Oral administration in horses refers to the delivery of medications, supplements, or nutrients via the mouth. This method is commonly used in equine veterinary medicine for its practicality and ease of use. Oral formulations can include powders, pastes, or liquids, which are designed to be palatable and easily ingested by horses. The effectiveness of oral administration depends on factors such as the horse's digestive physiology, the formulation of the product, and the consistency with which it is administered. This page compiles peer-reviewed research studies and scholarly articles that explore the techniques, efficacy, and considerations of oral administration in equine care.
Peroni DL, Stanley S, Kollias-Baker C, Robinson NE.Based on its efficacy for the treatment of human asthma, the corticosteroid prednisone is commonly used in horses for treatment of recurrent airway obstruction. However, recent studies have failed to show any benefit of prednisone tablets for the treatment of this condition. The purpose of this study was to determine why oral prednisone has poor efficacy for the treatment of heaves in horses. In a crossover study, 5 horses were given the following treatments: prednisone tablets, prednisone liquid, prednisolone tablets, prednisolone liquid and i.v. prednisolone sodium succinate (positive contro...
Pérez R, Cabezas I, Godoy C, Rubilar L, Muñoz L, Arboix M, Castells G, Alvinerie M.A study was undertaken in order to compare plasma disposition kinetic parameters of doramectin (DRM) and ivermectin (IVM) in horses after oral administration. Ten crossbreed adult horses, clinically healthy, weighing 380-470 kg body weight (bw) were selected for study. Faecal examinations were performed to determine faecal parasite egg counts. Horses were allocated to two groups of five animals to provide an even distribution considering the variables sex, body weight and faecal egg count. Group I, were treated with an oral paste formulation of IVM at 0.2 mg/kg b/w and Group II, were treated w...
Lakritz J, Wilson WD, Marsh AE, Mihalyi JE.Plasma concentrations and pharmacokinetics of erythromycin and related compounds were determined after administration of erythromycin ethylsuccinate to six healthy male foals 3 to 5 months of age. Hay was withheld from the foals overnight and erythromycin ethylsuccinate (25 mg/kg of body weight) was administered intragastrically. Plasma erythromycin concentrations were determined at specific times after drug administration by high-performance liquid chromatography assay. Maximum peak plasma concentrations, time to maximum concentrations, area under plasma concentration versus time curves, elim...
Gokbulut C, Nolan AM, McKellar QA.Oxibendazole (OBZ) was administered to eight horses at an oral dose of 10 mg kg(-1) bodyweight each. Parent OBZ could only be detected in plasma at the 0.5 and 1.0 hours post administration sampling times and the mean maximum plasma concentration was 0.008 microg ml(-1). Parent OBZ was detected in faeces between 12 and 72 hours after administration and the highest dry faecal concentration was detected at 24 hours. An unidentified metabolite was detected in plasma between 0.5 and 72 hours. The unidentified metabolite in the plasma of treated horses corresponded to the second eluted metabolite i...
Davis JL, Gardner SY, Jones SL, Schwabenton BA, Papich MG.The properties of azithromycin suggest that it may be an alternative to erythromycin for treatment of Rhodococcus equi pneumonia in foals. To investigate this possibility, the disposition of azithromycin in plasma, polymorphonuclear leukocytes (PMN), and alveolar cells was examined after a single administration in foals. Azithromycin suspension was administered orally (p.o.) at a dose of 10 mg/kg to five healthy 2-3-month-old foals. Two weeks later, azithromycin for injection was administered by intravenous (i.v.) infusion at a dose of 5 mg/kg to the same foals. Plasma samples were collected a...
Knoll U, Strauhs P, Schusser G, Ungemach FR.Olsalazine sodium (Dipentum*) has been used therapeutically against inflammatory bowel disease in human medicine as an alternative to sulphasalazine over the past 20 years. Bacteria in the colon split this prodrug into two molecules of the locally effective 5-aminosalicylic acid (5-ASA). Considering the potential therapeutic use in equine colitis, the pharmacokinetics of olsalazine (OLZ) after single oral administration to six horses at a dosage of 30 mg/kg was investigated. Plasma concentrations of OLZ, 5-ASA, and its main metabolite N-acetyl-5-aminosalicylic acid (Ac-5-ASA) were analysed by ...
Kollias-Baker C, Sams R.The objective of this study was to determine if the administration of poppy seeds to horses would result in detectable concentrations of morphine in urine and blood samples, as has been shown to occur in humans. In this study blood and urine samples were collected following administration of poppy seeds and morphine sulfate orally to four horses. Urine samples were subjected to enzyme-linked immunosorbent assay (ELISA) for the presence of morphine. All urine samples testing positive by ELISA, as well as plasma samples collected after administration of the 10-g doses of poppy seeds, were analyz...
Léguillette R, Désévaux C, Lavoie JP.To determine the effects of pentoxifylline (PTX) administration on lung function and results of cytologic examination of bronchoalveolar lavage fluid in horses affected by recurrent airway obstruction (RAO). Methods: 10 RAO-affected horses. Methods: 6 horses were orally administered PTX (16 g) mixed with corn syrup, and 4 horses were administered corn syrup alone, twice daily for 14 days. Pulmonary function was evaluated before administration (day 0) and on days 8 and 15. Bronchoalveolar lavage (BAL) was performed on days 0 and 15. Reversibility of airway obstruction was assessed by measuring ...
Dumasia MC, Houghton E, Hyde W, Greulich D, Nelson T, Peterson J.Studies related to the in vivo biotransforrmation and urinary excretion of fenspiride hydrochloride in the horse are described. After oral administration, the drug is metabolised by both phase I functionalisation and phase II conjugation pathways. Following enzymatic deconjugation, fenspiride and its phase I metabolites were isolated from post-administration biofluids using bonded co-polymeric mixed mode solid-phase extraction cartridges to isolate the basic compounds. Following trimethylsilylation (TMS), the parent drug and metabolites were identified by capillary gas chromatography-mass spec...
McKinney AR, Ridley DD, Suann CJ.The phase I and phase II metabolism of the anabolic steroid methandrostenolone was investigated following oral administration to a standardbred gelding. In the phase I study, metabolites were isolated from the urine by solid-phase extraction, deconjugated by acid catalysed methanolysis and converted to their O-methyloxime trimethylsilyl derivatives. GC-MS analysis indicated the major metabolic processes to be sequential reduction of the A-ring and hydroxylation at C6 and C16. In the phase II study, unconjugated, beta-glucuronidated and sulfated metabolites were fractionated and deconjugated us...
Beluche LA, Bertone AL, Anderson DE, Rohde C.To evaluate the effects of orally administered phenylbutazone on proteoglycan synthesis and chondrocyte inhibition by IL-1beta in articular cartilage explants of horses. Methods: 11 healthy 1- to 2-year-old horses. Methods: Horses were randomly assigned to the control (n = 5) or treated group (4.4 mg of phenylbutazone/kg of body weight, p.o., q 12 h; n = 6). Articular cartilage specimens were collected before treatment was initiated (day 0), after 14 days of treatment, and 2 weeks after cessation of treatment (day 30). Proteoglycan synthesis and stromelysin concentration in cartilage extracts ...
McDonnell SM.This study is part of ongoing work toward developing pharmacological methods for enhancing and inducing ejaculation in stallions with ejaculatory dysfunction or disabilities that interfere with normal breeding behavior. The objective was to evaluate a treatment regimen involving oral imipramine followed by intravenous xylazine that, in uncontrolled field clinical trials, had shown promise for a higher rate of ejaculation and fewer side effects using a more easily obtained and administered form of imipramine. Eight stallions each underwent eight trials in which treatment consisted of imipramine...
Latimer FG, Colitz CM, Campbell NB, Papich MG.To determine the pharmacokinetics of fluconazole in horses. Methods: 6 clinically normal adult horses. Methods: Fluconazole (10 mg/kg of body weight) was administered intravenously or orally with 2 weeks between treatments. Plasma fluconazole concentrations were determined prior to and 10, 20, 30, 40, and 60 minutes and 2, 4, 6, 8, 10, 12, 24, 36, 48, 60, and 72 hours after administration. A long-term oral dosing regimen was designed in which all horses received a loading dose of fluconazole (14 mg/kg) followed by 5 mg/kg every 24 hours for 10 days. Fluconazole concentrations were determined i...
Kirker-Head CA, Kirker-Head RP.Six healthy, adult female horses were administered five times the minimum maintenance dose of an oral low-molecular-weight chondroitin sulfate, glucosamine HCl, and manganese ascorbate chondroprotective agent (Cosequin; Nutramax Laboratories, Inc., Edgewood, MD) daily for 35 days. Hematology, serum biochemistry, and synovial fluid parameters were assessed twice prior to administering the product and again at the end of the treatment period. Physical examinations performed daily throughout the study showed no abnormal clinical changes attributable to the product. All hematologic parameters meas...
Gokbulut C, Nolan AM, McKellar QA.The present study was carried out to investigate whether the pharmacokinetics of avermectins or a milbemycin could explain their known or predicted efficacy in the horse. The avermectins, ivermectin (IVM) and doramectin (DRM), and the milbemycin, moxidectin (MXD), were each administered orally to horses at 200 microg/kg bwt. Blood and faecal samples were collected at predetermined times over 80 days (197 days for MXD) and 30 days, respectively, and plasma pharmacokinetics and faecal excretion determined. Maximum plasma concentrations (Cmax) (IVM: 21.4 ng/ml; DRM: 21.3 ng/ml; MXD: 30.1 ng/ml) w...
Kennedy T, Campbell J, Selzer V.Ponazuril, a triazine-derivative compound, is proposed as a treatment for equine protozoal myeloencephalitis caused by Sarcocystis neurona. Ponazuril 15% oral paste was administered to 24 horses at 0, 10, or 30 mg/kg body weight for either 28 or 56 days, representing zero, two, and six times the proposed dosage rate and one and two times the recommended duration of treatment, respectively. Serum chemistry analysis, coagulation profile, and hematology measurements were performed weekly and necropsy evaluations, including histopathology, were conducted for all animals at the end of the study. Mi...
Furr M, Kennedy T.Ponazuril was administered orally to 10 adult horses at 5 mg/kg body weight, once a day for 28 days. Blood was collected once a week from each horse from Days 0 through 35, daily from Days 35 through 42, and on Day 49. Cerebrospinal fluid (CSF) was also collected once a week from Day 0 through Day 49. Concentrations of ponazuril in the serum and CSF were determined, and pharmacokinetic calculations were performed. Ponazuril was readily absorbed following oral administration; and after 7 days of dosing, the serum concentration was 4.33 +/- 1.10 mg/L, and the mean CSF concentration was 0.162 +/-...
Ohmura H, Hiraga A, Aida H, Takahashi T, Nukada T.To determine oral dosage and to evaluate the pharmacokinetics in horses of orally administered flecainide, an antiarrhythmic drug, the correlations between its plasma concentration and PR, QRS and QT intervals in equine electrocardiograms (ECG) were investigated. Six healthy horses were administered a randomly ordered dose of 4 or 6 mg/kg of flecainide acetate. The ECG was monitored (heart rate (HR), PR, QRS, and QT intervals) and blood was taken at timed intervals to measure the plasma flecainide concentrations pre- and post-administration. The maximum plasma concentration reached 1014+/-285 ...
Lehner AF, Harkins JD, Karpiesiuk W, Woods WE, Robinson NE, Dirikolu L, Fisher M, Tobin T.Clenbuterol is a beta2 agonist/antagonist bronchodilator, and its identification in post-race samples may lead to sanctions. The objective of this study was to develop a specific and highly sensitive serum quantitation method for clenbuterol that would allow effective regulatory control of this agent in horses. Therefore, clenbuterol-d9 was synthesized for use as an internal standard, an automated solid-phase extraction method was developed, and both were used in conjunction with a multiple reaction monitoring liquid chromatography-tandem mass spectrometry (LC-MS-MS) method to allow unequivoca...
Soma LR, Uboh CE, Guan F, Birks EK, Teleis DC, Rudy JA, Tsang DS, Watson AO.To determine pharmacokinetics and excretion of phenytoin in horses. Methods: 6 adult horses. Methods: Using a crossover design, phenytoin was administered (8.8 mg/kg of body weight, IV and PO) to 6 horses to determine bioavailability (F). Phenytoin also was administered orally twice daily for 5 days to those same 6 horses to determine steady-state concentrations and excretion patterns. Blood and urine samples were collected for analysis. Results: Mean (+/- SD) elimination half-life following a single IV or PO administration was 12.6+/-2.8 and 13.9+/-6.3 hours, respectively, and was 11.2+/-4.0 ...
McKinney AR, Ridley DD, Suann CJ.After oral administration to a thoroughbred gelding, the anabolic steroid norethandrolone was converted into a complex mixture of oxygenated metabolites. These metabolites were extracted from the urine, deconjugated by methanolysis and converted to their O-methyloxime trimethylsilyl derivatives. Gas chromatographic/mass spectrometric analysis indicated the major metabolites to be 19-norpregnane-3,16,17-triols, 19-norpregnane-3,17,20-triols and 3,17-dihydroxy-19-norpregnan-21-oic acids. Some minor metabolites were also detected.
Boeckh S, Buchanan C, Boeckh A, Wilkie S, Davis C, Buchanan T, Boothe D.Following approval of a concentrated injectable formulation of enrofloxacin for cattle (Baytril 100 Injectable, Bayer Corp. Agricultural Division, Shawnee Mission, KS), equine practitioners have started administering this preparation both parenterally and orally to horses, despite the lack of pharmacokinetic data in this species. Six healthy horses received enrofloxacin at 7.5 mg/kg both orally and intravenously, with the sequence being randomly assigned and at least 1 week of washout allowed between administrations. Blood samples were collected from each horse at various intervals after drug ...
Hanson RR, Brawner WR, Blaik MA, Hammad TA, Kincaid SA, Pugh DG.Fourteen horses with a progressive forelimb lameness of 3 to 12 months' duration, diagnosed as navicular syndrome, were selected from clinical cases admitted to Auburn University Equine Hospital for evaluation of the efficacy of an orally administered nutraceutical (Cosequin, Nutramax Laboratories, Inc., Edgewood, MD) for ameliorating clinical signs associated with naturally occurring navicular syndrome. Horses were randomly allocated to treatment with the nutraceutical or a placebo. Treatment was five scoops (16.5 g) of powder twice daily in the feed. The test group (n = 8) received a patente...
Pearson EG, Andreasen CB.To evaluate the potential of excess dietary iron to cause hepatic lesions similar to those described in horses with suspected iron toxicosis or hemochromatosis. Methods: Prospective study. Methods: 6 adult male ponies. Methods: 4 ponies received 50 mg of iron/kg (22.7 mg/lb) of body weight each day by oral administration of ferrous sulfate, which contained 20% elemental iron; 2 ponies received only the carrier (applesauce). Complete blood counts, serum biochemical analyses, and hepatic tissue biopsies were performed, and serum iron concentrations were measured. Blood and tissue samples were ob...
Steinman A, Gips M, Lavy E, Sinay I, Soback S.Metronidazole pharmacokinetics in horses was studied after intravenous (i.v.), rectal (p.r.) and oral (p.o.) administration at 20 mg/kg using a triple crossover study design. Metronidazole mean+/-SD half-life was 196+/-39, 212+/-30 and 240+/-65 min after i.v., p.r. and p.o. administration, respectively. The metronidazole clearance was 2.8 (mL/min/kg) and the volume of distribution at steady state was 0.68 L/kg. The pharmacokinetic parameters calculated for metronidazole after administration of the drug by the various routes showed that bioavailability (74+/-18 vs. 30+/-9%) and maximum serum co...
Pérez R, Cabezas I, Sutra JF, Galtier P, Alvinerie M.A study was undertaken to evaluate and compare faecal excretion of moxidectin and ivermectin in horses after oral administration of commercially available preparations. Ten clinically healthy adult horses, weighing 390-446 kg body weight (b.w.), were allocated to two experimental groups. Group I was treated with an oral gel formulation of moxidectin at the manufacturer's recommended therapeutic dose of 0.4 mg/kg b.w. Group II was treated with an oral paste formulation of ivermectin at the recommended dose of 0.2 mg/kg b.w. Faecal samples were collected at different times between 1 and 75 days ...
Pollina GF, Zagotto G, Maritan P, Iacopetti I, Busetto R.Gallium (Ga), a metal in group IIIA of the periodic table, has shown a remarkable activity against bone resorption and could therefore possibly prove useful in the treatment of certain diseases in sport horses, for example navicular disease. The aim of this study was to gain more information concerning the kinetics of Ga after oral administration of gallium nitrate (GaN) in adult horses. Six horses received a single dose of 10 mg/kg of GaN mixed with the food ration. Absorption was slow (T(max) = 10 ± 3 h, T(½abs) = 2 ± 0.8 h), and a C(max) of 26 ± 11 μg/L was achieved. Excretion followed...
Robinson MA, Stefanovski D, You Y, Boston RC, Soma LR.Capsaicinoids deter horses from chewing on bandages and are applied topically to provide analgesia to musculoskeletal injuries. They are banned during competition due to their nerve blocking properties. The pharmacokinetics of oral (PO) and direct gastric administration via nasogastric tube (NG), or topical (TOP) administration of two capsaicinoid-containing products were investigated, and the withdrawal times required prior to competition were estimated. Capsaicin (CAP) and dihydrocapsaicin (DCAP) were quantified in plasma, and both compounds were best described by a delayed absorption two co...
DiPietro JA, Todd KS, Reuter V.Four groups of 10 horses (mares) each were treated with a 1% solution of ivermectin (200 micrograms/kg of body weight) in a propylene glycol-glycerol formal base orally, a 1% solution of ivermectin (200 micrograms/kg) in a propylene glycol-glycerol formal base via nasogastric tube, a 1.87% paste of ivermectin (200 micrograms/kg) orally, or a 22.7% paste of oxibendazole (10 mg/kg) orally. Fecal examinations were done before treatment and on posttreatment days (PTD) 14, 28, 42, 56, and 70. Strongyle egg per gram counts and sugar flotation fecal examinations were performed. Results of fecal exami...
Lehner AF, Harkins JD, Karpiesiuk W, Woods WE, Robinson NE, Dirikolu L, Fisher M, Tobin T.Clenbuterol is a beta2 agonist/antagonist bronchodilator, and its identification in post-race samples may lead to sanctions. The objective of this study was to develop a specific and highly sensitive serum quantitation method for clenbuterol that would allow effective regulatory control of this agent in horses. Therefore, clenbuterol-d9 was synthesized for use as an internal standard, an automated solid-phase extraction method was developed, and both were used in conjunction with a multiple reaction monitoring liquid chromatography-tandem mass spectrometry (LC-MS-MS) method to allow unequivoca...
Waitt Wolker LH, Veltri CA, Pearman K, Lozoya M, Norris JW.This study aimed to investigate pharmacokinetics of fluoxetine in horses and validate a method for liquid chromatography mass spectrometry analysis of serum levels. Fluoxetine pharmacokinetics were determined using 10 healthy, adult horses. Fluoxetine pharmacokinetics following a single oral dose (0.25 mg/kg) were determined using blood samples collected prior to and at several time points over 7 days following administration. Serum concentrations of fluoxetine and its bioactive metabolite norfluoxetine were measured using liquid chromatography coupled to an accurate mass/high-resolution ma...
Guerrero J, Newcomb K, Seibert BP, Michael BF.Two controlled tests were conducted in equine foals and yearlings to determine the optimal oral dosage and the duration of activity of closantel for the prevention of Gasterophilus spp larval infections. Additional data were collected on the activity of closantel against Strongylus vulgaris larval infections. In experiment 1, 12 foals and 12 yearlings were equally allocated to 4 experimental groups, and were given oral treatments with closantel at dosages of 0 (nontreated controls), 2, 5, or 8 mg/kg of body weight every 2 months during bot season. The foals and yearlings were allowed to graze ...
Knych HK, McKemie DS, Seminoff K, Hartmann P, Hovda L, Benson D.Ethylphenidate is a psychostimulant and analog of the commonly prescribed compound, methylphenidate (Ritalin®). There are a limited number of studies describing the disposition and pharmacologic/toxicological effects of ethylphenidate in any species. The abuse potential in equine athletes along with the limited data available regarding administration in horses necessitates further study. The objectives of the current study were to describe drug concentrations, develop an analytical method that could be used to regulate its use, and describe the pharmacodynamic effects of ethylphenidate in hor...
Greene EW, Woods WE, Tobin T.Caffeine (4 mg/kg) was given by rapid IV injection to 4 horses. Plasma concentrations of the drug peaked at 10 micrograms/ml and decreased rapidly at first, and then more slowly, with an apparent beta-phase half-life of 18.2 hours. Urinary concentrations of caffeine were remarkably consistent at about 3 times plasma values of the drug. Caffeine was detectable in both plasma and urine of the horses for up to 9 days after dosing. After oral administration, caffeine was absorbed poorly with an apparent bioavailability of 39%. Although blood concentrations of caffeine peaked rapidly after oral adm...
Tamura N, Okano A, Kuroda T, Niwa H, Kusano K, Matsuda Y, Fukuda K, Mita H, Nagata S.To clarify the detailed pharmacokinetics (PK) of orally administered voriconazole in tear fluid (TF) of horses for evaluating the efficacy of voriconazole secreted into TF against equine keratomycosis. Methods: Five healthy Thoroughbred horses. Methods: Voriconazole was administrated through a nasogastric tube to each horse at a single dose of 4.0 mg/kg. TF and blood samples were collected before and periodically throughout the 24 hours after administration. Voriconazole concentrations in plasma and TF samples were analyzed using liquid chromatography-electrospray tandem-mass spectrometry. T...
Tsitsimpikou C, Spyridaki MH, Georgoulakis I, Kouretas D, Konstantinidou M, Georgakopoulos CG.Flurbiprofen and its main acidic metabolites were detected in equine urine after a single-dose administration of 500 mg flurbiprofen to two 2.5-3.5-years-old mares, in order to be used in equine doping control routine analysis. The urine levels of the parent drug were determined using GC/MS. Five acidic metabolites were found in the urine. The structure of the proposed metabolites was confirmed by HRMS accurate mass measurements. The highest flurbiprofen concentration was 204 mug ml(-1) at 1-3 h post administration. Flurbiprofen could be detected for 24-37 h in urine using the standard screeni...
Gold JR, Grubb T, Court M, Villarino NF.Acetaminophen is a common analgesic and antipyretic drug used in human medicine and might be an alternative to nonsteroidal anti-inflammatory drugs for treating pain and pyrexia in foals. The pharmacokinetics and safety of differing doses of acetaminophen have not been investigated in foals. Objective: To determine the plasma pharmacokinetics and any changes in haematology and biochemistry profiles following oral administration of single doses of acetaminophen at 10, 20, and 40 mg/kg to foals. Methods: Randomised cross-over pharmacokinetic study. Methods: Six Quarter Horse (two colts and fou...
Soma LR, Gallis DE, Davis WL, Cochran TA, Woodward CB.Phenylbutazone (PBZ) was administered (8.8 mg/kg of body weight) every 24 hours for 5 consecutive days, orally for the first 4 days and IV on day 5. The half-life (t 1/2) after this daily administration was 6.2 hours and the volume of distribution was 0.152 +/- 0.014 L/kg; the bioavailability after oral administration was 91.8 +/- 2.5%. The plasma concentration of PBZ at experimental hour (EH) 24 (24 hours after the 1st oral dose) was 1.7 +/- 0.39 micrograms/ml and increased to 4.2 +/- 0.29 micrograms/ml at EH 48 (24 hours after the 2nd oral dose). Values at EH 72, 96, and 120 (24 hours after ...
Freeman SL, England GC.To compare sedative effects of romifidine following IV, IM, or sublingual (SL) administration in horses. Methods: 30 horses that required sedation for routine tooth rasping. Methods: Horses (n = 10/group) were given romifidine (120 microg/kg) IV, IM, or SL. Heart rate, respiratory rate, head height, distance between the ear tips, thickness of the upper lip, response to auditory stimulation, response to tactile stimulation, and degree of ataxia were recorded every 15 minutes for 180 minutes. Tooth rasping was performed 60 minutes after administration of romifidine, and overall adequacy of sedat...
Crosignani N, Luna SP, Dalla Costa T, Pimenta EL, Detoni CB, Guterres SS, Puoli Filho JN, Pantoja JC, Pigatto MC.We investigated the thermal, electrical and mechanical antinociceptive and physiological effects (heart rate, respiratory rate, arterial blood pressure, head height and abdominal auscultation score), and pharmacokinetics, of 0.5 mg/kg of the injectable formulation (ORAL) or nanoparticulated methadone (NANO) given orally, in six adult mares, using a crossover, blind and prospective design. Repeated-measure models were used to compare parametric data between and within treatments, followed by Tukey's test. Nonparametric data were analysed with Wilcoxon signed-rank, adjusted by Bonferroni tests....
Dirikolu L, Karpiesiuk W, Lehner AF, Tobin T.Toltrazuril sulfone (ponazuril) is a triazine-based antiprotozoal agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sul...
Ingvast-Larsson C, Paalzow G, Paalzow L, Ottosson T, Lindholm A, Appelgren LE.The pharmacokinetics of theophylline were determined in Standardbred trotters after single intravenous and oral administration. A bi-exponential equation was fitted to the intravenous data and a tri-exponential equation to the oral data. The biological half-life of theophylline was found to be 14.8 h, the volume of distribution 1.02 l/kg and the total plasma clearance 0.86 ml/kg/min. The oral absorption of the drug was complete (bioavailability 108%) and rapid (absorption half-life 0.4 h).
Johnson E, van Heemst J, Benavides J, Gray B.Etizolam is a benzodiazepine analogue that is approved for use in Japan, Italy and India but has recently appeared as a nonapproved product on the illicit drug market in Europe and North America. Etizolam was identified in a crystalline material seized at a Kentucky racetrack, raising concerns that this drug may have been used in racing. The aim of this study was to characterize the metabolism and excretion of etizolam in horses to generate information on its disposition and to incorporate the correct urinary and serum target analytes into anti-doping screening procedures. Etizolam was adminis...
Hilton HG, Magdesian KG, Groth AD, Knych H, Stanley SD, Hollingsworth SR.Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used systemically for the treatment of inflammatory ocular disease in horses. However, little information exists regarding the ocular penetration of this class of drugs in the horse. Objective: To determine the distribution of orally administered flunixin meglumine and firocoxib into the aqueous humor of horses. Methods: Fifteen healthy adult horses with no evidence of ophthalmic disease. Methods: Horses were randomly assigned to a control group and 2 treatment groups of equal sizes (n = 5). Horses assigned to the treatment groups rece...
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...
Longhofer SL, Reinemeyer CR, Radecki SV.The efficacy of top-dress antiinflammatory drugs ultimately depends on a patient's willingness to consume treated feed. The current study compares the palatability of two phenylbutazone top-dress formulations (Equipalazone Powder, Dechra Pharmaceuticals, and Pro-Dynam, VetXX, Ltd.) and a suxibuzone top-dress formulation (Danilon Equidos, Janssen Animal Health). Results of a three-period, crossover study on 18 healthy horses showed that Pro-Dynam was significantly less palatable, with significantly less consumption of treated feed compared with either Equipalazone Powder or Danilon Equidos. The...
Ohmura H, Hiraga A, Aida H, Takahashi T, Nukada T.To determine oral dosage and to evaluate the pharmacokinetics in horses of orally administered flecainide, an antiarrhythmic drug, the correlations between its plasma concentration and PR, QRS and QT intervals in equine electrocardiograms (ECG) were investigated. Six healthy horses were administered a randomly ordered dose of 4 or 6 mg/kg of flecainide acetate. The ECG was monitored (heart rate (HR), PR, QRS, and QT intervals) and blood was taken at timed intervals to measure the plasma flecainide concentrations pre- and post-administration. The maximum plasma concentration reached 1014+/-285 ...
Wong DM, Davis JL, Alcott CJ, Hepworth-Warren KL, Galow-Kersh NL, Rice S, Coetzee JF.The objective of this study was to evaluate the pharmacokinetic properties and physiologic effects of a single oral dose of alprazolam in horses. Seven adult female horses received an oral administration of alprazolam at a dosage of 0.04 mg/kg body weight. Blood samples were collected at various time points and assayed for alprazolam and its metabolite, α-hydroxyalprazolam, using liquid chromatography/mass spectrometry. Pharmacokinetic disposition of alprazolam was analyzed by a one-compartmental approach. Mean plasma pharmacokinetic parameters (±SD) following single-dose administration of ...
Lees P, Higgins AJ, Mawhinney IC, Reid DS.The absorption pattern of phenylbutazone was studied in five horses during administration of the drug in a paste formulation on days 1, 5, 8 and 12 of a 12-day dosing schedule. Since two or more plasma concentration peaks were usually obtained following each oral dose, it was concluded that phasic absorption was a particular feature of the oil:water formulation of the product. Possible causes of this unusual absorption pattern are discussed and the therapeutic implications of both phasic absorption and the recorded values of Cmax, tmax and AUC024 for phenylbutazone and its active metabolite ox...
Lees P, Taylor JB, Maitho TE, Millar JD, Higgins AJ.The pharmacokinetics, metabolism, excretion and tissue residues of phenylbutazone (PBZ) in the horse were studied following both intravenous and oral administration of the drug at a dose rate of 4.4 mg/kg. A 72-hour blood sampling schedule failed to demonstrate a third exponential phase; the plasma disposition following intravenous injection being described by a two compartment open model, with the following elimination phase parameters: beta = 0.13h-1, t1/2 beta = 5.46h, Vdarea = 0.141 1/kg and C1B = 17.9 ml/kg/h. The hydroxylated metabolites oxyphenbutazone (OPBZ) and gamma-hydroxyphenylbuta...
Soma LR, Uboh CE, Guan F, Birks EK, Teleis DC, Rudy JA, Tsang DS, Watson AO.To determine pharmacokinetics and excretion of phenytoin in horses. Methods: 6 adult horses. Methods: Using a crossover design, phenytoin was administered (8.8 mg/kg of body weight, IV and PO) to 6 horses to determine bioavailability (F). Phenytoin also was administered orally twice daily for 5 days to those same 6 horses to determine steady-state concentrations and excretion patterns. Blood and urine samples were collected for analysis. Results: Mean (+/- SD) elimination half-life following a single IV or PO administration was 12.6+/-2.8 and 13.9+/-6.3 hours, respectively, and was 11.2+/-4.0 ...
Kohn CW, Sams R, Kowalski JJ, Powers J, Wallace S.The disposition of rifampin in six healthy mares after single intravenous (i.v.) and oral (p.o.) doses and after seven oral doses of 10 mg/kg administered twice a day was investigated using a high performance liquid chromatographic (HPLC) method. Pharmacokinetic variables for rifampin determined using the HPLC method were comparable to variables reported from earlier studies utilizing a microbiological assay. Desascetylrifampin, a major metabolite of the parent compound, could not be detected in the serum but was detected at low concentrations in urine. Mean trough concentrations of rifampin i...
Miller PJ, Martin IC, Kohnke JR, Rose RJ.The effects of acepromazine maleate (ACP), given orally in a paste form, were examined in six standard-bred geldings over a 12 hour period. Three dose rates, zero (placebo paste), 0.13 mg kg-1 and 0.26 mg kg-1, given before or after feeding, were investigated. The data were divided into two sampling periods for analysis, one from zero to 120 minutes and the other from four to 12 hours. Sedation was assessed by a score (TS score) based on general appearance, anal sphincter relaxation and penile protrusion. This TS score was significantly elevated 40 minutes after dosing with ACP, irrespective o...
Teixeira FA, Araújo AL, Ramalho LO, Adamkosky MS, Lacerda TF, Coelho CS.The aim of this study was to evaluate the effects of oral creatine supplementation on the athletic performance of equines used for barrel racing. Ten healthy Quarter Horses, or Quarter Horse crossbred, weighing 429.7 ± 25.3 kg and with mean age of 3.8 ± 1.2 years, were used. Animals were evaluated in four different moments (M1, M2, M3, M4), and between M3 and M4, they were supplemented with 28 g of creatine/100 kg of body weight, orally, for 45 days. Although significant alterations for LDH activity, plasma glucose and packed cell volume were observed, it was possible to conclude th...
Beaumier PM, Fenwick JD, Stevenson AJ, Weber MP, Young LM.Plasma and urinary levels of salicylic acid were examined in Standardbred mares after administration of various feeds, containing different compositions of hay. In addition, horses were administered acetylsalicylic acid orally and methyl salicylate topically. Elevated salicylic acid levels were observed in horse urine and plasma in animals fed lucerne hay. The plasma and urinary elimination of salicylic acid exhibited a diurnal pattern which was related to the type of feed and the feeding schedule. Within 24 h after oral administration of acetylsalicylic acid, plasma and urine salicylic acid l...
Taguchi T, Morales Yniguez FJ, Takawira C, Andrews FM, Lopez MJ.Osteoarthritis (OA) accounts for up to 60% of equine lameness. Agmatine, a decarboxylated arginine, may be a viable option for OA management, based on reports of its analgesic properties. Six adult thoroughbred horses, with lameness attributable to thoracic limb OA, received either daily oral phenylbutazone (6.6 mg/kg), agmatine sulfate (25 mg/kg) or a control for 30 days, with 21-day washout periods between treatments. Subjective lameness, thoracic limb ground reaction forces (GRF), plasma agmatine and agmatine metabolite levels were evaluated using an established rubric, a force platform, an...
