Pharmaceuticals in equine medicine encompass a wide range of drugs and therapeutic agents used to treat various conditions in horses. These substances include analgesics, anti-inflammatories, antibiotics, sedatives, and anthelmintics, among others. Each class of pharmaceuticals is designed to address specific health issues, such as pain management, infection control, or parasitic infestations. The pharmacokinetics and pharmacodynamics of these drugs can vary significantly between horses and other species, necessitating careful consideration of dosage and administration methods. This page compiles peer-reviewed research studies and scholarly articles that explore the development, efficacy, safety, and regulatory aspects of pharmaceuticals used in equine healthcare.
Crotch-Harvey L, Thomas LA, Worgan HJ, Douglas JL, Gilby DE, McEwan NR.Anthelmintics are used as anti-worming agents. Although known to affect their target organisms, nothing has been published regarding their effect on other digestive tract organisms or on metabolites produced by them. The current work investigated effects of fenbendazole, a benzimidazole anthelmintic, on bacteria and ciliates in the equine digestive tract and on and their major metabolites. Animals receiving anthelmintic treatment had high faecal egg counts relative to controls. Analysis was performed over two weeks, with temporal differences detected in bacterial populations but with no other ...
Wong JKY, Choi TLS, Kwok KY, Lei ENY, Wan TSM.Equine hair is becoming an increasingly popular biological matrix for doping control of horse sports; one of the reasons for this is the significantly longer detection window hair can offer. Hair analysis opens up the opportunity for longitudinal monitoring of drug exposure which would otherwise not be possible with the more traditional and common biological matrices, such as urine and blood. As such, there is a need for more multi-target screening methods covering a broad range of prohibited substances in equine hair at the required sensitivities for equine doping control. This paper describe...
Wenzel R, Major D, Hesp K, Doble P.Regulating authorities in the racing industry have restricted the administration of potentially performance enhancing cobalt salts to horses. There are severe penalties for trainers presenting horses with elevated urine cobalt concentrations, and compliance is ensured via analysis of total urinary cobalt at thresholds of 100 μg/L. When cobalt is present as part of the cobalamin molecule it is not considered performance enhancing. This paper demonstrates that a horse can excrete a significant proportion of a commercially available vitamin B12 injection in urine without metabolic modification...
Emmerich IU.In 2017, no new active pharmaceutical ingredients were released on the German market for horses or food-producing animals. Four established veterinary active pharmaceutical ingredients became available for additional species: the ectoparasitic Fluralaner (Exzolt®) of the isoxazoline group was additionally authorized for chickens, the macrolide antibiotics Gamithromycin (Zactran®) and Tulathromycin (Draxxin®) for sheep and the nonsteroidal anti-inflammatory drug Tolfenamic Acid (Tolfedol®) from the fenamate group for cattle and pigs. Additionally, one drug with a new combination of active i...
Kim Y, Seo C, Oh S, Kwak J, Jung S, Sin E, Kim H, Ji M, Lee HS, Park HJ, Lee G, Yu J, Kim M, Lee W, Paik MJ.Loxoprofen is a non-steroidal anti-inflammatory drug of the 2-arylpropionic acid type, which has used to treat musculoskeletal disorders in the horse racing industry. However, it has also used illicitly to mask clinical signs of inflammation and pain in racehorses. Thus, its accurate analysis has become an important issue in horse doping laboratories. In this study, an analytical method of loxoprofen was developed as tert-butyldimethylsilyl (TBDMS) derivative by gas chromatography-mass spectrometry (GC-MS). Characteristic fragment ions of [M-15], [M-57], and [M-139] permitted the accurate and ...
Gray B, Viljanto M, Menzies E, Vanhaecke L.The detection of drugs in human hair samples has been performed by laboratories around the world for many years and the matrix is popular in disciplines, such as workplace drug testing. To date, however, hair has not become a routinely utilised matrix in sports drug detection. The analysis of hair samples offers several potential advantages to doping control laboratories, not least of which are the greatly extended detection window and the ease of sample collection and storage. This article describes the development, validation, and utilisation of a sensitive ultra-high performance liquid chro...
Waraksa E, Wójtowicz-Zawadka M, Kwiatkowska D, Jarek A, Małkowska A, Wrzesień R, Namieśnik J.A novel assay for the simultaneous determination of ibuprofen (IBU) and its four probable metabolites, 1-hydroxyibuprofen (1-OH IBU), 2-hydroxyibuprofen (2-OH IBU), 3-hydroxyibuprofen (3-OH IBU) and carboxyibuprofen (CBX IBU) in equine urine samples with the application of Gas Chromatography-Electron Ionization-Mass Spectrometry (GC-EI-MS) has been developed and elaborated. The new approach for sample preparation including minimizing matrix effects by the application of weak cation exchange solid-phase extraction together with strong cation exchange solid-phase extraction has been applied. The...
Waters LJ, Hanrahan JP, Tobin JM, Finch CV, Parkes GMB, Ahmad SA, Mohammad F, Saleem M.Three mesoporous silica excipients (Syloid® silicas AL-1 FP, XDP 3050 and XDP 3150) were formulated with a model drug known for its poor aqueous solubility, namely phenylbutazone, in an attempt to enhance the extent and rate of drug dissolution. Although other forms of mesoporous silica have been investigated in previous studies, the effect of inclusion with these specific Syloid® silica based excipients and more interestingly, with phenylbutazone, is unknown. This work reports a significant enhancement for both the extent and rate of drug release for all three forms of Syloid® silica at a ...
Soma LR, Robinson MA, You Y, Boston RC, Rudy J.Compartmental models were used to investigate the pharmacokinetics of intravenous (i.v.), oral (p.o.), and topical (TOP) administration of dimethyl sulfoxide (DMSO). The plasma concentration-time curve following a 15-min i.v. infusion of DMSO was described by a two-compartment model. Median and range of alpha (t ) and beta (t ) half-lives were 0.029 (0.026-0.093) and 14.1 (6.6-16.4) hr, respectively. Plasma concentration-time curves of DMSO following p.o. and TOP administration were best described by one-compartment absorption and elimination models. Following the p.o. administration, median a...
Hansson A, Knych H, Stanley S, Berndtson E, Jackson L, Bondesson U, Thevis M, Hedeland M.LGD-4033 has been found in human doping control samples and has the potential for illicit use in racehorses as well. It belongs to the pharmacological class of selective androgen receptor modulators (SARMs) and can stimulate muscle growth, much like anabolic steroids. However, SARMs have shown superior side effect profiles compared to anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors. The purpose of this study was to investigate the metabolites formed from LGD-4033 in the horse in order to find suitable analytical ...
Müntener CR, Müntener C, Kupper J, Naegeli H, Gassner B.A total of 253 reports of adverse reactions to veterinary medicinal products were received during the year 2016 representing a decrease of 13% compared to the previous year (292 reports). The majority of the reports described reactions affecting companion animals (178 dogs and 32 cats) as well as cattle (17 reports) and horses (10 reports). Most of the reactions reported were linked to the use of antiparasitics (145 reports), hormone products (26 reports) and antiinfectives (10 reports). 32 reports were generated from consultations with Tox Info Suisse in Zürich and involved mainly the excess...
Broux B, De Clercq D, Decloedt A, Vera L, Devreese M, Gehring R, Croubels S, van Loon G.Arrhythmias in horses may require long-term anti-arrhythmic therapy. Unfortunately, oral anti-arrhythmic drugs for use in horses are currently scarce. In human patients and small animals, sotalol, a β-blocker with class III anti-arrhythmic properties, is often used for long-term treatment. Objective: To determine the pharmacokinetics of sotalol at multiple oral dosages in unfasted horses, as well as the effects on electro- and echocardiographic measurements, right atrial and ventricular monophasic action potential (MAP) and effective refractory period (ERP). Methods: Placebo controlled, doubl...
Yuan M, Breitkopf SB, Asara JM.Horse urine is easily collected and contains molecules readily measurable using mass spectrometry that can be used as biomarkers representative of health, disease or drug tampering. This study aimed at analyzing microliter levels of horse urine to purify, identify and quantify proteins, polar metabolites and non-polar lipids. Urine from a healthy 12 year old quarter horse mare on a diet of grass hay and vitamin/mineral supplements with limited pasture access was collected for serial-omics characterization. The urine was treated with methyl tert-butyl ether (MTBE) and methanol to partition into...
Mizobe F, Nomura M, Kato T, Nambo Y, Yamada K.Problems associated with the proximal metacarpal region, such as an osseous injury associated with tearing of Sharpey's fibers or an avulsion fracture of the origin of the suspensory ligament (OISL), are important causes of lameness in racehorses. In the present study, four Thoroughbred racehorses (age range, 2-4 years) were diagnosed as having forelimb OISL and assessed over time by using standing magnetic resonance imaging (sMRI). At the first sMRI examination, all horses had 3 characteristic findings, including low signal intensity within the trabecular bone of the third metacarpus on T1-we...
Joré C, Loup B, Garcia P, Paris AC, Popot MA, Audran M, Bonnaire Y, Varlet-Marie E, Bailly-Chouriberry L.Erythropoiesis Stimulating Agents (ESAs) were developed for therapeutic purposes to stimulate red blood cell (RBC) production. Consequently, tissue oxygenation is enhanced as athlete's endurance and ESAs misuse now benefits doping. Our hypothesis is that most of ESAs should have similar mechanisms and thus have the same effects on metabolism. Studying the metabolome variations could allow suspecting the use of any ESAs with a single method by targeting their effects. In this objective, a metabolomic study was carried out on 3 thoroughbred horses with a single administration of 4.2μg/kg of Mir...
Gordon E, Sandquist C, Cebra CK, Heidel J, Poulsen K, Schlipf JW.To evaluate whether topical ocular application of 1% morphine sulfate would change corneal sensitivity and to identify the duration of action. Methods: Eight healthy adult horses. Methods: Corneal touch threshold (CTT) was measured in the center of one randomly selected eye of each horse by Cochet-Bonnet esthesiometer (Luneau Cochet-Bonnet Esthesiometer; Western Ophthalmics, Lynnwood, WA, USA). Immediately following baseline CTT measurement, 0.3 ml of 1.0% preservative-free morphine sulfate (Morphine Sulfate 25 mg/ml Preservative-free; Hospira, Lake Forest, IL, USA) (3 mg) was applied to th...
Wang J, Zhao T, Kong J, Peng H, Lv P, Li J, Cao X, Zhang S.Vitacoxib is an imidazole derivative and the novel COX-2 selective inhibitor to be marketed for veterinary use as nonsteroidal anti-inflammatory drugs. No analytical assay to quantify vitacoxib in equine plasma samples has been published to date. In the current study, we aim to develop and validate a brief, quick and sensitive UPLC-MS/MS method for quantification of vitacoxib in equine plasma samples. Plasma samples were precipitated with methyl tert-butyl ether. The Phenomenex column (Kinetex 50×2.1mm i.d. particle size=2.6μm, C18, 100Å) at 25°C was used in chromatographic separation with...
Shin HD, Suh JH, Kim J, Cho HD, Lee SD, Han KS, Wang Y, Han SB.A high throughput method for simultaneous screening of anabolic steroids and their metabolites (4-esterendione, trenbolone, boldenone, oxandrolone, nandrolone, methandrostenolone, testosterone, 1-androstendione, ethisterone, normethandrolone, methyltestosterone, 16β-Hydroxystanozolol, epitestosterone, bolasterone, norethandrolone, danazol, stanozolol and androstadienone) in equine urine by online turbulent flow extraction coupled with liquid chromatography-tandem mass spectrometry was developed. The use of turbulent flow chromatography could simplify pretreatment of horse urine, which has com...
McElligott EM, Sommardahl CS, Cox SK.OBJECTIVE To determine the pharmacokinetics of chloramphenicol base after PO administration at a dose of SO mg/kg (22.7 mg/lb) in adult horses from which food was not withheld. DESIGN Prospective crossover study. ANIMALS 5 adult mares. PROCEDURES Chloramphenicol base (SO mg/kg) was administered PO to each horse, and blood samples were collected prior to administration (0 minutes) and at 5, 10, 15, and 30 minutes and 1, 2, 4, 8, and 12 hours thereafter. Following a washout period, chloramphenicol sodium succinate (25 mg/kg [11.4 mg/lb]) was administered IV to each horse, and blood samples were ...
Wong JKY, Leung DKK, Curl P, Schiff PJ, Lam KKH, Wan TSM.The detection of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione in a urine sample collected from a gelding having been treated with testosterone (500 mg 'Testosterone Suspension 100', single dose, injected intramuscularly) in 2009 led the authors' laboratory to suspect that these 'testicular' steroids could be minor metabolites of testosterone in geldings. Administration trials on six castrated horses with Testosterone Suspension 100 confirmed that low levels of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione could indeed be detected ...
Wong JKY, Kwok WH, Chan GHM, Choi TLS, Ho ENM, Jaubert M, Bailly-Chouriberry L, Bonnaire Y, Cawley A, Ming Williams H, Keledjian J, Brooks L....Acadesine, 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, commonly known as AICAR, is a naturally occurring adenosine monophosphate-activated protein kinase (AMPK) activator in many mammals, including humans and horses. AICAR has attracted considerable attention recently in the field of doping control because of a study showing the enhancement of endurance performance in unexercised or untrained mice, resulting in the term 'exercise pill'. Its use has been classified as gene doping by the World Anti-Doping Agency (WADA), and since it is endogenous, it may only be possible to control del...
Emmerich IU.In 2016, only one newly developed active pharmaceutical ingredient for horses and food-producing animals was released on the German market for veterinary drug products. The immunomodulator Pegbovigrastim is now available as an injection solution for cattle (Imrestor). Four established veterinary active pharmaceutical ingredients are available for further species: the ectoparasitic Amitraz (Apitraz) from the triazapentadiene group was additionally authorized for honeybees, the expectorant Bromhexine (Exflow Vet) for chickens, turkeys and ducks and the macrolide antibiotic Gamithromycin (Zactran...
Wilson KE, Davis JL, Crisman MV, Kvaternick V, Zarabadipour C, Cheramie H, Hodgson DR.The purpose of this study was to determine the pharmacokinetic profile of intravenous firocoxib in neonatal foals. Six healthy foals were administered 0.09 mg/kg firocoxib intravenously once a day for 7 days. Blood was collected for plasma firocoxib analysis using high-performance liquid chromatography with fluorescence detection at times 0 (day 1 of study only) and 0.08, 0.25, 1, 2, 4, 6, 8, 16 and 24 hr on dose numbers 1, 5 and 7. Blood was also collected immediately prior to doses 3, 4, 5 and 7. Final samples were collected at 36, 48, 72 and 96 hr following the final dose. Noncompartmen...
Fragkaki AG, Kioukia-Fougia N, Kiousi P, Kioussi M, Tsivou M.The artificial increase of the physical capability of horses using drugs is well known in racing and other equine sports. Both illicit and therapeutic substances are regarded as prohibited substances in competition in most countries. Some countries make distinctions for a few, specific drugs which are, however, allowed for use in other countries. The primary objective in the case of doping control is the detection of any trace of drug exposure, either parent drug or any of its metabolites, using the most powerful analytical methods which are generally based on chromatographic/mass spectrometri...
Lee W, Ko BJ, Sim YE, Suh S, Yoon D, Kim S.Urine was most commonly used biological sample in drug test. To create a false-negative test result, some drug abusers were reported to submit animal urine instead of their own. So, the purpose of this study was to compare and differentiate human from animal urine (Rat 370, Pig 12, Horse 10, Cat 8, Dog 13, Cow 10, Monkey 10) samples through the uses of quantitative 1H-NMR and to find biomarkers that can be used for the discrimination of human urine from animal urine. The 1H-NMR spectroscopy was employed and metabolomic analysis with multivariate statistics was carried out. Human urine samples ...
Kollias-Baker C, Maxwell L, Stanley S, Boone T.Cocaine is a naturally occurring alkaloid that is commonly abused by human-beings for its psychostimulatory effects. Occasionally, very small concentrations (i.e. <100 ng/mL) of the primary cocaine metabolite, benzoylecgonine (BZE) have been detected in urine collected from horses competing in athletic events. In this study urine samples, collected from four horses following the administration of 2.5 and 20 mg of cocaine sublingually and 50 mg of cocaine intravenously, were analyzed for the presence of cocaine and/or its metabolites by enzyme-linked immunosorbent assay (ELISA) and gas chrom...
Chicca J, Cazeault NR, Rus F, Abraham A, Garceau C, Li H, Atwa SM, Flanagan K, Soto ER, Morrison MS, Gazzola D, Hu Y, Liu DR, Nielsen MK, Urban JF....Bacillus thuringiensis (Bt) is a Gram-positive soil bacterium that is widely and safely applied in the environment as an insecticide for combatting insect pests that damage crops or are disease vectors. Dominant active ingredients made by Bt are insect-killing crystal (Cry) proteins released as crystalline inclusions upon bacterial sporulation. Some Bt Cry proteins, e.g., Cry5B (formally Cry5Ba1), target nematodes (roundworms) and show exceptional promise as anthelmintics (cures for parasitic nematode diseases). We have recently described inactivated bacteria with cytosolic crystal(s) (IBaCC) ...
Rebhun WC, Tennant BC, Dill SG, King JM.Renal toxicosis attributable to vitamin K3 (menadione sodium bisulfite) was suspected in 5 young adult horses in which acute renal failure developed following parenteral administration of vitamin K3 at the manufacturers' recommended dosages. Renal disease was subsequently induced experimentally in 5 of 6 horses by administration of vitamin K3 at manufacturers' recommended dosages. Signs of renal disease in the clinical patients as well as in the horses treated experimentally included renal colic, hematuria, azotemia, and electrolyte abnormalities consistent with acute renal failure. Two clinic...
Trevisiol S, Moulard Y, Delcourt V, Jaubert M, Boyer S, Tendon S, Haryouli H, Taleb W, Caroff M, Chabot B, Drif L, André F, Garcia P, Loup B....According to international sport institutions, the use of peroxisome proliferator activated receptor (PPAR)-δ agonists is forbidden at any time in athlete career due to their capabilities to increase physical and endurance performances. The (PPAR)-δ agonist GW501516 is prohibited for sale but is easily available on internet and can be used by cheaters. In the context of doping control, urine is the preferred matrix because of the non-invasive nature of sampling and providing broader exposure detection times to forbidden molecules but often not detected under its native form due to the organi...
Popot MA, Garcia P, Hubert C, Bolopion A, Bailly-Chouriberry L, Bonnaire Y, Thibaud D, Guyonnet J.Tiludronate is a non-nitrogen-containing biphosphonate drug approved in equine veterinary medicine for the treatment of navicular disease and bone sparvin in horse. Its hydrophilic properties and its strong affinity for the bone have made the control of its use quite difficult. After an initial step of method development in plasma and urine, due to a strong matrix effect and erratic detection in urine, the final method development was conducted in plasma. After addition of (3-trifluoromethylphenyl) thiomethylene biphosphonic acid as internal standard, automated sample preparation consisted of ...
Broux B, De Clercq D, Decloedt A, Vera L, Devreese M, Gehring R, Croubels S, van Loon G.Arrhythmias in horses may require long-term anti-arrhythmic therapy. Unfortunately, oral anti-arrhythmic drugs for use in horses are currently scarce. In human patients and small animals, sotalol, a β-blocker with class III anti-arrhythmic properties, is often used for long-term treatment. Objective: To determine the pharmacokinetics of sotalol at multiple oral dosages in unfasted horses, as well as the effects on electro- and echocardiographic measurements, right atrial and ventricular monophasic action potential (MAP) and effective refractory period (ERP). Methods: Placebo controlled, doubl...
In the present study a general screening protocol was developed to detect prohibited substances and metabolites for doping control purposes in equine sports. It was based on the establishment of a unified sample preparation and on the combined implementation of liquid and gas chromatographic MS analysis. The sample pretreatment began with two parallel procedures: enzymatic hydrolysis of sulfate and glucuronide conjugates, and methanolysis of the 17β-sulfate steroid conjugates. The extracts were treated for LC-TOF-MS, GC-HRMS and GC-MS assays. The majority of the prohibited substances were ide...
Malone ED.Many compounds are being investigated for the control of symptoms of osteoarthritis in people and animals. Ideally, treatment should include analgesia, inflammation control, and chondroprotection. With further progress in this area, combination therapies tailored to the needs of the individual animal should enable us to maximize efficacy and minimize side effects. Only a few of the newer therapies and pharmaceutic agents have been investigated in the horse, however. With more rigorous investigation, they may be determined to be ineffective or unsafe. Meanwhile, as much information should be ga...
Spyridaki MH, Lyris E, Georgoulakis I, Kouretas D, Konstantinidou M, Georgakopoulos CG.Xylazine and its main metabolites were detected in equine urine after a single-dose intravenous administration of 0.98 and 1.01 mg/kg body weight xylazine, respectively, in two horses, in order to be used for equine doping control routine analysis. The urine levels of the parent drug and its metabolites were determined using gas chromatography-mass spectrometry (GC-MS). Xylazine is metabolised rapidly, down to a concentration level of about 1.0 microg/ml after 1-3h administration. Seven metabolites were identified in urine. 4-Hydroxy-xylazine, the major metabolite, could be traced for 25 h and...
Wang J, Xue J, Kong J, Li J, Zhang S, Cao X.The pharmacokinetic properties of vitacoxib have not been established completely; current dosage recommendations are based on clinical experiences. The primary objective of this study was to describe plasma concentrations and characterize the pharmacokinetics of vitacoxib formulation following oral administrations in horses. Also, the effect of the state of stomach contents on the absorption of vitacoxib was investigated in fed/fasted horses. Blood samples were collected prior to and at various times up to 72 hr post-administration. Drug concentrations were measured using ultra high-performan...
Rudolph W, Remane D, Wissenbach DK, Peters FT.1. Ergopeptine alkaloids like ergovaline and ergotamine are suspected to be associated with fescue toxicosis and ergotism in horses. Information on the metabolism of ergot alkaloids is scarce, especially in horses, but needed for toxicological analysis of these drugs in urine/feces of affected horses. The aim of this study was to investigate the metabolism of ergovaline, ergotamine, ergocristine, and ergocryptine in horses and comparison to humans. 2. Supernatants of alkaloid incubations with equine and human liver S9 fractions were analyzed by reversed-phase liquid-chromatography coupled to h...
Furr M, Kennedy T.Toltrazuril 5% suspension (Baycox, Bayer Canada, Ontario, Canada) was administered to six adult horses followed by blood collection and assay to determine the concentration of toltrazuril and its principal metabolites, toltrazuril sulfone and toltrazuril sulfoxide. From this data, the maximum concentration (C(max)), elimination half-life (T 1/2), and mean residence times of the plasma were determined from standard pharmacokinetic formulas. After a single oral dose of 10 mg/kg body weight a rapid absorption was found, with a mean peak serum concentration of 11.17 mg/L at 18 hours. Elimination w...
Ishii H, Shibuya M, Leung GN, Nozawa S, Yamashita S, Yamada M, Kushiro A, Kasashima Y, Okada J, Kawasaki K, Kijima-Suda I.GW1516 is a peroxisome proliferator-activated receptor-δ (PPAR-δ) agonist that is banned in horseracing and equestrian sports. Long-term detection and longitudinal distribution of GW1516 in the mane of a horse are reported for the first time and this hair analysis could prolong the detection window of GW1516 for doping control. Methods: Mane hairs were divided into three segments (0-7, 7-15, and >15 cm from the cut end) and completely pulverized and homogenized for analysis. The pulverized hair samples were extracted with methanol followed by further purification and the extracts were a...
Black HE.Non-steroidal anti-inflammatory drugs represent the most heavily prescribed and used class of drugs in human medicine. Most are derivatives of either salicylates, propionic acid, indoleacetic acid, anthranilic acid, pyrazolone, or oxicams. They depress the synthesis of prostaglandins from arachidonic acid by reversible inhibition of the enzyme cyclooxygenase. In the kidney, prostaglandins PGE2 and PGI2 modulate the vasoconstrictor effects of angiotensin II, norepinephrine, and vasopressin. In the presence of volume contraction, anesthesia, or disease states associated with high levels of these...
Wilson KE, Davis JL, Crisman MV, Kvaternick V, Zarabadipour C, Cheramie H, Hodgson DR.The purpose of this study was to determine the pharmacokinetic profile of intravenous firocoxib in neonatal foals. Six healthy foals were administered 0.09 mg/kg firocoxib intravenously once a day for 7 days. Blood was collected for plasma firocoxib analysis using high-performance liquid chromatography with fluorescence detection at times 0 (day 1 of study only) and 0.08, 0.25, 1, 2, 4, 6, 8, 16 and 24 hr on dose numbers 1, 5 and 7. Blood was also collected immediately prior to doses 3, 4, 5 and 7. Final samples were collected at 36, 48, 72 and 96 hr following the final dose. Noncompartmen...
Legere RM, Taylor DR, Davis JL, Bello K, Parker C, Judd RL, Wooldridge AA.Chronic insulin dysregulation is challenging to manage with pharmaceuticals in horses. Pioglitazone improves insulin sensitivity in humans, and the pharmacokinetics of pioglitazone have been evaluated in horses. The objectives of this study were to assess the pharmacodynamic effects of oral pioglitazone on morphometric parameters, hepatic enzyme activity and function, adipokines, and enteroinsular response to oral sugar. A prospective pilot study was performed using fifteen adult equids (8 ponies, 7 horses) to evaluate the effects of short-term pioglitazone administration (2 mg/kg PO q 24 hou...
Ishii H, Shibuya M, So YM, Wong JKY, Ho ENM, Kusano K, Sone Y, Kamiya T, Wakuno A, Ito H, Miyata K, Yamada M, Leung GN.IOX4 is a hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitor, which was developed for the treatment of anemia by exerting hematopoietic effects. The administration of HIF-PHD inhibitors such as IOX4 to horses is strictly prohibited by the International Federation of Horseracing Authorities and the Fédération Équestre Internationale. To the best of our knowledge, this is the first comprehensive metabolic study of IOX4 in horse plasma and urine after a nasoesophageal administration of IOX4 (500 mg/day, 3 days). A total of four metabolites (three mono-hydroxylated IOX4 and one ...
Kwok WH, Ho EN, Lau MY, Leung GN, Wong AS, Wan TS.In recent years, there has been an ongoing focus for both human and equine doping control laboratories on developing detection methods to control the misuse of peptide therapeutics. Immunoaffinity purification is a common extraction method to isolate peptides from biological matrices and obtain sufficient detectability in subsequent instrumental analysis. However, monoclonal or polyclonal antibodies for immunoaffinity purification may not be commercially available, and even if available, such antibodies are usually very costly. In our study, a simple mixed-mode anion exchange solid-phase extra...
Lees P, Higgins AJ, Sedgwick AD, May SA.The development of reproducible models of acute inflammation in which inflammatory heat is easily quantified and from which inflammatory exudate is readily harvested has facilitated studies in the horse of the actions of steroids and non-steroidal anti-inflammatory drugs (NSAIDS). Blockade of the synthesis of eicosanoids and suppression of inflammatory heat by clinical dose rates of NSAIDS suggests a causal link between the two events and provides further evidence for a role of these compounds in acute equine inflammation. The tendency for enolic and carboxylic acids NSAIDS to accumulate in in...
Tevell Aberg A, Olsson C, Bondesson U, Hedeland M.This paper describes a study where the metabolism of the non-steroidal anti-inflammatory drug meloxicam was investigated in six horses and in the filamentous fungus Cunninghamella elegans. The metabolites identified were compared between the species, and then the fungus was used to produce larger amounts of the metabolites for future use as reference material. C. elegans proved to be a good model of phase I meloxicam metabolism in horses since all four metabolites found were the same in both species. Apart from the two main metabolites, 5'-hydroxymethylmeloxicam and 5'-carboxymeloxicam, a seco...
Schediwy M, Mevissen M, Demuth D, Kupper J, Naegeli H.This retrospective study evaluated the frequency, etiology, therapy and prognosis of animal poisoning registered from 2003 to 2012. The relevant cases reported to the Swiss Toxicological Information Center (STIC) were compared with those from previously examined periods. Human medicines not approved for animals and pesticides represented the most common causes of poisoning in dogs. Novel cases occurred as a consequence of the exposure of dogs to ricinus fertilizers, grape residues from wineries, pepper lachrymatory spray and dry bouillon. Cats are still freequently poisoned by pyrethroid drugs...
