The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
Shnaiderman-Torban A, Navon-Venezia S, Dahan R, Dor Z, Taulescu M, Paitan Y, Edery N, Steinman A.An eighteen-hour-old Tennessee walking horse foal was referred due to weakness and abdominal pain. Physical examination revealed dehydration, distended abdomen, and uveitis. Blood analysis revealed leukopenia, neutrophils' toxicity and left shift. The foal developed bloody diarrhea, gastric reflux, and was diagnosed with sepsis and enterocolitis. The foal was treated with intravenous fluids, plasma, antibiotics (ceftriaxone and metronidazole), partial parenteral nutrition (dextrose and amino acids), flunixin meglumine, and ophthalmic drops. Umbilical ultrasound revealed a fluid pocket adjacent...
Sánchez-Aparicio P, Florán B, Rodríguez Velázquez D, Ibancovichi JA, Varela Guerrero JA, Recillas S.Osteoarticular equine disease is a common cause of malady; in general, its therapy is supported on steroids and nonsteroidal anti-inflammatories. Nevertheless, many side effects may develop when these drugs are administered. Nowadays, the use of new alternatives for this pathology attention is demanded; in that sense, cannabinoid CB2 agonists may represent a novel alternative. Cannabinoid belongs to a group of molecules known by their psychoactive properties; they are synthetized by the Cannabis sativa plant, better known as marijuana. The aim of this study was to contribute to understand the ...
Young JM, Schoonover MJ, Kembel SL, Taylor JD, Bauck AG, Gilliam LL.To evaluate the analgesic effects of orally administered gabapentin on horses with chronic thoracic limb lameness. Methods: Randomized, crossover design. Methods: A total of 14 adult horses with chronic thoracic limb lameness. Methods: Following baseline measurement of lameness, horses were administered each of four treatments orally in grain: treatment G, gabapentin (20 mg kg) twice daily for 13 doses; treatment F, firocoxib (171 mg once, then 57 mg once daily for six doses); treatment GF, gabapentin and firocoxib at previously stated doses and frequencies; or treatment C, grain only as a con...
Snowden RT, Schumacher J, Blackford JT, Cypher EE, Cox SK, Sun X, Whitlock BK.To determine whether therapeutic concentrations (> 0.5 to 1.0 μg/mL) of polymyxin B (PB) were achieved in the tarsocrural joint of horses when the drug was administered by IV regional limb perfusion (IV-RLP) via a saphenous vein at doses of 25, 50, and 300 mg and to describe any adverse systemic or local effects associated with such administration. Methods: 9 healthy adult horses. Methods: In the first of 2 experiments, 6 horses each received 25 and 50 mg of PB by IV-RLP via a saphenous vein with at least 2 weeks between treatments. For each treatment, a tourniquet was placed at the midmetata...
Markell R, Saviola G, Barker EA, Conway JD, Dujardin C.There has recently been some controversy over the use of bisphosphonates in horses and some confusion regarding the different classes of bisphosphonates and the differences between the mechanism of actions and effects of each class. This review article explores the different bisphosphonate classes and their different effects and mechanisms of action based on research from both the human and equine veterinary fields. This collaborative review between veterinary surgeons and medical doctors describes the latest use of bisphosphonates in humans and horses, including safety aspects, and allows com...
Habershon-Butcher J, Cutler C, Viljanto M, Hincks PR, Biddle S, Paine SW.Xylazine is widely used worldwide as a short-acting sedative in general equine and racing practice. In the UK, although it has a legitimate use during training, equine anti-doping rules state it is a prohibited substance on race day. The aim of the study was to produce a detection time (DT) to better inform European veterinary surgeons so that xylazine can be used appropriately under regulatory rules. Previous publications have various limitations pertaining to analysis method, particularly for plasma and limited length of time of sample collection. In this study, pharmacokinetic data were pro...
Lopp CT, McCoy AM, Boothe D, Schaeffer DJ, Lascola K.To characterize the pharmacokinetics of a clinically relevant dose of misoprostol administered PO or per rectum (PR) to horses. Methods: 8 healthy adult horses. Methods: In a randomized 3-way crossover design, horses received a single dose of misoprostol (5 μg/kg) administered PO (with horses fed and unfed) and PR, with a minimum 3-week washout period separating the experimental conditions. Blood samples were obtained before and at various points after drug administration (total, 24 hours), and plasma concentrations of misoprostol free acid were measured. Results: Mean maximum plasma concentr...
Magma (New York, N.Y.)October 4, 2019
Volume 33, Issue 2 299-307 doi: 10.1007/s10334-019-00781-z
Palfrey RM, Summers IR, Winlove CP.Quantitative magnetic resonance imaging was used to determine partition coefficients and characteristic time constants for diffusion of MRI contrast agents in disc tissue. Methods: Twenty-two excised equine intervertebral discs were exposed to a range of contrast agents: six to manganese chloride, eight to Magnevist (gadopentetate dimeglumine) and eight to Gadovist (gadobutrol), and uptake into the disc was quantified in T-weighted images. Results: Diffusion for all contrast agents was approximately 25% faster in the nucleus than in the outer annulus; disc-average time constants ranged from (2...
Gozalo-Marcilla M, Moreira da Silva R, Pacca Loureiro Luna S, Rodrigues de Oliveira A, Werneck Fonseca M, Peporine Lopes N, Taylor PM, Pelligand L.The alpha(α) -agonist detomidine is used for equine sedation with opioids such as methadone. We retrieved the data from two randomized, crossover studies where detomidine and methadone were given intravenously alone or combined as boli (STUDY 1) (Gozalo-Marcilla et al., 2017, Veterinary Anaesthesia and Analgesia, 2017, 44, 1116) or as 2-hr constant rate infusions (STUDY 2) (Gozalo-Marcilla et al., 2019, Equine Veterinary Journal, 51, 530). Plasma drug concentrations were measured with a validated tandem Mass Spectrometry assay. We used nonlinear mixed effect modelling and took pharmacokinetic...
Mendoza FJ, Perez-Ecija A, Toribio RE.Donkeys and mules show several pharmacodynamic and pharmacokinetic idiosyncrasies that have to be fully considered by any clinician dealing with these species. Because they possess an increased metabolic rate and cellular water content compared with horses, higher doses (or shorter dosing intervals) are usually recommended for those drugs where pharmacologic studies have been performed. Nonetheless, owing to the lack of species-specific information, this assumption cannot be arbitrarily applied. Thus, when a drug protocol published for horses is extrapolated to a donkey or a mule, a close moni...
Diez Bernal S, Studer N, Thormann W, Spadavecchia C, Levionnois O.To evaluate the effect of a romifidine infusion on antinociception and sedation, and to investigate its relationship with plasma concentration. Methods: Prospective, experimental, nonrandomized trial. Methods: A total of 10 healthy adult warmblood horses. Methods: Romifidine (loading dose: 0.08 mg kg, infusion: 0.03 mg kg hour) was administered intravenously over 120 minutes. Romifidine plasma concentrations were determined by capillary electrophoresis. Sedation quality and nociceptive thresholds were evaluated at regular time points before, during and after romifidine administration. The noci...
Nemoto M, Tamura N, Bannai H, Tsujimura K, Kokado H, Ohta M, Yamanaka T.Baloxavir marboxil (BXM), an inhibitor of the cap-dependent endonuclease of the influenza virus polymerase acidic protein (PA), exerts an antiviral effect against influenza A virus. It has been available in Japan since March 2018. This study evaluated the antiviral efficacy of BXM against equine influenza A virus (EIV) by an experimental challenge study using horses. Six horses were experimentally inoculated with EIV, and BXM was administered to the three horses at 2 days post inoculation. Horses treated with BXM showed milder clinical signs than horses without treatment and shed less virus. T...
Knych HK, Weiner D, Steinmetz S, Flynn K, McKemie DS.Hydroxyzine is a first-generation antihistamine and cetirizine, a second-generation antihistamine and active metabolite of hydroxyzine. Hydroxyzine is commonly used in performance horses and as such its use in closely regulated; however, there are no published studies suitable for establishing appropriate regulatory recommendations. In the current study, 12 exercised Thoroughbred research horses received a single oral administration of 500 mg of hydroxyzine. Blood and urine samples were collected prior to and up to 96 hr postdrug administration and concentrations of hydroxyzine and cetirizin...
Hollis AR, Pascal M, Van Dijk J, Jolliffe C, Kaartinen J.To compare the efficacy of a medetomidine constant rate infusion (CRI) with a detomidine CRI for standing sedation in horses undergoing high dose rate brachytherapy. Methods: Randomized, controlled, crossover, blinded clinical trial. Methods: A total of 50 horses with owner consent, excluding stallions. Methods: Each horse was sedated with intravenous acepromazine (0.02 mg kg-1), followed by an α2-adrenoceptor agonist 30 minutes later and then by butorphanol (0.1 mg kg-1) 5 minutes later. A CRI of the same α2-adrenoceptor agonist was started 10 minutes after butorphanol administration and ma...
Moorman VJ, Bass L, King MR.To determine the effects of 3 α2-adrenergic receptor agonists (α2-ARAs), alone or in combination with butorphanol tartrate, on objective measurements of lameness in horses. Methods: 17 adult polo horses with naturally occurring forelimb or hind limb lameness (or both). Methods: In a crossover design, each horse received each protocol (saline [0.09% NaCl] solution [2 mL, IV] or xylazine hydrochloride [0.33 mg/kg, IV], detomidine hydrochloride [0.007 mg/kg, IV], or romifidine hydrochloride [0.033 mg/kg, IV] alone or in combination with butorphanol [0.007 mg/kg, IV]) in random order, with a was...
Wenzel RG, Major D, Hesp KF, Hall E, Doble P.To monitor cobalt concentrations in urine, red blood cells and plasma after chronic parenteral administration of cobalt chloride evaluate these results against the current International Federation of Horseracing Authorities thresholds for detecting cobalt misuse. Methods: Eight mares were randomly assigned to four treatment groups, with two mares in each group: Group 1 - control group, Group 2 - 25 milligrams cobalt intravenously as CoCl weekly, Group 3 - 50 milligrams cobalt intravenously as CoCl weekly, and Group 4 - 25 milligrams cobalt intravenously mid-week and at the end of the week. Uri...
Tutunaru A, Dupont J, Gougnard A, Ida K, Serteyn D, Sandersen C.To the authors' knowledge, there are no reports describing the use of cis-atracurium in the horse. To describe the onset time and the duration of the neuromuscular blockade (NMB) of three different doses of cis-atracurium in horses and to determine the appropriate dose needed maintain a NMB. Retrospective study. Horses which received cis-atracurium as part of a balanced anaesthetic protocol at the Equine Teaching Hospital of the University of Liège between March 2014 and June 2017 were included in this study. A train-of-four (TOF) stimulation pattern was used to assess the NMB. The cis-atracu...
Pisello L, Rampacci E, Stefanetti V, Beccati F, Hyatt DR, Coletti M, Passamonti F.This study aimed to describe bacteria isolated from the reproductive tract of mares and to identify changes in antimicrobial susceptibility patterns to those antibiotics commonly used for the treatment of equine endometritis. A total of 4122 equine uterine swabs were collected from mares suffering from reproductive tract disorders in the period 2010-2017. Aerobic culture and antimicrobial susceptibility testing using agar disc diffusion were performed on each sample. Aerobic bacteria were isolated from 3171 of 4122 (76.9 per cent) samples. The most frequently isolated microorganisms were (885...
Knych HK, Arthur RM, Kanarr KL, McKemie DS, Kass PH.Methamphetamine is a central and peripheral nervous system stimulant. There is only a single study that describes exposure to and disposition of this compound in horses. The potential for abuse and inadvertent exposure in equine athletes along with the limited data available necessitates further study. The objectives of the current study were to describe drug and metabolite concentrations, develop an analytical method that could be used to regulate its use, and describe selected pharmacodynamic effects. In phase 1, six horses were randomized into three transmucosal dose groups (n = 2/group; ...
Tapio HA, Raekallio MR, Mykkänen AK, Al-Ramahi D, Scheinin M, Hautajärvi HJ, Männikkö S, Vainio O.A constant rate infusion (CRI) of medetomidine is used to balance equine inhalation anesthesia, but its cardiovascular side effects are a concern. This experimental crossover study aimed to evaluate the effects of vatinoxan (a peripheral α2-adrenoceptor antagonist) on cardiorespiratory and gastrointestinal function in anesthetized healthy horses. Six horses received medetomidine hydrochloride 7μg/kg IV alone (MED) or with vatinoxan hydrochloride 140μg/kg IV (MED+V). Anesthesia was induced with midazolam and ketamine and maintained with isoflurane and medetomidine CRI for 60min. Heart rate, ...
Guan F, You Y, Li X, Robinson MA.Bioactive peptides possess pharmacological effects and can be illicitly used in sports. To deter such misuse, an untargeted method using high resolution mass spectrometry (HRMS) has been developed for comprehensive detection of multitudinous exogenous peptides in equine plasma and urine. Forty-four peptides were extracted using mixed-mode solid-phase extraction (SPE) from plasma and urine, separated with a hydrophilic interaction liquid chromatography (HILIC) column, and detected on an HRMS instrument. Ammonium formate as a mobile phase additive had effects on HILIC retention and charge state ...
Knych HK, Baden RW, Gretler SR, McKemie DS.Despite their widespread popularity as sport and companion animals and published and anecdotal reports of vast difference in drug disposition and pharmacokinetics between individuals, studies describing equine drug metabolism are limited. It has been theorized that similar to humans, members of the CYP2D family in horses may be polymorphic in nature leading to differences in metabolism of substrates. This study aims to build on the limited current knowledge regarding P450 mediated metabolism in horses by describing the metabolism of the polymorphic CYP2D6 probe drug codeine in vitro. Codeine, ...
Kuroda T, Nagata SI, Tamura N, Mita H, Kusano K, Mizobe F, Takizawa Y, Fukuda K, Kasashima Y.To investigate the pharmacokinetics and antihistaminic effects (pharmacodynamics) of olopatadine in a small population of healthy horses after administration via nasogastric tube. Methods: 4 healthy adult Thoroughbreds. Methods: Olopatadine (0.1 mg/kg, once) was administered via nasogastric tube. Blood samples were collected at predetermined time points for pharmacokinetic analyses of the drug in plasma. Olopatadine effects were investigated by measurement of cutaneous wheals induced by ID histamine injection (0.1 mL [10 μg]/injection) at predetermined time points. Inhibition effect ratios we...
Mitchell A, Watts AE, Ebetino FH, Suva LJ.Bisphosphonates (BPs) are a family of molecules characterized by two key properties: their ability to bind strongly to bone mineral and their inhibitory effects on mature osteoclasts and thus bone resorption. Chemically two groups of BPs are recognized, non-nitrogen-containing and nitrogen-containing BPs. Non-nitrogen-containing BPs incorporate into the energy pathways of the osteoclast, resulting in disrupted cellular energy metabolism leading to cytotoxic effects and osteoclast apoptosis. Nitrogen-containing BPs primarily inhibit cholesterol biosynthesis resulting in the disruption of intrac...
Gajardo G, López-Muñoz R, Plaza A, Uberti B, Sarmiento J, Morán G, Henríquez C.Tamoxifen (TAM), a selective modulator of estrogen receptors (SERMs) has been recently explored as a therapeutic option for the oral treatment of airway inflammation in the horse. The objective of this work was to establish pharmacokinetic parameters of TAM and its main metabolites in equines, as well as to determine its clinical safety in short-term treatments. Results: We determined TAM and its three main metabolites (4-OH tamoxifen, endoxifen, and N-desmethyl tamoxifen) in plasma after single administration of 0.25 mg/kg in healthy adult horses ( = 12). A maximum concentration of TAM w...
Langston VC, Fontenot RL, Byers JA, Andrews CM, Mochal-King CA.The objective of this study was to determine the pharmacokinetics of meropenem in horses after intravenous (IV) administration. A single IV dose of meropenem was administered to six adult horses at 10 mg/kg. Plasma and synovial fluid samples were collected for 6 hr following administration. Meropenem concentrations were determined by bioassay. Plasma and synovial fluid data were analyzed by compartmental and noncompartmental pharmacokinetic methods. Mean ± SD values for elimination half-life, volume of distribution at steady-state, and clearance after IV administration for plasma samples ...
Seddighi R, Knych HK, Cox SK, Sun X, Moorhead KA, Doherty TJ.To determine the sedative effects and pharmacokinetic profile of detomidine when administered intravaginally as a gel formulation to horses. Methods: Randomized, crossover, masked experimental design. Methods: A group of six healthy adult mares (494 ± 56 kg). Methods: Mares were studied on two occasions and were administered either detomidine hydrochloride (10 μg kg) intravenously (treatment IV) or detomidine gel (40 μg kg) intravaginally (treatment IVG), separated by 1 week. Sedation, ataxia, muzzle-floor distance and heart rate (HR) were evaluated every 15 minutes for 240 minutes. Venous ...
Berryhill EH, Knych H, Edman JM, Magdesian KG.The neurokinin-1 (NK) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood and likely under-recognized in horses. Use of NK-1 receptor antagonists in horses has not been reported. The purpose of this study was to determine the pharmacokinetic profile of maropitant in seven adult horses after single intravenous (IV; 1 mg/kg) and intragastric (IG; 2 mg/kg) doses. A randomized, crossover design was performed. Serial blood samples were collected after dosing; maropitant concentrations were measured using LC-MS/MS. Pharmacokinetic pa...
Marcinkowska M, Bucki A, Panek D, Siwek A, Fajkis N, Bednarski M, Zygmunt M, Godyń J, Del Rio Valdivieso A, Kotańska M, Kołaczkowski M....Serotonin 5-HT receptors, butyrylcholinesterase (BuChE) and oxidative stress are related to the pathophysiology of Alzheimer's disease. Inhibition of BuChE provides symptomatic treatment of the disease and the same effect was demonstrated for 5-HT antagonists in clinical trials. Oxidative stress is regarded as a major and primary factor contributing to the development of Alzheimer's disease; therefore, antioxidant agents may provide a disease-modifying effect. Combining BuChE inhibition, 5-HT antagonism, and antioxidant properties may result in multitarget-directed ligands providing cognitio...
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...
da Silva Xavier AA, da Rosa PP, de Brum Mackmill L, Roll VFB.For several years, hyaluronic acid (HyA) and, more recently, polyacrylamide hydrogel (PHyd) have been used to reduce lameness and pain caused by osteoarthritis. However, there is still a lack of scientific evidence of the efficacy of these substances to allow veterinary experts to make decisions about their use in horses. The objective of this study was to evaluate, through a systematic review and network meta-analysis (NMA), the efficacy of HyA, associated or not with other drugs, and PHyd in relieving lameness in horses with osteoarthritis. The searches for primary studies were conducted on ...
Schoster A, Amsler M, Kirchgaessner C, Saleh L, Schwarzwald C, Schmitt S.The optimal dosage regimen of gentamicin in horses is still under investigation. The objectives of this study were to determine gentamicin plasma concentrations in hospitalized horses treated with 10 mg/kg gentamicin (IV, q 24 h) and to determine whether a plasma concentration to minimum inhibitory concentration (MIC) ratio of 10:1 is reached for equine pathogens using this dose. Methods: Prospective clinical observational study; retrospective study on MICs of 131 gram-negative bacteria isolated from horses (2012-2015). Methods: University teaching hospital. Methods: Ninety-eight horses >...
Bishop RM, Scott I, Gee EK, Rogers CW, Pomroy WE, Mayhew IG.To ascertain whether resistance was present in Parascaris equorum to the macrocyclic lactone anthelmintic ivermectin, using faecal egg count reduction tests. Methods: Thirty-nine foals aged between 11 and 28 weeks on three Thoroughbred stud farms (Farms A; n=20, B; n=5 and C; n=14) were treated with ivermectin (Day 0) and faecal egg counts (FEC) were monitored before and for 21 (Farms A and B) or 14 (Farm C) days after treatment. On Farms A and B, the foals were treated with a macrocyclic lactone/benzimidazole/praziquantel combination on Day 21 and FEC assessed on Day 35. The three farms were ...
Tapio H, Raekallio MR, Mykkänen A, Männikkö S, Scheinin M, Bennett RC, Vainio O.Medetomidine suppresses cardiovascular function and reduces gastrointestinal motility in horses mainly through peripheral α -adrenoceptors. Vatinoxan, a peripheral α -antagonist, has been shown experimentally to alleviate the adverse effects of some α -agonists in horses. However, vatinoxan has not been investigated during constant-rate infusion (CRI) of medetomidine in standing horses. Objective: To evaluate effects of vatinoxan on cardiovascular function, gastrointestinal motility and on sedation level during CRI of medetomidine. Methods: Experimental, randomised, blinded, cross-over stud...
Baggot JD.The route of administration and formulation of the dosage form affect the bioavailability (rate and extent of absorption) of a drug and may thereby influence the intensity and duration of the pharmacological effect. Location of injection site may affect the plasma concentration profile of drugs administered as aqueous suspensions or sustained release parenteral preparations (procaine penicillin G). When absorption influences the rate of elimination ('flip-flop' phenomenon), the apparent half-life of the drug will be increased (cefazolin sodium, i.m.; meclofenamic acid, p.o.). Absorption genera...
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 ...
Hébert L, Guitton E, Madeline A, Géraud T, Zientara S, Laugier C, Hans A, Büscher P, Cauchard J, Petry S.The aim of this study was to evaluate the ability of melarsomine hydrochloride (Cymelarsan) to cure horses suffering from a nervous form of dourine, a sexually-transmitted disease caused by Trypanosoma equiperdum. The recently described experimental model for assessing drug efficacy against horse trypanosomosis allowed us to obtain eight horses (Welsh pony mares) infected by T. equiperdum with parasites in their cerebrospinal fluid. The Cymelarsan treatment evaluated consisted of the daily administration of 0.5 mg/kg of Cymelarsan over 7 days. Two control horses remained untreated, three hor...
Rangel-Nava A, Ramírez-Uribe JM, Recillas-Morales S, Ibancovichi-Camarillo JA, Venebra-Muñoz A, Sánchez-Aparicio P.The objective of the study was to conduct a review of the pharmacological regulation and pharmacokinetic parameters of firocoxib when administered orally or intravenously in horses. A search for literature was done in SCOPUS and PubMed for studies that had to evaluate the pharmacological regulation as well as the pharmacokinetic parameters of firocoxib when administered in horses. The nonsteroidal anti-inflammatory drugs have analgesic, anti-inflammatory, antipyretics, and antiendotoxic effects. The newly developed is selective to COX2 characterized by less adverse effects in veterinary patien...
Winther L, Baptiste KE, Friis C.Cefquinome concentrations, following intravenous and aerosol administration to horses, in pulmonary epithelial lining fluid (PELF) were examined and compared to plasma concentrations. Single dose of cefquinome sulphate (1 mg/kg) was administered intravenously to six horses followed by a single aerosol administration (225 mg) with a wash-out period of 14 days between treatments. After each drug administration, cefquinome concentrations in plasma and PELF, obtained by intrabronchial cotton swabs, were determined. After intravenous administration, cefquinome concentrations in plasma declined fast...
Delguste C, Amory H, Guyonnet J, Thibaud D, Garnero P, Detilleux J, Lepage OM, Doucet M.Bioavailability and pharmacological effects of tiludronate were compared when administered as an intravenous (i.v.) bolus at a dosage of 0.1 mg/kg body weight (b.w.) once daily for 10 consecutive days (group 1, n = 6) and as a single constant rate infusion (CRI) at a total dose of 1 mg/kg b.w. (group 2, n = 6) in healthy adult horses. Tiludronate and carboxy-terminal cross-linking telopeptide of type I collagen (CTX-1) were measured in plasma and urine. There was no statistically significant difference in area under the curve (AUC) and clearance (Cl) between the two groups. Bioavailability of ...
Ryan CA, McNeal CD, Credille BC.Equine practitioners require recommendations that support antimicrobial stewardship and avoid generating resistance to medically important antibiotics. This review examines current inadequacies in antimicrobial stewardship standards within the veterinary community, related to antimicrobial categorisation and prescribing practices. Resistance to cephalosporin antibiotics in horses is also described. Properties of cephalosporin antibiotics are outlined and equine-specific studies of ceftiofur, a third-generation cephalosporin antibiotic with medical importance, are detailed. Readers are provided...
Vainionpää MH, Raekallio MR, Pakkanen SA, Ranta-Panula V, Rinne VM, Scheinin M, Vainio OM.To investigate plasma drug concentrations and the effect of MK-467 (L-659'066) on sedation, heart rate and gut motility in horses sedated with intravenous (IV) detomidine. Methods: Experimental randomized blinded crossover study. Methods: Six healthy horses. Methods: Detomidine (10 μg kg(-1) IV) was administered alone (DET) and in combination with MK-467 (250 μg kg(-1) IV; DET + MK). The level of sedation and intestinal sounds were scored. Heart rate (HR) and central venous pressure (CVP) were measured. Blood was collected to determine plasma drug concentrations. Repeated measures anova was ...
White G, Prior SD.A study was carried out on the bacteriological faecal flora of horses before and after oral doses of oxytetracycline or trimethoprim plus sulphadiazine. Administration of oxytetracycline was rapidly followed by large increases in counts of coliforms. Bacteroides and Streptococcus species, the disappearance of Veillonella species, the appearance of Clostridium perfringens type A in large numbers and the accumulation of watery fluid in the rectal contents. These changes were not seen following administration of trimethoprim-sulphadiazine and it was concluded that oral treatment of horses with th...
Rizk MA, El-Sayed SAE, Eltaysh R, Igarashi I.Equine piroplasmosis is a tick-transmitted disease that is considered one of the most serious infectious diseases affecting equines. Searching for novel antipiroplasm drugs remains indispensable due to the emergence and spreading of resistant piroplasm parasites against the limited currently used drugs, diminazene aceturate and imidocarb dipropionate. Therefore, novel drugs with specified targets need to be identified and exploited. The inhibitory effects of Medicines for Malaria Venture (MMV) Malaria Box compounds with potent in vitro anti-equine piroplasmosis activity were evaluated against ...
Matthews NS, Taylor TS, Hartsfield SM, Williams JD.Xylazine (1.1 mg/kg body weight [bwt])-ketamine (2.2 mg/kg bwt) (X/K) anaesthesia was evaluated, in nine Mammoth asses, for effectiveness and compared with two other injectable anaesthetic combinations: xylazine (1.1 mg/kg bwt)-butorphanol (0.044 mg/kg bwt)-ketamine (2.2 mg/kg bwt) (X/B/K); and xylazine (1.1 mg/kg bwt)-tiletamine-zolazepam (1.1 mg/kg bwt) (X/T). All drugs were given intravenously (i.v.). Heart rate, respiratory rate, systolic blood pressure, arterial blood pH, PCO2, PO2, recumbency time and number of attempts to stand were measured. Quality of induction and recovery, muscle re...
Love EJ, Taylor PM, Murrell J, Whay HR, Waterman-Pearson AE.The aim of this randomised, observer-blinded, crossover study was to compare the effects of six treatments, administered intravenously to six horses: saline and saline (S/S); detomidine and saline (D/S); detomidine and 5 µg/kg buprenorphine (D/B5); detomidine and 7.5 µg/kg buprenorphine (D/B7.5); detomidine and 10 µg/kg buprenorphine (D/B10); and detomidine and 25 µg/kg butorphanol (D/BUT). The detomidine dose was 10 µg/kg for all treatments in which it was included. Sedation was subjectively assessed and recorded on a visual analogue scale. Peak sedation, duration of sedation and the are...
Johnstone IB.Nonsteroidal anti-inflammatory drugs are commonly used in the treatment of inflammatory conditions, and have potential value in the treatment of thrombotic disease in the horse. This study compares the potency of three nonsteroidal anti-inflammatory drugs phenylbutazone, naproxen (equiproxen) and flunixin meglumine (banamine) with respect to their effects on equine platelets. Two functional responses of horse platelets were evaluated in vitro: their ability to aggregate and their ability to make available platelet factor 3 procoagulant activity. Flunixin at a concentration of 10(-6) M signific...
Crisman MV, Wilcke JR, Sams RA.To determine pharmacokinetic variables that describe the disposition of flunixin after i.v. administration of flunixin meglumine to foals < 24 hours old. Methods: 6 healthy foals, 2 males and 4 females (mean age, 11.6 hours; range, 6 to 22.5 hours). Methods: Flunixin (as flunixin meglumine) was administered to foals at a dosage of 1.1 mg/kg of body weight. Flunixin concentration in plasma samples was analyzed, using gas chromatography/mass spectroscopy. Concentration versus time profiles were analyzed according to standard pharmacokinetic techniques. Blood samples were obtained from foals by j...
Nieto JE, Spier S, Pipers FS, Stanley S, Aleman MR, Smith DC, Snyder JR.To compare effects of a commercially available omeprazole paste and a compounded omeprazole suspension on healing of gastric ulcers in Thoroughbred racehorses in active training. Methods: Randomized controlled trial. Methods: 32 horses with gastric ulcers. Methods: Horses were assigned to 2 groups on the basis of endoscopic gastric ulcer severity. Group-1 horses were treated with omeprazole suspension for 30 days and with omeprazole paste for an additional 30 days. Group-2 horses were treated with omeprazole paste for 30 days and omeprazole suspension for an additional 30 days. Serum omeprazol...
Haines GR, Brown MP, Gronwall RR, Merritt KA.Serum concentrations and pharmacokinetics of enrofloxacin were studied in 6 mares after intravenous (IV) and intragastric (IG) administration at a single dose rate of 7.5 mg/kg body weight. In experiment 1, an injectable formulation of enrofloxacin (100 mg/mL) was given IV. At 5 min after injection, mean serum concentration was 9.04 microg/mL and decreased to 0.09 microg/mL by 24 h. Elimination half-life was 5.33 +/- 1.05 h and the area under the serum concentration vs time curve (AUC) was 21.03 +/- 5.19 mg x h/L. In experiment 2, the same injectable formulation was given IG. The mean peak ser...
Mills PC, Cross SE.The rate and regional differences for the penetration of fentanyl through equine skin was investigated in vitro using a commercial transdermal therapeutic system (TTS) or 'patch'. Skin collected from the thorax, groin and leg (dorsal metacarpal) regions of five horses was placed in diffusion cells and a fentanyl TTS applied to each skin sample. Drug penetration through each skin sample over 48 h measured using high performance liquid chromatography (HPLC). Cumulative penetration (microg/cm2) was plotted against time (h) and used to regress the steady state flux (microg/cm2/h) of fentanyl throu...
Bermingham EC, Papich MG, Vivrette SL.To determine the pharmacokinetics of enrofloxacin administered IV and orally to foals. Methods: 5 clinically normal foals. Methods: A 2-dose cross-over trial with IV and oral administration was performed. Enrofloxacin was administered once IV (5 mg/kg of body weight) to 1-week-old foals, followed by 1 oral administration (10 mg/kg) after a 7-day washout period. Blood samples were collected for 48 hours after the single dose IV and oral administrations and analyzed for plasma enrofloxacin and ciprofloxacin concentrations by use of high-performance liquid chromatography. Results: For IV administ...
Lillich JD, Rakestraw PC, Roussel AJ, Finley MR, Ganta S, Freeman LC.To determine whether ether-a-go-go (ERG) potassium channels are expressed in equine gastrointestinal smooth muscle, whether ERG channel antagonists affect jejunal muscle contraction in vitro, and whether plasma cisapride concentrations in horses administered treatment for postoperative ileus (POI) are consistent with ERG channels as drug targets. Methods: Samples of intestinal smooth muscle obtained from 8 horses free of gastrointestinal tract disease and plasma samples obtained from 3 horses administered cisapride for treatment of POI. Methods: Membranes were prepared from the seromuscular la...
Davis JL, Messenger KM, LaFevers DH, Barlow BM, Posner LP.The purpose of this study was to determine the pharmacokinetics of buprenorphine following intravenous (i.v.) and intramuscular (i.m.) administration in horses. Six horses received i.v. or i.m. buprenorphine (0.005 mg/kg) in a randomized, crossover design. Plasma samples were collected at predetermined times and horses were monitored for adverse reactions. Buprenorphine concentrations were measured using ultra-performance liquid chromatography with electrospray ionization mass spectrometry. Following i.v. administration, clearance was 7.97±5.16 mL/kg/min, and half-life (T(1/2)) was 3.58 h (ha...
Elfenbein JR, Robertson SA, Corser AA, Urion RJ, Sanchez LC.Ketamine as continuous rate infusion (CRI) provides analgesia in hospitalized horses. Objective: Determine effects of prolonged CRI of ketamine on gastrointestinal transit time, fecal weight, vital parameters, gastrointestinal borborygmi, and behavior scores in healthy adult horses. Methods: Seven adult Thoroughbred or Thoroughbred cross horses, with permanently implanted gastric cannulae. Methods: Nonblinded trial. Random assignment to 1 of 2 crossover designed treatments. Ketamine (0.55 mg/kg IV over 15 minutes followed by 1.2 mg/kg/h) or lactated Ringer's solution (50 mL IV over 15 minutes ...
Passler NH, Chan HM, Stewart AJ, Duran SH, Welles EG, Lin HC, Ravis WR.The purpose of this study was to assess safety and alterations in body fluid concentrations of voriconazole in normal horses on days 7 and 14 following once daily dose of 4 mg/kg of voriconazole orally for 14 days. Body fluid drug concentrations were determined by the use of high performance liquid chromatography (HPLC). On day 7, mean voriconazole concentrations of plasma, peritoneal, synovial and cerebrospinal fluids, aqueous humor, epithelial lining fluid (ELF), and urine were 1.47 +/- 0.63, 0.61 +/- 0.22, 0.70 +/- 0.20, 0.62 +/- 0.26, 0.55 +/- 0.32, 79.45 +/- 69.4, and 1.83 +/- 0.44 microg...
Lees P, Serrano L.1 The butyrophenone tranquilizer, azaperone, was administered intramuscularly, at dose levels of 0.4 and 0.8 mg/kg, to ponies and its effects on cardiovascular and respiratory functions assessed. 2 Arterial blood pH, CO2 tension (PaCO2) and O2 tension (PaO2) remained relatively constant throughout the course of action of azaperone. 3 Azaperone did not modify plasma protein concentration but venous blood packed cell volume and haemoglobin concentration were reduced by 5 to 10% for at least 4 hours. These changes were probably caused by uptake of erythrocytes into the splenic reservoir. 4 Small ...
Van Duijkeren E, Vulto AG, Van Miert AS.The indications for use, side-effects, and pharmacokinetic parameters of trimethoprim, sulfonamides and their combinations in the horse are reviewed. Trimethoprim/sulfonamide (TMPS) combinations are used for the treatment of various diseases caused by gram-positive and gram-negative bacteria, including infections of the respiratory tract, urogenital tract, alimentary tract, skin joints and wounds. TMPS combinations can be administered orally, since absorption from the gastrointestinal tract is relatively good. However, peak serum concentrations can vary significantly between individual horses....
Koivunen AL, Maisi P, Konttinen YT, Prikk K, Sandholm M.The collagenolytic activity and its sensitivity to doxycycline inhibition in tracheal aspirates (TA) of horses with chronic obstructive pulmonary disease (COPD) was analyzed with SDS-PA gel electrophoresis (SDS-PAGE), using Type 1 collagen as the substrate. Both autoactive and total collagenase activities were significantly higher in TAs of horses with symptomatic COPD than in TAs of healthy horses. Doxycycline inhibition studies suggest that most of the TA collagenase is of the neutrophil type (MMP-8), but some is derived from other cells such as fibroblasts and monocyte/macrophages (MMP-1) a...
Schatzman U, Armbruster S, Stucki F, Busato A, Kohler I.The analgesic potency of butorphanol 25 microg/kg bodyweight (BW) and levomethadone 100 microg/kg BW, administered together with detomidine 10 microg/kg BW, was measured in twelve Warmblood horses in a randomized, blinded cross-over study. Detomidine with saline 10 ml 0.9% was used as placebo. The nociceptive threshold was determined using a constant current and a pneumatic pressure model for somatic pair Detomidine alone and in combination with butorphanol or levomethadone caused a significant temporary increase (P < 0.05) of the nociceptive threshold with a maximum effect within 15 min and a...
