin in male a... Read More about A clinical evaluation of the pharmacokinetics and pharmacodynamics of intravenous alfaxalone in cyclodextrin in male and female rats following a loading dose and constant rate infusion.

Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action (2014)
Journal Article
Stocks, M., Alcaraz, L., Bailey, A., Bonnert, R., Cadogan, E., Christie, J., …Young, A. (2014). Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action. ACS Medicinal Chemistry Letters, 5(4), 416-421. https://doi.org/10.1021/ml4005232

A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human β-adrenoreceptors demonstrated a series of highly potent and se... Read More about Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.

Review: The ubiquitin-proteasome system: contributions to cell death or survival in neurodegeneration (2010)
Journal Article
Rogers, N., Paine, S., Bedford, L., & Layfield, R. (2010). Review: The ubiquitin-proteasome system: contributions to cell death or survival in neurodegeneration. Neuropathology and Applied Neurobiology, 36(2), 113-124. https://doi.org/10.1111/j.1365-2990.2010.01063.x

The significance of the accumulation of ubiquitin-positive intraneuronal inclusions in the brains of those affected with different neurodegenerative diseases is currently unclear. While one interpretation is that the disease mechanism(s) involves dys... Read More about Review: The ubiquitin-proteasome system: contributions to cell death or survival in neurodegeneration.

Pharmacokinetics of meloxicam for medication control in racing greyhounds
Presentation / Conference Contribution
Morris, T. H., Paine, S. W., Viljanto, M., Colgan, S. A., & Karamatic, S. L. (2023, September). Pharmacokinetics of meloxicam for medication control in racing greyhounds. Paper presented at 23rd International Conference of Racing Analysts and Veterinarians, Hong Kong, China

Recent published disciplinary findings from regulators of greyhound racing in Australia, Great Britain and Ireland have shown overall that the most common non-steroidal anti-inflammatory drug (NSAID) adverse analytical finding is for meloxicam. Whils... Read More about Pharmacokinetics of meloxicam for medication control in racing greyhounds.