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Topic:Pharmacology
Pharmacology in horses involves the study and application of drugs and medications to diagnose, treat, and prevent diseases and conditions in equine species. This field encompasses the understanding of pharmacokinetics and pharmacodynamics specific to horses, including how drugs are absorbed, distributed, metabolized, and excreted by the equine body. Commonly studied pharmacological agents in horses include non-steroidal anti-inflammatory drugs (NSAIDs), antibiotics, sedatives, and anthelmintics. Research in equine pharmacology focuses on determining appropriate dosages, understanding drug interactions, and minimizing adverse effects. This page compiles peer-reviewed research studies and scholarly articles that investigate the efficacy, safety, and regulatory aspects of pharmacological interventions in equine veterinary practice.
Behavioural changes in stabled horses given nontherapeutic levels of virginiamycin. Abnormal behaviour commonly develops in intensively managed horses. A possible cause is the change in diet occurring when the horse is stabled. An experiment was performed to examine this possibility by manipulating the diet with the feed supplement virginiamycin, as Founderguard. During 4 weeks, 18 horses were fed diets ranging from hay alone to concentrate plus hay in the ratio of 3:1. The rations of half the horses given concentrate were supplemented with Founderguard. Horses eating high concentrate rations displayed abnormal oral behaviours at a higher frequency than those eating only hay....
Influence of tidal volume and positive end-expiratory pressure on inspiratory gas distribution and gas exchange during mechanical ventilation in horses positioned in lateral recumbency. To study effects of intermittent positive-pressure ventilation (IPPV) with large tidal volumes and addition of positive end-expiratory pressure (PEEP) on maldistribution of ventilation in anesthetized horses positioned in lateral recumbency. Methods: 6 healthy adult horses. Methods: Anesthesia was induced by i.v. infusion of thiopental sodium and guiafenesin and was maintained with supplemental doses of thiopental and i.v. infusion of chloral hydrate. Functional separation of the lungs was achieved, using a tube-in-tube intubation technique. Intermittent positive-pressure ventilation of both l...
Effect of alpha 2-adrenergic, cholinergic, and nonsteroidal anti-inflammatory drugs on myoelectric activity of ileum, cecum, and right ventral colon and on cecal emptying of radiolabeled markers in clinically normal ponies. To determine effect of xylazine hydrochloride (XYL), yohimbine hydrochloride (YOH), bethanechol chloride (BET), neostigmine methyl sulfate (NEO), or flunixin meglumine (FLU) on ileocecocolic myoelectric activity and passage of radiolabeled markers from the cecum. Methods: 6 healthy adult ponies. Methods: A cecal cannula was surgically implanted, and 12 were sutured to the ileum, cecum, and right ventral colon. After a 12-hour nonfeeding period, 370 MBq of technetium 99m-labeled sulfur colloid in egg albumen and 37 MBq of indium 111-labeled diethyltriaminepentaacetic acid in 60 ml of water were...
Effect of erythromycin lactobionate on myoelectric activity of ileum, cecum, and right ventral colon, and cecal emptying of radiolabeled markers in clinically normal ponies. To determine the effect of erythromycin lactobionate (ERY) on ileocecocolic myoelectric activity and passage of radiolabeled markers from the cecum. Methods: 6 healthy adult ponies. Methods: After a 12-hour nonfeeding period, 370 MBq of technetium 99m-labeled sulfur colloid in egg albumen and 37 MBq of indium 111-labeled diethyltriaminepentaacetic acid in 60 ml of water were administered directly into the cecal apex. The following drug concentrations were tested: ERY, 0.01, 0.10, 1.0, and 10.0 mg/kg of body weight; ERY, 0.10 mg/kg bolus; and saline (0.9% NaCl) solution, 10 ml. All treatments, ...
Determination of butorphanol in horse race urine by immunoassay and gas chromatography-mass spectrometry. An analytical procedure to screen butorphanol in horse race urine using ELISA kits and its confirmation by GC-MS is described. Urine samples (5 ml) were subjected to enzymatic hydrolysis and extracted by solid-phase extraction. The residues were then evaporated, derivatized and injected into the GC-MS system. The ELISA test (20 microl of sample) was able to detect butorphanol up to 104 h after the intramuscular administration of 8 mg of Torbugesic, and the GC-MS method detected the drug up to 24 h in FULL SCAN or 31 h in the SIM mode. Validation of the GC-MS method in the SIM mode using nalbup...
Persistent desensitisation of the beta 2 adrenoceptors expressed by cultured equine sweat gland epithelial cells. Adrenaline, forskolin and ATP all evoked accumulation of cyclic AMP in equine sweat gland epithelial cells, although the response to adrenaline was more transient than that to forskolin and ATP. Cells preincubated in adrenaline (10 micromol l-1, 32 min) showed essentially complete, homologous desensitisation, and this phenomenon reversed slowly (half-time 6.3+/-0.9 h). After 10 min of recovery from preincubation in adrenaline, isobutylmethylxanthine (IBMX, 5 mmol l-1) had no effect upon the desensitisation and the cells showed no loss of sensitivity to ATP and forskolin. After 10 h, however, t...
Inhibition and inactivation of equine aromatase by steroidal and non-steroidal compounds. A comparison with human aromatase inhibition. In order to approach the detailed structure-function relationships of aromatase, we studied the inhibitory and inactivatory potencies of several steroidal androstenedione analogues (1: 4-hydroxyandrostenedione, 2: 4-acetoxyandrostenedione and 3: 7 alpha-(4'-amino)phenylthio-4-androstene-3, 17-dione) and non-steroidal imidazole derivatives (4: ketoconazole, 5: miconazole and 6: fadrozole) on equine aromatase in placental microsomes, a well established mammalian model. Human placental microsomes and the purified enzyme from equine testis were also used to compare inhibition by 1 and 2. In equine...
A toxicity study of eltenac, a nonsteroidal anti-inflammatory drug, in horses. A double-blind study was performed, in horses, to determine the potential toxic effects of the nonsteroidal anti-inflammatory drug, eltenac(4-[(2,6-dichlorophenyl) amino]-3-thiopheneacetic acid). Four treatment groups of six horses were formed. The drug was injected intravenously, once daily, at a dose level of 0.5 mg/kg, 1.5 mg/kg or 2.5 mg/kg for 15 days. A control group was injected with sterile saline solution. Horses were monitored for changes in appetite, physical examinations, biochemical evaluations and gastroscopic examinations. Complete post-mortem examinations were also performed. A...
Efficacy of moxidectin 2% equine gel against natural nematode infections in ponies. The efficacy of moxidectin 2% oral gel (Equest, Fort-Dodge) against European worm strains was studied through post-mortem worm counts and feacal egg counts (FECs) in 12 young ponies naturally infected. The animals were allocated in two groups of six ponies each: the first one was treated at 0.4 mg/kg b.w. and the second one received a placebo and served as control. All the ponies were necropsied 14 days post-treatment. The efficacy of moxidectin in reducing strongyle FECs ranged from 99.8% to 100% from 3 to 14 days after treatment. Moxidectin efficacy was 100% against Trichostrongylus axei and...
The reappearance of strongyle eggs in the faeces of horses after treatment with moxidectin. The reappearance of strongyle eggs in the faeces of horses treated with moxidectin (0.4 mg/kg of body weight) was compared with that in the faeces of horses treated with ivermectin (0.2 mg/kg of body weight). The study was performed from December 1995 till June 1996. Horses were infected naturally in the preceding grazing period. Two groups of 24 horses each were treated with moxidectin and ivermectin respectively at week 0. No side effects were seen after treatment. Horses were housed from week -1 till week 17. From week 17 onwards the horses were on pasture. Faecal samples were taken from ea...
Duration of effects of phenylbutazone on serum total thyroxine and free thyroxine concentrations in horses. The objectives of this study were to determine if phenylbutazone decreased serum thyroxine (TT4) and free thyroxine (FT4) concentrations using radioimmunoassay and equilibrium dialysis techniques in horses, and, if so, an additional objective was to determine the duration of this decreased concentration once phenylbutazone administration was discontinued. Serum TT4 and FT4 concentrations were determined before and after administration of 4.4 mg/kg of phenylbutazone i.v. bid for 5 days. Treatment with phenylbutazone caused a significant decrease in TT4 and FT4 concentrations (P < .05). Serum...
Effects of enantiomers of beta 2-agonists on ACh release and smooth muscle contraction in the trachea. The beta 2-agonists currently used as bronchodilators are racemic mixtures of R- and S-enantiomers. In the present study, we examined the effects of enantiomers of the beta 2-agonists albuterol and formoterol on acetylcholine (ACh) release from equine trachealis parasympathetic nerves. ACh release was evoked by electrical field stimulation (20 V, 0.5 ms, 0.5 Hz) and measured by high-performance liquid chromatography coupled with electrochemical detection. We also tested the effects of enantiomers of albuterol and formoterol on equine tracheal smooth muscle (TSM) contraction in response to exog...
Plasma pharmacokinetics of ranitidine HCl in foals. Plasma pharmacokinetics of ranitidine HCl were investigated after intravenous (i.v.) and oral (p.o.) administration of drug to six healthy foals. Twelve- to sixteen-week-old foals received 2.2 mg ranitidine/kg i.v. and 4.4 mg ranitidine/kg p.o. Concentrations of ranitidine were determined using normal phase high performance liquid chromatography. Plasma concentrations of ranitidine HCl declined from a mean of 3266 ng/mL at 5 min to 11 ng/mL at 720 min after administration. The profile of the plot of concentrations of ranitidine HCl vs. time was best described by a two-exponent equation for two...
Effect of platelet-activating factor antagonist L-691,880 on low-flow ischemia-reperfusion injury of the large colon in horses. To determine the effect of platelet-activating factor (PAF) antagonist L-691,880 on low-flow ischemia and reperfusion (I-R) of the large colon in horses. Methods: 12 adult horses. Methods: Horses were anesthetized, and the large colon was exteriorized through a ventral median celiotomy and instrumented. Colonic arterial blood flow was reduced to 20% of baseline (BL) and maintained for 3 hours; flow was then restored, and the colon was reperfused for 3 hours. One of two solutions was administered intravenously 30 minutes before reperfusion: group 1, 10 mL/kg 0.9% NaCl; and group 2, 5 mg/kg PAF ...
Treatment of superficial ulcerative squamous cell carcinoma in three horses with topical 5-fluorouracil. Three horses with superficial ulcerative squamous cell carcinoma were successfully treated with topical 5-fluorouracil. Two of them remain in remission after a single course of treatment and the third case is controlled by the application of the cream for seven days every six weeks. No systemic side-effects were observed but there was a localised inflammatory reaction in the skin in each case.
In vitro responses to noradrenaline of small intestine taken from normal and grass sickness-affected horses. Small intestine was taken from the caudal flexure of the duodenum and the terminal ileum proximal to the ileocaecal fold of 25 horses, 9 with acute grass sickness (AGS), 12 with subacute grass sickness (SAGS) and 12 with chronic grass sickness (CGS). The motility in the samples was measured isometrically either within 1 h of death or after storage for 24 h at 4 degree C. In control tissue, noradrenaline produced contractions of muscle strips which did not involve a muscarinic cholinergic mechanism and which were unaffected by the alpha 1 antagonist prazosin but were blocked by the alpha 2 anta...
Role of oligosaccharides in the pharmacokinetics of tissue-derived and genetically engineered cholinesterases. To understand the role of glycosylation in the circulation of cholinesterases, we compared the mean residence time of five tissue-derived and two recombinant cholinesterases (injected intravenously in mice) with their oligosaccharide profiles. Monosaccharide composition analysis revealed differences in the total carbohydrate, galactose, and sialic acid contents. The molar ratio of sialic acid to galactose residues on tetrameric human serum butyrylcholinesterase, recombinant human butyrylcholinesterase, and recombinant mouse acetylcholinesterase was found to be approximately 1.0. For Torpedo ca...
Effects of hypochlorous acid and ascorbic acid on conductance, permeability, and structure of equine colonic mucosa in vitro. To study effects of hypochlorous acid (HOCl) on equine colonic mucosa in vitro, and determine whether addition of ascorbic acid protects against the effects. Methods: 6 healthy horses and ponies. Methods: Short-circuit current was measured in mucosa mounted in Ussing chambers. Incubation conditions were: control (no additions); 5 mM HOCl; 1 mM HOCl; same and 5 mM ascorbic acid; 3 mM HOCl; 3 mM HOCl and 5 mM ascorbic acid; 7 mM HOCl; and 7 mM HOCl plus 5 mM ascorbic acid. Permeability was measured with [3H]mannitol and, at the conclusion of each experiment, tissues were examined microscopically...
Cardiorespiratory effects of sevoflurane, isoflurane, and halothane anesthesia in horses. To determine and compare cardiorespiratory and recovery effects of sevoflurane, isoflurane, and halothane in horses. Methods: 8 clinically normal horses (4 mares, 4 geldings), 5 to 12 years old. Methods: Inhalation anesthesia was maintained for 90 minutes with sevoflurane, isoflurane, or halothane. Anesthesia depth was maintained at 1.5 minimum alveolar concentration of halothane, isoflurane, and sevoflurane, then was reduced at 30 and 60 minutes. A surgical plane of anesthesia was reinduced by administration of ketamine or thiopental or by increasing the fractional inspired concentration of s...
Evaluation of some parameters influencing the drug delivery from a dry powder inhalation device using an in vitro model of the horse airways. The aim of this study was to determine the effect of breathing pattern, air humidity and position of the device on the delivery of an aerosol generated by a dry powder inhalation (DPI) device (Inhalator M). The in vitro inhalation study was performed using the cascade impaction method (Andersen Sampler) adapted to imitate nasal breathing. The amount of ipratropium found in the device, the artificial upper airways and the six stages of the Andersen Sampler was measured using high precision liquid chromatography. Stage 1 of the Andersen Sampler was considered to be the respirable fraction and st...
[Doping test for racehorses in Japan]. The doping test method used in a horse race requires the accurate detection of a wide variety of drugs and metabolites as well as the rapidity in order to examine a large number of samples within a limited time. For this purpose, the routine method consists of a preliminary screening and a confirmatory test. In this paper, a historical review for the development of the doping test method in Japan is described. The metabolism and pharmacology of drugs in horses are also discussed.
Aerosol therapy in the equine species. Inhalation therapy plays an increasing role in the management of equine respiratory disorders. This alternative to systematic treatment permits a high concentration of medication to act locally while minimizing side effects and residues. In human medicine, literature in this field is prolific and continuously renewed, whereas in veterinary medicine, applications of aerosol therapy are less extensive. This review considers the principles of action of the different types of devices used for inhalation, i.e., nebulization, metered-dose inhalation and dry powder inhalation, describes the technical...
[Effect of flunixin meglumine on plasma prostanoid concentrations in horses with colic in the perioperative period]. In the present study the significance of eicosanoids in the development of shock in horses on the basis of ileus has been investigated using the prostanoids thromboxane B2 (TXB2) and prostaglandine E2 (PGE2) as indicators. The prostanoid synthesis inhibitor flunixin meglumine was to be examined regarding its efficacy in the effective blockade of the synthesis of these mediators within the peri-operative timeframe as well as its effects on clinical signs and laboratory parameters. 21 horses suffering from ileus and ready for surgical intervention received an intravenous flunixin dosis of 1.1 mg...
Mechanism of capsaicin-induced relaxation in equine tracheal smooth muscle. The effects of capsaicin and neuropeptides were examined in equine tracheal smooth muscle (TSM). Neither capsaicin nor substance P (SP) contracted TSM. Capsaicin (100 microM) elicited relaxation in TSM contracted with methacholine. This relaxation was not mimicked by SP or calcitonin gene-related peptide (CGRP). Relaxation was not attenuated by removal of the epithelium or by pretreatment of tissue with meclofenamate or the nitric oxide (NO) synthase inhibitor NG-nitro-L-arginine. Previous exposure of TSM to capsaicin did not eliminate the relaxation responses to subsequent capsaicin. Although...
Technical validation of a face mask adapted for dry powder inhalation in the equine species. Development of dry powder inhalation (DPI) for horses requires the use of an adapted face mask. In experiment I, 4 masks (A, B, C and D) were tested and factors influencing the delivery of the dry powder were determined. Mask A was one which is commercially available for metered-dose inhalation. Mask B had the same shape as Mask A but an airtight rubber seal was added for the connection between the mask and horse's head. Mask C was a prototype adapted for DPI with connection for the DPI device between the nostrils, airtight expiratory valves in front of each nostril and airtight rubber seal to...
Effects of omeprazole on healing of naturally-occurring gastric ulcers in thoroughbred racehorses. Seventeen Thoroughbred horses with moderate to severe gastric ulceration were purchased from a race track within 10 days of racing and were treated once daily with either omeprazole (9 horses) or vehicle (8 horses) and evaluated gastroscopically for ulcer healing. Horses were administered omeprazole (1.5 mg/kg bwt/day) or vehicle by nasogastric tube once daily. Gastroscopic examination was performed on Days 0, 4, 7, 11, 14, 17, 21, 24 and 28, until lesions healed completely. Selected images of gastric lesions were captured by computer at each endoscopic examination, with a measuring caliper in...
