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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.
Dexmedetomidine infusions improve cardiovascular and renal function in anaesthetised, experimentally endotoxaemic horses. Dexmedetomidine infusions are beneficial in anaesthetised endotoxaemic horses when administered concurrent to endotoxin, but post-conditioning effects are unknown. Objective: To evaluate whether a dexmedetomidine infusion is beneficial in horses administered Escherichia coli O55:B5 lipopolysaccharides (LPS) endotoxin prior to anaesthesia. Methods: Randomised controlled in vivo experiment. Methods: Ten systemically healthy horses were instrumented for acquisition of cardiac index (CI) using thermodilution. Horses received IV LPS (0.1 μg/kg bwt) immediately prior to anesthesia. Horses receive...
Pharmacokinetics of Ertugliflozin, a Sodium-Glucose Co-Transporter-2 Inhibitor (SGLT2i) in Horses After Enteral Administration. Ertugliflozin is a sodium-glucose co-transporter-2 inhibitor that has demonstrated promise as a treatment for hyperinsulinaemia in horses. Despite the frequent use of ertugliflozin in equine clinical practice, the pharmacokinetics of this drug in horses has not been established. The aim of the present study was to determine the pharmacokinetics of one supratherapeutic dose (0.25 mg/kg) of ertugliflozin in eight horses. Horses were defined as being healthy by physical examination, haematological, blood biochemical and oral sugar test (OST) results. Plasma concentrations of ertugliflozin were qu...
Clodronate disodium reduced TRAP5b independent of affecting other systemic biomarkers of bone resorption or formation in yearling, exercising Quarter Horses. Clodronate disodium (CD), a bisphosphonate, modulates bone metabolism. Though extra-label use in juvenile horses is anecdotally reported, impacts on skeletal development are unknown. The objective was to determine the effects of CD on systemic markers of bone turnover in yearling horses undergoing exercise, hypothesizing that biomarkers of bone resorption would decrease while biomarkers of bone formation would not change, and that repeat CD treatments would have greater effect. To test this, 32 yearling Quarter Horses were used in a 168-d trial. Horses were stratified by age (500 ± 13 d),...
An in vitro collagen gel contraction assay to assess the relaxing effect of potential pharmacological alternatives to oxytetracycline on foals’ tendons. Oxytetracycline has been successfully used to treat flexural limb deformities in foals. However, its antimicrobial properties and potential adverse side effects warrant the investigation of alternatives. Inhibition of matrix metalloproteinases (MMPs) or collagen cross-linking have been suggested as possible mechanisms of action. This study assessed the influence of potential alternative substances lacking antimicrobial properties on collagen gel contraction by juvenile equine myofibroblasts in vitro. Myofibroblasts were isolated from forelimb SDFTs and inferior check ligaments from foals eutha...
Evaluation of the tolerance and effects of 1-deoxynojirimycin on insulin and glucose dynamics in healthy horses and horses at risk for insulin dysregulation. Insulin dysregulation (ID) is common and diminishes welfare of horses. Current management relies on diet and exercise, with variable responses and limited medical options. Alpha-glucosidase inhibitors (AGIs) might provide adjunctive therapy. Objective: To evaluate the tolerance and effects of Reducose®, a Morus alba leaf extract standardized to 5% 1-deoxynojirimycin (DNJ), in healthy horses and horses at risk of ID. We hypothesized DNJ would be well-tolerated and reduce insulin responses to oral sugar tests (OSTs). Methods: Twenty-seven horses: 6 healthy (Phase I), 5 at risk for ID (Phase II)...
Erythrocyte sequestration of metformin in horses: impact on matrix-specific pharmacokinetics and detection windows. BACKGROUND: Metformin is used for the treatment of type 2 diabetes and is one of the most prescribed medications in human medicine. It is less commonly prescribed in equine medicine, and its use is tightly regulated in several performance horse disciplines. In horseracing, it is considered a banned substance. A previous pharmacokinetic study of metformin in horses demonstrated a prolonged, unpredictable elimination phase. In the current study it was hypothesized that this was due to sequestration of metformin in a “deep” compartment, specifically red blood cells. This could result in pharm...
Overview of the Current Osteoarthritis Treatment in Veterinary Medicine and Future Directions. Osteoarthritis (OA) is a chronic and progressive joint disease that can cause permanent loss of joint function. OA is highly prevalent in horses, dogs, and cats, affecting different joints and leading to reduced mobility and chronic pain. Different risk factors for animal OA have been identified, including trauma and breed. Inflammation is a hallmark of the disease, with various underlying mechanisms such as cyclooxygenase and metalloproteinase activation, nerve growth factor, cytokine, and prostaglandin upregulation, among others. Although disease complexity makes OA difficult to treat, eno...
Atropine induces narrowing of the superior and inferior iridocorneal angle and ciliary cleft in normal horse eyes. To investigate the effects of atropine on the iridocorneal angle (ICA) and ciliary cleft (CC) of normal equine eyes using ultrasound biomicroscopy (UBM). Unassigned: 12 normal adult horses underwent measurement of intraocular pressure (IOP), vertical and horizontal pupil diameter, and UBM of the superior, temporal, inferior, and nasal ICA/CC in both eyes. Measurements were repeated 2 hours following ophthalmic atropine 1% solution application. Measurements of the ICA and CC, including pectinate ligament distance (PLD), CC length (CCL), height of opening distance (HOD), CC area (CCA), and pecti...
Behavioral and cardiorespiratory effects of a medetomidine and tramadol combination in horses. The use of combinations of sedative and analgesic drugs during standing procedures in horses is necessary to provide reliable sedation with minimal ataxia and reduced responses to surgical or other stimuli in horses. Objective: This study assessed the behavioral and cardiorespiratory effects of medetomidine (M) administered with and without tramadol (T) in horses. Methods: Eight horses were sedated intravenously with M (5 µg/kg) alone or with T (2 mg/kg) in a arandomized, blind, two-way crossover trial. Behavioral responses, including head height above the ground (HHAG), postural instability ...
Molecular typing, biofilm characteristics and biofilm-targeted inhibition strategies of Streptococcus equi subsp. zooepidemicus isolated from donkey endometritis. Endometritis is a major cause of infertility in intensively farmed donkeys. Streptococcus equi subsp. zooepidemicus (SEZ) is a predominant pathogen that readily forms biofilms in equine endometritis, conferring resistance to conventional treatments. Objective: This study aimed to characterize the biofilm dynamics of SEZ isolates obtained from donkeys and to evaluate potential anti-biofilm strategies with different drug combinations. Methods: Uterine lavage samples were collected from 30 Dezhou Black donkeys with clinical endometritis. Bacterial cultures were performed on blood agar and MacConk...
Analytical Challenges and Emerging Detection Strategies of Synthetic Cannabinoids in Horse Doping Control. Synthetic cannabinoids (SCs) were originally synthesized to advance the understanding of the endocannabinoid system, facilitate disease research, and support the development of novel therapeutic agents. Compared with tetrahydrocannabinol, these compounds exhibit substantially higher psychoactive potency and enhanced receptor-binding affinity. The rapid and continuous evolution of SC derivatives presents significant challenges for analytical laboratories and increases the risk of misuse. Furthermore, SCs may be exploited to alter performance in both human and animal sports. The scarcity of comp...
Pharmacokinetics of 2 mg/kg Bupivacaine in a Rectus Abdominis Sheath Block in Horses. Administering large volumes of bupivacaine in the rectus abdominis sheath (RAS) block in horses could cause local anesthetic toxicity. This study aimed to evaluate the pharmacokinetics of 2 mg/kg bupivacaine in RAS blocks and the associated toxicity risk. Six healthy adult horses were sedated with xylazine and received an ultrasound-guided bilateral 2-point RAS block. Plasma samples were collected at baseline and from 5 min to 24 h after the block and analyzed using liquid chromatography-tandem mass spectrometry. A noncompartmental analysis was performed to determine the maximum concentr...
Nitric oxide and its role in the management of hypoxaemia in the anaesthetised horse-a narrative review. To outline historical aspects of nitric oxide, including its discovery and biological effects, to describe the current use of inhaled nitric oxide (iNO) in human healthcare, and to review the available evidence on the use of pulsed iNO (PiNO) for the management of hypoxaemia in anaesthetised horses. Methods: Google Scholar and PubMed databases were searched using the search terms nitric oxide, PiNO, environment, discovery, acute respiratory distress syndrome, COVID-19, SARS-CoV-2, horse, pony, hypoxaemia, and anaesthesia. Conclusions: Inhaled NO is licensed in the management of hypoxic respira...
Pharmacokinetics of Intramuscularly Administered Ketamine at Subanaesthetic Dosage in Horses. Subanaesthetic doses of ketamine (0.5 mg kg) provide analgesia in several species, but there is limited information on the pharmacokinetics and clinical effects of intramuscularly administered ketamine in horses. This study investigated the pharmacokinetics of ketamine and norketamine, and evaluated clinical effects, ataxia, and vital parameters, following intramuscular and intravenous administration of 0.5 mg kg ketamine in nine healthy horses, using a randomized two-period crossover design with a 1-week washout period. Plasma concentrations were analyzed using Ultra-High Performance ...
Plasma Concentrations Following Oral Administration of Two Different Forms of Resveratrol in Horses. Resveratrol is a compound found in multiple plants and there is evidence for its use as a supplement in horses, particularly through protection of chondrocytes. Previous studies on the clinical efficacy of resveratrol supplementation in horses have reported limited benefits. To date, there is no pharmacokinetic data of resveratrol in horses but the bioavailability of resveratrol in other species is poor. In this crossover study, the plasma concentrations of two forms of resveratrol were examined. Each horse received via nasogastric tube, either a single dose of resveratrol phospholipid or a st...
Synthesis and Characterization of Deuterated Detomidine for Use in Equine Medication Regulation. Detomidine, 5-[(2,3-dimethylphenyl)methyl]-1H-imidazole, is a tranquilizer/sedative/analgesic widely used in equine medicine and regulated by several different analyte concentrations of detomidine and its hydroxydetomidine and carboxydetomidine metabolites in plasma and urine. Accurate regulatory quantitation of detomidine at low picogram/mL concentrations requires the availability of a stable isotope internal standard of detomidine; however, to the best of our knowledge, no certified deuterated internal standard of detomidine is commercially available and its synthesis has not been reported. ...
Equine Protozoal Myeloencephalitis: An Ancient Parasite Meets Modern Compounding. EPM remains particularly rampant in racing populations due to transport stress, young age, and congregate housing conditions. For compounding pharmacists, understanding that we're managing chronic parasite suppression - not achieving cure - fundamentally changes our approach to formulation strategy, stability assessment, and client counseling. The two formulations presented separately represent years of refinement, demonstrating compounding's essential role when commercial products fall short.
Supramolecular Solvent Extraction for Doping Control Analysis of Prohibited Substances in Horse Urine. Despite the recent success in introducing supramolecular solvents (SUPRAS)-based extraction to drug analysis, its application and robustness in day-to-day regular urine testing have yet to be demonstrated. Moreover, the applicability of SUPRAS in equine doping control testing remains unexplored. In this work, we have successfully developed for the first time a simple, rapid, inexpensive, and environmentally friendly SUPRAS extraction method for analyzing 76 prohibited substances of different classes (selective androgen receptor modulators, hypoxia-inducible factor prolyl hydroxylase inhibitors...
Pharmacokinetic analysis and steady-state predictions of different preparations of metronidazole administered per rectum in adult horses. Manipulation of forms of rectally administered metronidazole to improve bioavailability in horses has not been reported. Objective: Evaluate the pharmacokinetics of 3 rectal metronidazole preparations compared to nasogastric (NG) administration. Methods: Seven healthy horses. Methods: Phase 1A was a randomized, 3-way crossover, single-dose pharmacokinetic study, and Phases 1B and 2 were non-randomized, single-dose follow-up studies. Metronidazole (20 mg/kg) was administered NG and rectally in water (RW20), as a rectal gel (RG), and in dimethyl sulfoxide (DMSO). Metronidazole (80 mg/kg) was a...
Cannabidiol-induced cellular and matrix-associated responses in primary equine sarcoid cells. Sarcoids are locally invasive skin tumors in equids, associated with bovine papillomavirus. Objective: Address potential applications of cannabidiol (CBD) in veterinary medicine. We evaluated the response of equine sarcoid cells to CBD in vitro, focusing on viability, invasiveness, and matrix remodeling. Methods: Three primary sarcoid cell lines. Methods: Cells were treated with CBD (20, 6.75, 2.25, 0.75 μM) and incubated for 6, 24, 48, 72 hours. Cell viability, cytotoxicity, and apoptosis were assessed using the ApoTox-Glo Assay. Based on these results, further analyses were performed for ...
Antibiofilm and resistance-modulating properties of tt-farnesol against Streptococcus equi subsp. equi and zooepidemicus. The aim of this study was to investigate the antibacterial, antibiofilm and modulating activities of trans-trans-farnesol (tt-farnesol) on two strains of Streptococcus equi subsp. equi and two strains of S. equi subsp. zooepidemicus, pathogenic or commensal bacteria of horses. Tt-farnesol showed bactericidal activity against all tested strains, with a minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) between 8 and 4 μg/mL. The sesquiterpene caused significant damage to the bacterial membrane, and its antibacterial activity did not appear to depend on oxidat...
Cannabidiol-rich extract suppresses the activation of proinflammatory genes IL-1β and IL-6 in equine mesenchymal stem cells stimulated with lipopolysaccharide. Peripheral nerve injuries (PNI) often lead to long-term functional impairment. Mesenchymal stem cells (MSCs) and cannabidiol (CBD) have shown anti-inflammatory and neuroprotective effects in vitro, which may be relevant for PNI research. The aim of this study was to evaluate CBD-rich cannabis extract’s potential to induce anti-inflammatory and neurotrophic gene expression in equine adipose tissue-derived MSCs (EqAT-MSCs) in an inflammatory in vitro environment. The morphology and metabolic activity of EqAT-MSCs (n = 4) were assessed after CBD-rich extract priming at concentrations of 3, ...
Pharmacopuncture with low-dose dexmedetomidine and saline aquapuncture at acupoint Governing Vessel 24 provides sedation in healthy adult horses. To evaluate sedation in horses following pharmacopuncture with dexmedetomidine at acupoint Governing Vessel 24 (GV-24) compared to aquapuncture at GV-24 or an equivalent dose of dexmedetomidine administered via IV or SC routes. Unassigned: 10 adult mares received 4 treatments in a blinded, randomized, crossover design: (1) dexmedetomidine administered at GV-24 (DexmedGV24; 1 μg/kg); (2) saline administered at GV-24 (SalineGV24; 1.5 mL); (3) dexmedetomidine administered SC on the lateral neck (DexmedSC; 1 μg/kg); or (4) dexmedetomidine administered IV (DexmedIV; 1 μg/kg). Sedation scores (fa...
Survey describing the perspectives and practices of Australian veterinarians to pain management in horses. To describe Australian practices and attitudes regarding equine analgesia. Methods: Cross-sectional anonymous, voluntary survey of Australian veterinarians treating equine patients. Methods: Australian veterinarians in equine or mixed practices completed a six-section, 60-question survey between November 2019 to August 2020. Information was gathered on demographics, analgesia prescription, pain assessment and attitudes surrounding specific analgesics. Respondents assigned a pain score ranging from 0 to 10 for various conditions; these were averaged to give each respondent an "average pain scor...
Effects of intravenous oxytocin on plasma serotonin and trainability in horses. Oxytocin (OXT) plays a crucial role in regulating the serotonin (5-HT) system and behavior. Although previous studies have reported significant relationships among OXT, 5-HT, and behavioral responses, the effects of OXT on 5-HT concentrations and behavioral traits in horses remain poorly understood. This study aimed to investigate the effects of intravenous OXT administration on plasma 5-HT concentrations and trainability in horses. A crossover design was employed using eight horses, each receiving either a 10-IU intravenous dose of OXT or normal saline. Blood samples were collected at baselin...
Treatment with ertugliflozin mitigates the hyperinsulinemic response to intra-articular triamcinolone acetonide. Intra-articular (IA) corticosteroids can cause hyperinsulinemia, which can subsequently increase the risk of laminitis, particularly in horses with insulin dysregulation (ID). Sodium glucose cotransporter 2 inhibitors (SGLT2i), a drug class that is being utilised more commonly in horses with insulin dysregulation, could potentially be used to control post-IA corticosteroid hyperinsulinemia. Objective: To determine whether treatment with the SGLT2i drug ertugliflozin decreases hyperinsulinemia following intra-articular corticosteroid administration in metabolically normal horses. Methods: Prosp...
Exposure to Subcutaneously Administered Butorphanol in Horses Pre-Treated With Detomidine or Detomidine-Vatinoxan. The aim of the study was to determine the exposure to subcutaneously administered butorphanol in horses pre-treated with intravenous (IV) detomidine, with or without vatinoxan, a peripherally selective alpha-adrenoceptor antagonist. Five healthy, adult horses received three IV treatments 7 days apart, in a randomized, cross-over design: detomidine 20 μg/kg (DET-B), detomidine 20 μg/kg with vatinoxan 200 μg/kg (DETVAT-B) and saline (S-B), all followed by 0.1 mg/kg of butorphanol administered subcutaneously 30 min later. Venous samples were collected between 10 and 270 min after...
Tafenoquine succinate inhibits the growth of the equine piroplasmosis hemoparasites Theileria equi and Babesia caballi. Equine piroplasmosis (EP) is a tick-borne disease of equids caused by the intraerythrocytic apicomplexan parasites Theileria equi, Babesia caballi and the recently identified Theileria haneyi. Acute cases can be severe, with anemia, jaundice, abortion or sudden death. Survivors remain lifelong carriers, serving as reservoirs for tick-borne and iatrogenic transmission. No vaccines are currently available, and control strategies rely heavily on accurate diagnostics and chemotherapeutic intervention. Imidocarb dipropionate (ID) is the current standard of care for both acute treatment and radical ...
Pharmacokinetics of Intragastric Ursodeoxycholic Acid and Its Impact on Bile Acid Profiles in Horses. Ursodeoxycholic acid (UDCA), a secondary bile acid (BA) with therapeutic applications, is standard therapy for cholestatic hepatopathies in humans. In recent years, its use has been increasingly explored in equine medicine for similar indications. Pharmacokinetic data for UDCA in horses are currently lacking. This study aimed to describe the pharmacokinetic parameters following a single intragastric administration of 15 mg/kg in nine healthy, fasted horses and to characterize the changes in their BA profiles. Plasma concentrations of UDCA were measured at specific time points using liquid ch...
