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.
Daniels SP, Leng J, Swann JR, Proudman CJ.Anthelmintic treatment is a risk factor for intestinal disease in the horse, known as colic. However the mechanisms involved in the onset of disease post anthelmintic treatment are unknown. The interaction between anthelmintic drugs and the gut microbiota may be associated with this observed increase in risk of colic. Little is known about the interaction between gut microbiota and anthelmintics and how treatment may alter microbiome function. The objectives of this study were: To characterise (1) faecal microbiota, (2) feed fermentation kinetics in vitro and (3) metabolic profiles following m...
Pennati A, Apfelbeck T, Brounts S, Galipeau J.Mammalian platelets participate in the immediate tissue injury response by initiating coagulation and further promoting tissue injury mitigation and repair. The latter properties are deployed following platelet release of presynthetized morphogens, cytokines, and growth and chemotactic factors, which launch a tissue regenerative, angiogenic, and anti-inflammatory program. Several blood-derived biologic products, like platelet-rich plasma (PRP) and platelet lysate (PL), are currently on the market to allow proper healing and tissue regeneration. However, not all growth factors are released from...
VanderBroek AR, Engiles JB, Kästner SBR, Kopp V, Verhaar N, Hopster K.Strangulating small intestinal lesions in the horse have increased morbidity and mortality compared to nonstrangulating obstructions due to mucosal barrier disruption and subsequent endotoxaemia. Objective: To investigate protective effects of dexmedetomidine on small intestinal ischaemia-reperfusion injury in the horse. Methods: Randomised, controlled, experimental study. Methods: Eighteen systemically healthy horses were randomly assigned to three groups: control, preconditioning, and post-conditioning. During isoflurane anaesthesia, complete ischaemia was induced in a 1-m segment of jejunum...
So YM, Wong JKY, Choi TLS, Prabhu A, Stewart B, Farrington AF, Robinson P, Wan TSM, Ho ENM.This paper describes the studies of the in vitro biotransformation of two selective androgen receptor modulators (SARMs), namely, RAD140 and S-23, and the in vivo metabolism of RAD140 in horses using ultra-high performance liquid chromatography-high resolution mass spectrometry. in vitro metabolic studies of RAD140 and S-23 were performed using homogenised horse liver. The more prominent in vitro biotransformation pathways for RAD140 included hydrolysis, hydroxylation, glucuronidation and sulfation. Metabolic pathways for S-23 were similar to those for other arylpropionamide-based SARMs. The a...
Shihadih DS, Harris TR, Kodani SD, Hwang SH, Lee KSS, Mavangira V, Hamamoto B, Guedes A, Hammock BD, Morisseau C.The veterinary pharmacopeia available to treat pain and inflammation is limited in number, target of action and efficacy. Inhibitors of soluble epoxide hydrolase (sEH) are a new class of anti-inflammatory, pro-resolving and analgesic drugs being tested in humans that have demonstrated efficacy in laboratory animals. They block the hydrolysis, and thus, increase endogenous concentrations of analgesic and anti-inflammatory signaling molecules called epoxy-fatty acids. Here, we screened a library of 2,300 inhibitors of the sEH human against partially purified feline, canine and equine hepatic sEH...
Ricord M, Andrews FM, Yñiguez FJM, Keowen M, Garza F, Paul L, Chapman A, Banse HE.Phenylbutazone is commonly prescribed for treatment of various painful or inflammatory disorders in horses, but is associated with gastrointestinal (GI) adverse effects. Anecdotally, many practitioners prescribe omeprazole concurrently with phenylbutazone to reduce development of equine gastric ulcer syndrome (EGUS), but the efficacy and safety of this practice remains unknown. Objective: To evaluate the effect of omeprazole on phenylbutazone-induced equine glandular gastric disease (EGGD) and equine squamous gastric disease (ESGD). Methods: Randomised block experimental design. Methods: Twent...
Ishii H, Leung GN, Yamashita S, Yamada M, Kushiro A, Kasashima Y, Okada J, Kawasaki K, Kijima-Suda I.GW1516 is a peroxisome proliferator-activated receptor-δ agonist in the class of hormones and metabolic modulators. The use of GW1516 is banned in both horseracing and equestrian competitions. To the best of our knowledge, this is the first metabolic study of GW1516 in horses. Methods: After protein precipitation of pre- and post-administration plasma GW1516 samples, the supernatants were analyzed using liquid chromatography/electrospray ionization Q-Exactive high-resolution mass spectrometry to detect GW1516 and its metabolites. Monoisotopic ions of GW1516 and its metabolites were monitored ...
Knych HK, Finno CJ, Baden R, Arthur RM, McKemie DS.The in vivo metabolism and pharmacokinetics of flunixin meglumine and phenylbutazone have been extensively characterized; however, there are no published reports describing the in vitro metabolism, specifically the enzymes responsible for the biotransformation of these compounds in horses. Due to their widespread use and, therefore, increased potential for drug-drug interactions and widespread differences in drug disposition, this study aims to build on the limited current knowledge regarding P450-mediated metabolism in horses. Drugs were incubated with equine liver microsomes and a panel of r...
Bermingham E, Davis JL, Whittem T.The goal of this editorial is to discuss best practice design, execution and reporting of a pharmacokinetic (PK) study in horses. Our target readers are clinicians who plan to perform this type of research, in a field, clinic or research setting but we also hope that this article might help readers of such work to appraise the articles and understand the quality of the studies. Our emphasis will be on appropriate study design and analytical method, drug and drug formulation choice and route of administration, animal choice, sample collection, storage and shipping, and reporting, rather than th...
Leung DKK, Wong ASY, Zhou QL, Wan TSM, Ho ENM.A non-target variable Data Independent Acquisition (vDIA) workflow based on accurate mass measurements using a Q Exactive OrbiTrap is presented for the first time for equine doping control testing. The vDIA workflow uses a combination of MS1 events (1 to 2) and multiple vDIA events to cover the analytes of interest. The workflow basically captures a digital image of a sample allowing all relevant MS1 and MS2 data to be recorded. In theory, the workflow can accommodate an unlimited number of analytes as long as they are amenable to the sample extraction protocol and fall within the mass limits ...
Garcia P, Pinètre J, Morel S, Jaubert M, Deruy X, Perot I, Delcourt V, Loup B, Popot MA, Bailly-Chouriberry L.Bisphosphonates are prohibited drugs according to Article 6 of the International Agreement on Breeding, Racing and Wagering of the International Federation of Horseracing Authorities (IFHA) and the International Equestrian Federation (FEI). These compounds are used for the treatment of lameness, navicular and bone diseases in horses and are divided into two groups: non-nitrogen-containing bisphosphonate drugs (e.g. clodronic acid) and nitrogen-containing bisphosphonate drugs (e.g. zoledronic acid). Their hydrophilic properties and the high affinity for the bone matrix make the control of their...
Schwarz B, Ihry P.A 26-year-old pony mare (ca. 180 kg bodyweight) was presented as an emergency because it had erroneously received 110 times its standard dose of pergolide (Prascend) per os approximately 4 hours earlier. Clinical examination initially was normal except tachycardia of 52 beats/min. The pony was treated symptomatically with paraffin oil and activated charcoal per nasogastric tube to prevent further systemic absorption and accelerate intestinal excretion of the pergolide. Furthermore, the pony received 400 mg of dopamine antagonist azaperone (Stresnil) intramuscularly (i.m.) followed by 80 mg...
Göktaş EF, Kabil E, Arıöz F.Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used in therapeutic doses in human and veterinary medicine for the treatment of inflammation, pain, and fever. A method for the simultaneous determination of nine NSAIDs, known as therapeutic prohibited substances, in equine urine was developed and fully validated according to the European Commission Decision 2002/657/EC and Association of Official Racing Chemists criteria. The validation was performed for naproxen, flunixin, ketoprofen, diclofenac, eltenac, meclofenamic acid, phenylbutazone, vedaprofen, and carprofen in equine urine i...
Ventura E, Gadaj A, Buckley T, Mooney MH.Selective androgen receptor modulators (SARMs) are a group of anabolic enhancer drugs posing threats to the integrity of animal sports and the safety of animal-derived foods. The current research describes for the first time the development of a semi-quantitative assay for the monitoring of SARM family compounds in blood and establishes the relative stability of these analytes under various storage conditions prior to analysis. The presented screening method validation was performed in line with current EU legislation for the inspection of livestock and produce of animal origin, with detection...
Ishii H, Obara T, Kusano K, Kijima-Suda I.Paracetamol is commonly used as an over-the-counter analgesic and antipyretic medication for humans, but not sold as a legitimate therapeutic medication for horses in Japan. However, paracetamol is commonly found in horses together with its two isomers, metacetamol and orthocetamol. We previously reported that paracetamol and orthocetamol were both present in selected feed consumed by Japanese racehorses. For the purpose of the doping control of paracetamol in local Japanese horses, we proposed establishing residue limits (Japanese residue limits, JRLs) to minimize the risk of reporting parace...
Waraksa E, Owczarek K, Kubica P, Kłodzińska E, Ozimek M, Wrzesień R, Bobrowska-Korczak B, Namieśnik J.Bromhexine (BH), expectorant used in the treatment of respiratory disorders associated with viscid or excessive mucus, is not permitted for use in the competing horse by many authorities in horseracing and Olympic disciplines. Metabolic studies are of the great importance in anti-doping field because they allow for updating the selection of the most appropriate markers for prohibited substances, such as metabolites present at higher concentration levels and/or lasted for a longer period of time in biological samples than a parent drug. This study describes LC-MS/MS-based method for simultaneou...
Gadaj A, Ventura E, Healy J, Botrè F, Sterk SS, Buckley T, Mooney MH.Selective androgen receptor modulators (SARMs) represent non-steroidal agents commonly abused in human and animal (i.e. equine, canine) sports, with potential for further misuse as growth promoting agents in livestock-based farming. As a direct response to the real and possible implications of illicit application in both sport as well as food production systems, this study incorporated enzymatic hydrolysis (β-glucuronidase/arylsulfatase) into a previously established protocol while maintaining the minimal volume (200 µL) of urine sample required to detect SARMs encompassing various pharmacop...
Shibany KA, Pratt SL, Aldurdunji M, Totemeyer S, Paine SW.Horses are exposed to various kinds of medication, however, there are limited determinations of plasma clearance (CL) for the drugs used due to the high cost of equine studies.Many of the CL values generated come from the equine sports industry for determining drug plasma screening limits in the control of medications at the time of competition.The kinetics of omeprazole metabolism were investigated in freshly isolated and cryopreserved equine hepatocytes and hepatic microsomes ( = 3 horses).The V, K and intrinsic clearance (CL) of omeprazole were determined via the substrate depletion me...
Wong JKY, Chan GHM, Choi TLS, Kwok KY, Lau MY, Leung GNW, Wan TSM, Ho ENM.A high-throughput method has been developed for the doping control analysis of 124 drug targets, processing up to 154 horse urine samples in as short as 4.5 h, from the time the samples arrive at the laboratory to the reporting deadline of 30 min before the first race, including sample receipt and registration, preparation and instrument analysis and data vetting time. Sample preparation involves a brief enzyme hydrolysis step (30 min) to detect both free and glucuronide-conjugated drug targets. This is followed by extraction using solid-supported liquid extraction (SLE) and analysis using liq...
Roberts D, Cotter HVT, Cubeta M, Gilger BC.To determine minimum inhibitory concentrations (MICs) of four fungal species isolated from horses presented with equine fungal keratitis (EFK) in the southeastern United States to previously untested azole, echinocandin, and carboxamide antifungal drugs. Methods: In vitro assays were performed to determine the susceptibility of Aspergillus flavus, A. fumigatus, Fusarium falciforme, and F. keratoplasticum to five antifungal drugs representing three modes of action. Results: Luliconazole exhibited increased growth inhibition against both Aspergillus and Fusarium compared to commonly used, stan...
Mizobe F, Mori M, Nagata SI, Yamashita S, Okada J, Kusano K.Ever since 'One Health' concept was introduced in early 2000s, judicious use of antimicrobials by veterinarians has become an issue of great concern. Recently, findings of anti-inflammatory effects in certain types of antimicrobials have raised a subject for discussion among racing authorities. Regulatory framework of antimicrobials in racing should be based on best interest of horse welfare and doping control perspective, but basic data on prevalence of antimicrobials are lacking. Analysis of 100 postrace urinary samples collected from 10 Japanese racecourses by targeting 21 antimicrobials us...
Wong ASY, Choi TLS, Kwok KY, Wong JKY, Wan TSM, Ho ENM.Antipsychotics are banned substances and considered by the Fédération Equestrian Internationale (FEI) to have no legitimate use in equine medicine and/or have a high potential for abuse. These substances are also prohibited in horseracing according to Article 6 of the International Agreement on Breeding, Racing and Wagering (published by the International Federation of Horseracing Authorities). Over the years, antipsychotics have been abused or misused in equestrian sports and horseracing. A recent review of literature shows that there is yet a comprehensive screening method for antipsychoti...
Emmerich IU.In 2019, one novel pharmaceutical agent for horses or food-producing animals was released on the German market: An injection suspension for horses containing chondrogenic-induced equine allogeneic peripheral blood-derived mesenchymal stem cells as the active ingredient (ArtiCell Forte) is now available. Two established veterinary active pharmaceutical ingredients became accessible for additional species: a salicylanilide anthelmintic oxyclozanide (Distocur) for the treatment and control of fascioliasis in sheep as well as a type-I synthetic pyrethroid permethrin (Z-Itch), which now has additio...
Gretler SR, Finno CJ, McKemie DS, Kass PH, Knych HK.To describe the pharmacokinetics and selected pharmacodynamic variables of codeine and its metabolites in Thoroughbred horses following a single oral administration. Methods: Prospective experimental study. Methods: A total of 12 Thoroughbred horses, nine geldings and three mares, aged 4-8 years. Methods: Horses were administered codeine (0.6 mg kg) orally and blood was collected before administration and at various times until 120 hours post administration. Plasma and urine samples were collected and analyzed for codeine and its metabolites by liquid chromatography-mass spectrometry, and plas...
Ishii H, Obara T, Kijima-Suda I.Paracetamol is used widely as an over-the-counter analgesic and antipyretic medication for humans, but not for Japanese racehorses. Paracetamol can be an environmental substance, and is found together with its two isomers, metacetamol and orthocetamol, in equine urine. However, the sources and routes of paracetamol exposure remain unclear. To control the misuse of paracetamol, it is appropriate to establish residue limits for paracetamol to differentiate the administration of paracetamol from its environmental levels. In this study, we developed and validated a quantitative method for paraceta...
Pritchard A, Nielsen BD, Robison C, Spooner H.Previous research documented that furosemide negatively impacted calcium balance for 3 days but did not determine when calcium balance returned to baseline. This study hypothesized that furosemide's impact on calcium would return to control values before 7 days post-administration. Ten mature geldings were assigned to either control (CON, n = 5) or treatment (FUR, n = 5) for the first of two 8-day total collections in crossover design. Treatment horses received one administration of furosemide (1 mg/kg, IV). A 10% sample of pooled faeces and urine from each day was kept. Calcium concent...
Gilday R, Richard H, Beauchamp G, Fogarty U, Laverty S.The administration of bisphosphonate medications, which target osteoclastic-bone remodelling, to juvenile and adult racehorses is a matter of debate owing to concerns that these molecules remain bound to the bone-mineralised matrix and may interfere with subsequent bone growth, adaptation to exercise and healing of bone microdamage in equine athletes. Osteoclasts participate in endochondral ossification, subchondral bone remodelling and bone repair. There is a knowledge gap on the role of equine osteoclast biology in the growth and maturation of joint surfaces and this information is important...
Estell KE, Knych HK, Patel T, Edman JM, Magdesian KG.To the authors' knowledge, there have been no studies evaluating the pharmacokinetics of chloramphenicol administered orally to horses at the currently recommended dose of 50 mg/kg PO q6 h for multiple days. The published antimicrobial susceptibility breakpoint is 8.0 ug/mL; it is unknown if this concentration is achievable at the recommended dose rate in horses. The aim of this prospective multi-dose pharmacokinetic study was to perform pharmacokinetic analysis of chloramphenicol after multiple doses. The authors hypothesize that the antimicrobial susceptibility breakpoint will not be reached...
Berryhill EH, Knych H, Chigerwe M, Edman J, Magdesian KG.The neurokinin-1 (NK-1) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood in horses, and clinical use of NK-1 receptor antagonists has not been reported. This study aimed to determine the pharmacokinetics and safety of maropitant after administration of multiple doses. We hypothesized that maropitant concentrations would be similar at steady state to those reported in dogs, with minimal adverse effects. Maropitant was administered at 4 mg/kg orally, once daily for 5 days in seven adult horses. Serial plasma maropitant concent...
Houghton E, Maynard S.This chapter reviews drug and medication control in equestrian sports and addresses the rules of racing, the technological advances that have been made in drug detection and the importance of metabolism studies in the development of effective drug surveillance programmes. Typical approaches to screening and confirmatory analysis are discussed, as are the quality processes that underpin these procedures. The chapter also addresses four specific topics relevant to equestrian sports: substances controlled by threshold values, the approach adopted recently by European racing authorities to control...
Dirikolu L, Lehner F, Nattrass C, Bentz BG, Woods WE, Carter WG, Karpiesiuk W, Jacobs J, Boyles J, Harkins JD, Granstrom DE, Tobin T.Diclazuril (4-chlorophenyl [2,6-dichloro-4-(4,5-dihydro-3H-3,5-dioxo-1,2,4-triazin-2-yl)pheny l] acetonitrile), is a benzeneacetonitrile antiprotozoal agent (Janssen Research Compound R 64433) marketed as Clinacox . Diclazuril may have clinical application in the treatment of Equine Protozoal Myeloencephalitis (EPM). To evaluate its bioavailability and preliminary pharmacokinetics in the horse we developed a sensitive quantitative high-pressure liquid chromatography (HPLC) method for diclazuril in equine biological fluids. MS/MS analysis of diclazuril in our HPLC solvent yielded mass spectral ...
Nizolek DJ, White KK.Degenerative arthrosis is perhaps the most common debilitating disease of performance horses. Treatment should be based upon a knowledge of the anatomy and physiology of normal joints and upon an understanding of the processes of degeneration and repair. These topics are briefly reviewed. Although rest is probably, the most beneficial therapy, physical and pharmaceutical treatments are often employed in an effort to speed recovery. The effects and relative benefits of intrasynovial injections of corticosteroids, hyaluronica cid, and Arteparon are considered in detail. Although local corticoste...
Mendoza FJ, Serrano-Rodriguez JM, Perez-Ecija A.Nonsteroidal anti-inflammatory drugs are administered in horses for several systemic diseases. Selective cyclooxygenase-2 inhibitors are preferred because of lower risk of adverse effects. Several meloxicam formulations have been tested in horses, but a recently marketed granule oral formulation has not been studied. Objective: To characterize the pharmacokinetics of a novel granule meloxicam formulation in fasted and fed horses, and to compare pharmacokinetic features with oral suspension and tablets. Methods: Seven healthy adult horses. Methods: Meloxicam was administered at 0.6 mg/kg in fas...
Grimsrud KN, Mama KR, Thomasy SM, Stanley SD.Detomidine is commonly used i.v. for sedation and analgesia in horses, but the pharmacokinetics and metabolism of this drug have not been well described. Objective: To describe the pharmacokinetics of detomidine and its metabolites, 3-hydroxy-detomidine (OH-detomidine) and detomidine 3-carboxylic acid (COOH-detomidine), after i.v. and i.m. administration of a single dose to horses. Methods: Eight horses were used in a balanced crossover design study. In Phase 1, 4 horses received a single dose of i.v. detomidine, administered 30 microg/kg bwt and 4 a single dose i.m. 30 microg/kg bwt. In Phase...
Gutierrez J, Eisenberg RL, Koval NJ, Armstrong ER, Tharappel J, Hughes CG, Tobin T.Pemoline is a central nervous system stimulant that has been used to treat attention-deficit hyperactivity disorder and narcolepsy in humans; its identification in horses could be considered evidence of attempts to influence performance. Two recent pemoline 'positives' in English racehorses led us to review the chemical relationships between tetramisole, levamisole, aminorex and pemoline. Pemoline is a simple oxidation product of aminorex, which has been shown in the United States and elsewhere to be an equine metabolite of levamisole. Based on the clear structural relationships between aminor...
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...
Ho EN, Wan TS, Wong AS, Lam KK, Stewart BD.Insulin and its analogues have been banned in both human and equine sports owing to their potential for misuse. Insulin administration can increase muscle glycogen by utilising hyperinsulinaemic clamps prior to sports events or during the recovery phases, and increase muscle size by its chalonic action to inhibit protein breakdown. In order to control insulin abuse in equine sports, a method to effectively detect the use of insulins in horses is required. Besides the readily available human insulin and its synthetic analogues, structurally similar insulins from other species can also be used a...
Nouws JF, Firth EC, Vree TB, Baakman M.Plasma disposition, protein binding, urinary recovery, and renal clearance of sulfamethazine (SMZ), sulfamerazine (SMR), and sulfadiazine (SDZ) and their N4-acetyl and hydroxy derivatives were studied in 4 horses in a crossover trial. The plasma concentration-time curves of the metabolites paralleled those of the parent drug in the elimination phase. Sulfamethazine and SMR were extensively metabolized. In plasma and urine, the main metabolite of the 3 sulfonamides tested was the 5-hydroxypyrimidine derivative, which was highly glucuronidated. Difference in elimination half-life of SMZ, SMR, an...
Ho EN, Kwok WH, Lau MY, Wong AS, Wan TS, Lam KK, Schiff PJ, Stewart BD.A veterinary preparation known as TB-500 and containing a synthetic version of the naturally occurring peptide LKKTETQ has emerged. The peptide segment (17)LKKTETQ(23) is the active site within the protein thymosin β(4) responsible for actin binding, cell migration and wound healing. The key ingredient of TB-500 is the peptide LKKTETQ with artificial acetylation of the N-terminus. TB-500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation. In order to control the misuse of TB-500 in equin...
Pérez R, Cabezas I, Godoy C, Rubilar L, Muñoz L, Arboix M, Castells G, Alvinerie M.A study was undertaken in order to compare plasma disposition kinetic parameters of doramectin (DRM) and ivermectin (IVM) in horses after oral administration. Ten crossbreed adult horses, clinically healthy, weighing 380-470 kg body weight (bw) were selected for study. Faecal examinations were performed to determine faecal parasite egg counts. Horses were allocated to two groups of five animals to provide an even distribution considering the variables sex, body weight and faecal egg count. Group I, were treated with an oral paste formulation of IVM at 0.2 mg/kg b/w and Group II, were treated w...
Kvaternick V, Malinski T, Wortmann J, Fischer J.A sensitive reversed-phase HPLC-UV method was developed for the determination of firocoxib, a novel and highly selective COX-2 inhibitor, in plasma. A 1.0 mL dog or horse plasma sample is mixed with water and passed through a hydrophobic-lipophilic copolymer solid-phase extraction column to isolate firocoxib. Quantitation is based on an external standard curve. The method has a validated limit of quantitation of 25 ng/mL and a limit of detection of 10 ng/mL. The validated upper limit of quantitation was 2500 ng/mL for horses and 10,000 ng/mL for dogs. The average recoveries ranged from 88-93% ...
Dickey EJ, McKenzie HC, Brown KA, de Solis CN.Continuous-rate infusions (CRI) of lidocaine are often used for prolonged duration but, to date, only limited time/concentration relationships administered as a short term (24 h) CRI have been reported. Objective: To determine the time/concentration profile of lidocaine and its active metabolites glycinexylidide (GX) and monoethylglycinexylidide (MEGX) during a 96 h lidocaine infusion. Methods: Lidocaine was administered to 8 mature healthy horses as a continuous rate infusion (0.05 mg/kg bwt/min) for 96 h. Blood concentrations of lidocaine, GX and MEGX were determined using high performance l...
McKinney AR, Suann CJ, Stenhouse AM.A method has been developed for the detection of modafinil and its major metabolite, modafinil acid, in equine urine by solid-phase extraction and positive ion electrospray ionisation liquid chromatography/mass spectrometry. The method has been applied to the analysis of equine urine samples obtained after the oral administration of modafinil. Modafinil acid was the major component in the urine, and was detected up to 4 days post-administration. Unchanged modafinil was present at substantially lower concentrations, and was detected for only 24 hours.
Levine DG, Epstein KL, Neelis DA, Ross MW.To determine whether topical application of 1% diclofenac sodium cream would decrease inflammation at sites of IV regional limb perfusion (IVRLP) in healthy horses. Methods: 6 healthy adult horses (12 forelimbs). Methods: Bilateral IVRLP with 2.5 g of amikacin sulfate was performed twice in each horse, with 24 hours between each session. Horses were treated with topical 1% diclofenac liposomal cream (treated limbs) or a placebo cream (control limbs). All injection sites were evaluated before the first IVRLP session and 24 hours after the second session by means of ultrasonographic examination ...
You Y, Uboh CE, Soma LR, Guan F, Taylor D, Li X, Liu Y, Chen J.A method involving ultra high-performance liquid chromatography-tandem mass spectrometry was developed and validated for the analysis of capsaicin and dihydrocapsaicin in equine plasma. The analytes were recovered from plasma by liquid-liquid extraction using methyl tert-butyl ether and separated on a sub-2 micron column. The mobile phase was composed of 2 mM ammonium formate and methanol. A triple quadrupole mass spectrometer was used to detect the analytes in positive electrospray ionization mode with selected reaction monitoring. The limits of detection, quantification and confirmation for ...
Edmunds JL, Worgan HJ, Dougal K, Girdwood SE, Douglas JL, McEwan NR.The present study uses in vitro analytical techniques to investigate the effect of activated charcoal on the microbial community of the equine hindgut and the metabolites they produce. Incubations were performed in Wheaton bottles using a 50 ml incubation of a high-energy feed or a low-energy feed, plus bottles with no added food source, together with five levels of activated charcoal (0, 10, 25, 50 or 100 mg per bottle) and fecal samples as a bacterial inoculum. Using this method the rate of gas production, volatile fatty acid and ammonia concentrations, and pH values were analyzed and found ...
Stojiljkovic N, Paris A, Garcia P, Popot MA, Bonnaire Y, Tabet JC, Junot C.Horse urine is the medium of choice for the implementation of metabolomic approaches aimed at improving horse doping control. However, drug analysis in this biofluid is a challenging task due to the presence of large amounts of interfering compounds. METHODOLOGY & RESULTS: A comparative study of sample preparation has been conducted to evaluate five sample-preparation methods, namely acetonitrile precipitation, proteinase K hydrolysis, membrane filtration and sample dilution with water by factors of five and 20, for metabolome analysis using liquid chromatography coupled to high resolution...
Mocchi M, Grolli S, Dotti S, Di Silvestre D, Villa R, Berni P, Conti V, Passignani G, Brambilla F, Bue MD, Catenacci L, Sorrenti M, Segale L, Bari E....In the last decades, it has been demonstrated that the regenerative therapeutic efficacy of mesenchymal stromal cells is primarily due to the secretion of soluble factors and extracellular vesicles, collectively known as secretome. In this context, our work described the preparation and characterization of a freeze-dried secretome (Lyosecretome) from adipose tissue-derived mesenchymal stromal cells for the therapy of equine musculoskeletal disorder. An intraarticular injectable pharmaceutical powder has been formulated, and the technological process has been validated in an authorized facility...
Mercer MA, McKenzie HC, Davis JL, Wilson KE, Hodgson DR, Cecere TE, McIntosh BJ.There are no published studies on the pharmacokinetics of acetaminophen at the dosage used clinically (20 mg/kg), nor has the safety of multiple doses in horses been investigated. Objective: Define the pharmacokinetic parameters of oral acetaminophen at 20 mg/kg in adult horses as a single dose, and twice daily for 14 days to assess the safety of multiple dosing. Methods: Pharmacokinetic study, multiple dose safety study. Methods: Eight healthy Thoroughbred geldings were given acetaminophen (20 mg/kg; 500 mg tablets) orally as a single dose followed by doses every 12 h for 14 days. Seri...
Moulard Y, Bailly-Chouriberry L, Boyer S, Garcia P, Popot MA, Bonnaire Y.Liquid chromatography-mass spectrometry (LC-MS) has been widely used in doping control laboratories over the last two decades. Currently, simple quadrupole, triple quadrupole and ion trap are the most commonly employed analyzers in toxicological analysis. Nevertheless, the main lack of these technologies is the restricted number of target compounds simultaneously screened without loss of sensitivity. In this article we present an innovative screening approach routinely applied in the French horse doping control laboratory based on high resolution (50000) and high mass accuracy (<5 ppm) in f...
Gray BP, Viljanto M, Bright J, Pearce C, Maynard S.The detection of the abuse of anabolic steroids in equine sport is complicated by the endogenous nature of some of the abused steroids, such as testosterone and nandrolone. These steroids are commonly administered as intramuscular injections of esterified forms of the steroid, which prolongs their effects and improves bioavailability over oral dosing. The successful detection of an intact anabolic steroid ester therefore provides unequivocal proof of an illegal administration, as esterified forms are not found endogenously. Detection of intact anabolic steroid esters is possible in plasma samp...
González JA, Vallejo JR.This review documents the wide and varied repertoire of traditional practices and remedies based on the use of domestic animals in Spanish ethnoveterinary medicine (EVM) from the early 20th century to the present. Empirical practices, both ritual and magical, are recorded, and these EVM data are compared with those of other countries in the Mediterranean region and Latin America. The data collected here could form a scientific foundation for future inventories of local veterinary knowledge (LVK) and research addressing the discovery of new drugs for livestock and the validation of the effects....
Guedes AG, Knych HK, Soares JH, Brosnan RJ.This study evaluated the pharmacokinetics and physiological effects of tramadol during repeated oral administrations in horses. Nine adult healthy horses were administered tramadol at 5 and 10 mg/kg orally every 12 h for 5 days in a randomized, crossover design with a 3-week washout between treatments. Plasma concentrations of tramadol, O- and N-desmethyltramadol (M1 and M2) were measured using Liquid-Chromatography-Mass Spectrometry at predetermined time points following each tramadol administration. Cardiovascular, respiratory and gastrointestinal physiological variables were monitored an...
Gilday R, Richard H, Beauchamp G, Fogarty U, Laverty S.The administration of bisphosphonate medications, which target osteoclastic-bone remodelling, to juvenile and adult racehorses is a matter of debate owing to concerns that these molecules remain bound to the bone-mineralised matrix and may interfere with subsequent bone growth, adaptation to exercise and healing of bone microdamage in equine athletes. Osteoclasts participate in endochondral ossification, subchondral bone remodelling and bone repair. There is a knowledge gap on the role of equine osteoclast biology in the growth and maturation of joint surfaces and this information is important...
Sutherland IH.Following the development of a unique claim structure encompassing both nematode and arthropod species, ivermectin was first introduced as a veterinary parasiticide in 1981. For cattle(c), sheep(s), horses(h) and pigs(p) injectable(c,s,p), oral(c,s,h) and topical(c) products are available delivering ivermectin at 200 to 500 micrograms/kg. Efficacy extends to nematodes of the gastrointestinal and respiratory tracts, conjunctival sac and soft tissues. Among the arthropod parasites claims have been established for the biting fly Haematobia irritans(c), the screw-worm Chrysomyia bezziana(c), larva...
