Stuart W. Paine
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View article: Plasma and Urine Pharmacokinetics of Long‐Acting Injectable Omeprazole Following Intramuscular Administrations to Healthy Thoroughbred Horses
Plasma and Urine Pharmacokinetics of Long‐Acting Injectable Omeprazole Following Intramuscular Administrations to Healthy Thoroughbred Horses Open
Omeprazole is a gastric acid secretion inhibitor used as an effective anti‐ulcer drug. Based on oral administration studies, its International Screening Limit (ISL) was established in plasma and urine at 1 ng/mL with a Detection Time (DT) …
View article: Establishing harmonised screening limits and detection times in greyhound racing — A considered approach
Establishing harmonised screening limits and detection times in greyhound racing — A considered approach Open
An outline of the approach taken by international greyhound regulators to establish internationally harmonised screening limits and detection times in greyhound racing, which included a program of administration studies and an extensive an…
View article: The drug disposition in the Spleen: A novel study of CYP and UGT-mediated drug metabolism
The drug disposition in the Spleen: A novel study of CYP and UGT-mediated drug metabolism Open
Understanding the fate of a drug, its disposition and pharmacokinetics as it reaches the site of action is key to any pharmaceutical research and development. The emerging role of the spleen in its involvement in regulating the immune syst…
View article: 497 PTT-4256 is a first-in-class small molecule inhibitor of GPR65 that counteracts the low pH-dependent immunosuppressive effects on immune cells and displays pronounced anti-tumor activity in mice
497 PTT-4256 is a first-in-class small molecule inhibitor of GPR65 that counteracts the low pH-dependent immunosuppressive effects on immune cells and displays pronounced anti-tumor activity in mice Open
Background An important facet of the hostile tumor microenvironment (TME) and a recognized driver of cancer immunosuppression is extracellular acidification which results from the glycolytic nature of rapidly proliferating cancer cells. Pa…
View article: 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
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 Open
Calcium 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 etamsy…
View article: Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes
Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes Open
The translation of new injectable anesthetic drugs from rodent to humans remains slow, despite the realization that reliance on the volatile agents is unsustainable from an environmental perspective. The aim of this study was to investigat…
View article: Alfaxalone population pharmacokinetics in the rat: model application for PK/PD design in inbred and outbred strains and sexes
Alfaxalone population pharmacokinetics in the rat: model application for PK/PD design in inbred and outbred strains and sexes Open
Background and purpose The translation of new injectable anaesthetic drugs from rodent to humans remains slow, despite the realisation that reliance on the volatile agents is unsustainable from an environmental perspective. The aim of this…
View article: Pharmacokinetics of paracetamol in the Thoroughbred horse following an oral multi‐dose administration
Pharmacokinetics of paracetamol in the Thoroughbred horse following an oral multi‐dose administration Open
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…
View article: Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses
Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses Open
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 th…
View article: Plasma and urine pharmacokinetics of two formulations of dexamethasone in greyhound dogs
Plasma and urine pharmacokinetics of two formulations of dexamethasone in greyhound dogs Open
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 240 h and analysed with a limit of quantific…
View article: Prediction of pharmacokinetic clearance and potential Drug-Drug interactions for omeprazole in the horse using<i>in vitro</i>systems
Prediction of pharmacokinetic clearance and potential Drug-Drug interactions for omeprazole in the horse using<i>in vitro</i>systems Open
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 …
View article: Pharmacokinetics of meloxicam for medication control in racing greyhounds
Pharmacokinetics of meloxicam for medication control in racing greyhounds Open
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 melox…
View article: Hydrostatic pressure regulates CYP1A2 expression in human hepatocytes via a mechanosensitive aryl hydrocarbon receptor-dependent pathway
Hydrostatic pressure regulates CYP1A2 expression in human hepatocytes via a mechanosensitive aryl hydrocarbon receptor-dependent pathway Open
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 cl…
View article: The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses
The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses Open
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…
View article: Re‐evaluation of the pharmacokinetics of xylazine administered to Thoroughbred horses
Re‐evaluation of the pharmacokinetics of xylazine administered to Thoroughbred horses Open
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 substance on race day. The a…
View article: Copper physiology in ruminants: trafficking of systemic copper, adaptations to variation in nutritional supply and thiomolybdate challenge
Copper physiology in ruminants: trafficking of systemic copper, adaptations to variation in nutritional supply and thiomolybdate challenge Open
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 th…
View article: Plasma and urine pharmacokinetics of intravenously administered flunixin in greyhound dogs
Plasma and urine pharmacokinetics of intravenously administered flunixin in greyhound dogs Open
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 characterize the plasma …
View article: The pharmacokinetics of orally administered butylscopolamine in greyhound dogs
The pharmacokinetics of orally administered butylscopolamine in greyhound dogs Open
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 re…
View article: Re‐evaluation of the regulation of omeprazole in racehorses: An evidence‐based approach
Re‐evaluation of the regulation of omeprazole in racehorses: An evidence‐based approach Open
Medication control and doping control have been established in horse racing 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,…
View article: The effects of aging on hepatic microsomal scaling factor and hepatocellularity number in the horse
The effects of aging on hepatic microsomal scaling factor and hepatocellularity number in the horse Open
1. 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 cytochrome (CYP) P…
View article: Pharmacokinetics of inorganic cobalt and a vitamin B <sub>12</sub> supplement in the Thoroughbred horse: Differentiating cobalt abuse from supplementation
Pharmacokinetics of inorganic cobalt and a vitamin B <sub>12</sub> supplement in the Thoroughbred horse: Differentiating cobalt abuse from supplementation Open
Summary Background While cobalt is an essential micronutrient for vitamin B 12 synthesis in the horse, at supraphysiological concentrations, it has been shown to enhance performance in human subjects and rats, and there is evidence that it…
View article: A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions
A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions Open
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 f…
View article: Equine hepatocytes: isolation, cryopreservation, and applications to in vitro drug metabolism studies
Equine hepatocytes: isolation, cryopreservation, and applications to in vitro drug metabolism studies Open
Despite reports of the successful isolation of primary equine hepatocytes, there are no published data regarding the successful cryopreservation of these isolated cells. In this study, a detailed description of the procedures for isolation…