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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.
The effect of an alpha2-adrenoceptor antagonist on equine carbohydrate metabolism after intravenous glucose load. Vatinoxan is a peripherally acting alpha2-adrenoceptor antagonist used in veterinary medicine to attenuate the side effects of alpha2-adrenoceptor agonists. Vatinoxan also increases insulin response and reduces blood glucose (BG) after intravenous glucose in other species. The aim of this study was to investigate the effects of vatinoxan on BG and insulin concentration in horses after intravenous glucose. The design was an assessor-blind cross-over study. Nine horses were assigned to intravenous vatinoxan (0.2 mg/kg; VAT) or saline (SAL). Horses were administered an intravenous glucose bolus (...
Population pharmacokinetics and clinical evaluation of intravenous acetaminophen and its metabolites in Andalusian horses. To date, no intravenous pharmacokinetics (PK) studies have assessed acetaminophen or its major metabolites (acetaminophen-glucuronide and acetaminophen-sulphate) in horses. The influence of sex on acetaminophen metabolism in horses is unclear, and Monte Carlo simulations have not been applied to explore potential clinical applications. This study aimed to determine the intravenous PK and safety of acetaminophen in Andalusian horses at 10 and 20 mg/kg, evaluate sex as a covariate, and simulate clinical regimens. Twenty mares and twenty stallions received intravenous acetaminophen, and plasma ...
Evaluation of the Effects of Detomidine on Equine Myoelectrical Activity Using Electrointestinography. To evaluate the effects of detomidine on equine intestinal slow-wave activity and frequency distribution measured by electrointestinography (EIG). Methods: Prospective, experimental study. Methods: University teaching hospital. Methods: A convenience sample of twelve 7- to 21-year-old clinically normal horses. Methods: Horses were randomly assigned to saline control (four horses) or detomidine treatment (eight). After obtaining a 30-min baseline EIG, a saline or detomidine bolus was administered, followed by a constant rate infusion, and another EIG was recorded. Ultrasonographic examinations ...
Metformin and rosiglitazone affect motility, lipid peroxidation and mitochondrial activity of thawed equine spermatozoa. Maintaining sperm energy homeostasis in vitro is very important to improve the efficacy of stallion sperm preservation. Equine spermatozoa preferentially utilize oxidative phosphorylation over glycolysis to generate ATP. Metformin and rosiglitazone are antidiabetic compounds that enhances metabolic flexibility and glucose utilization. The aim of this study was to evaluate metformin and rosiglitazone supplementation of the freezing medium on quality and oxidative status of thawed stallion semen. A total of 15 ejaculates from five horses were collected and supplemented before freezing with metfo...
Exploring the genetic influences on equine analgesic efficacy through genome-wide association analysis of ranked pain responses. Multimodal analgesic administration is a promising strategy for mitigating side effects typically associated with analgesia; nevertheless, variation in analgesic effectiveness still poses a considerable safety concern for both horses and veterinarians. Pharmacogenomic studies have started delving into genetic influences on varying drug effectiveness and related side effects. However, current findings have narrow implications and are limited in their ability to individualize analgesic dosages in horses. Hydromorphone and detomidine were administered to a cohort of 48 horses at standardized time...
Intratumoural tigilanol tiglate in the multicentre treatment of equine sarcoids and cutaneous melanomas. Intralesional chemotherapeutic administration represents an important treatment option for equine cutaneous neoplasia. Tigilanol-tiglate (TT), a novel molecule extracted from Fontainea picrosperma, an Australian rainforest plant, is registered for intratumoural treatment of canine MCT, leading to rapid oncosis and tumour slough. Evidence from horses is limited but suggests that efficacy may be similar. Objective: To evaluate the response to intratumoural TT treatment in horses with sarcoids (fibroblastic/nodular) and cutaneous melanomas. Methods: Two noncontrolled prospective multicentre clini...
Cardiopulmonary effects of oral trazodone administration prior to isoflurane anesthesia in healthy horses. To determine the cardiopulmonary effects of oral trazodone before isoflurane anesthesia in systemically healthy horses. Unassigned: 12 horses donated for euthanasia (from August 2022 through June 2023) due to conditions unrelated to the cardiovascular system were included in this prospective, randomized, controlled trial. Horses were assigned to receive oral trazodone (6 mg/kg; n = 7) or corn syrup (n = 5) 1 hour before xylazine (1 mg/kg, IV) sedation, ketamine (2.2 mg/kg, IV) and propofol (0.7 mg/kg, IV) induction, and anesthetic maintenance with inhaled isoflurane (target 1.6% expired) for 7...
Effects of vatinoxan on gastrointestinal motility, sedation, and antinociception during and after long-lasting detomidine infusion in horses. Sedation in horses is typically achieved using alpha-2 adrenoceptor agonists, although their use is associated with multiple side effects. A peripheral alpha-2 adrenoceptor antagonist, vatinoxan, can alleviate many of these. Objective: To evaluate the effects of vatinoxan infusion on gastrointestinal motility, sedation, and antinociception in horses sedated with detomidine infusion. Methods: Randomised, blinded cross-over in vivo experiments. Methods: Eight horses were given two 4-h infusions: detomidine (0.01 mg/kg + 0.015 mg/kg/h IV) (DET) and a combination of detomidine and vatinoxa...
Testing for trazodone, an antidepressant, in hair collected from horses. Trazodone, a medicine registered for human, is a serotonin agonist-antagonist. At low dose, the drug is sedative due to its antagonist properties. At high dose, it is an agonist with anxiolytic and antidepressant actions. Trazodone can be administered to the horse to reduce anxiety. However, according to the anti-doping rules for horses, the presence of trazodone in blood or urine is considered as a violation which will produce a suspension of both the athlete and the horse as the drug is listed banned on the International Federation of Horseracing Authorities prohibited substances list. As a ...
Dobutamine improves haemodynamics and oxygen delivery in standing and isoflurane-anaesthetised horses. Dobutamine is a first-line therapy for hypotension in anaesthetised horses, but the effects on haemodynamic parameters in standing and anaesthetised horses are not well studied. Objective: To investigate the effects of dobutamine in escalating dosages on haemodynamic performance in awake and anaesthetised horses. Methods: Randomised cross-over experimental study. Methods: Six healthy adult horses were enrolled, including both standing and isoflurane-anaesthetised experiments with 1-week washout. Heart rate, mean arterial pressure (MAP), central venous pressure, pulmonary arterial pressure, and...
Systemic, hemodynamic and neurological effects of caudal epidural administration of Neosaxitoxin in horses. The present study was conducted to evaluate the safety and the long-lasting anesthetic properties of Neosaxitoxin (NeoSTX) when injected into the intercoccygeal space in standing horses. A group of eighteen (n = 18) healthy client-owned mature crossbreed horses were enrolled in this study. Caudal epidural injection was ascertained by two methods, the "hanging drop" technique and radiographs. Horses were allocated into three groups (n = 6) each group receiving different dosages of NeoSTX. To assess the onset of action and duration of anesthesia, six horses received 20 μg in 2 mL, six 20...
Synthesis and Characterization of 3-Hydroxybupivacaine and Deuterated 3-Hydroxybupivacaine for Use in Equine Medication Regulation. Bupivacaine is a local anesthetic widely used in equine and human medicine. Use of bupivacaine in performance horses is regulated because its ability to block pain means that it can be misused for advantage in performance horses. In racing regulation, bupivacaine is classified by the Association of Racing Commissioners International (ARCI) as a Class 2 Penalty Class A Foreign substance, the detection of which can lead to significant penalties. In horses, bupivacaine is metabolized by Phase-I hydroxylation to yield 3-hydroxybupivacaine, which is then glucuronidated to yield the Phase-II metabol...
Evaluation of Celastrol Antiviral Activity Against Equid Alphaherpesvirus Type 8 Infection. Equid alphaherpesvirus type 8 (EHV-8) is a contagious pathogen that causes reproductive disorders, respiratory diseases, and viral encephalitis in equids, resulting in significant economic losses for the global horse and donkey industries. Currently, there are no approved antiviral drugs or vaccines available for EHV-8 control. In this study, we investigated the antiviral efficacy of celastrol against EHV-8 both in vitro and in vivo. Our results demonstrated that celastrol significantly inhibited EHV-8 infection in Rabbit kidney (RK-13) and equine dermal cells (NBL-6) in a dose-dependent manne...
Effect of Phenylbutazone Administration on Insulin Sensitivity in Horses With Insulin Dysregulation. Phenylbutazone is prescribed to manage pain caused by hyperinsulinemia-associated laminitis. Phenylbutazone reduces glucose and insulin concentrations in horses with insulin dysregulation (ID) but the underlying mechanism of action is unknown. Objective: Investigate the effect of phenylbutazone on tissue insulin sensitivity in horses. It is hypothesized that the reduced glucose and insulin concentrations in horses with ID receiving phenylbutazone are mediated by a higher tissue insulin sensitivity. Methods: Fifteen light breed horses, including seven with ID. Methods: Randomized cross-over stu...
Equine neutrophils selectively release neutrophil extracellular traps in response to chemical and bacterial agonists. Neutrophil extracellular traps (NETs) play a significant role in response to a variety of infectious and inflammatory stimuli in human and veterinary medicine. Although entrapment of bacteria can be an important function of NETs, the exuberant release of DNA and other intracellular molecules has also been negatively implicated in the pathogenesis of different diseases. Thus, NET formation must be tightly controlled and represents an opportunity for therapeutic interventions. Horses are particularly sensitive to bacterial stimuli that have previously been shown to cause NETs in other species, b...
Effects of constant intravenous infusion of detomidine alone or combined with butorphanol or methadone for standing sedation in horses: A randomized clinical trial. This study aimed to evaluate the sedation degree, cardiopulmonary effects, and detomidine-sparing during dental occlusal adjustment in standing horses using a bolus and constant rate infusion (CRI) of detomidine alone or in combination with butorphanol or methadone. In this randomized, blinded clinical trial, 24 healthy adult horses were assigned to the detomidine (DT), detomidine-butorphanol (DB), or detomidine-methadone (DM) group. DT received an intravenous bolus of detomidine (20 μg/kg), followed by CRI at 20 μg/kg/h. DB received detomidine (10 μg/kg) and butorphanol (0.02 mg/kg) boluse...
Pharmacokinetics of a single oral administration of two cannabidiol formulations in fed and fasted horses. Pain management in horses plays a pivotal role in the therapeutic approach to several diseases. Horses have cannabinoid receptors at the level of dorsal root ganglia, blood vessels, and synoviocytes that can be up or down- regulated by inflammatory conditions, justifying the possible efficacy of exogenous cannabinoids (i.e., phytocannabinoids) in managing several painful pathologies in this animal species. However, the current use of supplements containing cannabidiol (CBD) in equines is based on anecdotal evidence, without the support of sufficient pharmacokinetic studies. In humans, the conc...
Effect of pergolide treatment on insulin dysregulation in horses and ponies with pituitary pars intermedia dysfunction. Due to the high frequency of laminitis reported for both conditions, the relationship between pituitary pars intermedia dysfunction (PPID) and insulin dysregulation (ID), and the potential role of dopamine in modifying insulin secretion, requires further investigation. Objective: To evaluate the effect of pergolide mesylate on insulin sensitivity and postprandial insulin and glucose responses in horses and ponies with ID, both with or without concurrent PPID. Methods: Randomised crossover study. Methods: Sixteen horses and ponies, comprising eight matched pairs (PPID+ID or ID-only), were given...
Assessing omeprazole and flunixin meglumine co-administration in treating equine gastric ulcer syndrome in Mongolian horses. Flunixin meglumine (FM) is commonly used in painful conditions in horses; however, it may contribute to equine gastric ulcer syndrome (EGUS). Some veterinarians combine omeprazole (OME) and FM to reduce EGUS risk. However, the efficacy and safety of this combination in Mongolian horses with chronic lameness remain unknown. Objective: To investigate the changes in lameness and EGUS scores in Mongolian horses through the comparison of three treatment strategies: FM, FM + OME and placebo treated control (CON) and to assess the effects of these treatments on gastric fluid pH, serum total prote...
Analgesic and Gastrointestinal Effects of Morphine in Equines. Morphine has significant clinical and analgesic effects in horses, but its impact on the gastrointestinal tract requires further understanding. This study assessed the analgesic and gastrointestinal effects of morphine in horses undergoing elective orchiectomy in the quadrupedal position. Thirty uncastrated male horses were randomly assigned to three groups: orchiectomy without morphine and sedation protocol (OSM), orchiectomy with morphine and sedation protocol (OM), and administration of morphine alone in the absence of orchiectomy (M). The anesthetic protocol involved acepromazine (0.05 mg/...
Dexamethasone administration transiently increases insulin response to an oral carbohydrate challenge in horses. Dexamethasone is used to experimentally induce insulin resistance; however, its impact on insulin secretion is unclear. This study aimed to assess the responses to oral carbohydrate challenges in dexamethasone-treated horses. Unassigned: 8 healthy Standardbreds received 0.08 mg/kg of dexamethasone IM every 48 hours for 14 days in June 2022 (winter in the Southern hemisphere). Oral glucose tests (OGT) were conducted before treatment (day 1) and on days 8 and 15. Glucose, insulin, triglycerides, total and active glucagon-like peptide-1 (tGLP-1 and aGLP-1) and glucose-dependent insulinotropic pol...
Echocardiographic and clinical effects of two sedative doses of Dexmedetomidine in healthy horses. The effects of dexmedetomidine (DEX), as a sedative drug, on echocardiographic measurements have been investigated in many species but not in horses. Therefore, this study aimed to evaluate the echocardiographic and clinical effects of two sedative doses of DEX in healthy horses. Six female crossbred horses weighted 250-330 kg underwent echocardiography before and after sedation by intravenous administration of a low dose of 3.5 μg/kg (LD) and a high dose of 7 μg/kg (HD) of DEX. A significant increase (p≤ 0.05) was observed in the diameters of the pulmonary artery and the left atrium measu...
Imaging flow cytometry reveals the mechanism of equine arteritis virus entry and internalization. The process of viral entry into host cells is crucial for the establishment of infection and the determination of viral pathogenicity. A comprehensive understanding of entry pathways is fundamental for the development of novel therapeutic strategies. Standard techniques for investigating viral entry include confocal microscopy and flow cytometry, both of which provide complementary qualitative and quantitative data. Imaging flow cytometry, which integrates the advantages of both methodologies, offers significant potential in virological studies. In this investigation, we employed imaging flow ...
Screening analysis of doping agents in horse urine and plasma with dilute and shoot using liquid chromatography high resolution mass spectrometry. Various technical methodologies are required to accurately detect substances of different chemical and pharmacological properties in biological samples, which are increasing in number and variety daily. Therefore, laboratories where many samples and different factors are analyzed simultaneously need methods with easy sample preparation, short analysis times and low analysis costs. In this study, the objective was to scan substances susceptible to chemical degradation, amenable to analysis without hydrolysis, and exhibiting short-term stability by employing a straightforward, expeditious, and c...
Retrospective evaluation of the effect of xylazine infusion on survival to discharge in horses undergoing exploratory laparotomy for colic. To determine the influence of xylazine infusion on survival to discharge and describe the associated intraoperative requirement for isoflurane, use of positive inotropes and vasopressors, and recovery time in horses undergoing exploratory laparotomy. Methods: Retrospective cohort study. Methods: A total of 352 horses. Methods: Medical records of horses undergoing anesthesia for exploratory laparotomy from January 2018 to December 2023 were reviewed. Data collected included survival to discharge, results of diagnostic tests, end tidal isoflurane concentration (FE'Iso), use of vasopressors/inotr...
Comparing the effectiveness of four antihistamines with olopatadine in healthy Thoroughbred horses. We compared the antihistamine effect of four new antihistamines with olopatadine, which is used to treat equine allergic diseases. Six healthy Thoroughbred horses received oral doses of olopatadine (50 mg), levocetirizine (50 mg), bilastine (200 mg), rupatadine (100 mg), and desloratadine (50 mg) at >2-week intervals. The effects were investigated by measurement of the wheal area induced by histamine intradermal injection, and inhibition rate was compared with positive and negative controls. The maximum wheal inhibition rate (mean ± SD) of olopatadine (85.3% ± 7.7%) was significantly high...
3′-deoxytubercidin: A potent therapeutic candidate for the treatment of Surra and Dourine. Surra and Dourine are widespread diseases caused by two protozoan parasites Trypanosoma brucei evansi and Trypanosoma brucei equiperdum, respectively. A wide range of animals including camels, horses, cattle and buffaloes are susceptible to infection. These diseases pose a significant socio-economic burden, primarily due to the limited therapeutic options and the complications associated with toxicity and drug resistance, making disease management particularly challenging. This study evaluated the potential of 3'-deoxytubercidin, a previously identified antitrypanosomal nucleoside, as a therap...
Effect of rapid and slow intravenous injection of sodium penicillin on arterial blood pressure in isoflurane-anesthetized horses during surgery. To determine the effects of rapid (1 minute) and slow (10 minutes) intravenous (IV) injection of sodium penicillin on arterial blood pressure in anesthetized horses. Methods: Prospective randomized clinical trial. Methods: A group of 29 client-owned horses of various breeds, 1-20 years old, with body masses of 360-710 kg. Methods: General anesthesia was induced with a variety of anesthetic protocols and maintained with isoflurane under mechanical ventilation, with hourly doses of IV lidocaine and an infusion of dexmedetomidine. Horses were administered IV intraoperative penicillin every 2 hour...
Preparation of Molecularly Imprinted Electrochemical Sensors and Analysis of the Doping of Epinephrine in Equine Blood. In this paper, a novel molecularly imprinted polymer membrane modified glassy carbon electrode for electrochemical sensors (MIP-OH-MWCNTs-GCE) for epinephrine (EP) was successfully prepared by a gel-sol method using an optimized functional monomer oligosilsesquioxane-AlO sol-ITO composite sol (ITO-POSS-AlO). Hydroxylated multi-walled carbon nanotubes (OH-MWCNTs) were introduced during the modification of the electrodes, and the electrochemical behavior of EP on the molecularly imprinted electrochemical sensors was probed by the differential pulse velocity (DPV) method. The experimental conditi...
