Pharmacokinetics in horses involves the study of how drugs are absorbed, distributed, metabolized, and excreted in equine species. This field of study provides insights into the time course of drug concentrations within the horse's body and helps in understanding the effects of various pharmaceuticals. Key parameters in equine pharmacokinetics include absorption rates, bioavailability, half-life, and clearance. These parameters can vary significantly due to factors such as age, breed, and health status of the horse. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetic profiles of different drugs in horses, aiming to optimize dosing regimens and improve therapeutic outcomes in equine medicine.
Allen WE, Ayliffe TR.Endometrial concentrations of sodium benzylpenicillin were determined in biopsy samples from anoestrous pony mares after intramuscular administration of the penicillin at 22,000 iu/kg. Serum samples, collected at the same time as biopsies, were also assayed for their penicillin content. In experiment 1 a single pair of blood and tissue samples was taken from each mare between five and 360 minutes after injection. In experiment 2 each mare was sampled consecutively six times (between five and 300 minutes) after injection. Both serum and endometrial concentration reached a peak between 15 and 30...
Sigel CW, Byars TD, Divers TJ, Murch O, DeAngelis D.Two fasted and 2 fed horses were dosed orally with a combined trimethoprim and sulfadiazine paste formulation at a dose of 35 mg (1:5 combined active ingredients)/kg. Serum concentrations of each drug were determined periodically for 3 consecutive days for the 4 horses. The extent and rate of absorption for trimethoprim were variable, but peak serum concentrations occurred generally within 3 hours; sulfadiazine absorption was slower, reaching peak concentrations by 6 hours. Fasting did not have a consistent effect on the serum concentration profiles for either drug. Both drugs achieved serum c...
Brown MP, Stover SM, Kelly RH, Farver TB.Six healthy adult mares were given a single dose of kanamycin sulfate (200 mg/ml) IM at a dosage rate of 5 mg/kg of body weight. Kanamycin concentrations in serum, synovial fluid, peritoneal fluid, and urine were measured serially over a 48-hour period. The mean peak serum kanamycin concentration was 12.55 microgram/ml at 1 hour. Mean peak kanamycin concentrations in synovial fluid and peritoneal fluid were 7.25 microgram/ml and 9.27 microgram/ml at 2 hours and 3 hours, respectively. These concentrations decreased steadily in parallel with serum concentrations and were still measurable at 48 h...
Doyle A, Owen LN.Sixteen cytotoxic drugs used in cancer chemotherapy in man were studied for cytopathic effect on equine fibrosarcoma, melanoma and normal equine lung cells in vitro. Three drugs, vincristine, melphalan and methotrexate, produced cytopathic effect
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...
Marsh MV, Caldwell J, Smith RL, Horner MW, Houghton E, Moss MS.1. 14C-Labelled benzoic acid, salicylic acid and 2-naphthylacetic acid were administered orally to horses, and urinary metabolites investigated by chromatographic and mass spectral techniques. 2. [14C]Benzoic acid (5 mg/kg) was eliminated rapidly in the urine, and quantitatively recovered in 24 h. The major urinary metabolite was hippuric acid (95% of dose) with much smaller amounts of benzoic acid, benzoyl glucuronide and 3-hydroxy-3-phenylpropionic acid. Administration of [ring-D5]benzoic acid together with [14C]benzoic acid to a pony permitted the mass spectral determination of metabolites ...
Combie J, Blake JW, Ramey BE, Tobin T.Morphine was detected in equine biological fluids by a combination of liquid-liquid extraction and column chromatography, followed by derivatization and gas-liquid chromatographic assay, using electron capture detector. Recovery of morphine from the equine biological samples was poor. However, despite an overall recovery of less than 20%, this method had a detection limit of 0.2 ng/ml. Addition of 5,000 U of bovine liver beta-glucuronidase/ml of urine enabled detection of the drug in urine for up to 144 hours after horses were given 0.1 mg of morphine/kg of body weight. Morphine was found for ...
Pedersoli WM, Ravis WR, Belmonte AA, McCullers RM.Digoxin (elixir, 0.022 mg/kg) was administered via stomach tube to healthy horses of mixed breeding and sexes. Serum digoxin concentrations reached a peak (2.21 +/- 0.6 ng/ml) at approximately 1 hour after dosing and had a half-life of 28.8 +/- 10.7 hours. Digoxin kinetics followed a triexponential curve, indicating that at least a 2 compartmental model is required to characterize the serum concentration-time curve after this route of administration. It was calculated that to achieve average serum concentrations of 1.1 ng/ml, an oral dose of 17.4 microgram of digoxin elixir/kg/day and an IV do...
Gerring EL, Lees P, Taylor JB.Phenylbutazone was given orally to 2 groups of horses and the plasma levels of the drug and its 2 principal metabolites oxyphenbutazone and gamma-hydroxyphenylbutazone measured by high performance liquid chromatography. Animals in Group 1 received single oral doses in a range from 1.1 to 13.2 mg/kg and were sampled over the succeeding 24 h. Considerable individual variation was observed both in timing and magnitude of the plasma drug responses between horses, but 24 h after dosing a clear dose response relation was recorded. Group 2 horses were given the recommended therapeutic dosage regimen ...
Divers TJ, Byars TD, Murch O, Sigel CW.Proteus mirabilis cystitis was induced in 9 ponies by chemically eroding the bladder mucosa before the organism was inoculated. Comparisons were made in the treatment of P mirabilis cystitis between ponies treated daily for 13 days with a trimethoprim-sulfadiazine (TMP-SDZ) paste and both positive and negative controls. Urine cultures from ponies treated with TMP-SDZ became negative for P mirabilis between days 3 and 9 after the start of the treatment, whereas positive controls remained infected until day 13. Urine cultures from all ponies were negative for P mirabilis on day 28. Urine concent...
Hall LW, Taylor PM.One hundred anaesthetics were administered in a clinical trial to 95 equine patients, ranging in age from nine months to 19 years and in weight from 140 to 1270 kg, undergoing a variety of surgical procedures. Acepromazine maleate premedication (0.01 to 0.03 mg per kg intramuscularly) was given to seven animals, the remainder were not premedicated. Xylazine (1.1 mg per kg) was injected intravenously over a two minute period and after a pause of two minutes ketamine (2.2 mg per kg) was injected rapidly by the same route. For 30 procedures no other anaesthetic was given but in 59 cases anaesthes...
Slocombe JO, McCraw BM.Twelve pony foals were reared worm-free and inoculated with Strongylus vulgaris. On day 7 after inoculation, 6 ponies were given ivermectin IM at a dose of 200 micrograms/kg of body weight and on day 28 were necropsied. Ivermectin was effective in eliminating early 4th-stage S vulgaris larvae and reducing clinical signs associated with acute arteritis. After administrative ivermectin was effective against early 4th-stage Strongylus vulgaris larvae in ponies when administered at 100, 300, or 800 micrograms/kg of body weight. The purpose of the present study was to report on a more extensive tri...
Lyons ET, Drudge JH, Tolliver SC.Critical tests were conducted in 14 naturally infected equids (13 horses and 1 pony) to evaluate the antiparasitic activity of haloxon. Single doses were administered by stomach tube to 3 horses and 1 pony (60 mg/kg of body weight), by addition to the feed of 3 horses (60 mg/kg), and intraorally by powder gun to 7 horses (65 mg/kg). Haloxon was efficacious (99% to 100%) against infections of Parascaris equorum, Oxyuris equi (mature and immature), and Strongylus vulgaris at both dosage levels. Probstmayria vivipara parasites were removed in 1 horse treated at 60 mg/kg by stomach tube and S equi...
McGuirk SM, Muir WW, Sams RA.A pharmacokinetic study was made, using 7 healthy adult horses (weighing between 400 and 560 kg) given quinidine gluconate IV and quinidine sulfate orally. The apparent volume of distribution of quinidine base was 3.10 +/- 0.79 L/kg, total body clearance was 5.49 +/- 2.40 ml/minute/kg, and plasma half-life was 6.65 +/- 3.00 hours. The systemic availability of quinidine sulfate after oral administration of a 10 mg/kg dose was 48.5 +/- 20.4%. Oral administrations of quinidine sulfate in doses of 10 mg/kg and 10 g produced peak plasma concentrations of 0.79 microgram/ml at 146 minutes and 1.47 mi...
Garcia-Villar R, Toutain PL, Alvinerie M, Ruckebusch Y.The pharmacokinetic disposition of xylazine hydrochloride is described after both intravenous and intramuscular injection of a single dose, in four domestic species: horse, cattle, sheep and dog, by an original high performance liquid chromatographic technique. Remarkably small interspecific differences are reported. After intravenous administration, systemic half-life (t1/2 beta) ranged between 22 min (sheep) and 50 min (horse) while the distribution phase is transient with half-life (t1/2 alpha) ranging from 1.2 min (cattle) to 5.9 min (horse). The peak level of drug concentration in the pla...
Snow DH, Baxter P, Whiting B.The pharmacokinetics of meclofenamic acid were studied in Thoroughbred horses and in ponies. After intravenous (i.v.) administration of either 2 mg/kg or 4 mg/kg sodium meclofenamate the elimination half-life was of the order of 0.9 h while the volume of distribution was found to be 0.128 litre/kg. Elimination was in accordance with a one-compartment model. Following oral administration of either meclofenamic acid (4 mg/kg) or sodium meclofenamate (4 mg/kg) a much longer terminal half-life than that calculated for Kel from i.v. data was found. This anomaly indicated that the 'flip-flop' phenom...
Shults T, Kownacki AA, Woods WE, Valentine R, Dougherty J, Tobin T.In horses given (rapid IV) methylphenidate (Ritalin, alpha-phenyl-2-piperidinacetic acid methyl ester; 0.70 mg/kg), plasma concentrations of the drug decreased rapidly at first, with an apparent alpha half-life of about 19 minutes, and then more slowly, with an apparent beta half-life of about 2.4 hours. These data were well fitted by a 2-compartment open model. In blood, about 40% of the methylphenidate present was in the plasma fraction, and of this, about 80% was plasma-protein bound. If given by subcutaneous or IM injection, plasma concentrations of methylphenidate peaked in about 1 hour a...
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...
Burrows GE.Endotoxins are non-protein fragments of the cell wall of Gram-negative bacteria. They must be absorbed into the circulation to produce disease and systemic effects are similar, regardless of bacterial source. Absorption of endotoxins occurs in obstructive bowel disease and may play a significant part in determining the severity of the disease. Many of the responses to experimentally administered endotoxin are identical to those of bowel diseases or the horse and include circulatory, haematological and metabolic alterations. Therapeutic approaches are indirect and include many drugs currently e...
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 ...
Wong JKY, Leung DKK, Curl P, Schiff PJ, Lam KKH, Wan TSM.The detection of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione in a urine sample collected from a gelding having been treated with testosterone (500 mg 'Testosterone Suspension 100', single dose, injected intramuscularly) in 2009 led the authors' laboratory to suspect that these 'testicular' steroids could be minor metabolites of testosterone in geldings. Administration trials on six castrated horses with Testosterone Suspension 100 confirmed that low levels of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione could indeed be detected ...
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...
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...
Soma LR, Uboh CE, Rudy JA, Smith MS.To examine, in horses, the disposition and excretion of the active metabolite 6-methoxy-2-naphthylacetic acid (6MNA) of the nonsteroidal anti-inflammatory prodrug nabumetone. Methods: Pharmacokinetic analysis of 6MNA after oral administration of nabumetone and IV administration of 6MNA. Methods: Using a crossover design, 5 horses were orally administered 3.7 mg of nabumetone/kg of body weight. After a 3-week washout period, 4 horses were administered 2.5 mg of 6MNA/kg, IV. Results: Absorption of nabumetone from the gastrointestinal tract and its metabolism to 6MNA had a median appearance half-...
Skarda RT, Muir WW, Couri D.Arterial and/or central venous plasma concentrations of lidocaine were determined in 12 nonmedicated adult horses (422 +/- 59 kg of body weight, mean +/- SD) after injecting a 1% lidocaine HCl solution into the cervicothoracic ganglion (CTG). A mean dosage of 2.9 +/- 0.5 mg of lidocaine/kg of body weight was used to induce unilateral CTG blockade in 8 horses and 4.8 +/- 0.8 mg was used to induce bilateral CTG blockade in 4 horses. Blood samples were collected before and at 5, 15, 30, 45, 60, 75, 90, 105, and 120 minutes after injection. The plasma lidocaine concentrations were determined by us...
Yılmaz İ, Maraş Z, Uğur Y, Erkan Özgür M, Durmaz M, İbrahim Ulusoy H, Erdoğan S.Metamizole sodium (MT) is an analgesic and antipyretic drug molecule used in humans, horses, cattle, swine, and dogs. Metamizole rapidly hydrolyzes and turns into methylamino antipyrine (MAA), an active primary metabolite of MT. The present study aims to determine the pharmacokinetic (PK) profiles of MT metabolites after intravenous (IV) and intramuscular (IM) administration into sex of Arabian horses (Equus ferus caballus) using a cross-over study design. The plasma samples were extracted by solid-phase extraction (SPE) method, and plasma concentrations of MT metabolites were analyzed by high...
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...
Bhutia WD, Gupta S, Rani R, Batra K, Sethi K, Kumar S, Kumar R.Trypanosoma evansi is a causative agent of chronic wasting and fatal disease of livestock and wild animals known as surra. In this study, repurposing approach based on drug target was used to investigate the efficacy of kinase inhibitors (Barasertib-HQPA, BAR and Palbociclib isethionate, PAL) and protease inhibitors (Z-pro-prolinal, Z-PRO and Leupeptin hemisulphate, LEU) against T. evansi in HMI-9 medium. BAR, PAL and Z-PRO exhibited IC values of 13.52 µM, 0.6375 µM and 63.20 µM against T. evansi in terms of growth inhibition, in the contrary, LEU failed to exhibit a significant growth i...
Cox S, Yarbrough J.A new method of analysis has been developed and validated for the determination of firocoxib, a new nonsteroidal anti-inflammatory drug (NSAID) approved for use in horses and dogs to control pain and inflammation associated with osteoarthritis. Following a liquid extraction using ethyl acetate:hexane (40:60), samples were separated by isocratic reversed-phase HPLC on a Sunfire C(18) column and quantified using UV detection at 290 nm. The mobile phase was a mixture of water with 0.025% trifluoroacetic acid and acetonitrile, with a flow-rate of 1.1 ml/min. The procedure produced a linear curve o...
Chou CC, Chen CL, Asbury AC, Webb AI, Vickroy TW.To develop an ELISA that is sensitive and suitable for measurement of immunoreactive acepromazine (ACP) in horse serum and urine and to determine the acute effects of exercise on immunoreactive ACP values in Thoroughbreds. Methods: 12 healthy Thoroughbreds (5 mares, 5 geldings, 2 stallions), aged 2 to 8 years. Methods: A commercially available antibody and a horseradish peroxidase-conjugated oxime derivative of immunoreactive ACP were used to develop a one-step ELISA. Horses were used in a crossover design study to evaluate possible effects of treadmill exercise on serum and urine ACP concentr...
Ross J, Dallap BL, Dolente BA, Sweeney RW.To determine the pharmacokinetics and pharmacodynamics of epsilon-aminocaproic acid (EACA), including the effects of EACA on coagulation and fibrinolysis in healthy horses. Methods: 6 adult horses. Methods: Each horse received 3.5 mg of EACA/kg/min for 20 minutes, i.v. Plasma EACA concentration was measured before (time 0), during, and after infusion. Coagulation variables and plasma alpha(2)-antiplasmin activity were evaluated at time 0 and 4 hours after infusion; viscoelastic properties of clot formation were assessed at time 0 and 0.5, 1, and 4 hours after infusion. Plasma concentration ver...
Fatemikia H, Kamyab M, Movahed A, Sadeghi M, Kim E, Behdani M, Mohammadpour Dounighi N, Shahrivar M, Seyedian R.In this study, the neutralizing abilities of the equine and the recently introduced camelid antivenoms on the hemodynamic parameters (inotropism, chronotropism, and arrhythmogenicity) were assessed following envenomation by venom in rats. Methods: At first, the electrophoretic profiles of both products were obtained by using the SDS-PAGE method (12.5%) and stained with Coomassie blue and silver nitrate. Secondly, different doses of the camelid antivenom (10, 50, and 100 µl) were given intravenously in 10 min before venom injection (400 µg/rat). The neutralizing potencies of camelid and equi...
Harkins JD, Mundy GD, Stanley S, Woods WE, Sams RA, Richardson DR, Tobin T.Isoxsuprine is a therapeutic medication used to treat navicular disease and other lower limb problems in horses and is one of the more frequently detected therapeutic agents in racing horses. In a crossover study, horses were administered isoxsuprine i.v. to determine the character and duration of its pharmacological effects. Isoxsuprine significantly increased heart rate 5-150 min following injection. Unrestrained activity following isoxsuprine treatment was significantly greater than control activity for 105 min after treatment. There was an apparent, although statistically nonsignificant, i...
Chu KK, Wang N, Stanley S, Cohen ND.The pharmacokinetic behavior of furosemide concentrations in performance horses is of great interest to the equine industry and equine researchers. Specifically, such information is useful for the evaluation of the existing guidelines in several racing jurisdictions and for the possible development of new guidelines for varying time periods after administration. We studied several approaches within the framework of nonlinear mixed effects models to increase the accuracy of evaluating these guidelines. Theoretical properties of the proposed methods were examined and the variances of the resulti...
Van Eenoo P, Delbeke FT, Roels K, Baert K.Non-steroidal anti-inflammatory drugs (NSAIDs) are prohibited by the International Federation of Horse Racing Authorities but are commonly used in veterinary practice. Plasma and urinary concentrations of the NSAID tolmetin were determined by a high-performance liquid chromatographic procedure with UV detection following oral administration of a dose of 1 g to six fasted untrained standard bred mares. With a limit of quantitation (LOQ) of 0.05 microg/ml tolmetin was present in plasma for 9-12 h post-administration. Maximum concentrations of 2.1+/-0.89 microg/ml were found after 0.7+/-0.25 h. T...
Roberts CJ, Jackson LS.The development, validation, and application of an ELISA for dexamethasone in equine urine is described. The drug-protein conjugate was immobilised in microtitre plate wells and antiserum raised against the same drug-protein conjugate was allowed to compete with sample or standard drug and the immobilised drug-protein conjugate. The proportion of antiserum binding to the immobilised drug-protein conjugate was detected using a biotinylated protein G/extravidin-alkaline phosphatase complex in situ and measurement of the substrate product. The method was used to detect the presence of drug-derive...
Kim Y, Seo C, Oh S, Kwak J, Jung S, Sin E, Kim H, Ji M, Lee HS, Park HJ, Lee G, Yu J, Kim M, Lee W, Paik MJ.Loxoprofen is a non-steroidal anti-inflammatory drug of the 2-arylpropionic acid type, which has used to treat musculoskeletal disorders in the horse racing industry. However, it has also used illicitly to mask clinical signs of inflammation and pain in racehorses. Thus, its accurate analysis has become an important issue in horse doping laboratories. In this study, an analytical method of loxoprofen was developed as tert-butyldimethylsilyl (TBDMS) derivative by gas chromatography-mass spectrometry (GC-MS). Characteristic fragment ions of [M-15], [M-57], and [M-139] permitted the accurate and ...
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...
Delbeke FT, Landuyt J, Debackere M.A high-performance liquid chromatographic method to measure plasma and urinary alclofenac levels in equine biofluids is described. Isolation of the drug from plasma is achieved using liquid-liquid extraction with diethyl ether. Reversed-phase C18 solid phase extraction is used for the extraction of free and conjugated alclofenac from urine. The reproducibility and accuracy of the method were well within acceptable limits over the concentration ranges 0-10 and 0-20 micrograms/ml, respectively, for plasma and urine. Starting with 2 ml of plasma, a concentration of 0.1 microgram/ml could easily b...
Ekstrand C, Nostell K, Gehring R, Bondesson U, Bröjer J.Septicaemia in the neonatal foal is caused by both Gram positive and Gram negative bacteria. The life-threatening nature of this condition requires treatment to be initiated with broad spectrum antimicrobial drugs pending antimicrobial susceptibility testing. Potentiated sulphonamides, for example, trimethoprim combined with sulfadiazine, could be clinically relevant options but their pharmacokinetics in the neonatal foal are unknown. To describe the plasma disposition of trimethoprim and sulfadiazine in neonatal foals and to relate the results to patterns in the minimum inhibitory concentrati...
Berryhill EH, Knych H, Edman JM, Magdesian KG.The neurokinin-1 (NK) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood and likely under-recognized in horses. Use of NK-1 receptor antagonists in horses has not been reported. The purpose of this study was to determine the pharmacokinetic profile of maropitant in seven adult horses after single intravenous (IV; 1 mg/kg) and intragastric (IG; 2 mg/kg) doses. A randomized, crossover design was performed. Serial blood samples were collected after dosing; maropitant concentrations were measured using LC-MS/MS. Pharmacokinetic pa...
Fintl C, Ihler CF.D(+)-xylose absorption tests are commonly performed when investigating suspected small intestinal malabsorption in the horse. The test involves the administration of a D(+)-xylose solution via a nasogastric tube followed by serial blood sampling to determine its rate of absorption. In some horses, nasogastric intubation cannot be safely performed without prior administration of a sedative. Due to its short duration of action, the α(2) agonist xylazine is commonly used for this purpose. However, α(2) agonists have also been reported to influence the rate of gastric emptying as well as small i...
