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.
Hooser SB.Incidences of feed contamination are rare even though enormous amounts of animal feed are manufactured. However, there are still some cases of feed-related illness in horses. Veterinarians play a crucial role in recognizing and mitigating these events and in assessing the severity of risks. Due to these risks, proper reporting and consultation with government and state agencies are crucial. Accurate diagnosis and identification of the source of poisoning are promising when a thorough case workup is performed and agencies such as veterinary diagnostic laboratories and the US Food and Drug Admin...
Andersen C, Jacobsen S, Uvebrant K, Griffin JF, Vonk LA, Walters M, Berg LC, Lundgren-Åkerlund E, Lindegaard C.Integrin α10β1-selected mesenchymal stem cells (integrin α10-MSCs) have previously shown potential in treating cartilage damage and osteoarthritis (OA) and in animal models . The aim of this study was to further investigate disease-modifying effects of integrin α10-MSCs. Methods: OA was surgically induced in 17 horses. Eighteen days after surgery, horses received 2 × 10 integrin α10-MSCs intra-articularly or were left untreated. Lameness and response to carpal flexion was assessed weekly along with synovial fluid (SF) analysis. On day 52 after treatment, horses were euthanized, and carp...
Hedberg Alm Y, Halvarsson P, Martin F, Osterman-Lind E, Törngren V, Tydén E.Consisting of approximately 50 different species, the cyathostomin parasites are ubiquitous in grazing horses. Co-infection with several species is common, and large burdens can cause the fatal disease of larval cyathostominosis. Due to intense anthelmintic drug use, cyathostomin resistance has developed to all available anthelmintic drug groups. Resistance to the anthelmintic drug pyrantel (PYR) has been documented in over 90% of studies published over the past two decades. In Sweden, a study performed in the early 2000s only confirmed resistance in 4.5% of farms. Further, prescription-only a...
Webster A, Pezzanite L, Hendrickson D, Griffenhagen G.Equine practitioners frequently inject local anaesthetics (LA) intra-articularly in both diagnosis of lameness and for pain management intra- or post-operatively with synovial endoscopy. Recent reviews of the human and veterinary literature support the concept that chondrotoxicity of LA on joint tissues depends on the type of drug, dose administered, and duration of exposure. The purpose of this review is to summarise the current literature describing intra-articular local anaesthetic use, including both in vitro and in vivo studies, and to draw some comparisons to literature from other specie...
Citarella G, Heitzmann V, Ranninger E, Bettschart-Wolfensberger R.This systematic review aimed to identify the evidence concerning the analgesic efficacy of non-steroidal anti-inflammatory drugs to treat abdominal pain in horses, and to establish whether one non-steroidal anti-inflammatory drug could provide better analgesia compared to others. This systematic review was conducted following the "Systematic Review Protocol for Animal Intervention Studies". Research published between 1985 and the end of May 2023 was searched, using three databases, namely, PubMed, Embase, and Scopus, using the words equine OR horse AND colic OR abdominal pain AND non-steroidal...
Knych HK, Katzman S, McKemie DS, Arthur RM, Blea J.Lidocaine is a local anesthetic that is sometimes administered in combination with epinephrine. The addition of epinephrine increases the time lidocaine remains at the site of administration, thus prolonging the duration of effect. Due to their potential to prevent the visual detection of lameness, the administration of local anesthetics is strictly regulated in performance and racehorses. Recent reports of positive regulatory findings for lidocaine in racehorses suggests a better understanding of the behavior of this drug is warranted. The objective of the current study was to describe serum ...
Lindåse S, Nostell K, Forslund A, Bergsten P, Bröjer J.Decreasing hyperinsulinemia is crucial in preventing laminitis in insulin dysregulated (ID) horses. Complementary pharmacological treatments that efficiently decrease postprandial hyperinsulinemia in ID horses are needed. Objective: Compare short-term effects of canagliflozin vs placebo on glucose and insulin responses to an oral sugar test (OST) as well as the effects on body weight and triglyceride concentrations in horses with ID. Methods: Sixteen privately-owned ID horses. Methods: A single-center, randomized, double-blind, placebo-controlled, parallel design study. The horses were randomi...
Scantamburlo G, Nofziger C, Paulmichl M, Vanoni S.Because of their importance as companion animals or as racehorses, horses can be treated with various drugs. Although it is known that drug withdrawal times can vary for each horse, pharmacogenetics for these animals has not been adequately studied and requires further development. Since is responsible for the metabolism of 25-30% of drugs in humans, including some used to treat horses, a study of the family in horses was conducted to define its genetic structure as well as its expression pattern in the liver. Unassigned: Genomic DNA extracted from venous blood and mRNA from fresh liver tiss...
Schneider ST, Isbrandt R, Gehlen H, Langkabel N, Meemken D.The 'positive list for equines' (Regulation (EC) No 1950/2006) was implemented in the European Union in 2006. The drugs listed are approved for use in slaughter equines under certain conditions, although those drugs are not approved for use in livestock and are not listed in Table 1 of the annex to Regulation (EU) No 37/2010. The usage of such drugs has to be documented in the equine passport and a withdrawal period of six months must be adhered to before the equine can be slaughtered for human consumption. Since the withdrawal period is long, correct documentation is particularly important. T...
Flood J, Byrne D, Bauquier J, Agne GF, Wise JC, Medina-Torres CE, Wood K, Sullivan O, Stewart AJ.Right dorsal colitis (RDC) is a nonsteroidal anti-inflammatory drug (NSAID) induced, protein losing enteropathy in horses associated with a high case fatality rate. Objective: To describe signalment, NSAID usage, clinical presentations, clinical pathology, ultrasonographic findings, treatments, outcomes, and factors associated with survival in horses diagnosed with RDC. Methods: Thirty-five horses from 7 Australian equine hospitals diagnosed with RDC. Methods: Retrospective case series. Clinical records of cases were accepted if definitively or presumptively diagnosed by an internist with RDC ...
Kikuchi M, Ishige T, Minamijima Y, Hirota KI, Nagata SI, Tozaki T, Kakoi H, Ishiguro-Oonuma T, Kizaki K.Circulating microRNAs (miRNAs) are stable in bodily fluids and are potential biomarkers of various diseases and physiological states. Although several studies have been conducted on humans to detect drug doping by miRNAs, research on drugs and miRNAs in horses is limited. In this study, circulating miRNAs in horses after hydrocortisone administration were profiled and variations in miRNAs affected by hydrocortisone administration during endogenous hydrocortisone elevation were examined. The miRNAs were extracted from thoroughbred horse plasma before and after hydrocortisone administration and ...
Page AE, Johnson M, Parker JL, Jacob O, Swan M, Adam E.The use of dexamethasone to control equine asthma is a common and effective treatment. Although short-term systemic dexamethasone treatment has not been shown to induce systemic immunosuppression in the horse, the goal of this study was to determine whether inhaled ciclesonide, an FDA-approved drug for the treatment of equine asthma, exerts any systemic immunosuppressive effects when compared to dexamethasone-treated and untreated horses. Eighteen light, mixed breed horses, ranging in age from 3 to 8 years of age, were used for this study and randomly assigned to one of three treatment groups:...
Sundra T, Gough S, Rossi G, Kelty E, Rendle D.Oral omeprazole is the accepted treatment for equine squamous gastric disease (ESGD); however, it is not universally effective. Esomeprazole results in more consistent and pronounced acid suppression in men and is more effective than omeprazole in the treatment of oesophageal and gastric disease. Pharmacodynamic and pilot clinical studies have indicated esomeprazole might also be more effective than omeprazole in horses. Objective: To compare the efficacy and safety of oral esomeprazole and omeprazole pastes in the treatment of ESGD and, where present, concurrent equine glandular gastric disea...
Araújo RA, Sales NAA, Basile RC, Feringer-Junior WH, Apparício M, Ferraz GC, Queiroz-Neto A.Firocoxib is a non-steroidal anti-inflammatory drug specifically formulated for veterinary medicine and selectively acts on inhibiting the cyclooxygenase 2 enzyme (COX-2). This study evaluated the possible adverse effects of administering oral therapeutic firocoxib on gastric mucosa, hematological parameters, coagulation cascade, and hepatic and renal biochemistry in healthy horses. Nine clinically healthy Arabian horses, approximately 9 years old, received 0.1 mg/kg of oral firocoxib for 14 days. The gastroscopic examination was conducted 1 day before starting treatment (D0) and two days afte...
Ishii H, Shibuya M, Kusano K, Sone Y, Kamiya T, Wakuno A, Ito H, Miyata K, Yamada M, Leung GN.Vadadustat is a newly launched hypoxia-inducible factor stabilizer with anti-anemia and erythropoietic effects; however, its use in horses is expressly forbidden in both racing and equestrian competitions. Following our previous report on the pharmacokinetic study of vadadustat in horse plasma and urine, a long-term longitudinal analysis of vadadustat in horse hair after nasoesophageal administration (3 g/day for 3 days) to three thoroughbred mares is described in this study. Our main objective is to further extend the detection period of vadadustat for the purpose of doping control. Three...
Flores L, Hargrave S, Clifford A, Alarcio G, Moeller BC.The abuse of prohibited agents including peptides and basic small-molecule drugs is an area of great concern in horseracing due to their high potential to act as doping agents. These compound classes include agents such as growth hormone-releasing peptides, peptide analgesics, beta-2-adrenergic receptor agonists, and quaternary ammonium drugs that can be challenging to detect and regulate because of their chemical properties and potential rapid elimination following administration. The use of highly sensitive and selective analytical techniques such as liquid chromatography-mass spectrometry (...
Colmer SF, Adams AA, Adam E, Miller R, Stefanovski D, Kulp JC, van Eps A.A single dose of metformin administered 1 h prior to oral glucose challenge was previously shown to reduce insulinaemic responses in horses with experimentally-induced insulin dysregulation (ID). Targeted administration could be useful for controlling post-prandial hyperinsulinaemia in horses with naturally-occurring ID.
Ortega McCormack JJ, Reed RA, Epstein KL, Camus MS, Knych HK.To determine if transdermally delivered fentanyl can achieve greater concentrations of fentanyl in synovial fluid when applied over a synovial structure. Conclusion: Application of fentanyl matrix patches directly over the CMCJ did not result in increased fentanyl concentrations in the synovial fluid of the treated intercarpal joint in normal horses.
Hobbs K, Luethy D, Davis J, Mallicote M, Torcivia C, Kulp J, Stefanovski D, Futterman C, Cooper F, van Eps A.Trazodone, a serotonin receptor antagonist and reuptake inhibitor, might be a useful adjunctive treatment in the initial management of horses with acute laminitis if it minimizes ambulation or encourages recumbency. Objective: (1) Evaluate the effects of PO trazodone on ambulatory activity and recumbency in healthy horses; and (2) assess the pharmacokinetics of multiple PO doses of trazodone. Methods: In a randomized cross-over design, 8 healthy horses received placebo or trazodone at 2 doses (2.5 and 7.5 mg/kg) PO q12h for 48 hours with a 14-day washout period between treatments. Forelimb...
Faivre C, Wong DM, Villarino NF, Court M, Gold JR.To determine the pharmacokinetics and clinical safety of acetaminophen after oral administration of 40 mg/kg q 12 hours or 60 mg/kg q 24 hours for 14 days. Methods: 12 healthy light-breed neonatal foals. Methods: 6 foals received acetaminophen at 40 mg/kg q 12 hours and 6 foals received 60 mg/kg q 24 hours for 14 days. The study dates were January 31 to April 15, 2023. Physical examinations were performed daily. Plasma disposition of acetaminophen was determined after the first, mid-point drug administration. Hematology and biochemistry analysis was performed before the study, day 7, and the l...
Ishii H, Shibuya M, Kusano K, Sone Y, Kamiya T, Wakuno A, Ito H, Miyata K, Yamada M, Leung GN.Daprodustat is a hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) inhibitor and is used as an erythropoiesis stimulant for the treatment of anemia in humans. In general, administering daprodustat to horses will result in a lifetime ban from both equestrian sports and horseracing by the International Federation of Horseracing Authorities and the Fédération Équestre Internationale, respectively. To control the misuse/abuse of daprodustat, we conducted nasoesophageal administration of daprodustat (100 mg/day for 3 days) to three thoroughbred mares and the post-administration hair ...
Vergara-Hernandez FB, Nielsen BD, Kottwitz JJ, Panek CL, Robison CI, Paris BL, Welsh TH, Bradbery AN, Leatherwood JL, Colbath AC.To determine the single-dose pharmacokinetics of clodronate disodium (CLO) in juvenile sheep and the plasma protein binding (PPB) of CLO in juvenile sheep and horses. Methods: 11 juvenile crossbred sheep (252 ± 6 days) for the pharmacokinetic study. Three juvenile crossbred sheep (281 ± 4 days) and 3 juvenile Quarter Horses (599 ± 25 days) for PPB analysis. Methods: CLO concentrations were determined using liquid chromatography-mass spectrometry. Pharmacokinetic parameters were calculated by noncompartmental analysis from plasma samples obtained at 0, 0.5, 1, 3, 6, 12, 24, 48, and 72 hours ...
Bello K, Lorch G, Kim K, Toribio RE, Yan L, Xie Z, Hill K, Phelps M.Additional efficacious immunomodulatory treatment is needed for the management of immune-mediated disease in horses. Mycophenolate mofetil (MMF) is an immunosuppressive drug that warrants assessment as a viable therapeutic agent for horses. Objective: To evaluate the pharmacokinetics (PK) of multiple-day oral dosing of MMF in healthy horses and to determine the tolerability of this dosing regimen. Methods: Six healthy Standardbred mares. Methods: Horses received MMF 10 mg/kg PO q12h for 7 days in the fed state. Serial sampling was performed over 12 hours on Days 1 and 7 with trough sampl...
Scala E, van Galen G, Skärlina EM, Durie I.Pyelonephritis is a serious condition that is rarely described in horses. In contrast, urinary tract infections are common in humans and small animals, and multi-drug-resistant urinary infections are an emerging threat. In this report, we describe a horse with unilateral pyelonephritis caused by extended-spectrum beta-lactamase-producing bacteria belonging to the Enterobacter cloacae complex. [Correction added on 9 August 2023, after first online publication: The preceding sentence was corrected.] An 11-year-old Swedish warmblood gelding was diagnosed with a cystolith and a cystotomy through a...
Pearson GB, Papa B, Mosaddegh A, Cooper H, Aprea M, Pigott J, Altier C, Cazer CL, Reesink HL.To investigate (1) variables associated with the likelihood of obtaining a positive culture, (2) commonly isolated microorganisms, and (3) antimicrobial resistance patterns of isolates from horses with presumptive synovial sepsis. Methods: Synovial fluid, synovium, and bone samples from equine cases with presumptive synovial sepsis submitted to the Cornell University Animal Health Diagnostic Center from 2000 to 2020 for microbial culture and antimicrobial sensitivity testing. Methods: Univariable and multivariable analyses were performed to determine the effect of variables on the likelihood o...
Chen Q, Wang Z, Chen H.Aromatase inhibitors (AIs) can indirectly cause increased testosterone in animals, which leads to the improvement of the athletic ability of horses. For the protection of horses and the consideration of fair competition, AIs were listed as prohibited drugs by the Federation Equestre Internationale (FEI). There were several disadvantages using traditional pretreatment methods before analyzing these drugs from biological samples. A rapid and green pretreatment method has been developed by utilizing the hydrophobic deep eutectic solvent (DES)-based vortex-assisted liquid-liquid microextraction (D...
Knych HK, McKemie DS, Kass PH, Stanley SD, Blea J.Ketoprofen is an anti-inflammatory drug that is commonly administered to racehorses for the alleviation of musculoskeletal pain and inflammation. This study represents a comprehensive examination of the metabolism (in vivo and in vitro), pharmacokinetics and ex vivo pharmacodynamics, of ketoprofen in horses. The in vitro metabolism as well as specific enzymes responsible for metabolism was determined by incubating liver microsomes and recombinant CYP450 and UGT enzymes with ketoprofen. For the in vivo portion, 15 horses were administered a single intravenous dose of 2.2-mg/kg ketoprofen. Blood...
Gold JR, Grubb T, Court MH, Villarino NF.Acetaminophen is utilized in human infants for pain management and fever. Neonatal foals might benefit from administration of acetaminophen but effective and safe dosage regimens for neonatal foals remains to be determined. Unassigned: The objective was to determine the plasma pharmacokinetics of acetaminophen following oral administration of a single dose of 20 mg/kg or 40 mg/kg to neonatal foals. A secondary objective was to evaluate any changes in hematology and biochemistry profiles. Unassigned: Randomized study. Unassigned: Eight clinically healthy 7-9-day old Quarter Horse foals (3 c...
Wong KS, Cheung HW, Choi YC, To NS, Wan TSM, Ho ENM.Recombinant human follistatin (rhFST) is a potential performance-enhancing agent owing to its stimulating effect on muscle growth. Administration of rhFST to athletes is prohibited in human sports by the World Anti-Doping Agency (WADA) and in horseracing according to Article 6 of the International Agreement on Breeding, Racing and Wagering published by the International Federation of Horseracing Authorities (IFHA). For effective control of the potential misuse of rhFST in flat racing, methods for screening and confirmatory analysis are required. This paper describes the development and validat...
Sánchez de Medina A, Serrano-Rodríguez JM, Díez de Castro E, García-Valverde MT, Saitua A, Becero M, Muñoz A, Ferreiro-Vera C....Intravenous pharmacokinetics and oral bioavailability of cannabidiol (CBD) with different formulations have not been investigated in horses and may represent a starting point for clinical studies. Objective: To describe pharmacokinetics after intravenous and oral administrations with oil and micellar formulations and simulate different treatments. Methods: Single intravenous experiment and two-way randomised oral experiments, Latin-square design. Methods: Eight healthy horses received intravenous CBD at 1.00 mg/kg dose, oral CBD in sesame oil and in micellar formulation, both at 10.00 mg/k...
Haugaard MM, Pehrson S, Carstensen H, Flethøj M, Hesselkilde EZ, Praestegaard KF, Diness JG, Grunnet M, Jespersen T, Buhl R.Only few pharmacologic compounds have been validated for treatment of atrial fibrillation (AF) in horses. Studies investigating the utility and safety of flecainide to treat AF in horses have produced conflicting results, and the antiarrhythmic mechanisms of flecainide are not fully understood. Objective: To study the potential of flecainide to terminate acutely induced AF of short duration (≥ 15 minutes), to examine flecainide-induced changes in AF duration and AF vulnerability, and to investigate the in vivo effects of flecainide on right atrial effective refractory period, AF cycle length...
Natalini CC, Robinson EP.To evaluate and compare effects of epidurally administered morphine, alfentanil, butorphanol, tramadol, and U50488H on avoidance threshold to noxious electrical stimulation over the dermatomes of the perineal, sacral, lumbar, and thoracic regions in horses. Methods: 5 healthy adult horses. Methods: Using a Latin square complete repeated-measures design, horses were randomly assigned to receive 1 of 6 treatments (morphine, alfentanil, butorphanol, tramadol, U50488H, or sterile water) at intervals of at least 7 days. Agents were injected epidurally at the first intercoccygeal epidural space, and...
Schnepf A, Bienert-Zeit A, Ertugrul H, Wagels R, Werner N, Hartmann M, Feige K, Kreienbrock L.The usage of antimicrobial drugs (AMs) leads to an increase in antimicrobial resistance (AMR). Although different antimicrobial usage (AMU) monitoring programs exist for livestock animals in Germany, there is no such system for horses. However, with the increasing usage of electronic practice management software (EPMS), it is possible to analyze electronic field data generated for routine purposes. The aim of this study was to generate AMU data for German horses with data from the Clinic for Horses (CfH), University of Veterinary Medicine Hannover (TiHo), and in addition to show that different...
Hustace JL, Firshman AM, Mata JE.To determine pharmacokinetics and oral bioavailability of metformin in healthy horses. Methods: 4 adult horses. Methods: 6 g of metformin was administered 3 times IV and PO (fed and unfed) to each horse, by use of a crossover design, with a 1-week washout period between treatments. Plasma metformin concentration was determined via high-pressure liquid chromatography. Results: Mean +/- SD distribution half-life of metformin following IV administration was 24.9 +/- 0.4 minutes with a volume of distribution of 0.3 +/- 0.1 L/kg. Mean area under the curve was 20.9 +/- 2.0 h.microg/mL for IV adminis...
Charvet CL, Guégnard F, Courtot E, Cortet J, Neveu C.The control of parasitic nematodes impacting animal health relies on the use of broad spectrum anthelmintics. However, intensive use of these drugs has led to the selection of resistant parasites in livestock industry. In that respect, there is currently an urgent need for novel compounds able to control resistant parasites. Nicotine has also historically been used as a de-wormer but was removed from the market when modern anthelmintics became available. The pharmacological target of nicotine has been identified in nematodes as acetylcholine-gated ion channels. Nicotinic-sensitive acetylcholin...
Clarke KW, Paton BS.The effects of administration of one of four opiates (pethidine 1 mg/kg bodyweight (bwt), morphine 0.1 mg/kg bwt, methadone 0.1 mg/kg bwt, and butorphanol 0.05 mg/kg bwt) given intravenously to horses and ponies already sedated with detomidine (10 micrograms/kg bwt) were investigated. Behavioural, cardiovascular and respiratory effects of the combinations were compared with those occurring with detomidine alone. Addition of the opiate increased the apparent sedation and decreased the response of the animal to external stimuli. At doses used, butorphanol produced the most reliable response. Sid...
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 ...
Díaz-Bertrana ML, Deleuze S, Pitti Rios L, Yeste M, Morales Fariña I, Rivera Del Alamo MM.Endometritis is one of the main causes of infertility in mares. In the present study, 363 mares with a history of repetitive infertility, and positive endometrial cytology and/or vaginal discharge were included. An endometrial swab for microbiological purposes plus sensitivity test was obtained from each mare. A positive culture was obtained in 89% of mares. The main isolated genera were (25.1%), (18.2%), (17.3%) and (12.1%). With regard to species, the most isolated microorganism was (17.3%), spp. (15.6%) and spp. (13.5%). Sensitivity tests showed that the most efficient antimicrobial ...
Klöppel H, Leece EA.To compare alfaxalone with ketamine for total intravenous anaesthesia in ponies undergoing castration. Methods: Prospective, randomised, blinded clinical study. Methods: Forty-two, 12-month-old Welsh Mountain ponies. Methods: Ponies were assigned randomly to receive ketamine or alfaxalone. After administration of romifidine 100 μg kg(-1) and butorphanol 50 μg kg(-1) intravenously (IV), sedation and response to tactile stimulation were scored. If sedation was insufficient, romifidine 30 μg kg(-1) was administered IV. Anaesthesia was induced with ketamine 2.2 mg kg(-1) or alfaxalone 1 mg kg(-...
Costa GL, Cristarella S, Quartuccio M, Interlandi C.To evaluate the anti-nociceptive and sedative effects of slow intravenous (IV) injection of tramadol, romifidine, or a combination of both drugs in ponies. Methods: Within-subject blinded. Methods: Twenty ponies (seven male, 13 female, weighing mean ± SD 268.0 ± 128 kg). Methods: On separate occasions, each pony received one of the following three treatments IV; romifidine 50 μg kg(-) (R) tramadol 3 mg kg(-1) given over 15 minutes (T) or tramadol 3 mg kg(-1) followed by romifidine 50 μg kg(-1) (RT). Physiologic parameters and caecal borborygmi (CB) were measured and sedation ...
Terry RL, McDonnell SM, Van Eps AW, Soma LR, Liu Y, Uboh CE, Moate PJ, Driessen B.Gabapentin is being used in horses although its pharmacokinetic (PK) profile, pharmacodynamic (PD) effects and safety in the equine are not fully investigated. Therefore, we characterized PKs and cardiovascular and behavioral effects of gabapentin in horses. Gabapentin (20 mg/kg) was administered i.v. or p.o. to six horses using a randomized crossover design. Plasma gabapentin concentrations were measured in samples collected 0-48 h postadministration employing liquid chromatography-tandem mass spectrometry. Blood pressures, ECG, and sedation scores were recorded before and for 12 h after gaba...
Guedes AGP, Aristizabal F, Sole A, Adedeji A, Brosnan R, Knych H, Yang J, Hwang SH, Morisseau C, Hammock BD.This study determined the pharmacokinetics, antinociceptive, and anti-inflammatory effects of the soluble epoxide hydrolase (sEH) inhibitor t-TUCB (trans-4-{4-[3-(4-Trifluoromethoxy-phenyl)-ureido]-cyclohexyloxy}-benzoic acid) in horses with lipopolysaccharide (LPS)-induced radiocarpal synovitis. A total of seven adult healthy mares (n = 4-6/treatment) were administered 3 μg LPS into one radiocarpal joint and t-TUCB intravenously (i.v.) at 0 (control), 0.03, 0.1, 0.3, and 1 mg/kg in a blinded, randomized, crossover design with at least 3 weeks washout between. Two investigators independe...
Brophy PM, MacKintosh N, Morphew RM.Anthelmintics are the cornerstone of parasitic helminth control. Surprisingly, understanding of the biochemical pathways used by parasitic helminths to detoxify anthelmintics is fragmented, despite the increasing global threat of anthelmintic resistance within the ruminant and equine industries. Reductionist biochemistry has likely over-estimated the enzymatic role of glutathione transferases in anthelmintic metabolism and neglected the potential role of the cytochrome P-450 superfamily (CYPs). Proteomic technologies offers the opportunity to support genomics, reverse genetics and pharmacokine...
Rezende ML, Grimsrud KN, Stanley SD, Steffey EP, Mama KR.The aim of the study was to describe the pharmacokinetics and selected pharmacodynamics of intravenous dexmedetomidine in horses. Eight adult horses received 5 μg/kg dexmedetomidine IV. Blood samples were collected before and for 10 h after drug administration to determine dexmedetomidine plasma concentrations. Pharmacokinetic parameters were calculated using noncompartmental analysis. Data from one outlier were excluded from the statistical summary. Behavioral and physiological responses were recorded before and for 6 h after dexmedetomidine administration. Dexmedetomidine concentrations dec...
Makhaeva GF, Lushchekina SV, Kovaleva NV, Yu Astakhova T, Boltneva NP, Rudakova EV, Serebryakova OG, Proshin AN, Serkov IV, Trofimova TP, Tafeenko VA....We synthesized eleven new amiridine-piperazine hybrids 5a-j and 7 as potential multifunctional agents for Alzheimer's disease (AD) treatment by reacting N-chloroacetylamiridine with piperazines. The compounds displayed mixed-type reversible inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Conjugates were moderate inhibitors of equine and human BChE with negligible fluctuation in anti-BChE activity, whereas anti-AChE activity was substantially dependent on N4-substitution of the piperazine ring. Compounds with para-substituted aromatic moieties (5g, 5h, and bis-amirid...
Merritt AM, Burrow JA, Hartless CS.To evaluate the effect on equine duodenal motility of some analgesic agents commonly used to treat colic. Methods: 4 healthy adult healthy horses--2 mares and 2 geldings--which were carrying an indwelling gastric cannula made of silastic rubber. One horse also carried 2 long-term indwelling bipolar electrodes that had been sutured onto the duodenum and jejunum. Methods: To ensure an empty stomach, solid food was withheld from horses for around 20 hours prior to an experiment. Using videoendoscopic guidance, an 8-F catheter with 3 small, discrete pressure sensors was passed through the gastric ...
Silva MG, Bastos RG, Stone Doggett J, Riscoe MK, Pou S, Winter R, Dodean RA, Nilsen A, Suarez CE.The most common apicomplexan parasites causing bovine babesiosis are Babesia bovis and B. bigemina, while B. caballi and Theileria equi are responsible for equine piroplasmosis. Treatment and control of these diseases are usually achieved using potentially toxic chemotherapeutics, such as imidocarb diproprionate, but drug-resistant parasites are emerging, and alternative effective and safer drugs are needed. The endochin-like quinolones (ELQ)-300 and ELQ-316 have been proven to be safe and efficacious against related apicomplexans, such as Plasmodium spp., with ELQ-316 also being effective aga...
Johnson CB, Taylor PM.We have investigated in eight ponies the effects of three different end-tidal concentrations of halothane, isoflurane and methoxyflurane on median (F50) and 95% spectral edge (F95) frequencies of the EEG and the second differential (DD) of the middle latency auditory evoked potential (MLAEP). The three concentrations of each agent were chosen to represent approximately the minimum alveolar concentration (MAC), 1.25 MAC and 1.5 MAC for each agent. During halothane anaesthesia, F95 decreased progressively as halothane concentration increased, from mean 13.9 (SD 2.6) at 0.8% to 11.9 (1.1) at 1.2%...
Sellon DC, Monroe VL, Roberts MC, Papich MG.To determine an infusion rate of butorphanol tartrate in horses that would maintain therapeutic plasma drug concentrations while minimizing development of adverse behavioral and gastrointestinal tract effects. Methods: 10 healthy adult horses. Methods: Plasma butorphanol concentrations were determined by use of high-performance liquid chromatography following administration of butorphanol by single IV injection (0.1 to 0.13 mg/kg of body weight) or continuous IV infusion (loading dose, 17.8 microg/kg; infusion dosage, 23.7 microg/kg/h for 24 hours). Pharmacokinetic variables were calculated, a...
Schott HC, Ewart SL, Walker RD, Dwyer RM, Dietrich S, Eberhart SW, Kusey J, Stick JA, Derksen FJ.Between May 1996 and February 1997, 27 horses and a veterinary student at a veterinary teaching hospital developed apparent nosocomial Salmonella Typhimurium infection. The source of the multiple-drug resistant Salmonella Typhimurium was a neonatal foal admitted for treatment of septicemia. A high infection rate (approx 13% of hospitalized horses) coupled with a high case fatality rate (44%) for the initial 18 horses affected led to a decision to close the hospital for extensive cleaning and disinfection. Despite this effort and modification of hospital policies for infection control, 9 additi...
Gough MR, Thibaud D, Smith RK.Tiludronate regulates bone remodelling through a decrease of the resorptive process and should therefore ameliorate the remodelling processes active in osteoarthritis of the distal tarsal joints ('bone spavin') and alleviate pain associated with abnormal bone lysis. Objective: To confirm the efficacy of tiludronate, administered as a single infusion at a dose of 1 mg/kg bwt, in the treatment of bone spavin in the horse. Methods: A double blind placebo controlled trial on 108 clinical cases of bone spavin was undertaken. The lameness score of the lamest limb was assessed following distal tarsal...
Okamura K, Sasaki N, Yamada M, Yamada H, Inokuma H.Although extensive work has been done to elucidate the beneficial and unfavorable effects of gastrointestinal prokinetic agents in humans, little is known on the effects of these agents in horses. In this study, we compared the effects of mosapride, metoclopramide, cisapride, and lidocaine on equine gastric emptying, jejunal and caecal motility and evaluated these agents' adverse drug reactions (ADRs). Methods: Seven healthy adult Thoroughbreds. Methods: Mosapride 1.0mg/kg and 2.0mg/kg, metoclopramide 0.2mg/kg, and cisapride 1.0mg/kg were dissolved in 100mL distilled water for oral administrat...
Toutain PL, Lassourd V.The current performance of analytical techniques used for drug control in horses lead the Regulatory Authorities to decide whether trace levels of drugs legitimately used for therapeutic medication should or should not be reported. Here, we propose a well-ordered and nonexperimental pharmacokinetic/pharmacodynamic approach for the determination of irrelevant drug plasma (IPC) and urine concentrations (IUC). The published plasma clearance is used to transform an effective (marketed) dose into an effective concentration (EPC). EPC is transformed into an IPC by applying a safety factor (SF). This...
Noble G, Edwards S, Lievaart J, Pippia J, Boston R, Raidal SL.Safety of meloxicam, a potent NSAID with selective COX-2 inhibition, has not been evaluated in horses. Objective: To evaluate pharmacokinetics and safety of single and repeated oral doses of meloxicam in adult horses. Methods: Forty-nine healthy, university-owned adult lightbreed horses. Methods: Study conducted in 2 parts. Part I addressed pharmacokinetics of single oral dose meloxicam (0.6 mg/kg) in 16 horses. Part II, 33 horses were randomly assigned to 5 treatment groups to assess prolonged administration (0.6 mg/kg PO q24h for 6 weeks, n = 7) or higher doses (1.8 mg/kg, n = 7, or 3.0 mg/k...
Jinks MR, Miller EJ, Diaz-Campos D, Mollenkopf DF, Newbold G, Gemensky-Metzler A, Chandler HL.To identify the minimum inhibitory concentration (MIC) distribution for commonly used topical antibiotics from isolates of dogs and horses with ulcerative bacterial keratitis, and to investigate changes in MIC values over time and following treatment with topical fluoroquinolones. Methods: One hundred thirty-four client-owned dogs and 20 client-owned horses with bacterial ulcerative keratitis. Methods: Minimum inhibitory concentration values for 14 topical antibiotics were reported for canine and equine cases of bacterial ulcerative keratitis between 2013 and 2018. Changes in MIC values over t...
Rohrbach H, Korpivaara T, Schatzmann U, Spadavecchia C.To evaluate and compare the antinociceptive effects of the three alpha-2 agonists, detomidine, romifidine and xylazine at doses considered equipotent for sedation, using the nociceptive withdrawal reflex (NWR) and temporal summation model in standing horses. Methods: Prospective, blinded, randomized cross-over study. Methods: Ten healthy adult horses weighing 527-645 kg and aged 11-21 years old. Methods: Electrical stimulation was applied to the digital nerves to evoke NWR and temporal summation in the left thoracic limb and pelvic limb of each horse. Electromyographic reflex activity was reco...
Whitfield-Cargile CM, Chamoun-Emanuelli AM, Cohen ND, Richardson LM, Ajami NJ, Dockery HJ.Non-steroidal anti-inflammatory drugs (NSAIDs) are routinely used in both veterinary and human medicine. Gastrointestinal injury is a frequent adverse event associated with NSAID use and evidence suggests that NSAIDs induce gastrointestinal microbial imbalance (i.e., dysbiosis) in both animals and people. It is unknown, however, whether cyclooxygenase (COX)-2-selective NSAIDs induce dysbiosis, or if this phenomenon occurs in horses administered any class of NSAIDs. Therefore, our objectives were to determine whether the composition and diversity of the fecal microbiota of adult horses were alt...
