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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.
Evaluation of the effects of the R- and S-enantiomers of salbutamol on equine isolated bronchi.
Pulmonary pharmacology & therapeutics    December 31, 2010   Volume 24, Issue 2 221-226 doi: 10.1016/j.pupt.2010.12.008
Matera MG, Calzetta L, Rogliani P, Bardaro F, Page CP, Cazzola M.Equine obstructive pulmonary disease, also known as heaves or recurrent airway obstruction (RAO) is a common equine pulmonary disease with some similarities to human asthma and COPD, which represents a major cause of morbidity and loss of lung performance. Salbutamol has been widely used for the treatment of human airway diseases and has usually been prepared as the racemic form of the drug. However, recently the R-enantiomer of salbutamol has been introduced into clinical practice in the treatment of asthma in humans and this has been suggested to be an improvement on the racemic form of the ...
Screen and confirmation of PEG-epoetin β in equine plasma.
Drug testing and analysis    December 29, 2010   Volume 3, Issue 1 68-73 doi: 10.1002/dta.212
Chang Y, Maylin GM, Matsumoto G, Neades SM, Catlin DH.Methods have been developed to screen for and confirm darbepoetin alfa, recombinant human EPO, and methoxy polyethylene glycol-epoetin β (PEG-epoetin β) in horse plasma. All three methods screen samples with an enzyme-linked immunosorbent assay (ELISA) and confirm by liquid chromatography-tandem mass spectrometry (LC-MS/MS). This report focuses on PEG-epoetin β. The ELISA assay was able to detect PEG-epoetin β at 0.02 ng/mL in 50 µL of horse plasma. Many samples had high background levels of immunoreactivity; however, introducing polyethylene glycol 6000 (PEG 6000) into the samples before...
Different contribution of bovine papillomavirus type 1 oncoproteins to the transformation of equine fibroblasts.
The Journal of general virology    December 22, 2010   Volume 92, Issue Pt 4 773-783 doi: 10.1099/vir.0.028191-0
Yuan Z, Gault EA, Campo MS, Nasir L.Equine sarcoids represent the most common skin tumours in equids worldwide, characterized by localized invasion, rare regression and high recurrence following surgical intervention. Bovine papillomavirus type 1 (BPV-1) and less commonly BPV-2 are now widely recognized as the causative agents of the disease. Fibroblasts isolated from sarcoids are highly invasive. Invasion is associated with a high level of viral gene expression and matrix metalloproteinase upregulation. However, it remains unclear to what extent BPV-1 proteins are involved in the transformation of equine cells. To address this ...
Duration of corneal anaesthesia following multiple doses and two concentrations of tetracaine hydrochloride eyedrops on the normal equine cornea.
Equine veterinary journal    December 15, 2010   Volume 43, Issue 1 69-73 doi: 10.1111/j.2042-3306.2010.00118.x
Monclin SJ, Farnir F, Grauwels M.There is a clinical impression that tetracaine hydrochloride (THCl) eyedrops is a suitable topical anaesthetic in horses. Objective: To determine the duration of corneal anaesthesia following instillation of multiple doses and 2 concentrations of THCl in 10 healthy horses. Methods: The corneal touch threshold (CTT) was determined, in both eyes, before (basal CTT) and after application of one drop of 0.5% THCl, 2 drops at a 1 min interval of 0.5% THCl or one drop of 1% THCl. CTT was measured in mm every 5 min until complete recovery of the basal CTT. Treatments were separated by an interval of ...
Contemporary use of acepromazine in the anaesthetic management of male horses and ponies: a retrospective study and opinion poll.
Equine veterinary journal    December 15, 2010   Volume 43, Issue 1 88-98 doi: 10.1111/j.2042-3306.2010.00107.x
Driessen B, Zarucco L, Kalir B, Bertolotti L.Current use of acepromazine in the anaesthetic management of male horses and ponies and associated risks are largely unknown. Objective: To explore anaesthetic acepromazine use and related adverse effects in the male horse. Methods: Of 8533 anaesthetised horses and ponies medical records of male animals treated perianaesthetically with acepromazine were reviewed. Demographic data, time and dose of acepromazine administration, co-administered drugs, quality of induction and recovery from anaesthesia, arterial blood pressures, and occurrence of penile dysfunction were recorded. Practising ACVA a...
Determination of tear break-up time reference values and ocular tolerance of tetracaine hydrochloride eyedops in healthy horses.
Equine veterinary journal    December 15, 2010   Volume 43, Issue 1 74-77 doi: 10.1111/j.2042-3306.2010.00119.x
Monclin SJ, Farnir F, Grauwels M.Tetracaine hydrochloride (THCl) has been reported to cause irritation in dogs. In man, some topical anaesthetics have been shown to disrupt the tear film. Tear break-up time (TBUT) is a useful test allowing an assessment of the quality of the precorneal tear film. Only one TBUT value has been reported in horses with no information on the technique used. Objective: To provide a method for performing the TBUT in horses and to report any side effects of a single application of THCl in clinically normal horses, particularly on the stability of the tear film. Methods: In Study 1, one drop of 0.5 or...
Suspect novel adverse drug reactions to trimethoprim-sulphonamide combinations in horses: a case series.
Equine veterinary journal    December 15, 2010   Volume 43, Issue 1 117-120 doi: 10.1111/j.2042-3306.2010.00158.x
Stack A, Schott HC.Adverse drug reactions to trimethoprim-sulphonamide combinations are common in many species, manifesting as gastrointestinal tract disorders, dermatopathies and blood dyscrasias. In this case series, neurological abnormalities in 4 horses being treated with trimethoprim-sulphonamide combinations at normal dosages and in one foal that received an overdose are described. The horses developed hypermetric gait, agitation and erratic behaviour. All signs resolved once medication was withdrawn, and no horse had residual deficits. No other cause for observed neurological deficits could be determined....
Receptor-mediated enhancement of beta adrenergic drug activity by ascorbate in vitro and in vivo.
PloS one    December 13, 2010   Volume 5, Issue 12 e15130 doi: 10.1371/journal.pone.0015130
Dillon PF, Root-Bernstein R, Robinson NE, Abraham WM, Berney C.Previous in vitro research demonstrated that ascorbate enhances potency and duration of activity of agonists binding to alpha 1 adrenergic and histamine receptors. Objective: Extending this work to beta 2 adrenergic systems in vitro and in vivo. Methods: Ultraviolet spectroscopy was used to study ascorbate binding to adrenergic receptor preparations and peptides. Force transduction studies on acetylcholine-contracted trachealis preparations from pigs and guinea pigs measured the effect of ascorbate on relaxation due to submaximal doses of beta adrenergic agonists. The effect of inhaled albuter...
Effects of clopidogrel and aspirin on platelet aggregation, thromboxane production, and serotonin secretion in horses.
Journal of veterinary internal medicine    December 8, 2010   Volume 25, Issue 1 116-122 doi: 10.1111/j.1939-1676.2010.0647.x
Brainard BM, Epstein KL, LoBato D, Kwon S, Papich MG, Moore JN.Critically ill horses are susceptible to thrombotic disease, which might be related to increased platelet reactivity and activation. Objective: To compare the effect of oral clopidogrel and aspirin (ASA) on equine platelet function. Methods: Six healthy adult horses. Methods: Horses received clopidogrel (2 mg/kg p.o. q24h) or ASA (5 mg/kg p.o. q24h) for 5 days in a prospective randomized cross-over design. Platelet aggregation responses to adenosine diphosphate (ADP) and collagen via optical aggregometry, and platelet secretion of serotonin (5HT) and production of thromboxane B(2) (TXB(2) ) by...
Effect of heparin administration on urine protein excretion during the developmental stage of experimentally induced laminitis in horses.
American journal of veterinary research    December 2, 2010   Volume 71, Issue 12 1462-1467 doi: 10.2460/ajvr.71.12.1462
Uberti B, Pressler BM, Alkabes SB, Chang CY, Moore GE, Lescun TB, Sojka JE.To investigate the effects of heparin administration on urine protein excretion during the developmental stages of experimentally induced laminitis in horses. Methods: 13 horses. Procedures-Horses received unfractionated heparin (80 U/kg, SC, q 8 h; n=7) or no treatment (control group; 6) beginning 3 days prior to induction of laminitis. All horses were given 3 oligofructose loading doses (1 g/kg each) at 24-hour intervals and a laminitis induction dose (10 g of oligofructose/kg) 24 hours following the final loading dose (designated as 0 hours) via nasogastric tube. Serum glucose and insulin c...
Expression and function of 5-hydroxytryptamine 4 receptors in smooth muscle preparations from the duodenum, ileum, and pelvic flexure of horses without gastrointestinal tract disease.
American journal of veterinary research    December 2, 2010   Volume 71, Issue 12 1432-1442 doi: 10.2460/ajvr.71.12.1432
Prause AS, Guionaud CT, Stoffel MH, Portier CJ, Mevissen M.To evaluate the expression of the 5-hydroxytryptamine 4 (5-HT4) receptor subtype and investigate the modulating function of those receptors on contractility in intestinal tissues obtained from horses without gastrointestinal tract disease. Methods: Smooth muscle preparations from the duodenum, ileum, and pelvic flexure collected immediately after slaughter of 24 horses with no history or signs of gastrointestinal tract disease. Methods: In isometric organ baths, the contractile activities of smooth muscle preparations in response to 5-hydroxytryptamine and electric field stimulation were asses...
Use of in vitro technologies to study phase II conjugation in equine sports drug surveillance.
Bioanalysis    November 30, 2010   Volume 2, Issue 12 1971-1988 doi: 10.4155/bio.10.135
Taylor P, Scarth JP, Hillyer LL.Within equine drug surveillance, there is significant interest in analyzing intact phase II conjugates of drugs in urine, but progress has been limited by a lack of reference material. Methods: In this study, in vitro techniques using equine liver fractions were employed to produce glucuronide and sulfate conjugates of stanozolol, 16β-hydroxystanozolol and nandrolone, the glucuronide conjugate of morphine and the glutathione metabolite of chlordinitrobenzene for the first time in equine sports drug surveillance. Results: The glucuronide conjugate of the synthetic progestagen altrenogest was a...
Systemic treatment with high dose of flunixin-meglumine is able to block ovulation in mares by inducing hemorrhage and luteinisation of follicles.
Theriogenology    November 26, 2010   Volume 75, Issue 4 707-714 doi: 10.1016/j.theriogenology.2010.10.011
Cuervo-Arango J, Domingo-Ortiz R.Prostaglandins play an obligatory role during the process of ovulation in mammals. Ovulation can be blocked by intrafollicular administration of non-steroidal anti-inflammatory drugs (NSAIDs) in several domestic species including the mare as well as by systemic administration of these drugs in women. In the mare, the effect of systemic NSAIDs treatment on ovulation has not been critically studied. The objectives of this study were: a) to determine whether high dose of flunixin-meglumine (FM) administered systemically to mares during the periovulatory period was able to block ovulation; and b) ...
Comparative human-horse sequence analysis of the CYP3A subfamily gene cluster.
Animal genetics    November 26, 2010   Volume 41 Suppl 2 72-79 doi: 10.1111/j.1365-2052.2010.02111.x
Schmitz A, Demmel S, Peters LM, Leeb T, Mevissen M, Haase B.Cytochrome P450 enzymes (CYP450s) represent a superfamily of haem-thiolate proteins. CYP450s are most abundant in the liver, a major site of drug metabolism, and play key roles in the metabolism of a variety of substrates, including drugs and environmental contaminants. Interaction of two or more different drugs with the same enzyme can account for adverse effects and failure of therapy. Human CYP3A4 metabolizes about 50% of all known drugs, but little is known about the orthologous CYP450s in horses. We report here the genomic organization of the equine CYP3A gene cluster as well as a compara...
Atipamezole antagonism of an ACTH stimulation test in ponies sedated with detomidine.
Journal of veterinary pharmacology and therapeutics    November 22, 2010   Volume 34, Issue 5 508-511 doi: 10.1111/j.1365-2885.2010.01251.x
Luna SP, Taylor PM, Carregaro AB.No abstract available
Pharmacokinetics and toxicity of ciprofloxacin in adult horses.
Journal of veterinary pharmacology and therapeutics    November 11, 2010   Volume 33, Issue 6 587-594 doi: 10.1111/j.1365-2885.2010.01167.x
Yamarik TA, Wilson WD, Wiebe VJ, Pusterla N, Edman J, Papich MG.Using a randomized, cross-over study design, ciprofloxacin was administered i.g. to eight adult mares at a dose of 20 mg/kg, and to seven of the eight horses at a dose of 5 mg/kg by bolus i.v. injection. The mean C(0) was 20.5 μg/mL (±8.8) immediately after i.v. administration. The C(max) was 0.6 μg/mL (±0.36) at T(max) 1.46 (±0.66) h after the administration of oral ciprofloxacin. The mean elimination half-life after i.v. administration was 5.8 (±1.6) h, and after oral administration the terminal half-life was 3.6 (±1.7) h. The overall mean systemic availability of ...
Preface: Pain in horses: physiology, pathophysiology, and therapeutic implications.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 xi-xii doi: 10.1016/j.cveq.2010.08.003
Muir WW.No abstract available
Opioid analgesia in horses.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 493-514 doi: 10.1016/j.cveq.2010.07.002
Clutton RE.Opioid analgesics have been the foundation of human pain management for centuries, and their value in animals has increased since it was proposed that it is the veterinarian's duty to alleviate pain whenever it may occur. Compared with other domesticated species, the horse has benefitted less from the increased understanding of opioid pharmacology in animals, because early literature was overlooked and later work, which examined adverse side effects rather than analgesia, concluded that analgesic and excitatory doses were irreconcilably close. More recent studies have indicated a widening role...
NMDA receptor antagonists and pain: ketamine.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 565-578 doi: 10.1016/j.cveq.2010.07.009
Muir WW.N-Methyl-D-aspartate (NMDA) is a synthetic chemical binding molecule (ligand) that selectively binds to the "slow response" glutamate NMDA receptor (NMDAR). NMDARs are important for normal brain function and play a central role in learning, memory, and the development of central nervous system hyperactive states. Diverse chemicals belonging to various drug families have demonstrated NMDAR antagonistic effects. Ketamine has been shown to produce antihyperalgesic effects produced by incision and tissue or nerve damage, and has become popular in equine practice as an anesthetic and more recently ...
Local anesthetics as pain therapy in horses.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 533-549 doi: 10.1016/j.cveq.2010.07.004
Doherty TJ, Seddighi MR.This article describes the rationale behind the use of systemically administered lidocaine as an analgesic. The analgesic efficacy of intravenously administered lidocaine is well documented by studies in human patients and laboratory animals. The mechanism by which systemically administered lidocaine produces analgesia is uncertain but is thought to include action at sodium, calcium, and potassium channels and the N-methyl-D-aspartate acid receptor. In addition, the anti-inflammatory actions of lidocaine are important in producing analgesia because inflammatory mediators augment neuronal excit...
Spinal anesthetics and analgesics in the horse.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 551-564 doi: 10.1016/j.cveq.2010.07.005
Natalini CC.In the past 10 years, there have been many recent advances in spinal techniques in horses, both epidural and subarachnoid, to identify drugs or drug combinations that have sensory effects without motor nerve paralysis, thus providing pain control without these horses becoming recumbent. Opioids, alpha-2 agonists, dissociative drugs, and others have been investigated. Many of these drugs, which have serious side effects when injected systemically in horses, have been shown to have useful analgesic effects when injected spinally. Morphine-like opioids have the greatest potential for spinal use a...
Pain in osteoarthritis.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 619-642 doi: 10.1016/j.cveq.2010.07.007
van Weeren PR, de Grauw JC.This article focuses on pain associated with osteoarthritis (OA). It first describes the basic biology of articular cartilage and other joint structures and the defining features of the osteoarthritic disease process. Subsequently, the possible origins of pain in OA are discussed before embarking on how to manage this clinical entity. The emphasis is on the pharmacologic management of joint pain, and attention is paid to systemic therapeutic strategies as well as to local (intra-articular) treatment modalities. Nonmedical ways of modulating joint pain are briefly mentioned, but not extensively...
Alpha-2 agonists as pain therapy in horses.
The Veterinary clinics of North America. Equine practice    November 9, 2010   Volume 26, Issue 3 515-532 doi: 10.1016/j.cveq.2010.07.003
Valverde A.Alpha-2 agonists, such as xylazine, clonidine, romifidine, detomidine, medetomidine, and dexmedetomidine, are potent analgesic drugs that also induce physiologic and behavioral changes, such as hypertension, bradycardia, atrioventricular block, excessive sedation and ataxia, all of which can potentially limit their systemic use as analgesics in some clinical cases. The use of medetomidine and dexmetomidine has been introduced for equine anesthesia/analgesia, and although not approved in this species, their increased specificity for alpha-2 receptors may offer some potential advantages over the...
Effect of different workload and hydrocortisone in vitro on platelet aggregation in athletic horse.
Polish journal of veterinary sciences    November 3, 2010   Volume 13, Issue 3 501-506 
Casella S, Giannetto C, Giudice E, Piccione G.The objective of the present study was to evaluate the platelet response to different workload in athletic horse and the influence of hydrocortisone on this response. For this purpose, six Sella Italiana gelding athletic horses, ranging in age from 8 to 10 years and clinically healthy, were subjected to four different exercises: horse-walker, treadmill, obstacle course of 1.00 m and obstacle course of 1.25 m. From all the horses, citrated plasma samples were collected at rest, immediately after exercise and 30 min after the end of the exercise to assess the maximum degree of platelet aggregati...
Drug metabolism in the horse: a review.
Drug testing and analysis    October 22, 2010   Volume 3, Issue 1 19-53 doi: 10.1002/dta.174
Scarth JP, Teale P, Kuuranne T.A detailed understanding of equine drug metabolism is important for detection of drug abuse in horseracing and also in veterinary drug development and practice. To date, however, no comprehensive review of equine drug metabolism has been published. The majority of literature regarding equine drug metabolite profiles is derived from sports drug detection research and is generally targeted at detecting marker metabolites of drug abuse. However, the bulk of the literature on equine drug metabolism enzymology is derived from veterinary studies aimed at determining the molecular basis of metabolism...
Antimicrobial activity of tulathromycin and 14 other antimicrobials against virulent Rhodococcus equi in vitro.
Veterinary therapeutics : research in applied veterinary medicine    October 20, 2010   Volume 11, Issue 2 E1-E9 
Carlson KL, Kuskie KR, Chaffin KM, Libal MC, Giguère S, Lawhon SD, Cohen ND.This study determined the antimicrobial activity of tulathromycin against Rhodococcus equi in vitro. Ninety-eight virulent isolates of R. equi from equine clinical cases were examined, of which 20 isolates were macrolide resistant. A custom 96-well antimicrobial susceptibility testing plate was used, allowing 14 additional antimicrobials to be tested against R. equi. Isolates were cultured with various concentrations of antimicrobials, and minimal inhibitory concentration (MIC) values were determined. Tulathromycin was found to have poor activity in vitro against R. equi isolates susceptible o...
The effects of deferoxamine mesylate on iron elimination after blood transfusion in neonatal foals.
Journal of veterinary internal medicine    October 19, 2010   Volume 24, Issue 6 1475-1482 doi: 10.1111/j.1939-1676.2010.0621.x
Elfenbein JR, Giguère S, Meyer SK, Javsicas LH, Farina LL, Zimmel DN, Sanchez LC.Hepatic failure is one of the more common complications in foals requiring blood transfusion to treat neonatal isoerythrolysis. Iron intoxication is likely the cause of hepatic injury. Objective: To determine the effects of deferoxamine on iron elimination in normal foals. Methods: Thirteen neonatal foals. Methods: Randomized-controlled trial. At 1-3 days of age, foals received either 3 L of washed packed dam's red blood cells (RBC) or 3 L of saline IV once. Foals were treated with deferoxamine (1 g) or saline (5 mL) SC twice daily for 14 days. Foals were randomly assigned to 1 of 3 gr...
Therapy of equine infectious keratitis: a review.
Equine veterinary journal. Supplement    October 14, 2010   Issue 37 19-23 doi: 10.1111/j.2042-3306.2010.tb05630.x
Clode AB.The following article briefly discusses the pathogenesis of infectious keratitis in the horse, followed by discussion of management and pharmacological aspects to be considered when devising a therapeutic protocol for affected patients.
Equine recurrent uveitis: the viewpoint from the USA.
Equine veterinary journal. Supplement    October 14, 2010   Issue 37 57-61 doi: 10.1111/j.2042-3306.2010.tb05636.x
Gilger BC.Equine recurrent uveitis (ERU) is a common disease in horses in the USA. There have been many advances in the treatment of ERU; however, frequent misdiagnosis of ERU occurs in cases of primary corneal or uveal disease. It is critical to remember that primary uveitis (i.e. one bout of inflammation) is a different disease to ERU, which is an immune mediated recurrent uveitis. Standard symptomatic anti-inflammatory therapy is effective to control most cases of ERU; however, some horses require advanced therapy, such as placement of drug delivery devices or removal of the vitreous, when they fail ...
[The efficacy of anthelmintic drugs against horse strongyles in the area of Salzburg and preliminary results of selective anthelmintic treatment].
Wiener klinische Wochenschrift    October 7, 2010   Volume 122 Suppl 3 71-75 doi: 10.1007/s00508-010-1441-y
Becher AM, Pfister K.In recent years more and more cases of anthelmintic resistant equine strongyles were reported. The latest developments are cases of resistance against macrocyclic lactones. In order to delay this process less anthelmintics and only those which have been previously tested for their efficacy on each individual farm should be used. During the grazing season 2008 faecal samples of 281 horses and 5 donkeys from 26 farms were analysed in the area of Salzburg. To 164 of these horses selective anthelmintic treatment was implemented. Every four weeks faecal samples from the 164 horses were quantitative...
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