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.
Erichsen DF, Aviad AD, Schultz RH, Kennedy TJ.A field study of 239 horses was conducted to determine the efficacy and safety of clenbuterol HCl, a beta 2-adrenergic bronchodilator, when administered incrementally to effect in the treatment of chronic obstructive pulmonary disease (COPD). The severity of COPD (heaves) and response to treatment was determined by clinical evaluation; an overall 'heaveiness rating' (OHR) was assigned at each observation. The horses were treated orally b.i.d. with clenbuterol (as Ventipulmin Syrup), beginning with the lowest dosage of 0.8 micrograms/kg. On day 10 of treatment at the effective dose (0.8, 1.6, 2...
Horne MM, Pascoe PJ, Ducharme NG, Barker IK, Grovum WL.This study compared the severity of ischemic injury to the equine jejunal mucosa caused by arteriovenous obstruction (AVO) or venous obstruction (VO) with that caused by reperfusion after ischemia. The degree of mucosal damage and regeneration was scored according to a modified version of an established light microscopic classification for ischemic injury. Biopsy specimens taken after 3 and 4 hours of obstruction, and after 3 hours of obstruction and 1 hour of reperfusion, were compared. There were no changes in the severity of mucosal injury (characterized by epithelial sloughing, loss of vil...
Roger T, Bardon T, Ruckebusch Y.The electrical and mechanical activity of the large intestine and its response to administration of opiate mu and kappa agonists were assessed from electrodes and inductograph coils chronically implanted on the cecocolic segment in six ponies given a diet of hay and concentrates. Before the drugs were given, migrating complexes propagating from the cecum into the colon occurred at the rate of 1.5 to 16/hour. During this propulsive activity, the cecocolic sphincter opened and closed allowing the outflow of cecal contents and preventing the backflow of colic contents. Each pony was used as its o...
Stevenson AJ, Weber MP, Trudel R, Leavitt R, Woodard D, Todi F, Mendonca M, Robillo V, Young L, Kacew S.Analytical procedures were developed to monitor furosemide concentrations in post-race serum and urine samples obtained from horses participating in an exercise-induced pulmonary haemorrhage (EIPH) program. High performance liquid chromatography with ultraviolet light detection proved a reliable, sensitive method for measuring urinary furosemide concentrations up to 12 h after administration of either 150 or 250 mg of the drug to race horses. However, this method was unreliable for determination of serum furosemide concentration. High performance liquid chromatography with fluorescence detecti...
Xiao L, Herd RP, Majewski GA.Efficacies of moxidectin and ivermectin were compared in four groups of eight ponies with natural parasite infections: placebo (Control), oral moxidectin gel at 0.3 mg kg-1 of body weight (Mox 0.3), oral moxidectin gel at 0.4 mg kg-1 of body weight (Mox 0.4), and oral ivermectin paste at 0.2 mg kg-1 of body weight (Ivermectin). Fecal samples were taken 0 and 2 weeks after treatment. Animals were necropsied and worms were collected 2 weeks after treatment. Moxidectin and ivermectin showed similar efficacy (99%) against adult cyathostomes, Strongylus spp., Triodontophorus spp. and Habronema musc...
Ensink JM, Barneveld A, Klein WR, van Miert AS, Vulto AG.The plasma disposition of ampicillin after intravenous administration at a dose rate of 15 mg/kg was studied in six healthy, 1-month-old foals. The oral bioavailability of pivampicillin was determined in the same foals at four ages, ranging from 11 days to 4 months. Pivampicillin was administered orally at a dose rate of 19.9 mg/kg, which is equivalent on a molecular basis to 15 mg/kg ampicillin. Ampicillin concentrations in plasma were determined up to 12 hours after administration. After intravenous administration, the mean distribution and elimination half-lives of ampicillin were 0.121 and...
Hildebrand SV, Hill T.Evoked hind limb digital extensor tension (hoof twitch) was maintained at 40% of baseline for 1 h by atracurium infusion in 7 horses anaesthetised with halothane. After 1 h, atracurium was discontinued and hoof twitch allowed to recover to 75%. Atracurium was again given by infusion to maintain 40% twitch for a second hour, then 2 mg gentamycin/kg bwt were given i.v. Atracurium infusion was continued for a third hour, and then hoof twitch was again allowed to recover spontaneously to 75%. Gentamycin reduced twitch strength from 40 +/- 1% (mean +/- sem) to 29 +/- 4% within 7.0 +/- 1.5 min (P = ...
Baggot JD.The neonatal period in foals refers to the first 7 days of postnatal life. The effects of drugs (pharmacologic agents) may be different in neonatal foals, particularly during the first 3 days of postnatal life, from those in older foals and adult horses. The changed drug effects decrease as the physiologic processes that affect absorption, distribution, and elimination (metabolism and excretion) of drugs mature. Dosage regimens should take into account the altered pharmacokinetic profiles of drugs, and because of wide individual variation, the response to therapy should be closely monitored fo...
Pompa G, Caloni F, Montana M, Pasqualucci C.1. Isoxsuprine [1-(4-hydroxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-1- propanol] serum concentrations after single- and multiple-dose administration to horse were investigated using immunoenzymatic ELISA, HPLC-UV and thermospray HPLC-MS methods. 2. Using HPLC-MS, isoxsuprine was detected up to 72 h after a single administration (1.2 mg/kg by gastric probe) and up to 96 h after the end of serial administration (1.2 mg/kg every 12 h for 7 days). 3. ELISA detected the drug up to 96 h after a single dose and up to 6 days after the end of prolonged administration. 4. Isoxsuprine is present in hors...
Lyons ET, Drudge JH, Tolliver SC, Swerczek TW, Stamper S, Granstrom DE.Studies in a band of ponies harboring Population S benzimidazole-resistant small strongyles were initiated in 1974 and have continued for 18 years. Treatment (bimonthly) was with cambendazole for the first 4 years and with oxibendazole (OBZ) for the next 14 years. Data on the first 10 years have been published. The present investigation includes the last 8 years (4 October 1984-11 September 1992), which are the seventh through fourteenth years, of treatment with OBZ. Pre- and posttreatment mean counts of strongyle eggs (epg) and larvae (lpg) per gram of feces were determined biweekly during th...
Sarasola P, McKellar QA.Ampicillin is an antibiotic commonly administered to horses by both the intramuscular (i.m.) and the intravenous (i.v.) route. Its physicochemical properties restrict its absorption after oral administration and explain its rapid elimination from the body. To prolong the effects of ampicillin in the horse, attempts have been made to alter its elimination and absorption rates. The alteration of urinary pH did not change the plasma disposition of the antibiotic but when probenecid was administered concurrently with ampicillin, a significant reduction of total body clearance was achieved. Ampicil...
Stanley S, Wood T, Goodman JP, Henry PA, Woods WE, Chang SL, Tai HH, Watt D, Kwiatkowski S, Blake JW.We have raised antibodies and developed one-step enzyme-linked immunosorbent assays (ELISA) for the diuretics ethacrynic acid and bumetanide as part of a panel of pre- and post-race tests for high potency drugs in racing horses. These ELISA tests are rapid (completed within one hour), sensitive, and can be read by eye. The ELISA detects ethacrynic acid at a drug concentration for half-maximal inhibition (I-50) of about 2.5 ng/mL for the parent drug. After dosing horses intravenously with 5 mg ethacrynic acid per horse, the parent drug or its metabolites are detectable in urine for at least 8 h...
Hagedorn HW, Schulz R, Jaeschke G.An enzyme linked immunosorbent assay (ELISA) was developed to detect the anabolic steroid boldenone in equine blood and urine. The polyclonal antiserum was raised in rabbits, employing boldenone-17-hemisuccinate-bovine serum albumin as antigen. Boldenone-17-hemisuccinate-horseradish peroxidase served as enzyme conjugate. Sensitivity of the assay was 26.0 +/- 3.0 pg/well. Among the endogenous steroids tested only progesterone and testosterone exhibited moderate cross-reactivities, 3.4 and 2.5%, respectively. These cross-reactivities are of no importance for the boldenone assay. For the reductio...
Maddison JE.Fifty-nine reports of suspected adverse drug reactions (ADRs) were received by the Adverse Drug Reaction Subcommittee of the Australian Veterinary Association from April 1992-March 1993 inclusive. The number of reports received/number of animals involved per species was: dogs (30/43); cats (11/14); horses (8/10); cattle (9/30); ferret (1/1). Of these, 37 (63%) were classified as definite ADRs and 12 (20%) as probable ADRs. In 10 (17%) reports an ADR could not be substantiated or there was insufficient information available to make a decision. Twenty-three reports involved apparent hypersensiti...
Van Duijkeren E, Vulto AG, Van Miert AS.The indications for use, side-effects, and pharmacokinetic parameters of trimethoprim, sulfonamides and their combinations in the horse are reviewed. Trimethoprim/sulfonamide (TMPS) combinations are used for the treatment of various diseases caused by gram-positive and gram-negative bacteria, including infections of the respiratory tract, urogenital tract, alimentary tract, skin joints and wounds. TMPS combinations can be administered orally, since absorption from the gastrointestinal tract is relatively good. However, peak serum concentrations can vary significantly between individual horses....
Ewing PJ, Burrows G, MacAllister C, Clarke C.The pharmacokinetic properties of four erythromycin formulations were compared in six adult horses after administration of single and multiple oral doses. Formulations of erythromycin administered were estolate and phosphate given 37.5 mg/kg every 12 h and 25 mg/kg every 8 h, and stearate and ethylsuccinate given 25 mg/kg every 8 h. Areas under the curve (AUC) and maximum plasma erythromycin concentrations (Cmax) were equal or greater (P > or = 0.05) following administration of erythromycin phosphate and stearate compared with those values following administration of erythromycin estolate or e...
Browning AP, Collins JA.Combinations of romifidine and butorphanol were used to sedate 55 horses for a variety of surgical, therapeutic and diagnostic procedures. Eighteen of the horses were given the drugs separately, romifidine first followed by butorphanol four minutes later, and 37 were given the drugs together. The levels of sedation and ataxia were assessed and graded, and there were no statistically significant differences between the two methods of administration. The side effects were typical of the alpha-2 agonists, including bradycardia, heart block and some sweating. Box-walking was observed in one horse....
Weiss DJ, Evanson OA, Geor RJ.The effects of various concentrations of furosemide and pentoxifylline on equine RBC in vitro were evaluated to facilitate better understanding of the potential effects of these drugs on blood flow properties. Furosemide induced increased mean cell volume (MCV), increased RBC potassium concentration, increased whole blood viscosity, and decreased the RBC filtrability. These data indicate that furosemide may block the RBC membrane transport pathways resulting in potassium and water retention. The increase in size and the resultant decrease in the surface-area-to-volume ratio may have caused the...
Schumacher J, Spano JS, Wilson RC, DeGraves FJ, Duran SH, Ruffin DC.The pharmacokinetic properties of intravenously administered caffeine were studied in 10 horses using a commercially available automated enzyme immunoassay. The harmonic mean for the distribution half-life was 5.2 min (range 1.4-18.7). The harmonic mean for the elimination half-life was 10.18 h (range 6.82-20.92). The harmonic mean of the volume of distribution was 0.32 L/kg (range 0.22-0.53). There was no correlation between the dose of caffeine/kg body weight and the elimination half-life (Spearman's coefficient of rank correlation = 0.19).
Barr AR, Duance VC, Wotton SF, Waterman AE.The influence of repeated intra-articular injections of sodium hyaluronate and polysulphated glycosaminoglycan on the repair of full-thickness osteochondral defects was examined in the midcarpal joints of ponies. The study showed no significant difference between treated and control groups with regard to total collagen content, uronic acid content or the relative proportions of Type I and Type II collagen in the repair tissue, indicating that the drugs did not affect the biochemical composition of the repair tissue 11 weeks after defect induction.
Manohar M, Hutchens E, Coney E.Catheter mounted micro-tip-manometers (the signals from which were matched with fluid-filled pressure signals from same cardiovascular sites and zeroed at the point of the shoulder), were used to study pulmonary haemodynamics in 8 healthy sound horses at rest and during exercise performed at 8, 10, 12 and 14 m/s on a treadmill. Measurements were made without frusemide (control) and 4 h after iv administration of 250 mg frusemide. Post-frusemide data were also obtained on a separate day, and these observations were not significantly different from those made on the same day as controls. Pre-fru...
Delbeke FT, Debackere M.A high performance liquid chromatographic method to measure plasma and urine fenoprofen levels in equine biofluids is described. Liquid-liquid extraction with diethylether was used to isolate the drug from plasma and urine. The accuracy and reproducibility of the method were within acceptable limits over the concentration range 0-10 micrograms/mL and 0-20 micrograms/mL respectively from plasma and urine. Detection limits were 0.05 microgram/mL (2 mL plasma) and 0.2 microgram/mL (0.5 mL urine). This procedure was applied to ascertain the pharmacokinetics of a 3 g dose of fenoprofen calcium in a...
Lin HC, Wallace SS, Robbins RL, Harrison IW, Thurmon JC.In 4 mares suffering from dystocia, general anesthesia was induced with xylazine (1.1 mg/kg, IV) and ketamine (2.2 mg/kg, IV) and maintained with continuous intravenous infusion of ketamine (2 mg/ml), xylazine (0.5 mg/ml) and guaifenesin (50 mg/ml) in 1 L of 5% dextrose. The duration of the procedure of these mares were 40, 45, 180, and 35 minutes, respectively. For procedures required more than 1 hour (Mare 3), the dose of ketamine and xylazine in the mixture was reduced to 1 mg/ml and 0.25 mg/ml, respectively. Average infusion rate of the mixture used to maintain anesthesia for each mare was...
Dyke TM.Drugs of relevance to equine practice that modify the central nervous system (CNS) can be broadly classified as depressants or stimulants. The pharmacologic mechanisms of action, uses, and side effects of selected CNS depressant and stimulant drugs in horses are reviewed. Knowledge of the way these CNS-modifying drugs may affect performance is limited.
Geor RJ, Weiss DJ.Pharmacologic alterations in the hematologic and rheologic properties of blood may have an important effect on transport and delivery of oxygen to working muscle during exercise. This article briefly reviews erythropoiesis, hematologic and rheologic responses to training and exercise, and the influence of these alterations on exercise performance. The hemorrheologic and performance effects of hematinics, hematopoietic stimulants, and alterations in blood rheology are discussed. The effects of exercise on blood coagulation, fibrinolysis and platelet function, and the effects of drugs that alter...
van der Velden MA, Klein WR.Seventy horses surgically treated for colic caused by disorders of the small intestine were included in a randomized blind trial to determine the effects of cisapride (0.1 mg/kg bw intramuscularly at 8-h intervals) on the post-operative restoration of gut motility. Cisapride appeared to reduce the incidence of post-operative ileus. It accelerated the restoration of bowel motility, reducing the period of post-operative intensive care. It is concluded that cisapride is an effective and useful drug in the post-operative treatment of horses after surgery of the small intestine.
Kamerling SG.Few definitive studies have been performed that unequivocally demonstrate the ability of a drug to alter the performance of a horse. Nonetheless, the use of drugs in competing horses is regulated worldwide. Drugs have been categorized according to their abuse potential. However, there is still some confusion over what is meant by the terms "performance" and "drug." In the racing community, performance means speed, and fatigue and pain are among its greatest detractors. Speed is most appropriately measured on the racetrack. There are a multiplicity of internal and external variables that influe...
Dyke TM.Tables of values of pharmacokinetic variables (volume of distribution, total body clearance, and plasma elimination half-life) of drugs frequently administered to performance horses are accompanied by explanatory notes. Drugs described include the nonsteroidal anti-inflammatory drugs, corticosteroids, anabolic steroids, central nervous system-modifying drugs, respiratory system drugs, diuretics, local anesthetics, and antibacterial drugs.
Yoxall AT.This paper is an introduction to a series of commissioned articles on therapeutic medicine to be published in Equine Veterinary Journal under differing authorship, during the next 2 years. It presents an account of fundamental concepts common to the use of all drugs and introduces some pharmacokinetic principles to which reference will be made in later articles.
Lorenzo-Figueras M, Merritt AM.To measure plasma cholecystokinin (CCK) activity and the effect of a CCK-1 receptor antagonist on accommodation of the proximal portion of the stomach, and subsequent gastric emptying, in horses after ingestion of high-fat or high-carbohydrate meals. Methods: 6 healthy adult horses with gastric cannulas. Methods: In the first study, horses were offered a high-fat (8% fat) or a high-carbohydrate (3% fat) pelleted meal of identical volume, caloric density, and protein content. Related plasma CCK-like activity was measured by radioimmunoassay (RIA). In a separate experiment, a horse was fed a gra...
Dyke TM.Drugs of relevance to equine practice that modify the central nervous system (CNS) can be broadly classified as depressants or stimulants. The pharmacologic mechanisms of action, uses, and side effects of selected CNS depressant and stimulant drugs in horses are reviewed. Knowledge of the way these CNS-modifying drugs may affect performance is limited.
Daugschies A.Drug resistance of parasites is a worldwide problem of increasing importance in animal production. Considerable information is available on the development of resistance in chicken coccidia and in strongyles of horses, sheep, goats and pigs. A review is given of the development, incidence, and management of drug resistance with emphasis on the situation in Germany.
Uehara N, Momose A.The doping test method used in a horse race requires the accurate detection of a wide variety of drugs and metabolites as well as the rapidity in order to examine a large number of samples within a limited time. For this purpose, the routine method consists of a preliminary screening and a confirmatory test. In this paper, a historical review for the development of the doping test method in Japan is described. The metabolism and pharmacology of drugs in horses are also discussed.
Clark ES, Becht JL.This article discusses the various drugs that affect the equine gastrointestinal tract. Drugs that alter intestinal motility, that protect the gastrointestinal tract, and that alter secretions, as well as analgesics, appetite stimulants, and orally administered antimicrobial agents are reviewed.
Schwark WS, Ducharme NG, Shin SJ, Beilman WT, Elwell JT.Serum levels of phenoxymethyl penicillin (penicillin V; Pen V) were measured following oral administration of two different formulations of the drug to five healthy horses. The mean serum concentration profile was described by a two-compartment model with a first order rate of absorption. Half-lives of the absorption, distribution and elimination phases were, respectively, 0.199 +/- 0.035, 0.362 +/- 0.060 and 3.650 +/- 0.575 hours. The distribution of the drug to body fluid compartments other than serum was examined. Mean peak levels of Pen V in serum, synovial fluid, peritoneal fluid and urin...