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.
Sheahan BJ, Schubert AG, Schubert W, Sheats MK, Schnabel LV, Gilbertie JM.Neutrophil extracellular traps (NETs) play a significant role in response to a variety of infectious and inflammatory stimuli in human and veterinary medicine. Although entrapment of bacteria can be an important function of NETs, the exuberant release of DNA and other intracellular molecules has also been negatively implicated in the pathogenesis of different diseases. Thus, NET formation must be tightly controlled and represents an opportunity for therapeutic interventions. Horses are particularly sensitive to bacterial stimuli that have previously been shown to cause NETs in other species, b...
Júnior GS, de Souza JV, de Souza Ferreira W, Florentino VRD, Valente TC, Comassetto F, Oleskovicz N.This study aimed to evaluate the sedation degree, cardiopulmonary effects, and detomidine-sparing during dental occlusal adjustment in standing horses using a bolus and constant rate infusion (CRI) of detomidine alone or in combination with butorphanol or methadone. In this randomized, blinded clinical trial, 24 healthy adult horses were assigned to the detomidine (DT), detomidine-butorphanol (DB), or detomidine-methadone (DM) group. DT received an intravenous bolus of detomidine (20 μg/kg), followed by CRI at 20 μg/kg/h. DB received detomidine (10 μg/kg) and butorphanol (0.02 mg/kg) boluse...
Pain management in horses plays a pivotal role in the therapeutic approach to several diseases. Horses have cannabinoid receptors at the level of dorsal root ganglia, blood vessels, and synoviocytes that can be up or down- regulated by inflammatory conditions, justifying the possible efficacy of exogenous cannabinoids (i.e., phytocannabinoids) in managing several painful pathologies in this animal species. However, the current use of supplements containing cannabidiol (CBD) in equines is based on anecdotal evidence, without the support of sufficient pharmacokinetic studies. In humans, the conc...
Galinelli NC, Bamford NJ, Erdody ML, Mackenzie SA, Warnken T, Harris PA, Sillence MN, Bailey SR.Due to the high frequency of laminitis reported for both conditions, the relationship between pituitary pars intermedia dysfunction (PPID) and insulin dysregulation (ID), and the potential role of dopamine in modifying insulin secretion, requires further investigation. Objective: To evaluate the effect of pergolide mesylate on insulin sensitivity and postprandial insulin and glucose responses in horses and ponies with ID, both with or without concurrent PPID. Methods: Randomised crossover study. Methods: Sixteen horses and ponies, comprising eight matched pairs (PPID+ID or ID-only), were given...
Guo W, Li Z, Mao W, Liu X, Yang Y, Yu J, Yang H, Gao R.Flunixin meglumine (FM) is commonly used in painful conditions in horses; however, it may contribute to equine gastric ulcer syndrome (EGUS). Some veterinarians combine omeprazole (OME) and FM to reduce EGUS risk. However, the efficacy and safety of this combination in Mongolian horses with chronic lameness remain unknown. Objective: To investigate the changes in lameness and EGUS scores in Mongolian horses through the comparison of three treatment strategies: FM, FM + OME and placebo treated control (CON) and to assess the effects of these treatments on gastric fluid pH, serum total prote...
Guzmán JFC, Gontijo AS, Melgaço ES, Faria SA, Baldi MLC, Sousa LN, Wenceslau RR, Fantini P, Xavier ABDS, Beier SL.Morphine has significant clinical and analgesic effects in horses, but its impact on the gastrointestinal tract requires further understanding. This study assessed the analgesic and gastrointestinal effects of morphine in horses undergoing elective orchiectomy in the quadrupedal position. Thirty uncastrated male horses were randomly assigned to three groups: orchiectomy without morphine and sedation protocol (OSM), orchiectomy with morphine and sedation protocol (OM), and administration of morphine alone in the absence of orchiectomy (M). The anesthetic protocol involved acepromazine (0.05 mg/...
Roustaei A, Masoudifard M, Azari O, Keshipour H, Koohestani O.The effects of dexmedetomidine (DEX), as a sedative drug, on echocardiographic measurements have been investigated in many species but not in horses. Therefore, this study aimed to evaluate the echocardiographic and clinical effects of two sedative doses of DEX in healthy horses. Six female crossbred horses weighted 250-330 kg underwent echocardiography before and after sedation by intravenous administration of a low dose of 3.5 μg/kg (LD) and a high dose of 7 μg/kg (HD) of DEX. A significant increase (p≤ 0.05) was observed in the diameters of the pulmonary artery and the left atrium measu...
Kublicka A, Lorek D, Mikołajczyk-Martinez A, Chodaczek G, Chwirot A, Bażanów B, Matczuk AK.The process of viral entry into host cells is crucial for the establishment of infection and the determination of viral pathogenicity. A comprehensive understanding of entry pathways is fundamental for the development of novel therapeutic strategies. Standard techniques for investigating viral entry include confocal microscopy and flow cytometry, both of which provide complementary qualitative and quantitative data. Imaging flow cytometry, which integrates the advantages of both methodologies, offers significant potential in virological studies. In this investigation, we employed imaging flow ...
The AnalystJanuary 23, 2025
doi: 10.1039/d4an01501k
Göktaş EF, Kabil E, Söylemez Yeşilçimen E, Dirikolu L.Various technical methodologies are required to accurately detect substances of different chemical and pharmacological properties in biological samples, which are increasing in number and variety daily. Therefore, laboratories where many samples and different factors are analyzed simultaneously need methods with easy sample preparation, short analysis times and low analysis costs. In this study, the objective was to scan substances susceptible to chemical degradation, amenable to analysis without hydrolysis, and exhibiting short-term stability by employing a straightforward, expeditious, and c...
Reed RA, Carroll AT, Dantino SC, Quandt JE, Barletta M, Sakai DM.To determine the influence of xylazine infusion on survival to discharge and describe the associated intraoperative requirement for isoflurane, use of positive inotropes and vasopressors, and recovery time in horses undergoing exploratory laparotomy. Methods: Retrospective cohort study. Methods: A total of 352 horses. Methods: Medical records of horses undergoing anesthesia for exploratory laparotomy from January 2018 to December 2023 were reviewed. Data collected included survival to discharge, results of diagnostic tests, end tidal isoflurane concentration (FE'Iso), use of vasopressors/inotr...
Ikeda Y, Kuroda T, Mita H, Tamura N, Ohta M.We compared the antihistamine effect of four new antihistamines with olopatadine, which is used to treat equine allergic diseases. Six healthy Thoroughbred horses received oral doses of olopatadine (50 mg), levocetirizine (50 mg), bilastine (200 mg), rupatadine (100 mg), and desloratadine (50 mg) at >2-week intervals. The effects were investigated by measurement of the wheal area induced by histamine intradermal injection, and inhibition rate was compared with positive and negative controls. The maximum wheal inhibition rate (mean ± SD) of olopatadine (85.3% ± 7.7%) was significantly higher ...
Henderson ARP, Valverde A, Marchiori J, Tisotti T, Torrent A, Côté N, Gomez DE.To determine the effects of rapid (1 minute) and slow (10 minutes) intravenous (IV) injection of sodium penicillin on arterial blood pressure in anesthetized horses. Methods: Prospective randomized clinical trial. Methods: A group of 29 client-owned horses of various breeds, 1-20 years old, with body masses of 360-710 kg. Methods: General anesthesia was induced with a variety of anesthetic protocols and maintained with isoflurane under mechanical ventilation, with hourly doses of IV lidocaine and an infusion of dexmedetomidine. Horses were administered IV intraoperative penicillin every 2 hour...
Wang Z, Li Y, Xi X, Zou Q, Zhang Y.In this paper, a novel molecularly imprinted polymer membrane modified glassy carbon electrode for electrochemical sensors (MIP-OH-MWCNTs-GCE) for epinephrine (EP) was successfully prepared by a gel-sol method using an optimized functional monomer oligosilsesquioxane-AlO sol-ITO composite sol (ITO-POSS-AlO). Hydroxylated multi-walled carbon nanotubes (OH-MWCNTs) were introduced during the modification of the electrodes, and the electrochemical behavior of EP on the molecularly imprinted electrochemical sensors was probed by the differential pulse velocity (DPV) method. The experimental conditi...
Costa GL, Tabbì M, Bruschetta G, Spadola F, Leonardi F, Bruno F, Iannelli NM, Licata P, Macrì F, Passino ES, Macrì D, Interlandi C.The study aimed to evaluate the analgesic efficacy of tapentadol in horses, by determining plasma serotonin concentration and adrenocortical response, as biomarkers of pain stress in chronic joint disorders. Thirty-six horses (20 females and 16 males) were divided into three groups of 12 subjects each: group A, osteoarthritis (OA), grade 3-4 lameness; group B, OA, grade 5 lameness; and group C, no OA, no lameness, were enrolled. The orthopedic examination included flexion tests, and radiological and ultrasound examinations. The degree of lameness has been estimated from 0 to 5 according to the...
So YM, Kwok WH, Ching CCW, Wong COL, Wan TSM, Ho ENM.Anabolic-androgenic steroids (AAS) are banned substances in both human and equine sports. They are often administered intramuscularly to horses in esterified forms for the purpose of extending their duration of action. As such, the detection of intact esters of endogenous steroids in hair is particularly advantageous, as it can provide unequivocal proof of their external origin. Compared with urine and blood matrices, hair in general allows a longer detection window as long as the administered drug can be incorporated into hair and has not degraded. This can be useful in doping control of equi...
Aragona F, Tabbì M, Gugliandolo E, Giannetto C, D'Angelo F, Fazio F, Interlandi C.Cannabidiol (CBD) is a non-psychotropic cannabinoid obtained from hemp (Cannabis sativa L.) used for pain management in companion animals including horses. The present study aimed to evaluate the efficacy of cannabidiolic acid (CBDA) and cannabigerol/cannabidiol oil (CBG/CBD) oral administration in alleviating pain in adult horses affected by chronic osteoarthritis (OA). Twenty-four horses (10 geldings and 14 mares), aged between 11 and 18 years old, were equally divided into two groups. One group received CBDA 15% oil and the other group received CBG/CBD oil (CBG20%-CBD10%) for 14 consecuti...
Equine asthma, a prevalent chronic inflammatory condition affecting the equine population, significantly compromises the performance and quality of life in affected horses. Inhaled corticosteroids (ICS) are often the first-line pharmacological intervention due to their potent anti-inflammatory properties. This meta-analysis investigates the clinical efficacy of ICS in treating equine asthma, emphasizing the number needed to treat (NNT) and the likelihood of achieving a clinical response. A comprehensive literature search identified relevant studies comparing ICS with placebo (PCB) controlled t...
Jargielo MM, Kritchevsky JE, Bertin FR.Pergolide, labeled for the treatment of pituitary pars intermedia dysfunction, is 90% protein bound and might cause a decrease in blood thyroid hormone concentrations by displacing them from binding proteins. This study investigated the effect of pergolide on the equine thyroid function. Methods: This was an analytic, observational, cohort study. Six horses (17 to 24 years old and 530 to 599 kg) received 1 mg of pergolide mesylate orally once a day from days 1 to 6. Total T4 (tT4) was measured daily from day 0 to 11 (before, during, and after pergolide treatment). Thyrotropin-releasing hormone...
Mascarenhas C, Castro D, Lascola KM, Hofmeister E, Clark-Price SC.To assess the effect of two different doses of intramuscular atipamezole on head height (HH) in horses after sedation with detomidine. Methods: Randomized, blinded, triple crossover study. Methods: Eight healthy adult horses. Methods: Baseline HH was measured before detomidine (40 μg kg) was injected intravenously. HH was measured at 10 and 20 minutes after injection. Then, saline, atipamezole 60 μg kg (AT60) or 120 μg kg (AT120) was injected intramuscularly. HH measurements were repeated at 10 minutes intervals for 100 minutes. HH data were analyzed with a linear mixed model. Significance ...
Kemp KL, Skinner JE, Bertin FR.Phenylbutazone is prescribed for laminitis-associated pain and decreases glucose and insulin responses to an oral glucose test (OGT) in horses with insulin dysregulation (ID). Objective: Investigate the effect of phenylbutazone administration on the enteroinsular axis in horses. Methods: Sixteen horses, including 7 with ID. Methods: Randomized cross-over study design, with horses assigned to treatment with phenylbutazone (4.4 mg/kg IV q24h) or placebo (5 mL 0.9% saline). On Day 9 of treatment, an OGT was conducted, followed by a 10-day washout period, administration of the alternative trea...
Sundra T, Knowles E, Rendle D, Kelty E, Lester G, Rossi G.The metabolic and lipid profiles of horses treated with sodium-glucose cotransporter 2 inhibitors are not well understood. This retrospective study evaluated blood parameters in hyperinsulinemic horses treated with either ertugliflozin (0.05 mg/kg) or dapagliflozin (0.02 mg/kg) orally once daily. Blood samples were collected at baseline (day 0) and after 7 and/or 30 days of treatment. Statistical analyses were conducted using Wilcoxon signed-rank, Mann-Whitney and Spearman's rank correlation tests. Thirty-four horses received dapagliflozin and 24 received ertugliflozin. Significant (p<0.05)...
Kwak YB, Seo SA, Kim M, Yoon J.Ethyl pyruvate (EP) has emerged as a promising compound with potential therapeutic benefits attributed to its anti-inflammatory and antioxidant properties. This study aimed to understand the effects of EP on plasma metabolites and immune cells in horses, utilizing advanced liquid chromatography-mass spectrometry (LC-MS)-based metabolomics, quantitative polymerase chain reaction (qPCR), and blood chemistry analyses. Our comprehensive analysis detected 2,366 ions, and 126 metabolites were accurately identified. Remarkably, EP administration induced significant changes in 28 metabolites at 1 h a...
Li S, Li L, Sun Y, Khan MZ, Yu Y, Ruan L, Chen L, Zhao J, Jia J, Li Y, Wang C, Wang T.Equid herpesvirus type 8 (EqHV-8) is known to cause respiratory disease and miscarriage in horses and donkeys, which is a major problem for the equine farming industry. However, there are currently limited vaccines or drugs available to effectively treat EqHV-8 infection. Therefore, it is crucial to develop new antiviral approaches to prevent potential pandemics caused by EqHV-8. This study evaluates the antiviral and antioxidant effects of cepharanthine against EqHV-8 by employing both in vitro assays and in vivo mouse models to assess its therapeutic efficacy. To assess the effectiveness of ...
Ohnuma K, Hirano-Kodaira M, Bannai M, Shimizu Y, Yamada M, Kinoshita K, Ngai-Wa Leung G, Ishii H.The abuse of prohibited peptide-based drugs with a broad spectrum of chemical characteristics poses a significant concern for the horseracing industry. Recently, there has been a notable increase in positive cases of small-peptide drugs reported in equine and canine sports. In addition to small peptides, large peptides (over 2 kDa) with structural diversity have also entered the market in increasing numbers as drugs for humans and livestock. However, the simultaneous analysis of both small- and large-peptide-based drugs is still challenging. In this study, a screening method was developed to c...
Sousa LN, Winter IC, Varela DD, Luvison EZ, Guzmán JFC, Machado AMV, Figueiredo RDV, Pena GT, Dos Santos ACS, Faleiros RR, Carvalho AM.The present study involved seven horses in a randomized crossover clinical trial to evaluate the effect of lidocaine on horses with induced endotoxemia. Horses received intravenous lidocaine (1.5 mg/kg bolus, followed by 0.05 mg/kg bwt/min) or placebo (0.9% sodium chloride at the same manner) one hour before LPS administration (0.03 μg/kg, IV infusion over 30 min). We monitored clinic and hematologic parameters, abdominal auscultation, ultrasound, and pain over time. No relevant clinical differences existed between treatments regarding peristalsis, abdominal pain, or any other parameters befo...
Mersich I, Bishop RC, Diaz Yucupicio S, Nobrega AD, Austin SM, Barger AM, Fick ME, Wilkins PA.Coagulopathy is common in equine critical illness, with its early recognition being crucial for patient management and prognosis. In vitro viscoelastic (VE) hypercoagulability with decreased RCM/PCV has been demonstrated in dogs but not horses. Our objective was to evaluate the effects of acepromazine-induced (0.1 mg/kg IV) decreased RCM on VE and plasma coagulation parameters using a prospective interventional study of eight adult horses. Complete blood count (CBC), fibrinogen, prothrombin time (PT), partial thromboplastin time (PTT), packed cell volume (PCV), total solids (TS), and VCM Vet...
Wong AM, Schier MF, Hosgood G, Drynan E, Raisis AL.To explore the influence of acepromazine on the cardiovascular effects of dobutamine in isoflurane-anaesthetised horses premedicated with romifidine. Methods: Prospective randomised clinical trial. Methods: A total of 18 horses undergoing elective arthroscopy were enrolled, of which 12 horses requiring dobutamine were included. Methods: Horses were randomised to receive acepromazine 0.02 mg kg (Group A+) intravenously (IV) or none (Group A-), 35 minutes before anaesthesia. Horses received xylazine 0.2 mg kg concurrently to facilitate IV access. Horses were premedicated with romifidine 0.08 mg ...
Lehman ML, Domenig O, Ames MK, Morgan JM.Furosemide, a commonly used diuretic, activates the renin-angiotensin-aldosterone system (RAAS) in other species. Little is known about RAAS peptide activation in horses. Objective: To evaluate equilibrium analysis as a practical method for RAAS quantification in horses and describe the RAAS response to a single dose of furosemide. We hypothesize that furosemide would cause transient increase in RAAS peptides in horses. Methods: 14 healthy adult thoroughbreds from a university teaching herd. Methods: Horses received either furosemide (1 mg/kg IV) or saline IV in a crossover study design. Pro...
Elbourne M, Keledjian J, Cawley A, Fu S.Altrenogest, also known as allyltrenbolone, is a synthetic form of progesterone used therapeutically to suppress unwanted symptoms of estrus in female horses. Altrenogest affects the system by decreasing levels of endogenous gonadotrophin and luteinizing and follicle-stimulating hormones, which in turn decreases estrogen and mimics the increase of progesterone production. This results in more manageable mares for training and competition alongside male horses while improving the workplace safety of riders and handlers. However, when altrenogest is administered, prohibited steroid impurities su...
Scepek S, Coorssen JR, Lindau M.Using the patch-clamp technique, we studied the role of protein phosphorylation and dephosphorylation on the exocytotic fusion of secretory granules with the plasma membrane in horse eosinophils. Phorbol 12-myristate 13-acetate (PMA) had no effect on the amplitude and dynamics of degranulation, indicating that the formation of fusion pores is insensitive to activation of protein kinase C (PKC). Fusion pore expansion, however, was accelerated approximately 2-fold by PMA, and this effect was abolished by staurosporine. Elevating intracellular Ca2+ to 1.5 microM also resulted in a 2-fold accelera...
van der Kraan PM.Osteoarthritis (OA) is the most common joint disease but an effective pharmacological therapy has not been developed yet. To identify targets for treatment and ways to interfere with OA development and progression both spontaneous and induced OA models are still needed. In this narrative review it is discussed what variables can be identified that lead to variation in OA animal model studies. Literature was screened (Pubmed) with the following terms; OA animal models in combination with species, age, strain, gender/sex, housing, diet, fighting, circadian rhythm, transgenic. Relevant articles ...
Perkins GA, Lamb S, Erb HN, Schanbacher B, Nydam DV, Divers TJ.Plasma ACTH levels have been variable in horses with a positive clinical response for therapy for equine Cushing's Disease (ECD). Therefore, our purpose was to determine the value of monitoring plasma adrenocorticotropin (ACTH) levels during treatment of equine Cushing's disease (ECD) with either cyproheptadine (n = 32) or pergolide (n = 10). First, we validated the chemiluminescent ACTH assay (specificity, precision, accuracy, intra-assay and interassay variations) and tested methods of handling the whole blood from the time of collection to when the ACTH was assayed. The sensitivity and spec...
Iyer U, Kadambi VJ.Antibody drug conjugates (ADCs) consist of an antibody attached to a cytotoxic drug by means of a linker. ADCs provide a way to couple the specificity of a monoclonal antibody (mAb) to the cytotoxicity of a small-molecule drug and, therefore, are promising new therapies for cancer. ADCs are prodrugs that are inactive in circulation but exert their cytotoxicity upon binding to the target cancer cell. Earlier unsuccessful attempts to generate ADCs with therapeutic value have emphasized the important role each component plays in determining the efficacy and safety of the final ADC. Scientific adv...
de Grauw JC, van de Lest CH, Brama PA, Rambags BP, van Weeren PR.Meloxicam is a commonly used nonsteroidal anti-inflammatory drug in equine practice, but little is known about its in vivo effects on joint inflammation and cartilage turnover. Objective: To study the effects of meloxicam on biomarkers of inflammation, matrix metalloproteinase (MMP) activity, and cartilage biomarkers in joints with experimental synovitis. Methods: In a 2-period cross-over study, synovitis was induced at T = 0 h in the L or R intercarpal joint of 6 horses by intraarticular injection of 0.5 ng lipopolysaccharide (LPS). Horses received once daily meloxicam (0.6 mg/kg bwt per os) ...
Nielsen MK, Reinemeyer CR, Donecker JM, Leathwick DM, Marchiondo AA, Kaplan RM.Anthelmintic resistance is becoming increasingly prevalent among equine nematode parasites. The first reports documenting resistance were published in the 1960s, just a short time after introduction of the first modern anthelmintics phenothiazine and thiabendazole. Several factors are known to influence development of resistance, but evidence specific to equine parasites is limited. Most current knowledge and applications have been extrapolated from research with trichostrongylid parasites of sheep. The number of cyathostomin species co-infecting horses adds to the complexity of investigating ...
Clegg PD, Strassburg S, Smith RK.Injuries to tendons are common in both human athletes as well as in animals, such as the horse, which are used for competitive purposes. Furthermore, such injuries are also increasing in prevalence in the ageing, sedentary population. Tendon diseases often respond poorly to treatment and require lengthy periods of rehabilitation. The tendon has a unique extracellular matrix, which has developed to withstand the mechanical demands of such tensile-load bearing structures. Following injury, any repair process is inadequate and results in tissue that is distinct from original tendon tissue. There ...
Harlow BE, Lawrence LM, Flythe MD.Antibiotics are important to equine medicine, but antibiotic-associated diarrhea (AAD) can lead to poor performance and even mortality. AAD is attributed to disruption of the hindgut microbiota, which permits proliferation of pathogenic microbes. The goal of this study was to evaluate the effects of common antibiotics on cellulolytic bacteria, lactobacilli, and AAD-associated pathogens in the feces of healthy horses. Fifteen horses were assigned to three treatment groups (blocked by age and sex): control (no antibiotics), trimethoprim-sulfadiazine (PO), or ceftiofur (IM). Fecal samples (n=8 pe...
England GC, Clarke KW, Goossens L.The sedative effects of a new alpha 2-adrenoceptor agonist, romifidine, were compared with those of xylazine and detomidine. Five horses were treated with two doses of romifidine (40 micrograms/kg body weight and 80 micrograms/kg body weight), two doses of detomidine (10 micrograms/kg body weight and 20 micrograms/kg body weight) and one dose of xylazine (1 mg/kg body weight) given by intravenous injection using a Latin-square design. The dose of 80 micrograms/kg romifidine appeared equipotent to 1 mg/kg xylazine and 20 micrograms/kg detomidine, although at these doses both xylazine and detomi...
Walshe N, Duggan V, Cabrera-Rubio R, Crispie F, Cotter P, Feehan O, Mulcahy G.The interactions between parasitic helminths and gut microbiota are considered to be an important, although as yet incompletely understood, factor in the regulation of immunity, inflammation and a range of diseases. Infection with intestinal helminths is ubiquitous in grazing horses, with cyathostomins (about 50 species of which are recorded) predominating. Consequences of infection include both chronic effects, and an acute inflammatory syndrome, acute larval cyathostominosis, which sometimes follows removal of adult helminths by administration of anthelmintic drugs. The presence of cyathosto...
England GC, Clarke KW.In recent years the usefulness of the alpha 2 adrenoceptor agonist drugs has been recognized in equine practice. Several agents have become available and are now licensed for use in a number of countries. The principle actions of all alpha 2 adrenoceptor agonists are similar, in that they produce a reduction in heart rate and alteration of heart rhythm, an initial hypertension followed by a prolonged hypotension, a decrease in the cardiac output and respiratory depression. For clinical purposes, these agents produce sedation and analgesia, they are useful for premedication and markedly potenti...
Cemazar M, Tamzali Y, Sersa G, Tozon N, Mir LM, Miklavcic D, Lowe R, Teissie J.Electropermeabilization is a method that uses electric field pulses to induce an electrically mediated reorganization of the plasma membrane of cells. Electrochemotherapy combines local or systemic administration of chemotherapeutic drugs such as bleomycin or cisplatin that have poor membrane permeability with electropermeabilization by direct application of electric pulses to the tumors. Preclinical studies have demonstrated excellent antitumor effectiveness of electrochemotherapy on different animal models and various tumor types, minimal toxicity, and safety of the procedure. Based on resul...
Rizk MA, El-Sayed SA, Terkawi MA, Youssef MA, El Said el Sel S, Elsayed G, El-Khodery S, El-Ashker M, Elsify A, Omar M, Salama A, Yokoyama N....A rapid and accurate assay for evaluating antibabesial drugs on a large scale is required for the discovery of novel chemotherapeutic agents against Babesia parasites. In the current study, we evaluated the usefulness of a fluorescence-based assay for determining the efficacies of antibabesial compounds against bovine and equine hemoparasites in in vitro cultures. Three different hematocrits (HCTs; 2.5%, 5%, and 10%) were used without daily replacement of the medium. The results of a high-throughput screening assay revealed that the best HCT was 2.5% for bovine Babesia parasites and 5% for equ...
Wang ZW, Nara M, Wang YX, Kotlikoff MI.The effects of sulfhydryl reduction/oxidation on the gating of large-conductance, Ca(2+)-activated K+ (maxi-K) channels were examined in excised patches from tracheal myocytes. Channel activity was modified by sulfhydryl redox agents applied to the cytosolic surface, but not the extracellular surface, of membrane patches. Sulfhydryl reducing agents dithiothreitol, beta-mercaptoethanol, and GSH augmented, whereas sulfhydryl oxidizing agents diamide, thimerosal, and 2,2'-dithiodipyridine inhibited, channel activity in a concentration-dependent manner. Channel stimulation by reduction and inhibit...
Chung DH, Jonsson CB, Tower NA, Chu YK, Sahin E, Golden JE, Noah JW, Schroeder CE, Sotsky JB, Sosa MI, Cramer DE, McKellip SN, Rasmussen L, White EL....Alphaviruses present serious health threats as emerging and re-emerging viruses. Venezuelan equine encephalitis virus (VEEV), a New World alphavirus, can cause encephalitis in humans and horses, but there are no therapeutics for treatment. To date, compounds reported as anti-VEEV or anti-alphavirus inhibitors have shown moderate activity. To discover new classes of anti-VEEV inhibitors with novel viral targets, we used a high-throughput screen based on the measurement of cell protection from live VEEV TC-83-induced cytopathic effect to screen a 340,000 compound library. Of those, we identified...
Stellingwerff T, Decombaz J, Harris RC, Boesch C.Interest into the effects of carnosine on cellular metabolism is rapidly expanding. The first study to demonstrate in humans that chronic β-alanine (BA) supplementation (~3-6 g BA/day for ~4 weeks) can result in significantly augmented muscle carnosine concentrations (>50%) was only recently published. BA supplementation is potentially poised for application beyond the niche exercise and performance-enhancement field and into other more clinical populations. When examining all BA supplementation studies that directly measure muscle carnosine (n=8), there is a significant linear correlation...
Lyons ET, Tolliver SC, Drudge JH.Small strongyles are highly prevalent in horses and can be found worldwide. Even though over 50 species of these parasites have been described, about 10 species comprise the bulk of the total number present in horses. Efforts to control small strongyles and other equine internal parasites have been undertaken for many years. Some of the early medications and control measures provided questionable activity against endoparasites; whether effective or not, they could be detrimental to the horse. Beginning in the early 1900s, scientific effort was used to evaluate activity of antiparasitic compoun...
Chotwiwatthanakun C, Pratanaphon R, Akesowan S, Sriprapat S, Ratanabanangkoon K.The purpose of this study was to prepare a potent polyvalent antivenom against three elapids namely, the Thai cobra (Naja kaouthia, NK), the King cobra (Ophiophagus hannah, OH) and the banded krait (Bungarus fasciatus, BF). Two groups of horses were immunized. Group 1, comprising five horses, was immunized twice with a mixture of postsynaptic neurotoxins followed by an additional six immunizations with a mixture of crude venoms of the three elapids. Group 2, comprising four horses, was immunized with a mixture of crude venoms throughout the course. For the first immunization, the immunogens we...
Bujacz A, Zielinski K, Sekula B.Serum albumin, a protein naturally abundant in blood plasma, shows remarkable ligand binding properties of numerous endogenous and exogenous compounds. Most of serum albumin binding sites are able to interact with more than one class of ligands. Determining the protein-ligand interactions among mammalian serum albumins is essential for understanding the complexity of this transporter. We present three crystal structures of serum albumins in complexes with naproxen (NPS): bovine (BSA-NPS), equine (ESA-NPS), and leporine (LSA-NPS) determined to 2.58 Å (C2), 2.42 Å (P61), and 2.73 Å (P2₁2₁...
Bullone M, Vargas A, Elce Y, Martin JG, Lavoie JP.Asthmatic airways are inflamed and undergo remodelling. Inhaled corticosteroids and long-acting β2-agonist combinations are more effective than inhaled corticosteroid monotherapy in controlling disease exacerbations, but their effect on airway remodelling and inflammation remains ill-defined. This study evaluates the contribution of inhaled fluticasone and salmeterol, alone or combined, to the reversal of bronchial remodelling and inflammation. Severely asthmatic horses (6 horses/group) were treated with fluticasone, salmeterol, fluticasone/salmeterol, or with antigen avoidance for 12 weeks. ...
Park J, Sutradhar BC, Hong G, Choi SH, Kim G.To compare the chondrotoxicity of bupivacaine, lidocaine, and mepivacaine in equine articular chondrocytes in vitro. Methods: Prospective, experimental study. Methods: Equine articular chondrocytes. Methods: Primary cultured equine chondrocytes were exposed to 0.5% bupivacaine, 2% lidocaine, or 2% mepivacaine for 30 or 60 minutes. After treatment, cell viability was evaluated by trypan blue exclusion and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay in a dose dependent manner. Apoptosis and necrosis of chondrocytes were analyzed with the double stain...
Oyarzun-Ampuero F, Vidal A, Concha M, Morales J, Orellana S, Moreno-Villoslada I.The treatment of skin wounds represents an important research area due to the important physiological and aesthetic role of this tissue. During the last years, nanoparticles have emerged as important platforms to treat skin wounds. Silver, gold, and copper nanoparticles, as well as titanium and zinc oxide nanoparticles, have shown potential therapeutic effects on wound healing. Due to their specific characteristics, nanoparticles such as nanocapsules, polymersomes, solid lipid nanoparticles, and polymeric nanocomplexes are ideal vehicles to improve the effect of drugs (antibiotics, growth fact...
Stock ML, Elazab ST, Hsu WH.Triazines are relatively new antiprotozoal drugs that have successfully controlled coccidiosis and equine protozoal myeloencephalitis. These drugs have favorably treated other protozoal diseases such as neosporosis and toxoplasmosis. In this article, we discuss the pharmacological characteristics of five triazines, toltrazuril, ponazuril, clazuril, diclazuril, and nitromezuril which are used in veterinary medicine to control protozoal diseases which include coccidiosis, equine protozoal myeloencephalitis, neosporosis, and toxoplasmosis.
Neuder LE, Keener JM, Eckert RE, Trujillo JC, Jones SL.Endotoxemia occurs when bacterial lipopolysaccharide (LPS) in the blood induces a dysregulated inflammatory response, resulting in circulatory shock and multi-organ failure. Laminitis is a common complication in endotoxemic horses and is frequently the reason for humane euthanasia of these cases. Blood leukocytes are a principal target of LPS in endotoxemia leading to activation of multiple signal transduction pathways involved in the induction of a number of pro-inflammatory genes. In other animal models, the p38 mitogen activated protein kinase (MAPK) pathway has been associated with induced...
Giles CJ, Urquhart KA, Longstaffe JA.Clinical and laboratory findings are recorded from a series of 15 cases (aged one to 16 years) of sudden-onset chronic diarrhoea with weight loss, progressing in many cases to emaciation and death, associated with the emergence of fourth stage cyathostome (trichoneme) larvae in large numbers through the colonic and caecal mucosae. Apart from a single incident in mid-October, disease only occurred in winter and spring (January to May). Characteristic features included hypoalbuminaemia, increased alpha and beta plasma globulin levels and neutrophilia without left shift. Faecal egg counts were fr...
Sykes BW, Sykes KM, Hallowell GD.A previous study demonstrated that a dose effect between 1.6 and 4.0 mg/kg bwt of omeprazole per os s.i.d. is present in the treatment of equine gastric ulceration. In the same study, healing of glandular ulceration appeared inferior to healing of squamous ulceration. However, several limitations were recognised in that study and further investigation is warranted. Objective: To further investigate the presence of a dose relationship in the treatment of gastric ulceration under conditions that may favour omeprazole efficacy such as administration prior to exercise and after a brief fast, and...
Chauret N, Gauthier A, Martin J, Nicoll-Griffith DA.As domestic animals such as cat, horse, and dog increasingly become the clinical targets for drug discovery programs, the need to understand how these animals metabolize xenobiotics becomes more important. In the present study, substrates and inhibitors that were reported to be selective for particular P450 isozymes were used as probes to study in vitro metabolism in horse, dog, cat, and human liver microsomes. Seven selective catalytic activity markers for cytochrome P450-mediated reactions were measured: phenacetin O-deethylase (P4501A1/2), coumarin 7-hydroxylase (P4502A6), tolbutamide hydro...
Fenton JI, Chlebek-Brown KA, Peters TL, Caron JP, Orth MW.Objective To determine whether glucosamine inhibits experimentally induced degradation of equine articular cartilage explants. Methods Articular cartilage was obtained from the antebrachio-carpal and middle joints of horses (2-8 years old) killed for reasons unrelated to lameness. Cartilage discs were harvested from the weight-bearing region of the articular surface and cultured. Media were exchanged daily and the recovered media stored at 4 degrees C. Explants were maintained in basal media 2 days prior to the start of four treatment days. On days 1-4 lipopolysaccharide (LPS, 10 microg/ml) or...
Zhao S, McDermott PF, White DG, Qaiyumi S, Friedman SL, Abbott JW, Glenn A, Ayers SL, Post KW, Fales WH, Wilson RB, Reggiardo C, Walker RD.Three hundred and eighty Salmonella isolates recovered from animal diagnostic samples obtained from four state veterinary diagnostic laboratories (AZ, NC, MO, and TN) between 2002 and 2003 were tested for antimicrobial susceptibilities and further characterized for bla(CMY) beta-lactamase genes, class 1 integrons and genetic relatedness using PFGE. Forty-seven serovars were identified, the most common being S. Typhimurium (26%), S. Heidelberg (9%), S, Dublin (8%), S. Newport (8%), S. Derby (7%), and S. Choleraesuis (7%). Three hundred and thirteen (82%) isolates were resistant to at least one ...
