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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.
On the search for in vitro in vivo correlations in the field of intra-articular drug delivery: administration of sodium diatrizoate to the horse. Development of suitable in vitro release models for formulation development as well as quality control purposes has to be initiated in the early design phase of injectable depots. Optimally, construction of an in vitro release model may lead to the establishment of in vitro in vivo correlations. By using a model compound (sodium diatrizoate, DTZ), the purpose of this study was to investigate the possibility of establishing in vitro in vivo relations between the DTZ disappearance profile obtained from the donor compartment of the rotating dialysis cell model and the joint disappearance profile ...
Determination of (13)C/(12)C ratios of urinary excreted boldenone and its main metabolite 5beta-androst-1-en-17beta-ol-3-one. Boldenone (androsta-1,4-dien-17beta-ol-3-one, Bo) is an anabolic steroid known to have been used in cattle breeding or equine sport as a doping agent for many years. Although not clinically approved for human application, Bo or its main metabolite 5beta-androst-1-en-17beta-ol-3-one (BM1) were detected in several doping control samples. For more than 15 years the possibility of endogenous Bo production in human beings has been discussed. This is a challenging issue for doping control laboratories as Bo belongs to the list of prohibited substances of the World Anti-Doping Agency and therefore th...
[Comparative efficacy of homologous and heterologous biologicals against diphtheria]. Comparative assessment of efficacy of homologous and heterologous diphtheria antitoxins on the example of diphtheria intoxication. Methods: Homologous hyperimmune sera were obtained through immunization of rabbits and guinea-pigs with diphtheria toxoid according to schedule. Immune rabbit sera contained 70 - 100 IU/mL of antitoxin antibodies and guinea-pig sera contained 60 - 80 IU/mL. Equine diphtheria antitoxin was used as a heterologous one. Measurement of antitoxin level using experimental animals is based on quantitative assessment of ability of studied sera to neutralize specific dermone...
Partial intravenous anaesthesia in 5 horses using ketamine, lidocaine, medetomidine and halothane. A partial intravenous protocol was used successfully to maintain anaesthesia in 5 healthy horses. Horses were premedicated with acepromazine, romifidine and butorphanol, induced with guaifenesin and ketamine and maintained on a constant rate infusion of lidocaine, ketamine and medetomidine together with halothane inhalation anaesthesia. Mean end-tidal halothane concentration to maintain a surgical plane of anaesthesia was 0.8 +/- 0.2%. Mean dobutamine requirement to maintain mean arterial pressure above 9.31 kPa was 0.42 +/- 0.3 microg/kg/min. The administration of relatively low doses of lido...
Tachypnea and antipyresis in febrile horses after sedation with alpha-agonists. Signs of tachypnea after sedation of febrile horses with alpha2-agonists have been noted previously but have not been further investigated. Objective: To examine the effects of xylazine and detomidine on respiratory rate and rectal temperature in febrile horses and to investigate if either drug would be less likely than the other to cause changes in these variables. Methods: Nine febrile horses and 9 healthy horses were included in the study. Methods: Horses were randomly assigned to sedation with xylazine 0.5 mg/kg or detomidine 0.01 mg/kg. Heart rate and respiratory rate were recorded before...
Concentrations of altrenogest in plasma of mares and foals and in allantoic and amniotic fluid at parturition. Treatment with the progestin altrenogest is widely used in pregnant mares. The fact that foals born from healthy mares treated with altrenogest until term suffered from neonatal problems raises the question of direct effects of altrenogest on vital functions in the neonate. We have therefore investigated altrenogest concentrations in maternal and neonatal blood plasma and in fetal fluids. Pregnant mares were treated with altrenogest orally once daily (0,088 mg/kg bodyweight, n = 7) or left untreated (n = 8) from 280 d of gestation until foaling. Altrenogest concentration was determined in plas...
In vivo administration of acepromazine or promethazine to horse decreases the reactive oxygen species production response of subsequently isolated neutrophils to stimulation with phorbol myristate acetate. The previous experiments have shown that some phenothiazines have antioxidant and anti-inflammatory properties in vitro. In this study the inhibition of the production of reactive oxygen species (ROS) by neutrophils was studied in two groups of horses, which received a dose of 0.1 mg/kg of either acepromazine or promethazine intravenously. Blood samples were collected before (T0) and 0.5, 1, 3 and 5 h after drug administration. The chemiluminescence (CML) response of neutrophils was measured ex vivo in the presence of luminol for a period of 10 min and the maximum CML value (peak value) record...
Distribution of voriconazole in seven body fluids of adult horses after repeated oral dosing. The purpose of this study was to assess safety and alterations in body fluid concentrations of voriconazole in normal horses on days 7 and 14 following once daily dose of 4 mg/kg of voriconazole orally for 14 days. Body fluid drug concentrations were determined by the use of high performance liquid chromatography (HPLC). On day 7, mean voriconazole concentrations of plasma, peritoneal, synovial and cerebrospinal fluids, aqueous humor, epithelial lining fluid (ELF), and urine were 1.47 +/- 0.63, 0.61 +/- 0.22, 0.70 +/- 0.20, 0.62 +/- 0.26, 0.55 +/- 0.32, 79.45 +/- 69.4, and 1.83 +/- 0.44 microg...
Aqueous humor and plasma concentrations of ciprofloxacin and moxifloxacin following topical ocular administration in ophthalmologically normal horses. To determine the degree of ocular penetration and systemic absorption of commercially available topical ophthalmic solutions of 0.3% ciprofloxacin and 0.5% moxifloxacin following repeated topical ocular administration in ophthalmologically normal horses. Methods: 7 healthy adult horses with clinically normal eyes as evaluated prior to each treatment. Methods: 6 horses were used for assessment of each antimicrobial, and 1 eye of each horse was treated with topically administered 0.3% ciprofloxacin or 0.5% moxifloxacin (n = 6 eyes/drug) every 4 hours for 7 doses. Anterior chamber paracentesis wa...
Evaluation of the effect of phosphodiesterase on equine platelet activation and the effect of antigen challenge on platelet phosphodiesterase activity in horses with recurrent airway obstruction. To determine whether expression of equine platelet activation-dependent surface markers is influenced by phospodiesterase (PDE) isoenzyme activity and whether antigen challenge alters platelet PDE activity in horses with recurrent airway obstruction (RAO). Methods: 16 horses. Methods: 7 healthy horses were used for in vitro experiments, 6 horses with RAO were used for antigen challenge, and 6 healthy horses were used as control animals. Three of the healthy horses had also been used in the in vitro experiments. Effects of PDE inhibition and activation of adenylyl cyclase on CD41/61 and CD62P e...
Administration of perioperative penicillin reduces postoperative serum amyloid A response in horses being castrated standing. To compare postoperative inflammatory responses in horses administered perioperative procaine penicillin and those not administered penicillin using acute phase protein serum amyloid A (SAA) as a marker of inflammation. Methods: Randomized clinical trial. Methods: Stallions (n=50) castrated under field conditions. Methods: SAA concentrations were determined on days 0, 3, and 8. Six horses were subsequently excluded because of elevated SAA concentrations on day 0. Of the remaining 50 horses, 26 were administered nonsteroidal anti-inflammatory drug (NSAID) therapy and 24 were administered NSAID ...
Are macrocyclic lactones useful drugs for the treatment of Parascaris equorum infections in foals? A study was carried out to assess the field efficacy of moxidectin (MOX) against Parascaris equorum in foals. A total of 70 foals from 2 Italian thoroughbred (Farms 1 and 2) stud farms and one trotter stud farm (Farm 3), aged 3-5 months and with faecal egg counts (FEC) f>or=300 eggs per gram (EPG) were included in the study. On each farm, foals were divided into 2 groups (of 10, 8 and 10 foals, respectively) and treated with either moxidectin (MOX, 400 mcg/kg b.w.) or ivermectin (IVM, 200 mcg/kg b.w.) on day 0 and examined for faecal count reduction (FECR) on day 14. Five, 4 and 5 foals, re...
Treatment efficacy of trimethoprim sulfamethoxazole, pentoxifylline and altrenogest in experimentally induced equine placentitis. The objective was to determine if long-term treatment with trimethoprim sulfamethoxazole (antimicrobial), pentoxifylline (anti-inflammatory/anti-cytokine) and altrenogest (synthetic progestin), would improve pregnancy outcome in mares with experimentally induced placentitis. Seventeen normal, pregnant pony mares were enrolled in the study at 280-295 d of pregnancy. Placentitis was induced in all mares by intra-cervical inoculation of Streptococcus equi subsp. zooepidemicus (10(7) CFU). Five mares served as infected, untreated control animals (Group UNTREAT). Twelve mares (Group TREAT) were inf...
Type 2 diabetes mellitus with pancreatic beta cell dysfunction in 3 horses confirmed with minimal model analysis. Type 2 diabetes mellitus (T2DM) is diagnosed rarely in equine practice although it may be under-recognised. A greater awareness of the condition and therapeutic considerations would be to the benefit of such cases presenting in practice. More investigation into the pharmacological management of these cases is needed. Objective: Three cases of diabetes mellitus were investigated using a specific test for insulin sensitivity and pancreatic beta cell function in order to define accurately and characterise the existence of T2DM in all 3 subjects. Methods: The insulin-modified frequently sampled i....
The pharmacologic basis for the treatment of developmental and acute laminitis. The treatment of laminitis has been fraught with confusion and controversy for several decades, mainly because of a lack of understanding of the pathophysiology of the disease process. However, recent advances in laminitis research have greatly improved our understanding of the disease process. This article discusses the various treatment options for laminitis in the context of the findings of recent scientific investigations of laminitis pathophysiology.
Fecal microbiota of horses in the clinical setting: potential effects of penicillin and general anesthesia. Antimicrobial treatment is associated with the spread of antimicrobial resistance and disturbances in the ecological balance of intestinal microbiota. In horses, the main adverse effect of antimicrobial treatment is colitis. We used culture and 16S rRNA gene based molecular methods to monitor the prevalence of antimicrobial resistance and changes in predominant fecal populations during penicillin treatment and general anesthesia of horses in the clinical setting. After 5 days of parenteral administration of penicillin, fecal Escherichia coli were resistant to multiple unrelated antimicrobial a...
Determination of ivermectin efficacy against cyathostomins and Parascaris equorum on horse farms using selective therapy. Ivermectin resistance has recently been described in Parascaris equorum and there have been reports from several countries of a shortened egg reappearance period (ERP) following ivermectin treatment for cyathostomins. This study was aimed at determining the efficacy of ivermectin in treating cyathostomins and P. equorum in Danish horses. A total of 196 animals were selected from 52 farms, all of which were using a selective anthelmintic treatment strategy. ERP was investigated with weekly samples from 96 horses from nine farms. Horses were treated with ivermectin oral paste by their owners at ...
Cell entry of the aphthovirus equine rhinitis A virus is dependent on endosome acidification. Equine rhinitis A virus (ERAV) is genetically closely related to foot-and-mouth disease virus (FMDV), and both are now classified within the genus Aphthovirus of the family Picornaviridae. For disease security reasons, FMDV can be handled only in high-containment facilities, but these constraints do not apply to ERAV, making it an attractive alternative for the study of aphthovirus biology. Here, we show, using immunofluorescence, pharmacological agents, and dominant negative inhibitors, that ERAV entry occurs (as for FMDV) via clathrin-mediated endocytosis and acidification of early endosomes...
Effects of intravenous fentanyl administration on end-tidal sevoflurane concentrations in thoroughbred racehorses undergoing orthopedic surgery. To evaluate the effects of IV fentanyl administration on the end-tidal sevoflurane concentration (ET(SEVO)) in thoroughbred racehorses, the ET(SEVO) required for internal fixation of longitudinal fractures was compared between horses anesthetized with sevoflurane-fentanyl (Group SF; n=9) and those anesthetized with sevoflurane alone (Group S; n=9). The loading dose of fentanyl (5.0 µg/kg) was administered over 15 min followed by a maintenance dose of fentanyl (0.1 µg/kg/min) throughout the operation in Group SF. The mean ET(SEVO) during the operation in Group SF (2.6 ± 0.2%) was significant...
Comparison between horse and rabbit antithymocyte globulin as first-line treatment for patients with severe aplastic anemia: a single-center retrospective study. The best antithymocyte globulin preparation for first-line immune suppression in patients with severe aplastic anemia is still not clear. The aim of this study was to compare hematological response and overall survival in patients submitted to horse or rabbit antithymocyte globulin as first-line treatment for severe aplastic anemia. We retrospectively compared 71 consecutive patients with severe aplastic anemia, classified according to the antithymocyte globulin preparation. Analyses included variables related to patients and to immune suppression. Forty two patients (59.1%) received horse and...
Efficacy of Cymelarsan and Diminasan against Trypanosoma equiperdum infections in mice and horses. Trypanocidal sensitivity studies were conducted to assess the efficacy of Diminazene diaceturate (Diminasan) and Bis (aminoethylthio) 4-melaminophenylarsine dihydrochloride (Cymelarsan) against Trypanosoma equiperdum (isolated from two mares with chronic cases of dourine) 713/943 and 834/940 Dodola strains in experimentally infected mice and horses. Diminasan at doses from 3.5 mg/kg to 28 mg/kg and Cymelarsan at doses of 0.25 mg/kg and 0.5 mg/kg body weight failed to cure any of the mice, indicating a clear dose dependent relationship in the mean time of relapse observed in mice. Indeed, mice ...
Rho kinase activation and ROS production contributes to the cooling enhanced contraction in cutaneous equine digital veins. A decrease in environmental temperature can directly affect the contractility of cutaneous vasculature, mediated in part by alpha(2)-adrenoceptors. Most of the cellular mechanisms underlying the cooling-enhanced contractility to alpha(2)-adrenoceptor agonists have been reported in cutaneous arteries but little information is available on cutaneous veins. To investigate the cellular mechanisms associated with the cooling-enhanced contraction to UK-14304 (alpha(2)-adrenoceptor agonist), isolated equine digital veins (EDVs) were studied at 30 degrees C and 22 degrees C. The effects of inhibitors ...
[A survey on anthelmintic resistance in Strongyles to ivermectin and pyrantel and macrocyclic lactone-resistance in Parascaris equorum]. This survey was carried out on a horse farm in order to acquire recent data on macrocyclic lactone-resistant Parascaris equorum which had been previously detected on this farm and to determine efficacies of ivermectin and pyrantel against strongyles in order to determine whether a resistance problem also exists in these parasites. In the first part of the study, abamectin was given to horses infected with P. equorum. In 11 out of 12 horses, zero efficacy (0%) was seen against P. equorum. Subsequently, horses which were Parascaris-positive after abamectin treatment received pyrantel pamoate and...
Endotoxin-induced HIF-1alpha stabilisation in equine endothelial cells: synergistic action with hypoxia. Hypoxia may enhance the deleterious effects of lipopolysaccharide (LPS) in the endotoxaemic horse. This study has examined some of the actions of LPS and hypoxia, alone and in combination, on cultured equine digital vein endothelial cells (EDVEC) and the signalling molecules involved. Methods: EDVEC were exposed to LPS, 5% O(2) and LPS then 5% O(2) for up to 24 h. HIF-1alpha stabilisation, neutrophil adhesion and EDVEC permeability were assessed by immunoblotting, measurement of myeloperoxidase and movement of FITC-dextran, respectively. Pharmacological inhibitors were used to assess the roles...
Effects of adding butorphanol to a balanced anaesthesia protocol during arthroscopic surgery in horses. Three groups of horses scheduled for arthroscopic surgery were premedicated with 0.025 mg/kg acepromazine, 88 microg/kg romifidine and 25 mg/kg guaifenesin, and anaesthesia was induced with 2.2 mg/kg ketamine. In group 1 (14 horses), anaesthesia was maintained by halothane vaporised in oxygen, with supplementary doses of 20 microg/kg romifidine and 0.5 mg/kg ketamine every 20 minutes. The 17 horses in group 2 were maintained as for group 1; however, an additional dose of 0.05 mg/kg butorphanol was administered before the first incision. The 14 horses in group 3 were maintained as for group 2, ...
Depletion of urinary zilpaterol residues in horses as measured by ELISA and UPLC-MS/MS. Three horses were dosed with dietary zilpaterol and the urine concentrations measured from withdrawal day 0 to withdrawal day 21. The analyses were carried out using both enzyme-linked immunosorbent assay (ELISA) and an ultraperformance liquid chromatography with triple-quadrupole-tandem mass spectrometric detection (UPLC-MS/MS). The UPLC-MS/MS method was developed to provide rapid analysis with positive analyte identification by following three product ions and computing the two independent ion ratios. When urinary zilpaterol concentrations were between 0.2 and 2 ng/mL, the ELISA had interday...
Efficacy of pyrantel pamoate against a macrocyclic lactone-resistant isolate of Parascaris equorum in horses. The expanding prevalence of Parascaris equorum populations that are resistant to macrocyclic lactone (ML) anthelmintics makes it desirable to identify dewormers which remain effective. The objective was to evaluate the efficacy of pyrantel pamoate in 14 suckling foals that had been infected orally with approximately 600 larvated eggs of a P. equorum isolate selected for ML resistance (ML-R). Seventy days after inoculation, foals were weaned, housed individually, and fecal samples were examined frequently to detect the onset of patency. Between 73 and 80 days post-inoculation, all 14 foals deve...
Efficacy of pyrantel pamoate and ivermectin paste formulations against naturally acquired Oxyuris equi infections in horses. In recent years, numerous veterinary practitioners have reported anecdotal episodes in which anthelmintic treatment did not appear to deliver the expected efficacy against equine pinworms (Oxyuris equi). Anthelmintic resistance has not been demonstrated formally in equine pinworms, so a clinical study was designed to evaluate the efficacy of paste formulations of pyrantel pamoate or ivermectin against naturally acquired infections with O. equi. Twenty-one horses (>4 months to 15 years of age) with patent, naturally acquired pinworm infections were blocked by source of origin and allocated rand...
