Topic:Drug
The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
[New drugs for horses and production animals in 2021]. In 2021, one novel pharmaceutical agent for horses or food-producing animals was released on the German market, making the anti-haemorrhagic etamsylate (Hemosilate) available for horses, cattle, pigs, sheep, goats, dogs and cats, for the first time. The authorization of one established veterinary active ingredient was extended to an additional species: The endectocide eprinomectin (Eprecis) from the group of macrocyclic lactones was also approved for sheeps and goats. Additionally, two veterinary formulations with a new active substance content (bromhexine, tiamulin) and one active ingredient ...
Equus roundworms (Parascaris univalens) are undergoing rapid divergence while genes involved in metabolic as well as anthelminic resistance are under positive selection. The evolution of parasites is often directly affected by the host's environment. Studies on the evolution of the same parasites in different hosts are of great interest and are highly relevant to our understanding of divergence. Methods: Here we performed whole-genome sequencing of Parascaris univalens from different Equus hosts (horses, zebras and donkeys). Phylogenetic and selection analyses were performed to study the divergence and adaptability of P. univalens. Results: At the genetic level, multiple lines of evidence indicate that P. univalens is mainly separated into two clades (horse-de...
Is the Use of Bisphosphonates Putting Horses at Risk? An Osteoclast Perspective. Osteoclasts are unique and vital bone cells involved in bone turnover. These cells are active throughout the individual's life and play an intricate role in growth and remodeling. However, extra-label bisphosphonate use may impair osteoclast function, which could result in skeletal microdamage and impaired healing without commonly associated pain, affecting bone remodeling, fracture healing, and growth. These effects could be heightened when administered to growing and exercising animals. Bisphosphonates (BPs) are unevenly distributed in the skeleton; blood supply and bone turnover rate determ...
In vitro and in vivo evaluation of kinase and protease inhibitors against Trypanosoma evansi. Trypanosoma evansi is a causative agent of chronic wasting and fatal disease of livestock and wild animals known as surra. In this study, repurposing approach based on drug target was used to investigate the efficacy of kinase inhibitors (Barasertib-HQPA, BAR and Palbociclib isethionate, PAL) and protease inhibitors (Z-pro-prolinal, Z-PRO and Leupeptin hemisulphate, LEU) against T. evansi in HMI-9 medium. BAR, PAL and Z-PRO exhibited IC values of 13.52 µM, 0.6375 µM and 63.20 µM against T. evansi in terms of growth inhibition, in the contrary, LEU failed to exhibit a significant growth i...
Characterization of growth hormone secretagogue small molecule ibutamoren (MK-0677) and its possible metabolites in thoroughbred horses for doping control. It is important to remember that performance-enhancing agents such as non-peptide growth hormone secretagogues present a significant risk of abuse. Ibutamoren (MK-0677) is a potent, long-acting, selective non-peptide growth hormone secretagogue that can be taken orally. Methods: This study examines ibutamoren and its metabolites in thoroughbred horses after oral administration. Liquid chromatography/high-resolution mass spectrometry was used to determine the probable structures of the detected metabolites. Results: In this study, 22 metabolites of ibutamoren were identified (17 phase I and 5 p...
Comparison of hydromorphone and butorphanol for management of pain in equine patients undergoing elective arthroscopy: a randomized clinical trial. To compare the effects of hydromorphone and butorphanol in horses undergoing arthroscopy and describe the pharmacokinetics of hydromorphone in anesthetized horses. Methods: Randomized controlled clinical trial. Methods: A total of 40 adult horses admitted for elective arthroscopy. Methods: Horses were randomly assigned to be administered intravenous hydromorphone (0.04 mg kg-1; group TxH; n = 19) or butorphanol (0.02 mg kg-1; group TxB; n = 21) prior to surgery as part of a standardized anesthetic protocol. Pain was scored by two observers unaware of group assignment using the Equine Utrecht...
Polidocanol monotherapy for a superficial orbital venous malformation in a horse. To describe the use of 1% polidocanol as the sole treatment for a superficial orbital venous malformation in a horse. Methods: A 23-year-old Welsh Cobb cross gelding with a distensible swelling affecting the left lower eyelid, and secondary palpebral margin abnormalities and superficial keratitis. Methods: Color flow Doppler ultrasonography revealed non-pulsatile blood flow within the tortuous vascular network most consistent with a superficial orbital venous malformation appearing to involve the lateral palpebral and transverse facial veins. An intravenous catheter was placed within the later...
Pharmacokinetics of grapiprant and effects on TNF-alpha concentrations following oral administration to horses. Grapiprant is a prostaglandin E2 receptor antagonist that has been found to be an effective anti-inflammatory in dogs and that is devoid of some of the adverse effects associated with traditional NSAIDs that elicit their effects through inhibition of PGE2 production. Previously published reports have described the pharmacokinetics of this drug in horses when administered at 2 mg/kg; however, pharmacodynamic effects in this species have yet to be described. The objective of the current study was to describe the pharmacokinetics and pharmacodynamics of grapiprant at a higher dose. Eight horses...
Opioid-free sedation for atlantoaxial cerebrospinal fluid collection in adult horses. Atlantoaxial (AA) cerebrospinal fluid (CSF) collection in standing horses utilizes the controlled narcotic morphine, thereby limiting feasibility in field practice settings. Objective: To compare AA CSF collection time and reaction scores in horses sedated with morphine-containing and opioid-free sedation protocols: detomidine + morphine (DM), detomidine + xylazine (DX), detomidine + detomidine (DD), detomidine alone (D0); To develop a novel method for assessing sedation in standing horses using open-source motion-tracking software. Methods: Six healthy adult horses. Methods: Randomi...
Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses. In humans, codeine is a commonly prescribed analgesic that produces its therapeutic effect largely through metabolism to morphine. In some species, analgesic effects of morphine have also been attributed to the morphine-6-glucuronide (M6G) metabolite. Although an effective analgesic, administration of morphine to horses produces dose-dependent neuroexcitation at therapeutic doses. Oral administration of codeine at a dose of 0.6 mg/kg has been shown to generate morphine and M6G concentrations comparable to that observed following administration of clinically effective doses of morphine, witho...
Pharmacokinetic-Pharmacodynamic Study of Ampicillin-Cloxacillin Combination in Indian Thoroughbred Horses (Equus caballus) and Safety Evaluation of the Computed Dosage Regimen. The pharmacokinetics of ampicillin-cloxacillin, given as single intravenously dose of 10 mg.kg-1 (5 mg.kg-1 of ampicillin plus 5 mg.kg-1 of cloxacillin) was examined in clinically presented Indian thoroughbred horses (n = 6) in order to design appropriate dosing strategies. Drug concentrations in plasma were determined by high performance liquid chromatography (HPLC) and pharmacokinetic parameters were derived by non-compartmental analysis using WinNonlin software. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of ampicillin-cloxacillin against qualit...
Sporadic worldwide “clusters” of feed driven Zilpaterol identifications in racing horses: a review and analysis. Zilpaterol is a β2-adrenergic agonist medication approved in certain countries as a cattle feed additive to improve carcass quality. Trace amounts of Zilpaterol can transfer to horse feed, yielding equine urinary "identifications" of Zilpaterol. These "identifications" occur because Zilpaterol is highly bioavailable in horses, resistant to biotransformation and excreted as unchanged Zilpaterol in urine, where it has a 5 day or so terminal half-life.In horses, urinary steady-state concentrations are reached 25 days (5 half-lives) after exposure to contaminated feed. Zilpaterol readily presen...
Retrospective Analysis of the Use of Tiludronate in Equine Practice: Safety on 1804 Horses, Efficacy on 343 Horses. The objective of this retrospective study was to assess the safety and efficacy of a slow IV administration of 1mg/kg tiludronate in a large number of horses. Each horse that received at least one tiludronate-based treatment between 2006 and August 2019 at Virginia Equine Imaging or Fairfield Equine was included in the study. Concomitant medical treatments, preliminary nonsteroidal anti-inflammatory drug injection and potential side effects were recorded after each administration. Horses for which follow-up was available over 1 year were subject to clinical evolution assessment via lameness gr...
Morphine with or without Acepromazine in Horses: A Kinematic Evaluation. The objective was to demonstrate walking locomotor pattern alterations after co-administration of acepromazine and morphine in horses. Six mature horses receiving four different treatments were used. Treatments consisted of a single dose of saline solution, 0.2 mg/kg bwt of morphine hydrochloride, 0.02 mg/kg bwt of acepromazine maleate, and a combination of 0.2 mg/kg bwt of morphine hydrochloride with 0.02 mg/kg bwt of acepromazine maleate. A three-dimensional accelerometric device was used to collect data. Walking tests were performed 10 min prior to injection, and then at 5, 10, 15, and 20 m...
Ivermectin-induced gene expression changes in adult Parascaris univalens and Caenorhabditis elegans: a comparative approach to study anthelminthic metabolism and resistance in vitro. The nematode Parascaris univalens is one of the most prevalent parasitic pathogens infecting horses but anthelmintic resistance undermines treatment approaches. The molecular mechanisms underlying drug activity and resistance remain poorly understood in this parasite since experimental in vitro models are lacking. The aim of this study was to evaluate the use of Caenorhabditis elegans as a model for P. univalens drug metabolism/resistance studies by a comparative gene expression approach after in vitro exposure to the anthelmintic drug ivermectin (IVM). Methods: Twelve adult P. univalens worms...
Parasympathetic Tone Changes in Anesthetized Horses after Surgical Stimulation, and Morphine, Ketamine, and Dobutamine Administration. Autonomic nervous system (ANS) activity can modify cardiovascular parameters in response to nociceptive stimuli or drugs in anesthetized animals. The aim of this study was to determine if a surgical nociceptive stimulus and morphine, ketamine, and dobutamine administration would modify ANS activity observed as a change in the mean parasympathetic tone activity (PTAm) in anesthetized horses. In 20 anesthetized horses, heart rate (HR), mean arterial pressure (MAP), and PTAm were monitored before and 1, 3, and 5 min after surgical incision, and before and 10 min after the administration of morphi...
Effects of Intravenous Antimicrobial Drugs on the Equine Fecal Microbiome. Alterations in the gastrointestinal microbiota after antimicrobial therapy in horses can result in loss of colonization resistance and changes in bacterial metabolic function. It is hypothesized that these changes facilitate gastrointestinal inflammation, pathogen expansion and the development of diarrhea. The objectives of this study were to determine the effect of intravenous administration of antimicrobial drugs (ceftiofur, enrofloxacin, oxytetracycline) on equine fecal bacterial communities over time, to investigate whether those changes are detectable after 5 days of treatment and whether...
Intelligence benefit of the 3-methoxytyramine to tyramine ratio in equine urine. Equine urine analysis has evolved over time to detect thousands of urinary compounds for doping control in the horse racing industry. The longitudinal assessment of 3-methoxytyramine to tyramine ratio (3-MT/T) values in equine urine by GC-MS profiling was investigated to support the Racing NSW Equine Biological Passport (EBP) for detection of dopaminergic manipulation in racehorses. This involved comparison of routine urine samples to administration studies of Sinemet, a common Parkinson's disease medication containing levodopa. Using an endogenous reference compound (ERC) in a urinary ratio e...
First study on diversity and antimicrobial-resistant profile of staphylococci in sports animals of Southern Thailand. Staphylococci are commensal bacteria and opportunistic pathogens found on the skin and mucosa. Sports animals are more prone to injury and illness, and we believe that antimicrobial agents might be extensively used for the treatment and cause the existence of antimicrobial-resistant (AMR) bacteria. This study aimed to investigate the diversity and AMR profile of staphylococci in sports animals (riding horses, fighting bulls, and fighting cocks) in South Thailand. Unassigned: Nasal (57 fighting bulls and 33 riding horses) and skin swabs (32 fighting cocks) were taken from 122 animals. Staphyloc...
Equine ulcerative keratitis in Belgium: Associated bacterial isolates and in vitro antimicrobial resistance in 200 eyes. To describe bacterial isolates and associated antibiotic resistance from horses with ulcerative keratitis in Belgium. Methods: Medical records from horses with ulcerative keratitis presented to the ophthalmology service of the Veterinary teaching hospital of Liege, Belgium, between 2014 and 2021 were evaluated. Bacterial isolates were identified and VITEK® 2 (Biomérieux) provided antimicrobial susceptibility testing and resistance detection. Results: Two hundred eyes of 196 horses were sampled. Ninety-seven eyes had a positive bacterial culture (48.5%) and 139 bacterial isolates were identif...
Anti-Methanogenic Traits of Safflower Oil Compounds Against Methyl-Coenzyme M Reductase Receptor in Equines: An In Silico Docking Analysis. Greenhouse gases emission from livestock is the major concern for the ecosystem. Despite the lower contribution of non-ruminants towards greenhouse gas emission as compared to the ruminants, the emission of methane (CH) gas from equines is expected to be increased in future due to its increasing population. Thus, it is essential to find or screen potential anti-methanogenic agent in a cost-effective and quicker manner. Considering this, the present investigation was aimed to analyze anti-methanogenic characteristic of bioactive compounds of safflower oil by targeting methanogenesis catalyzing ...
Concentration of amikacin sulphate in synovial fluid when given in combination with dexamethasone phosphate in intravenous regional limb perfusion in standing horses. Eight horses underwent IVRLP at two occasions through a 23-gauge 2 cm long butterfly catheter. Regional anaesthesia of the ulnar, median and medial cutaneous antebrachial nerves was performed prior, and an 8 cm rubber tourniquet was placed on the proximal radius for 30 minutes following the infusion. The first infusion consisted of 2 g of amikacin sulphate and 10 mg of dexamethasone phosphate diluted with 0.9% NaCl to a total volume of 100 ml. The second perfusion was performed after a 2-week washout period, the same protocol was used but without dexamethasone phosphate. Synovial fluid s...
Nanoforming Hyaluronan-Based Thermoresponsive Hydrogels: Optimized and Tunable Functionality in Osteoarthritis Management. Hyaluronic acid (HA) constitutes a versatile chemical framework for the development of osteoarthritis pain treatment by means of injection in the joints, so-called viscosupplementation. Without appropriate physico-chemical tuning, such preparations are inherently hindered by prompt in vivo degradation, mediated by hyaluronidases and oxidative stress. To prolong hydrogel residence time and confer optimized product functionality, novel thermoresponsive nanoforming HA derivatives were proposed and characterized. Combined use of sulfo-dibenzocyclooctyne-PEG4-amine linkers and poly(N-isopropylacryl...
Long-term monitoring of IOX4 in horse hair and its longitudinal distribution with segmental analysis using liquid chromatography/electrospray ionization Q Exactive high-resolution mass spectrometry for the purpose of doping control. IOX4, a hypoxia-inducible factor stabilizer, is classified as a banned substance for horses in both horse racing and equestrian sports. We recently reported the pharmacokinetic profiles of IOX4 in horse plasma and urine and also identified potential monitoring targets for the doping control purpose. In this study, a long-term longitudinal analysis of IOX4 in horse hair after a nasoesophageal administration of IOX4 (500 mg/day for 3 days) to three thoroughbred mares is presented for the first time for controlling the abuse/misuse of IOX4. Six bunches of mane hair were collected at 0 (pre), ...
Measurements of hydrocortisone and cortisone for longitudinal profiling of equine plasma by liquid chromatography-tandem mass spectrometry. The conventional detection of exogenous drugs in equine doping samples has been used for confirmation and subsequent prosecution of participants responsible. In recent years, alternative methods using indirect detection have been investigated due to the expanding number of pharmaceutical agents available with the potential of misuse. The monitoring of endogenous biomarkers such as hydrocortisone (HC) has been studied in equine urine with an international threshold of 1 μg/ml established; however, there is no current threshold for equine plasma. The aim of this research was to investigate pl...
Effect of perfusate volume on amikacin concentrations after saphenous intravenous regional limb perfusion in standing, sedated horses. To determine the influence of perfusate volume on synovial fluid amikacin concentrations in the joints of the hind limb after standing saphenous intravenous regional limb perfusion (IVRLP). Methods: Randomized crossover design. Methods: Six adult horses. Methods: Saphenous IVRLP was performed in 6 standing horses with 1 g of amikacin diluted with 0.9% NaCl to volumes of 10 ml, 60 ml, and 120 ml. Samples of synovial fluid from the tarsocrural, metatarsophalangeal, and hind limb distal interphalangeal joints were collected at 15 and 30 min after perfusate administration. Concentrations ...
Acquisition and use of analgesic drugs by horse owners in the United States. Little is known about the acquisition and use of equine analgesic drugs by horse owners in the United States (US). Objective: To determine factors associated with possession of analgesic drugs by horse owners in the US or with analgesic drug acquisition from sources noncompliant with a valid veterinarian-client-patient (VCPR) relationship. Methods: Cross-sectional survey. Methods: An internet-based questionnaire included items related to experiences with horses and equine analgesic drugs. Factors associated with possession of ≥5 types of analgesic drugs and with the acquisition of drugs from...
Comparative Evaluation of the Sedative and Analgesic Effects of Caudal Epidural Administration of Lidocaine Alone or in Combination With Xylazine, Detomidine, Medetomidine, and Dexmedetomidine in Mediterranean Miniature Donkeys. The present study aimed to compare the sedative and analgesic effects of caudal epidural administration of lidocaine alone or in combination with four different α-adrenergic agonists in Mediterranean miniature donkeys. A total of ten clinically healthy (five males and five females) Mediterranean miniature donkeys with an age of 5 ± 1 years, a weight of 100 ± 2 kg and a height at the withers of 0.8 ± 0.06 m (mean ± standard deviation) were used in experimental, crossover (Latin square), randomized, and blinded study. Animals were assigned to five treatment groups including lidocaine alone ...
Effective Penetration of a Liposomal Formulation of Bleomycin through Ex-Vivo Skin Explants from Two Different Species. Bleomycin is a chemotherapy agent that, when administered systemically, can cause severe pulmonary toxicity. Bleosome is a novel formulation of bleomycin encapsulated in ultra-deformable (UD) liposomes that may be applicable as a topical chemotherapy for diseases such as non-melanoma skin cancer. To date, the ability of Bleosome to effectively penetrate through the skin has not been evaluated. In this study, we investigated the ability of Bleosome to penetrate through ex vivo skin explants from dogs and horses. We visualized the penetration of UD liposomes through the skin by transmission elec...
The disposition of trimethoprim and sulfadiazine in neonatal foals after intravenous administration. Septicaemia in the neonatal foal is caused by both Gram positive and Gram negative bacteria. The life-threatening nature of this condition requires treatment to be initiated with broad spectrum antimicrobial drugs pending antimicrobial susceptibility testing. Potentiated sulphonamides, for example, trimethoprim combined with sulfadiazine, could be clinically relevant options but their pharmacokinetics in the neonatal foal are unknown. To describe the plasma disposition of trimethoprim and sulfadiazine in neonatal foals and to relate the results to patterns in the minimum inhibitory concentrati...