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.
Cabler P, Geddes LA, Rosborough J.Ultrasonic energy, provided by a commercially available water vaporizer, was used to vaporize methoxyflurane, halothane, and chloroform. The vaporizer was placed directly in the respiratory line, and the anaesthetic liquid was vaporized one drop at a time. Anaesthesia was maintained for periods up to 6 hr in horses, ponies, calves, sheep, dogs, and one pig. This method of vaporizing liquids is applicable to a wide variety of anaesthetics. It is easily controlled, and the same vaporizer can be used with a wide range of sizes of subjects. The vaporizer can be placed directly in the respiratory c...
Drudge JH, Lyons ET, Tolliver SC.Three formulations of cambendazole were evaluated for anthelmintic activity by critical testing method in 21 horses. Cambendazole suspension was administered via stomach tube at the dose rate of 10 mg/kg to 3 horses and at the dose rate of 20 mg/kg to 3 horses. Cambendazole paste was given intraorally to 8 horses, and the pellet formulation was fed to 7 horses at the dose rate of 20 mg/kg. Anthelmintic activity of cambendazole was similar for all dose rates and formulations. Gasterophilus intestinalis, Gasterophilus nasalis, Draschia megastoma, Anoplocephala perfoliata, and Anoplocephala magna...
Sisodia CS, Kramer LL, Gupta VS, Lerner DJ, Taksas L.Pharmacological disposition of chloramphenicol was studied in horses. Minimum levels of the antibiotic (greater than or equal to 5 mu g/ml) in blood or plasma recommended to combat infections could not be achieved by 4.4 and 8.8 mg/kg I.V. or 30 and 50 mg/kg I.M. or 30 mg/kg oral (as palmitate salt) doses of chloramphenicol. Increasing the dose to 19.8 and 26.4 mg/kg I.V. provided such levels for about two and three hours respectively. A combination of 20 mg/kg I.V. and 30 mg/kg I.M. administered simultaneously did not provide more prolonged levels than 26.4 mg/kg I.V. alone. Chloramphenicol s...
Hariharan H, Barnum DA, Mitchell WR.Prevalence of antimicrobial drug resistance among over 3000 clinical isolates of animal pathogens in Ontario during 1971-72 has been studied. A high number of multiple resistance patterns is prevalent among members of Enterobacteriaceae, especially Escherichia coli and Salmonella typhimurium. The most common resistance pattern among bovine strains was against not less than six drugs in common use. Among different animal species the bovine population was found to be the source of a high percentage of chloramphenicol resistant E. coli and S. typhimurium organisms. All the isolates resistant to t...
Stewart GA.The research focuses on understanding the physiological responses, mainly cardiovascular and respiratory, of racehorses during exercise and how drugs can impact these responses. The study aims to set up a […]
Kowalczyk DF, Beech J.The pharmacokinetics of the anti-convulsant phenytoin were investigated in clinically healthy horses after oral (p.o.) and intravenous (i.v.) administration. A single dose of phenytoin (8.8 mg/kg body weight) was given i.v. as a bolus to nine horses and one horse received 13.2 mg/kg. A two-compartment open model was used to describe the disposition of phenytoin. Four of the horses that received an i.v. dose (three at 8.8 mg/kg and one at 13.2 mg/kg) were then given the same dose 3 days later by the oral route. Phenytoin achieved a peak concentration in serum within 1-4 h after p.o. administrat...
Frey LP, Kline KH, Foreman JH.Analysis of data collected at racetracks showed that temperature, the diuretic drug, frusemide, exercise, temperature/exercise interaction and sex/age had significant (P < 0.05) effects on pH and bicarbonate ion concentration (P < 0.01). Sodium concentrations were significantly (P < 0.001) affected by temperature and frusemide. We suggest that the normal range limits for blood sodium, bicarbonate and pH used in prerace testing procedures should be adjusted for ambient temperature and for horses given frusemide and/or prerace exercise. These adjustments should improve the precision of ...
Combie J, Shults T, Nugent EC, Dougherty J, Tobin T.The locomotor responses of horses given morphine and fentanyl were blocked or lessened by administration of naloxone or acepromazine. Naloxone given at the dosage of 0.015 mg/kg completely blocked the locomotor activity induced in horses given fentanyl (0.020 mg/kg of body weight). The locomotor stimulation produced by morphine given at the dosage of 2.4 mg/kg was reduced by 75% of naloxone (0.020 mg/kg). Acepromazine partially blocked the locomotor responses to fentanyl and morphine. This blockade activity reached its peak about 30 minutes after acepromazine was given (IV) and lasted more tha...
Boyd EH, Allen WE.Plasma drug concentrations were measured after two commercially available potentiated sulphonamides, trimethoprim and sulfadoxine and trimethoprim and sulphadiazine, were infused daily for 2 and 3 days, respectively, into the uteri of pony mares which had been mated before ovulation. Intravenous administration of trimethoprim and sulfadoxine allowed uterine absorption of trimethoprim (23-43%) and sulfadoxine (29-34%) to be calculated. After intra-uterine administration trimethoprim and sulphadiazine were detected in the milk of a lactating mare. In order to maintain plasma concentrations likel...
Fidani M, Gamberini MC, Pasello E, Palazzoli F, Dimasi T, Montana M.A development of a rapid and sensitive LC-MS/MS method for the simultaneous detection of active ingredients of the euthanasic veterinarian drug Tanax mixture is described. The method proposed, with a retention time of few minutes (6 min) was developed for an equine serum sample with solid-phase extraction (S.P.E). This S.P.E. procedure has been revealed useful for the determination of very low concentrations of Tanax analytes (0.05-1 ng/ml). The method was validated in terms of specificity/selectivity, sensitivity, recovery and precision.
Hill DW, Hyde WG, Kind AJ, Greulich D, Hopkins S.Aramine (metaraminol bitartrate) has been found in the possession of horse trainers and veterinarians who have been investigated for possible inappropriate drug administration to racing horses. Metaraminol (3-hydroxyphenylisopropanolamine) is a sympathomimetic amine that directly and indirectly affects adrenergic receptors, with alpha effects being predominant. Because it has the potential to affect the performance of a racing horse, its use is prohibited. In the present study, methods for the detection of metaraminol were developed. Metaraminol was found to be extracted with poor recovery ( 9...
Drudge JH, Lyons ET, Tolliver SC, Kubis JE.The efficacy of oxibendazole given at dose level of 10 mg/kg of body weight was determined by 10 critical tests in foals and by 2 clinical trials in 20 foals (16 treated, 4 nontreated), with special interest in the drug activity against Parascaris equorum. The drug was uniformly efficacious (100%) against P equorum in the 10 critical-test foals, each having between 22 and 236 ascarids. Posttreatment reductions of ascarid egg counts in fecal samples were also 100% in suckling foals treated with oxibendazole given as a drench. Ascarid eggs did not reappear in fecal samples until the 8th week aft...
Cutler C, Viljanto M, Taylor P, Hincks P, Biddle S, Van Eenoo P.Selective androgen receptor modulators, SARMs, are a large class of compounds developed to provide therapeutic anabolic effects with minimal androgenic side effects. A wide range of these compounds are available to purchase online and thus provide the potential for abuse in sports. Knowledge of the metabolism of these compounds is essential to aid their detection in doping control samples. In vitro models allow a quick, cost-effective response where administration studies are yet to be carried out. In this study, the equine phase I metabolism of the non-steroidal SARMs GSK2881078, LGD-2226, LG...
Cokelaere SM, Groen WMGAC, Plomp SGM, de Grauw JC, van Midwoud PM, Weinans HH, van de Lest CHA, Tryfonidou MA, van Weeren PR, Korthagen NM.There is an increasing interest in controlled release systems for local therapy in the treatment of human and equine joint diseases, aiming for optimal intra-articular concentrations with no systemic side effects. In this study, the intra-articular tolerability and suitability for local and sustained release of tacrolimus (FK506) from monospheres composed of [PDLA-PEG1000]-b-PLLA multiblock copolymers were investigated. Unloaded and tacrolimus-loaded (18.4 mg tacrolimus/joint) monospheres were injected into the joints of six healthy horses, with saline and hyaluronic acid (HA) in the contralat...
Adams SB, Lamar CH, Masty J.Bipolar stainless steel electrodes were surgically implanted in 4 ponies to record myoelectrical and mechanical activity of the distal portion of the jejunum and pelvic flexure. After determining normal activity, the effects of neostigmine, xylazine, flunixin meglumine, dipyrone, panthenol, and atropine sulfate were determined. Flunixin meglumine, dipyrone, and panthenol had no effect on the motility of the jejunum or pelvic flexure. Xylazine and atropine sulfate decreased motility of the distal portion of the jejunum and pelvic flexure, with atropine sulfate having a greater effect and lastin...
Smith ML, Chapman CB.An acepromazine (ACP) hapten was synthesised, coupled to bovine serum albumin and injected into a horse to produce antibodies to the drug. A competitive ELISA was developed whereby ACP attached to the solid phase via lysozyme competed with free ACP present in phosphate buffered saline, horse serum or horse urine for limiting amounts of antibody. The assay could detect the presence of ACP and, or, some of its metabolites in horse urine for at least 25 hours after intravenous injection of 0.1 mg kg-1 ACP maleate, but because of non-specific interference, horse serum could not be used. As little ...
Egenvall A, Nødtvedt A, Roepstorff L, Bonnett B.In a world of limited resources, using existing databases in research is a potentially cost-effective way to increase knowledge, given that correct and meaningful results are gained.Nordic examples of the use of secondary small animal and equine databases include studies based on data from tumour registries, breeding registries, young horse quality contest results, competition data, insurance databases, clinic data, prescription data and hunting ability tests. In spite of this extensive use of secondary databases, integration between databases is less common. The aim of this presentation is to...
Sams RA, Gerken DF, Dyke TM, Reed SM, Ashcraft SM.Cimetidine was administered intravenously and by the intragastric route to six mares at a dose of 4.0 mg/kg of body weight (bw). Specific and sensitive high performance liquid chromatographic methods for the determination of cimetidine in horse plasma and urine and cimetidine sulfoxide in urine are described. Plasma cimetidine concentration vs. time data were analysed by non-linear least squares regression analysis to determine pharmacokinetic parameter estimates. The median (range) plasma clearance (Cl) was 8.20 (4.96-10.2) mL/min.kg of body weight, that of the steady-state volume of distribu...
Coakley M, Peck KE, Taylor TS, Matthews NS, Mealey KL.To compare serum disposition of flunixin meglumine after i.v. administration of a bolus to horses, donkeys, and mules. Methods: 3 clinically normal horses, 5 clinically normal donkeys, and 5 clinically normal mules. Methods: Blood samples were collected at time zero (before) and 5, 10, 15, 30, and 45 minutes, and at 1, 1.25, 1.5, 1.75, 2, 2.5, 2.75, 3, 3.5, 4, 4.5, 5, 5.5, 6, and 8 hours after i.v. administration of a bolus of flunixin meglumine (1.1 mg/kg of body weight). Serum was analyzed in duplicate by the use of high-performance liquid chromatography for determination of flunixin meglumi...
Scare JA, Dini P, Norris JK, Steuer AE, Scoggin K, Gravatte HS, Howe DK, Slusarewicz P, Nielsen MK.Ascarid parasites infect a variety of hosts and regular anthelmintic treatment is recommended for all species. Parascaris spp. is the only ascarid species with widespread anthelmintic resistance, which allows for the study of resistance mechanisms. The purpose of this study was to establish an in vitro drug exposure protocol for adult anthelmintic-naïve Parascaris spp. and report a preliminary transcriptomic analysis in response to drug exposure. Live worms were harvested from foal necropsies and maintained in RPMI-1640 at 37 °C. Serial dilutions of oxibendazole (OBZ) and ivermectin (IVM) we...
Klaus AM, Hapke HJ.Drug treatment of horses which are used in horse-racing is restricted by the regulations of the anti-doping control. Veterinarians and anti-doping control commissions are faced with the problems resulting from the discrepancy between the demand "no drugs in blood/urine of horses at the time of competition" and the need for treatment. The pharmacokinetic data of important antiphlogistics/analgetics (NSAID) for horses given in this article shall facilitate the decision of the veterinarians and commissions whether a horse having been treated with NSAID may participate in a competition or not. Fur...
Stein F, Gilliam L, Davis J, Taylor J.In a randomized crossover design study, 10 adult horses were administered crushed metronidazole tablets rectally at 20 mg/kg. Horses' rectums were either evacuated (E) or not evacuated (NE) of manure prior to the administration of the drug. Serum samples were taken over 24 hr and plasma concentrations were determined via high pressure liquid chromatography. At 15 min post-administration, group E had a significantly higher plasma concentration (p = 0.027), but there were no concentration differences at any other time points. There was large variability in relative bioavailability in the NE...
Gronwall R, Brown MP.Para-aminohippuric acid (PAHA, 0.1 mg/min/kg of body weight) was infused IV into 2 mares, followed by concurrent IV infusion of PAHA and probenecid (0.075, 0.15, 0.25, or 0.35 mg of probenecid/min/kg). Probenecid infusion reduced the clearance of PAHA at serum probenecid concentrations greater than 55 micrograms/ml. At 12-hour intervals, probenecid (in 5 repeated doses - 50, 75, 100, or 200 mg/kg) was administered by gavage to 2 mares. Mean serum probenecid concentration was greater than 55 micrograms/ml for all dosages. At dosages less than 200 mg/kg, accumulation of probenecid in the serum w...
Redmond JS, Stang BV, Schlipf JW, Christensen JM.Diphenhydramine is an H1 receptor antagonist used to control urticaria and other allergic signs caused by type I hypersensitivity reactions in horses (Equus caballus). Limited studies have been conducted on pharmacokinetics of this drug in horses, with no studies involving oral formulations. Our study investigated pharmacokinetics of an oral diphenhydramine formulation compared to intravenous administration in non-fasted adult horses. Six healthy horses underwent a single administration of three different doses of diphenhydramine (1 mg/kg intravenously, 1 mg/kg intragastrically, and 5 mg/kg...
Waraksa E, Woźniak MK, Kłodzińska E, Wrzesień R, Bobrowska-Korczak B, Namieśnik J.Ibuprofen is widely used in human and veterinary medicine for the treatment of chronic pain as well as rheumatic and musculoskeletal disorders. However, the analgesic and anti-inflammatory properties of Ibuprofen have contributed to frequent drug abuse in equestrian sports. A sensitive and rapid gas chromatography with tandem mass spectrometry based method with a simple liquid-liquid extraction and derivatization requiring 200 μL volume of sample and 2 mL of extraction solvent for the simultaneous determination of ibuprofen and its metabolites was developed. The proposed procedure was optim...
Parra N, Jaume M, Boscán K, Hernández A, Mijares A, González M, Alvarado Y, Restrepo J.Trypanosoma equiperdum is the causative agent of dourine, a venereal disease in horses and donkeys. This parasite has a widely distribution, is found in Africa, Asia, Southern and Eastern Europe, Russia, Mexico and Venezuela. The T. equiperdum is morphologically indistinguishable to other Trypanozoon species, however differs from other mammalian trypanosomes due to the fact that it is primarily a tissue parasite, generating cutaneous plaques, swelling of genitalia and neurological signs. The aim of this study was to evaluate the trypanocidal effectiveness of a set of derivatives of thiosemicar...
Hariharan H, Barnum DA, Mitchell WR.Prevalence of antimicrobial drug resistance among over 3000 clinical isolates of animal pathogens in Ontario during 1971-72 has been studied. A high number of multiple resistance patterns is prevalent among members of Enterobacteriaceae, especially Escherichia coli and Salmonella typhimurium. The most common resistance pattern among bovine strains was against not less than six drugs in common use. Among different animal species the bovine population was found to be the source of a high percentage of chloramphenicol resistant E. coli and S. typhimurium organisms. All the isolates resistant to t...
Steinman A, Gips M, Lavy E, Sinay I, Soback S.Metronidazole pharmacokinetics in horses was studied after intravenous (i.v.), rectal (p.r.) and oral (p.o.) administration at 20 mg/kg using a triple crossover study design. Metronidazole mean+/-SD half-life was 196+/-39, 212+/-30 and 240+/-65 min after i.v., p.r. and p.o. administration, respectively. The metronidazole clearance was 2.8 (mL/min/kg) and the volume of distribution at steady state was 0.68 L/kg. The pharmacokinetic parameters calculated for metronidazole after administration of the drug by the various routes showed that bioavailability (74+/-18 vs. 30+/-9%) and maximum serum co...
Muir WW.The cardiovascular effects of serial increasing infusions of dopexamine HCl were investigated in six conscious (1, 2, 4, 6, 10 micrograms/kg bodyweight [bwt]/min) and eight (0.5, 1, 5, 10, 20 micrograms/kg bwt/min) halothane-anaesthetised horses. Dopexamine produced dose-dependent increases in heart rate, +dP/dtmax' -dP/dtmax and cardiac output, and a decrease in systemic vascular resistance in conscious and halothane-anaesthetised horses. Mean arterial blood pressure did not change in conscious horses but increased to a maximum value at 10 micrograms/kg bwt/min in halothane-anaesthetised hors...
Bosken JM, Lehner AF, Hughes CG, Woods WE, Camargo FC, Harkins JD, Boyles J, Tobin T.Isoxsuprine is used to treat navicular disease and other lower-limb problems in the horse. Isoxsuprine is regulated as a class 4 compound by the Association of Racing Commissioners, International (ARCI) and, thus, requires regulatory monitoring. A gas chromatography-mass spectrometry method utilizing electron impact ionization was developed and validated for the quantitation of isoxsuprine in equine plasma or equine urine. The method utilized robotic solid-phase extraction and tri-methyl silyl ether products of derivatization. Products were bis-trimethylsilyl (TMS) isoxsuprine and tris-TMS rit...
Soma LR, Sams R, Duer W, Tobin T, Woodward C, McDonald J.The plasma and serum concentrations of phenylbutazone (PBZ) and oxyphenbutazone were measured in 158 Thoroughbred horses after various doses of PBZ wer given. All horses were competing or training at racetracks in various parts of the country. All horses used in the study had not been given PBZ 24 hours before they were placed on a specific dosage schedule. Samples were collected 24 hours after the last PBZ administration. Four grams of PBZ were given daily by stomach tube, paste, or tablet for 3 days. On day 4, 24 hours before sample collection, an IV dose of 2 g of PBZ was given, regardless ...
Bachmann V, von Salis B, Fürst A.The goal of this study was to describe the development of equine drug testing in horses in Switzerland. This was achieved through evaluation of a film made by the Institute of Forensic Medicine at the University of Basel entitled 'Doping von Rennpferden' [Doping of Race Horses], toxicological detection, 1962', the analysis of doping test results of the Swiss Equestrian Federation and by interviewing individuals of various professions who were involved in equine drug testing at the time. The study compares early and modern methods of drug testing and highlights the changes in the attitude of eq...
Foreman JH, Bergstrom BE, Golden KS, Roark JJ, Coren DS, Foreman CR, Schumacher SA.There are no refereed controlled documentations of the skeletal analgesic efficacy of different dosages of flunixin meglumine (FM). Objective: The objective of this experiment was to compare the efficacy of various dosages of FM with a negative control. The hypothesis was that higher doses would result in improved efficacy in a dose-dependent manner when tested in a reversible model of foot lameness. Methods: Ten horses shod with adjustable heart bar shoes had weekly modified AAEP grade 4.0/5.0 lameness induced by tightening a set screw against the heart bar. Heart rate (HR) and lameness score...
Tydén E, Dahlberg J, Karlberg O, Höglund J.The development of anthelmintic resistance (AR) to macrocyclic lactones in the equine roundworm Parascaris equorum has resulted in benzimidazoles now being the most widely used substance to control Parascaris infections. However, over-reliance on one drug class is a risk factor for the development of AR. Consequently, benzimidazole resistance is widespread in several veterinary parasites, where it is associated with single nucleotide polymorphisms (SNPs) in drug targets encoded by the β-tubulin genes. The importance of these SNPs varies between different parasitic nematodes, but it has been h...
Wang CC, Hartmann-Fischbach P, Krueger TR, Wells TL, Feineman AR, Compton JC.Dermorphin and HYP(6) -dermorphin are hepta-peptides and natural opioids originally isolated from the skin of South American frogs. They are more potent than morphine but less likely to produce drug tolerance and addiction. These properties make them ideal candidates for the doping of racehorses to enhance performance during competition. Dermorphin was recently classified as a Class I drug by Racing Commissioners International (RCI), indicating that it is a banned substance in equine athletes. To enforce this ban, a fast and sensitive method was developed for dermorphin and HYP(6)-dermorphin a...
