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.
Autefage A, Alvinerie M, Toutain PL.Synovial fluid and plasma kinetics of methylprednisolone acetate (MPA) and methylprednisolone (MP) after a single intra-articular administration of MPA at a therapeutic dose (111 mg in toto) was measured in five horses. MPA was detected in synovial fluid for two to six days post injection and MP, which results from synovial MPA hydrolysis, was present in pharmacologically significant concentrations for 4.8 to 39 days, depending on the horse. MPA synovial concentration was maximal (289 +/- 284 micrograms/ml) at the first sampling time (2 h after administration) and MP synovial concentration was...
May SA, Wyn-Jones G, Church S, Brouwer GJ, Jones RS.The use of the non-ionic, water-soluble contrast agent iopamidol for myelography in seven horses is described. Contrast columns of diagnostic quality were produced in all seven cases and the procedure did not invoke any adverse reactions in the five cases which were recovered from general anaesthesia. It is concluded that iopamidol is a safe and effective contrast agent for myelography in the horse.
Woods WE, Weckman T, Wood T, Chang SL, Blake JW, Tobin T.A commercially available radioimmunoassay kit was used to screen for the presence of etorphine in post-race urines from horses racing in Kentucky. Most horse urines contained small amounts of materials which reacted positively in this immunoassay. These materials are apparently endogenous to the horse and were called apparent etorphine equivalents. The levels of these apparent etorphine equivalents in post-race urines from 70 horses were estimated. Their modal level averaged 0.1 ng/ml, the population distribution was log normal, and individual horses showed levels of up to 0.8 ng/ml.
Walker M, Geiser D.Heart rate, blood velocity, volumetric blood flow, and arterial diameter for 10 horses given acetylpromazine were determined from measurements of the dorsal metatarsal artery 3 (the great metatarsal artery), using 2-dimensional real-time and gated pulsed Doppler ultrasonography. Acetylpromazine induced significant increases in arterial diameter (P less than 0.01) and volumetric flow rate (P less than 0.05)--all compatible with adrenergic blockade. There was a trend indicating that there was increased blood velocity. Heart rate was unchanged.
Bondesson U, Johansson IM.This study demonstrates the development of a method using gas chromatography-mass spectrometry for determining nefopam, a non-narcotic pain reliever that is sometimes abused in horse doping, in equine plasma. Background […]
Dumasia MC, Houghton E, Sinkins S.A gas chromatographic-mass spectrometric (GC-MS) method using three analytes to detect and confirm the administration to equine male castrates of veterinary pro-drugs based upon esters of testosterone is described. The method involves extraction of steroid conjugates from horse urine by C18-bonded cartridges and fractionation into glucuronic acid and sulpho-conjugates by Sephadex LH-20 column chromatography. After deconjugation, the free neutral steroids were partially purified by thin-layer chromatography and following derivatization (methyloxime-trimethylsilyl ether) were analysed by capilla...
Brown MP, Gronwall RR, Houston AE.Six healthy adult horse mares were each given a single injection of sodium cephapirin (20 mg/kg of body weight, IV), and serum cephapirin concentrations were measured serially over a 6-hour period. The mean elimination rate constant was 0.78 hour-1 and the elimination half-life was 0.92 hours. The apparent volume of distribution (at steady state) and the clearance of the drug were estimated at 0.17 L/kg and 598 ml/hour/kg, respectively. Each mare was then given 4 consecutive IM injections of sodium cephapirin (400 mg/ml) at a dosage level of 20 mg/kg. Cephapirin concentrations in serum, synovi...
Brown MP, Gronwall RR, Martinez DS, Beal C.Six healthy pony foals, from 2 to 11 days of age, were given a single IM injection of amikacin sulfate (250 mg/ml) at a dosage rate of 7 mg/kg of body weight. Serum amikacin concentrations were measured serially over a 24-hour period. The mean peak serum concentration was 14.7 micrograms/ml at 0.5 hour. The elimination rate constant for amikacin was 0.24/hour, the elimination half-life was 3.0 hours, and the apparent volume of distribution was 0.58 L/kg.
Skrabalak DS, Henion JD.Betamethasone and its major unconjugated metabolite, 6-beta-hydroxybetamethasone, were detected in equine urine by thin-layer chromatography and characterized by micro-liquid chromatography/mass spectrometry (micro-LC/MS). Their structures were confirmed by a combination of infrared spectroscopy and nuclear magnetic resonance spectroscopy.
Kamerling SG, Dequick DJ, Weckman TJ, Tobin T.Sensitive methods for measuring the analgesic, physiological and behavioural effects of opioids in the horse have recently been developed. Fentanyl, a prototypic mu-opiate receptor agonist, has been previously shown to produce a syndrome characterized by marked analgesia and locomotor stimulation as well as tachycardia, tachypnoea and behavioural arousal. To determine whether other opiate receptors mediate some of the actions of the narcotic analgesics in the horse, an agent with activity at kappa- and to lesser extent mu-receptors was studied using a vigorous experimental protocol. Like fenta...
Whitton DL, Trim CM.Heart block is a relatively common arrhythmia in the adult horse. It may be a normal physiologic phenomenon or it may have pathologic implication. Four foals in which advanced heart block developed during anesthesia were unresponsive to atropine sulfate and supportive treatment alone. Resolution of the heart blocks was achieved after the addition of dopamine hydrochloride to the therapeutic regimen.
Uhlinger C, Johnstone C.A survey was conducted to determine the prevalence of benzimidazole (BZ)-resistant small strongyles in horses in a southeastern Pennsylvania practice. Resistant parasites were found in 291 of 342 horses surveyed. Anthelmintic practices and pasture management factors in use for 3 to 6 years did not correlate with the presence of resistant small strongyles. Benzimidazole-resistant small strongyles were recovered in horses that had been treated alternately with BZ and non-BZ products and in horses receiving BZ products as infrequently as twice a year. However, inasmuch as the horses may have been...
Christensen JM, Blythe LL, Craig AM.Phenylbutazone was administered to six Thoroughbred horses in a cross-over study in which the horses received cimetidine pretreatment or no cimetidine pretreatment. Blood samples were collected at various times for 48 h after phenylbutazone administration and the plasma was analysed for phenylbutazone. Cimetidine pretreatment elevated phenylbutazone plasma concentrations during the first 8 h after phenylbutazone administration. The absorption rate, maximum phenylbutazone plasma concentrations and AUC were significantly greater with cimetidine pretreatment. The half-life of phenylbutazone did n...
Drudge JH, Lyons ET, Tolliver SC, Swerczek TW.Oxibendazole (OBZ; 10 mg/kg of body weight) was administered to ponies at 8-week intervals to control strongylosis in a breeding band of Shetland-type ponies (n = 29 to 50) from October 1978 through September 1984. A similar use of cambendazole (CBZ; 20 mg/kg of body weight) in this band of ponies during the preceding 4-year period resulted in the survival of a CBZ-resistant population (S) of small strongyles. Effectiveness of OBZ treatments was monitored by pre- and posttreatment counts of the number of strongyle eggs per gram of feces (epg) and of the number of strongyle larvae per gram of f...
Ayres JW, Pearson EG, Riebold TW, Chang SF.The pharmacokinetics of theophylline and dyphylline were determined after IV administration in horses. In a preliminary experiment, the usual human dosage (milligram per kilogram) of each drug was given to 1 horse. Results were used to calculate dosages for a cross-over study, using 6 horses for each drug. Theophylline plasma concentrations decreased triexponentially in 5 of 6 healthy horses after IV infusion of 10 mg of aminophylline/kg of body weight for 16 to 32 minutes. In the 6 horses, total body elimination rate constants were variable, and the half-life of theophylline was 9.7 to 19.3 h...
Woods WE, Chay S, Houston T, Blake JW, Tobin T.The efficacy of testing for illegal drugs in race horses was surveyed by evaluating 27 questionnaires received from 28 racing jurisdictions polled. Large variations in the number of samples tested and drugs detected were reported. Some jurisdictions reported only illegal medications, whereas others also reported permitted medications. To facilitate comparison, stimulants, depressants, local anesthetics, narcotic analgesics, and tranquilizers were classified as hard drugs. Other drugs, which are legal in some jurisdictions, were classified as soft. To evaluate the efficacy of testing, positive ...
Gerken DF, Sams RA.The effects of i.v. chloramphenicol sodium succinate on the pharmacokinetics of i.v. phenylbutazone in six healthy adult horses were investigated. Administration of chloramphenicol sodium succinate to mares reduced mean (+/- SD) phenylbutazone clearance from 0.600 +/- 0.222 to 0.339 +/- 0.123 ml/min per kg and increased mean (+/- SD) half life from 244 +/- 59.8 to 371 +/- 80.8 min and mean residence time from 333 +/- 86.2 to 533 +/- 124 min. The mean steady-state volume of distribution of phenylbutazone was unchanged, with mean (+/- SD) values of 187 +/- 28.9 ml/kg in control animals and 170 +...
Ruoff WW, Sams RA.The pharmacokinetics and bioavailability of cephalothin given to 6 horse mares at a dosage level of 11 mg/kg of body weight IV or IM were investigated. The disposition of cephalothin given IV was characterized by a rapid disposition phase with a mean half-life of 2.89 minutes and a subsequent slower elimination phase with a mean half-life of only 14.7 minutes. The mean residence time of cephalothin was 10.6 +/- 2.11 minutes. The total plasma clearance of cephalothin averaged 13.6 ml/min/kg and was caused by metabolism and renal elimination. Renal clearance of cephalothin averaged 1.32 ml/min/k...
Errecalde JO, Button C, Mülders MS.A single intravenous administration of theophylline as aminophylline at 10 mg/kg to four mares induced a diuresis in which maximal urine production was more than seven times the control volume. The diuretic effect was maximal within the first hour post-administration, and lasted approximately 6 h. Theophylline resulted in dose-related tachycardia, polypnoea and nervous symptoms (tactile, visual and auditory hypersensitivity, muscle tremor, sweating) in normal mares, but had only minor effects on arterial and central venous blood pressures, intrapleural pressure, red blood cell variables and pl...
Nouws JF, Vree TB, Baakman M, Driessens F, Smulders A, Holtkamp J.The plasma disposition of sulfadimidine (SDM) and its metabolites N4-acetylsulfadimidine (N4-SDM), 6-hydroxymethyl-4-methyl-pyrimidine (SCH2OH) and 5-hydroxy-4,6-dimethyl-pyrimidine (SOH), was studied in three horses following intravenous administration of SDM at dose levels of 20 and 200 mg/kg in cross-over trials. The percentages of N4-SDM (0.58-0.90%), SOH (0.83-6.75%) and SCH2OH (0.38-0.71%) in plasma, expressed as a percentage of the total sulfonamide concentration, were small and their plasma concentrations were parallel with SDM from 4 h following administration. At high doses (200 mg/k...
Steffey EP, Kelly AB, Farver TB, Woliner MJ.Circulatory and respiratory effects of intravenously administered acetylpromazine (0.033 and 0.067 mg/kg) and xylazine (0.5 and 1.0 mg/kg) were studied in drug cross-over fashion in eight laterally recumbent horses anesthetized only with halothane (1.06%, end-tidal) in O2. Both doses of acetylpromazine caused a significant and sustained elevation in cardiac output via a rise in stroke volume. Xylazine produced an initial significant fall in cardiac output followed by a return to control levels. Halothane anesthesia did not prevent xylazine-related atrioventricular conduction block. All treatme...
Haddad NS, Pedersoli WM, Ravis WR, Fazeli MH, Carson RL.Healthy mature pony mares (n = 6) were given a single dose of gentamicin (5 mg/kg of body weight) IV or IM 8 days apart. Venous blood samples were collected at 0, 5, 10, 20, 30, and 45 minutes and at 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 18, 24, 30, 36, 40, and 48 hours after IV injection of gentamicin, and at 10, 20, 30, and 45 minutes and at 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 18, 24, and 30 hours after IM injection of gentamicin. Gentamicin serum concentration was determined by a liquid-phase radioimmunoassay. The combined data of IV and IM treatments were analyzed by a nonlinear least-square...
Drudge JH, Lyons ET, Taylor EL.Three series of critical tests were completed on a combined total of 46 horses to determine the efficacy of single doses of trichlorfon against bots, ascarids, pinworms, and large strongyles. Different formulations of trichlorfon were administered by tubing intragastrically, mixing with the daily grain ration, injecting intramuscularly, or pouring on the back at dose rates between 20 and 100 mg/kg. Administration by feeding tended to be more efficacious for removal of bots and less toxic to the horese than administration by stomach tube. In many of the tests, trichlorfon was given in the grain...
Koupai-Abyazani MR, Esaw B, Laviolette B.A high-performance liquid chromatographic method was used for the detection of etodolac in equine serum and urine. The method consisted of a one-step liquid-liquid extraction, separation on a reversed-phase (RP-18) column and detection using an ultraviolet detector. Additional confirmation methods included a HPLC coupled with an atmospheric pressure chemical ionization mass spectrometer (APCI-MS). Free (unbound) etodolac and its conjugates were present in the samples. Concentrations of the drug in the serum and urine samples collected from four standardbred mares after a single oral administra...
Swan GE, Guthrie AJ, Mülders MS, Killeen VM, Nurton JP, Short CR, van den Berg JS.The pharmacokinetics of gentamicin following single and multiple intravenous and intramuscular doses were compared in a two phase, randomised cross-over study in horses. Gentamicin was administered to 6 healthy, conditioned Thoroughbred mares at a dosage of 3.3 mg/kg body weight every 12 hours for 5 intravenous or intramuscular consecutive treatments. Equal numbers of horses were treated by either route during each phase. There was a wash-out period of 5 days between phases. During each phase serial blood samples were collected from each mare immediately before treatment and at 16 intervals fo...
Brown MP, Stover SM, Kelly RH, Farver TB.Six adult mares were given a single dose of ampicillin trihydrate (250 mg/ml) intramuscularly at a dosage of 20 mg/kg body weight. Serum, synovial fluid, peritoneal fluid and urine ampicillin concentrations were measured serially over a 48 h period. The mean peak serum ampicillin concentration was 2.49 micrograms/ml at 6 h. Ampicillin was found in synovial fluid and peritoneal fluid, which obtained mean peak ampicillin concentrations of 1.65 micrograms/ml and 1.81 micrograms/ml at 6 h and 4 h respectively. These concentrations declined in parallel with serum concentrations and were still detec...
Benoit E, Jaussaud P, Besse S, Videmann B, Courtot D, Delatour P, Bonnaire Y.A benzhydrolic metabolite of ketoprofen, formed by reduction of the keto group of the drug, has been identified by gas chromatography-mass spectrometry in equine plasma and urine. After partial synthesis, its structure has been confirmed by UV, IR and 1H NMR spectroscopy. The kinetics of ketoprofen and this metabolite have been monitored in plasma by high-performance liquid chromatography. The two products were quantified in plasma up to 4 and 3 h, respectively, and were detected in urine up to 72 and 24 h, respectively, after a single intravenous administration to horses at the dose of 2.2 mg...
Watson TD, Sullivan M.The effects of sedation with detomidine on oesophageal function were assessed by contrast radiography in 10 healthy adult thoroughbred horses. Barium swallows were monitored by means of image intensification, first without sedation and then after the intravenous administration of detomidine at doses of 10 and 20 micrograms/kg bodyweight. The transit time of contrast agent to the oesophageal hiatus was recorded and each swallow was scored for markers of oesophageal dysfunction. Analysis of the data indicated that there were highly significant dose dependent increases in the transit time, the re...
Alexander F.The effect of ethacrynic acid, bumetanide, frusemide, spironolactone and anti-diuretic hormone (ADH) on the urinary and faecal excretion of water and electrolytes by ponies was studied. Ethacrynic acid, bumetanide, and frusemide given intravenously, increased urinary sodium excretion, and, excepting frusemide, decreased faecal sodium excretion. Given by stomach tube ethacrynic acid reduced urinary and faecal sodium. Bumetanide, given intravenously, spironolactone, frusemide and ADH increased urinary sodium and all except frusemide intravenously decreased faecal sodium regardless of route of ad...
Engelking LR, Lofstedt J, Blyden GT, Greenblatt DJ.The following studies were designed to evaluate plasma elimination kinetics of intravenously administered antipyrine, acetaminophen and lidocaine among 9 healthy adult horses and 9 healthy drug-free humans (3 each per drug group), in order to compare potential species differences in drug-metabolizing ability. Acetaminophen is largely biotransformed in humans by hepatic glucuronide and sulfate conjugation, whereas both antipyrine and lidocaine are oxidized by hepatic microsomal mixed-function oxidases. Thus, plasma clearances of these drugs are thought to reflect differences in hepatic oxidativ...
Lyons ET, Drudge JH, Tolliver SC.Thirteen critical tests (n = 11 horses and 2 ponies) and 4 controlled tests (n = 4 donkeys and 6 horses) were performed to evaluate the activity of the experimental macrocyclic lactone compound F28249-alpha against internal parasites of equids. In the critical tests, activity was determined mainly against the large parasites, but 1 critical test also included benzimidazole-resistant small strongyles. In the controlled tests, evaluation of drug activity included large parasites and stomach worms in all 4 tests, and lungworms in 2 tests. The period between treatment and euthanasia was 6 to 9 day...
Seddighi R, Knych HK, Cox SK, Sun X, Moorhead KA, Doherty TJ.To determine the sedative effects and pharmacokinetic profile of detomidine when administered intravaginally as a gel formulation to horses. Methods: Randomized, crossover, masked experimental design. Methods: A group of six healthy adult mares (494 ± 56 kg). Methods: Mares were studied on two occasions and were administered either detomidine hydrochloride (10 μg kg) intravenously (treatment IV) or detomidine gel (40 μg kg) intravaginally (treatment IVG), separated by 1 week. Sedation, ataxia, muzzle-floor distance and heart rate (HR) were evaluated every 15 minutes for 240 minutes. Venous ...
van den Bogaard AE, Thijssen HH, Hemker HC.The anticoagulant, warfarin, has been reported to be effective as treatment for navicular disease in horses. Since other forms of treatment for this disease are palliative, this new anticoagulant therapy has become widely employed. Despite the fact that initiation of anticoagulant therapy is relatively simple, attending veterinary practitioners should be aware that careful monitoring of this therapy is required for both safety and efficacy. Navicular disease is an example of equine thrombotic disease, and the goal of warfarin therapy is the prevention of new thrombus formation, while at the sa...
Sinn D, Wintzer HJ.The pharmacokinetics of racemic phenprocoumon were studied in 8 adult horses after the single intravenous and oral administration of 0.75 mg/kg. After i.v. administration the plasma concentration of phenprocoumon showed a biphasic decline in time. The pharmacokinetics were calculated on the two-compartment open model. The average plasma half-life (beta-phase) was 22 hours, the apparent volume of distribution was 0.61 l/kg, Cltot was 25.2 ml/kg/h (13.9-40.9 ml/kg/h). The systemic bioavailability of oral phenprocoumon was 97.6%, Tmax was found to be 4-12 hours. The effect of phenprocoumon on the...
Bello TR.A controlled test was done in 30 naturally infected ponies to evaluate the antiparasitic activity of the dienbendazole analog VET 220-S given alone or with trichlorfon (TCF) by nasogastric intubation. Six ponies were nontreated; 6 were given VET 220-S (5.0 mg/kg); 6 were given TCF (40 mg/kg); 6 were given VET 220-S (2.5 mg/kg) and TCF (40 mg/kg); and 6 were given VET 220-S (5.0 mg/kg) and TCF (40 mg/kg). All ponies were euthanatized and necropsied 7 or 8 days after treatment. Draschia megastoma, Oxyuris equi, Strongylus vulgaris, S edentatus, and small strongyles were removed efficaciously by ...
Adams AR, Haines GR, Brown MP, Gronwall R, Merritt K.Pharmacokinetics of difloxacin and its distribution within the body fluids and endometrium of 6 mares were studied after intragastric (IG) administration of 5 individual doses. Difloxacin concentrations were serially measured in serum, urine, peritoneal fluid, synovial fluid, cerebrospinal fluid, and endometrium over 120 h. Bacterial susceptibility to difloxacin was determined for 174 equine pathogens over a 7-month period. Maximum serum concentration (Cmax) was 2.25 +/- 0.70 microg/mL at 3.12 +/- 2.63 h and Cmax after the 5th dose was 2.41 +/- 0.86 microg/mL at 97.86 +/- 1.45 h. The mean elim...
Pu F, McKinney AR, Stenhouse AM, Suann CJ, McLeod MD.A study of the equine phase II metabolism of the anabolic agent boldenone is reported. Boldenone sulfate, boldenone glucuronide and their C17-epimers were synthesised as reference standards in our lab and a method was developed for their detection in a horse urine matrix. Solid phase extraction was used to purify the analytes, which were then detected by ion trap LC/MS. Negative and positive ionisation mode MS(2) were used for the detection of sulfate and glucuronide conjugates, respectively. Boldenone sulfate and 17-epiboldenone glucuronide were detected as the major and minor phase II metabo...
Cook G, Papich MG, Roberts MC, Bowman KF.To determine the i.v. pharmacokinetics of cisapride and measure systemic absorption after rectal administration. Methods: 5 healthy adult mares (380 to 610 kg). Methods: Cisapride was administered, i.v., at a dosage of 0.1 mg/kg of body weight. In the same horses, after a 1-week washout period, cisapride was administered rectally at a dosage of 1 mg/kg by mixing crushed tablets with propylene glycol and administering the mixture into the rectum. After each drug administration, a series of blood samples were collected. Plasma was obtained and analyzed by high-performance liquid chromatography t...
Wise IK, Klöppel H, Leece EA.Ketamine-based total intravenous anaesthesia techniques are commonly used in equine practice for ponies requiring short procedures such as castration in field conditions. When a longer duration of recumbency than provided by the initial dose of anaesthetic agents is required, administration of supplementary 'top-up' doses of anaesthetic agents is required. Ideally, a single dose of anaesthetic agents would reliably achieve a longer duration of action whilst maintaining adequate anaesthetic, surgical and recovery qualities. Objective: This prospective, randomised and blinded study aimed to comp...
Stover SM, Brown MP, Kelly RH, Farver TB.Six healthy adult mares were given a single dose (25 mg/kg of body weight) of sodium oxacillin IM. Oxacillin concentrations in serum, synovial fluid, peritoneal fluid, and urine were measured serially over a 48-hour period. The mean peak serum oxacillin concentration was 9.75 microgram/ml at 0.5 hour after injection. Mean peak oxacillin concentrations in synovial and peritoneal fluids were 1.45 microgram/ml and 2.60 microgram/ml at 1 hour and 2 hours, respectively. These concentrations decreased in parallel with serum values and were not measurable at 48 hours. Urine concentrations of oxacilli...
Drumev D.Stated is the use of promising therapeutic formulae that produce prophylactic, metaphylactic, and curative effects at lower input of labour and handling, inciting lower unrest with animals, belonging chiefly to the type of the so-called 'therapeutic systems'. Particular attention is paid to drugs for programmed, continuous, and checkable release of the active ingredients in compliance with what is needed at the time (sustained release forms)-type OROS (oral osmotic system), type 'liquid reservoir', type 'glass cylinders', tablets and boluses of higher relative weight, or multilayer and mosaic ...
Brosnan RJ, Steffey EP.We hypothesized that propofol can produce rapidly-reversible, dose-dependent standing sedation in horses. Methods: Prospective randomized, blinded, experimental trial. Methods: Twelve healthy horses aged 12 +/- 6 years (mean +/- SD), weighing 565 +/- 20 kg, and with an equal distribution of mares and geldings. Methods: Propofol was administered as an intravenous bolus at one of three randomized doses (0.20, 0.35 and 0.50 mg kg(-1)). Cardiovascular and behavioral measurements were made by a single investigator, who was blinded to treatment dose, at 3 minute intervals until subjective behavior s...
Knych HK, Finno CJ, Baden R, Arthur RM, McKemie DS.The in vivo metabolism and pharmacokinetics of flunixin meglumine and phenylbutazone have been extensively characterized; however, there are no published reports describing the in vitro metabolism, specifically the enzymes responsible for the biotransformation of these compounds in horses. Due to their widespread use and, therefore, increased potential for drug-drug interactions and widespread differences in drug disposition, this study aims to build on the limited current knowledge regarding P450-mediated metabolism in horses. Drugs were incubated with equine liver microsomes and a panel of r...
Delbeke FT, Baert K, De Backer P.Urinary and plasma concentrations of the nonsteroidal anti-inflammatory drug tiaprofenic acid were determined following oral and intramuscular administration of a dose of 1 g to five fasted horses. Quantitation was performed by high-performance liquid chromatography (HPLC). The limit of quantitation (LOQ) was 0.1 microg/ml and 0.5 microg/ml in 2 ml plasma and 1 ml urine, respectively. Assay precision and extraction recovery were between acceptable values. Tiaprofenic acid pharmacokinetics were described by non-compartment analysis of the data. Absorption was faster after oral administration as...
Maxwell L, McCarrel TM, Hay S, Cole C.The antifibrinolytic agent aminocaproic acid (ACA) is occasionally used prior to episodes of intense training in racehorses suffering from exercise-induced pulmonary hemorrhage. Although a previous study indicated that the drug is cleared rapidly in horses, some racetrack practitioners claim that recent adverse analytical findings for ACA in postrace samples were from ACA administrations 5-7 days before the race. The purpose of this study was to re-examine the pharmacokinetics of ACA in horses to address this apparent conundrum. Eight exercise-conditioned thoroughbred horses were administere...
Tobin T, Watt DS, Kwiatkowski S, Tai HH, Blake JW, McDonald J, Prange CA, Wie S.We have introduced large scale non-isotopic immunoassay testing into pre- and post-race drug testing in racehorses. The technologies utilized are Particle Concentration Fluorescence Immuno Assay (PCFIA) and the one-step Enzyme Linked Immuno Sorbent Assay (ELISA). These technologies are rapid, inexpensive, and highly effective. On introduction into post-race testing in the Western United States, these ELISA tests exposed several previously undetected patterns of drug abuse. The drugs detected were buprenorphine, oxymorphone, mazindol, sufentanil and cocaine. This led to the suspension of a larg...
Brewer K, Machin J, Maylin G, Fenger C, Morales-Briceño A, Tobin T.Gabapentin, 1-(Aminomethyl)cyclohexaneacetic acid, MW 171.240, is a frequently prescribed high dose human medication that is also used recreationally. Gabapentin is orally absorbed; the dose can be 3,000 mg/day and it is excreted essentially unchanged in urine. Gabapentin is stable in the environment and routinely detected in urban wastewater. Gabapentin randomly transfers from humans to racing horses and is at times detected at pharmacologically ineffective / trace level concentrations in equine plasma and urine. In Ohio racing between January 2019 and July 2020,18 Gabapentin identifications...
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).
Corveleyn S, Henrist D, Remon JP, Van Der Weken G, Baeyens W, Haustraete J, Aboul-Enein HY, Sustronck B, Deprez P.Ketoprofen (KTP) is a chiral non-steroidal anti-inflammatory drug (NSAID) of the propionic acid class, approved by the FDA for the allevation of pain associated with musculoskeletal disorders in horses. The present study was designed to examine the bioavailability of ketoprofen enantiomers after rectal administration of the racemate to healthy horses. One gram of racemic ketoprofen was injected intravenously and administered rectally as a fat based suppository in a cross-over design study (n = 4). Blood samples were analysed for KTP enantiomers using HPLC. After IV administration, the S(+) ena...
Knych HK, Steffey EP, Stanley SD.To describe the pharmacokinetics of detomidine and yohimbine when administered in combination. Methods: Randomized crossover design. Methods: Nine healthy adult horses aged 9 ± 4 years and weighing of 561 ± 56 kg. Methods: Three dose regimens were employed in the current study. 1) 0.03 mg kg(-1) detomidine IV (D), 2) 0.2 mg kg(-1) yohimbine IV (Y) and 3) 0.03 mg kg(-1) detomidine IV followed 15 minutes later by 0.2 mg kg(-1) yohimbine IV (DY). Each horse received all three dose regimens with a minimum of 1 week in between subsequent regimens. Blood samples were obtained and plasma analyzed f...
Wood T, Tai CL, Taylor DG, Woods WE, Wang CJ, Houtz PK, Tai HH, Weckman TJ, Yang JM, Sturma L.Detomidine is a potent non-narcotic sedative agent which is currently in the process of being approved for veterinary clinical use in the United States. Since no effective screening method in horses is available for detomidine, we have developed an 125I radioimmunoassay for detomidine in equine blood and urine as part of a panel of tests for illegal drugs in performance horses. Our 125I radioimmunoassay has an I-50 for detomidine of approximately 2 ng/ml. Our assay shows limited cross-reactivity with the pharmacodynamically similar xylazine, but does not cross-react with acepromazine, epinephr...
Paine SW, Aldurdunji M, Garth-Greeves A, Muir T, Hincks PR.Hydroxyzine and cetirizine are first- and second-generation oral antihistamine drugs, respectively, used to treat allergic reactions in horses. Cetirizine is also a metabolite of hydroxyzine, which may lead to complexities in regulating their use in equine sporting events. The aim of the research was to be able to provide detection times (DT) from pharmacokinetic studies in thoroughbred horses to better inform trainers, and their veterinary surgeons, prescribing these substances for treatment of Thoroughbred racehorses. Six and two horses were given 9 repeated administrations of hydroxyzine HC...
