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.
Thijssen HH, van den Bogaard AE, Wetzel JM, Maes JH, Muller AP.The pharmacokinetics of racemic warfarin were studied in 6 adult horses. After IV administration, the plasma concentration of warfarin showed a biphasic decline in time. Analysis of the data, according to 2-compartment kinetics, revealed the following constants: biological half-life was 13.3 hours, apparent volume of distribution was 0.46 L X kg-1, body clearance was 25.3 ml X hour-1 X kg-1. Warfarin was bound (91.5%) to plasma proteins. Unchanged warfarin was not detected in the urine. Absorption from the gastrointestinal tract was almost complete. Concentrations of warfarin in tissue were ex...
Taylor JB, Walland A, Lees P, Gerring EL, Maitho TE, Millar JD.Five pairs of matched horses were used to study the biochemical and haematological effects of a revised dosage schedule of phenylbutazone. One group of five horses received a phenylbutazone paste formulation daily for 12 days and a second group of five animals received a placebo preparation for a similar time. Some statistically significant differences were recorded from pretreatment levels in both groups of horses. These changes represented instability in baseline levels and could not be ascribed to phenylbutazone administration.
Snow DH, Douglas TA.The absorption characteristics of a new paste preparation of phenylbutazone were studied in ponies and thoroughbreds. The results suggested that at a similar dose rate of 5 mg/kg greater bioavailability results from the paste than from a powder preparation. Delivery of an accurate dosage of the paste was not possible using the multidose applicator. Repeated administration of the paste preparation (5 mg/kg twice daily) indicated that it is more toxic to both ponies and thoroughbreds than a powder preparation. In addition to the toxic manifestations previously reported, a neutropenia developed d...
Harrington DD, Page EH.Acute vitamin D toxicosis was diagnosed in 2 horses fed a grain ration containing 1,102,311 IU of cholecalciferol (vitamin D3)/kg (500,000 IU/lb) for about 30 days. Horse 1 died acutely with extensive mineralization of cardiovascular and other soft tissues. Horse 2, which had severe clinical signs and clinicopathologic changes of toxicosis, was treated with nonsteroidal antiinflammatory drugs and recovered in about 6 months. In an experimental study, the toxicity of ergocalciferol (vitamin D2) and cholecalciferol was compared in 2 horses (No. 3 and 4) given the respective vitamins at a daily d...
Parry BW, Anderson GA.The effect of acepromazine maleate (ACP) on the equine venous haematocrit and total plasma protein concentration was studied in six clinically normal horses. Total plasma protein concentration was not appreciably influenced by ACP. However, the haematocrit decreased with the duration, but not the degree, of the decrease being dose-related. Mean haematocrit values returned to control levels by 12 h after 0.05 mg ACP/kg body weight and 21 h after 0.15 mg ACP/kg body weight.
Howey WP, Jochle W, Barnes WJ.Alfaprostal (K 11941), a novel prostaglandin F2 alpha analogue was clinically tested in 24 dioestrous mares, 40 anoestrous mares and 31 postpartum mares, all being given 2 or 3 mg intramuscularly. Blood samples were taken for the determination of plasma progesterone levels and the objective confirmation of luteolytic drug effects. Two hundred and thirty-six mares at the same location were used for comparisons of the rates of pregnancy, early embryonic loss and foaling. Alfaprostol was found to act as a potent luteolytic agent with good oestrus induction, follicular development and normal conce...
Suquet CM, Leid RW.Platelet-activating factor (PAF), a lipid released as a result of immediate allergic reactions from basophils and mast cells as well as by a variety of other cell types and stimuli, is one of the most potent platelet agonists and hypotensive agents known. Equine platelets stimulated over a wide range of PAF concentrations aggregated in a time- and dose-dependent manner. Maximum aggregation was observed at concentrations of PAF as low as 3.58 x 10(-14) M with platelet-rich plasma (PRP) and 3.58 x 10(-16) M with washed platelets. Furthermore, the aggregation observed did not appear to be breed-d...
Kowalczyk DF, Beech J.The pharmacokinetics of the anti-convulsant phenytoin were investigated in clinically healthy horses after oral (p.o.) and intravenous (i.v.) administration. A single dose of phenytoin (8.8 mg/kg body weight) was given i.v. as a bolus to nine horses and one horse received 13.2 mg/kg. A two-compartment open model was used to describe the disposition of phenytoin. Four of the horses that received an i.v. dose (three at 8.8 mg/kg and one at 13.2 mg/kg) were then given the same dose 3 days later by the oral route. Phenytoin achieved a peak concentration in serum within 1-4 h after p.o. administrat...
DiPietro JA, Paul A, Todd KS.Forty horses from a herd known to have benzimidazole-resistant small strongyles were treated with mebendazole (8.8 mg/kg) or combinations of mebendazole and piperazine monohydrochloride (25, 40, or 55 mg of piperazine base/kg). Pretreatment and 7-day posttreatment fecal examinations were done. Fecal cultures and strongyle egg per gram (epg) counts, and in vitro testing for benzimidazole resistance were performed. Results of fecal examinations prior to treatment were similar in all horses, and results of testing were positive for benzimidazole resistance. Horses treated with mebendazole and pip...
Davies JV, Gerring EL.The effect of acepromazine, Buscopan (Crown Chemicals), pethidine and methadone was evaluated in ponies prepared with Thiry-Vella (T-V) loops. Motility was assessed by electrophysiological means (bipolar electrodes and strain gauge transducers) and by the passage through the T-V loop of a fluid test meal. Results were obtained from 26 experiments in three ponies and compared with six control experiments, in which saline had been administered to the same ponies. Each pony acted as its own control in each experiment and pre and post treatment values for slow wave frequency, spiking activity, del...
Chay S, Woods WE, Rowse K, Nugent TE, Blake JW, Tobin T.Studies were undertaken to determine blood levels of furosemide in horses after 0.5- and 1.0-mg/kg doses administered iv. Analyses indicated that the pharmacokinetic parameters were dose independent and best described by a three-compartment open model. The alpha-, beta-, and gamma-phase half-lives of 5.6, 22.3, and 158.5 min, respectively, were observed after the 0.5-mg/kg dose. Similarly, the respective half-lives after the 1.0-mg/kg dose were 5.8, 24.1, and 177.2 min. After a 0.5-mg/kg dose of furosemide, population frequency distributions were evaluated at 1 hr and 4 hr post-drug administra...
Nádasdi L, Yamashiro D, Li CH, Izdebski J.Five analogs of equine β-melanotropin have been synthesized by the solid phase method. The NH2-terminal aspartic acid was substituted with amino acids (Gly, Trp, Ile, Lys and Nα-acetyl-Asp) differing widely in physicochemical properties. On the basis of their lipolytic potencies it was concluded that this position plays a negligible role in this activity.
Ralston JS, Main AR, Kilpatrick BF, Chasson AL.Two large-scale methods based primarily on the use of procainamide-Sepharose gels were developed for the purification of horse and human serum non-specific cholinesterases. With method I, the procainamide-Sepharose 4B gel was used in the first step to handle large volumes of serum. With method II, the procainamide-Sepharose 4B gel was used in the final step to obtain pure enzyme. Although both methods gave electrophoretically pure cholinesterase preparations in good yields, they were significantly more efficient at purifying the horse enzyme than the human enzyme. To study this problem, the re...
Glade MJ, Krook L, Schryver HF, Hintz HF.Epiphyseal and articular cartilages were examined in pony foals treated with intramuscular injections of either 0.5 mg dexamethasone per 100 kg bodyweight daily for 3, 8 or 11 months, or 5.0 mg per 100 kg for 11 months, and in horse foals treated with 5.0 mg per 100 kg for 20 weeks. The proximal femoral growth plates exhibited increased spatial separation between chondrocyte columns, narrowed zones of disorganized columnar and hypertrophic cartilage, abnormal penetration of hypertrophic cartilage by metaphyseal capillaries, retained cartilage in the spongiosa, distal terminal plate formation, ...
Johnstone IB.Nonsteroidal anti-inflammatory drugs are commonly used in the treatment of inflammatory conditions, and have potential value in the treatment of thrombotic disease in the horse. This study compares the potency of three nonsteroidal anti-inflammatory drugs phenylbutazone, naproxen (equiproxen) and flunixin meglumine (banamine) with respect to their effects on equine platelets. Two functional responses of horse platelets were evaluated in vitro: their ability to aggregate and their ability to make available platelet factor 3 procoagulant activity. Flunixin at a concentration of 10(-6) M signific...
Moore CP, Fales WH, Whittington P, Bauer L.Gram-negative bacteria were the most common microbial isolates from 38 eyes of 37 horses with ulcerative keratitis. Pseudomonas sp, Enterobacter group, and Acinetobacter sp were the most prevalent. Fungi were cultured from 15 eyes and included 7 genera, with Aspergillus sp being the most prevalent. Ten of the eyes with fungal keratitis had been treated with corticosteroids. Eleven of 38 eyes had mixed bacterial and fungal infections. Clinically, the most severe cases were those in which Aspergillus and gram-negative bacteria existed in a mixed infection. On the basis of susceptibility testing,...
Brimijoin S, Mintz KP, Prendergast FG.Interactions between dansylarginine N-(3-ethyl-1,5-pentanediyl)amide (DAPA) and the cholinesterases were examined by the techniques of enzyme kinetics and fluorescence spectroscopy. When tested with partially purified enzyme preparations, DAPA was a potent inhibitor of butyrylcholinesterase (IC50 = 2 x 10(-7) M) but not of acetylcholinesterase (IC50 = 4 x 10(-4) M). For a detailed study of the effects of DAPA on butyrylcholinesterase (BuChE), the enzyme was purified to homogeneity from horse serum, with the aid of affinity chromatography on N-methyl acridinium. The kinetics of the inhibition o...
Slone DE, Purohit RC, Ganjam VK, Lowe JL.Three ponies and 1 horse were bilaterally adrenalectomized (BADX). The initial hypoadrenal episode after BADX was reversed with 20 mg of dexamethasone (DXM) IM (n = 2) or 20 mg of triamcinolone (TMC) IM (n = 2). Nine hypoadrenal crises were reversed with 20 mg of DXM given IM (n = 4) or 20 mg of TMC given IM (n = 5). Sodium and chloride retention and potassium excretion were documented based on changes in serum electrolytes and urinary excretion. Eight intact adult horses were randomly assigned to 2 groups to study the effects of a single IM injection of DXM (0.044 mg/kg of body weight) or TMC...
Ducharme NG, Fubini SL.Atropine sulfate was given at 2 dosages (0.044 mg/kg, 0.176 mg/kg) to clinically normal ponies in order to evaluate the drug's effect on the gastrointestinal tract. Intestinal motility, as assessed by ausculation of borborygmus, was stopped 30 minutes after injection, but it gradually returned to normal within 12 hours. Signs of abdominal pain developed in 3 of 10 ponies. In 3 clinical cases of gastrointestinal disorder, prior atropine treatment was confusing to the diagnostician and resulted in delayed surgical treatment in 1 case. It was concluded that atropine should not be used for allevia...
Threlfall WR, Keefe TJ.Serum levels of ticarcillin disodium, a semi-synthetic penicillin (Beecham Laboratories, Bristol, Tennessee, 37620), were measured at various time intervals up to and including 24 h after intrauterine and intramuscular administration in adult female horses. Three separate studies were conducted in Part I: in the first and second studies, serum levels were measured after intrauterine administration of 1 and 3 g of ticarcillin, respectively, and in the third study, levels were measured after intramuscular administration of 6 g of ticarcillin. In Part II, serum levels of ticarcillin were measured...
Ludwig KG, Craig TM, Bowen JM, Ansari MM, Ley WB.Twenty-eight foals whose dams were treated IM with ivermectin (200 micrograms/kg of body weight) on the day of parturition were compared with 35 foals whose dams were administered only the vehicle. The effect of ivermectin on the vertical transmission of Strongyloides westeri and foal heat diarrhea was determined by a comparison of results obtained in the 2 groups. Foals from treated mares had significantly fewer S westeri eggs per gram of feces from 17 to 28 days postpartum. There were no differences observed in the frequencies of severity of foal heat diarrhea between the treated and control...
Guerrero J, Michael BF, Rohovsky MW, Campbell BP.Eighteen pony foals were experimentally infected with 500 third stage larvae of Strongylus vulgaris at 2 weeks, and at 2, 4, 6 and 8 months after birth. For the duration of the study, all foals were kept in the same pasture with their mothers to allow natural infection with other parasites by exposure to a contaminated environment. Twelve of the foals were utilized in groups of 3 and treated orally five times at two month intervals starting at one month of age with closantel at doses of 5, 10, 20 or 40 mg kg-1. Ten months after birth the foals were necropsied to determine the parasitic burdens...
Sandbaumhüter FA, Vimercati S, Thormann W, Mevissen M.The anesthetic ketamine is often combined with analgesics and benzodiazepines in equine medicine. Therefore, drug-drug interactions are possible. Enzyme kinetics for ketamine N-demethylation were determined using equine CYP3A94, CYP3A95 and CYP3A97, and the effect of medetomidine, diazepam and methadone on the ketamine metabolism was studied in vitro. Ketamine was incubated with the CYPs or equine liver microsomes (ELM) alone or in presence of medetomidine, diazepam and/or methadone for different times. Norketamine levels were determined using enantioselective capillary electrophoresis (CE) wi...
Marshall JF, Bhatnagar AS, Bowman SG, Morris NN, Skorich DA, Redding CD, Blikslager AT.Flunixin meglumine is used for treatment of equine colic despite evidence of inhibited recovery of mucosal barrier function following small intestinal ischaemic injury. This study aimed to characterise an alternative treatment (AHI-805) for abdominal pain in the horse. Objective: To determine the effect of AHI-805, an aza-thia-benzoazulene derivative, on the cyclooxygenase enzymes and the recovery of mucosal barrier function following ischaemic injury. Methods: Effect of AHI-805 on in vitro COX-1 and COX-2 activity was determined by measuring coagulation-induced thromboxane B(2) (TXB(2)) and l...