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 Detection Time (DT) of 48 h. A novel formulation injectable omeprazole has since been released, therefore, pharmacokinetic study performed to assess the DT above ISL against current advice. Six Thoroughbred horses were given four repeated weekly intramuscular administrations (4...

LGD-4033 is one of a number selective androgen receptor modulators (SARMs) that are being developed by the pharmaceutical industry to provide therapeutic benefits anabolic androgenic steroids, without less desirable side effects. Though not available therapeutically, SARMs for purchase online as supplement products. The potential performance enhancing effects associated with these products makes them significant concern regards doping control in sports. purpose this study was investigate...

Abstract The detection of drugs in human hair samples has been performed by laboratories around the world for many years and matrix is popular disciplines, such as workplace drug testing. To date, however, not become a routinely utilised sports detection. analysis offers several potential advantages to doping control laboratories, least which are greatly extended window ease sample collection storage. This article describes development, validation, utilisation sensitive ultra‐high...

Abstract Methandienone is an anabolic‐androgenic steroid that prohibited in equine sports due to its potential performance enhancing properties. Metabolism and detection of methandienone urine have been investigated comprehensively literature; however, there a limited knowledge about metabolites plasma no information hair. Following multi‐dose oral administration two Thoroughbred horses, 17‐epimethandienone, methyltestosterone, mono‐hydroxylated, di‐hydroxylated three...

Abstract FG‐4592 is a hypoxia‐inducible factor inhibitor that has been approved for therapeutic use in some countries. This class of compounds can increase the oxygen carrying capacity blood and thus have potential to be used as performance enhancing agents sports. The purpose this study was investigate detection metabolites equine plasma mane hair following multiple dose oral administration two Thoroughbred racehorses, identify best analytical targets doping control laboratories. Urine...

Detection of testosterone and/or its pro-drugs in the gelding is currently regulated by application an international threshold for urinary 20 ng/mL. The use steroid ratios may provide a useful supplementary approach to aid differentiating between administration these steroids and unusual physiological conditions that result atypically high concentrations. In current study, ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) method was developed quantify (T)...

Selective androgen receptor modulators, SARMs, are a large class of compounds developed to provide therapeutic anabolic effects with minimal androgenic side effects. A wide range these available purchase online and thus the potential for abuse in sports. Knowledge metabolism is essential aid their detection doping control samples. In vitro models allow quick, cost-effective response where administration studies yet be carried out. this study, equine phase I non-steroidal SARMs GSK2881078,...

Abstract Boldenone (1‐dehydrotestosterone) is an exogenous anabolic‐androgenic steroid (AAS) but also known to be endogenous in the entire male horse and potentially formed by microbes voided urine, gastrointestinal tract, or feed resulting its detection urine samples. In this study, equine fecal samples were incubated presence of selected stable isotope labeled AAS precursors investigate whether microbial activity could result 1‐dehydrogenation, particular formation boldenone. Fecal matter...

AC-262536 is one of a number selective androgen receptor modulators that are being developed by the pharmaceutical industry for treatment range clinical conditions including replacement therapy. Though not available therapeutically, widely to purchase online as (illegal) supplement products. The growth- and bone-promoting effects, along with fewer associated negative side effects compared anabolic-androgenic steroids, make these compounds significant threat regard doping control in sport....

Boldenone is an anabolic-androgenic steroid that prohibited in equine sports. However, certain situations, it endogenous or believed to be formed by microbes urine, and therefore, approach for the differentiation required. Following identification of Δ1-progesterone 20(S)-hydroxy-Δ1-progesterone as potential biomarkers microbial activity, presence six steroids was investigated postrace urine castrated male horses (geldings, n = 158). In line with findings from several other species when...

Abstract Boldenone is an anabolic–androgenic steroid (AAS) that prohibited in equine sports. However, certain situations, it endogenous, potentially formed by the microbes urine. An approach to differentiation based on detection of biomarkers Δ1‐progesterone, 20(S)‐hydroxy‐Δ1‐progesterone and 20(S)‐hydroxyprogesterone was assessed, their concentrations were monitored urine untreated female horses (n = 291) alongside boldenone, boldienone, testosterone androstenedione. Using ultra‐sensitive...

Medication control and doping have been established in horse racing to ensure the integrity of sport welfare horses. This ensures that horses do not compete under influence any drugs, including omeprazole, a therapeutic medication used treat equine gastric ulcer syndrome. In this study, pharmacokinetic data were produced plasma urine following an oral administration 4 mg/kg generic buffered formulation omeprazole six Thoroughbred five daily doses determine appropriate screening limit...

Ibutamoren mesylate, or MK-0677, is an orally active, nonpeptide growth hormone secretagogue that has been developed to stimulate excretion of endogenous hormone. It evaluated for the treatment a range clinical conditions but not available therapeutically. Nonetheless, MK-0677 widely purchase online, sold as 'supplement' products. The mode action and relative ease make potential threat with regard sports doping. aim this study was investigate metabolism MK0677 in horse following vitro...

MK-0677 (ibutamoren) is an orally active non-peptide growth hormone secretagogue that binds to the ghrelin receptor stimulating secretion of endogenous hormone. It one most prevalent performance-enhancing compounds currently available online and potentially subject abuse both in human equine sports. The aim current study was investigate whether it could be detected hair following oral administration mesylate a Thoroughbred racehorse. its O-dealkylated metabolite were extracted using existing...

Abstract Xylazine is widely used worldwide as a short‐acting sedative in general equine and racing practice. In the UK, although it has legitimate use during training, anti‐doping rules state prohibited substance on race day. The aim of study was to produce detection time (DT) better inform European veterinary surgeons so that xylazine can be appropriately under regulatory rules. Previous publications have various limitations pertaining analysis method, particularly for plasma limited length...

Oxandrolone is an anabolic-androgenic steroid with favourable anabolic to androgenic ratio, making it effective agent less side effects. Although its metabolism has been studied in humans, phase I and II not previously reported the horse. The purpose of this study was investigate vitro oxandrolone (using both equine liver microsomes S9) vivo following oral administration (three daily doses 50 mg a single Thoroughbred horse), using gas liquid chromatography-mass spectrometry techniques....

The effective analysis of anabolic-androgenic steroids in urine usually requires a suitable deconjugation method for the phase II metabolites such as sulphates and glucuronides. Acid hydrolysis using methanolysis is one adopted that efficiently rapidly cleaves both glucuronides contemporaneously. formation artefactual by-products known disadvantage this harsh method. However, possible promotion deuterium-hydrogen exchange isotopically labelled internal standards has received little attention...

Abstract Calcium dobesilate (CD) is a synthetic venoactive drug used in veterinary medicine to treat equine navicular disease. Etamsylate haemostatic agent horses for the treatment of exercise‐induced pulmonary haemorrhage. Both etamsylate and CD dissociate circulatory system with 2,5‐HBSA as active drug. The aim research was be able provide detection time (DT) advice from pharmacokinetic (PK) studies Thoroughbred better inform trainers, their surgeons, prescribing these substances...

YK-11 is a steroidal selective androgen receptor modulator, compound class prohibited in both equine racing and human sports because of their potentially performance enhancing properties. easily accessible via internet-based supplement vendors making this possible candidate for doping; however, its phases I II metabolism has not yet been reported the horse. The purpose study was to investigate vivo metabolites urine plasma following oral administration with three daily doses 50 mg two...

Abstract The use of testosterone and its pro‐drugs, such as dehydroepiandrosterone (DHEA), is currently regulated in horseracing by the application international thresholds. However, additional steroidomic approaches, steroid ratios, to distinguish overall adrenal stimulation from drug administrations an equine biological passport for longitudinal profiling individual animals could be advantageous doping testing. Thus, DHEA concentrations related ratios (testosterone [T] epitestosterone [E])...

SR-9009 is a synthetic compound widely available to purchase online as 'supplement' products due its potential performance-enhancing effects, presenting significant threat with regard doping control in sport. In vitro metabolism equine liver microsomes was performed identify targets for detection of SR-9009. Six metabolites were identified, the most abundant consisting N-dealkylated (M1-M3). The addition identified high-resolution accurate mass databases resulted positive finding metabolite...

Abstract S‐23 is an arylpropionamide selective androgen receptor modulator that has been investigated in animal models for use as a male hormonal contraceptive but not yet available therapeutically. alongside other modulators (SARMs) to purchase online via uncontrolled sites, sold supplement products. It detected several human doping cases, highlighting the importance of identifying best analytical targets equine control. The purpose this study was investigate detection and its phase I...