Topic:Pharmaceuticals
Pharmaceuticals in equine medicine encompass a wide range of drugs and therapeutic agents used to treat various conditions in horses. These substances include analgesics, anti-inflammatories, antibiotics, sedatives, and anthelmintics, among others. Each class of pharmaceuticals is designed to address specific health issues, such as pain management, infection control, or parasitic infestations. The pharmacokinetics and pharmacodynamics of these drugs can vary significantly between horses and other species, necessitating careful consideration of dosage and administration methods. This page compiles peer-reviewed research studies and scholarly articles that explore the development, efficacy, safety, and regulatory aspects of pharmaceuticals used in equine healthcare.
Determination of zearalenone and its metabolites in urine, plasma and faeces of horses by HPLC-APCI-MS. The paper describes a method for the sensitive and selective determination of zearalenone and its metabolites in urine, plasma and faeces of horses by high performance liquid chromatography and atmospheric pressure chemical ionisation (APCI) mass spectrometry (MS). While only one step sample clean-up by an immunoaffinity column (IAC) was sufficient for plasma samples, urine and faeces samples had to be prepared by a combination of a solid-phase extraction (SPE) and an immunoaffinity column. The method allows the simultaneous determination of zearalenone and all of its metabolites; alpha-zearal...
Comprehensive screening of anabolic steroids, corticosteroids, and acidic drugs in horse urine by solid-phase extraction and liquid chromatography-mass spectrometry. This paper reports two highly efficient liquid chromatography-mass spectrometry (LC-MS) methods for the screening of anabolic steroids, corticosteroids, and acidic drugs for the purpose of doping control in equine sports. Sample extraction was performed using a mixed-mode C8-SCX solid-phase extraction (SPE) cartridge. The first eluted fraction (acidic/neutral fraction) was base-washed and the resulting organic extract was used for the screening of anabolic steroids and corticosteroids by LC-MS using multiple reaction monitoring (MRM) in the positive electrospray ionisation (ESI) mode. The rema...
Modulation of leptin, insulin, and growth hormone in obese pony mares under chronic nutritional restriction and supplementation with ractopamine hydrochloride. Horses fed beyond their nutritional requirement and that are physically inactive will develop obesity, which is often accompanied by insulin resistance and heightened risk of laminitis. The use of pharmacologic agents in combination with nutritional restriction may promote weight loss in obese horses unable to exercise because of laminitic pain. This study shows that reducing feed intake of brome grass hay to 75% of ad libitum intake in obese pony mares reduces body weight without induced exercise. Additional supplementation of ractopamine hydrochloride for 6 weeks resulted in a tendency for i...
Detection of altrenogest and its metabolites in post administration horse urine using liquid chromatography tandem mass spectrometry–increased sensitivity by chemical derivatisation of the glucuronic acid conjugate. Altrenogest (17alpha-allyl-17beta-hydroxyestra-4,9,11-trien-3-one) is a steroid used for the control of estrus in horses. This drug can potentially be abused in racehorses as the occurrence of estrus can alter their performance. This work describes an analytical method based on liquid chromatography-tandem mass spectrometry for the detection of altrenogest in horse urine down to a concentration of 13 pg/mL (0.042 nM). Furthermore, the qualitative aspect of metabolism of altrenogest in the horse has been studied. The main transformations that were found for this species were conjugation with gl...
The role of protective lead clothing in reducing radiation exposure rates to personnel during equine bone scintigraphy. Bone scintigraphy is often used in horses because of its sensitivity and noninvasive nature. A 99mTc labeled radiopharmaceutical is injected at a dose of between 5.7 and 7.3GBq. Images are acquired immediately postinjection and 2-4h post. People are often in the room with the horse during the acquisition process. Objectives of this study were to (a) document the radiation exposure rates at different distances from various sites of the horse at varying times post injection and (b) study the usefulness of wearing lead aprons to reduce exposure rates to personnel. Radiation exposure rates were me...
The use of nutraceuticals for osteoarthritis in horses. In horses, lameness is often attributable to some degree of osteoarthritis (OA), a complex disease process that is highlighted by eventual degradation of articular cartilage. Conventional therapies for OA in horses are designed to relieve pain and discomfort and often include pharmacologic intervention with nonsteroidal anti-inflammatory drugs or intra-articular steroids. Oral administration of nutraceutical products to the horse is common and easy and is perceived to be a benign treatment for OA in horses. The main goal for use of nutraceuticals is to use them in OA cases to attempt to lower ...
In vivo biotransformation of metoprolol in the horse and on-column esterification of the aminocarboxylic acid metabolite by alcohols during solid phase extraction using mixed mode columns. The in vivo biotransformation of metoprolol tartrate in the thoroughbred racehorse was studied after administration of a single oral dose. Metoprolol and its basic and bifunctional phase I metabolites were isolated from urine and plasma using mixed mode solid phase extraction (SPE) cartridges. The isolates were derivatised as trimethylsilyl ethers and analysed by capillary column gas chromatography--positive ion electron ionisation and ammonia chemical ionisation mass spectrometry. Metabolism was primarily confined to the oxidative transformations of the p-(2-methoxy)ethyl substituent. Metopro...
[Suspected adverse drug reactions in 2004]. We received 62 reports of suspected adverse events (SARs) for the year 2004. Their number and repartition according to affected animals and active substances were comparable with the previous year. The distributors or manufacturers submitted most of the declarations, but the proportion submitted by practicing veterinarians is slowly growing. 72% of the declarations dealt with adverse reactions in small animals (cats and dogs), followed by cattle and horses. Antiparasitics, anti-inflammatory drugs and immunologicals were the most frequently mentioned therapeutic classes, which are listed here a...
Analysis of anabolic steroids in the horse: development of a generic ELISA for the screening of 17alpha-alkyl anabolic steroid metabolites. Due to the potential for misuse of a wide range of anabolic steroids in horse racing, a screening test to detect multiple compounds, via a common class of metabolites, would be a valuable forensic tool. An enzyme-linked immunosorbent assay (ELISA) has been developed to detect 17alpha-alkyl anabolic steroid metabolites in equine urine. 16beta-Hydroxymestanolone (16beta,17beta-dihydroxy-17alpha-methyl-5alpha-androstan-3-one) was synthesised in six steps from commercially available epiandrosterone (3beta-hydroxy-5alpha-androstan-17-one). Polyclonal antibodies were raised in sheep, employing mesta...
Control of endoparasites in horses with a gel containing moxidectin and praziquantel. A gel formulation containing moxidectin (20 g/kg) and praziquantel (125 g/kg) reduced the geometric mean faecal strongyle egg count in horses to below 100 eggs per gram of faeces (epg) for at least 12 weeks despite their being exposed continuously to reinfection from pasture grazed by treated and untreated horses. The geometric mean egg count of horses treated with a proprietary paste containing abamectin (3.7 g/kg) and praziquantel (46.2 g/kg) increased steadily from six weeks after the treatment, peaking at over 820 epg after 12 weeks. Relative to the efficacy of the abamectin/praziquantel t...
Influence of vedaprofen (Quadrisol) on quality and freezability of stallion semen. The objective of this study was to evaluate the effect of the non-steroidal anti-inflammatory drug (NSAID) vedaprofen (Quadrisol) on quality and freezability of stallion semen. Experiments were performed using 22 Franches Montagnes stallions from the National Stud in Avenches (Switzerland) randomly divided into a control and test group. Vedaprofen was given orally to all stallions of the test group at the recommended therapeutic dose (initial dose of 2mg/kg followed by 1mg/kg body weight every 12h) for 14 days. Control animals received the same amount of carrier substance. During treatment, bl...
Screening of anabolic steroids in horse urine by liquid chromatography-tandem mass spectrometry. Anabolic steroids have the capability of improving athletic performance and are banned substances in the Olympic games as well as in horseracing and equestrian competitions. The control of their abuse in racehorses is traditionally performed by detecting the presence of anabolic steroids and/or their metabolite(s) in urine samples using gas chromatography-mass spectrometry (GC-MS). However, this approach usually requires tedious sample processing and chemical derivatisation steps and could be very insensitive in detecting certain steroids. This paper describes a high performance liquid chromat...
The detection of modafinil and its major metabolite in equine urine by liquid chromatography/mass spectrometry. A method has been developed for the detection of modafinil and its major metabolite, modafinil acid, in equine urine by solid-phase extraction and positive ion electrospray ionisation liquid chromatography/mass spectrometry. The method has been applied to the analysis of equine urine samples obtained after the oral administration of modafinil. Modafinil acid was the major component in the urine, and was detected up to 4 days post-administration. Unchanged modafinil was present at substantially lower concentrations, and was detected for only 24 hours.
Development of an electrospray ionization mass spectrometric method for the quantification of theophylline in horse serum. A rapid and selective method has been developed for the determination of theophylline in horse serum by LC-ESI/MS/MS. The analytical method includes a protein precipitation extraction for sample preparation, liquid chromatography separation technique and ionspray tandem mass spectrometry. The drug was extracted from serum using a protein precipitation with acetonitrile and the supernatants were analyzed using an LC-ESI/MS/MS instrument. The chromatography was performed using a 50 x 2.1 mm C(8) analytical column and an isocratic mobile phase composes of 60:40 acetonitrile-0.5% formic acid in wa...
Pharmacokinetics of dexamethasone with pharmacokinetic/pharmacodynamic model of the effect of dexamethasone on endogenous hydrocortisone and cortisone in the horse. A compartmental model was used to describe the pharmacokinetics of dexamethasone (DXM) and changes in the plasma concentration of endogenous cortisone (COR) and hydrocortisone (HYD) following intravenous (i.v.) administration of DXM (0.05 mg/kg) in horses. Quantification of DXM, COR and HYD in equine plasma was achieved using liquid chromatography interfaced with triple spray quadrupole quantum tandem mass spectrometry (LC/TSQ-MS/MS). The median alpha (t(1/2alpha)), beta (t(1/2beta)), and gamma (t(1/2gamma)) half-lives were 0.33, 2.2, and 10.7 h respectively. The area under the DXM plasma conc...
Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion. Flurbirpofen (FBP), a member of the 2-aryl propionate nonsteroidal anti-inflammatory drug class, has potent anti-inflammatory and analgesic properties. The commercial preparation is a racemic mixture of the R(-) and S(+) enantiomers of FBP. In this study, R(-) and S(+) FBP were used to investigate the metabolic chiral inversion. Each enantiomer was administered separately (0.25 mg/kg) and in a racemic mixture (0.5 mg/kg) intravenously to horses. Plasma and synovial concentration of each enantiomer was determined and the disposition of each was analyzed. After intravenous administration of R(-)...
Limitations to veterinary applications of new technologies in treatment and diagnostics. Technology promises to improve the lifestyle and life quality of humankind. As a rule, wherever human medicine goes, veterinary medicine is sure to follow. Nevertheless, the promise of technologic advances does not shine as bright for veterinarians as for human physicians. This trend is echoed in the business of animal health as pharmaceutic company after pharmaceutic company spins off or otherwise eliminates their animal health division. Instead, a small group of strictly animal health-oriented companies compete for the animal health dollar, promising that fewer and fewer expensive technologi...
Pharmacodynamics and pharmacokinetics of nonsteroidal anti-inflammatory drugs in species of veterinary interest. This review summarises selected aspects of the pharmacokinetics (PK) and pharmacodynamics (PD) of nonsteroidal anti-inflammatory drugs (NSAIDs). It is not intended to be comprehensive, in that it covers neither minor species nor several important aspects of NSAID PD. The limited objective of the review is to summarise those aspects of NSAID PK and PD, which are important to an understanding of PK-PD integration and PK-PD modelling (the subject of the next review in this issue). The general features of NSAID PK are: usually good bioavailability from oral, intramuscular and subcutaneous administ...
Pharmacokinetics of meloxicam in plasma and urine of horses. To determine pharmacokinetic parameters for meloxicam, a nonsteroidal anti-inflammatory drug, in horses. Methods: 8 healthy horses. Methods: In the first phase of the study, horses were administered meloxicam once in accordance with a 2 x 2 crossover design (IV or PO drug administration; horses fed or not fed). The second phase used a multiple-dose regimen (daily oral administration of meloxicam for 14 days), with meloxicam administered at the recommended dosage (0.6 mg/kg). Plasma and urine concentrations of meloxicam were measured by use of validated methods with a limit of quantification of...
Direct detection of boldenone sulfate and glucuronide conjugates in horse urine by ion trap liquid chromatography-mass spectrometry. A study of the equine phase II metabolism of the anabolic agent boldenone is reported. Boldenone sulfate, boldenone glucuronide and their C17-epimers were synthesised as reference standards in our lab and a method was developed for their detection in a horse urine matrix. Solid phase extraction was used to purify the analytes, which were then detected by ion trap LC/MS. Negative and positive ionisation mode MS(2) were used for the detection of sulfate and glucuronide conjugates, respectively. Boldenone sulfate and 17-epiboldenone glucuronide were detected as the major and minor phase II metabo...
Development of a method for the detection and confirmation of the alpha-2 agonist amitraz and its major metabolite in horse urine. Amitraz (N'-(2,4-dimethylphenyl)-N-[[(2,4-dimethylphenyl)imino]methyl]-N-methyl-methanimidamide) is an alpha-2 adrenergic agonist used in veterinary medicine primarily as a scabicide- or acaricide-type insecticide. As an alpha-2 adrenergic agonist, it also has sedative/tranquilizing properties and is, therefore, listed as an Association of Racing Commissioners International Class 3 Foreign Substance, indicating its potential to influence the outcome of horse races. We identified the principal equine metabolite of amitraz as N-2,4-dimethylphenyl-N'-methylformamidine by electrospray ionization(+...
Pharmacokinetics, stability, and retrospective analysis of use of an oral gel formulation of the bovine injectable enrofloxacin in horses. In many cases of equine infectious disease, long-term administration of antimicrobial drugs is required. Oral agents are preferred because of the relative ease of administration compared with other routes. Enrofloxacin has been shown to be effective against a variety of equine pathogens, but oral administration of this drug has proved difficult in horses. An oral gel formulation made from the injectable cattle product produces blood levels sufficient to resolve infections caused by a variety of common equine pathogens.