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.
Nolen-Walston RD, Moore CM, Barr CA, Tomlinson JE, Boston RC, Soma LR.To determine the anabolic and lipolytic effects of a low dosage of clenbuterol administered orally in working and nonworking equids. Methods: 8 nonworking horses and 47 polo ponies in active training. Methods: Each polo pony continued training and received either clenbuterol (0.8 μg/kg) or an equal volume of corn syrup (placebo) orally twice daily for 21 days, and then was evaluated for another 21-day period. Nonworking horses received clenbuterol or placebo at the same dosage for 21 days in a crossover trial (2 treatments/horse). For working and nonworking horses, percentage body fat (PBF) w...
Sykes BW, Underwood C, McGowan CM, Mills PC.The objectives of this study were to investigate the impact of formulation (enteric coated and buffered) and feeding on pharmacokinetic variables associated with the oral administration of omeprazole in the horse. Six thoroughbred racehorses were studied in a crossover design. Each received 2 g of an enteric coated or buffered formulation in both the fed and fasted state. Plasma omeprazole concentrations were determined by UHPLC-MS. The effects of feeding or formulation on AUC0-inf_obs, half-life, Tmax or Cmax were not statistically significant. However, a wider-than-expected degree of variati...
Kim TW, Della Rocca G, Di Salvo A, Ryschanova R, Sgorbini M, Giorgi M.To determine the pharmacokinetics of cimicoxib and to assess the inhibition of cyclooxygenase (COX) after a 5 mg/kg, single oral administration in horses that were fasted or fed. Methods: The study was conducted using an open, single dose (5 mg/kg), two treatment (fasted and fed), two-period, crossover design with a 2-week interval between dosages. Six healthy mares received 5 mg/kg of cimicoxib via nasogastric tube after fasting for 12 hours, or 2 hours after feeding. After administration, blood samples were collected for up to 24 hours and plasma used for pharmacokinetic analysis. Addi...
Roscher KA, Failing K, Moritz A.This study aimed to validate a loading and maintenance clopidogrel dosing scheme for the inhibition of platelet function, measured by whole blood impedance aggregometry in healthy adult horses. Ten Warmblood horses received oral clopidogrel once daily. Doses were based on 50 kg weight categories and resulted in one loading dose of 6-6.5 mg/kg bodyweight and maintenance doses of 1.2-1.4 mg/kg over the next 4 days. Platelet function was measured via whole blood multiple electrode impedance aggregometry prior to (T0) and at 6, 12, 24, 48, 72, 96, 144, 192 and 240 h following the loading d...
Kwok WH, Kwok KY, Leung DK, Leung GN, Wong CH, Wong JK, Wan TS.The positive findings of norbolethone in 2002 and tetrahydrogestrinone in 2003 in human athlete samples confirmed that designer steroids were indeed being abused in human sports. In 2005, an addition to the family of designer steroids called 'Madol' [also known as desoxy-methyltestosterone (DMT)] was seized by government officials at the US-Canadian border. Two years later, a positive finding of DMT was reported in a mixed martial arts athlete's sample. It is not uncommon that doping agents used in human sports would likewise be abused in equine sports. Designer steroids would, therefore, pose...
Ishizaka S, Matsuda A, Amagai Y, Oida K, Jang H, Ueda Y, Takai M, Tanaka A, Matsuda H.The effects of probiotics on horses are still controversial. The present study was a randomized, double-blinded, placebo-controlled crossover study designed to evaluate the ability of probiotics to improve intestinal conditions in adult horses. Fermented probiotics were administered to 10 healthy adult geldings for 28 days. The clinical condition of the horses was monitored daily, and the blood and feces were biochemically analyzed every 14 days. In the probiotic-treated group, the concentration of carboxylic acids in the feces was increased at days 14 and 28. In contrast to the fecal pH in th...
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 ...
Vendrig JC, Coffeng LE, Fink-Gremmels J.In the first phase of life, in which the immune system is primed and the bacterial colonization of epithelial surfaces takes place, foals are highly susceptible to bacterial infections. Next to strategies to optimize maternally acquired immunity in individual foals, current research explores other options to modulate immune responses in foals. During the past decades, oligosaccharide supplements were developed to mimic beneficial properties of the oligosaccharides, which are present in colostrum and milk. In human infants and laboratory animal species, dietary supplementation with galacto-olig...
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 ...
Holland B, Fogle C, Blikslager AT, Curling A, Barlow BM, Schirmer J, Davis JL.The objectives of this study were to compare the pharmacokinetics and COX selectivity of three commercially available formulations of firocoxib in the horse. Six healthy adult horses were administered a single dose of 57 mg intravenous, oral paste or oral tablet firocoxib in a three-way, randomized, crossover design. Blood was collected at predetermined times for PGE2 and TXB2 concentrations, as well as plasma drug concentrations. Similar to other reports, firocoxib exhibited a long elimination half-life (31.07 ± 10.64 h), a large volume of distribution (1.81 ± 0.59L/kg), and a slow clearanc...
Donnell JR, Frisbie DD.This review presents the pathogenesis and medical treatment of equine osteoarthritis (OA), focusing on firocoxib. Inhibition of prostaglandin E remains a fundamental treatment for decreasing clinical symptoms (ie, pain and lameness) associated with OA in horses. Nonsteroidal anti-inflammatory drugs (NSAIDs), which inhibit the production of prostaglandin E from the arachidonic acid pathway, continue to be a mainstay for the clinical treatment of OA. Firocoxib is a cyclooxygenase (COX)-2-preferential NSAID that has been shown to be safe and to have a 70% oral bioavailability in the horse. Three ...
Hunyadi L, Papich MG, Pusterla N.The purpose of this study was to determine the pharmacokinetics of the FDA-approved labeled dose of diclazuril and compare it to a low dose in plasma and CSF in adult horses. During each research period, six healthy adult horses received 0.5 mg/kg of 1.56% diclazuril pellets (Protazil(TM) , Merck Animal Health) compared to the approved labeled dose of 1 mg/kg orally once in two separate phases. A dose of 0.5 mg/kg was calculated to each horse's weight. Blood was then collected immediately before diclazuril administration and then at regular intervals up to a 168 h. After the last blood collect...
Sykes BW, Underwood C, McGowan CM, Mills PC.The objectives were to document the pharmacokinetics of intravenous, enteric-coated oral and plain oral omeprazole in fasted horses and to investigate the impact of feeding on the bioavailability of an enteric-coated omeprazole. Twelve horses received four treatments: intravenous omeprazole (0.5 mg/kg) in the fasted state (IV-Fasted), enteric-coated omeprazole (4 mg/kg) orally in the fasted state (ECO-Fasted), enteric-coated omeprazole (4 mg/kg) orally in the fed state (ECO-Fed) and plain omeprazole (4 mg/kg) orally in the fasted state (PL-Fasted). Plasma omeprazole concentrations were det...
Lopez BS, Giguère S, Berghaus LJ, Mullins MA, Davis JL.The objectives of this study were to investigate the pharmacokinetics of danofloxacin and its metabolite N-desmethyldanofloxacin and to determine their concentrations in synovial fluid after administration by the intravenous, intramuscular or intragastric routes. Six adult mares received danofloxacin mesylate administered intravenously (i.v.) or intramuscularly (i.m.) at a dose of 5 mg/kg, or intragastrically (IG) at a dose of 7.5 mg/kg using a randomized Latin square design. Concentrations of danofloxacin and N-desmethyldanofloxacin were measured by UPLC-MS/MS. After i.v. administration, da...
The locomotor pattern alterations produced after the administration of a sublingual detomidine gel was measured by an accelerometric method in horses. Using a randomized two-way crossover design, all animals (n = 6) randomly received either detomidine gel or a placebo administered sublingually. A triaxial accelerometric device was used for gait assessment 15 minutes before (baseline) and every 10 minutes after each treatment for a period of 180 minutes. Eight different parameters were calculated, including speed, stride frequency, stride length, regularity, dorsoventral, propulsion, mediolater...
Walker WT, Callan RJ, Hill AE, Tisher KB.This study evaluated the effects of administering oral powder electrolytes on packed cell volume (PCV), plasma chemistry parameters, and incidence of colic in horses participating on a 6-day 162-km trail ride in which water was not offered ad libitum. Twenty-three horses received grain with powder electrolytes daily while 19 control horses received grain only. Horses were ridden approximately 32 km a day at a walk or trot. Packed cell volume and plasma chemistry parameters were analyzed daily. Episodes of colic were diagnosed and treated by a veterinarian unaware of treatment group allocation....
Knych HK, Steinmetz SJ, McKemie DS.The anti-anxiety and calming effects following activation of the GABA receptor have been exploited in performance horses by administering products containing GABA. The primary goal of the study reported here was to describe endogenous concentrations of GABA in horses and the pharmacokinetics, selected pharmacodynamic effects, and CSF concentrations following administration of a GABA-containing product. The mean (±SD) endogenous GABA level was 36.4 ± 12.5 ng/mL (n = 147). Sixteen of these horses received a single intravenous and oral dose of GABA (1650 mg). Blood, urine, and cerebrospin...
Lindinger MI, Anderson SC.We describe a safety assessment of an oral supplement designed to nutritionally support the gastrointestinal system of horses. The supplement comprised a mixture of essential (l-threonine) and conditionally essential (l-glutamine) amino acids, polar lipids, oat bran rich in beta glucans and yeast extract. Young (1-2years) horses of both sexes were allocated to control (n=7) and treatment groups (n=7) and studied for 9weeks. Horses in the treatment group received the supplement daily for 8weeks. After 8weeks of supplementation, horses were studied for one additional week. Outcome measures inclu...
Gómez-Díez M, Muñoz A, Caballero JM, Riber C, Castejón F, Serrano-Rodríguez JM.Pharmacokinetic and pharmacodynamic of IV enalapril at 0.50 mg/kg, PO placebo and PO enalapril at three different doses (0.50, 1.00 and 2.00 mg/kg) were analyzed in 7 healthy horses. Serum concentrations of enalapril and enalaprilat were determined for pharmacokinetic analysis. Angiotensin-converting enzyme (ACE) activity, serum ureic nitrogen (SUN), creatinine and electrolytes were measured, and blood pressure was monitored for pharmacodynamic analysis. The elimination half-lives of enalapril and enalaprilat were 0.67 and 2.76 h respectively after IV enalapril. Enalapril concentrations ...
Kranenburg LC, Westermann CM, de Sain-van der Velden MG, de Graaf-Roelfsema E, Buyse J, Janssens GP, van den Broek J, van der Kolk JH.Insulin resistance in horses is an emerging field of interest as it is thought to be a contributing factor in the pathogenesis of many equine conditions. Objective: The objectives of the present study were to determine the effects of long-term oral administration of L-carnitine on insulin sensitivity, glucose disposal, plasma leptin concentrations and acylcarnitine spectrum both in plasma and urine. Methods: Six 3-year-old healthy warmblood geldings were used. In a double blind 2 × 2 Latin square design at a dosage of 100 mg/kg body weight (BW)/day for 28 days the effects of oral supplementat...
Hussein H, Ishihara A, Menendez M, Bertone A.Plasma pharmacokinetic (PK) and bone resorption biomarker [carboxy-terminal cross-linking telopeptide of type I collagen (CTX-1)] analyses were performed following single and multiple oral dose protocols of a Cathepsin K inhibitor (VEL-0230) in horses. Outcomes included plasma and urine drug and CTX-1 concentrations. In the dose range study, 2, 4, and 8 mg/kg body weight (b.w.) doses were administered in a Latin square design to three mares and evaluated for 1 week. Based on the PK characteristics of VEL-0230, 4 mg/kg b.w. was selected for the dose interval study in which 3.25 days (d) and 7 d...
Collins CW, Monfort SL, Vick MM, Wolfe BA, Weiss RB, Keefer CL, Songsasen N.To date, there has been limited research on manipulation of the estrous cycle in endangered equids. The objectives of this study were to assess the efficacy of using combinations of: (a) oral altrenogest and PGF2α, and (b) injectable altrenogest and PGF2α for manipulation of ovarian activity in Przewalski's mares. Reproductive cycles were monitored by assessing follicular changes with rectal ultrasound and changes in urinary steroid hormones. In Study 1, five cycling mares were treated with oral altrenogest (n=11 cycles) for 14 days. In Study 2, cycling mares were treated with oral altrenoge...
Davis JL, Kruger K, LaFevers DH, Barlow BM, Schirmer JM, Breuhaus BA.Angiotensin converting enzyme (ACE) inhibitors improve survival and quality of life in human patients and small animals with cardiovascular and renal disease. There is limited information regarding their effects in horses. Objective: The purpose of this study was to determine the pharmacokinetics of quinapril and its effects on ACE and renin in horses. Methods: Experimental study using healthy mature horses. Methods: Six healthy horses were administered quinapril at 120 mg i.v., 120 mg per os and 240 mg per os in a 3-way crossover design. Blood was collected for measurement of quinapril ...
Knych HK, Stanley SD, Arthur RM, Mitchell MM.The use of firocoxib in horses and its ability to affect performance and potential to allow a horse to compete when it otherwise should not, necessitates establishing appropriate withdrawal time guidelines prior to performance. Objective: To describe plasma concentrations and characterise the pharmacokinetics of 3 firocoxib formulations following multiple administrations of the label dose, with respect to recommended plasma thresholds for performance horses. Methods: Balanced 3-way crossover prospective study. Methods: Nine healthy mature horses were administered firocoxib injectable solution ...
Kivett L, Taintor J, Wright J.Simultaneous administration of a nonselective COX inhibitor and a COX-2 specific NSAID has not been previously reported in horses. The goal of this study was to determine the safety of a 10-day dosage regimen of phenylbutazone and firocoxib, both at their standard dosages, in horses. Six horses were administered 2.2 mg/kg of phenylbutazone and 0.1 mg/kg of firocoxib by mouth, daily for 10 days. Horses were assessed daily for changes in behavior, appetite, fecal consistency, signs of abdominal pain, and oral mucous membrane ulceration. Horses were assessed prior to and on the last day of treatm...
Della Rocca G, Di Salvo A, Cagnardi P, Marchesi MC, Conti MB.It is well-known that old animals show physiologic and/or pathologic variation that could modify the pharmacokinetics of drugs and the related pharmacodynamic response. In order to define the most appropriate therapeutic protocol in old horses, pharmacokinetic profile and safety of naproxen were investigated in horses aged over 18 years after oral administration for 5 days at the dose of 10 mg/kg b.w./day. After the first administration, the maximum concentration (Cmax 44.21 ± 9.21 μg/mL) was reached at 2.5 ± 0.58 h post-treatment, the harmonic mean terminal half-life was 6.96 ± 1.73 h, AU...
Maher MC, Schnabel LV, Cross JA, Papich MG, Divers TJ, Fortier LA.To determine whether low-dose, low-frequency doxycycline administration is capable of achieving chondroprotective concentrations within synovial fluid (SF) while remaining below minimum inhibitory concentration 90 (MIC90 ) of most equine pathogens and would be an option in the management of osteoarthritis. Objective: To determine whether low-dose, low-frequency oral administration of doxycycline can attain in vivo SF concentrations capable of chondroprotective effects through reduction of matrix metalloproteinase (MMP)-13 activity, while remaining below MIC90 of most equine pathogens. Method...
Guedes AG, Knych HK, Soares JH, Brosnan RJ.This study evaluated the pharmacokinetics and physiological effects of tramadol during repeated oral administrations in horses. Nine adult healthy horses were administered tramadol at 5 and 10 mg/kg orally every 12 h for 5 days in a randomized, crossover design with a 3-week washout between treatments. Plasma concentrations of tramadol, O- and N-desmethyltramadol (M1 and M2) were measured using Liquid-Chromatography-Mass Spectrometry at predetermined time points following each tramadol administration. Cardiovascular, respiratory and gastrointestinal physiological variables were monitored an...
Hovanessian N, Davis JL, McKenzie HC, Hodgson JL, Hodgson DR, Crisman MV.The purpose of this study was to determine the pharmacokinetics and safety profile of firocoxib in neonatal foals. Seven healthy foals were administered 0.1 mg/kg firocoxib orally q24 h for nine consecutive days, commencing at 36 h of age. Blood was collected for firocoxib analysis using high-pressure liquid chromatography with fluorescence detection at 0 (dose #1 only), 0.25, 0.5, 1, 2, 4, 8, 16, and 24 h after doses 1, 5, and 9. For all other doses (2, 3, 4, 6, 7, and 8), blood was collected immediately prior to the next dose (24 h trough). Elimination samples (36, 48, 72, 96, 120, and 1...
Bergan T, Versland I.To be active, antimicrobials must reach the bacteria in the infectious foci in adequate concentrations. Direct measurements of levels in the various foci are difficult to perform, but a number of animal models with artificial extravascular foci have been developed. In many ways, the physiology of pigs resemble that of humans. Consequently, it was thought that pigs might also parallel humans in the handling of penicillins. General pharmacokinetics of ampicillin and flucloxacillin and the penetration of the substances to subcutaneously implanted teflon tistisue chambers were investigated. Ampici...
Knych HK, Mama KR, Steffey EP, Stanley SD, Kass PH.OBJECTIVE To measure concentrations of trazodone and its major metabolite in plasma and urine after administration to healthy horses and concurrently assess selected physiologic and behavioral effects of the drug. ANIMALS 11 Thoroughbred horses enrolled in a fitness training program. PROCEDURES In a pilot investigation, 4 horses received trazodone IV (n = 2) or orally (2) to select a dose for the full study; 1 horse received a vehicle control treatment IV. For the full study, trazodone was initially administered IV (1.5 mg/kg) to 6 horses and subsequently given orally (4 mg/kg), with a 5-week ...
Frank N, Buchanan BR, Elliott SB.To determine the effects of long-term oral levothyroxine sodium (L-T(4)) administration on serum thyroid hormone concentrations, thyroid gland function, clinicopathologic variables, and echocardiographic examination measurements in adult euthyroid horses. Methods: 6 healthy adult mares. Methods: Horses received L-T(4) (48 mg/d) orally for 48 weeks. Every 4 weeks, physical examinations were performed; blood samples were collected for CBC, plasma biochemical analyses, and assessments of serum total triiodothyronine (tT(3)) and thyroxine (tT(4)) concentrations. Plasma creatine kinase MB activity ...
Snow DH, Gash SP, Cornelius J.The effects of oral administration of high doses of ascorbic acid on plasma concentrations were investigated in both experimental Thoroughbred horses and those within racing stables. A single oral dose (20 g) did not result in any increase in plasma concentrations. However, daily administration of either 4.5 g or 20 g doses resulted in significant increases in plasma concentrations. Monthly variations in plasma ascorbate concentrations were found in both supplemented (20 g daily) and unsupplemented stables. It is concluded that oral supplementation with ascorbic acid is a satisfactory route to...
Trevisiol S, Moulard Y, Delcourt V, Jaubert M, Boyer S, Tendon S, Haryouli H, Taleb W, Caroff M, Chabot B, Drif L, André F, Garcia P, Loup B....According to international sport institutions, the use of peroxisome proliferator activated receptor (PPAR)-δ agonists is forbidden at any time in athlete career due to their capabilities to increase physical and endurance performances. The (PPAR)-δ agonist GW501516 is prohibited for sale but is easily available on internet and can be used by cheaters. In the context of doping control, urine is the preferred matrix because of the non-invasive nature of sampling and providing broader exposure detection times to forbidden molecules but often not detected under its native form due to the organi...
Broux B, De Clercq D, Decloedt A, Vera L, Devreese M, Gehring R, Croubels S, van Loon G.Arrhythmias in horses may require long-term anti-arrhythmic therapy. Unfortunately, oral anti-arrhythmic drugs for use in horses are currently scarce. In human patients and small animals, sotalol, a β-blocker with class III anti-arrhythmic properties, is often used for long-term treatment. Objective: To determine the pharmacokinetics of sotalol at multiple oral dosages in unfasted horses, as well as the effects on electro- and echocardiographic measurements, right atrial and ventricular monophasic action potential (MAP) and effective refractory period (ERP). Methods: Placebo controlled, doubl...
Stowe HD.Thirty-four adult ponies were used to determine the effects of single oral doses of copper (Cu) supplements (0, 20, and 40 mg of Cu/kg of body weight) on the toxicity of oral doses of selenium (Se) supplements (0, 2, 4, 6, and 8 mg of Se/kg of body weight) administered 24 hours after the copper was given. Signs of Se toxicosis-sweating, diarrhea, tachycardia, tachypnea, mild pyrexia, lethargy, and colic-developed in ponies given 6 and 8 mg of Se/kg of body weight without Cu pretreatment. Two of 4 ponies given 6 mg of Se/kg and both ponies given 8 mg of Se/kg without Cu pretreatment died within...
Serpa PBS, Brooks MB, Divers T, Ness S, Birschmann I, Papich MG, Stokol T.Horses with inflammatory and infectious disorders are often treated with injectable heparin anticoagulants to prevent thrombotic complications. In humans, a new class of direct oral acting anticoagulants (DOAC) appear as effective as heparin, while eliminating the need for daily injections. Our study in horses evaluated apixaban, a newly approved DOAC for human thromboprophylaxis targeting activated factor X (Xa). Our goals were to: (1) Determine pharmacokinetics and pharmacodynamics of apixaban after oral (PO) and intravenous (IV) administration in horses; (2) Detect any inhibitory effects of...
Gardner RB, White GW, Ramsey DS, Boucher JF, Kilgore WR, Huhtinen MK.To determine whether sublingual detomidine gel administration to horses would be effective in providing an appropriate degree of sedation and restraint to facilitate completion of veterinary and husbandry procedures under field conditions. Methods: Multicenter, prospective, randomized, blinded, placebo-controlled clinical study. Methods: 270 client-owned horses known to require sedation or strong restraint to enable veterinary and husbandry procedures to be performed. Methods: Horses randomly received a single dose of detomidine gel (0.04 mg/kg [0.018 mg/lb]) or placebo gel administered sublin...
Wang J, Xue J, Kong J, Li J, Zhang S, Cao X.The pharmacokinetic properties of vitacoxib have not been established completely; current dosage recommendations are based on clinical experiences. The primary objective of this study was to describe plasma concentrations and characterize the pharmacokinetics of vitacoxib formulation following oral administrations in horses. Also, the effect of the state of stomach contents on the absorption of vitacoxib was investigated in fed/fasted horses. Blood samples were collected prior to and at various times up to 72 hr post-administration. Drug concentrations were measured using ultra high-performan...
Sanchez LC, Lester GD, Merritt AM.To determine intragastric pH in newborn foals and to examine the effect of i.v. or oral administration of an H2-receptor antagonist on intragastric pH. Methods: Prospective controlled study. Methods: 6 healthy mixed-breed neonatal foals. Methods: Intragastric pH was measured, using an antimony electrode. Foals were monitored on days 2, 4, and 6 after birth, and each received 3 treatments. The pH was recorded for 4 hours before treatment and for 10 hours after ranitidine administration (2 mg/kg [0.91 mg/lb] of body weight, i.v.; 6.6 mg/kg [3 mg/lb], PO) or 20 hours after corn syrup administrati...
Furr M, Kennedy T.Toltrazuril 5% suspension (Baycox, Bayer Canada, Ontario, Canada) was administered to six adult horses followed by blood collection and assay to determine the concentration of toltrazuril and its principal metabolites, toltrazuril sulfone and toltrazuril sulfoxide. From this data, the maximum concentration (C(max)), elimination half-life (T 1/2), and mean residence times of the plasma were determined from standard pharmacokinetic formulas. After a single oral dose of 10 mg/kg body weight a rapid absorption was found, with a mean peak serum concentration of 11.17 mg/L at 18 hours. Elimination w...
Horspool LJ, Taylor DJ, McKellar QA.Amikacin was detectable (> 0.02 micrograms/ml) in plasma for 12 h in horses and donkeys and for 8 h in ponies following intravenous (i.v.) administration at a dose rate of 6 mg/kg bodyweight. The elimination half-life (harmonic mean) of amikacin was 2.8, 1.6 and 1.9 h in horses, ponies and donkeys, respectively, and the mean body clearance was relatively slow (45.2, 82.4 and 58.0 ml/h.kg, respectively). A suitable dosage interval for the i.v. administration of amikacin sulphate to horses, ponies and donkeys, at a dose rate of 6 mg/kg, would be every 8 h in horses, and every 6 h in ponies an...
Wise JC, Hughes KJ, Edwards S, Jacobson GA, Narkowicz CK, Raidal SL.Omeprazole preparations vary in bioavailability in horses. Objective: To characterize the pharmacokinetics and pharmacodynamics of an existing enteric-coated oral omeprazole paste (REF) and a novel, in-feed, enteric-coated dry granule preparation (NOV). Methods: Twelve Standardbred/Thoroughbred mares free from clinical disease. Methods: A prospective, blinded randomized interventional study was trial, conducted in 3 parts: (a) bioavailability study, (b) dose titration study, and (c) comparative clinical pharmacodynamic study, each using a blocked crossover design. Results: Consistent with the ...
Kim TW, Della Rocca G, Di Salvo A, Ryschanova R, Sgorbini M, Giorgi M.To determine the pharmacokinetics of cimicoxib and to assess the inhibition of cyclooxygenase (COX) after a 5 mg/kg, single oral administration in horses that were fasted or fed. Methods: The study was conducted using an open, single dose (5 mg/kg), two treatment (fasted and fed), two-period, crossover design with a 2-week interval between dosages. Six healthy mares received 5 mg/kg of cimicoxib via nasogastric tube after fasting for 12 hours, or 2 hours after feeding. After administration, blood samples were collected for up to 24 hours and plasma used for pharmacokinetic analysis. Addi...
Symonds KD, MacAllister CG, Erkert RS, Payton ME.To evaluate the musculoskeletal analgesic effect of etodolac administered PO every 12 or 24 hours in chronically lame horses by use of force plate analysis. Methods: 22 horses with navicular syndrome. Methods: Horses received etodolac (23 mg/kg, PO, q 12 h; n = 7), etodolac (23 mg/kg, PO, q 24 h; 8), or corn syrup (20 mL, PO, q 24 h; control treatment; 7) for 3 days. Combined forelimb peak vertical ground reaction force (PVF) was measured via force plate analysis before the first treatment (baseline) and at 6, 12, 24, and 36 hours after the last treatment. Differences in mean PVF (mPVF) betwee...
Yamanaka T, Tsujimura K, Kondo T, Hobo S, Matsumura T.We investigated the efficacy of the oral administration of oseltamivir phosphate (OP) in horses experimentally infected with equine influenza A virus (H3N8). Nine horses were divided into three horses each of control, treatment and prophylaxis groups. An administration protocol for the treatment group (2 mg/kg of body weight, twice a day for five days) was started immediately after the onset of pyrexia (above 38.9 degrees C). An administration protocol for the prophylaxis group (2 mg/kg of body weight, once a day for five days) was started on a day before viral inoculation. In the treatment gr...
Legere RM, Taylor DR, Davis JL, Bello K, Parker C, Judd RL, Wooldridge AA.Chronic insulin dysregulation is challenging to manage with pharmaceuticals in horses. Pioglitazone improves insulin sensitivity in humans, and the pharmacokinetics of pioglitazone have been evaluated in horses. The objectives of this study were to assess the pharmacodynamic effects of oral pioglitazone on morphometric parameters, hepatic enzyme activity and function, adipokines, and enteroinsular response to oral sugar. A prospective pilot study was performed using fifteen adult equids (8 ponies, 7 horses) to evaluate the effects of short-term pioglitazone administration (2 mg/kg PO q 24 hou...
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...
Monk CS, Jeong SY, Gibson DJ, Plummer CE.Tetracyclines have activity against matrix metalloproteinases (MMP). Oral medications with effects on the ocular surface are of interest in patients where repeated topical dosing is limited. The aim of this study was to characterize the concentration of minocycline in the tears of normal horses after oral administration and to determine if this level directly inhibits MMP activity. Methods: Five healthy adult ponies were administered oral minocycline (Wedgewood Pharmacy; Swedesboro, NJ) at 4 mg/kg every 12 h for 5 days. Tears were collected at T = 2, 26, 50, 56, 74, 80, and 98 h. Tear minocycl...
Rendle DI, Doran G, Ireland J, Edwards S.Published information on the pharmacokinetic and pharmacodynamic properties of pergolide is limited. The aim of this study was to investigate the pharmacokinetic and pharmacodynamic properties of oral pergolide in horses with pituitary pars intermedia dysfunction (PPID). The study design was a nonrandomized clinical trial. Six horses with PPID diagnosed by thyrotropin-releasing hormone (TRH) stimulation tests received pergolide at 4 μg/kg for 18 d. Plasma samples for determination of pergolide and ACTH concentration were collected 0.5 h before and 2 and 12 h after each administration of p...
Sullivan M, Snow DH.The absorption of orally administered phenylbutazone (5 mg/kg) was studied in 10 thoroughbreds, eight ponies and four pony foals. Large variations in area under the curve (AUC) and peak plasma concentrations were found both within an animal and within groups of animals. Administration of phenylbutazone (5 mg/kg) following an overnight fast resulted in no difference among the three groups of animals with respect to AUC (0 to 24 hours), mean (+/- sd) values of which were 132 +/- 68, 107 +/- 48 and 98 +/- 6, respectively. Absorption characteristics of two oral phenylbutazone preparations (Equipal...
Colles CM.Twenty horses suffering from navicular disease were treated with warfarin given orally. The dosage was to effect, to give a 2 to 4 second prolongation of the one stage prothrombin time (OSPT). Dosage was initially at a rate of 0.018 mg/kg, changing the dose by amounts of 20 per cent until the required dose was achieved. Final dose rates varied from 0.012 mg/kg to 0.75 mg/kg. All the cases treated received warfarin daily throughout the trial. Seventeen of the animals became sound and the remaining 3 showed a marked improvement in their gait. The mean of the ages of the horses was 7.5 years, the...
Sanchez LC, Murray MJ, Merritt AM.To evaluate the efficacy of omeprazole paste, a commonly used antiulcer drug, on intragastric pH in clinically normal neonatal foals. Methods: 6 clinically normal foals between 5 and 14 days of age. Methods: Intragastric pH was recorded in each foal by use of a disposable antimony pH electrode with internal reference. Values for intragastric pH were recorded every 4 seconds by use of an ambulatory pH monitor. There were two 24-hour recordings of intragastric pH for each foal, with 24 hours between recordings. Foals were not administered any drugs during the first recording. Foals were administ...
Sampieri F, Schott HC, Hinchcliff KW, Geor RJ, Jose-Cunilleras E.There is no evidence that use of oral electrolyte pastes enhances performance in competing endurance horses. Objective: To ascertain whether oral administration of a high dose (HD) of sodium chloride (NaCl) and potassium chloride (KCl) to endurance horses would differentially increase water intake, attenuate bodyweight (bwt) loss and improve performance when compared to a low dose (LD). Methods: A randomised, blinded, crossover study was conducted on 8 horses participating in two 80 km rides (same course, 28 days apart). Thirty minutes before and at 40 km of the first ride 4, horses received o...
Soma LR, Rudy JA, Uboh CE, Xu F, Snapp HM.To investigate the pharmacokinetics and behavioral effects of aminorex administered IV and PO in horses. Methods: 7 Thoroughbreds. Methods: In a cross-over design, aminorex (0.03 mg/kg) was administered IV or PO. Plasma and urinary aminorex concentrations were determined via liquid chromatography- mass spectrometry. Results: Decrease of aminorex from plasma following IV administration was described by a 3-compartment pharmacokinetic model. Median (range) values of alpha, beta, and gamma half-lives were 0.04 (0.01 to 0.28), 2.30 (1.23 to 3.09), and 18.82 (8.13 to 46.64) hours, respectively. Tot...
Duncan JL, Reid JF.In a controlled trial in naturally-infected young ponies, oxfendazole administered orally at dose-rates of 10 mg per kg and 50 mg per kg resulted in complete elimination of Trichostrongylus axei, Parascaris equorum, Oxyuris equi and adult Strongylus vulgaris. Also, all migrating Strongylus edentatus larvae recovered from the subperitoneal tissues of the flank were found to be dead. Minimum efficiencies of 99.8 per cent and 99.1 per cent were obtained against adult small strongyles (Trichonema spp) and 97.6 per cent and 100 per cent of developing small strongyle larvae at dose-rates of 10 mg pe...
Knych HK, Arthur RM, Steinmetz S, McKemie DS.Ketoprofen (KTP) is currently only available as an injectable formulation for intravenous administration to horses. The primary goal of the study reported here was to characterize the pharmacokinetics of KTP, including determination of bioavailability following oral administration of the currently available injectable formulation as well as a paste formulation. KTP was administered intravenously and orally, and blood and urine samples were collected at various time points up to 96 h. KTP enantiomer concentrations were determined using LC–MS/MS, and pharmacokinetic analyses were performed. Me...
Schott HC, Axiak SM, Woody KA, Eberhart SW.To determine whether the composition of electrolyte pastes formulated for oral administration influences voluntary water intake (WI) by horses recovering from furosemide-induced dehydration. Methods: 6 horses. Methods: Voluntary WI, body weight, and blood and urine constituents were measured before and after induction of dehydration by furosemide administration and overnight withholding of water; these same variables also were measured during a 36-hour rehydration period. Each horse was evaluated 4 times with random application of 4 treatments (electrolyte pastes) that provided 0.5 g of KCl/kg...
