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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.
Pituitary Pars Intermedia Dysfunction. Pituitary pars intermedia dysfunction (PPID) is one of the most common equine endocrine disorders. It is caused by oxidative damage to dopaminergic neurons in the hypothalamus and results in loss of inhibition of the pituitary pars intermedia. This leads to increased circulating concentrations of adrenocorticotropic hormone (ACTH) and related peptides. Diagnosis is based on increased resting and/or thyrotropin releasing hormone-stimulated ACTH concentrations. Assessment of insulin regulation is also important, as insulin dysregulation occurs in at least one-third of PPID cases and is associate...
Analgesic use, safety and pharmacokinetics of acetaminophen in equids: A structured scoping review. Despite its frequent use in equine clinical practice, scientific data on the use of acetaminophen in horses remain limited. Objective: To map and critically appraise the available evidence on the analgesic use, safety and pharmacokinetics of acetaminophen in horses. Methods: Structured scoping review. Methods: A comprehensive search was performed in accordance with the PRISMA Extension for Scoping Reviews using the terms '(paracetamol OR acetaminophen) AND (pain OR safety OR toxicosis OR pharmacokinetics) AND (horse OR pony OR donkey OR mule)' across Web of Science, Scopus, and PubMed from dat...
Quantifying the Equine Pain Response to Paracetamol Administration in Horses With Chronic Lameness Already Receiving Non-Steroidal Anti-Inflammatories. Paracetamol is used in horses alongside non-steroidal anti-inflammatories (NSAIDs) for multi-modal analgesia; however to date there are few studies published which have investigated its analgesic effect in the horse. Horses were recruited to this study from a population of geriatric horses at The Horse Trust. Horses were selected based on the following inclusion criteria; documented naturally occurring chronic lameness and being treated with an NSAID at the licensed dose and dosing interval. This population was assessed with a five-point subjective lameness grading system performed live by two...
Effects of omeprazole therapy administered via different routes on urinary parameters and selected interleukins in horses with equine gastric ulcer syndrome. Equine gastric ulcer syndrome (EGUS) is commonly treated with proton pump inhibitors such as omeprazole, administered orally or by injection. In humans, omeprazole has been associated with acute interstitial nephritis (AIN) and acute kidney injury (AKI), potentially linked to oxidative stress, and urinary interleukins may serve as early non-invasive markers. However, this association has not been established in horses. Objective: To evaluate the effects of oral and injectable omeprazole on basic urinary parameters and selected interleukin levels, with particular emphasis on the potential risk ...
Pharmacokinetic/Pharmacodynamic Analysis of Quinidine-Induced Dominant Frequency Reduction in Thoroughbred Horses With Atrial Fibrillation. Quinidine has long been used for the pharmacological treatment of atrial fibrillation (AF) in horses; however, the plasma concentration required for conversion to sinus rhythm remains unclear. Dominant frequency (DF), derived from surface electrocardiograms, reflects atrial activation rate during AF. This study aimed to quantify the relationship between plasma quinidine concentration and DF using a pharmacokinetic/pharmacodynamic (PK/PD) approach. Ten Thoroughbred horses with naturally occurring AF received quinidine sulfate via a nasogastric tube. Plasma quinidine concentrations and DF values...
Detection of Cyclosporine in Horse Hair After Ocular Implant Administration. This study describes the detection and temporal distribution of cyclosporine in equine hair following ocular implant administration in a Thoroughbred gelding. Mane hair samples were collected at 172- and 217-day post-implantation and analysed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) after alkaline hydrolysis and liquid-liquid extraction. The method achieved an estimated limit of detection of 0.1 pg/mg. Cyclosporine was detected in hair at both sampling time points, with segmental analysis revealing distribution patterns consistent with systemic exposure and incorporation ...
Horses undergoing supramaximal fixed-speed treadmill exercise after administration of furosemide experience less severe acidosis and slower onset of fatigue. To document changes in acid-base and ion balance during exercise following furosemide administration and to relate them to performance. Unassigned: 6 fit Thoroughbred horses received 0.5 mg/kg IV furosemide (F) or a placebo (C) in randomized crossover order 4 hours before galloping to fatigue on a treadmill at the speed equated with an oxygen demand of 1.15 X maximum oxygen consumption (V˙o2max). Arterial and mixed venous blood was sampled before treatment, preexercise, after 2-minute warm-up, at fatigue, and 1 minute postexercise. The pH, temperature-corrected Pco2, total CO2, and sodium, po...
Detection and confirmation of hypoxia-inducible factor activating agents in equine plasma and urine by liquid chromatography coupled to mass spectrometry. Hypoxia-inducible factor (HIF) activating agents can promote the transcription of the erythropoietin gene, enhancing an athlete's performance, and are therefore prohibited in sports. A liquid chromatography coupled to high-resolution mass spectrometry (LCHRMS) method was developed for the detection and confirmation of 11 HIF-activating substances in equine plasma and urine. Ammonium formate added to the mobile phase system suppressed the responses of all the analytes in either positive or negative ion mode and thus was not used. The starting organic percentage in the mobile phase gradient and ...
The effect of fenugreek (Trigonella foenum-graecum) on stallion spermatozoa motility and vitality in vitro. This study evaluated the effects of Trigonella foenum-graecum L. (fenugreek) seed extract on stallion spermatozoa quality in vitro, focusing on motility, vitality, and functional competence. In vitro spermatozoa analyses showed that fenugreek seed extract did not demonstrate overt cytotoxicity under the tested conditions: S1 = 1562 µg/mL; S2 = 781 µg/mL; S3 = 390.5 µg/mL; S4 = 195.25 µg/mL; S5 = 97.62 µg/mL; S6 = 48.81 µg/mL; S7 = 24.40 µg/mL. Computer-assisted semen analysis (CASA) revealed a concentration- and time-dependent Treatment × Time interac...
Canagliflozin treatment of a horse with hyperinsulinemia, including pharmacokinetic analysis of different dosing protocols: a case report. Laminitis is a complex and painful disease of the equine foot. Insulin dysregulation (ID) resulting in hyperinsulinemia is responsible for more than 90% of cases in the general horse and pony population. Sodium-glucose cotransporter 2 inhibitors (SGLT2i) are a relatively new class of drug that has gained considerable popularity as an off-label treatment of hyperinsulinemia-associated laminitis (HAL) in horses when traditional management changes and treatments are unsuccessful. In Canada, canagliflozin is the SGLT2i most available to equine veterinarians; although no dosing protocols have been ...
Simple and efficient HPLC-MS/MS method for simultaneous extraction and quantification of anthelmintics in equine manure. Anthelmintic treatment is a common practice in horses. The presence of pharmaceutical residues in fields and pastures is well-documented affecting various organisms, like nematodes. This study describes the development and validation of a high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method using multiple reaction monitoring (MRM) for extracting and determining the concentrations of four commonly used anthelmintics in horse manure. Manure was initially dried, then spiked with various concentrations (10-10,000 ng) of anthelmintics and extracted using an acetonit...
Detection of ionisable lipids in equine plasma by supported liquid extraction and liquid chromatography-high-resolution tandem mass spectrometry for doping control of mRNA agents. Messenger ribonucleic acid (mRNA) has emerged as a new class of therapeutic agent with unprecedented potential. In particular, the lipid nanoparticle (LNP)-mRNA formulations enabled safe and effective delivery of mRNA in vivo, leading to the success of mRNA vaccines during the COVID-19 pandemic. To control the potential misuse of LNP-mRNA agents in equine sports, a simple and sensitive method has been developed for the detection of ionisable lipids in equine plasma using supported liquid extraction (SLE) followed by liquid chromatography-high-resolution tandem mass spectrometry. To overcome th...
Efficacy and safety of canagliflozin in insulin dysregulated horses: a 4-week multi-arm, double-blind, randomized, clinical trial. Sodium-glucose cotransporter-2 (SGLT2) inhibitors are promising drugs for treatment of hyperinsulinemia in insulin-dysregulated (ID) horses. Objective: Compare short-term effects of the SGLT2 inhibitor canagliflozin versus placebo on glucose and insulin responses during an oral sugar test (OST) and a forage-based feed challenge test (FCT), and to assess adverse effects. Methods: Forty-two privately owned severely ID horses. Methods: Multi-center, randomized, double-blind, placebo-controlled, parallel-group study. Horses were allocated (1:1:1) to receive canagliflozin (0.6 or 1.2 mg/kg PO q24h...
Antibiotics in Veterinary Ophthalmology: Resistance, Stewardship, and Emerging Antibiotic-Sparing Strategies. Antimicrobial resistance (AMR) is a growing challenge in veterinary ophthalmology, particularly in cases of bacterial keratitis, where progressive stromal infection can threaten vision and globe integrity within hours to days. This review synthesizes current evidence on pathogen distribution, antimicrobial susceptibility profiles, multidrug resistance (MDR) prevalence, and determinants of nonsusceptibility in veterinary patients, highlighting the emerging role of antibiotic-sparing alternatives. Across contemporary studies, Staphylococcus pseudintermedius, β-hemolytic streptococci, and Pseud...
Feasibility and safety of repeated 23% hypertonic saline boluses for electrical impedance tomography contrast enhancement in anaesthetised horses. Hypertonic saline (HS) has been used to enhance electrical impedance tomography (EIT) cardiac-related signals associated with pulmonary perfusion in other species, but its suitability and physiological effects in horses are unknown. This exploratory study aimed to determine whether intravenous administration of 100 mL of 23% HS produces a detectable change in thoracic impedance in anaesthetised horses, and to evaluate the physiological effects of repeated bolus administration. Six adult horses were anaesthetised twice using total intravenous anaesthesia. Hypertonic saline 23% was administered ...
Comparative Pharmacokinetics of Gentamicin in Healthy Young-Adult and Geriatric Horses. Aging may modify the pharmacokinetic disposition and excretion of gentamicin, although drug dose adjustments in aged horses are uncommon in clinical practice. Since high-dose, once daily dosing of gentamicin is considered therapeutically most effective, a comparative single-dose study was conducted to evaluate the differences in pharmacokinetics between healthy young-adult (5-10 years) and geriatric (≥ 25 years) horses receiving 6.6 mg/kg gentamicin intravenously. Blood samples were collected at designated time-points following drug administration and frozen at -80°C until assayed b...
Pharmaceutical and Nutraceutical Therapies for Liver Disease. Liver dysfunction may reduce the metabolism of drugs that undergo extensive hepatic processing. This will lead to reduced clearance and elimination, and can cause accumulation of the drug, increasing the risk of toxicity. Pentoxifylline and ursodeoxycholic acid are 2 pharmaceuticals that can provide benefits for a variety of equine hepatic diseases. Nutraceuticals are frequently used in horses with hepatopathy, targeting oxidative stress, inflammation, and hepatocellular injury. Neutraceuticals such as S-adenosylmethionine, silymarin and vitamin E are most commonly used although extensive rese...
Single-dose intravenous α2-agonists do not acutely alter anti-inflammatory bioactive protein profiles but reduce interleukin-8 in equine autologous protein solution and platelet-rich plasma. Determine the acute effects of xylazine and detomidine on concentrations of selected growth factors, cytokines, and α2-macroglobulin (A2M) in platelet-rich plasma (PRP) and autologous protein solution (APS) and the long-term effects of these sedatives on serum A2M. We hypothesized that sedative administration would decrease concentrations of all bioactive proteins in PRP and APS acutely and A2M in serum for 6 days following sedative administration. Unassigned: 6 horses were randomized to receive IV xylazine (200 mg) or detomidine (10 mg). Blood was collected before and 5 minutes after sedativ...
OPTIMIZING EXTRACTION AND CONCENTRATION METHODS FOR LC-MS/MS ANALYSIS OF VETERINARY PHARMACEUTICALS IN EQUINE-ASSOCIATED ENVIRONMENTAL MATRICES. This study developed a method for the simultaneous quantification of six potentially environmentally toxic veterinary drugs: benzylpenicillin, acepromazine, flunixin, dexamethasone, ketamine and romifidine, in soils, sediments, equine faeces and natural waters. Three methods were compared for their extraction from solid matrices: Ultrasonic extraction (USE), QuEChERS and Accelerated Solvent Extraction (ASE). ASE method was optimized according to temperature and extraction cycles. Quantification was performed by LC-MS/MS. LC and MS parameters were optimized. The method was validated according t...
Plasma and urinary exposure of cannabidiol and cannabidiolic acid in horses following consumption of contaminated feed. Cannabidiol (CBD) and cannabidiolic acid (CBDA) are non-psychoactive cannabinoids naturally present in hemp-derived products. While these compounds are prohibited during equine competition, horses may be inadvertently exposed through contaminated feed. Data describing systemic and urinary exposure to CBD and CBDA following such low-dose, involuntary intake are limited. This study aimed to describe plasma and urine concentration-time profiles of CBD and CBDA in horses after consumption of experimentally contaminated feed. Results: Twelve Standardbred horses received feed containing low doses (1...
Oclacitinib for Controlling Pruritus and Associated Skin Lesions in 16 Horses With Allergic Dermatitis. Oclacitinib is a Janus kinase inhibitor approved for the treatment of pruritus associated with allergic dermatitis in dogs and may be effective in horses. Objective: To evaluate the efficacy of oclacitinib in reducing pruritus and skin lesions in horses with allergic dermatitis. Methods: Sixteen horses aged ≥ 18 months. Methods: Horses received oclacitinib at 0.25 mg/kg orally once daily for 21 days. Changes in haematological and biochemical parameters were measured on Day (D)0 and D21. The owners were instructed to evaluate the horses using the pruritus Visual Analog Scale (PVAS) on...
Recent Advances in Natural Products for Colitis: Mechanisms and Translational Perspectives. Colitis is a chronic relapsing inflammatory disorder characterized by persistent mucosal inflammation, epithelial barrier disruption, oxidative stress, immune dysregulation, and gut microbiota imbalance. Although current therapies have improved disease management, their long-term use is still limited by incomplete response, relapse, adverse effects, and high cost. Natural products have attracted increasing attention as promising candidates for colitis intervention because of their structural diversity, broad bioactivity, and multitarget regulatory potential. In veterinary medicine, colitis and...
Topical betulinic acid for treatment of equine melanoma and sarcoid. Betulinic acid, a natural pentacyclic triterpenoid, has demonstrated anti-inflammatory and anti-tumor properties in vitro, including activity against equine melanoma and sarcoid. However, there is limited in vivo evidence evaluating its clinical efficacy. The objective of this study was to assess the safety and efficacy of a compounded 1% betulinic acid cream for the treatment of equine cutaneous melanoma and sarcoid. Unassigned: This prospective, randomized, double-blinded, placebo-controlled clinical trial enrolled client-owned horses with melanoma or sarcoid tumors. Horses received either a...
The effect of romifidine on endoscopic grading of laryngeal function in horses. To our knowledge, the effect of sedation with romifidine on the grading of laryngeal function in horses has not been studied. Our objective was to examine the effects of romifidine on the grading of laryngeal function and the cross-sectional area of the rima glottis (CSARG). Methods: Ten horses underwent three endoscopic examinations of the larynx: once while unsedated (group R1), once after being sedated with romifidine (0.04 mg/kg intravenously; group R2) and once again, while still sedated, after receiving a repeat dose of romifidine (0.08 mg/kg intravenously, total dose; group R3). The r...
A Genetic Algorithm-Based Approach for Quantitative Prediction of Drug-Drug Interactions Caused by Cytochrome P450 3A Inhibition or Induction in Horses. A genetic algorithm (GA)-based approach was designed to predict drug-drug interactions (DDIs) triggered by cytochrome P450 3A (CYP3A) inhibition or induction in horses. Area under the concentration-time curve ratios (AUCRs), obtained from published in vivo DDI studies in horses, were used to compute the following parameters: (1) the contribution ratio (CR), i.e., the fraction of the substrate dose metabolized via the CYP3A pathway, and (2) the interacting drug's inhibitory potency or inducing efficacy (IR or IC, respectively). AUCRs for 9 substrates, 12 inhibitors, and 1 inducer of equine C...
Protective effects of adiponectin receptor agonists against equine lamellar endoplasmic reticulum stress. Lamellar endoplasmic reticulum (ER) stress occurs in hyperinsulinemia-associated and sepsis-related laminitis. Adiponectin is associated with reduced laminitis risk and inhibits ER stress in other species. Objective: To induce ER stress in ex vivo equine lamellar cells using pharmacological agents. To determine whether co-treatment with adiponectin receptor agonists (ARAs) reduces ER stress. Methods: In vitro. Methods: Lamellar cells from n = 4-5 horses were treated with tunicamycin or thapsigargin (10-1000 nM) for 2-24 h. ER-stressed cells were co-treated with full-length adiponectin ...
Pharmacokinetics of Diclazuril in the Plasma and Cerebrospinal Fluid of Healthy Adult Horses After a Single Oral Dose Administered as a Pelleted Topdressing. Equine protozoal myeloencephalitis can cause acute infections with rapid onset of neurologic signs, necessitating immediate empiric therapy with antiprotozoal medication. The objective of the study was to identify when concentrations of diclazuril reached the MIC of Sarcocystis neurona in CSF (1 ng/mL) of healthy adult horses after a single oral dose. Six healthy adult horses were used. Blood and CSF were collected from indwelling intravenous jugular catheters and intrathecal catheters in the lumbosacral space prior to drug administration and then at 1-, 4-, 8-, 12-, 16-, 24-, 48-, 72-, 96-,...
Metabolic effects and pharmacokinetics of oral cannabidiol (CBD) in Connemara ponies following 21 days of treatment. Cannabidiol (CBD) has gained interest in equine medicine due to its potential therapeutic effects. Preclinical studies suggest that CBD may influence metabolic pathways relevant to metabolic syndrome, which present in both human and equine populations. The aim of this study was to evaluate the effects of oral CBD on metabolic parameters in Connemara ponies and to characterize its pharmacokinetics. Unassigned: A total of 13 Connemara ponies [seven with equine metabolic syndrome (EMS)] were stratified by EMS status and age and randomly assigned to a CBD-treated group (2 mg/kg orally, twice dai...
Short-term clinical responses in horses and ponies treated with canagliflozin: A clinical field study. Treatment with the sodium-glucose co-transporter 2 (SGLT2) inhibitor canagliflozin in insulin dysregulated (ID) horses has shown promising results in randomised clinical trials. Larger field studies are needed to further evaluate treatment responses and potential adverse effects under real-world conditions. Objective: To assess the short-term effects of canagliflozin on postprandial glucose and insulin responses in client-owned horses and ponies with ID using a single-sample feed-challenge test (FCT), and to characterise treatment-associated changes in bodyweight, liver enzyme activities, and ...
Bexagliflozin controls hyperinsulinemia in horses with naturally occurring insulin dysregulation: a placebo-controlled crossover trial. To evaluate bexagliflozin for insulin control in horses with naturally occurring insulin dysregulation. Unassigned: In a randomized, placebo-controlled crossover study, 10 client-owned Arabian horses with hyperinsulinemia (> 30 μIU/mL) were treated with bexagliflozin (0.03 mg/kg, PO, q 24 h; BEXA03) or placebo control for a 10-day treatment period, crossing over after a 4-day washout. After a further 12-day washout, 8 of the horses were treated with bexagliflozin (0.06 mg/kg, PO, q 24 h; BEXA06) for an additional 7-day treatment period. Oral sugar tests were performed at the beginning of e...
