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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.
The pharmacokinetics, pharmacological responses and behavioral effects of acepromazine in the horse. After intravenous (i.v.) injection, acepromazine was distributed widely in the horse (Vd = 6.6 litres/kg) and bound extensively (greater than 99%) plasma proteins. Plasma levels of drug declined with an alpha half-life of 4.2 min, while the beta phase or elimination half-life was 184.8 min. At a dosage level of 0.3 mg/kg acepromazine was detectable in the plasma for 8 h post dosing. The whole blood partitioning of acepromazine was 46% in the plasma phase and 54% in the erythrocyte phase. Penile prolapse was clearly evident at doses from 0.01 mg/kg to 0.4 mg/kg i.v., and the duration and extent...
Effects of enkephalins versus opiates on locomotor activity of the horse. The enkephalins are small, pentapeptide neurotransmitter molecules which have reportedly been used in racing horses. In our experiments, D-Ala2-Metenkephalinamide and leucine enkephalin were administered to horses intravenously (IV) and intracisternally (IC). Leucine enkephalin had little effect on locomotor activity by either route at doses of 0.01 mg/Kg or less. Methionine enkephalinamide, an enzyme resistant enkephalin analog, had no significant effect when given IV (0.002 and 0.008 mg/kg). Other experiments involving intracisternal dosing with this long acting form at higher levels (0.005-...
Controlled tests of fenbendazole against migrating Strongylus vulgaris in ponies. Sixteen pony foals were reared worm-free and inoculated with Strongylus vulgaris. On day 7 after inoculation, 12 ponies were given a fenbendazole 10% suspension at dose rate of 50 mg/kg of body weight by stomach tube. On day 8 after inoculation, 8 of these ponies were given the 2nd treatment of the anthelmintic and on day 9, 4 of these ponies were given the 3rd treatment. (The other 4 of the 16 ponies were given only tap water, as controls.) The ponies were necropsied at death or on day 28 after inoculation. Fenbendazole was effective in minimizing the appearance of clinical signs associated w...
Purification of horse eosinophil peroxidase. Eosinophil peroxidase (donor: hydrogen-peroxidase oxidoreductase, EC 1.11.1.7) was isolated in a highly purified form (415/280 nm ratio, 1.05) from horse peripheral blood eosinophil. Eosinophil peroxidase was extracted from intact eosinophils (98-100% purity) or isolated eosinophil granules with 0.05 M acetate buffer (pH 4.7)/0.18 M NaCl and purified by chromatography on Sephadex G-200 and carboxymethylcellulose. Final elution was with 0.05 M acetate buffer (pH 4.7)/ 1 M NaCl. Horse eosinophil peroxidase is a strongly basic protein with bacterial properties when combined with H2O2 and iodide, ...
Forelimb tic in a horse. An 18-month-old male Quarter Horse was referred for evaluation of a tic that had started after injury to the right forelimb 4 weeks earlier. The right forelimb appeared paretic and had constant regular twitches of variable intensity that were usually sufficiently forceful to move the trunk, neck, and head. The horse frequently threw the limb forward. The twitch persisted during sleep but disappeared during general anesthesia and following sedation with xylazine. It was unaffected by acetylpromazine, diphenylhydantoin, diazepam, carbamazepine, trimethadione, procainamide, quinidine, propranolol...
Effect of diethylcarbamazine on Strongylus vulgaris infection in ponies. Shetland ponies (n = 4) were given diethylcarbamazine orally at a dose level of 22 mg/kg/day for 1 week before they were inoculated with 800 third-stage larvae of Strongylus vulgaris. Treatment was continued for 86 (1 pony) or 200 days (3 ponies) after the inoculation. As compared with the changes seen in a similarly inoculated group of ponies (group 2) which were not treated, diethylcarbamazine did not prevent the clinical or pathologic changes due to the migrating larvae. Fewer adult parasites were recovered at necropsy from treated ponies than from nontreated (group 2) ponies, even when tre...
Systemic d-phenylalanine and d-leucine for effective treatment of pain in the horse. This study showed that subcutaneous injection of a solution of D-amino acids produced effective analgesia in horses. It is postulated that systemic D-phenylalanine and D-leucine may become one of the safe, effective and nonaddictive drugs for acute and chronic pain treatment. These D-amino acids cause analgesia by presumably preserving brain endorphins. They may bind reversibly to enkephalinases and prevent enzymatic degradation of enkephalins.
A comparison of agents for inducing parturition in mares in the pre-viable and premature periods of gestation. Various regimens of prostaglandins, alone or followed by oxytocin, were given to induce parturition in mares during the pre-viable and premature periods of gestation and in near-term mares. The most successful method of induction was found to be 2 i.m. injections of 500 micrograms fluprostenol (Equimate: I.C.I.) at a 2-h interval followed (if necessary) by 10-20 i.u. oxytocin injected i.v. in 5 i.u. serial increments every 15-20 min. Peak concentrations of the prostaglandin metabolite (PGFM) in response to the inducing agents were shown to be associated with delivery at, but not before, 320 da...
Glucocorticoid suppression of oestrus, follicles, LH and ovulation in the mare. Dexamethasone, a synthetic glucocorticoid, was administered (30 mg/day) from Day 10 after ovulation to assess the involvement of the adrenal glands in the ovulatory cycle. Only 1 of 8 mares treated in this way exhibited behavioural oestrus, compared to 7 of 8 control mares. Mean maximum LH concentration and follicle size were significantly reduced. Ovulation occurred in 1 and possibly in 2 other treated mares, compared to all 8 control mares. The results demonstrated that dexamethasone can interfere with ovulation and associated events in the mare, but the mechanism of action is uncertain.
Anthelmintic efficacy of ivermectin given intramuscularly in horses. The anthelmintic activity of ivermectin was evaluated in 18 female horses with naturally acquired parasitic infections. Horses were treated once (IM) with vehicle only (n = 6), 200 microgram/kg of body weight (n = 6), and 300 microgram/kg (n = 6). Efficacy of both dosages of ivermectin was greater than 99% against Gasterophilus spp, 100% against Trichostrongylus axei, Habronema muscae, H majus, and Draschia megastoma, 98% to 99% against adult cyathostomes, 86% to 97% against 4th-stage cyathostomes, and 100% against adult large strongyles. Although ivermectin was incomplete in its activity agai...
Effects of adenosine and deoxyadenosine on PHA-stimulation of lymphocytes of man, horse and pig. 1. Adenosine inhibits thymidine and uridine incorporation of PHA-stimulated lymphocytes of man and horse at concentrations higher than 50 and 10 microM, respectively. Deoxyadenosine is inhibitory at concentrations higher than 100 microM. Thymidine and uridine incorporation of porcine lymphocytes are elevated 5-7-fold by 25-100 microM adenosine, deoxyadenosine, inosine and hypoxanthine. Leucine incorporation of PHA-stimulated lymphocytes was affected by adenosine and deoxyadenosine in the same way, but to a lower extent. 2. Effects of adenosine and deoxyadenosine were more pronounced at shorter...
Effect of prolonged administration of anabolic and androgenic steroids on reproductive function in the mare. Administration to mares of the anabolic steroid, methandriol, at the maximum recommended dose (300 mg every 3 weeks) for 1 1/2 years had no effect on reproductive characteristics except for suppression of GnRH-induced LH release and a tendency to suppress basal LH levels and the height of the ovulatory LH surge. A 4-fold increase in dosage caused marked suppression of basal LH, the LH surge, and GnRH-induced LH release. Other reproductive responses were minimally affected. There were no behavioural effects, and no changes in weight occurred when mares were compared with matched controls. Small...
Effect of pregnancy and collection technique on prostaglandin F in the uterine lumen of Pony mares. Uterine flushings were obtained through the cervix (Method A) and through the wall of the uterus after hysterectomy (Method B) of ovariectomized Pony mares after s.c. injection of oestrogen for 1 week and progesterone for 2 weeks (Exp. 1). Non-pregnant and pregnant mares were flushed by Method A on Day 14 after ovulation and the flushings compared with those of non-pregnant mares injected i.v. with flunixen meglumine, a prostaglandin synthetase inhibitor, shortly before flushing (Exp. 3). Uterine flushings were also collected by Methods A and B from non-pregnant and pregnant Pony mares on Day ...
Equine immunology 2: immunopharmacology–biochemical basis of hypersensitivity. In general, 4 types of hypersensitivity reactions can be defined according to their immunological basis and clinical appearance. The differing mechanisms of these responses are described with particular reference to chemical mediators which through their pharmacological actions contribute to the clinical manifestations of hypersensitivity. Chemical mediators may exert their influence locally or systemically through their action on effector, tissues or organs and in addition, may be involved in the recruitment of cells of specific type to the site of the reaction. The possible role of these med...
Furosemide, Patella vulgata beta-glucuronidase and drug analysis: conditions for enhancement of the TLC detection of apomorphine, butorphanol, hydromorphone, nalbuphine, oxymorphone and pentazocine in equine urine. We have investigated the action of five sources of beta-glucuronidase enzymes on the hydrolysis of glucuronides of apomorphine, butorphanol, hydromorphone, nalbuphine, oxymorphone and pentazocine in equine urine. For all glucuronides tested, Patella vulgata beta-glucuronidase yielded the largest thin layer chromatographic (TLC) spots. For oxymorphone, P. vulgata was the only treatment to yield detectable TLC spots under test parameters. For these six drugs, TLC spot size and chromatographic quality were compared between control horses and horses pretreated with furosemide four hours earlier. F...
Effect of PGF-2 alpha on LH receptors in the equine corpus luteum. As quantified by Scatchard analysis, a 27 000 g crude luteal membrane fraction contained a single population of unoccupied LH receptors characterized by high affinity, ka = 0.647 +/- 0.158 X 10(11) M-1 and low binding capacity, Rt = 4.91 +/- 0.78 X 10(-11) M/mg membrane fraction. Acceptable hormonal specificity, reversibility, saturability, high affinity and tissue specificity indicated that the binding protein was a physiological receptor. To ensure that the methods used for Scatchard analysis were valid, hCG was characterized for specific activity and maximum bindability, non-specific bindin...
Effect of adrenergic neurotransmitters upon the ejaculatory process in the stallion. Successful empirical treatment of 17 out of 24 stallions, which had failed to ejaculate after normal penile erection, intromission and friction, by chemical blockage of beta-receptors and additional stimulation of alpha-receptors led us to investigate stallions with normal ejaculatory patterns. In an initial experiment one adult half-bred stallion was injected with 4.88 mg noradrenaline hydrochloride (treatment A), 10 mg bunitrolol (treatment B = beta-receptor blockage) and a combination of treatment A and B. Investigations of the same stallion on dated occasions without treatment served as co...
Sweating in the intact horse and isolated perfused horse skin. 1. In intact horses, heat-induced sweating occurred initially as pulses, then as a continuous, synchronously fluctuating discharge. 2. I.V. adrenaline (Adr) induced sweating immediately; isoprenaline (Isop) elicited sweating after a delay; and phenylephrine (PhE) had no sudorific effect. 3. In isolated perfused skin, PhE induced an immediate small sweat discharge, Isop a slower sustained output and Adr a biphasic discharge. alpha- and beta-adrenergic antagonists blocked the first and second phases, respectively, of Adr-induced sweating. 4. The observed sweating patterns are consistent with ind...
Glucocorticoid-induced inhibition of osteolysis and the development of osteopetrosis, osteonecrosis and osteoporosis. Changes in the developing femoral epiphysis, especially those concerning the osteocytes, were examined in pony foals systemically treated with daily intramuscular injections of either 0.5 or 5.0 mg of dexamethasone per 100 kg bodyweight for either 3, 8 or 11 months. Midsagittal sections of proximal femur from animals treated for 3 months contained significantly more bone tissue subchondrally and epiphyseally than did sections from untreated ponies. Large portions of the bone tissue appeared necrotic, although osteoblasts and patent capillaries were abundant. After 8 months the bone sections re...
Control of the oestrous cycle in mares with altrenogest. The clinical effectiveness of the synthetic progestagen, altrenogest, was evaluated in field trials with 449 mares during the 1980 breeding season. An oral dose of 27 mg altrenogest was administered daily for 15 days. In the first trial treated mares were compared with controls, and in the second trial the effectiveness of treatment for prolonged or erratic spring oestrus was evaluated. Oestrus was suppressed in 94% of the treated mares in the first trial. The post-treatment response was related to the stage during the transition from winter anoestrus to the spring breeding season and degree o...
Termination of twin gestation by blastocyst crush in the broodmare. Manual crushing of one blastocyst performed on 181 bicornuate twin pregnancies between Days 24 and 45 has shown that the uncrushed blastocyst can either survive and develop normally to full term or may be rejected and resorbed like its crushed twin, depending mainly on the stage of pregnancy. Crushing, which causes rupture of fetal membranes, results in a rapid fall in the survival rate of the uncrushed blastocyst when performed after Day 31. In some mares rupture is not possible after Day 35 even if extreme pressure is used. Crushed, but unruptured, blastocysts mainly between Days 35 and 45 m...
Limited trypsinolysis of porcine and equine colipases. Spectroscopic and kinetic studies. Porcine and equine colipases have been submitted to mild tryptic digestion. Proteolysis occurs at the Arg5-Gly6 bond with the loss of the N-terminal pentapeptide. Studies of native and trypsin-treated colipases by circular dichroism and laser chemically induced dynamic nuclear polarization indicate that proteolysis induces conformational changes in the region of the tyrosine cluster. Experiments in the presence of phospholipid provide further evidence showing that these residues are in or close to the region of the protein interacting with aggregated lipids. Kinetic studies of the reaction of ...
Plasma and tissue concentrations of oxytetracycline in the horse after intravenous administration. Oxytetracycline (OTC) was administered IV to 3 clinically normal horses at a dosage of 10 mg of OTC/kg of body weight. Plasma OTC concentrations were determined at 30-minute intervals until postinjection minute (PIM) 240. At PIM 240, the mean OTC concentration in pulmonary tissue was 3.96 microgram/g of tissue (wet weight) and in renal tissue was 25.47 micrograms/g. diluted bronchial fluid had a mean concentration of 0.288 microgram of OTC/ml at PIM 240. The data demonstrated that OTC has adequate tissue distribution in horses.
Influence of prostaglandin F2 alpha on sperm production and seminal characteristics of the stallion. Six mature stallions were used to test the effect of prostaglandin F2 alpha (PGF2 alpha ) on sperm production and seminal characteristics. Semen was collected from each stallion twice weekly 1 hr following a 10 mg intramuscular injection of PGF2 alpha or a sham injection. A switchback design was used so that three stallions received PGF2 alpha and three served as controls during the first 9 weeks (period 1). Treatment regimens were reversed during the second 9 weeks (period 2). Treatment of stallions with PGF2 alpha resulted in an increase (P less than .05) in gel free seminal volume and a dec...
Serum concentrations of trimethoprim and sulfadiazine following oral paste administration to the horse. Two fasted and 2 fed horses were dosed orally with a combined trimethoprim and sulfadiazine paste formulation at a dose of 35 mg (1:5 combined active ingredients)/kg. Serum concentrations of each drug were determined periodically for 3 consecutive days for the 4 horses. The extent and rate of absorption for trimethoprim were variable, but peak serum concentrations occurred generally within 3 hours; sulfadiazine absorption was slower, reaching peak concentrations by 6 hours. Fasting did not have a consistent effect on the serum concentration profiles for either drug. Both drugs achieved serum c...
Restoration of reproductive capacity of stallions after suppression with exogenous testosterone. Twelve stallions that had been given 0, 50 or 200 micrograms testosterone propionate (TP)/kg body weight every other day for 88 days were examined for the effects of androgen withdrawal on spermatozoal production, seminal quality and libido. Although the lower dosage did not affect most of the traits studied, the higher dosage severely reduced scrotal width, spermatozoal production, the number of sperm per ejaculate, the percentage of progressively motile spermatozoa and the percentage of normal spermatozoa. These adverse effects were found to be largely reversible. By 90 days after the cessat...
