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.
Kowalski KA, McConnell LA, Sadoff DA, Leid RW.Equine platelets, when treated with the anthelmintic drug diethylcarbamazine (DEC), gave a dose-dependent release of radiolabeled serotonin without concomitant aggregation. At levels of the drug that gave only minimal release of radiolabel, marked dose-dependent inhibition of platelet aggregation to three of four platelet agonists tested--adenosine diphosphate (ADP), collagen, and arachidonic acid--was observed. With ADP, inhibition was observed to be reversed by removal of DEC prior to agonist challenge. However, with collagen, inhibition was only partially reduced by prior removal of DEC; wh...
Brumbaugh GW, Martens RJ, Knight HD, Martin MT.Chloramphenicol sodium succinate was administered as an intravenous bolus (50 mg/kg) to eight foals which weighed 49-57 kg (mean +/- 1 standard deviation = 53.19 +/- 2.66) each, and were 1-9 days (4.5 +/- 2.56) of age. The drug was rapidly distributed and followed first-order elimination. Mean pharmacokinetic values were: zero-time serum concentration (C0) = 36.14 microgram/ml (+/- 14.80); apparent specific volume of distribution (Vd) = 1.614 1/kg (+/- 0.669); and elimination rate constant (K) = 0.7295 h-1 (+/- 0.3066) which corresponds to a biological half-life (t1/2) = 0.95 h. These values d...
Wilson RC, Moore JN, Eakle N.The pharmacokinetics of gentamicin (3 mg/kg of body weight) were evaluated in 6 healthy horses and in 6 horses after they were given Escherichia coli endotoxin (0.113 microgram/kg). In the horses given endotoxin, there were a maximum temperature increase of 1.97 +/- 0.44 degrees (C) and a fever index (between the 2 groups) of 8.754 units. Other mild signs of endotoxemia also occurred. Statistically significant changes were not observed in the rate constants for distribution (alpha) or elimination (beta) or in body clearance (ClB) of gentamicin in the 2 groups of horses. In the horses given end...
Robertson JT, Muir WW.A xylazine and butorphanol drug combination produced minimal and transient hemodynamic effects and no significant respiratory depression when administered to 6 healthy horses. Combining xylazine and butorphanol produced a synergistic analgesic effect and provided good chemical restraint for a standing surgical procedure.
Brumbaugh GW, Thomas WP, Enos LR, Kaneko JJ.Digoxin was administered orally and intravenously to seven healthy adult mares and geldings in two separate trials. At a dose of 44 microgram digoxin/kg body weight, the oral study was characterized by an absorption phase with a mean (+/- 1 standard deviation) peak serum digoxin concentration of 2.21 ng/ml (+/- 0.45) at a mean of 2.29 h (+/- 1.52) after administration. A second rise in serum digoxin concentration started about 6-8 h after administration and extended to about 20 h after administration. The mean bioavailability (F) was 23.38% (+/- 5.96). At a dose of 22 microgram digoxin/kg body...
Science (New York, N.Y.)August 26, 1983
Volume 221, Issue 4613 823-828 doi: 10.1126/science.6308762
Campbell WC, Fisher MH, Stapley EO, Albers-Schönberg G, Jacob TA.Ivermectin is the 22,23-dihydro derivative of avermectin B1, a macrocyclic lactone produced by an actinomycete, Streptomyces avermitilis. It is active at extremely low dosage against a wide variety of nematode and arthropod parasites, apparently by virtue of its action on the mediation of neurotransmission by gamma-aminobutyric acid. It is now in commercial use in various countries for the treatment and control of parasites in cattle, horses, and sheep, and is expected to become available for use in swine and dogs. Since studies with the drug in man are in a preliminary stage, it is not yet kn...
Rollinson EA, White G.Compound BW759 (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine) was shown to be about 230 times more active than acyclovir (9-[2-hydroxyethoxymethyl]guanine) (ACV) against Equid herpesvirus type 1 infection in Syrian hamsters and was more effective against Aujeszky's disease in mice. The therapeutic superiority of BW759 over ACV was greater than expected from quantitative inhibitory results in tissue culture with these viruses. When administered to hamsters at dose rates sufficient to prevent any Equid herpesvirus type 1-induced mortality (100 mg of ACV per kg per day; 3 mg of BW759 per kg...
Toro M, León E, López R, Pallota F, Garcia JA, Ruíz A.Assays dealing with the therapeutic and prophylactic activity of isometamidium on experimental infections by Trypanosoma vivax and T. evansi were carried out. The drug was found to be highly effective against T. vivax infection in sheep and cattle in which periods of protection ranging from 118 to 195 days were achieved. No complete effects against infection by T. evansi were observed. The drug was well tolerated in sheep and cattle while side-effects were noted in treated mares. It was concluded that isometamidium could be used to prevent damage and economical losses caused by T. vivax in Ven...
Shideler RK, Voss JL, Aufderheide WM, Hessemann CP, Squires EL.Twenty mares were assigned to 1 of 4 groups: no altrenogest; altrenogest at 0.044 mg/kg BW; altrenogest at 0.132 mg/kg BW; or altrenogest at 0.220 mg/kg BW. Treatment was administered daily for 86 days. No signs of illness attributable to feeding altrenogest were observed during the trial. Treatment had no effect (P greater than .05) on the following parameters: WBC, differential WBC, platelet number, creatinine, LDH, CPK, total bilirubin, cholesterol, globulin, BSP, and erythrocyte sedimentation rate. When comparing values over time with pretreatment means or among treatment groups, there wer...
Rose RJ, Allen JR, Hodgson DR, Kohnke JR.A peripheral vasodilating agent, isoxsuprine hydrochloride, administered as an oral paste, was evaluated to determine its efficacy for the treatment of navicular disease. In a clinical trial, 13 horses with navicular disease were treated at a dose rate of 0.6 mg/kg body weight (bwt) twice daily for periods of six to 14 weeks. Twelve of the horses became completely sound while being treated, although two required a 50 per cent increase in dose. Nine of the horses have remained sound two to 10 months after ceasing therapy. In a controlled randomised double blind clinical trial, 16 horses with na...
Roberts MC, Seawright AA.Colic was induced in horses and ponies following topical or intravenous (iv) administration of amitraz, a formamidine acaricide. The condition was characterised by rapid cessation of intestinal sounds, stasis, extensive impaction and tympany throughout the large colon. Three animals that were necropsied had a faecalith obstructing the proximal small colon aboral to marked colonic impaction. A reproducible and reversible impaction colic syndrome could be induced by an iv injection of 1 mg amitraz/kg body weight in solvent. There were immediate central nervous system and intestinal signs. Large ...
Taylor JB, Walland A, Lees P, Gerring EL, Maitho TE, Millar JD.Five pairs of matched horses were used to study the biochemical and haematological effects of a revised dosage schedule of phenylbutazone. One group of five horses received a phenylbutazone paste formulation daily for 12 days and a second group of five animals received a placebo preparation for a similar time. Some statistically significant differences were recorded from pretreatment levels in both groups of horses. These changes represented instability in baseline levels and could not be ascribed to phenylbutazone administration.
Snow DH, Douglas TA.The absorption characteristics of a new paste preparation of phenylbutazone were studied in ponies and thoroughbreds. The results suggested that at a similar dose rate of 5 mg/kg greater bioavailability results from the paste than from a powder preparation. Delivery of an accurate dosage of the paste was not possible using the multidose applicator. Repeated administration of the paste preparation (5 mg/kg twice daily) indicated that it is more toxic to both ponies and thoroughbreds than a powder preparation. In addition to the toxic manifestations previously reported, a neutropenia developed d...
Parry BW, Anderson GA.The effect of acepromazine maleate (ACP) on the equine venous haematocrit and total plasma protein concentration was studied in six clinically normal horses. Total plasma protein concentration was not appreciably influenced by ACP. However, the haematocrit decreased with the duration, but not the degree, of the decrease being dose-related. Mean haematocrit values returned to control levels by 12 h after 0.05 mg ACP/kg body weight and 21 h after 0.15 mg ACP/kg body weight.
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...
DiPietro JA, Paul A, Todd KS.Forty horses from a herd known to have benzimidazole-resistant small strongyles were treated with mebendazole (8.8 mg/kg) or combinations of mebendazole and piperazine monohydrochloride (25, 40, or 55 mg of piperazine base/kg). Pretreatment and 7-day posttreatment fecal examinations were done. Fecal cultures and strongyle egg per gram (epg) counts, and in vitro testing for benzimidazole resistance were performed. Results of fecal examinations prior to treatment were similar in all horses, and results of testing were positive for benzimidazole resistance. Horses treated with mebendazole and pip...
Davies JV, Gerring EL.The effect of acepromazine, Buscopan (Crown Chemicals), pethidine and methadone was evaluated in ponies prepared with Thiry-Vella (T-V) loops. Motility was assessed by electrophysiological means (bipolar electrodes and strain gauge transducers) and by the passage through the T-V loop of a fluid test meal. Results were obtained from 26 experiments in three ponies and compared with six control experiments, in which saline had been administered to the same ponies. Each pony acted as its own control in each experiment and pre and post treatment values for slow wave frequency, spiking activity, del...
Chay S, Woods WE, Rowse K, Nugent TE, Blake JW, Tobin T.Studies were undertaken to determine blood levels of furosemide in horses after 0.5- and 1.0-mg/kg doses administered iv. Analyses indicated that the pharmacokinetic parameters were dose independent and best described by a three-compartment open model. The alpha-, beta-, and gamma-phase half-lives of 5.6, 22.3, and 158.5 min, respectively, were observed after the 0.5-mg/kg dose. Similarly, the respective half-lives after the 1.0-mg/kg dose were 5.8, 24.1, and 177.2 min. After a 0.5-mg/kg dose of furosemide, population frequency distributions were evaluated at 1 hr and 4 hr post-drug administra...
Combie JD, Nugent TE, Tobin T.Morphine could be detected in horses dosed with 0.1 mg of drug/kg of body weight for up to 48 hours in blood and 144 hours in urine. This dose of morphine elicited no observable effects and is a suggested analgesic dose. Computer analysis revealed that a 3-compartment open system was the best fitting model with a serum half life (t1/2(beta)) of 87.9 minutes and a urine t1/2(beta) of 101.1 minutes. Binding to equine serum proteins was linear over a drug concentration range of 3.88 X 10(-5)M to 3.50 X 10(-8)M and averaged 31.6%. In RBC-partitioning experiments, 78.1% of the drug was found in the...
Marsh MV, Caldwell J, Sloan TP, Smith RL, Horner M, Moss MS.14C-Fenclofenac (2-(2'-4'-dichlorophenoxy)-phenylacetic acid) was administered orally to horses, and urinary metabolites investigated by chromatography. Fenclofenac was rapidly absorbed and eliminated, with a plasma half-life (t1/2) of 2.3 h, with 83.2 and 85.8% of the dose being recovered in the urine in 0-24 h. The major urinary metabolite was the ester glucuronide (58.8, 70.0% dose), and evidence is presented that this metabolite undergoes a structural rearrangement to give beta-glucuronidase-resistant isomers. The other 14C-labelled components in horse urine were unchanged fenclofenac (13....
Johnstone IB.Nonsteroidal anti-inflammatory drugs are commonly used in the treatment of inflammatory conditions, and have potential value in the treatment of thrombotic disease in the horse. This study compares the potency of three nonsteroidal anti-inflammatory drugs phenylbutazone, naproxen (equiproxen) and flunixin meglumine (banamine) with respect to their effects on equine platelets. Two functional responses of horse platelets were evaluated in vitro: their ability to aggregate and their ability to make available platelet factor 3 procoagulant activity. Flunixin at a concentration of 10(-6) M signific...
Brown MP, Kelly RH, Stover SM, Gronwall R.Six healthy adult mares were given a single IV injection of trimethoprim (TMP)-sulfadiazine (SDZ) at a dosage rate of 2.5 mg of TMP/kg of body weight and 12.5 mg of SDZ/kg. Serum, synovial, peritoneal, and urine TMP-SDZ concentrations were measured serially over a 48-hour period. The highest measured mean concentrations of TMP and SDZ were found in the first (0.5 hour) sample of serum, synovial fluid, and peritoneal fluid. The mean peak concentrations of TMP and SDZ averaged 4.37 micrograms/ml and 21.81 micrograms/ml for serum, 2.95 micrograms/ml and 15.31 micrograms/ml for synovial fluid, and...
Igwe OJ, Blake JW.The disposition kinetics of pemoline after iv and oral administration of 2.4 mg/kg of the drug were studied. The elimination half-life was 39.4 hr. The mean volume of distribution was 1.5 liters/kg indicating extensive tissue distribution and sequestration for an amphoteric drug. Plasma protein binding determined by in vitro equilibrium dialysis was concentration dependent. The mean binding capacity was found to be 0.80 mu-mol/g, an apparent dissociation constant of 3.73 X 10(-5) molar, and a total plasma protein concentration of 64.7 g/liter. The mean systemic availability by oral administrat...
Prescott JF, Hoover DJ, Dohoo IR.The pharmacokinetic parameters of erythromycin in foals were determined following intravenous administration of 5.0 mg/kg to animals aged 1, 3, 5 and 7 weeks. The distribution of the drug was described by a two-compartment open model, and no significant differences were observed between coefficients on which the parameters were based. Pharmacokinetic values were also determined for four mares given 5.0 mg/kg intravenously and for six 10-12-week-old foals given 20.0 mg/kg intravenously. The half-life of erythromycin for all groups of animals (foals less than 7 weeks, mares, foals 10-12 weeks) w...
Ducharme NG, Fubini SL.Atropine sulfate was given at 2 dosages (0.044 mg/kg, 0.176 mg/kg) to clinically normal ponies in order to evaluate the drug's effect on the gastrointestinal tract. Intestinal motility, as assessed by ausculation of borborygmus, was stopped 30 minutes after injection, but it gradually returned to normal within 12 hours. Signs of abdominal pain developed in 3 of 10 ponies. In 3 clinical cases of gastrointestinal disorder, prior atropine treatment was confusing to the diagnostician and resulted in delayed surgical treatment in 1 case. It was concluded that atropine should not be used for allevia...
Trolldenier H, Klarmann D, Krabisch P, Rohde J, Steiner A, Verspohl J.368 streptococcal strains from udder secretions of cattle (Sc. agalactiae, Sc. dysgalactiae, Sc. uberis) and 191 streptococcal isolates from horse specimens (Sc. equi ssp. zooepidemicus, Sc. equi ssp. equi) originating from different agricultural regions in Germany (Lower Saxony, in particular the region of Weser-Ems, Bavaria, Altmark) were investigated for their sensitivity to 4 beta-lactam antibiotics (benzylpenicillin, ampicillin, oxacillin, cefotaxime). Two different test methods were applied: the agar diffusion test for determination of the diameter of the zone of inhibition and the E-tes...
Brotherton HO, Yost RA.A screening and confirmation procedure for drugs and metabolites in the blood serum and urine of racing animals was developed. Equine blood serum was spiked with low concentrations of several drugs of interest. Canine blood serum and urine were collected following oral doses of diethylcarbamazine, procaine, and phenylbutazone. Serum, urine, and extracts of each were analyzed, using a triple quadrupole mass spectrometer. Simultaneous screening of up to 50 drugs was possible in a single sample, in less than 2 minutes. Detection limits for most compounds were in the ng/ml to microgram/ml range, u...
Vonaparti A, Lyris E, Panderi I, Koupparis M, Georgakopoulos C.Two simple and rapid LC/MS methods with direct injection analysis were developed and validated for the quantification and identification of hydrocortisone in equine urine using the same sample preparation but different mass spectrometric systems: ion trap mass spectrometry (IT-MS) and time-of-flight mass spectrometry (TOF-MS). The main advantage of the proposed methodology is the minimal sample preparation procedure, as particle-free diluted urine samples were directly injected into both LC/MS systems. Desonide was used as internal standard (IS). The linear range was 0.25-2.5 microg ml(-1) for...
Zertuche JM, Brown MP, Gronwall R, Merritt K.Pharmacokinetic values for flunixin meglumine (1 mg/kg of body weight) and phenylbutazone (4 mg/kg) dosages were determined after a single IV injection with and without concurrent intragastric administration of probenecid (50 mg/kg) in 6 healthy mares. Significant difference was not apparent in the pharmacokinetic values of flunixin meglumine with and without concurrent probenecid administration. Significant (P less than or equal to 0.05) increase was evident in the 12-hour mean concentration of phenylbutazone (11.45 +/- 1.66 micrograms/ml without probenecid; 14.56 +/- 1.20 micrograms/ml with ...
Karatt TK, Sathiq MA, Laya S, Philip M, Karakka Kal AK, Subhahar MB.An effective alternative to testosterone therapy is selective androgen receptor modulators, a class of compounds that has a tissue-specific effect on muscle and bone. These drugs, which enhance performance, pose a severe abuse risk in competitive sports. GLPG0492 is one of the selective androgen receptor modulators discovered in recent decades. This compound has a unique tissue-specific action for muscle and bone against steroid receptors and acts as a partial agonist for androgen receptors. This study examined GLPG0492 and its metabolites in vitro using equine liver microsomes. Liquid chromat...
Lyons ET, Drudge JH, Tolliver SC.Antiparasitic activity of a micronized formulation of the benzothiazole compound, tioxidazole, at the dose rate of 11 mg/kg, was evaluated by the critical test method. Drug was given by stomach to 3 horses and on feed to 3 horses. Excellent removal activity was found for Strongylus vulgaris (100%) in 5 naturally infected horses, S edentatus (91% to 100%) in 5 horses, small strongyles (88% to 99%) in 6 horses, immature Oxyuris equi (100%) in 5 horses, and Parascaris equorum (100%) in 5 horses (a 6th horse had 10 small specimens present at necropsy). There was no measurable activity against bots...
Kamerling SG, Cravens WM, Bagwell CA.1. Detomidine is a novel veterinary sedative analgesic which is thought to act by stimulation of alpha 2 adrenoreceptors. The present study was undertaken to determine the direction, time course, and dose-response relationship of detomidine on specific autonomic responses in the unanaesthetized horse. 2. Detomidine was administered intravenously to eight adult thoroughbred racehorses at doses of 0.010-0.040 mg kg-1, according to a double-blind Latin square crossover design. Cardiac and respiratory rates, pupil diameter and rectal temperature were monitored for 180 min postinjection. 3. Detomid...
Camargo FC, Robinson NE, Dirikolu L, Berney C, Eberhart S, Derksen FJ, Lehner AF, May J, Hughes C, Tobin T.Trimetoquinol (TMQ) is a very potent and fast acting bronchodilator in horses with heaves. This study assessed the plasma and urinary concentrations of TMQ in horses with heaves following administration via the intravenous (IV, 0.2 microg/kg) and intra-tracheal (IT, 2 microg/kg) routes. TMQ was administered to six horses affected with heaves (RAO - Recurrent Airway Obstruction, used interchangeably) by the above routes and plasma and urine samples collected and stored at -20 degrees C until analyzed. Solid Phase Extraction (SPE) of TMQ was followed by highly sensitive ESI(+)-LC-MS-MS (ElectroS...
Stanley SD, McKemie D, Skinner W.A rapid, sensitive, and rugged method for detecting drugs and drug metabolites in extracts of horse urine is described. The use of large-volume injection (LVI) gas chromatography-mass spectrometry (GC-MS) for analysis of horse urine extracts allowed automation of the derivatization procedure and reduction of the sample volume from 5 mL to 1 mL of urine. An autosampler and temperature-programmable inlet were used to automatically dissolve the sample extract and form trimethylsilyl derivatives of over 200 analytes. The suitability of this procedure for routine GC-MS detection of approximately 80...
Gowen RR, Lengel JG.The control of drug use in performance horses and the policing of rules and regulations to prevent unauthorized drug use are important tasks for agencies overseeing equestrian events. This article describes the roles of the American Horse Shows Association, the Federation Equestre Internationale, and the Association of Racing Commissioners International, Inc, in the policing of drug use in horses competing in events under their control.
Kwok WH, Choi TLS, Leung GNW, Wong ASY, Yue SK, Wan TSM, Ho ENM.The insulin-like peptide relaxin (RLX), an endogenous peptide hormone produced in human for pregnancy and reproduction, is also known to exert a range of physiological and pathological effects. Its use is banned in human sports, horseracing, and equestrian competitions due to its potential performance enhancing effect through vasodilation resulting in the increase of blood and oxygen supplies to muscles. Little is known about the biotransformation and elimination of RLX in horses. This paper describes an administration study of rhRLX-2 and its elimination in horses, and the development of sens...
Camargo FC, Robinson NE, Berney C, Eberhart S, Baker S, DeTolve P, Derksen FJ, Harkins JD, Lehner AF, Tobin T.Trimetoquinol (TMQ) is a potent beta-adrenoceptor agonist bronchodilator used in human medicine but has not been evaluated for potential use as a therapeutic agent for horses with 'heaves'. Objective: To assess the pharmacodynamics of TMQ in horses with 'heaves' to determine potential therapeutic effects. Methods: Increasing doses of TMQ were administered to horses with 'heaves' by i.v. and intratracheal (i.t.) routes. Doses ranged 0.001-0.2 microg/kg bwt i.v. and 0.01-2 microg/kg bwt i.t. Cardiac and airways effects were assessed by measurement of heart rate (HR) and maximal change in pleural...
McKeever KH.This article has presented information on the importance of the sympathetic nervous system in the response to exercise. The authors have reviewed the very limited information on the effects of sympathomimetic and sympatholytic drugs on exercise performance in the horse. Most of these drugs are specifically prohibited under the rules of racing, and they have significant side effects that either decrease performance or make their use dangerous to both the horse and horse-man. Additionally, all of these drugs or their metabolites are readily detected by current drug testing protocols. Further inf...
Popot MA, Donval A, Bonnaire Y, Huau J.Feces are a possible medium to be used for horse doping control. Efficient methods for detecting drugs in feces collected from various animals are routinely applied in institutes of food safety in Belgium. We have already tested whether they are applicable to horse feces. In this report, accelerated solvent extraction (ASE), an efficient method for extracting compounds from solid material, has been tested. ASE has been used to replace the diethyl ether liquid-liquid extraction step present in the method initially set up. This technique has been optimized for detecting several non-steroidal ant...
Errecalde JO, Landoni MF.The pharmacokinetics of a slow-release theophylline formulation was investigated following intravenous and oral administration at 10 mg/kg in horses. A tricompartmental model was selected to describe the intravenous plasma profile. The elimination half-life (t1/2 beta) was 16.91 +/- 0.93 h, the apparent volume of distribution (Vd) was 1.35 +/- 0.18 L/kg and the body clearance (ClB) was 0.061 +/- 0.009 L kg-1 h. After oral administration the half-life of absorption was 1.24 +/- 0.30 h, and the calculated bioavailability was above 100%. The t1/2 beta after oral administration was 18.51 +/- 1.75 ...
Pinetre J, Delcourt V, Becher F, Garcia P, Barnabé A, Loup B, Popot MA, Fenaille F, Bailly-Chouriberry L.Many innovative biotherapeutics have been marketed in the last decade. Monoclonal antibodies (mAbs) and Fc-fusion proteins (Fc-proteins) have been developed for the treatment of diverse diseases (cancer, autoimmune diseases, and inflammatory disorders) and now represent an important part of targeted therapies. However, the ready availability of such biomolecules, sometimes characterized by their anabolic, anti-inflammatory, or erythropoiesis-stimulating properties, raises concerns about their potential misuse as performance enhancers for human and animal athletes. In equine doping control labo...
McDonald J, Gall R, Wiedenbach P, Bass VD, DeLeon B, Brockus C, Stobert D, Wie S, Prange CA, Yang JM.We investigated the use of particle concentration fluorescence immunoassay (PCFIA) as a technique for drug detection in racing horses. The test was constructed from an antiserum to a carboxyfentanyl-BSA conjugate and carboxyfentanyl linked to b-Phycoerythrin. Using these reagents and a PCFIA apparatus levels of fentanyl as low as 0.1 ng/ml could be detected by the assay. In addition, cross-reactivity studies on this assay showed that the anti-serum cross-reacted well with carfentanil, sufentanil and the methylated analogs of fentanyl. We therefore evaluated the ability of these agents to produ...
Fuentes VO, Gonzalez H, Sanchez V, Fuentes P, Rosiles R.The toxic effect of neomycin on the horse kidney was studied. Twelve horses were used, and were divided at random into three groups of four. The first group was treated twice a day with 10 mg/kg I.M. for 15 days and then euthanised; kidney and liver samples were studied and no histopathological changes were observed. Group 2 was treated with neomycin sulphate as in group 1, and group 3 was used as control. Blood samples were taken at 8.00 h and 20.00 h daily from both neomycin treated and control horses. Serum creatinine, potassium, sodium and urinary creatinine remained without change. On day...
Haywood PE, Chalmers P.The chromatographic and spectroscopic properties of several unusual substances which have been detected in the "alkaloidal" chloroform extract from racehorse urine and saliva samples are reported. Some of these substances have been identified by combined gas chromatography-mass spectrometry and the source of the substance is stated where this is known. Other substances whose identity is not known have been detected and their mass spectra show characteristic amine fragments. The occurrence of these unidentified substances is more frequent in aged urine samples and it would therefore appear that...
Jöchle W.Ovuplant (deslorelin STI), when used in estrous mares with a follicle > or = 30 mm, reliably causes acceleration of ovulation and assurance that > 80% of the treated mares will ovulate within 48 hours. Time to ovulation is reduced by 30 hours or more. Treatment with Ovuplant had no adverse effects on pregnancy rates and did not increase the rate of early twin pregnancies. Treatment did not cause local or systemic side effects beyond short-term local irritation. Mares can be treated repeatedly without the development of tolerance or the loss of effectiveness. These studies have shown that...
Marzok M, Almubarak AI, Kandeel M, El-Khodery S.Epidural analgesia using the alpha-2 agonist detomidine (DE), alone or in combination with lidocaine (LD), is frequently employed for standing surgical procedures in horses, but its use has not been evaluated in donkeys. Methods: In a randomised controlled prospective trial, 24 healthy adult donkeys were assigned to four groups (n = 6), each receiving 40 μg/kg of DE, 0.22 mg/kg of LD, combined DE and LD (DELD) or 0.9% sterile normal saline epidurally. After epidural injection of each treatment, the onset, degree and duration of sedation and anatomical extension of anti-nociception were obse...
Beech J, Kohn C, Leitch M, Weinstein AJ, Gallagher M.Serum, synovial fluid, and urine concentrations of gentamicin were measured in normal mature horses which had been given a single dose of the drug. Mean peak serum concentration (16.8 microgram/ml) occurred in horses 30 minutes after they were given a single intramuscular dose of 4.4 mg of gentamicin/kg of body weight. In horses given a smaller dose of gentamicin (1.7 mg/kg), mean peak serum concentrations of gentamicin (10.2 microgram/ml) appeared at 1 hour. Synovial fluid concentration was maximum at 2 hours for both doses; in horses given the larger dose, mean peak concentration was 6.4 mic...
Britt DP, Clarkson MJ.The presence of benzimidazole-resistant strains of equine small strongyles was confirmed in horses at two properties in north west England by a series of faecal egg counts and larval cultures after treatment with mebendazole. A trail formulation of mebendazole in combination with piperazine citrate gave greater reductions in faecal egg counts than mebendazole alone but was much less effective than pyrantel embonate or dichlorvos.
Smetzer DL, Senta T, Hensel JD.Each of nine horses was treated with amphetamine alone, with atropine alone, and with amphetamine and atropine in combination. Cardiac effects of these drugs were studied by electrocardiography during resting and exercising states and immediately after exercise. Although each treatment increased heart rate significantly during the resting state, only the amphetamine plus atropine treatment increased heart rate significantly during exercise. Decrease in heart rate immediately after exercise differed significantly for each treatment; the most rapid decrease in heart rate was found after the amph...
Snow DH, Douglas TA.The absorption characteristics of a new paste preparation of phenylbutazone were studied in ponies and thoroughbreds. The results suggested that at a similar dose rate of 5 mg/kg greater bioavailability results from the paste than from a powder preparation. Delivery of an accurate dosage of the paste was not possible using the multidose applicator. Repeated administration of the paste preparation (5 mg/kg twice daily) indicated that it is more toxic to both ponies and thoroughbreds than a powder preparation. In addition to the toxic manifestations previously reported, a neutropenia developed d...
Schellenberg LM, Regenthal R, Abraham G.The present study addresses the effect of the Rho-kinase (ROCK) inhibitor Y-27632 on the β-adrenoceptor density and β-agonist-stimulated intracellular second messenger cAMP formation in primary equine bronchial epithelial cells (EBEC). Y-27632 significantly decreased the β-adrenoceptor number (B) without markedly affecting the receptor affinity (dissociation constant, K) to the radioligand [I]-iodocyanopindolol (ICYP). In contrast, Y-27632 augmented the β-agonist-stimulated intracellular cAMP production. Herein, Y-27632 markedly increased the maximal cAMP responses (E) (isoproterenol >...
Hermans H, van den Berg EMH, Slenter IJM, Vendrig DJC, de Nijs-Tjon LJL, Vernooij JCM, Brommer H, Boevé MH, Gehring R.Topical dexamethasone and prednisolone are currently the mainstay treatment for equine ophthalmic inflammatory diseases, such as equine recurrent uveitis. Comparative pharmacokinetic studies in horses are lacking and current guidelines are mainly based on empirical data and extrapolation from other species. Objective: To investigate the penetration and local concentrations of topically applied dexamethasone and prednisolone in normal equine ocular fluids and serum. Methods: Prospective randomised experimental pharmacokinetic study. Methods: Twenty-one Shetland ponies without ophthalmic disease...
Craig AM, Blythe LL, Appell LH, Slizeski ML.Dimethyl sulfoxide (DMSO) had been postulated to be a 'masking agent' when used concurrently with therapeutic or prohibited drugs in racing animals. Eight drugs (flunixin, furosemide, caffeine, apomorphine, phenylbutazone, lidocaine, cocaine, and acepromazine maleate) were administered to six horses singly and with concurrent intravenous DMSO. Urine samples were analyzed for the presence of the drugs and/or their metabolites by thin layer chromatography. Direct comparison of thin layer chromatograms of extracts of positive urine samples with and without DMSO verified that DMSO did not interfer...
Rauws AG, van Schothorst M, Frik JF.The protein binding, the plasma half-life and the residue depletion of sulfamonomethoxine (SMM) after intramuscular administration were investigated in pigs, horses and cattle. Protein binding was weakly concentration-dependent. The bound fraction in plasma in the therapeutic range amounted to approximately 45, 40 and 50% for pigs, horses and cattle respectively, and the plasma half-lives were approximately 5.1, 5.7 and 3.1 hours respectively. SMM levels were less than 1 mug/g in muscle tissue after 36, 20 and 12 hours in pigs, horses and cattle respectively. In the kidney SMM levels were not ...
Knox DA, Ravis WR, Pedersoli WM, Spano JS, Nostrandt AC, Krista LM, Schumacher J.Six healthy mature horses were orally administered a single dose of phenobarbital (26 mg/kg of body weight), then multiple doses (13 mg/kg) orally for 42 consecutive days. Seventeen venous blood samples were collected from each horse after the single dose study and again after the last dose on day 42. Plasma phenobarbital concentration was determined by use of a fluorescence assay validated for horses. Additional blood samples (n = 11) were collected on days 8 and 25 to determine peak and trough concentrations, as well as total body clearance. Phenobarbital disposition followed a one-compartme...
