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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.
Plasma and synovial fluid pharmacokinetics of a single intravenous dose of meropenem in adult horses. The objective of this study was to determine the pharmacokinetics of meropenem in horses after intravenous (IV) administration. A single IV dose of meropenem was administered to six adult horses at 10 mg/kg. Plasma and synovial fluid samples were collected for 6 hr following administration. Meropenem concentrations were determined by bioassay. Plasma and synovial fluid data were analyzed by compartmental and noncompartmental pharmacokinetic methods. Mean ± SD values for elimination half-life, volume of distribution at steady-state, and clearance after IV administration for plasma samples ...
Evaluation of the sedative effects and pharmacokinetics of detomidine gel administered intravaginally to horses. To determine the sedative effects and pharmacokinetic profile of detomidine when administered intravaginally as a gel formulation to horses. Methods: Randomized, crossover, masked experimental design. Methods: A group of six healthy adult mares (494 ± 56 kg). Methods: Mares were studied on two occasions and were administered either detomidine hydrochloride (10 μg kg) intravenously (treatment IV) or detomidine gel (40 μg kg) intravaginally (treatment IVG), separated by 1 week. Sedation, ataxia, muzzle-floor distance and heart rate (HR) were evaluated every 15 minutes for 240 minutes. Venous ...
Pharmacokinetics of single doses of maropitant citrate in adult horses. The neurokinin-1 (NK) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood and likely under-recognized in horses. Use of NK-1 receptor antagonists in horses has not been reported. The purpose of this study was to determine the pharmacokinetic profile of maropitant in seven adult horses after single intravenous (IV; 1 mg/kg) and intragastric (IG; 2 mg/kg) doses. A randomized, crossover design was performed. Serial blood samples were collected after dosing; maropitant concentrations were measured using LC-MS/MS. Pharmacokinetic pa...
Anti-Alzheimer’s multitarget-directed ligands with serotonin 5-HT6 antagonist, butyrylcholinesterase inhibitory, and antioxidant activity. Serotonin 5-HT receptors, butyrylcholinesterase (BuChE) and oxidative stress are related to the pathophysiology of Alzheimer's disease. Inhibition of BuChE provides symptomatic treatment of the disease and the same effect was demonstrated for 5-HT antagonists in clinical trials. Oxidative stress is regarded as a major and primary factor contributing to the development of Alzheimer's disease; therefore, antioxidant agents may provide a disease-modifying effect. Combining BuChE inhibition, 5-HT antagonism, and antioxidant properties may result in multitarget-directed ligands providing cognitio...
Pharmacokinetics of chloramphenicol base in horses and comparison to compounded formulations. Chloramphenicol is commonly used in horses; however, there are no studies evaluating the pharmacokinetics of veterinary canine-approved tablets. Studies using different formulations and earlier analytical techniques led to concerns over low bioavailability in horses. Safety concerns about human health have led many veterinarians to prescribe compounded formulations that are already in suspension or paste form. The objective of this study was to evaluate the pharmacokinetics of approved chloramphenicol tablets in horses, along with compounded preparations. The hypothesis was that chloramphenico...
Evaluation of phenylephrine and exercise with or without trocarization for treatment of suspected nephrosplenic entrapment in horses. To report the outcomes of horses with suspected nephrosplenic entrapment (NSE) of the large colon treated by IV phenylephrine administration and exercise with and without trocarization (ie, medical management). Retrospective, observational study. 134 horses. Electronic medical records were searched to identify horses that underwent medical management for suspected NSE at a veterinary teaching hospital between 1995 and 2014. Demographic information, physical and ultrasonographic examination findings, treatment information (including the number of times the treatment was performed and patien...
Effect of fentanyl on thermal and mechanical nociceptive thresholds in horses and estimation of anti-nociceptive plasma concentration. There are few investigations relating anti-nociception to plasma concentrations of fentanyl in horses. The study objective was to evaluate analgesic efficacy and duration in horses and determine the minimum anti-nociceptive plasma concentrations. Eight horses were treated with saline (P) and fentanyl (F=2.5μg/kg; F=5μg/kg; F=10μg/kg) given IV over 5min, with a wash-out period of 10 days. To evaluate thermal (°C) and mechanical (N) nociceptive threshold single stimulations were applied prior to (baseline) and 10, 30, 60, 90, 120, 180, 240, 300, 360, 420, 540min and 22.5h after treatment. Pl...
Prevalence of Strongylus vulgaris in horses after ten years of prescription usage of anthelmintics in Sweden. Strongylus vulgaris is considered the most pathogenic nematode parasite of the horse. Frequent deworming programs since the 1970s have reduced the prevalence of S. vulgaris to low levels, but to the price of widespread benzimidazole resistance in the small strongyles (cyathostominae) and ivermectin resistance especially in the equine roundworm Parascaris spp. To slow down the progression of anthelmintic resistance in Sweden, horse anthelmintics were made prescription only medicine in 2007 and selective therapy principles were introduced. This means that only individuals with high egg excretion...
Paper spray high-resolution accurate mass spectrometry for quantitation of voriconazole in equine tears. Paper spray high-resolution accurate mass spectrometry is a fast and versatile analysis method. This ambient ionization technique enables the quantitation of xenobiotics in complex biological matrices without chromatography or conventional sample extraction. The simplicity, rapidity, and affordability of the paper spray mass spectrometry (PS-MS) method make the technique especially attractive for clinical investigations where fast and affordable sample analysis is crucial. A new PS-MS method for the quantitation of voriconazole in equine tears was developed and validated. For a concentration r...
In silico and in vitro analysis of genetic variants of the equine CYP3A94, CYP3A95 and CYP3A97 isoenzymes. Cytochrome P450 enzymes (CYPs) of the equine CYP3A subfamily are predominantly involved in drug metabolism. In this study, genetic variants of the equine CYP3A94, CYP3A95, and CYP3A97 were identified and characterized using in silico modeling and in vitro enzyme kinetics. The genomes of 81 horses were sequenced to obtain the genetic variants. Structural CYP modifications of the most frequent variants were analyzed in silico using the 3D-structures predicted by homology modeling. Enzyme kinetic analyses were performed using testosterone as substrate. Twenty genetic variants were found including...
The Effects of Xylazine Administration on Peripheral Leukocyte Values in Thoroughbred Horses. This study was conducted to determine whether xylazine administration is associated with clinically significant changes on leukocyte numbers in horses, as has been previously reported in other species. The study was designed to detect 20% changes in primary endpoint leukocyte parameters with 85% statistical power. No clinically significant changes in leukocyte numbers meeting the requirements of the statistical analysis were detected; no consistent changes capable of confounding a clinical diagnosis or treatment were detected. No gross changes in secondary endpoints including erythrocyte and p...
Pharmacokinetics and competitive pharmacodynamics of ADP-induced platelet activation after oral administration of clopidogrel to horses. To determine pharmacokinetics and pharmacodynamics after oral administration of a single dose of clopidogrel to horses. Methods: 6 healthy adult horses. Methods: Blood samples were collected before and at various times up to 24 hours after oral administration of clopidogrel (2 mg/kg). Reactivity of platelets from each blood sample was determined by optical aggregometry and phosphorylation of vasodilator-stimulated phosphoprotein (VASP). Concentrations of clopidogrel and the clopidogrel active metabolite derivative (CAMD) were measured in each blood sample by use of liquid chromatography-tandem...
A kinematic comparison of the locomotor pattern of horses sedated with detomidine alone and in combination with low doses of butorphanol. Chemical restraint is often used to perform diagnostic and minor surgical procedures; α2 -adrenoceptor agonists are the most commonly used drugs; however, the combination with an opiate can induce a profound sedation. There is a lack of kinematic studies examining the effects of the combination of these drugs on locomotor patterns. Objective: The objective of the study was to evaluate the duration of the effects of sedation with detomidine and detomidine combined with a low dose of butorphanol on the movement patterns of horses. Methods: The study was a controlled, randomised, blinded and cro...
Pilot study to quantify the time to clear dexamethasone from plasma and urine of adult horses following a single nebulisation. To quantify the time to clear dexamethasone from plasma and urine of horses following a single nebulisation. Methods: Experimental using six Standardbred mares. Methods: Dexamethasone sodium phosphate (0.04 mg/kg) diluted in 0.9% sodium chloride was administered as an aerosol using a Flexineb E2® nebuliser. Blood samples (0, 2, 4, 6, 8, 10, 12, 24, 32, 48, 72 and 96 h) and urine samples (0, 1, 4, 8, 24, 32, 48, 72 and 96 h) were collected for analysis using liquid chromatography mass spectrometry. Results: Maximum plasma concentrations (t ) were reached by the earliest detection point (...
Pharmacokinetics and safety of repeated oral dosing of acetaminophen in adult horses. There are no published studies on the pharmacokinetics of acetaminophen at the dosage used clinically (20 mg/kg), nor has the safety of multiple doses in horses been investigated. Objective: Define the pharmacokinetic parameters of oral acetaminophen at 20 mg/kg in adult horses as a single dose, and twice daily for 14 days to assess the safety of multiple dosing. Methods: Pharmacokinetic study, multiple dose safety study. Methods: Eight healthy Thoroughbred geldings were given acetaminophen (20 mg/kg; 500 mg tablets) orally as a single dose followed by doses every 12 h for 14 days. Seri...
Simultaneous quantitation of 9 anabolic and natural steroidal hormones in equine urine by UHPLC-MS/MS triple quadrupole. A new fast and easy analytical procedure for the simultaneous detection and quantification of 9 anabolic steroids (deslorelin, dexamethasone sodium phosphate, prednisolone, methylprednisolone, stanozolol, boldenone, nandrolone, dexamethasone isonicotinate and altrenogest) in horse urine for doping control have been developed by using the ultra-high-performance liquid chromatography coupled with tandem mass spectrometry technique (UHPLC-MS/MS). A total amount of 400 μl of sample was evaporated, restored and injected in the UHPLC-MS/MS. The proposed method was fully validated showing a recove...
Antimicrobial dosing for common equine drugs: a content review and practical advice for veterinarians in Australia. Appropriate dosing with antimicrobial agents is critical for effective treatment and to prevent the development of antimicrobial resistance. Methods: A review was undertaken of equine journal articles (Equine Veterinary Journal, Equine Veterinary Education, Australian Veterinary Journal, Australian Equine Veterinarian, Journal of Veterinary Internal Medicine and Journal of Equine Veterinary Science) between January 2015 and August 2018. Those with dosing regimens for procaine penicillin G, gentamicin or trimethoprim-sulfonamide in adult horses were examined and evaluated. Pharmacokinetics and ...
Safety and efficacy of three trypanocides in confirmed field cases of trypanosomiasis in working equines in The Gambia: a prospective, randomised, non-inferiority trial. Globally, working equines have a continued and growing socioeconomic role in supporting the livelihoods of between 300-600 million people in low income countries which is rarely recognised at a national or international level. Infectious diseases have significant impact on welfare and productivity in this population and equine trypanosomiasis is a priority disease due to its severity and prevalence. Strategies are required to improve the prevention, diagnosis, management and treatment of trypanosomiasis in equines and more data are required on the efficacy and safety of current trypanocidal dr...
Potent inhibitors of equine steroid isomerase EcaGST A3-3. Equine glutathione transferase A3-3 (EcaGST A3-3) belongs to the superfamily of detoxication enzymes found in all higher organisms. However, it is also the most efficient steroid double-bond isomerase known in mammals. Equus ferus caballus shares the steroidogenic pathway with Homo sapiens, which makes the horse a suitable animal model for investigations of human steroidogenesis. Inhibition of the enzyme has potential for treatment of steroid-hormone-dependent disorders. Screening of a library of FDA-approved drugs identified 16 out of 1040 compounds, which at 10 μM concentration afforded at ...
Pharmacokinetics, metabolism and excretion of celecoxib, a selective cyclooxygenase-2 inhibitor, in horses. Celecoxib, a nonsteroidal anti-inflammatory drug, is frequently used to treat arthritis in humans with minimal gastrointestinal side effect compared to traditional NSAIDs. The primary aim of this study was to determine the pharmacokinetic profile of celecoxib-a selective cyclooxygenase-2 (COX-2) inhibitor in horses. Six horses were administered a single oral dose of celecoxib at 2 mg/kg (body weight). After oral dosing, the drug reached a maximum concentration (mean ± SD) in blood of 1,088 ± 324 ng/ml in 4.58 hr. The elimination half-life was 13.60 ± 3.18 hr, and the area under th...
Pharmacokinetics of regional limb perfusion using a combination of amikacin and penicillin in standing horses. The objectives of this study were to evaluate the compatibility and the pharmacokinetic properties of combined amikacin and penicillin administration by intravenous regional limb perfusion (IVRLP) in horses. A tourniquet was applied proximal to the carpus of 7 clinically healthy adult horses and 2 g of amikacin and 10 × 10 IU of penicillin (100 mL total volume) were sequentially injected into the cephalic vein just distal to the tourniquet. Synovial samples were collected from the joint at several times after injection. All samples were analyzed for amikacin and penicillin concentration. The ...
Effects of vatinoxan on cardiorespiratory function and gastrointestinal motility during constant-rate medetomidine infusion in standing horses. Medetomidine suppresses cardiovascular function and reduces gastrointestinal motility in horses mainly through peripheral α -adrenoceptors. Vatinoxan, a peripheral α -antagonist, has been shown experimentally to alleviate the adverse effects of some α -agonists in horses. However, vatinoxan has not been investigated during constant-rate infusion (CRI) of medetomidine in standing horses. Objective: To evaluate effects of vatinoxan on cardiovascular function, gastrointestinal motility and on sedation level during CRI of medetomidine. Methods: Experimental, randomised, blinded, cross-over stud...
Viability of Equine Chondrocytes After Exposure to Mepivacaine and Ropivacaine In Vitro. Chondrocyte health is altered when exposed to local anesthetics, raising concerns as to the long-term effects of local anesthetics intra-articularly for diagnosis and analgesia. To investigate the drug with the lowest toxic potential, the effect of ropivacaine and mepivacaine on chondrocytes was evaluated. Articular cartilage from normal metacarpophalangeal joints of five equine cadaver specimens was used to establish chondrocyte cultures. Following seven days, chondrocytes were exposed to standard culture medium (DMEM), ropivacaine 7.5 mg/ml (ROP7.5), ropivacaine 10 mg/ml (ROP10), mepivacaine...
Modulation of TNF-α, IL-1Ra and IFN-γ in equine whole blood culture by glucocorticoids. Glucocorticoids are important drugs in the treatment of many inflammatory, autoimmune and allergic diseases in humans and animals. We investigated the effects of hydrocortisone and dexamethasone on TNF-α, IL-1Ra and INF-γ release in stimulated whole blood cell culture from healthy horses. Whole blood cell cultures proved to be useful for the characterization of the anti-inflammatory properties of new drugs. Diluted equine whole blood was exposed to lipopolysaccharide (LPS) and PCPwL (a cocktail consisting of phythemagglutinin E, concanavalin A, pokeweed mitogen and lipopolysaccharide) in the...
Pharmacological Regulation in the USA and Pharmacokinetics Parameters of Firocoxib, a Highly Selective Cox-2, by Pain Management in Horses. The objective of the study was to conduct a review of the pharmacological regulation and pharmacokinetic parameters of firocoxib when administered orally or intravenously in horses. A search for literature was done in SCOPUS and PubMed for studies that had to evaluate the pharmacological regulation as well as the pharmacokinetic parameters of firocoxib when administered in horses. The nonsteroidal anti-inflammatory drugs have analgesic, anti-inflammatory, antipyretics, and antiendotoxic effects. The newly developed is selective to COX2 characterized by less adverse effects in veterinary patien...
Detection of ESAs in equine urine and blood by SAR-PAGE. Erythropoiesis-stimulating agents (ESAs) have been used in horses for doping purposes to increase the performance of these animals in endurance sports. Currently, enzyme-linked immunosorbent assay (ELISA) and mass spectrometry methods are used to detect ESA abuse in equines. However, the sarcosyl polyacrylamide gel-electrophoresis (SAR-PAGE) technique could also be used, since its application in human doping control is well established and has proven to be more sensitive. In this work, the SAR-PAGE method was used to detect recombinant human erythropoietin (rHuEPO), novel erythropoiesis stimul...
Effects of dofetilide and ranolazine on atrial fibrillatory rate in a horse model of acutely induced atrial fibrillation. The atrial fibrillatory rate is a potential biomarker in the study of antiarrhythmic drug effects on atrial fibrillation (AF). The purpose of this study was to evaluate whether dose-dependent changes in the atrial fibrillatory rate can be monitored on surface electrocardiography (ECG) following treatment with dofetilide, ranolazine, and a combination of the two in an acute model of AF in horses. Eight horses were subjected to pacing-induced AF on 4 separate days. Saline (control), dofetilide, ranolazine, or a combination of dofetilide and ranolazine was administered in four incremental doses. ...
Compounds commonly used in equine medicine inhibits the voltage-gated potassium channel Kv11.1. The voltage-gated K-channel K11.1 has a central role in cardiac repolarization. Blockage of K11.1 has been linked to severe cardiovascular side effects, such as acquired long QT syndrome (aLQTS), torsade de pointes arrhythmia and sudden cardiac death (SCD). K11.1 is susceptible to unspecific drug interactions due to the presence of two aromatic amino acids residing in the inner vestibule of the pore. These aromatic residues are also present in the equine orthologue of K11.1. This suggests that equine K11.1 may also be prone to high-affinity block by a range of different chemical entities, whic...
An immuno polymerase chain reaction screen for the detection of CJC-1295 and other growth-hormone-releasing hormone analogs in equine plasma. CJC-1295 is a 30 amino acid peptide-based drug that stimulates the release of growth hormone (GH) from the pituitary gland. It is unique among performance-enhancing peptides due to the presence of a reactive maleimidopropionic acid group that covalently links the peptide to free thiols on the surface of plasma proteins. Once conjugated, CJC-1295 remains active in the bloodstream for significantly longer than non-conjugated peptide-based drugs that are rapidly excreted. Conjugation of CJC-1295 to plasma proteins prevents its detection by top-down mass-spectrometry-based peptide screening protoc...
Sedative and antinociceptive effects of different detomidine constant rate infusions, with or without methadone in standing horses. Standing surgery avoids the risks of general anaesthesia in horses. Objective: To assess sedation, antinociception and gastrointestinal motility in standing horses after a detomidine loading dose and 2-h constant rate intravenous (i.v.) infusion, with or without methadone. Methods: Blinded, randomised, crossover with seven healthy adult cross-bred horses, three geldings and four females (404 ± 22 kg). Methods: Five i.v. treatments were administered to all horses with 1-week washout period: saline (SAL), detomidine low (2.5 μg/kg bwt + 6.25 μg/kg bwt/h) (DL) and high doses (5 μg/kg ...
