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.
Benbarek H, Ayad A, Deby-Dupont G, Boukraa L, Serteyn D.The purpose of this study was to explore the potential modulation of equine neutrophil oxidative burst by a series of classical NSAIDs which was subsequently monitored by the luminol or lucigenin-enhanced chemiluminescence (CL) technique. A significant dose-dependent inhibition of the luminol CL was observed with the majority of investigated drugs. This inhibition was very significant for phenylbutazone and Indomethacin; while for aspirin, a higher concentration is required. The action of Ketoprofen was significant during the first 5 min and only when the concentration was above 1 mM. Indometh...
Bonin CP, Baccarin RY, Nostell K, Nahum LA, Fossum C, de Camargo MM.Engagement of Toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS) is a master trigger of the deleterious effects of septic shock. Horses and humans are considered the most sensitive species to septic shock, but the mechanisms explaining these phenomena remain elusive. Analysis of tlr4 promoters revealed high similarity among LPS-sensitive species (human, chimpanzee, and horse) and low similarity with LPS-resistant species (mouse and rat). Four conserved nuclear factor kappa B (NFκB) binding sites were found in the tlr4 promoter and two in the md2 promoter sequences that are likely to be t...
Handing KB, Shabalin IG, Szlachta K, Majorek KA, Minor W.Serum albumin (SA) is the main transporter of drugs in mammalian blood plasma. Here, we report the first crystal structure of equine serum albumin (ESA) in complex with antihistamine drug cetirizine at a resolution of 2.1Å. Cetirizine is bound in two sites--a novel drug binding site (CBS1) and the fatty acid binding site 6 (CBS2). Both sites differ from those that have been proposed in multiple reports based on equilibrium dialysis and fluorescence studies for mammalian albumins as cetirizine binding sites. We show that the residues forming the binding pockets in ESA are highly conserved in h...
Dillon AM, Heath MF.The effects of the protein tyrosine kinase inhibitors tyrphostins B42 and B46 on equine platelet function and protein tyrosine phosphorylation (PTP) were assessed. Tyrphostins B42 and B46 (both at 100 microM concentration) produced significant inhibition of thrombin-stimulated equine platelet aggregation. The effect of tyrphostin B46 was also time-dependent. The same concentration of these inhibitors produced very little or no inhibition of platelet-activating factor (PAF)-induced aggregation. The effects of tyrphostins B42 and B46 on thrombin- and PAF-stimulated PTP were generally similar, al...
Martin F, Eydal M, Höglund J, Tydén E.The equine roundworm Parascaris univalens has developed resistance to the three anthelmintic substances most commonly used in horses. The mechanisms responsible for resistance are believed to be multi-genic, and transport proteins such as the P-glycoprotein (Pgp) family have been suggested to be involved in resistance in several parasites including P. univlaens. To facilitate further research into the mechanisms behind drug metabolism and resistance development in P. univalens we aimed to develop an in vitro model based on larvae. We developed a fast and easy protocol for hatching P. univalens...
Hinrichs K, Riera FL.Ten mares were used to investigate the effect of administration of prostaglandin F2 alpha on uterine tubal motility, as reflected by embryo recovery from the uterus 5 days after ovulation (day 0). Mares were assigned to 3 groups: group A, uterine flush for embryo recovery on day 7; group B, uterine flush for embryo recovery on day 5; and group C, uterine flush for embryo recovery on day 5, after treatment with prostaglandin F2 alpha (10 mg, IM) on day 3. Each mare was assigned to each group once. Embryo recovery rates for the 3 groups were: A, 6 of 10; B, 2 of 8; and C, 0 of 10. The embryo rec...
Flammini L, Mantelli L, Volpe A, Domenichini G, Di Lecce R, Dondi M, Cantoni AM, Barocelli E, Quintavalla F.Rifaximin is an unabsorbed oral antibiotic showing anti-inflammatory properties in human pathologies like irritable bowel syndrome and inflammatory bowel disease. In veterinary medicine, rifaximin is primarily used in the treatment of dermatological diseases in all animal species, in therapy and prophylaxis of mastitis in cows and in the treatment of endometritis in cattle and horses. The aim of this preliminary study was to evaluate the anti-inflammatory properties of rifaximin on primary cell cultures from bovine endometrium in which inflammatory response was induced by Lipopolysaccaride (LP...
Drudge JH, Lyons ET, Tolliver SC.Critical tests were carried out in 10 horses to evaluate the antiparasitic activity of febantel given alone or with trichlorfon. Paste formulations were administered intraorally at dose levels of 6 mg of febantel (active ingredient)/kg and 35 mg of trichlorfon (active ingredient)/kg. In 5 tests with febantel alone, removal of 100% was recorded for mature or immature Parascaris equorum from 2 infected horses. Strongylus vulgaris from 4 infected horses, S edentatus from 5 infected horses, and mature Oxyuris equi from 1 infected horse; and removal of 96% was recorded for small strogyles from 1 ho...
Walters B, Trumble TN, Wendt-Hornickle E, Kennedy M, Guedes A.Apoptosis is an important mechanism underlying chondrocyte loss in osteoarthritis that could be affected by modulation of lipid signaling via inhibition of cyclooxygenases (COX) and soluble epoxide hydrolase (sEH). Objective: To determine the impact of inhibiting COX and sEH alone or in combination on apoptosis of equine chondrocytes. Methods: Cultured primary equine chondrocytes were subjected to serum deprivation or incubation with 1 μg/ml tunicamycin for 24 h to induce apoptosis via caspase activation and endoplasmic reticulum (ER) stress, respectively. Cells were treated with the non-se...
Helal IE, Al-Abbadi HA, El-Daharawy MH, Ahmed MF.Delayed healing associated with distal limb wounds is highly challenging in equine clinical practice. This study aimed to evaluate healing rates between chronic non-granulating wounds of horse distal limbs that were treated with maltodextrin/ascorbic acid gel alone or in combination with povidone-iodine 1% solution and those treated with povidone-iodine 1% only throughout the study period (35 days) in clinical settings. The study was conducted on 18 adult horses (3-15 years old). Based on the treatment regimen utilized, the horses were divided into three groups (n = 6), with each group having ...
Berardinelli P, Barazzoni AM, Russo V, Brunetti O, Della Torre G, Scapolo PA, Muttini A, Bortolami R.Based on previous observations that capsaicin can selectively damage group III and IV afferents and induce muscle fibre transformation, we hypothesized that eliminating, by means of capsaicin, the group III and IV afferents of a peripheral territory it could lead to a fibre transformation in a muscle involved in the flexor reflexes of the same peripheral territory. Therefore, capsaicin was injected into the palmar nerves of the forelimb of the horse to investigate if eliminating group III and IV afferents from the hand of the horse a muscle fibre transition would occur in the flexor carpi radi...
Stewart DR, Papkoff H.It has been previously determined that the equine placenta is the sole significant source of relaxin during pregnancy and that relaxin immunoactivity is also present in term placentas. Therefore, placentas obtained at the time of foaling were selected for starting material for purification of equine relaxin. Frozen whole placentas were ground and then extracted with 0.5 N HCl-85% acetone. Relaxin was precipitated by raising the acetone concentration to 97%. Equine relaxin was further purified by stepwise elution ion exchange, gel filtration, and gradient elution ion exchange chromatographies a...
Koenig J, Cote N.Colic is a common problem encountered in equine practice. Alteration of gastrointestinal motility is often the underlying cause for abdominal pain. Gastrointestinal motility can be measured as myoelectric activity, mechanical activity, and transit of intraluminal contents. Regulation of motility is based on a complex interaction between central innervation, autonomic innervation, and the enteric nervous system. Various humoral and neurochemical substances are required to interact flawlessly to allow propulsive motility. Ileus is defined as the absence of propulsive aboral movement of gastroint...
Roscher KA, Failing K, Schenk I, Moritz A.The reasons for this prospective experimental study were to determine a dosing scheme with loading and maintenance dose of aspirin inducing inhibition of platelet function measured by whole blood impedance aggregometry. Ten horses received aspirin orally in the morning with one loading dose of 4.7-5 mg/kg and maintenance doses of 1-1.3 mg/kg daily the following 4 days. Aggregometries (COLtest, ASPItest, ADPtest) and serum salicylic acid were measured. ASPItest showed significant difference in inhibition at 24 and 48 hr (p < .05) and 96 hr (p < .01). Significant change for ADPtes...
Decloedt A, Broux B, De Clercq D, Deprez P, Van Steenkiste G, Vera L, Ven S, van Loon G.Based on its pharmacokinetic profile and electrophysiological effects in healthy horses, sotalol potentially could be used as a long-term PO antiarrhythmic drug in horses. Objective: To evaluate the effect of sotalol on heart rate (HR), QT interval, atrial fibrillatory rate, and success of cardioversion in horses with naturally occurring chronic atrial fibrillation (AF). Methods: Twenty-eight horses referred for transvenous electrical cardioversion of AF were treated with 2 mg/kg sotalol PO q12h for 3 days before cardioversion, and 13 horses underwent the same protocol without sotalol administ...
Lester GD, Rice BL.To determine effects of leukotriene (LT) C(4) on ion transport across equine tracheal epithelium. Sample-Tracheal epithelium from cadavers of 24 horses considered free of respiratory tract disease. Methods: Mucosae were mounted into Ussing chambers, and short-circuit current (I(sc)) was monitored over time. Effects of LTC(4) were examined for various conditions, including addition of amiloride (10μM) to the mucosal bath solution, addition of bumetanide (10μM) to the serosal bath solution, addition of barium (1mM) to the serosal bath solution, and substitution of gluconate for chloride and HE...
Wijnberg ID, van der Kolk JH.Atrial fibrillation is a disorder of cardiac rhythmicity, and its importance in the horse depends on the underlying cause and the function of the horse. Before the decision is taken to start treatment, it has first to be ascertained whether treatment is worthwhile and whether the horse is an appropriate candidate for treatment. This article gives a short overview of current opinion on the cause and treatment of atrial fibrillation in the horse. The most used treatment at the moment, oral chinidine sulphate, is discussed. The hemodynamic consequences of atrial fibrillation and the response of a...
Georgi JR, Rendano VT, King JM, Bianchi DG, Theodorides VJ.Albendazole was effective in destroying Strongylus vulgaris larvae in verminous lesions of the cranial mesenteric artery when administered as a 20% suspension by stomach tube to ponies. Fifty mg/kg body weight administered twice a day for 2 days caused death and gradual disintegration of larvae over a period of 3 to 6 weeks with mild toxic signs appearing in 3 of 11 ponies. Higher total doses of albendazole (50 mg/kg twice a day for 4 days and 25 mg/kg three times a day for 5 days) lead to more rapid disintegration of the larvae but fatal toxicity was observed in 3 of 6 ponies so treated. In a...
Coomer RPC, Terschuur JA, Pressanto MC, Walker I.To assess the efficacy of commercial intra-articular blood-derived allogeneic-induced mesenchymal stem cells (CIMSCs) to treat tarsometatarsal lameness in horses. Methods: This was a retrospective cohort study. Methods: Records from 167 adult light breed horses with bilateral tarsometatarsal lameness. Methods: Horses with tarsometatarsal lameness were retrospectively selected from medical records. Diagnosis followed subjective graded lameness assessment before and after intra-articular analgesia, with graded radiographic tarsal examination. Horses were excluded if they were diagnosed or treate...
Stammwitz V, Honnens Ä, Hochhuth D, Schuberth HJ.Between 2015 and 2017, a marked increase of anaphylactic-like reactions after intravenous administration of gentamicin was observed first in horses and, later, also in humans. This worldwide issue led to safety measures including product recalls and safety warnings. Here, a German Marketing Authorization Holder (MAH) of an early and intensely affected veterinary product containing gentamicin describes the clinical approach of the company to analyze the root cause and identify the causative agent in the active pharmaceutical ingredient (API). The pharmacovigilance data of the MAH are presented,...
Meier A, de Laat M, Reiche D, Fitzgerald D, Sillence M.A previous six-week (wk) study demonstrated the potential of the sodium-glucose linked transport inhibitor velagliflozin as a novel treatment for equine insulin dysregulation. The present study examined the safety and efficacy of velagliflozin over 16 wk. of treatment, and over 4 wk. of withdrawal. Twenty-four insulin dysregulated ponies were selected, based on their hyper-responsiveness to a diet challenge meal containing 3.8 g non-structural carbohydrates (NSC)/kg bodyweight (BW). Ponies with serum insulin > 90 μIU/mL either 2 or 4 h after feeding were enrolled, and randomly allocated...
Davis JL, Posner LP, Elce Y.A 24-year-old 732-kg (1,610-lb) pregnant Belgian draft horse mare developed neuropathy and signs of intractable pain following colic surgery. Results: Following recovery from colic surgery to treat compression of the small and large intestines because of a large fetus, the mare was noticed to have signs of femoral neuropathy involving the left hind limb. Within 36 hours after recovery, the mare developed signs of severe pain that were unresponsive to conventional treatment. No gastrointestinal tract or muscular abnormalities were found, and the discomfort was attributed to neuropathic pain. Re...
McDonnell SM.This study is part of ongoing work toward developing pharmacological methods for enhancing and inducing ejaculation in stallions with ejaculatory dysfunction or disabilities that interfere with normal breeding behavior. The objective was to evaluate a treatment regimen involving oral imipramine followed by intravenous xylazine that, in uncontrolled field clinical trials, had shown promise for a higher rate of ejaculation and fewer side effects using a more easily obtained and administered form of imipramine. Eight stallions each underwent eight trials in which treatment consisted of imipramine...
Hajek P, Ungemach FR, Abraham G.Muscarinic acetylcholine receptor (mAChR)-mediated guanine nucleotide-binding regulatory protein (G protein) activation and the functional interaction between receptors and the respective G proteins were investigated using an agonist-induced [(35)S]guanosine-5'-O-(gamma-thiotriphosphate) ([(35)S]GTPgammaS)-binding approach in membranes of 3 native equine airway segments (trachea, bronchus and lung), which differ tremendously in mAChR density and subtype distribution; especially subtypes that couple negatively to adenylyl cyclase through G(i/0) proteins, i.e. M(2) receptors. The assay was initi...
Vergara-Hernandez FB, Panek CL, Nielsen BD, Robison CI, Colbath AC.To determine the effects of clodronate disodium (CLO) on control and recombinant equine interleukin-1β (IL-1β)-treated equine joint tissues. Methods: In vitro experimental study. Methods: Cartilage explants, chondrocytes, and synoviocytes (n = 3 horses). Methods: Monolayer cultures of chondrocytes and synoviocytes from three horses were subjected to: control media (CON), 5 ng/ml CLO (C/low), 50 ng/ml CLO (C/med), 100 ng/ml CLO (C/high), with and without IL-1β, and 10 ng/ml IL-1β (IL) alone for 72 hours. Cartilage explants from three horses were subjected to CON, IL, C/low, and C/...
Dimaio Knych HK, Steffey EP, Stanley SD.Yohimbine is an alpha 2 adrenergic receptor antagonist, which has been shown to counteract the CNS depressant effects of alpha 2 receptor agonists in a number of species. Recently, our laboratory identified yohimbine in the absence of detectable concentrations of an alpha 2 agonist in a regulatory sample collected from a horse racing in California. This coupled with anecdotal reports of CNS stimulation and documented reports of cardiovascular changes when administered in conjunction with an agonist led us to investigate the pharmacokinetics and pharmacodynamics of yohimbine when administered a...
Authie EC, Garcia P, Popot MA, Toutain PL, Doucet M.Equine antidoping rules were established to prevent a horse's performance being altered after the administration of prohibited substances, including approved drugs used for legitimate treatment. Veterinarians have to advise owners or trainers on appropriate withholding times to guarantee that their horses may safely compete after drug administration. In order to propose tailored withdrawal times, several horse organisations released detection time (DT) values, for the main veterinary drugs used in horses. One of the possible limits to the information provided by published DTs in horses is the ...
A review of the literature is given concerning the anatomy and pathophysiology of the equine penis with regard to priapism: a prolonged erection of the penis not associated with sexual arousal. Several treatment options, such as flushing of the corpus cavernosum penis with heparinized saline and the creation of shunt between the corpus cavernosum penis and the corpus spongiosum penis are discussed. Subsequently, a case of priapism in a stallion following the injection of acepromazine, is discussed. The priapism resolved after the corpus cavernosum penis was flushed with the stallion under gene...
Rubio-Martínez LM, Rioja E, Castro Martins M, Wipawee S, Clegg P, Peffers MJ.Chondrotoxic effects of local anaesthetics are well reported in humans and some animal species but knowledge on their toxic effects on synoviocytes or equine chondrocytes or the effects on cellular production of inflammatory cytokines is limited. The purpose of this study was to evaluate the in vitro effects of local anaesthetics, morphine, magnesium sulphate (MgSO4) or their combinations on cell viability and pro-inflammatory cytokine gene expression of equine synoviocytes and chondrocytes. Equine synoviocytes and cartilage explants harvested from normal joints in a co-culture system were exp...
