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.
BRAYE ET, HINSMAN EJ, RILEY WF.No horse receiving combined streptokinase, streptodornase, and human plasminogen alone in either 125,000-unit or 375,000-unit doses manifested any clinical reaction. Untoward reactions occurred in 2 horses receiving both the combined streptokinase, streptodornase, and human plasminogen (125,000 units), and chlortetracycline. The reaction was transitory and subsided without treatment.
DRUDGE JH, LELAND SE, WYANT ZN, ELAM GW, HUTZLER LB.In five horses dosed with polymethylenepiperazine at dose levels of 21, 51 or 106 mg. per Ib. body-weight clearance of ascarids was obtained with all dosages. The effect against oxyurids was much less marked and large numbers of immature worms were found at autopsy four days after treatment. About 85% of small strongyles were removed at dosages of 21 mg. per Ib. and above and about 50% of Strongylus vulgaris were removed at dosages of 51 mg. per Ib. and above. The drug was inactive against S. edentatus, Trichostrongylus axei, Habronema muscae and Strongyloides westeri. In another eight horses ...
Zscherpe P, Kalbitz J, Weber LA, Paschke R, Mäder K, von Rechenberg B, Cavalleri JV, Meißner J, Klein K.Gray horses are predisposed to equine malignant melanoma (EMM) with advancing age. Depending on the tumor's location and size, they can cause severe problems (e.g., defaecation, urination, feeding). A feasible therapy for EMM has not yet been established and surgical excision can be difficult depending on the location of the melanoma. Thus, an effective and safe therapy is needed. Naturally occurring betulinic acid (BA), a pentacyclic triterpene and its synthetic derivate, NVX-207 (3-acetyl-betulinic acid-2-amino-3-hydroxy-2-hydroxymethyl-propanoate) are known for their cytotoxic properties ag...
Straticò P, Guerri G, Bandera L, Celani G, Di Nunzio L, Petrizzi L, Varasano V.(1) The main goals of general anesthesia include pain management and a safe anesthetic protocol for smooth recovery. In this retrospective study, we compared two anesthetic protocols for general anesthesia with isoflurane during emergency laparotomy: sedation with xylazine and the intraoperative infusion of lidocaine (X group) versus medetomidine as a preoperative sedation and intraoperative infusion (M group). (2) The medical records of horses who underwent emergency laparotomies between 2016 and 2023 were reviewed. According to the anesthetic protocol, patients were allocated to the X or M g...
Pereira R, Bowen M, Rapezzano G, Redpath A, Pratt S, Hallowell G.Recombinant intracameral tissue plasminogen activator (rTPA) administration can aid clearance of fibrin from the anterior chamber. In this retrospective multicentre case series, the effect of intracameral rTPA administration to treat fibrin in the anterior chamber resulting from trauma or inflammatory ocular disease was evaluated. Clinical data from 30 treatments in 29 horses were obtained from medical records from 2003 to 2022. Association between time from onset of clinical signs and time for rTPA treatment to effect was studied with regression analysis. Twenty-seven horses (93.1%) had no pr...
Shnaiderman-Torban A, Pe'er O, Gustafsson K, Tatz A, Brizi M, Soback S, Abu Ahmad W, Magen R, Ofri R, Kelmer G.In equine glaucoma, topical treatment with carbonic anhydrase inhibitors (CAIs) is recommended. Oral acetazolamide, a systemic CAI, is used in horses with hyperkalemic periodic paralysis. Information regarding its effect on equine intraocular pressure (IOP) is scarce. The aim of the study was to determine the effect of oral acetazolamide treatment on IOP in horses, in a case-control study. Methods: Ten healthy horses. Methods: Horses were treated with oral acetazolamide (4.4 mg/kg) BID for 1 week. Serum acetazolamide concentrations were determined by liquid chromatography/tandem mass spect...
Gibb Z, Aitken RJ, Sheridan AR, Holt B, Waugh S, Swegen A.The in vitro storage of stallion spermatozoa for use in artificial insemination leads to oxidative stress and imbalances in calcium homeostasis that trigger the formation of the mitochondrial permeability transition pore (mPTP), resulting in premature cell death. However, little is understood about the dynamics and the role of mPTP formation in mammalian spermatozoa. Here, we identify an important role for mPTP in stallion sperm Ca2+ homeostasis. We show that stallion spermatozoa do not exhibit "classical" features of mPTP; specifically, they are resistant to cyclosporin A-mediated inhibition...
Hart KA, Kimura S.Immunomodulators can stimulate, suppress, or regulate one or many aspects of the immune response. Use of a variety of immunostimulants, immunosuppressors, and anti-inflammatory drugs are described in horses, but the evidence supporting their efficacy is variable. Corticosteroids and nonsteroidal anti-inflammatory drugs are the best characterized immunomodulators in horses, but further study is needed to fully define their ideal dosing protocols and indications and to characterize the efficacy of other immunomodulators in equine medicine.
Hubbell JAE, Muir WW, Gorenberg E, Hopster K.Horses are the most challenging of the common companion animals to anesthetize. Induction of anesthesia in the horse is complicated by the fact that it is accompanied by a transition from a standing position to recumbency. The purpose of this article is to review the literature on induction of anesthesia with a focus on the behavioral and physiologic/pharmacodynamic responses and the actions and interactions of the drugs administered to induce anesthesia in the healthy adult horse with the goal of increasing consistency and predictability.
Grob AJ, Delarocque J, Feige K, Warnken T.In insulin dysregulation, hyperinsulinemia (HI) can be accompanied by peripheral insulin resistance (IR) in horses, which can be diagnosed with an insulin-tolerance test (ITT). The administration of 0.1 IU/kg body weight of recombinant regular human insulin (RHI) should elicit a 50 % reduction of the initial blood glucose concentration at 30 min after insulin administration in insulin sensitive horses. Compared to RHI, porcine zinc insulin (PZI) is veterinary-approved and therefore easier accessible for many practitioners. The aim of this study was to compare the insulin and glucose dynami...
Ignácio FS, Garcia LV, de Souza GG, Amatti LZ, de Barros LD, Bergfelt DR, Camargo GS, de Meira C, de Almeida BFM.Non-steroidal anti-inflammatory drugs (NSAIDs) represent one of the most commonly used classes of drugs in both human and veterinary medicine. However, many clinical side effects have been observed, especially when treatment has been prolonged. While the anti-inflammatory efficacy and safety of repeated administration of firocoxib (Previcox®), which is a selective NSAID COX-2 inhibitor, has been evaluated for short-term use (one to fourteen days), its clinical relevance for longer-term use is not known. As a preliminary study, healthy, adult male and female horses (n = 7) were treated with fi...
Wong ASY, Yuen BP, Wong COL, Kong FK, So YM, Kwok WH, Brooks L, Wan TSM, Ho EN.Bisphosphonates and myo-inositol trispyrophosphate (ITPP) are two classes of difficult-to-detect polar drugs that are prohibited under the rules of racing. ITPP is a drug capable of increasing the amount of oxygen in hypoxic tissues, and studies have shown that administration of ITPP increases the maximal exercise capacity in mice. The properties of ITPP make it an ideal candidate as a doping agent to enhance performance in racehorses. In recent years, ITPP had indeed been detected in racehorses and confiscated items. As for bisphosphonates, it is especially critical to control their use as si...
Brandon AM, Williams JM, Davis JL, Martin EG, Capper AM, Crabtree NE.To determine the pharmacokinetics (PK) of metoclopramide administered via intravenous continuous rate infusion (IV CRI) and subcutaneous (SC) bolus and evaluate for gastrointestinal motility and adverse side effects. Methods: Experimental study; randomized, crossover design. Methods: Six healthy adult horses. Methods: Each horse received metoclopramide via IV CRI (0.04 mg/kg/h for 24 h) and SC bolus (0.08 mg/kg once), with ≥1 week washout period between. Plasma was analyzed by UPLC-MS/MS. Compartmental modeling was used to determine PK parameters for each treatment; nonparametric sup...
Zaghloul IY, Bedenice D, Ceresia ML, Jones PH, Sanchez-Londono A, Lobo MN, Böhlke M, Paradis MR.To evaluate the effects of aging on phenylbutazone (PBZ) disposition in older horses (≥ 25 years old) compared to young adults (4 to 10 years old) by characterizing the pharmacokinetic profile of PBZ and its active metabolite, oxyphenbutazone (OPBZ), following a 2.2-mg/kg dose, IV. We hypothesized that the disposition of PBZ will be affected by age. Methods: 16 healthy horses (8 young adults aged 4 to 10 years and 8 geriatric horses ≥ 25 years old). Methods: Horses were administered a single 2.2-mg/kg PBZ dose, IV. Plasma samples were collected at designated time points and frozen at -80 Â...
Uchida T, Kisugi T, Ishii H, Yamada M, Kinoshita K, Leung GN.To uphold the integrity of horseracing and equestrian sports, it is critical for an equine doping control laboratory to develop a comprehensive screening method to cover a wide range of target substances at the required detection levels in equine urine. Methods: The procedure involved the enzymatic hydrolysis of 3 mL urine samples followed by solid-phase extraction using HF Bond Elut C18 cartridge. The resulting extracts were then separated on a C18 reversed-phase column and analyzed using liquid chromatography/high-resolution mass spectrometry (LC/HRMS) in both electrospray ionization positiv...
Khan Y, El-Shalofy A, Kaps M, Gautier C, Aurich C.We aimed to determine associations between experimentally impaired uterine clearance or treatment with ecbolic drugs on luteal development in estrous mares after insemination. In a crossover design, eight mares were treated with saline (CON), clenbuterol (CLEN), oxytocin (OXY) and carbetocin (CARB) from the day of first insemination until 2 days after ovulation. Between treatments, the mares rested for one cycle. Estrous mares were examined for the presence of free intrauterine fluid by transrectal ultrasound. Endometrial swabs for cytology and bacteriology were collected on days 1 and 14. Blo...
Cutler C, Viljanto M, Hincks P, Habershon-Butcher J, Scarth J, van Eenoo P.S-23 is an arylpropionamide selective androgen receptor modulator that has been investigated in animal models for use as a male hormonal contraceptive but is not yet available therapeutically. S-23 is available alongside other selective androgen receptor modulators (SARMs) to purchase online via uncontrolled sites, sold as supplement products. It has been detected in several human doping cases, highlighting the importance of identifying the best analytical targets for equine doping control. The purpose of this study was to investigate the detection of S-23 and its phase I metabolites in equine...
Menzies-Gow NJ, Knowles EJ.Laminitis is a common and painful condition of the equine foot and approximately 90% of cases are associated with insulin dysregulation (ID) that is a central feature of the common endocrine disorder equine metabolic syndrome (EMS) and occurs in a subset of animals with pituitary pars intermedia dysfunction. Additional features of EMS include obesity, altered circulating concentrations of adipokines (particularly adiponectin and leptin) and hypertriglyceridaemia. Obesity, ID, hypoadiponectinaemia, hyperleptinaemia and an altered plasma lipid profile are also features of human metabolic syndrom...
Bacon EK, Donnelly CG, Bellone RR, Haase B, Finno CJ, Velie BD.The pleiotropic effects of the melanocortin system show promise in overcoming limitations associated with large variations in opioid analgesic effectiveness observed in equine practice. Of particular interest is variation in the melanocortin-1-receptor (MC1R) gene, which dictates pigment type expression through its epistatic interaction with the agouti signalling protein (ASIP) gene. MC1RÂ has previously been implicated in opioid efficacy in other species; however, this relationship is yet to be explored in horses. In this study, analgesic effectiveness was scored (1-3) based on noted response...
Mita H, Kuroda T, Minamijima Y, Tamura N, Ohta M.Surgical-site infections (SSIs) at implant sites in horses are sometimes difficult to control with systemic antimicrobials. Because one of the likely reasons is insufficient antimicrobial concentrations, there is a need to increase these concentrations in and around the infected tissue. Marbofloxacin (MAR)-encapsulated microparticles (MAR-MPs) made of biodegradable poly (lactic-co-glycolic) acid are capable of sustained release in vitro. We examined the concentration of MAR in the subcutaneous tissue fluid at sites where MAR-MPs had been administered. On day 0, six 3- × 4-cm subcutaneous pock...
Mascaró Triedo CE, Karar S, Abunemeh M, Portier K.Pupillometry is used in humans to monitor pain, nociception and analgesia. This single-center, non-randomized, non-blinded intervention trial, evaluated the effect of nose twitching on the pupil size in awake, sedated, and anesthetized horses. Pupil height (H) and length (L) were measured before (Be) and after (Af) nose twitching in fourteen non-painful adult awake horses (T0). The percentage of variation (PSV) was calculated (PSVTn = [(TnAf-TnBe)/TnBe]*100). Measurements were repeated (Tn) after acepromazine (0.04 mg kg IV) (T1), romifidine (0.04 mg kg IV) (T2), morphine (0.1 mg...
Lomnicka I, Dubey S, Waller P, Vora D, Dirikolu L.The screening of drugs in plasma and urine often requires initial extraction (such as liquid-liquid extraction and solid-phase extraction) before the samples are submitted to instrumental analyses. These extraction procedures are often laborious and time-consuming. In this manuscript, a high-throughput automated assay based on liquid chromatography-high-resolution mass spectrometry (LC-HRMS) suitable for use as an initial testing procedure covering multiple classes of compounds prohibited in horse racing is described. The assay requires a 600-μL plasma aliquot, which is subjected to solid pha...
Michanek P, Bröjer J, Lilliehöök I, Fjordbakk CT, Löwgren M, Hedeland M, Bergquist J, Ekstrand C.Canagliflozin (CFZ) is a sodium-glucose cotransporter-2 inhibitor that has shown promising results as a drug for the treatment of insulin dysregulation in horses. Even though CFZ is used clinically, no pharmacokinetic data has previously been published. In this study, the pharmacokinetics of CFZ after administration of a single oral dose of 1.8 mg/kg in eight healthy Icelandic horses was examined. Additionally, the effect of treatment on glucose and insulin levels in response to a graded glucose infusion was investigated. Plasma samples for CFZ quantification were taken at 0, 0.33, 0.66, 1, ...
Izquierdo-Moreno J, de Paz MI, Manso-DÃaz G, Villalba-Orero M, López-Sanromán J.An accurate evaluation of the degree of sedation is mandatory to adjust the dosage of sedative drugs. Objective: To determine the correlation between head height above the ground and ataxia degree in horses sedated with detomidine and the correlation existing between accelerometric variables and both parameters. Methods: Retrospective study. Methods: Twelve horses were given 0.01 mg/kg of detomidine hydrochloride iv. Measured accelerometric parameters, with one accelerometer positioned between both sacral tuberosities, included speed, stride frequency and length, regularity, dorsoventral, lo...
Di Salvo A, Chiaradia E, Sforna M, Della Rocca G.Since the discovery of the endocannabinoid system and due to the empirical evidence of the therapeutic effects on several illnesses both in humans and animals that follow the administration of exogenous cannabinoids (i.e., phytocannabinoids), numerous studies have been conducted. These investigations aimed to identify the expression and distribution of cannabinoid receptors in healthy and pathologic organs and tissues of different animal species and to define the interactions of phytocannabinoids with these receptors. In the last decade, pharmacokinetics, efficacy and tolerability of many Cann...
Bedogni G, Michelena LV, Seremeta K, Okulik N, Salomon C.Fenbendazole is an antiparasitic drug widely used in veterinary medicine to treat parasitic infections caused in animals like cattle, horses, sheep, and dogs. Recently, it has been repositioned as a potential alternative for cancer treatment. However, it is a highly hydrophobic molecule (0.9 ug/mL), which can compromise its dissolution rate and absorption. Thus, this work aimed to apply a nanotechnological approach to improve drug solubility and dissolution performance. Fenbendazole nanoparticles stabilized by different poloxamers were obtained by lyophilization without cryoprotectants. The be...
Le Breton A, Lewis N.Assisted reproductive technologies (ARTs) are performed worldwide in the equine industry to produce genetically valuable foals. Among them, ovum pick up (OPU) combined with intra-cytoplasmic sperm injection (ICSI) can now be more efficient than embryo transfer (ET) under optimal conditions. However, OPU is not a benign procedure for the mare and the process is costly. Improved efficiency is therefore in the interest of everyone, maximizing mare welfare and optimizing economics for the client. One of the key factors of success is the antral follicle count (AFC) at the time of OPU and subsequent...
Swanton WE, Johnson R, Zhao Q, Schroeder C.To evaluate sedation and IV xylazine requirements to achieve 45% of baseline head height above ground measurements following oral (PO) administration of 2 trazodone dosages. Methods: 8 healthy, adult mares of various weights and breeds belonging to a university teaching herd were utilized in a blinded, crossover study design. Horses were randomly assigned to 1 of 3 PO treatments: control (no trazodone), trazodone at 3 mg/kg (low dose [LD]), or trazodone at 6 mg/kg (high dose [HD]). Before treatment, cardiac auscultation, EquiSed sedation score, and head height above ground (HHAG; cm) measureme...
Adam E, Scollay M, Howard B, Taormina J, Hartmann P, Knych H.Levamisole is a regulated substance sometimes administered to racehorses to treat equine protozoal myelitis. Metabolites include compound II, aminorex, and pemoline. Aminorex and pemoline are Horseracing Integrity and Safety Authority-banned substances. Previous studies have examined single doses of the drug. This study examined the disposition of levamisole after 7 days of dosing. Methods: 6 healthy Thoroughbred geldings. Methods: Horses were treated with 500 mg (approx 0.91 to 1 mg/kg) of compounded levamisole hydrochloride paste PO every 12 hours for a total of 13 doses over 7 days. Serum a...
Philip M, Kal AKK, Subhahar MB, Karatt TK, Graiban FM, Ajeebsanu MM, Joseph M, Jose SV.Phosphodiesterase 4 (PDE4) inhibitors are a newer class of drugs that induce bronchodilation and have anti-inflammatory effects, making them susceptible to misuse as performance enhancers in competitive sports. Methods: This study explores the metabolic conversion of PDE4 inhibitor ibudilast in thoroughbred horses after oral administration and in vitro using equine liver microsomes and Cunninghamella elegans. A liquid chromatography-high resolution mass spectrometry method was used to postulate the plausible structures of the detected metabolites. Results: A total of 20 in vivo metabolites wer...
