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.
Knych HK, Corado CR, McKemie DS, Scholtz E, Sams R.Tramadol is a synthetic opioid used in human medicine, and to a lesser extent in veterinary medicine, for the treatment of both acute and chronic pain. In humans, the analgesic effects are owing to the actions of both the parent compound and an active metabolite (M1). The goal of the current study was to extend current knowledge of the pharmacokinetics of tramadol and M1 following oral administration of three doses of tramadol to horses. A total of nine healthy adult horses received a single oral administration of 3, 6, and 9 mg/kg of tramadol via nasogastric tube. Blood samples were collected...
L'Ami JJ, Vermunt LE, van Loon JP, Sloet van Oldruitenborgh-Oosterbaan MM.A single dose of 40 μg/kg bodyweight (BW) of oromucosal detomidine gel was administered sublingually to 10 healthy Dutch Warmblood mares aged 7 ± 4 years (mean ± SD) and BW 580 ± 69 kg. Blood and urine samples were collected before and for 8 days following administration and evaluated qualitatively in an FEI Reference Laboratory and quantitatively in a research laboratory. Clinical effects were evaluated at baseline and for 24 h after administration. Sedation was determined using head height and scores of reaction to auditory and mixed auditory/sensory stimuli. Mechanical nociceptive thres...
Noble G, Edwards S, Lievaart J, Pippia J, Boston R, Raidal SL.Safety of meloxicam, a potent NSAID with selective COX-2 inhibition, has not been evaluated in horses. Objective: To evaluate pharmacokinetics and safety of single and repeated oral doses of meloxicam in adult horses. Methods: Forty-nine healthy, university-owned adult lightbreed horses. Methods: Study conducted in 2 parts. Part I addressed pharmacokinetics of single oral dose meloxicam (0.6 mg/kg) in 16 horses. Part II, 33 horses were randomly assigned to 5 treatment groups to assess prolonged administration (0.6 mg/kg PO q24h for 6 weeks, n = 7) or higher doses (1.8 mg/kg, n = 7, or 3.0 mg/k...
Witte TS, Melkus E, Walter I, Senge B, Schwab S, Aurich C, Heuwieser W.Persistent breeding-induced endometritis is ranked as the third most common medical problem in the adult mare and leads to enormous economic loss in horse breeding. In mares suffering from persistent breeding-induced endometritis, increased amounts of intrauterine (i.u.) fluid or viscous mucus in estrus or after breeding may act as a barrier for sperm and can contribute to low fertility. Current therapies of these mares aim to eliminate i.u. fluid and mucus by uterine lavage and/or administration of ecbolic drugs. Recently, i.u. administration of N-acetylcysteine (NAC) has been shown to suppor...
Soma LR, Uboh CE, Liu Y, Li X, Robinson MA, Boston RC, Colahan PT.This study investigated and compared the pharmacokinetics of intra-articular (IA) administration of dexamethasone sodium phosphate (DSP) into three equine joints, femoropatellar (IAS), radiocarpal (IAC), and metacarpophalangeal (IAF), and the intramuscular (IM), oral (PO) and intravenous (IV) administrations. No significant differences in the pharmacokinetic estimates between the three joints were observed with the exception of maximum concentration (Cmax ) and time to maximum concentration (Tmax ). Median (range) Cmax for the IAC, IAF, and IAS were 16.9 (14.6-35.4), 23.4 (13.5-73.0), and 46.9...
Orsini JA, Ryan WG, Carithers DS, Boston RC.To generate data on the effects of firocoxib administration to horses with osteoarthritis. Methods: Client-owned horses with signs of lameness and joint pain associated with osteoarthritis. Methods: Firocoxib was administered as an oral paste (0.1 mg/kg, q 24 h) for 14 days. Assessments were performed on day 0 (baseline) and days 7 and 14. Results: 390 of 429 horses from 80 sites in 25 states met the criteria for analysis. Quarter Horse and Thoroughbred were the 2 most commonly represented breeds, comprising half of the study population. Signs of musculoskeletal pain or lameness attributed to ...
Ralston S, Stives M.Though horses synthesize ascorbic acid in their liver in amounts that meet their needs under normal circumstances, prolonged stress results in low plasma concentrations due to enhanced utilization and renal excretion and can reduce immune function. It was hypothesized that plasma ascorbic acid could be maintained in weanling horses by oral supplementation following prolonged transportation. Weanlings were supplemented with no ascorbic acid (Tx 0: n = 4), 5 grams ascorbic acid twice daily for 5 days (Tx 1: n = 4) or for 10 days (Tx 2: n = 4) following >50 hours of transportation. Supplementa...
Endo Y, Tsuchiya T, Sato F, Murase H, Omura T, Korosue K, Nambo Y, Ishimaru M, Wakui Y.Prevalence of equine gastric ulcer syndrome in 85 young Thoroughbreds was investigated. The presence of gastric ulcers was confirmed in 27.1% (23/85) of the horses by endoscopic examination. Sixty-two horses without gastric ulcers were allocated randomly to either the treated group (31 horses) or sham-dosed control group (31 horses) in order to investigate the efficacy of omeprazole oral paste in the prevention of gastric ulcers. At the second endoscopic examination conducted after 28 days of administration, only 1 horse in the treated group developed gastric ulcers, while 12 horses developed ...
Hartnack AK, Van Metre DC, Morley PS.To evaluate the potential association between Salmonella enterica shedding in hospitalized horses and the risk of diarrhea among stablemates, and to characterize gastrointestinal-related illness and death following discharge among horses that shed S. enterica while hospitalized. Methods: Retrospective cohort study [corrected]. Methods: 221 horses (59 that shed S. enterica during hospitalization and 162 that tested negative for S. enterica shedding ≥ 3 times during hospitalization). Methods: Information from medical records (signalment, results of microbial culture of fecal samples, clinical ...
Rumpler MJ, Sams RA, Colahan P.We describe a validated, rapid, sensitive, and specific UHPLC-MS/MS method to detect and quantify glycopyrrolate in 0.5 mL of horse urine. Further, we investigated the elimination of glycopyrrolate in urine after both intravenous and oral administration of clinically relevant doses to Thoroughbred horses. Quantification was performed by weighted, linear regression analysis using a deuterated analogue of glycopyrrolate as internal standard (IS). The method was characterized by a linear range of 5-2500 pg/mL, a lower limit of quantification of 5 pg/mL and a limit of detection of 1 pg/mL. The int...
Linardi RL, Stokes AM, Keowen ML, Barker SA, Hosgood GL, Short CR.To characterize the bioavailability and pharmacokinetics of oral and injectable formulations of methadone after IV, oral, and intragastric administration in horses. Methods: 6 healthy adult horses. Methods: Horses received single doses (each 0.15 mg/kg) of an oral formulation of methadone hydrochloride orally or intragastrically or an injectable formulation of the drug orally, intragastrically, or IV (5 experimental treatments/horse; 2-week washout period between each experimental treatment). A blood sample was collected from each horse before and at predetermined time points over a 360-minute...
Nieto JE, Aleman M, Anderson JD, Fiack C, Snyder JR.To assess gene expressions of cyclooxygenase-1 and -2 in oral, glandular gastric, and urinary bladder mucosae and determine the effect of oral administration of phenylbutazone on those gene expressions in horses. Methods: 12 healthy horses. Methods: Horses were allocated to receive phenylbutazone or placebo (6 horses/group); 1 placebo-treated horse with a cystic calculus was subsequently removed from the study, and those data were not analyzed. In each horse, the stomach and urinary bladder were evaluated for ulceration via endoscopy before and after experimental treatment. Oral, glandular gas...
Dimaio Knych HK, Stanley SD.To characterize pharmacokinetics and pharmacodynamics of detomidine gel administered sublingually in accordance with label instructions to establish appropriate withdrawal guidelines for horses before competition. Methods: 12 adult racehorses. Methods: Horses received a single sublingual administration of 0.04 mg of detomidine/kg. Blood samples were collected before and up to 72 hours after drug administration. Urine samples were collected for 5 days after detomidine administration. Plasma and urine samples were analyzed via liquid chromatography-mass spectrometry, and resulting data were anal...
Appolonova SA, Baranov PA, Mesonzhnik NV, Brazhnikova DO, Rodchenkov GM.A method is described for the determination of mesocarb abuse in equestrian sport by combining gradient liquid chromatography and electrospray ionization tandem mass spectrometry. Mesocarb was administrated orally to two horses at a dose of 50 µg/kg. Urine samples were collected up to 120 h post administration. Hydrolyzed and conjugated urine fractions were handled using liquid-liquid extraction (LLE). The identity of the parent drug and metabolites was confirmed using liquid chromatography combined with tandem mass spectrometry (MS/MS). Mesocarb and seven metabolites were detected in horse...
Schnabel LV, Papich MG, Divers TJ, Altier C, Aprea MS, McCarrel TM, Fortier LA.Minocycline holds great potential for use in horses not only for its antimicrobial effects but also for its anti-inflammatory and neuroprotective properties. However, there are no pharmacokinetic or safety data available regarding the use of oral minocycline in horses. Objective: To determine pharmacokinetics, safety and penetration into plasma, synovial fluid, aqueous humour (AH) and cerebral spinal fluid (CSF) of minocycline after oral administration of multiple doses in horses and to determine the minimum inhibitory concentrations (MIC) of minocycline for equine pathogenic bacteria. Methods...
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...
Cayzer J, Hedderley D, Gray S.Lyophilised products from green-lipped mussel (Perna canaliculus[LPPC]) are used to orally treat horses with osteoarthritis (OA). However, no randomised, controlled or double-blinded studies on the efficacy of this treatment in horses have been reported to date. Objective: To investigate the effects of a unique LPPC (Biolane)(1) in improving clinical signs of OA in the fetlock. Methods: Data were analysed from 26 horses with primary fetlock lameness in a controlled, randomised and double-blinded, multi-centre clinical trial. The study design was a partial crossover with a washout period and co...
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...
Stewart AJ, Boothe DM, Cruz-Espindola C, Mitchum EJ, Springfield J.To determine the pharmacokinetics of tramadol and its metabolites O-desmethyltramadol (ODT) and N-desmethyltramadol (NDT) in adult horses. Methods: 12 mixed-breed horses. Methods: Horses received tramadol IV (5 mg/kg, over 3 minutes) and orally (10 mg/kg) with a 6-day washout period in a randomized crossover design. Serum samples were collected over 48 hours. Serum tramadol, ODT, and NDT concentrations were measured via high-performance liquid chromatography and analyzed via noncompartmental analysis. Results: Maximum mean ± SEM serum concentrations after IV administration for tramadol, ODT, ...
Cutolo AA, Santos AT, Allegretti SM.Twenty horses naturally infected with nematodes were included in a blind, controlled field study on efficacy and safety of an oral 2% ivermectin formulation at a dose of 0.2 mg.kg(-1). Horses were divided into treated and non-treated (control) groups with ten animals each based on preliminary counts of eggs per gram of feces (EPG). Stool samples were collected after treatment for identification of nematode species. Clinical evaluations and EPG counts were performed on days 0, +5, +14 and +19. Nineteen nematode species were identified: Coronocyclus ulambajari, Craterostomum acuticaudatum, Cyath...
Peters J, Block W, Oswald S, Freyer J, Grube M, Kroemer HK, Lämmer M, Lütjohann D, Venner M, Siegmund W.The delivery of clarithromycin (CRL) to its site of action in bronchial/alveolar epithelial cells (EC), bronchial epithelial lining fluid (ELF), and bronchoalveolar lavage cells (BALC) may be influenced by CYP3A4 and the drug transporters, ATP-binding cassette (ABC) B1 and ABCC2 and organic anion-transporting polypeptides (OATPs), which can be modulated and/or up-regulated via the nuclear pregnane X receptor (PXR) by rifampicin (RIF). Therefore, we evaluated the disposition and pulmonary distribution of CLR (7.5 mg/kg b.i.d., 21 days) and expression of ABCB1, ABCC2, OATP1A2, and OATP2B1 in EC ...
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...
McKenzie EC, Garrett RL, Payton ME, Riehl JH, Firshman AM, Valberg SJ.Dantrolene sodium is used to prevent exertional rhabdomyolysis in predisposed horses. Food intake might negatively impact dantrolene bioavailability in horses; however, prolonged feed restriction might be detrimental to performance. Objective: To determine a minimum duration of feed restriction that would optimise plasma dantrolene concentrations in horses after nasogastric administration. It was hypothesised that feed restriction for 4, 8 or 12 h before dantrolene administration would result in higher plasma dantrolene concentrations than achieved with no feed restriction before treatment. Me...
DiMaio Knych HK, Arthur RM, Taylor A, Moeller BC, Stanley SD.Dantrolene is a skeletal muscle relaxant used commonly in performance horses to prevent exertional rhabdomyolysis. The goal of the study reported here was to begin to characterize cytochrome P450-mediated metabolism of dantrolene in the horse and describe the pharmacokinetics of the compound, formulated as a capsule or a compounded paste formulation, following oral administration. Dantrolene is rapidly metabolized to 5-hydroxydantrolene both in vivo and in vitro. Preliminary work with equine liver microsomes suggest that two enzymes are responsible for the metabolism of dantrolene, as evidence...
Williams MM, Davis EG, KuKanich B.The objective of the study was to assess the pharmacokinetics of terbinafine administered orally to horses and Greyhound dogs. A secondary objective was to assess terbinafine metabolites. Six healthy horses and six healthy Greyhound dogs were included in the pharmacokinetic data. The targeted dose of terbinafine was 20 and 30 mg/kg for horses and dogs, respectively. Blood was collected at predetermined intervals for the quantification of terbinafine concentrations with liquid chromatography and mass spectrometry. The half-life (geometric mean) was 8.1 and 8.6 h for horses and Greyhounds, respe...
Giorgi M, Mengozzi G, Raffaelli A, Saba A.Tepoxalin is a veterinary drug registered for use in the dog as a dual inhibitor (cyclooxygenase-5 lipoxygenase). In the horse, it predominantly triggers a strong cyclooxygenase inhibition; this bias seems to be due to the action of its metabolite(s). Among these, only the RWJ-20142 is well known, while to the best of our knowledge no information is available on the other metabolites produced in vivo. Hence, the identification of its main metabolic pathway is pivotal to better understand its clinical activity. A suitable high performance liquid chromatography method has been applied to liquid ...
Kaukinen H, Aspegrén J, Hyyppä S, Tamm L, Salonen JS.The objective of the study was to determine the absorption, bioavailability and sedative effect of detomidine administered to horses as an oromucosal gel compared to intravenous and intramuscular administration of detomidine injectable solution. The study was open and randomized, with three sequences crossover design. Nine healthy horses were given 40 μg/kg detomidine intravenously, intramuscularly or administered under the tongue with a 7-day wash-out period between treatments. Blood samples were collected before and after drug administration for the measurement of detomidine concentration...
Davis JL, Marshall JF, Papich MG, Blikslager AT, Campbell NB.The purpose of this study was to determine the pharmacokinetics of deracoxib following oral administration to horses. In addition, in vitro equine whole blood cyclooxygenase (COX) selectivity assays were performed. Six healthy adult horses were administered deracoxib (2 mg/kg) orally. Plasma samples were collected prior to drug administration (time 0), and 10, 20, 40 min and 1, 1.5, 2, 4, 6, 8, 12, 24, and 48 h after administration for analysis with high pressure liquid chromatography using ultraviolet detection. Following PO administration, deracoxib had a long elimination half-life (t(...
Milne EM, Doxey DL, Woodman MP, Cí·¯ord D, Pearson RA.A clinical trial was carried out to determine the effect of cisapride on rate of passage of digesta and clinical parameters in horses with chronic grass sickness. Sixteen horses were given intramuscular cisapride (0.1 mg kg-1 three times daily) (group I), and 15 received oral cisapride (0.8 mg kg-1 three times daily) (group O). A liquid-phase marker (cobalt-EDTA) and a solid-phase marker (polystyrene pellets) were given by stomach tube at the beginning of each of three consecutive 7 day periods, i.e., before, during and after cisapride therapy. Seven horses in each group completed the rate of ...
Moss AL, Hritz RL, Hector RC, Wotman KL.To investigate the effects of orally administered trazodone on intraocular pressure (IOP), pupil diameter measured in the vertical plane (ie, vertical pupil diameter [VPD]), selected physical examination variables, and sedation level in healthy equids. Methods: 7 horses and 1 pony. Methods: Food was withheld for 12 hours prior to drug administration. After baseline (time 0) sedation scoring, physical examination, and measurement of IOP and VPD, equids received 1 dose (approx 6 mg/kg) of trazodone orally. Examination and measurement procedures were repeated 0.5, 1, 2, 4, 8, 12, and 24 hours aft...
Sweeney RW, Sweeney CR, Soma LR, Woodward CB, Charlton CA.Serum and peritoneal fluid concentrations of metronidazole were determined in 6 healthy adult horses given the drug (25 mg/kg) by IV or oral routes. The disposition of metronidazole in horses given the drug by the IV route conformed to a 2-compartment model with a distribution half-life of 0.16 hours, an elimination half-life of 2.9 hours, and a body clearance of 0.40 +/- 0.05 L/kg/hr. The oral absorption half-life was 0.40 hours, and the bioavailability, 85.0 +/- 18.6%. Peritoneal fluid concentrations were approximately equal to serum concentrations at all times, regardless of the route of ad...
Hodgson D, Howe S, Jeffcott L, Reid S, Mellor D, Higgins A.Oral administration of altrenogest for oestrus suppression in competition horses is believed to be widespread in some equestrian disciplines, and can be administered continuously for several months during a competition season. To examine whether altrenogest has any anabolic or other potential performance enhancing properties that may give a horse an unfair advantage, we examined the effect of oral altrenogest (0.044 mg/kg), given daily for a period of eight weeks, on social hierarchy, activity budget, body-mass and body condition score of 12 sedentary mares. It was concluded that prolonged ora...
Rehbein S, Holste JE, Doucet MY, Fenger C, Paul AJ, Reinemeyer CR, Smith LL, Yoon S, Marley SE.The efficacy of an oral formulation of ivermectin plus praziquantel in the reduction of nematode and cestode egg counts in horses was assessed in 273 horses under field conditions at 15 sites in North America (n = 6) and Europe (n = 9). Horses were confirmed by fecal examination to have natural infections of strongyles (100%) and tapeworms (76%). Replicates of four horses were formed at each site, and in each replicate three animals received ivermectin (0.2 mg/kg body weight) plus praziquantel (1 mg/kg body weight) oral paste and one animal remained untreated or received vehicle paste. Fecal s...
McClure SR, White GW, Sifferman RL, Bernard W, Hughes FE, Holste JE, Fleishman C, Alva R, Cramer LG.To determine whether omeprazole oral paste administered at a dosage of 0.5 or 1 mg/kg (0.23 or 0.45 mg/lb), PO, every 24 hours would effectively prevent the recurrence of gastric ulcers in horses in race training. Methods: Prospective study. Methods: 135 horses. Methods: Horses with gastric ulcers were treated with omeprazole at a dosage of 4 mg/kg (1.8 mg/lb), PO, every 24 hours for 28 days. Horses in the dose selection portion of the study were sham dose treated or received 0.5 or 1 mg of omeprazole/kg, PO, every 24 hours for an additional 28 days. Horses in the dose confirmation portion of ...
Crisman MV, Wilcke JR, Correll LS, Irby MH.The pharmacokinetics of pentoxifylline (P) and its alcohol metabolite I (MI) were determined after administration of intravenous pentoxifylline, sustained release pentoxifylline tablets (Trental), and crushed pentoxifylline tablets in corn syrup, to five healthy adult horses. Pharmacokinetics were evaluated in a model-independent manner. After intravenous administration, pentoxifylline was rapidly eliminated (mean residence time 1.09 +/- 0.67 h), had a large steady-state volume of distribution (2.81 +/- 1.16 l/kg), and high clearance (3.06 +/- 1.05 l/kg/h). Oral absorption of pentoxifylline fr...
Marlin DJ, Scott CM, Mills PC, Louwes H, Vaarten J.The effects of administering (1) 6L isotonic oral rehydration solution (ORS), similar in composition to plasma (except for an elevated potassium concentration) and with an osmotic skeleton and (2) 6L water (no osmotic skeleton), were evaluated in five thoroughbred horses following exercise-induced dehydration. The horses were exercised on a treadmill for 10 min at walk (1.7 m.s-1; approximately 15% VO2max), 40 min at trot (3.7 m.s-1; approximately 25% VO2max) and 10 min at walk (1.7 m.s-1; approximately 15% VO2max). Exercise was undertaken on a 3 degrees incline at 30 degrees C/80% RH. Solutio...
Giorgi M, Cuniberti B, Ye G, Barbero R, Sgorbini M, Vercelli C, Corazza M, Re G.Tepoxalin is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory, and antipyretic properties and has been recently introduced into veterinary medicine. The aim of this study was to evaluate the pharmacokinetic/pharmacodynamic (PK/PD) profile of tepoxalin to assess whether it would be suitable for clinical use in horses. Six female fasting/fed horses were given 10mg/kg tepoxalin orally in a cross-over study. After administration, tepoxalin underwent rapid and extensive hydrolytic conversion to its carboxylic acid metabolite RWJ-20142. In animals that had been fed, the plasm...
Yamada ALM, do Prado Vendruscolo C, Marsiglia MF, Sotelo EDP, Agreste FR, Seidel SRT, Fülber J, Baccarin RYA, da Silva LCLC.Combined chondroitin sulfate (CS) and glucosamine (GlcN) has been widely used in oral formulations to prevent and treat osteoarthritis. CS is effective for controlling pain in osteoarthritic patients, whereas GlcN can stimulate glycosaminoglycan synthesis, thus reducing extracellular matrix degradation. Although several studies have been published on this topic, the effectiveness of treatment with oral CS and GlcN remains uncertain. The objective of this study was to analyze the progression of experimentally induced osteoarthritis in horses and verify the effectiveness of an oral compound base...
Herd RP, Stinner BR, Purrington FF.Environmental consequences of treating horses with recommended dosages of ivermectin paste were studied in two controlled experiments with 29 horses in Ohio. In 1988, dung dispersal rates were measured by changes in dry weight over time of 48 copromes (300 g) formed from feces taken from four treatment and four control horses 3 days post ivermectin treatment. There was delayed dispersal of copromes from horses treated with ivermectin in June, resulting in significantly heavier ivermectin copromes compared with those of control horses by September. There was no difference in ivermectin or contr...
Davis JL, Marshall JF, Papich MG, Blikslager AT, Campbell NB.The purpose of this study was to determine the pharmacokinetics of deracoxib following oral administration to horses. In addition, in vitro equine whole blood cyclooxygenase (COX) selectivity assays were performed. Six healthy adult horses were administered deracoxib (2 mg/kg) orally. Plasma samples were collected prior to drug administration (time 0), and 10, 20, 40 min and 1, 1.5, 2, 4, 6, 8, 12, 24, and 48 h after administration for analysis with high pressure liquid chromatography using ultraviolet detection. Following PO administration, deracoxib had a long elimination half-life (t(...
Soma LR, Uboh CE, Guan F, Luo Y, Teleis D, Runbo L, Birks EK, Tsang DS, Habecker P.Plasma and tissue concentrations of clenbuterol (CLB) were determined following oral (p.o.) administration of 1.6 microg/kg twice daily (b.i.d.) for 2 weeks. Horses were administered the last dose on morning of day 15, killed at 0.25, 24, 48, and 72 h post-administration. At 0.25 h, the highest tissue concentrations of CLB were found in the liver (16.21 ng/g), lung (6.48 ng/g), left ventricle (4.99 ng/g), kidney (3.35 ng/g), bronchi (2.56 ng/g), right ventricle (2.08 ng/g), and eye fluids (1.09 ng/g) all of which were higher than that of plasma (1.10 ng/mL). The elimination half-lives (t(1/2k)...
Rees WA, Harkins JD, Lu M, Holland RE, Lehner AF, Tobin T, Chambers TM.To determine pharmacokinetics of single and multiple doses of rimantadine hydrochloride in horses and to evaluate prophylactic efficacy of rimantadine in influenza virus-infected horses. Methods: 5 clinically normal horses and 8 horses seronegative to influenza A. Methods: Horses were given rimantadine (7 mg/kg of body weight, i.v., once; 15 mg/kg, p.o., once; 30 mg/kg, p.o., once; and 30 mg/kg, p.o., q 12 h for 4 days) to determine disposition kinetics. Efficacy in induced infections was determined in horses seronegative to influenza virus A2. Rimantadine was administered (30 mg/kg, p.o., q 1...
Knych HK, Stucker K, Gretler SR, Kass PH, McKemie DS.In humans, codeine is a commonly prescribed analgesic that produces its therapeutic effect largely through metabolism to morphine. In some species, analgesic effects of morphine have also been attributed to the morphine-6-glucuronide (M6G) metabolite. Although an effective analgesic, administration of morphine to horses produces dose-dependent neuroexcitation at therapeutic doses. Oral administration of codeine at a dose of 0.6 mg/kg has been shown to generate morphine and M6G concentrations comparable to that observed following administration of clinically effective doses of morphine, witho...
Brown MP, Gronwall RR, Houston AE.Six healthy adult mares were each given an oral loading dose of ormetoprim(OMP)-sulfadimethoxine (SDM) at a dosage of 9.2 mg of OMP/kg and 45.8 mg of SDM/kg, followed by four maintenance doses of 4.6 mg of OMP/kg and 22.9 mg of SDM/kg, at 24 h intervals. Ormetoprim and SDM concentrations were measured in serum, synovial fluid, peritoneal fluid, cerebrospinal fluid, urine and endometrium. The highest mean serum OMP concentration was 0.92 micrograms/mL 0.5 h after the first dose; the highest mean SDM concentration was 80.9 micrograms/mL 8 h after the first dose. The highest mean synovial fluid c...
Arnbjerg J.Peroral application of iron salts in various types of anemia was previously considered atoxic. The increased use of iron has, however, led to an increasing number of poisoning in children, taking iron tablets for candy. There have only been reported a few number of spontaneous intoxications in animals, but experimentally it has been possible to produce fatal intoxications in various kinds of animal species. The clinical findings are quite similar in the various animals, starting with vomiting, bloody diarrhoea and metabolic acidosis. If the intoxication is severe, shock and coma may develop, a...
Dembek KA, Hurcombe SD, Schober KE, Toribio RE.To describe a case of supraventricular tachycardia and sudden death in a horse following administration of flecainide acetate. Methods: An 8-year-old Hanoverian warmblood gelding was treated for chronic, naturally occurring, supraventricular tachycardia with digoxin, procainamide hydrochloride, quinidine sulfate, and flecainide acetate. After oral administration of flecainide, polymorphic ventricular tachycardia (torsades de pointes) and ventricular fibrillation developed, leading to cardiovascular collapse and death. Conclusions: Atrial fibrillation is the most commonly diagnosed dysrhythmia ...
De Clercq D, Baert K, Croubels S, van Loon G, Maes A, Tavernier R, Deprez P, De Backer P.To determine the clinical effects and pharmacokinetics of amiodarone after single doses of 5 mg/kg administered orally or intravenously. Methods: 6 healthy adult horses. Methods: In a cross over study, clinical signs and electrocardiographic variables were monitored and plasma and urine samples were collected. A liquid chromatography-mass spectrometry method was used to determine the percentage of protein binding and to measure plasma and urine concentrations of amiodarone and the active metabolite desethylamiodarone. Results: No adverse clinical signs were observed. After IV administration, m...
van Duijkeren E, Vulto AG, Sloet van Oldruitenborgh-Oosterbaan MM, Kessels BG, van Miert AS, Breukink HJ.In the present study, the pharmacokinetic parameters of a trimethoprim/sulphachlorpyridazine preparation following intravenous administration, administration by nasogastric tube and administration with concentrate were determined in the horse. Eight adult horses were dosed at 1 week intervals in a sequentially designed study at a dose of 5 mg/kg trimethoprim (TMP) and 25 mg/kg sulphachlorpyridazine (SCP) on all occasions. Plasma concentrations of both drugs were measured serially for 48 h. Pharmacokinetic parameters of clinical importance (distribution and elimination half-lives, clearance, bi...
Ensink JM, Vulto AG, van Miert AS, Tukker JJ, Winkel MB, Fluitman MA.To determine the oral bioavailabilities of 3 ampicillin esters (pivampicillin, bacampicillin, and talampicillin) and ampicillin sodium, and to determine in vitro stability of the ampicillin esters in ileal contents (pH 8.3 to 8.5). Methods: A crossover design to administer the 4 drugs orally, and ampicillin i.v. to all horses in the study. Methods: 4 healthy adult horses. Methods: The drugs were administered intragastrically to the horses at a dosage equimolar to 15 mg of ampicillin/kg of body weight. Also, ampicillin sodium was administered i.v. at the same dosage. Blood samples were taken up...
Chaffin MK, Fajt V, Martens RJ, Arnold CE, Cohen ND, O'Conor M, Taylor RJ, Bernstein LR.Gallium is a trivalent semi-metal with anti-microbial effects because of its incorporation into crucial iron-dependent reproductive enzyme systems. Gallium maltolate (GaM) provides significant gallium bioavailability to people and mice following oral administration and to neonatal foals following intragastric administration. To study the prophylactic and therapeutic effects of GaM against Rhodococcus equi pneumonia in foals, we developed a methylcellulose formulation of GaM (GaM-MCF) for oral administration to neonatal foals. Normal neonatal foals were studied. Six foals received 20 mg/kg and ...
Winther L, Baptiste KE, Friis C.Ampicillin concentrations in pulmonary epithelial lining fluid (PELF) and plasma was studied after single intravenous ampicillin administration (15mg/kg) or single intragastric administration of its prodrug, pivampicillin (19.9mg/kg) to horses and discussed in relation to minimum inhibitory concentrations (MIC) of common equine respiratory pathogens. After intravenous administration, elimination of ampicillin was fast and not detectable in plasma after 12h in three out of six horses. Pivampicillin was absorbed well in non-fasted horses with an oral bioavailability of 36%. The degree of penetra...
Cirak VY, Güleğen E, Yildirim F, Durmaz M.The aim of the present study was to determine the efficacy and the so-called "egg reappearance period" (ERP) of doramectin in horses naturally infected with strongyles during a period of 34 weeks. A group of yearlings of 10 animals was treated intramuscularly with doramectin at a dose rate of 0.2 mg/kg bodyweight (BW) at the begin of the grazing season. To obtain comparable data, another group of yearlings (n = 10) was treated orally with ivermectin at a dose rate of 0.2 mg/kg BW. Individual faecal samples were examined for strongyle egg counts per gram of faeces (EPG) in two-week intervals. T...
Serrano-Rodríguez JM, Gómez-Díez M, Esgueva M, Castejón-Riber C, Mena-Bravo A, Priego-Capote F, Ayala N, Caballero JMS, Muñoz A.Pharmacokinetic and pharmacodynamic (PK/PD) properties of the angiotensin-converting enzyme inhibitor (ACEI) benazeprilat have not been evaluated in horses. This study was designed to establish PK profiles for benazepril and benazeprilat after intravenous (IV) and oral (PO) administration of benazepril using a PK/PD model. This study also aims to determine the effects of benazeprilat on serum angiotensin converting enzyme (ACE), selecting the most appropriate dose that suppresses ACE activity. Six healthy horses in a crossover design received IV benazepril at 0.50mg/kg and PO at doses 0 (place...
Soma LR, Robinson MA, You Y, Boston RC, Rudy J.Compartmental models were used to investigate the pharmacokinetics of intravenous (i.v.), oral (p.o.), and topical (TOP) administration of dimethyl sulfoxide (DMSO). The plasma concentration-time curve following a 15-min i.v. infusion of DMSO was described by a two-compartment model. Median and range of alpha (t ) and beta (t ) half-lives were 0.029 (0.026-0.093) and 14.1 (6.6-16.4) hr, respectively. Plasma concentration-time curves of DMSO following p.o. and TOP administration were best described by one-compartment absorption and elimination models. Following the p.o. administration, median a...
Kuroda T, Nagata S, Takizawa Y, Tamura N, Kusano K, Mizobe F, Hariu K.The pharmacokinetics of d-chlorpheniramine (CPM), a histamine H1-receptor antagonist, and its ability to inhibit of histamine-induced cutaneous wheal formation, were studied in healthy Thoroughbred horses (n=5). Following an intravenous (IV) dose of 0.5mg/kg bodyweight (BW), plasma drug disposition was very rapid, with the mean terminal half-life and total body clearance calculated as 2.7h and 0.7 L/h/kg, respectively. The observed maximal inhibition of wheal formation following IV doses of 0.1 and 0.5mg/kg BW were 37.8% and 60.6% at 0.5h, respectively. Oral administration of CPM (0.5mg/kg BW)...
Sykes BW, Underwood C, McGowan CM, Mills PC.This study aimed to investigate the effect of diet and dose on the pharmacokinetics of omeprazole in the horse. Six horses received two doses (1 and 4 mg/kg) of omeprazole orally once daily for 5 days. Each dose was evaluated during feeding either a high-grain/low-fibre (HG/LF) diet or an ad libitum hay (HAY) diet in a four-way crossover design. Plasma samples were collected for pharmacokinetic analysis on days 1 and 5. Plasma omeprazole concentrations were determined by ultra-high pressure liquid chromatography-mass spectrometry. In horses being fed the HG/LF diet, on day 1, the area under...
Sleeper MM, McDonnell SM, Ely JJ, Reef VB.Enalapril is an angiotensin converting enzyme (ACE) inhibitor that is frequently used in human, feline and canine patients with cardiac disease. Its use has been associated with impotence in human patients. The purpose of this study was to evaluate if enalapril (0.5mg/kg PO, q24h) is likely to alter behavior in stallions and to assess its effect on ACE activity at the standard dose used in dogs and cats. Twelve pony stallions were evaluated by physical examination and echocardiography followed by treatment with enalapril (n=6) or placebo (n=6) for 2 months. After one month, blood was drawn and...
Burrows GE, MacAllister CG, Beckstrom DA, Nick JT.The plasma concentrations and pharmacokinetics of rifampin disposition were determined after a single IV, IM, or oral dose of 10 mg/kg of body weight and an oral dose of 25 mg/kg. The overall elimination rate constants per minute were similar for the 10 mg/kg dose (0.0021 +/- 0.0004, IV; 0.0017 +/- 0.0002, IM; and 0.0023 +/- 0.0006, orally). The apparent bioavailability was moderate to low for IM and oral administrations (59.8% +/- 3.2% and 39.5% +/- 5.0%, respectively). The rate of absorption was most rapid for oral administration with an absorption half-life of 249.7 +/- 71.6 minutes as comp...
