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Topic:Drug

The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
Quantitative DNA metabarcoding reveals species composition of a macrocyclic lactone and pyrantel resistant cyathostomin population in the UK.
International journal for parasitology. Drugs and drug resistance    December 22, 2024   Volume 27 100576 doi: 10.1016/j.ijpddr.2024.100576
Bull KE, Hodgkinson J, Allen K, Poissant J, Peachey LE.Cyathostomins are the most abundant equid endoparasites globally. There are approximately fifty cyathostomin species and, whilst they occupy distinct niches within the large intestine, they are generally considered to share similar characteristics in terms of pathogenicity and response to drug treatment. There are three classes of anthelmintic licensed in the UK to treat cyathostomins (benzimidazoles, tetrahydropyrimidines and macrocyclic lactones) and cases of resistance have been documented for all classes. Previously, faecal egg count reduction tests (FECRT) on four UK Thoroughbred studs re...
Doping Control Analysis of Methylsulfonylmethane in Horses.
Drug testing and analysis    December 21, 2024   doi: 10.1002/dta.3844
Wong JKY, Choi TLS, Wong COL, Curl P, Wan TSM, Ho ENM.Methylsulfonylmethane (MSM), also known as dimethyl sulfone, is a naturally occurring sulphur-containing compound that can be found in plants, animals and humans. MSM can also be a metabolite of dimethyl sulfoxide (DMSO). Due to their anti-inflammatory and analgesic effects, both MSM and DMSO are prohibited substances in horseracing. As both substances are naturally occurring, their misuse in horses is controlled by International Residue Limits (IRL) of 1200 and 15 μg/mL, respectively, in horse urine as established by the International Federation of Horseracing Authorities. The elimination ...
Electrochemotherapy with bleomycin for bilateral ocular squamous cell carcinoma in a horse.
Veterinary ophthalmology    December 16, 2024   doi: 10.1111/vop.13310
Larsen MME, Eriksson A, Impellizeri JA.To describe the procedure and outcome of electrochemotherapy (ECT) with bleomycin as a first-line treatment for bilateral ocular surface squamous neoplasia (OSSN) in the eye of a horse. Methods: A client-owned 5-year-old Haflinger gelding with limbal-conjunctival squamous cell carcinoma. Methods: During general and local anesthesia, injection of bleomycin in the ocular tumor was followed by electroporation, applied with a 15 mm needle electrode, needles held parallel to the ocular surface. Results: Treatment with ECT resulted in therapeutic electric pulses and complete tumor response with no...
Successful management of two horses with suspected pulmonary haemorrhage in recovery from general anaesthesia.
Veterinary anaesthesia and analgesia    December 16, 2024   doi: 10.1016/j.vaa.2024.11.002
Hordle T, Ranninger E, Bettschart-Wolfensberger R.A 24 year old warmblood mare (case 1) and a 12 year old Holsteiner gelding (case 2) were anaesthetized for bursoscopy and phacoemulsification, respectively. Both were premedicated with intramuscular acepromazine (30 μg kg-1). The horses were sedated with intravenous (IV) medetomidine (7-9 μg kg-1 to effect), before anaesthetic induction with ketamine-diazepam. Anaesthesia was maintained with isoflurane in a mixture of oxygen and medical air, alongside a medetomidine constant rate infusion at 3.5 μg kg-1 hour-1. In recovery, 3 and 5 μg kg-1 of medetomidine were administered IV to cases 1 an...
Anti-Pythium insidiosum activity of three novel triazole compounds: synthesis, pharmacokinetic and toxicological parameters.
Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology]    December 12, 2024   Volume 56, Issue 1 331-340 doi: 10.1007/s42770-024-01572-y
Fernandes CM, Prestes AS, Ianiski LB, Maciel AF, Noro BG, da Silva FD, Vizzotto BS, Botton SA, Schumacher RF, Pereira DIB, Barbosa NV.Pythiosis, caused by Pythium insidiosum, is an infectious and non-transmissible disease affecting horses, dogs, and humans, with no effective drug treatment available. Triazoles are compounds of interest for their potential pharmacological properties against fungi and bacteria. In this study, we synthesized three new triazole compounds (C1, C2, and C3) to assess their in vitro activities against P. insidiosum and their safety on human leukocytes. Susceptibility testing was performed against P. insidiosum isolates (n = 15) to determine the minimum inhibitory concentration (MIC) and minimum ...
Detection of Over 110 Anabolic-Androgenic Steroids, Corticosteroids and/or Their Esters in Horse Hair Using Ultra-High-Performance Liquid Chromatography-High-Resolution Mass Spectrometry and Gas Chromatography-Tandem Mass Spectrometry After Solid-Supported Liquid Extraction.
Drug testing and analysis    December 10, 2024   doi: 10.1002/dta.3837
So YM, Kwok WH, Ching CCW, Wong COL, Wan TSM, Ho ENM.Anabolic-androgenic steroids (AAS) are banned substances in both human and equine sports. They are often administered intramuscularly to horses in esterified forms for the purpose of extending their duration of action. As such, the detection of intact esters of endogenous steroids in hair is particularly advantageous, as it can provide unequivocal proof of their external origin. Compared with urine and blood matrices, hair in general allows a longer detection window as long as the administered drug can be incorporated into hair and has not degraded. This can be useful in doping control of equi...
Egg reappearance periods associated with anthelmintic treatments given to horses in winter and summer over two years.
Veterinary parasitology, regional studies and reports    December 9, 2024   Volume 57 101182 doi: 10.1016/j.vprsr.2024.101182
Scott I, Lawrence KE, Gee EK.Shortened egg reappearance periods (ERP) have been seen as an early warning of anthelmintic resistance development in cyathostomins in horses. The hypothesis has been that in these instances, efficacy against egg laying adult cyathostomins remains high, but a decline in activity against later larval stages leads to the earlier resumption of egg shedding after treatment. In this study using a single herd of horses we investigated the ERP of a number of commonly used equine anthelmintics and examined whether ERP might show seasonal variation between winter and summer. Four main Faecal egg count ...
Clinical efficacy of inhaled corticosteroids in equine asthma: A meta-analysis and number needed to treat.
Pulmonary pharmacology & therapeutics    December 5, 2024   Volume 88 102342 doi: 10.1016/j.pupt.2024.102342
Equine asthma, a prevalent chronic inflammatory condition affecting the equine population, significantly compromises the performance and quality of life in affected horses. Inhaled corticosteroids (ICS) are often the first-line pharmacological intervention due to their potent anti-inflammatory properties. This meta-analysis investigates the clinical efficacy of ICS in treating equine asthma, emphasizing the number needed to treat (NNT) and the likelihood of achieving a clinical response. A comprehensive literature search identified relevant studies comparing ICS with placebo (PCB) controlled t...
The effect of intramuscular atipamezole on head height and sedation scores in detomidine-sedated horses.
Veterinary anaesthesia and analgesia    November 26, 2024   S1467-2987(24)00345-3 doi: 10.1016/j.vaa.2024.11.008
Mascarenhas C, Castro D, Lascola KM, Hofmeister E, Clark-Price SC.To assess the effect of two different doses of intramuscular atipamezole on head height (HH) in horses after sedation with detomidine. Methods: Randomized, blinded, triple crossover study. Methods: Eight healthy adult horses. Methods: Baseline HH was measured before detomidine (40 μg kg) was injected intravenously. HH was measured at 10 and 20 minutes after injection. Then, saline, atipamezole 60 μg kg (AT60) or 120 μg kg (AT120) was injected intramuscularly. HH measurements were repeated at 10 minutes intervals for 100 minutes. HH data were analyzed with a linear mixed model. Significance ...
Effect of Low-Molecular-Weight Hyaluronate-Based Nanoparticles on the In Vitro Expression of Cartilage Markers.
International journal of molecular sciences    November 21, 2024   Volume 25, Issue 23 12486 doi: 10.3390/ijms252312486
Bianchera A, Borghetti P, Ravanetti F, Bertocchi L, De Angelis E, Bettini R.Hyaluronic acid (HA) is a key component of synovial fluid as it plays a crucial role in joint physiology. Its biological activity is influenced by molecular weight, local concentration, and persistence in joints. High-molecular-weight HA has a consolidated history of clinical use, whereas little is known about the metabolic effect of low-molecular-weight hyaluronate on cartilage differentiation. This study explores the potential of HA-based nanoparticles (NPs) on chondrocytes differentiation in vitro. Starting from 25 kDa and 250 kDa sodium hyaluronate solutions, two types of NPs were prepared...
Pharmacokinetics of Salbutamol in Thoroughbred Horses After a Single Intravenous or Inhaled Administration.
Journal of veterinary pharmacology and therapeutics    November 11, 2024   doi: 10.1111/jvp.13491
Nomura M, Kuroda T, Ohta M, Kusano K, Minamijima Y, Nagata S.Salbutamol is a short-acting and selective beta-2 adrenergic agonist. Inhaled (IH) administration of salbutamol is widely used to control lower respiratory tract disease in horses. Here, we estimated the pharmacokinetic parameters of salbutamol after a single intravenous (IV) or IH administration in six horses, and we statistically analysed the detection times with various dosing regimens. Plasma and urine concentrations of salbutamol were measured by liquid chromatography-tandem mass spectrometry, and data were modelled by using a nonlinear mixed effect model followed by Monte Carlo simulatio...
Potential adverse effects of SGLT2i in horses.
The Veterinary record    November 1, 2024   Volume 195, Issue 6 253-254 doi: 10.1002/vetr.4726
McGorum BC, Keen JA, McCullagh S, Marr CM, MacKenzie C, Carslake H, Menzies-Gow N, Dunkel B, Hewetson M, Reed J, Knowles E.No abstract available
Retrospective evaluation of the impact of atropine administration on incidence of post-operative colic in healthy, isoflurane-anaesthetised horses.
Equine veterinary journal    October 29, 2024   doi: 10.1111/evj.14428
Varner KM, Curtiss AL, Hogan PM, Love K, Dodam JR.In anaesthetised horses, bradycardia secondary to high vagal tone can reduce cardiac output and blood pressure. The use of anticholinergics in horses is limited due to concerns about ileus and abdominal discomfort. This retrospective study sought to determine the prevalence of post-operative abdominal discomfort in healthy horses that received atropine under isoflurane anaesthesia. Methods: A retrospective evaluation of 222 general anaesthesia events between January 2019 and December 2019 was undertaken. Methods: One hundred and eleven horses that received atropine were identified, and 111 cas...
Influence of acepromazine on the cardiovascular effects of dobutamine in isoflurane-anaesthetised horses premedicated with romifidine.
Veterinary anaesthesia and analgesia    October 24, 2024   S1467-2987(24)00334-9 doi: 10.1016/j.vaa.2024.10.141
Wong AM, Schier MF, Hosgood G, Drynan E, Raisis AL.To explore the influence of acepromazine on the cardiovascular effects of dobutamine in isoflurane-anaesthetised horses premedicated with romifidine. Methods: Prospective randomised clinical trial. Methods: A total of 18 horses undergoing elective arthroscopy were enrolled, of which 12 horses requiring dobutamine were included. Methods: Horses were randomised to receive acepromazine 0.02 mg kg (Group A+) intravenously (IV) or none (Group A-), 35 minutes before anaesthesia. Horses received xylazine 0.2 mg kg concurrently to facilitate IV access. Horses were premedicated with romifidine 0.08 mg ...
Effect of furosemide on comprehensive renin-angiotensin-aldosterone system activity of Thoroughbred horses.
Journal of veterinary internal medicine    October 22, 2024   doi: 10.1111/jvim.17208
Lehman ML, Domenig O, Ames MK, Morgan JM.Furosemide, a commonly used diuretic, activates the renin-angiotensin-aldosterone system (RAAS) in other species. Little is known about RAAS peptide activation in horses. Objective: To evaluate equilibrium analysis as a practical method for RAAS quantification in horses and describe the RAAS response to a single dose of furosemide. We hypothesize that furosemide would cause transient increase in RAAS peptides in horses. Methods: 14 healthy adult thoroughbreds from a university teaching herd. Methods: Horses received either furosemide (1 mg/kg IV) or saline IV in a crossover study design. Pro...
Administration Route Differentiation of Altrenogest via the Metabolomic LC-HRMS Analysis of Equine Urine.
Molecules (Basel, Switzerland)    October 22, 2024   Volume 29, Issue 21 4988 doi: 10.3390/molecules29214988
Elbourne M, Keledjian J, Cawley A, Fu S.Altrenogest, also known as allyltrenbolone, is a synthetic form of progesterone used therapeutically to suppress unwanted symptoms of estrus in female horses. Altrenogest affects the system by decreasing levels of endogenous gonadotrophin and luteinizing and follicle-stimulating hormones, which in turn decreases estrogen and mimics the increase of progesterone production. This results in more manageable mares for training and competition alongside male horses while improving the workplace safety of riders and handlers. However, when altrenogest is administered, prohibited steroid impurities su...
Erratum for “Effect of phenylbutazone on insulin secretion in horses with insulin dysregulation”.
Journal of veterinary internal medicine    October 7, 2024   Volume 38, Issue 6 3695 doi: 10.1111/jvim.17210
No abstract available
Antibiotics: Our part in their downfall.
Equine veterinary journal    October 4, 2024   Volume 56, Issue 6 1092-1095 doi: 10.1111/evj.14211
Bladon B.No abstract available
Investigating the Suitability of Mare’s Milk-Derived Exosomes as Potential Drug Carriers.
Biomolecules    October 1, 2024   Volume 14, Issue 10 1247 doi: 10.3390/biom14101247
Sergazy S, Zhetkenev S, Shulgau Z, Chulenbayeva L, Kamyshanskiy Y, Nurgaziyev M, Nurgozhina A, Mukhanbetzhanova Z, Berikkhanova K, Gulyayev A....Exosomes are cell-derived, membrane-surrounded particles that deliver bioactive molecules to various cells. Due to their small size, low immunogenicity, extended blood circulation, and involvement in cellular communication, they hold potential as effective drug carriers. Exosomes are present in various biological fluids, including mare's milk, a traditional drink in Central Asia. This study aims to compare exosome isolation methodologies and determine the stability of mare's milk-derived exosomes as potential therapeutic carriers. Three extraction methods-immunoprecipitation, size exclusion ch...
Equine metabolic investigation of the phosphodiesterase-4 inhibitor ibudilast as a potential performance enhancer.
Rapid communications in mass spectrometry : RCM    September 23, 2024   Volume 38, Issue 23 e9916 doi: 10.1002/rcm.9916
Philip M, Kal AKK, Subhahar MB, Karatt TK, Graiban FM, Ajeebsanu MM, Joseph M, Jose SV.Phosphodiesterase 4 (PDE4) inhibitors are a newer class of drugs that induce bronchodilation and have anti-inflammatory effects, making them susceptible to misuse as performance enhancers in competitive sports. Methods: This study explores the metabolic conversion of PDE4 inhibitor ibudilast in thoroughbred horses after oral administration and in vitro using equine liver microsomes and Cunninghamella elegans. A liquid chromatography-high resolution mass spectrometry method was used to postulate the plausible structures of the detected metabolites. Results: A total of 20 in vivo metabolites wer...
Discovery of Biomarkers of a Recombinant Human Erythropoietin Administration to Thoroughbred Geldings by Label-Free Proteomics.
Drug testing and analysis    September 22, 2024   doi: 10.1002/dta.3810
Cheung HW, Wong KS, Tam JCL, Farrington AF, Bond AJ, Wan TSM, Ho ENM.Erythropoiesis-stimulating agents (ESAs) continue to be a significant threat to the integrity of human and equine sports. Besides conventional direct testing, monitoring the biomarkers associated with the effects of ESAs may provide a complementary approach via indirect detection to enhance doping control. In this study, we applied label-free proteomics to discover plasma protein biomarkers in Thoroughbred geldings after administration with a long-acting form of recombinant human erythropoietin (rhEPO), methoxy polyethylene glycol epoetin beta, Mircera. Increased haematocrit, haemoglobin and r...
Pharmacokinetics of Two Formulations of Altrenogest Administered to Mares.
Drug testing and analysis    September 22, 2024   doi: 10.1002/dta.3796
Loy J, Cawley A, Sornalingam K, Scrivener CJ, Keledjian J, Noble GK.Altrenogest is a synthetic progestin that suppresses reproductive behaviours and assists pregnancy maintenance in female horses. Two formulations are available, a 'weekly' intramuscular injection and a daily oral formulation. Altrenogest administration has returned positive swabs for steroids; consequently, using injectable altrenogest in racing mares is prohibited. Oral administration may be permitted in race mares if there is one clear day between dosing and racing. The only pharmacokinetic data available were generated from geldings. Therefore, to assist veterinarians and analysts in determ...
Pharmacokinetics and thermal anti-nociceptive effects of oral morphine in horses.
Frontiers in veterinary science    September 17, 2024   Volume 11 1461648 doi: 10.3389/fvets.2024.1461648
Knych HK, Steinmetz SJ, Traynham ML, McKemie DS, Kass PH.Morphine is an effective analgesic in horses, however, IV administration at therapeutic doses has been shown to produce dose-dependent neuroexcitation and unwanted gastrointestinal effects. The analgesic effects of morphine have, at least in part, been attributed to the morphine-6-glucuronide (M6G) metabolite. Oral administration to horses results in comparable M6G concentrations to that achieved following IV administration of a therapeutic dose without the adverse effects. The anti-nociceptive effects have not yet been reported. In the current study the thermal anti-nociceptive effects of sin...
Evaluating the Effects of Solid-Phase Cartridge Chemistry on Extraction of Bisphosphonates and ITPP From Equine Plasma.
Drug testing and analysis    September 16, 2024   Volume 17, Issue 7 997-1001 doi: 10.1002/dta.3800
Klingberg J, Richards S, Hochwallner T, Kennan L, Keledjian J.Bisphosphonate drugs and myo-inositol trispyrophosphate are of concern to the racing industry and have been listed as prohibited substances in equine sports. The current bisphosphonate plasma screening analysis employed at the Australian Racing Forensic Laboratory involves the use of sequential solid-phase extraction procedures, passing the samples through a mixed mode cartridge, followed by a weak anion exchange cartridge. The eluates collected following the second extraction are then methylated and analysed by liquid chromatography-mass spectrometry. Under these extraction conditions, some b...
Pharmacokinetics of Ethyl Glucuronide and Ethyl Sulfate and Pharmacodynamic Effects Following Intravenous and Oral Administration of Ethanol to Exercised Horses.
Drug testing and analysis    September 15, 2024   doi: 10.1002/dta.3803
Knych HK, Blea J, Scollay M, Kass PH, McKemie DS.Ethanol, a central nervous system depressant and banned substance in horseracing, has reportedly been administered to horses prior to competition to "calm a horse's nerves." In this study, the pharmacokinetics of two metabolites of ethanol were studied to better understand the behavior of this compound in the horse and provide a scientific basis for regulation of its administration. Six horses received a single intravenous (30 mL; 1200 mg) and oral (90 mL; 3600 mg) administration of ethanol (vodka, 40% ABV) in a balanced cross-over design. Blood and urine samples were collected at vari...
Detection of levamisole and its metabolites in horses after oral levamisole administration over seven days.
Journal of the American Veterinary Medical Association    September 13, 2024   Volume 262, Issue 12 1632-1638 doi: 10.2460/javma.23.06.0340
Adam E, Scollay M, Howard B, Taormina J, Hartmann P, Knych H.Levamisole is a regulated substance sometimes administered to racehorses to treat equine protozoal myelitis. Metabolites include compound II, aminorex, and pemoline. Aminorex and pemoline are Horseracing Integrity and Safety Authority-banned substances. Previous studies have examined single doses of the drug. This study examined the disposition of levamisole after 7 days of dosing. Methods: 6 healthy Thoroughbred geldings. Methods: Horses were treated with 500 mg (approx 0.91 to 1 mg/kg) of compounded levamisole hydrochloride paste PO every 12 hours for a total of 13 doses over 7 days. Serum a...
Oral trazodone results in quantifiable sedation but does not result in a xylazine-sparing effect in healthy adult horses.
American journal of veterinary research    September 6, 2024   1-6 doi: 10.2460/ajvr.24.07.0185
Swanton WE, Johnson R, Zhao Q, Schroeder C.To evaluate sedation and IV xylazine requirements to achieve 45% of baseline head height above ground measurements following oral (PO) administration of 2 trazodone dosages. Methods: 8 healthy, adult mares of various weights and breeds belonging to a university teaching herd were utilized in a blinded, crossover study design. Horses were randomly assigned to 1 of 3 PO treatments: control (no trazodone), trazodone at 3 mg/kg (low dose [LD]), or trazodone at 6 mg/kg (high dose [HD]). Before treatment, cardiac auscultation, EquiSed sedation score, and head height above ground (HHAG; cm) measureme...
Quantification of osilodrostat in horse urine using LC/ESI-HRMS to establish an elimination profile for doping control.
Bioanalysis    September 5, 2024   1-12 doi: 10.1080/17576180.2024.2385848
Ishii H, Shigematsu R, Takemoto S, Ishikawa Y, Mizobe F, Nomura M, Arima D, Kunii H, Yuasa R, Yamanaka T, Tanabe S, Nagata SI, Yamada M, Leung GN. The use of osilodrostat, developed as a medication for Cushing's disease but categorized as an anabolic agent, is banned in horses by both the International Federation of Horseracing Authorities and the Fédération Equestre Internationale. For doping control purposes, elimination profiles of hydrolyzed osilodrostat in horse urine were established and the detectability of free forms of osilodrostat and its major metabolite, mono-hydroxylated osilodrostat (M1c), was investigated. Post-administration urine samples obtained from a gelding and three mares were analyzed to establish the eliminatio...
Exploring the Dissolution, Solid-state Properties, and Long-term Storage Stability of Cryoprotectant-free Fenbendazole Nanoparticles.
AAPS PharmSciTech    August 28, 2024   Volume 25, Issue 7 199 doi: 10.1208/s12249-024-02921-8
Bedogni G, Michelena LV, Seremeta K, Okulik N, Salomon C.Fenbendazole is an antiparasitic drug widely used in veterinary medicine to treat parasitic infections caused in animals like cattle, horses, sheep, and dogs. Recently, it has been repositioned as a potential alternative for cancer treatment. However, it is a highly hydrophobic molecule (0.9 ug/mL), which can compromise its dissolution rate and absorption. Thus, this work aimed to apply a nanotechnological approach to improve drug solubility and dissolution performance. Fenbendazole nanoparticles stabilized by different poloxamers were obtained by lyophilization without cryoprotectants. The be...
Bupivacaine and liposomal bupivacaine do not produce prolonged perineural anesthesia in a lameness model and are detectable beyond clinical effect in conditioned Thoroughbreds.
American journal of veterinary research    August 23, 2024   1-9 doi: 10.2460/ajvr.24.06.0167
McCarrel TM, Cole C, Maxwell LK, Roe HA, Morton AJ.To determine (1) the dose of liposomal bupivacaine (LB) to eliminate grade 2 of 5 lameness, the (2) duration of analgesia of LB versus bupivacaine hydrochloride (BH), and (3) LB pharmacokinetics versus BH. Methods: A reversible lameness model was validated in conditioned Thoroughbred horses (n = 12), aged 3 to 10 years. A dose-response trial compared subjective and objective lameness following abaxial sesamoid block with 25 mg BH/nerve or 30, 60, or 133 mg LB/nerve (n = 3/group). The LB dose that eliminated lameness and reduced lameness for the longest was used for blinded, randomized, crossov...
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