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.
Johnson LM, Holcombe SJ, Shearer TR, Watson V, Gandy J, Southwood LL, Lynch TM, Schroeder EL, Fogle CA, Sordillo LM.Identifying therapies that mitigate ischemic colonic injury and improve mucosal healing and intestinal viability are crucial to improving survival in horses with ≥360° large colon volvulus (LCV). Ethyl pyruvate is the ethyl ester of pyruvate with diverse pharmacologic effects that limit ischemic injury and hasten intestinal mucosal repair in preclinical rodents, sheep and swine models. The objective of this study was to determine the effects of ethyl pyruvate on systemic indices of colon viability, expression of inflammatory genes in whole blood, morbidity and survival after surgical correc...
Knych HK, Arthur RM, McKemie DS, Baden RW, Seminoff K, Kass PH.Flunixin meglumine (FM) and phenylbutazone (PBZ) are potent anti-inflammatory agents and as such their potential to mask injuries that would otherwise keep a horse from training or racing is concerning. A common practice in racetrack medicine in the USA is to administer the two drugs within close proximity (24 hours apart) of each other, raising the concern of pharmacokinetic interactions and enhanced anti-inflammatory effects. Objective: Describe the pharmacokinetics and effects of PBZ on the clearance of FM when administered in close proximity as well as effects on inflammatory mediators. M...
Furr M, Kennedy T.Ponazuril is used for the treatment of equine protozoal myeloencephalitis (EPM). Coadministration of ponazuril with oil could result in higher serum and cerebrospinal fluid (CSF) concentrations of ponazuril. Objective: Coadministration of corn oil will result in higher serum and CSF concentrations of ponazuril than when ponazuril is administered alone. Methods: Ten resident university-owned adult horses of either sex and >2 years of age. Methods: Cohort study. Ponazuril oral paste (5 mg/kg BW; ponazuril treatment group (PON); n = 5), or ponazuril oral paste (5 mg/kg BW; ponazuril and oil tre...
Mora-Pereira M, Abarca EM, Duran S, Ravis W, McMullen RJ, Fischer BM, Lee YP, Wooldridge AA.Keratomycosis is a relatively common, sight threatening condition in horses, where treatment is often prolonged and costly. Subconjunctival (SCo) injections offer less resistance to drug diffusion than the topical route, resulting in better penetration to the ocular anterior segment. Voriconazole, a second generation triazole antifungal, is effective against common fungal organisms causing keratomycosis. If combined with a thermogel biomaterial, voriconazole can be easily injected in the SCo space to provide sustained drug release. The purpose of this study was to evaluate the drug concentrati...
Martins FC, Keating SC, Clark-Price SC, Schaeffer DJ, Lascola KM, DiMaio Knych H.To determine the physiologic and behavioral effects and pharmacokinetic profile of hydromorphone administered intravenously (IV) to horses. Methods: Prospective, randomized, crossover study. Methods: A group of six adult healthy horses weighing 585.2 ± 58.7 kg. Methods: Each horse was administered IV hydromorphone (0.025 mg kg; treatment H0.025), hydromorphone (0.05 mg kg; treatment H0.05) or 0.9% saline in random order with a 7 day washout period. For each treatment, physiologic, hematologic, abdominal borborygmi scores and behavioral data were recorded over 5 hours and fecal output was tota...
Ishii H, Obara T, Kijima-Suda I.Paracetamol is used widely as an over-the-counter analgesic and antipyretic medication for humans, but not for Japanese racehorses. Paracetamol can be an environmental substance, and is found together with its two isomers, metacetamol and orthocetamol, in equine urine. However, the sources and routes of paracetamol exposure remain unclear. To control the misuse of paracetamol, it is appropriate to establish residue limits for paracetamol to differentiate the administration of paracetamol from its environmental levels. In this study, we developed and validated a quantitative method for paraceta...
Rostang A, Desjardins I, Espana B, Panzuti P, Berny P, Prouillac C, Pin D.This study aimed to investigate both the pharmacokinetic behavior and tolerance of methotrexate (MTX) in horses to design a specific dosing regimen as a new immunomodulatory drug for long-term treatment. To determine the primary plasma pharmacokinetic variables after single intravenous, subcutaneous or oral administration, six horses were administered 0.3 mg/kg MTX in a crossover design study. After a 10-week washout, MTX was administered subcutaneously to three of the six previously treated horses at a dose of 0.3 mg/kg once per week for 3 months. In both studies, MTX and metabolite concen...
Verhaar N, Pfarrer C, Neudeck S, König K, Rohn K, Twele L, Kästner S.Pharmacological preconditioning of dexmedetomidine on small intestinal ischaemia/reperfusion injury has been reported in different animal models including horses. Objective: The objective was to assess if xylazine and lidocaine have a preconditioning effect in an experimental model of equine jejunal ischaemia. Methods: Terminal in vivo experiment. Methods: Ten horses under general anaesthesia were either preconditioned with xylazine (group X; n = 5) or lidocaine (group L; n = 5). A historical untreated control group (group C; n = 5) was used for comparison. An established experimental mo...
Crandall A, Hopster K, Grove A, Levine D.In horses undergoing castration, direct comparison of intratesticular lidocaine vs mepivacaine as analgesic adjuncts has not yet been analysed. Objective: To compare the effects of intratesticular lidocaine and mepivacaine during equine castration using the Henderson drill under total intravenous anesthesia. Methods: Randomised, double-blinded clinical study. Methods: Thirty-four stallions were anaesthetised using xylazine-ketamine and randomly selected to receive 10 mL either lidocaine or mepivacaine injected into each testicle. Both surgeon and anaesthetist were blinded to the selected trea...
Guedes A, Knych H, Tucker L, Almeida DC, Baldo CF, Wendt-Hornickle E, Allweiler S.This study determined the pharmacokinetics and compared the clinical effects of xylazine and dexmedetomidine in horses recovering from isoflurane anesthesia. Six healthy horses aged 8.5 ± 3 years and weighing 462 ± 50 kg were anesthetized with isoflurane for 2 hr under standard conditions on two occasions one-week apart. In recovery, horses received 200 μg/kg xylazine or 0.875 μg/kg dexmedetomidine intravenously and were allowed to recover without assistance. These doses were selected because they have been used for postanesthetic sedation in clinical and research studies. Serial ...
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...
Fatemikia H, Kamyab M, Movahed A, Sadeghi M, Kim E, Behdani M, Mohammadpour Dounighi N, Shahrivar M, Seyedian R.In this study, the neutralizing abilities of the equine and the recently introduced camelid antivenoms on the hemodynamic parameters (inotropism, chronotropism, and arrhythmogenicity) were assessed following envenomation by venom in rats. Methods: At first, the electrophoretic profiles of both products were obtained by using the SDS-PAGE method (12.5%) and stained with Coomassie blue and silver nitrate. Secondly, different doses of the camelid antivenom (10, 50, and 100 µl) were given intravenously in 10 min before venom injection (400 µg/rat). The neutralizing potencies of camelid and equi...
Kritchevsky JE, Muir GS, Leschke DHZ, Hodgson JK, Hess EK, Bertin FR.In metabolically stable horses, alpha-2-agonists suppress insulin secretion with transient hyperglycemia and rebound hyperinsulinemia. In horses with insulin dysregulation (ID), the effect of alpha-2-agonists has not been investigated; however, both the alpha-2-agonist-induced suppression of insulin secretion and rebound hyperinsulinemia could have clinical relevance. Objective: In horses with ID, alpha-2-agonists will alter insulin and glucose dynamics. Methods: Seven horses with ID and 7 control horses. Methods: In this randomized crossover study, xylazine hydrochloride (1.1 mg/kg) or detomi...
Mendez-Angulo JL, Granados MM, Modesto R, Serrano-Rodriguez JM, Funes FJ, Quiros S, Gomez-Villamandos RJ, Zaldívar S, Trumble TN.Local anaesthetics are being combined clinically with amikacin in intravenous regional limb perfusion (IVRLP), with limited knowledge on the analgesia provided and its onset and duration of action after tourniquet application and release. Objective: To evaluate the systemic clinical effect, limb withdrawal to nociceptive stimulation, and plasma and synovial fluid concentrations after IVRLP with lidocaine or mepivacaine in standing sedated horses. Methods: Prospective, controlled, randomised, cross-over study. Methods: Six healthy adult horses were sedated and received IVRLP with lidocaine, mep...
Krueger CR, Mitchell CF, Leise BS, Knych HK.Clodronate is a non-nitrogenated bisphosphonate approved for use in horses. There are no peer-reviewed published reports describing the pharmacokinetics or evaluating renal health indices and urinary excretion patterns in conjunction with plasma and synovial fluid concentration following the systemic administration of clodronate to horses. Objective: Describe clodronate concentrations in plasma, urine and synovial fluid and evaluate the effects on renal indices after intramuscular administration to healthy horses. Methods: Experimental study with repeated measures. Methods: Six healthy adult h...
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...
Berryhill EH, Knych H, Chigerwe M, Edman J, Magdesian KG.The neurokinin-1 (NK-1) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood in horses, and clinical use of NK-1 receptor antagonists has not been reported. This study aimed to determine the pharmacokinetics and safety of maropitant after administration of multiple doses. We hypothesized that maropitant concentrations would be similar at steady state to those reported in dogs, with minimal adverse effects. Maropitant was administered at 4 mg/kg orally, once daily for 5 days in seven adult horses. Serial plasma maropitant concent...
Gold JR, Grubb TL, Green S, Cox S, Villarino NF.In humans, gabapentin an analgesic, undergoes non-proportional pharmacokinetics which can alter efficacy. No information exists on the pharmacokinetics of dosages >20 mg/kg, escalating dosages or dose proportionality of gabapentin in horses. Objective: Gabapentin exposure in plasma would not increase proportionally relative to the dose in horses receiving dosages ≥20 mg/kg. To assess the plasma pharmacokinetics of gabapentin after nasogastric administration of gabapentin at dosages of 10 to 160 mg/kg in adult horses. Methods: Nine clinically healthy adult Arabian and Quarter Horses....
Khusro A, Aarti C, Salem AZM, Pliego AB, Rivas-Caceres RR.Methane (CH) emission from nonruminant livestock, particularly equines, is a colossal burden for veterinarians worldwide. In view of this, the present context was investigated to predict the antimethanogenic attributes of Moringa oleifera L. associated phytocomponents by targeting methyl-coenzyme M reductase (MCR) receptor in horses using in silico tools. Initially, the pharmacokinetics and ADME (absorption, distribution, metabolism, and excretion) properties of 26 phytocomponents were analyzed using Lipinski's rule of five and Swiss ADME tool, respectively. Among all the tested phytocomponent...
Paine SW, Bright J, Scarth JP, Hincks PR, Pearce CM, Hannan C, Machnik M, Hillyer L.In equine and racing practice, detomidine and butorphanol are commonly used in combination for their sedative properties. The aim of the study was to produce detection times to better inform European veterinary surgeons, so that both drugs can be used appropriately under regulatory rules. Three independent groups of 7, 8 and 6 horses, respectively, were given either a single intravenous administration of butorphanol (100 µg/kg), a single intravenous administration of detomidine (10 µg/kg) or a combination of both at 25 (butorphanol) and 10 (detomidine) µg/kg. Plasma and urine concentratio...
Subhahar MB, Singh J, Albert PH, Kadry AM.Etoricoxib, a selective inhibitor of cyclooxygenase-2, is used in the treatment of many inflammatory diseases and dental pain in humans. The aim of this study was to determine the pharmacokinetics and metabolism of etoricoxib in horses. Six horses weighing an average of 475 ± 25 kg were administered a single oral dose of etoricoxib at 1 mg/kg body weight. The results show that the drug reached a maximum concentration of 505.2 ± 67.8 ng/mL in 48 minutes after administration. The elimination half-life was calculated to be 10.20 ± 1.30 hours. Mass spectrometric analysis confirmed that eto...
Mirra A, Birras J, Diez Bernal S, Spadavecchia C.Epidural administration of morphine has been shown to be an effective analgesic strategy in horses; however, the possible occurrence of side effects limits its usage. In order to decrease their frequency, it is important to target the minimal effective plasma concentration and avoid overdosing. As to date species-specific pharmacokinetics data are not available for epidural morphine, the dosing regimen is usually established on the basis of clinical reports and personal experience. In certain physiological conditions, like gestation, the outcome of an empirical dosing scheme can be unpredictab...
Kwok WH, Choi TLS, Leung GNW, Wong ASY, Yue SK, Wan TSM, Ho ENM.The insulin-like peptide relaxin (RLX), an endogenous peptide hormone produced in human for pregnancy and reproduction, is also known to exert a range of physiological and pathological effects. Its use is banned in human sports, horseracing, and equestrian competitions due to its potential performance enhancing effect through vasodilation resulting in the increase of blood and oxygen supplies to muscles. Little is known about the biotransformation and elimination of RLX in horses. This paper describes an administration study of rhRLX-2 and its elimination in horses, and the development of sens...
Storgaard IH, Kristensen J, Larsen C, Mertz N, Østergaard J, Larsen SW.Intra-articular depot injectables based on in situ suspension formation of ester prodrugs of nonsteroidal anti-inflammatory drugs are promising for management of joint pain. As candidates for this delivery approach, 5 diclofenac ester prodrugs comprising different imidazole-containing promoieties were synthesized and their physicochemical properties characterized. In vitro hydrolysis rates were investigated in buffer solutions, in 40% (v/v) human, equine, canine, and rat plasma, and in 80% (v/v) human and equine synovial fluid. Bioconversion of the prodrugs to diclofenac was found to be enzym...
Karakka Kal AK, Nalakath J, Kunhamu Karatt T, Perwad Z, Mathew B, Subhahar M.The detection and separation of medetomidine enantiomers from the complex biological matrices poses a great analytical challenge, especially in the field of forensic toxicology and pharmacology. Couple of researchers reported resolution of medetomidine using protein-based chiral columns, but the reported method is quiet challenging and tedious to be employed for routine analysis. This research paper reported a method that enables the enantio-separation of medetomidine by using polysaccharide cellulose chiral column. The use of chiralcel OJ-3R column was found to have the highest potential for ...
Reginato GM, Xavier NV, Alonso BB, Lima DP, Pereira Sirqueira TC, Carregaro AB.The study evaluated the effect of a 1/10 dose of flunixin meglumine administered into the governing vessel 1 (GV1) acupoint in horses that underwent castration. Twenty animals received 0.02 mg/kg detomidine intravenously, followed by 2.2 mg/kg ketamine and 0.1 mg/kg diazepam by the same route, and also a local anesthesia with 30 mL lidocaine. As postoperative analgesia, the animals received 1.1 mg/kg flunixin meglumine IV (FIV) or 0.11 mg/kg flunixin meglumine into the GV1 acupoint (FGV). Behavioral parameters were assessed 12 hours before the procedure (baseline) and at 4, 6, 12, and 2...
Zielinski K, Sekula B, Bujacz A, Szymczak I.Serum albumin, the most abundant transport protein of mammalian blood, interacts with various nonsteroidal anti-inflammatory drugs (NSAIDs) affecting their disposition, metabolism, and excretion. A big group of chiral NSAIDs transported by albumin, profens, is created by derivatives of 2-arylpropionic acid. The chiral center in the structures of profens is adjacent to the carboxylate moiety and often determines different pharmacological properties of profen enantiomers. This study describes crystal structures of two albumins, isolated from equine and leporine serum, in complexes with three pro...
Boone LH, DeGraves FJ, Klein CE, Cole RC, Schumacher J.To assess onset of analgesia for 3% chloroprocaine hydrochloride and 2% mepivacaine hydrochloride when used for median and ulnar nerve blocks in lame horses. Methods: 6 naturally lame horses. Methods: A crossover experiment was conducted. Horses were assigned to 1 of 2 treatment groups (3% chloroprocaine or 2% mepivacaine first). Median and ulnar nerve blocks were performed in the lame limb with the assigned treatment. Lameness was objectively evaluated before treatment administration and at various points for 120 minutes after treatment with a wireless inertial sensor-based motion analysis sy...
Scare JA, Leathwick DM, Sauermann CW, Lyons ET, Steuer AE, Jones BA, Clark M, Nielsen MK.An alternative control regimen for drug-resistant parasites is combination deworming, where two drugs with different modes of action are administered simultaneously to target the same parasite. Few studies have investigated this in equine cyathostomins. We previously reported that an oxibendazole (OBZ) and pyrantel pamoate (PYR) combination was not sustainable against a cyathostomin population with high levels of OBZ and PYR resistance. This study consisted of a field study and two computer simulations to evaluate the efficacy of a moxidectin-oxibendazole (MOX-OBZ) combination against the same...
Foreman JH, Barange A, Lawrence LM, Hungerford LL.The objective was to test the hypothesis that phenylbutazone (PBZ) alleviates lameness in an adjustable heart bar shoe model of equine foot pain. Eight Quarter Horse mares underwent 4-weekly treatments randomly: 0.9% saline placebo (SAL: 1 mL/45 kg body weight i.v.) with no lameness; SAL with lameness; PBZ (4.4 mg/kg body weight i.v.) with no lameness; and PBZ with lameness. Blinded heart rate (HR) and lameness score (LS) were assessed every 20 min for 2 h and then hourly through 9 h. At 1 h SAL or PBZ was administered. Jugular venous samples were obtained at hours 0, 1, 2, 4, 6, and 8 and wer...
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...
Slocombe JO, McCraw BM, Pennock PW, Vasey J.Twelve pony foals were reared worm-free and inoculated with Strongylus vulgaris. Approximately 8 weeks after they were inoculated, 6 foals were given ivermectin IM at a dosage rate of 200 micrograms/kg of body weight and 6 were given a placebo. All foals were necropsied 35 days after treatment. Ivermectin was 98.9% effective in eliminating later 4th-stage S vulgaris larvae located near the origin of major intestinal arteries and in reducing clinical signs and permitting resolution of lesions associated with verminous arteritis. One pony foal reared on pasture and with evidence of arteritis of ...
Malsa J, Courtot É, Boisseau M, Dumont B, Gombault P, Kuzmina TA, Basiaga M, Lluch J, Annonay G, Dhorne-Pollet S, Mach N, Sutra JF, Wimel L....Alternative strategies to chemical anthelmintics are needed for the sustainable control of equine strongylids. Bioactive forages like sainfoin () could contribute to reducing drug use, with the first hints of activity against cyathostomin free-living stages observed in the past. We analysed the effect of a sainfoin-rich diet on cyathostomin population and the efficacy of oral ivermectin treatment. Two groups of 10 naturally infected horses were enrolled in a 78-day experimental trial. Following a 1-week adaptation period, they were either fed with dehydrated sainfoin pellets (70% of their die...
Raidal SL, Edwards S, Pippia J, Boston R, Noble GK.The pharmacokinetics, efficacy, and safety of meloxicam have been evaluated in adult horses, but not foals. Physiologic differences between neonates and adults might alter drug pharmacokinetics and therapeutic index. Objective: The pharmacokinetics of meloxicam will be different in foals compared with adult horses, and foals could be at increased risk for adverse drug effects. Methods: Twenty lightbreed foals less than 6 weeks of age at commencement of the study. Methods: Single and repeated oral dose pharmacokinetics were determined for meloxicam (0.6 mg/kg) in 10 foals. The safety of the d...
Papadopoulos E, Rowlinson M, Bartram D, Carpenter S, Mellor P, Wall R.An in vitro assay was used to assess the efficacy of the proprietary pyrethroid insecticide cypermethrin applied to horses (Deosect spray, 5.0%, w/v Fort Dodge Animal Health) against the biting midge Culicoides nubeculosus (Meigen) (Diptera: Ceratopogonidae) and the mosquitoes Aedes aegypti Linneaus and Culex quinquefasciatus Say (Diptera: Culicidae). Hair was collected from the back, belly and legs of the horses immediately prior to treatment and 7, 14, 21, 28 and 35 days after treatment, and also from untreated controls. In laboratory assays groups of 10 adult female C. nubeculosus, Ae. aegy...
Zak A, Siwinska N, Slowikowska M, Borowicz H, Szpot P, Zawadzki M, Niedzwiedz A.Capsaicin and dihydrocapsaicin are alkaloids with analgesic effects in humans and animals. When used locally, both of them minimalise pain sensation by defunctionalising nerve endings. According to the Federation Equestrian International Prohibited Substances List, these are substance banned in horse competitions. The aim of the study was to determine the detection time of capsaicin in both plasma and serum after long-term use of a gel recommended for commercial use and applied as intended. The objective of the study was to select the best material for the detection of capsaicin as a doping su...
Mama KR, Steffey EP, Pascoe PJ.This study provides baseline information on the potential use of propofol as a general anesthetic for horses. Using a Latin square design, propofol (2, 4, and 8 mg/kg) was administered intravenously on three separate occasions to six mature horses. Information about anesthetic induction, duration, and recovery was recorded along with results of rectal temperature, heart rate, respiratory rate, pHa, PaCO2 and PaO2. Statistical analysis included a mixed model analysis of variance, a general linear model analysis and least square means test for post hoc comparisons. A P < .05 was considered si...
Mealey KL, Matthews NS, Peck KE, Burchfield ML, Bennett BS, Taylor TS.To compare plasma disposition of the R(-) and S(+) enantiomers of carprofen after IV administration of a bolus dose to donkeys and horses. Methods: 5 clinically normal donkeys and 3 clinically normal horses. Methods: Blood samples were collected from all animals at time 0 (before) and at 10, 15, 20, 30, and 45 minutes and 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 24, 28, 32, and 48 hours after IV administration of a bolus of carprofen (0.7 mg/kg). Plasma was analyzed in triplicate via high-performance liquid chromatography to determine the concentrations of the carprofen enantiomers. A plasma concent...
Landoni MF, Lees P.A comparative study in horses of the pharmacokinetics (PK) and pharmacodynamics (PD) of 2 extensively used nonsteroidal anti-inflammatory drugs (NSAIDs), flunixin (FXN) and ketoprofen (KTP), was carried out applying PK/PD modelling. To evaluate the anti-inflammatory properties of these drugs a model of acute inflammation, comprising surgically implanted subcutaneous tissue cages stimulated by intracaveal injection of carrageenan, was used. FXN elimination half-life (T1/2 beta) in plasma was 3.37 +/- 1.09 h. However, in exudate a much longer T1/2 beta was obtained (15.99 +/- 3.80 h). Apparent v...
Lees P, Sedgwick AD, Higgins AJ, Pugh KE, Busch U.The novel non-steroidal anti-inflammatory drug (NSAID) miloxicam was administered intravenously to six New Forest ponies at a dosage rate of 0.6 mg/kg in a two-part cross-over study. In each part, three horses received miloxicam and three were given a placebo preparation. The actions of miloxicam, compared to placebo, were assessed in a carrageenan-sponge model of acute inflammation. The rise in skin temperature over the site of the acute inflammatory reaction was less in treated ponies, but differences were not statistically significant. Concentrations of the enzymes acid phosphatase (AP) and...
Sykes BW, Underwood C, Greer R, McGowan CM, Mills PC.Conflicting data are presented in the current literature regarding the efficacy of omeprazole for suppressing gastric acidity in the horse. Objective: The objective of this study was to investigate the duration of intraday acid suppression achieved with two doses of omeprazole under two different dietary conditions. Methods: A four-way crossover design. Methods: Six adult Thoroughbred horses instrumented with percutaneous gastrotomy tubes were used. Intragastric pH was measured for continuous 23 h periods (08.00-07.00 h) for six consecutive days (Days 0-5). Baseline data was recorded on Day 0 ...
Messenger KM, Davis JL, LaFevers DH, Barlow BM, Posner LP.To describe the pharmacokinetics and adverse effects of intravenous (IV) and sublingual (SL) buprenorphine in horses, and to determine the effect of sampling site on plasma concentrations after SL administration. Methods: Randomized crossover experiment; prospective study. Methods: Eleven healthy adult horses between 6 and 20 years of age and weighing 487-592 kg. Methods: In the first phase; buprenorphine was administered as a single IV or SL dose (0.006 mg kg(-1)) and pharmacokinetic parameters were determined for each route of administration using a noncompartmental model. In the second phas...
Wojtasiak-Wypart M, Soma LR, Rudy JA, Uboh CE, Boston RC, Driessen B.Romifidine HCl (romifidine) is an α(2)-agonist commonly used in horses. This study was undertaken to investigate the pharmacokinetics (PK) of romifidine following intravenous (i.v.) administration and describe the relationship between PK parameters and simultaneously recorded pharmacodynamic (PD) parameters. Romifidine (80 μg/kg) was administered by i.v. infusion over 2 min to six adult Thoroughbred horses, and plasma samples were collected and analyzed using liquid chromatography-mass spectrometry. Limit of quantification was <0.1 ng/mL. PD parameters and arterial blood gases were measur...
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...
Ryan CA, Sanchez LC, Giguère S, Vickroy T.Proton pump inhibitors (PPIs) are a mainstay of treatment for acid-related ulceration in man and horses. Currently, only an oral preparation of omeprazole is approved for use in horses in the USA. Intravenous administration of a PPI would provide a useful therapeutic alternative for those foals in which oral medication is not feasible. Objective: To investigate the pharmacokinetics and pharmacodynamics of pantoprazole following i.v. or intragastric administration in healthy neonatal foals. Methods: Seven healthy foals age 6-12 days at the start of the study were evaluated. Treatments included ...
de Vries A, Pakkanen SA, Raekallio MR, Ekiri A, Scheinin M, Taylor PM, Vainio OM.To investigate the effects of MK-467 on sedation quality, and cardiopulmonary and pharmacokinetic variables in horses sedated intravenously (IV) with romifidine. Methods: Experimental, randomized, crossover design. Methods: Seven healthy mares. Methods: Romifidine (80 μg kg-1 ; R) and MK-467 (200 μg kg-1 ; MK) were administered IV alone and in combination (R + MK). Levels of sedation and borborygmi were scored. Heart rate (HR), direct arterial blood pressure (ABP) and respiratory rate (fR ) were recorded. Arterial and venous blood gas analyses were performed and venous plasma drug conc...
Baker A, Plummer CE, Szabo NJ, Barrie KP, Brooks DE.To determine the concentration of doxycycline in preocular tear film following oral administration in horses as a possible therapeutic modality for infectious and keratomalacic equine keratitis. Methods: Eight broodmares without ocular disease from a Thoroughbred breeding facility were included in this study. Each mare received 20 mg/kg of doxycycline by mouth once daily in the morning for five consecutive days. Tears were collected 1 h after doxycycline administration starting on day one of administration and continuing for 10 consecutive days. Doxycycline levels in the tears were measured us...
Larenza MP, Knobloch M, Landoni MF, Levionnois OL, Kronen PW, Theurillat R, Schatzmann U, Thormann W.The pharmacokinetics of ketamine and norketamine enantiomers after administration of intravenous (IV) racemic ketamine (R-/S-ketamine; 2.2 mg/kg) or S-ketamine (1.1 mg/kg) to five ponies sedated with IV xylazine (1.1mg/kg) were compared. The time intervals to assume sternal and standing positions were recorded. Arterial blood samples were collected before and 1, 2, 4, 6, 8 and 13 min after ketamine administration. Arterial blood gases were evaluated 5 min after ketamine injection. Plasma concentrations of ketamine and norketamine enantiomers were determined by capillary electrophoresis and wer...
Hyde RM, Lynch TM, Clark CK, Slone DE, Hughes FE.This study investigated the influence of perfusate volume on antimicrobial concentration in synovial fluid following intravenous regional limb perfusion (IVRLP) and assessed the efficacy of low volume IVRLP. The front limbs of 9 horses were randomly assigned to 1 of 3 volume groups: 10 mL (Group 1), 30 mL (Group 2), or 60 mL (Group 3). A tourniquet was applied distal to the carpus and the limbs were perfused with 500 mg genta-micin diluted to the assigned volume via a catheter placed in the lateral palmar digital vein at the level of the proximal sesamoid bones. Synovial fluid samples were col...
Knych HK, Magdesian KG.Equine antimicrobial therapy has advanced over time with the availability of increasing pharmacokinetic and pharmacodynamic studies in horses, allowing for greater evidence-based clinical decision-making. However, many challenges to optimal antimicrobial therapy remain and further research is needed to address these areas. There are a limited number of approved antimicrobials for use in horses, which creates a need for compounded preparations for clinicians. Extra-label drug use is commonplace in equine practice, which warrants continual education of veterinarians about policies and updates. P...
Casoni D, Spadavecchia C, Wampfler B, Thormann W, Levionnois OL.Intravenous anaesthetic drugs are the primary means for producing general anaesthesia in equine practice. The ideal drug for intravenous anaesthesia has high reliability and pharmacokinetic properties indicating short elimination and lack of accumulation when administered for prolonged periods. Induction of general anaesthesia with racemic ketamine preceded by profound sedation has already an established place in the equine field anaesthesia. Due to potential advantages over racemic ketamine, S-ketamine has been employed in horses to induce general anaesthesia, but its optimal dose remains und...
Oreff GL, Dahan R, Tatz AJ, Raz T, Britzi M, Kelmer G.To determine the influence of 3 perfusate volumes on amikacin concentration in the metacarpophalangeal joint following cephalic regional limb perfusion (RLP) in standing horses. Methods: Seven healthy horses. Methods: Three perfusate volumes (100, 60, and 30 mL), containing 2 grams of amikacin, were tested during intravenous RLP at the cephalic vein, placing the tourniquet at mid antebrachium, in standing sedated horses. Synovial fluid was collected from the metacarpophalangeal joint before perfusion and at 30 and 120 minutes after perfusion. Serum samples were taken from the jugular vein at t...
Theurillat R, Knobloch M, Schmitz A, Lassahn PG, Mevissen M, Thormann W.CE with multiple isomer sulfated beta-CD as the chiral selector was assessed for the simultaneous analysis of the enantiomers of ketamine and metabolites in extracts of equine plasma and urine. Different lots of the commercial chiral selector provided significant changes in enantiomeric ketamine separability, a fact that can be related to the manufacturing variability. A mixture of two lots was found to provide high-resolution separations and interference-free detection of the enantiomers of ketamine, norketamine, dehydronorketamine, and an incompletely identified hydroxylated metabolite of no...
Davis JL, Salmon JH, Papich MG.To determine the pharmacokinetics of itraconazole after IV or oral administration of a solution or capsules to horses and to examine disposition of itraconazole in the interstitial fluid (ISF), aqueous humor, and polymorphonuclear leukocytes after oral administration of the solution. Methods: 6 healthy horses. Methods: Horses were administered itraconazole solution (5 mg/kg) by nasogastric tube, and samples of plasma, ISF, aqueous humor, and leukocytes were obtained. Horses were then administered itraconazole capsules (5 mg/kg), and plasma was obtained. Three horses were administered itraconaz...
Berlin S, Randow T, Scheuch E, Grube M, Venner M, Siegmund W.The long-acting azalide antibiotic gamithromycin is marketed for intramuscular treatment of bovine and swine infections. Off-label use in foals leads to severe local lesions likely caused by hyperosmolality of the injected solution. We provide evidence from a pharmacokinetic study in 10 warm-blooded healthy foals for intravenous bolus injection of gamithromycin diluted in distilled water to be a safe and well tolerated alternative. By intravenous dosing, markedly higher plasma exposure and better penetration into bronchoalveolar lavage cells but lower distribution into epithelial lining fluid ...
Léguillette R, Désévaux C, Lavoie JP.To determine the effects of pentoxifylline (PTX) administration on lung function and results of cytologic examination of bronchoalveolar lavage fluid in horses affected by recurrent airway obstruction (RAO). Methods: 10 RAO-affected horses. Methods: 6 horses were orally administered PTX (16 g) mixed with corn syrup, and 4 horses were administered corn syrup alone, twice daily for 14 days. Pulmonary function was evaluated before administration (day 0) and on days 8 and 15. Bronchoalveolar lavage (BAL) was performed on days 0 and 15. Reversibility of airway obstruction was assessed by measuring ...
Burton AJ, Giguère S, Arnold RD.Although gentamicin is highly active against Rhodococcus equi in vitro, its clinical efficacy has been limited presumably due to poor cellular uptake. Encapsulation of drugs in liposomes enhances their cellular uptake. Objective: To compare the disposition of liposomal gentamicin (LG) and free gentamicin (FG) in the plasma, pulmonary epithelial lining fluid and bronchoalveolar cells of healthy foals after i.v. administration or by nebulisation, and to assess the tolerability of the drug after repeated i.v. dosing. Methods: Experimental study. Methods: Eight healthy foals received a single i.v....
