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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.
Evidence of boldenone, nandrolone, 5(10)-estrene-3β-17α-diol and 4-estrene-3,17-dione as minor metabolites of testosterone in equine. The detection of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione in a urine sample collected from a gelding having been treated with testosterone (500 mg 'Testosterone Suspension 100', single dose, injected intramuscularly) in 2009 led the authors' laboratory to suspect that these 'testicular' steroids could be minor metabolites of testosterone in geldings. Administration trials on six castrated horses with Testosterone Suspension 100 confirmed that low levels of boldenone, nandrolone, 5(10)-estrene-3β,17α-diol, and 4-estrene-3,17-dione could indeed be detected ...
Doping control study of AICAR in post-race urine and plasma samples from horses. Acadesine, 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, commonly known as AICAR, is a naturally occurring adenosine monophosphate-activated protein kinase (AMPK) activator in many mammals, including humans and horses. AICAR has attracted considerable attention recently in the field of doping control because of a study showing the enhancement of endurance performance in unexercised or untrained mice, resulting in the term 'exercise pill'. Its use has been classified as gene doping by the World Anti-Doping Agency (WADA), and since it is endogenous, it may only be possible to control del...
[New drugs for horses and production animals in 2016]. In 2016, only one newly developed active pharmaceutical ingredient for horses and food-producing animals was released on the German market for veterinary drug products. The immunomodulator Pegbovigrastim is now available as an injection solution for cattle (Imrestor). Four established veterinary active pharmaceutical ingredients are available for further species: the ectoparasitic Amitraz (Apitraz) from the triazapentadiene group was additionally authorized for honeybees, the expectorant Bromhexine (Exflow Vet) for chickens, turkeys and ducks and the macrolide antibiotic Gamithromycin (Zactran...
Pharmacokinetics of firocoxib after intravenous administration of multiple consecutive doses in neonatal foals. The purpose of this study was to determine the pharmacokinetic profile of intravenous firocoxib in neonatal foals. Six healthy foals were administered 0.09Â mg/kg firocoxib intravenously once a day for 7Â days. Blood was collected for plasma firocoxib analysis using high-performance liquid chromatography with fluorescence detection at times 0 (day 1 of study only) and 0.08, 0.25, 1, 2, 4, 6, 8, 16 and 24Â hr on dose numbers 1, 5 and 7. Blood was also collected immediately prior to doses 3, 4, 5 and 7. Final samples were collected at 36, 48, 72 and 96Â hr following the final dose. Noncompartmen...
Challenges in detecting substances for equine anti-doping. The artificial increase of the physical capability of horses using drugs is well known in racing and other equine sports. Both illicit and therapeutic substances are regarded as prohibited substances in competition in most countries. Some countries make distinctions for a few, specific drugs which are, however, allowed for use in other countries. The primary objective in the case of doping control is the detection of any trace of drug exposure, either parent drug or any of its metabolites, using the most powerful analytical methods which are generally based on chromatographic/mass spectrometri...
In vitro phase I metabolism of selective estrogen receptor modulators in horse using ultra-high performance liquid chromatography-high resolution mass spectrometry. Selective estrogen receptor modulators (SERMs) are chemicals that possess the anti-oestrogenic activities that are banned 'in' and 'out' of competition by the World Anti-Doping Agency (WADA) in human sports, and by the International Federation of Horseracing Authorities (IFHA) in horseracing. SERMs can be used as performance-enhancing drugs to boost the level of androgens or to compensate for the adverse effects as a result of extensive use of androgenic anabolic steroids (AASs). SERMs have indeed been abused in human sports; hence, a similar threat can be envisaged in horseracing. Numerous an...
Screening of over 100 drugs in horse urine using automated on-line solid-phase extraction coupled to liquid chromatography-high resolution mass spectrometry for doping control. A fast method for the direct analysis of enzyme-hydrolysed horse urine using an automated on-line solid-phase extraction (SPE) coupled to a liquid-chromatography/high resolution mass spectrometer was developed. Over 100 drugs of diverse drug classes could be simultaneously detected in horse urine at sub to low parts per billion levels. Urine sample was first hydrolysed by β-glucuronidase to release conjugated drugs, followed by centrifugal filtration. The filtrate (1mL) was directly injected into an on-line SPE system consisting of a pre-column filter and a SPE cartridge column for the separa...
Therapeutics for Equine Endocrine Disorders. Equine endocrine disease is commonly encountered by equine practitioners. Pituitary pars intermedia dysfunction (PPID) and equine metabolic syndrome (EMS) predominate. The most logical therapeutic approach in PPID uses dopamine agonists; pergolide mesylate is the most common. Bromocryptine and cabergoline are alternative drugs with similar actions. Drugs from other classes have a poor evidence basis, although cyproheptadine and trilostane might be considered. EMS requires management changes as the primary approach; reasonable justification for use of drugs such as levothyroxine and metformin m...
Influence of respiratory tract disease and mode of inhalation on detectability of budesonide in equine urine and plasma. OBJECTIVE To evaluate the influence of respiratory tract disease (ie, recurrent airway obstruction [RAO]) and mode of inhalation on detectability of inhaled budesonide in equine plasma and urine samples. ANIMALS 16 horses (8 healthy control horses and 8 horses affected by RAO, as determined by results of clinical examination, blood gas analysis, bronchoscopy, and cytologic examination of bronchoalveolar lavage fluid). PROCEDURES 4 horses of each group inhaled budesonide (3 μg/kg) twice daily for 10 days while at rest, and the remaining 4 horses of each group inhaled budesonide during lunging ...
The Analysis of Phenylbutazone and Its Active Metabolite, Oxyphenbutazone, in Equine Tissues (Muscle, Kidney, and Liver), Urine, and Serum by LC-MS/MS. This study reports the use of two validated LC with tandem MS (MS/MS) methods to study the residue depletion profile of phenylbutazone (PBZ) and its metabolite oxyphenbutazone (OXPBZ) from equine serum, urine, and muscle, kidney, and liver tissues. One LC-MS/MS method, with an LOQ of 1.0 ng/mL for PBZ and 2.0 ng/mL for OXPBZ, was used for the analysis of the two drugs in the biological fluids (equine urine and serum); the other LC-MS/MS method, with an LOQ of 0.5 ng/g for PBZ and OXPBZ, was used for the analysis of the drugs in the equine tissue samples. PBZ was administered intravenously to t...
Pharmacokinetics and in vitro efficacy of salicylic acid after oral administration of acetylsalicylic acid in horses. Although acetylsalicylic acid (ASA) is not frequently used as a therapeutic agent in horses, its metabolite SA is of special interest in equestrianism since it is a natural component of many plants used as horse feed. This led to the establishment of thresholds by horse sport organizations for SA in urine and plasma. The aim of this study was to investigate plasma and urine concentrations of salicylic acid (SA) after oral administration of three different single dosages (12.5Â mg/kg, 25Â mg/kg and 50Â mg/kg) of acetylsalicylic acid (ASA) to eight horses in a cross-over designed study. Results:...
Effects of xylazine and dexmedetomidine on equine articular chondrocytes in vitro. To assess the effects of xylazine and dexmedetomidine on equine chondrocytes, in vitro. Methods: Prospective, experimental study. Methods: Equine articular chondrocytes from five male horses. Methods: Chondrocytes were isolated from healthy equine articular cartilage of the metacarpo/metatarsophalangeal joints. Cell viability was assessed using the WST-8 assay by exposing chondrocytes to xylazine (0.5, 1, 2, 4, 8, 16.6, 25, 50 mg mL) or dexmedetomidine (0.001, 0.005, 0.01, 0.05, 0.175, 0.25 mg mL) for 15, 30 and 60 minutes. Based on the results of these tests, cells were treated with xyla...
Pharmacokinetics of intravenous continuous rate infusions of sodium benzylpenicillin and ceftiofur sodium in adult horses. OBJECTIVE To determine plasma drug concentrations after IV administration of a bolus followed by continuous rate infusion (CRI) of sodium benzylpenicillin and ceftiofur sodium to healthy adult horses. ANIMALS 6 Thoroughbred mares (3 to 9 years old; mean ± SD body weight, 544 ± 55 kg) with no history of recent antimicrobial treatment. PROCEDURES Horses were used in 2 experiments conducted 14 days apart. For each experiment, horses were housed individually in stables, and catheters were placed bilaterally in both jugular veins for drug administration by CRI (left catheter) and for intermittent...
Pharmacokinetics and tolerability of a new formulation of omeprazole in the horse. A new formulation of omeprazole in gastro-resistant granules was tested with regard to its pharmacokinetics and tolerability. Twenty-four horses were randomly divided into three groups (8 horses/group) and treated, according a parallel study design, as follows: Group A untreated (control group), Group B received 4Â mg/kg of omeprazole, and Group C received 12Â mg/kg of omeprazole, both of which were treated orally once a day for 90Â days. Blood samples, taken from Group B subjects during the 1st and the 29th day of treatment at pre-established time points, were used to determine the concentrat...
Validation of a method for sedatives and β-blockers determination in swine, bovine and equine kidney using liquid chromatography coupled with tandem mass spectrometry. A method for the determination of five sedatives and 14 β-blocker residues in swine, bovine and equine kidney was validated. Samples were extracted with acetonitrile and purified using dispersive solid phase extraction (d-SPE) with Celite 545 with subsequent analysis by LC-MS/MS. A simplified protocol was applied to validate the method scope extension to include new matrices. Parameters such as recovery, trueness, linearity (r), relative standard deviation (RSD), decision limit (CCα) and method capability (CCβ) were measured for the bovine and equine kidney matrices. The method was applied ...
Evaluation of xylazine and ketamine for maintenance of anesthesia in horses. Eight horses [5.6 ± 3.6 years, 489 ± 48.6 kg (mean ± SD)] were anesthetized four times under laboratory conditions to characterize physiologic and behavioral (reported elsewhere) responses associated with a 1-hours period of total intravenous anesthesia (TIA). Each horse was premedicated with xylazine (X, 0.75 mg kg−1) and anesthesia induced 5 minutes later with 5% guaifenesin (75 mg kg−1) and ketamine (K, 2 mg kg−1), all given IV After anesthetic induction, horses were intubated and received one of six treatments [X 35, K 90, O2; X 35, K 120, O2; X 35, K 120, air; X 35, K150, O2; X 7...
Shortened egg reappearance after ivermectin or moxidectin use in horses in the UK. This study reports ivermectin and moxidectin egg reappearance periods (ERP) from UK horses with persistently positive faecal egg counts (FEC), defined as positive FEC within the ERP of an anthelmintic post-treatment, or with FECs that remained positive after the normal ERP post-anthelmintic treatment. A selected population of UK pleasure horses deemed at high risk of strongyle infection was studied. The earliest ERP recorded after ivermectin or moxidectin, using first positive FEC, was 5 weeks. From 16 premises where moxidectin was used, five had ERP ≥12 weeks using two further metrics. For ...
[Vigilance for veterinary medicinal products: Reports of adverse reactions in the year 2015]. A total of 292 adverse reactions to veterinary medicinal products were reported during the year 2015. This represents an increase of 9% compared to the previous year (268 reports). Similar to previous years, most of the reactions reported were linked to the use of antiparasitics (55.1%), non-steroidal anti-inflammatory products (8.9%) or antiinfectives (9.3%). The affected animal species were primarily dogs (198 reports) and cats (42 reports), followed by cattle (31 reports) and horses (8 reports). Additional 42 reports were provided within the frame of consultations with Tox Info Suisse in ZÃ...
Quantification of dimethylsulfoxide (DMSO) in equine plasma and urine using HILIC-MS/MS. This paper describes quantitative methods for the determination of dimethylsulfoxide (DMSO) in equine plasma and urine based on simple precipitation and dilution followed by hydrophilic interaction liquid chromatography coupled to tandem mass spectrometry (HILIC-MS/MS). DMSO is a polar solvent with analgesic and anti-inflammatory properties. Its pharmacological features make it prohibited in horse racing. However, since DMSO is naturally present in the horses' environment, international threshold values have been implemented for plasma and urine (1 and 15 µg/mL, respectively). Previously pr...
Effect of topical ophthalmic latanoprost 0.005% solution alone and in combination with diclofenac 0.1% solution in healthy horses: a pilot study. To evaluate the effect of topical ophthalmic 0.005% latanoprost alone and in combination with 0.1% diclofenac on healthy horses. Methods: Twelve healthy adult horses. Methods: A randomized, masked crossover design was used with horses divided into three groups for once daily treatment in one randomly selected eye. For arm 1 of the study, Group D (n = 3) received 0.1% diclofenac, Group L (n = 3) received 0.005% latanoprost, and Group DL (n = 6) received 0.005% latanoprost and 0.2 ml of 0.1% diclofenac. For arm 2 of the study, horses from Group D and L were placed into Group DL and horses from G...
Evaluation of an oral direct factor Xa inhibitor anticoagulant in healthy adult horses. To assess whether an oral direct factor Xa inhibitor (DiXaI) anticoagulant drug used at the low end of the recommended dose in people achieves presumed prophylactic plasma concentrations and does not induce bleeding in horses. Methods: Experimental study. Methods: Field study. Methods: Ten healthy adult horses. Methods: A DiXaI was administered at a dose of 0.125 mg/kg every 24 h orally for 4 days. Following a wash-out period of 2 weeks, 8 of 10 horses received daily subcutaneous doses of a low molecular weight heparin (dalteparin) for 4 consecutive days at 50 IU/kg. In both trials, antifactor...
Doping control analysis of anabolic steroids in equine urine by gas chromatography-tandem mass spectrometry. Anabolic steroids are banned substances in equine sports. Gas chromatography-mass spectrometry (GC-MS) has been the traditional technique for doping control analysis of anabolic steroids in biological samples. Although liquid chromatography-mass spectrometry (LC/MS) has become an important technique in doping control, the detection of saturated hydroxysteroids by LC-MS remains a problem due to their low ionization efficiency under electrospray. The recent development in fast-scanning gas-chromatography-triple-quadrupole mass spectrometry (GC-MS/MS) has provided a better alternative with a sign...
Confirmatory analysis of etanercept in equine plasma by LC-MS for doping control. Etanercept is a protein-based medication for the treatment of human patients with rheumatoid arthritis and other autoimmune-based diseases; its pharmacological action is to inhibit and antagonize tumour necrosis factor alpha. Etanercept was rumoured to be used in horse racing in North America. To detect such use, the aim of this study was to develop a liquid chromatography-mass spectrometry (LC-MS) method for confirmation of etanercept in equine plasma. Etanercept was extracted from plasma by anti-human IgG antibody linked to magnetic beads. The analyte was reduced and alkylated, and then dige...
Pharmacokinetics of dextromethorphan and its metabolites in horses following a single oral administration. Dextromethorphan is an N-methyl-D-aspartate (NMDA) non-competitive antagonist commonly used in human medicine as an antitussive. Dextromethorphan is metabolized in humans by cytochrome P450 2D6 into dextrorphan, which is reported to be more potent than the parent compound. The goal of this study is to describe the metabolism of and determine the pharmacokinetics of dextromethorphan and its major metabolites following oral administration to horses. A total of 23 horses received a single oral dose of 2 mg/kg. Blood samples were collected at time 0 and at various times up to 96 h post drug ad...
