Pharmacokinetics in horses involves the study of how drugs are absorbed, distributed, metabolized, and excreted in equine species. This field of study provides insights into the time course of drug concentrations within the horse's body and helps in understanding the effects of various pharmaceuticals. Key parameters in equine pharmacokinetics include absorption rates, bioavailability, half-life, and clearance. These parameters can vary significantly due to factors such as age, breed, and health status of the horse. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetic profiles of different drugs in horses, aiming to optimize dosing regimens and improve therapeutic outcomes in equine medicine.
Javsicas LH, Sanchez LC.Administration of omeprazole paste per os to healthy neonatal foals has been shown to effectively increase intragastric pH, but has not been evaluated in sick neonatal foals. Objective: To determine the effect of orally administered omeprazole paste on intragastric pH in clinically ill neonatal foals requiring nasogastric intubation. Methods: Intragastric pH was measured continuously for 24 h using an indwelling electrode and continuous data recording system in hospitalised neonatal foals age < or =2 days. Intragastric pH was measured for 12 h prior to (pretreatment period) and 12 h followi...
Leise BS, Fugler LA, Stokes AM, Eades SC, Moore RM.To determine the magnitude and duration of effects of acepromazine administered intramuscularly (IM) on digital and systemic hemodynamic variables in clinically healthy horses. Methods: Experimental study. Methods: Healthy adult horses (n=12). Methods- An ultrasonic Doppler flow probe was surgically implanted around the medial palmar digital artery before the study. Catheters were inserted in the transverse facial artery, lateral palmar digital artery, and jugular vein. A treatment group (n=6) was administered 0.04 mg/kg body weight of acepromazine IM; control horses (n=6) were administered an...
Dunkel B, Rickards KJ, Page CP, Cunningham FM.To determine the phosphodiesterase (PDE) isoenzymes in equine platelets and evaluate their influence on platelet adhesion. Methods: Platelets obtained from healthy New Forest Pony geldings that ranged from 12 to 20 years of age (mean +/- SEM, 17.3 +/- 1.1 years). Methods: PDE isoenzyme activity in equine platelets was determined by use of a 2-step radioactive assay. Functional importance of PDE isoenzymes was established by use of selective inhibitors in a colorimetric adhesion assay. Results: PDE1, PDE2, PDE3, and PDE5 and small amounts of PDE4 were found in equine platelets. Inhibition of PD...
Giguère S, Sanchez LC, Shih A, Szabo NJ, Womble AY, Robertson SA.To determine and compare the effects of caffeine and doxapram on cardiorespiratory variables in foals during isoflurane-induced respiratory acidosis. Methods: 6 clinically normal foals (1 to 3 days old). Methods: At intervals of > or = 24 hours, foals received each of 3 IV treatments while in a steady state of hypercapnia induced by isoflurane anesthesia (mean +/- SD, 1.4 +/- 0.3% endtidal isoflurane concentration). After assessment of baseline cardiorespiratory variables, a low dose of the treatment was administered and variables were reassessed; a high dose was then administered, and vari...
Hendrix DV, Stuffle JL, Cox SK.To evaluate the pharmacokinetics of topically applied ciprofloxacin 0.3% ophthalmic solution in tears of healthy horses. Methods: Twenty healthy, adult, mixed-breed horses. Methods: Twenty study horses were confirmed free of ophthalmic disease by complete ophthalmic examination. Seventy microliters of 0.3% ciprofloxacin (Ciloxan) was placed in the ventral cul-de-sac of each eye using a microliter syringe and 19-g cannula. Population kinetics were carried out by sampling the tear film from the lower cul-de-sac of each eye with tear test strips at 5, 10, 15 and 30 min and 1, 2, 4 and 6 h post ad...
Sanchez LC, Robertson SA, Maxwell LK, Zientek K, Cole C.Transdermal fentanyl is used clinically in horses based on pharmacokinetic data and antinociceptive effects documented in other species. Objective: Fentanyl IV administration increases both visceral and somatic nociceptive threshold in conscious horses. Methods: Six clinically normal horses, each fitted with a permanent gastric cannula. Methods: Visceral nociception was evaluated with 2 methods of threshold detection--olorectal distention and duodenal distention. Somatic nociception was assessed by measurement of thermal threshold. Fentanyl was administered as an increasing stepwise infusion f...
Nannarone S, Gialletti R, Veschini I, Bufalari A, Moriconi F.Alpha-2 agonists are synthetic drugs which cause sedation, analgesia and myorelaxation due to their interaction with alpha-2 adrenoreceptors, widely distributed throughout bodily systems. Because of these actions such drugs are generally used in veterinary practice: to tranquilize animals (pharmacologic restraint) for the safety of both veterinar-ians and cooperators. Such properties facilitate diagnostic examinations or minimally in-vasive and poorly painful surgical procedures, as well as limiting stress factors to the patients. The aim of this study is to find out the minor dosage able to m...
Martens RJ, Mealey K, Cohen ND, Harrington JR, Chaffin MK, Taylor RJ, Bernstein LR.To determine the pharmacokinetics of gallium maltolate (GaM) after intragastric administration in healthy foals. Methods: 6 healthy neonatal foals. Methods: Each foal received GaM (20 mg/kg) by intragastric administration. Blood samples were obtained before (time 0) and at 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, and 48 hours after GaM administration for determination of serum gallium concentrations by use of inductively coupled plasma mass spectroscopy. Results: Mean +/- SD pharmacokinetic variables were as follows: peak serum gallium concentration, 1,079 +/- 311 ng/mL; time to peak serum concentra...
Colitz CM, Latimer FG, Cheng H, Chan KK, Reed SM, Pennick GJ.To determine the pharmacokinetics of voriconazole following IV and PO administration and assess the distribution of voriconazole into body fluids following repeated PO administration in horses. Methods: 6 clinically normal adult horses. Methods: All horses received voriconazole (10 mg/kg) IV and PO (2-week interval between treatments). Plasma voriconazole concentrations were determined prior to and at intervals following administration. Subsequently, voriconazole was administered PO (3 mg/kg) twice daily for 10 days to all horses; plasma, synovial fluid, CSF, urine, and preocular tear film con...
Xu Y, Jia Z, Zhou L, Wang L, Li J, Liang Y, Zhao T, Ni B, Wu Y.To warrant potential clinical testing, the equine anti-SARS-CoV F(ab')(2) requires evaluation in as many animal models as possible and a safety test in a primate model. In this study, we evaluated the pharmacokinetics, tolerance and immunity of this kind of antibody in macaques and rats. Results showed that the F(ab')(2) fragments had a normal metabolism in injected animals. The general physiological indexes did not differ between animals injected with anti-SARS-CoV F(ab')(2) or saline. However, a mild inflammatory response in local injection site and a moderate immune response against this an...
Derossi R, Medeiros U, de Almeida RG, Righetto FR, Frazílio FO.The aim of the study was to evaluate and compare the effects of caudal epidural administration of meperidine (MP), lidocaine (LD), and a combination of the two (MPLD) in six mature saddle horses. Horses were randomly assigned to receive three treatments (MP 0.3 mg/kg; LD 0.2 mg/kg; and MPLD: MP 0.3 mg/kg and LD 0.2 mg/kg), with at least 1 week between treatments. Drugs were injected into the epidural space between the first and second coccygeal areas in conscious standing horses. Analgesia, ataxia, sedation, cardiovascular and respiratory effects, and rectal temperature were recorded at differ...
Beaudry F, Vachon P.Glucosamine is an amino sugar involved in the biosynthesis of glycosylated proteins and lipids. Recently, with increased public interest in natural products medicine, glucosamine has been widely used to treat osteoarthritis, even though demonstrations of its actual efficacy remain relatively unknown. Information related to the pharmcokinetics of glucosamine is sparse. A recent analytical method published used 13C-glucosamine as an internal standard to analyse study samples. The method lacked accuracy owing to an important natural isotopic contribution of glucosamine to 13C-glucosamine ion abun...
Garré B, Shebany K, Gryspeerdt A, Baert K, van der Meulen K, Nauwynck H, Deprez P, De Backer P, Croubels S.The purpose of this study was twofold. The first aim was to evaluate the oral bioavailability and pharmacokinetics (PKs) of acyclovir in horses after intravenous (i.v.) administration and after oral administration of acyclovir and its prodrug, valacyclovir. Second, we aimed to combine these PK data with pharmacodynamic (PD) information, i.e., 50% effective concentrations (EC(50) values) from in vitro studies, to design an optimal dosage schedule. Three treatments were administered to healthy adult horses: 10 mg of acyclovir/kg of body weight delivered as an i.v. infusion over 1 h, 20 mg of acy...
Gasthuys F, Pockelé K, Vervaet C, Weyenberg W, De Prijck K, Pille F, Vlaminck L, Nelis H, Remon JP.The in vivo behaviour of 5% gentamicin sulphate ocular mini-tablets (2-mm diameter, 6.525 mg weight) was compared with gentamicin eye drops in six ponies. Two mini-tablets were inserted on the bulbar conjunctiva of the right eye while a similar dose of gentamicin was administered via eye drops in the left eye. Irritation induced by the mini-tablets and the eye drops was evaluated using a visual analogue scale (0-10). Tears were sampled with ophthalmologic absorption triangles for 1 min for the determination of the concentration of gentamicin sulphate using a microbiological plate diffusion met...
Sun WC, Moore JN, Hurley DJ, Vandenplas ML, Linden JM, Murray TF.To evaluate anti-inflammatory effects of several novel adenosine receptor agonists and to determine their specificity for various adenosine receptor subtypes on neutrophils, cells heterologously expressing equine adenosine receptors, or equine brain membranes. Methods: Neutrophils isolated from 8 healthy horses. Methods: Radioligand binding experiments were performed to compare binding affinities of adenosine receptor agonists to equine adenosine A(1), A(2A), and A(3) receptor subtypes. Effects of these agonists on endotoxin-induced production of reactive oxygen species (ROS) by equine neutrop...
Ross J, Dallap BL, Dolente BA, Sweeney RW.To determine the pharmacokinetics and pharmacodynamics of epsilon-aminocaproic acid (EACA), including the effects of EACA on coagulation and fibrinolysis in healthy horses. Methods: 6 adult horses. Methods: Each horse received 3.5 mg of EACA/kg/min for 20 minutes, i.v. Plasma EACA concentration was measured before (time 0), during, and after infusion. Coagulation variables and plasma alpha(2)-antiplasmin activity were evaluated at time 0 and 4 hours after infusion; viscoelastic properties of clot formation were assessed at time 0 and 0.5, 1, and 4 hours after infusion. Plasma concentration ver...
Bliss G.The Department of Pharmacology at the North Carolina State University College of Veterinary Medicine is currently conducting stability studies of oral suspensions of pergolide for the treatment of Cushing's disease. While those results are not available at this time, this paper summarizes the results of a literature search on possible clinical treatments for equine Cushing's and is intended to provide insight into the pathophysiology of the disease. Pharmacological options for treatment of equine Cushing's are discussed.
De Clercq D, van Loon G, Baert K, Tavernier R, Croubels S, De Backer P, Deprez P.Good results have been obtained with a human amiodarone (AD) i.v. protocol in horses with chronic atrial fibrillation (AF) and a pharmacokinetic study is required for a specific i.v. amiodarone treatment protocol for horses. Objective: To study the efficacy of this pharmacokinetic based i.v. AD protocol in horses with chronic AF. Methods: Six horses with chronic AF were treated with an adapted AD infusion protocol. The protocol consisted of 2 phases with a loading dose followed by a maintenance infusion. In the first phase, horses received an infusion of 6.52 mg AD/kg bwt/h for 1 h followed by...
Schauvliege S, Van den Eede A, Duchateau L, Gasthuys F.Enoximone is a phosphodiesterase III inhibitor frequently used to improve cardiac output (CO) in man. As the use of enoximone has not been reported in horses, the effects of this inodilator were examined in isoflurane anaesthetized ponies. Methods: Prospective, randomised, experimental study. Methods: Six healthy ponies, weighing 286 (212-367) +/- 52 kg, aged 5.0 +/- 1.6 years (4-6.5). Methods: After sedation with romifidine [80 microg kg(-1) intravenously (IV)], general anaesthesia was induced with midazolam (0.06 mg kg(-1) IV) and ketamine (2.2 mg kg(-1) IV) and maintained with isoflurane in...
Bidwell LA, Wilson DV, Caron JP.To measure concentrations of lidocaine serum after application of two 5% patches on horses. Methods: Prospective experimental trial Methods: Six client-owned, systemically healthy horses. Methods: The hair was clipped on the medial aspect above the carpus of both fore limbs and 2 patches of 5% lidocaine were applied within 30 minutes of jugular catheter placement and the area was then bandaged. Venous blood was drawn from a jugular vein catheter that was inserted using lidocaine as a local block. Samples were drawn immediately before and at 2, 4, 6, 8, and 12 hours after patch application. The...
Williams CA, Lamprecht ED.Most herbs and functional foods have not been scientifically tested; this is especially true for the horse. This paper reviews some of the literature pertinent to herbal supplementation in horses and other species. Common supplements like Echinacea, garlic, ginger, ginseng, and yucca are not regulated, and few studies have investigated safe, efficacious doses. Ginseng has been found to exert an inhibitory effect on pro-inflammatory cytokines and cyclooxygenase-2 expression. Equine studies have tested the anti-inflammatory effects of a single dose of ginger, post-exercise. Echinacea has been re...
Casini A, Mastrobuoni G, Terenghi M, Gabbiani C, Monzani E, Moneti G, Casella L, Messori L.The interactions with protein targets of the ruthenium(III) complex imidazolium trans-[tetrachloro(dimethyl sulfoxide)(imidazole)ruthenate(III)], NAMI-A, an effective anticancer and antimetastatic agent now in clinical trials, deserve great attention as they are believed to be at the basis of the mechanism of action of this innovative molecule. Here, we report on the reactions of NAMI-A with two well-known model proteins, namely, hen egg white lysozyme and horse heart cytochrome c; these reactions were investigated by a variety of physicochemical methods, including optical spectroscopy, (1)H N...
Lowden S, Gray S, Dawson K.The horse biting louse (Werneckiella equi) is a common global equine ectoparasite. To our knowledge, benzoyl(phenyl)urea insecticides (triflumuron, diflubenzuron) commonly used as sheep lousicides, have not been evaluated for efficacy against W. equi. The aim of this study was to determine louse control efficacy, general wellness and dermal safety following triflumuron application as a backline pour-on to horses. Two efficacy trials using 25 adult naturally infested lousy horses, and a dermal safety trial using 10 adult louse-free horses were conducted over a 14-month period. Lousy animals wer...
González F, Rodríguez C, De Lucas JJ, Waxman S, San Andrés MD, Serres C, Nieto J, San Andrés MI.Six donkeys each received 2 mg/kg marbofloxacin as a 10 per cent aqueous solution administered intravenously. Principal pharmacokinetic parameters were determined and two efficacy indices were computed by using pharmacokinetic parameters and selected mic90 values of marbofloxacin against pathogenic equine strains to predict the efficacy of the drug at this dose. The pharmacokinetics of marbofloxacin in donkeys was characterised by a large mean volume of distribution at a steady state (1.15 [0.09] l/kg) and a long mean (sd) elimination half-life of 9.24 (1.96) hours. It was also characterised b...
Bertone JJ.The nature of the equine industry and equine veterinary medicine often requires veterinarians to prescribe drugs with little evidence for a drug's formulation safety or efficacy, or even assurance of the chemistry of the drug used. This means that equine veterinarians must remain skeptics and understand the limitations in their ability to attribute safety and efficacy to a particular drug or treatment. An evidence-based approach to pharmacology demands rigorous testing and an unbiased analysis of results.
Hubenov H, Bakalov D, Krastev S, Yanev S, Haritova A, Lashev L.The objective of the study was to evaluate the pharmacokinetics of tobramycin in plasma and urine in the horse (n = 7) after intravenous administration of a dose of 4 mg/kg b.w. Plasma tobramycin concentrations were assayed microbiologically and by means of HPLC analyses. Pharmacokinetic parameters, calculated on the basis of concentrations determined with the microbiological assay were not statistically different from those obtained when data from HPLC analysis were used, but the microbiological assay was more sensitive in the detection of low plasma and urine values. The values of the total ...
Minguet G, Franck T, Joris J, Ceusters J, Mouithys-Mickalad A, Serteyn D, Sandersen C.Volatile anaesthestics have shown to modulate the oxidative response of polymorphonuclear neutrophils (PMNs). We investigated the effects of isoflurane and sevoflurane on the degranulation of total and active myeloperoxidase (MPO) from horse PMNs and their direct interaction with MPO activity. Whole blood from horse was incubated in 1 and 2 minimal alveolar concentrations (MAC) of isoflurane or sevoflurane for 1h and PMNs were stimulated with cytochalasin B (CB) plus N-formyl-méthionyl-leucyl-phenylalanine (fMLP). After stimulation, the plasma was collected to measure total and active MPO by ...
Moorman VJ, Pezzanite LM, Griffenhagen GM.To compare the efficacy and duration of action for perineural analgesia with liposomal bupivacaine (LB) versus bupivacaine hydrochloride (BHCl) in a sole-pressure induced model of forelimb lameness in horses. Methods: 6 healthy adult research horses. Methods: In 1 randomly assigned forelimb, grade 3/5 lameness was induced by use of a sole-pressure lameness model. Objective lameness (vector sum [VS]) was determined with an inertial sensor system at 0, 1, 6, and 24 hours after lameness induction to evaluate the model. Mechanical nociceptive thresholds (MNTs) and objective lameness (VS and force ...
Giorgi M, De Vito V, Poapolathep A, Rychshanova R, Sgorbini M, Owen H.Flupirtine (FLU) is a non-opioid analgesic drug, with no antipyretic or anti-inflammatory effects, used in the treatment of a wide range of pain states in human beings. It does not induce the side effects associated with the classical drugs used as pain relievers. The aim of this study was to evaluate the pharmacokinetic profiles of FLU after IV and PO administration in healthy horses. Six mixed breed adult mares were randomly assigned to two treatment groups using an open, single-dose, two-treatment, two-phase, paired, cross-over design (2 × 2 Latin-square). Group 1 (n = 3) received ...
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, ...
Edwards-Milewski ML, Morello SL, Zhao Q, Mattan-Bell C.To compare the gross and histological effects of intravenous regional limb perfusion (IVRLP) using amikacin sulfate on second intention healing of distal limb wounds in adult horses with healing in untreated wounds. Methods: In vivo experimental study. Methods: Adult horses (n = 7). Methods: Two full thickness wounds (2.5 × 2.5 cm) were created aseptically on the dorsal aspect of each metacarpus and maintained under sterile bandages. One forelimb was randomly selected from each horse for IVRLP on days 2, 3, and 4 post-wounding. Sequential biopsies were taken from 1 wound on each limb to evalu...
Brosnan RJ, Steffey EP, Escobar A, Palazoglu M, Fiehn O.To evaluate whether guaifenesin can prevent adverse anesthetic induction events caused by propofol and whether a guaifenesin-propofol induction combination has brief cardiovascular effects commensurate with rapid drug washout. Methods: 8 healthy adult horses. Methods: Guaifenesin was administered IV for 3 minutes followed by IV injection of a bolus of propofol (2 mg/kg). Additional propofol was administered if purposeful movement was detected. Anesthesia was maintained for 2 hours with isoflurane or sevoflurane at 1.2 times the minimum alveolar concentration with controlled normocapnic ventila...
Marsh MV, Caldwell J, Sloan TP, Smith RL, Horner M, Moss MS.14C-Fenclofenac (2-(2'-4'-dichlorophenoxy)-phenylacetic acid) was administered orally to horses, and urinary metabolites investigated by chromatography. Fenclofenac was rapidly absorbed and eliminated, with a plasma half-life (t1/2) of 2.3 h, with 83.2 and 85.8% of the dose being recovered in the urine in 0-24 h. The major urinary metabolite was the ester glucuronide (58.8, 70.0% dose), and evidence is presented that this metabolite undergoes a structural rearrangement to give beta-glucuronidase-resistant isomers. The other 14C-labelled components in horse urine were unchanged fenclofenac (13....
Hubbell JA, Muir WW, Gaynor JS.Six horses scheduled for euthanasia were instrumented for the measurement of blood flow by thermodilution, pulmonary arterial, right atrial and arterial blood pressures and collection of arterial blood for pH and blood gas analysis. The horses were anaesthetised with intravenous (iv) thiamylal sodium (10 mg/kg) and placed in right lateral recumbency. After euthanasia with an overdose of pentobarbitone sodium (100 mg/kg, iv) and loss of the electrocardiogram and arterial pulse pressure, thoracic compression at rates of 40, 60 and 80 compressions/min was instituted. Thoracic compression was acco...
Wang J, Qiu J, Xiao H, Gong X, Sun P, Li J, Zhang S, Cao X.The pharmacokinetic properties of three formulations of vitacoxib were investigated in horses. To describe plasma concentrations and characterize the pharmacokinetics, 6 healthy adult Chinese Mongolian horses were administered a single dose of 0.1 mg/kg bodyweight intravenous (i.v.), oral paste, or oral tablet vitacoxib in a 3-way, randomized, parallel design. Blood samples were collected prior to and at various times up to 72 hr postadministration. Plasma vitacoxib concentrations were quantified using UPLC-MS/MS, and pharmacokinetic parameters were calculated using noncompartmental analysis...
Tappenbeck K, Hoppe S, Geburek F, Feige K, Huber K.By blocking the enteric nervous system (ENS) using tetrodotoxin (TTX), previous studies have documented the contractility-enhancing (CE) effects of lidocaine in equine intestinal smooth muscle (SM) at the level of SM cells and/or interstitial cells of Cajal (ICC). The present study examined the impact of ENS deactivation on CE lidocaine effects, and investigated the effects of lidocaine on ENS activity. TTX application did not affect the CE effects of lidocaine, indicating that these were not mediated by TTX-sensitive sodium channels. Application of TTX or ≥100 mg/L lidocaine reduced ENS a...
Gustafsson K, Tatz AJ, Dahan R, Abu Ahmad W, Britzi M, Sutton GA, Kelmer G.The aim of this study was to investigate the safety and pharmacokinetics of trimethoprim-sulphadiazine administered via intravenous regional limb perfusion (IVRLP) into the cephalic vein. According to the hypothesis, the drug could be administered without adverse effects and the synovial concentrations would remain above the minimum inhibitory concentration (MIC) for trimethoprim-sulphadiazine (0.5 and 9.5 µg/mL) for 24 h. Ten ( = 10) horses underwent cephalic vein IVRLP with an Esmarch tourniquet applied for 30 min. Four grams (4 g) of trimethoprim-sulphadiazine (TMP-SDZ) were diluted at 0.9...
Pérez R, Godoy C, Palma C, Muñoz L, Arboix M, Alvinerie M.A study was done to compare plasma disposition kinetics and the fecal elimination profile of doramectin (DRM) after oral or intramuscular (IM) administration in horses. Ten clinically healthy horses, 328-502 kg body weight (bw), were assigned to 2 experimental groups of 5 horses each. Group 1 was treated with an oral dose of 0.2 mg DRM/kg bw, while Group 2 was treated with 0.2 mg DRM/kg bw by IM route. Blood and fecal samples were collected at different times between 0.5h and 60 days post-treatment. After plasma and fecal drug extraction and derivatization, samples were analysed by high perfor...
Jensen RC, Fischer JH, Cwik MJ.The effect of age and training status on the pharmacokinetics of flunixin meglumine was evaluated in 16 Thoroughbreds. Horses were assigned to 1 of 3 groups on the basis of age and training status: group A (n = 6), horses in active training and less than or equal to 5 years old; group B (n = 5), horses out of training for a minimum of 6 weeks and less than or equal to 5 years old; and group C (n = 5), horses out of training for at least 2 years and greater than or equal to 9 years old. After administration of 500 mg of flunixin meglumine IV, multiple serum and urine samples were obtained over ...
Patel T, Magdesian KG, Estell KE, Edman JM, Knych HK.Chloramphenicol is commonly used in horses; however, there are no studies evaluating the pharmacokinetics of veterinary canine-approved tablets. Studies using different formulations and earlier analytical techniques led to concerns over low bioavailability in horses. Safety concerns about human health have led many veterinarians to prescribe compounded formulations that are already in suspension or paste form. The objective of this study was to evaluate the pharmacokinetics of approved chloramphenicol tablets in horses, along with compounded preparations. The hypothesis was that chloramphenico...
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...
Park SC, Yun HI.The pharmacokinetic properties of norfloxacin-glycine acetate (NFLXGA) were determined in six horses following a single intravenous (i.v.) and intramuscular (i.m.) dose of 4 mgkg(-1) body weight. Following i.v. and i.m. administration, the plasma drug concentrations were best fitted by an open two-compartment model with a rapid distribution phase. After i.v. NFLXGA administration, the distribution (t(1/2alpha)) and elimination half-life (t(1/2beta)) were 0.42 (0.05) and 5.44 (1.36)h. The volume of distribution of NFLXGA at steady state (Vd(ss)) was 2.19 (0.53) Lkg(-1). After NFLXGA i.m. admini...
Breuhaus BA, DeGraves FJ, Honore EK, Papich MG.To determine pharmacokinetics of ibuprofen in healthy foals and to determine clinical effects after oral administration for 6 days. Methods: 7 healthy 5- to 10-week-old foals. Methods: Serum concentrations of ibuprofen were measured after IV and oral (nasogastric tube) administration at dosages of 10 and 25 mg/kg of body weight. Foals were given ibuprofen (25 mg/kg, PO, q 8 h) as a paste for 6 days. Serum and urine were obtained before and after the 6-day period. Results: Half-life of elimination (Kel t1/2) of IV-administered ibuprofen (ie, 10 and 25 mg/kg), was 79 and 108 minutes, maximal ser...
Steffey EP, Woliner MJ, Puschner B, Galey FD.To quantitate the effects of desflurane and mode of ventilation on cardiovascular and respiratory functions and identify changes in selected clinicopathologic variables and serum fluoride values associated with desflurane anesthesia in horses. Methods: 6 healthy adult horses. Methods: Horses were anesthetized on 2 occasions: first, to determine the minimum alveolar concentration (MAC) of desflurane in O2 and second, to characterize cardiopulmonary and clinicopathologic responses to 1X, 1.5X, and 1.75X desflurane MAC during both controlled and spontaneous ventilation. Results: Mean +/- SEM MAC ...
Van Hoogmoed LM.Intestinal stasis or ileus is a significant cause of mortality and morbidity in horses and has been attributed to a variety of causes, including loss of intrinsic or extrinsic electrical activity, incoordination of contractile activity from regional stimuli, and dissociation between electrical and mechanical activity. Proposed mechanisms include systemic shock, electrolyte disturbances, persistent luminal distention, ischemia, inflammation, peritonitis, endotoxemia, and anesthesia. Because the cause of ileus is likely multifactorial, a variety of pharmaceutics have been used to target specific...
Kelmer G, Martin-Jimenez T, Saxton AM, Catasus C, Elliot SB, Lakritz J.There are no reported studies evaluating the use of erythromycin for regional limb perfusion (RLP) in horses. Our hypothesis was that using the cephalic and saphenous veins for RLP will enable delivery of therapeutic concentrations of erythromycin to the distal limb. Nineteen healthy horses participated in the study. The cephalic, saphenous or palmar digital (PD) vein was used to perfuse the limb with erythromycin. Synovial samples were collected from the metacarpo/metatarso-phalangeal (MCP/MTP) joint and blood samples were collected from the jugular vein. Maximum concentration (C(max)) of ery...
Haven ML, Dave K, Burrow JA, Merritt AM, Harris D, Zhang D, Hickey GJ.The antisecretory activity of omeprazole on gastric acid when administered i.v., intragastrically or per os, was evaluated in 2 female and 3 castrated male horses. Each horse had been prepared with a chronic indwelling gastric cannula. A single i.v. administration of omeprazole (1.5 mg/kg bwt) was effective in abolishing basal and pentagastrin (PG)-stimulated acid secretion. Once daily, nasogastric administration of omeprazole in acid-stable granules for 5 days inhibited acid secretion in a dose-dependent manner: 57% (1.5 mg/kg bwt) and 98% (5.0 mg/kg bwt) reduction of PG-stimulated acid secre...
Wyse CA, Murphy DM, Preston T, Morrison DJ, Love S.The aim of this study was to assess the feasibility of applying the 13C-octanoic acid breath test for assessment of gastric emptying in ponies by investigating the pattern of 13C enrichment in breath following the administration of a test meal +/- 13C-octanoic acid. After a 14 h fast, the ponies received either no meal (Test I) or a standardised test meal labelled with 0 mg (Test II), 125 mg (Test III), 250 mg (Test IV) or 500 mg (Test V) 13C-octanoic acid. For each test (I-V), exhaled breath samples were collected in duplicate at 1 h and immediately before ingestion of the test meal and at fr...
Estell KE, Knych HK, Patel T, Edman JM, Magdesian KG.To the authors' knowledge, there have been no studies evaluating the pharmacokinetics of chloramphenicol administered orally to horses at the currently recommended dose of 50 mg/kg PO q6 h for multiple days. The published antimicrobial susceptibility breakpoint is 8.0 ug/mL; it is unknown if this concentration is achievable at the recommended dose rate in horses. The aim of this prospective multi-dose pharmacokinetic study was to perform pharmacokinetic analysis of chloramphenicol after multiple doses. The authors hypothesize that the antimicrobial susceptibility breakpoint will not be reached...
Castro-Cuellar G, Cremer J, Queiroz-Williams P, Knych HK, Leise BS.The objective of this study was to describe the pharmacokinetics of intra-articular (IA) administered buprenorphine in horses with lipopolysaccharide (LPS)-induced synovitis. Radiocarpal synovitis was induced in six healthy adult horses with the IA injection of LPS (0.5 ng/joint) on two occasions in a randomized cross-over design. Treatments (IA buprenorphine (IAB) at 5 μg/kg plus intravenous saline; and intravenous buprenorphine (IVB) at 5 μg/kg plus IA saline) were administered 4 h following LPS injection. Concentrations of buprenorphine were assessed in plasma and synovial fluid (SF) ...
Errecalde JO, Button C, Baggot JD, Mulders MS.The pharmacokinetics and bioavailability of theophylline in horses were investigated following both intravenous and intragastric administration of aminophylline solutions at doses corresponding to 15 and 10 mg/kg theophylline base. A rapid distributive phase with a half-life of approximately 15-30 min was followed by a slower elimination half-life averaging 15-17 h. The apparent volume of distribution averaged 850-900 ml/kg. Theophylline, administered as aminophylline solution, was both rapidly and completely absorbed from the equine digestive tract. Based on the bioavailability and dispositio...
Brainard BM, Epstein KL, LoBato D, Kwon S, Papich MG, Moore JN.Critically ill horses are susceptible to thrombotic disease, which might be related to increased platelet reactivity and activation. Objective: To compare the effect of oral clopidogrel and aspirin (ASA) on equine platelet function. Methods: Six healthy adult horses. Methods: Horses received clopidogrel (2 mg/kg p.o. q24h) or ASA (5 mg/kg p.o. q24h) for 5 days in a prospective randomized cross-over design. Platelet aggregation responses to adenosine diphosphate (ADP) and collagen via optical aggregometry, and platelet secretion of serotonin (5HT) and production of thromboxane B(2) (TXB(2) ) by...
Lawless SP, Moorman VJ, Hendrickson DA, Mama KR.To compare efficacy and safety of a continuous rate infusion of detomidine hydrochloride and romifidine hydrochloride for standing elective bilateral laparoscopic ovariectomy in mares. Methods: Blinded, randomized prospective clinical study. Methods: Eighteen healthy mares presenting for elective bilateral ovariectomy METHODS: Mares were randomly assigned to one of two sedation protocols. Prior to surgery, baseline head height, heart rate, respiratory rate, and postural sway were recorded. An IV loading dose of α2-agonist (46 μg/kg romifidine or 13.9 μg/kg detomidine) was administered. S...
Orsini JA, Moate PJ, Engiles J, Norman T, Poppenga R, Benson CE, Boston RC.Cefotaxime powder was diluted with sterile water to a concentration of 100 mg/mL. The volume of solution was adjusted for each experimental horse to provide a total dose of 15, 20, and 25 mg/kg and was administered by infusion through a jugular vein catheter over a 10-min period. All three doses were administered to each of the six experimental horses at three different times. Cefotaxime concentrations in plasma and synovial fluid samples were measured by high-performance liquid chromatography (HPLC). Standard compartmental analysis techniques and the WinSAAM modeling program were used to dete...
Derossi R, Miguel GL, Frazílio FO, Nunes DB, Kassab TA.Bupivacaine is available as a racemic mixture of its enantiomers, d-bupivacaine and l-bupivacaine (LB). The aim of this randomized, double-blind study was to investigate the clinical efficacy and safety of S(-)-bupivacaine compared with standard racemic bupivacaine (RB) in horses under caudal epidural analgesia. Two treatments were administered to each horse, with a 2-week interval between subsequent treatments. Treatment 1 consisted of 0.5% LB at a dose of 0.06 mg/kg of body weight, and treatment 2 consisted of 0.5% RB at a dose of 0.06 mg/kg of body weight. Epidural injections were given in ...
Littlewood JD, Rose JF, Paterson S.A single blind controlled clinical trial of oral ivermectin paste at a dose rate of 0.1 mg/kg daily for seven days for the treatment of chorioptic mange in horses was carried out. There was a statistically significant reduction in the numbers of mites in the samples taken from the treated horses compared with the untreated horses, but the mites were not eliminated from all the treated animals. Two further groups of horses were treated, one at a dose rate of 0.1 mg/kg daily for 10 days and the other with two doses of 0.2 mg/kg given two weeks apart. There were no statistically significant diffe...
