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Topic:Biological Half-Life
Biological half-life refers to the time required for a substance to decrease by half in its concentration within the body. In horses, understanding the biological half-life of various substances, such as medications, nutrients, or toxins, is important for determining dosing schedules, withdrawal times, and potential effects on equine health. The biological half-life can vary significantly depending on the substance in question, as well as factors such as the horse's metabolism, age, and health status. This page compiles peer-reviewed research studies and scholarly articles that explore the biological half-life of different substances in horses, examining factors that influence these rates and their implications for veterinary medicine and equine management.
Interference of maternal antibodies with the immune response of foals after vaccination against equine influenza. The purpose of the study was twofold. First, using two groups of 22 foals each, we investigated the extent to which maternal antibodies interfere with the humoral response against equine influenza. The foals were born to mares that had been vaccinated twice yearly against influenza since 1982. Foals of group I were vaccinated three times at early ages (12, 16, and 32 weeks of age), and foals of group II were likewise vaccinated but a later ages (24, 28, and 44 weeks of age). After the first and second vaccinations, neither group showed an increase in antibodies that inhibit haemagglutination. ...
The pharmacokinetics of a slow-release theophylline preparation in horses after intravenous and oral administration. The pharmacokinetics of a slow-release theophylline formulation was investigated following intravenous and oral administration at 10 mg/kg in horses. A tricompartmental model was selected to describe the intravenous plasma profile. The elimination half-life (t1/2 beta) was 16.91 +/- 0.93 h, the apparent volume of distribution (Vd) was 1.35 +/- 0.18 L/kg and the body clearance (ClB) was 0.061 +/- 0.009 L kg-1 h. After oral administration the half-life of absorption was 1.24 +/- 0.30 h, and the calculated bioavailability was above 100%. The t1/2 beta after oral administration was 18.51 +/- 1.75 ...
An estimate of melanosome concentration in pigment tissues. Concentration of melanosomes in various tissues has been unknown because of the impracticability of their direct quantification. Using an indirect approach comprising the estimation of melanin both in freeze-dried tissue samples and in isolated melanosomes, we obtained data on the amount of melanosomes in various pigment tissues. The concentrations of melanosomes found in the tissues were relatively high, not only reflecting the dark color of pigment tissues but also explaining their capacity to perform various functions ascribed to the presence of melanin.
Glyoxalase 2 deficiency in the erythrocytes of a horse: 1H NMR studies of enzyme kinetics and transport of S-lactoylglutathione. In mammalian red blood cells the metabolism of methylglyoxal, and some alpha-ketoaldehydes, takes place via two, generally, highly active enzymes, glyoxalase 1 and 2. The 1H NMR spin-echo spectra of horse erythrocytes, and the various reactants in the glyoxalase system, were characterized as a prelude to obtaining series of spectra in time courses of methylglyoxal metabolism. We characterized the kinetics of the enzyme system in red cells from a normal horse and also from one which had very low activity of glyoxylase 2. The kinetics of the reaction scheme, with methylglyoxal as the starting su...
Pharmacokinetics of caffeine and its metabolites in horses after intravenous, intramuscular or oral administration. The pharmacokinetics of caffeine (CAF) and its metabolites, dimethylxanthines, were examined in horses administered 2.5 mg/kg of CAF intravenously (i.v.), intramusculary (i.m.), or orally (p.o.). The plasma samples were extracted by Extrelut and the concentrations of CAF and metabolites were determined by high performance liquid chromatography (HPLC) with a short column. The pharmacokinetics of CAF after bolus i.v. injection were described by the assumption of a two-compartment model, and those of CAF after i.m. or p.o. administration were done by the assumption of a one-compartment model. The...
Effects of carbohydrates on the pharmacokinetics and biological activity of equine chorionic gonadotropin in vivo. The sialylation of eCG was examined to determine its influence on the in vivo metabolism and biological activity of the molecule. Sialic acid was decrementally removed from eCG by incubation with agarose-linked neuraminidase for varying time periods. Pharmacokinetic parameters for the disappearance of 4,000 IU (267 micrograms) of three desialylated eCG preparations (20%, 53%, and 80% sialic acid removed) and control eCG were determined in sheep. The clearance rate of eCG increased (p less than 0.05) with each decrement of sialic acid. The removal of 53% sialic acid enhanced the distribution of...
Clenbuterol plasma concentrations after repeated oral administration and its effects on cardio-respiratory and blood lactate responses to exercise in healthy Standardbred horses. To evaluate the effects of clenbuterol on cardio-respiratory parameters and blood lactate relation to exercise tolerance, experimental horses performed standardized exercise tests on a high-speed treadmill before and after administration of the drug. Clenbuterol was administered in feed to six healthy Standardbreds at a dose rate of 0.8 micrograms/kg b.wt twice daily for 5.5 days. Each horse was tested twice, without and with a respiratory mask, during two consecutive days. One week elapsed between the baseline tests without drug and the tests with clenbuterol treatment (each horse served as i...
The pharmacokinetics and locomotor activity of alfentanil in the horse. The pharmacokinetics of alfentanil were investigated in the horse. Four doses of alfentanil (4, 10, 20 and 40 micrograms/kg) were given to four horses at different times and their locomotor activity monitored. Doses of 20 and 40 micrograms/kg produced a significant increase in locomotor activity. The plasma concentrations of alfentanil were measured in six standing horses and the pharmacokinetics calculated. It was found that the decay curves were best described by a biexponential equation. The elimination half-life (t1/2 beta) was 21.65 +/- 3.99 min and the clearance (Cl) was 14.1 +/- 0.7 ml/...
Studies of meclofenamic acid and two metabolites in horses–pharmacokinetics and effects on exercise tolerance. The pharmacokinetics and the effects on treadmill exercise of the anti-inflammatory drug meclofenamic acid were studied in seven Standardbred horses after single intravenous and/or oral doses. The decline in plasma concentration after a single intravenous dose of meclofenamic acid (2.2 mg/kg b.wt) was described by a two-compartment open model. The average elimination half-life was 1.4 h, the apparent volume of distribution 0.14 l/kg and the plasma clearance 0.12 l/h kg. Absorption was the rate-limiting step after oral administration. Non-compartmental analysis showed a mean absorption time of ...
Detection of reserpine in horses by high-performance liquid chromatography. A high-performance liquid chromatography (HPLC) assay was developed for the detection of reserpine. The assay was used to monitor the plasma concentrations of the drug given intramuscularly on one or two occasions to five horses. The blood concentrations of reserpine varied quite considerably between horses given the same dose of the drug. However, on average, reserpine could be detected consistently, and quantified, for 48 h after a single dose of 2.5 mg, and for a similar period after the second of two 2.5 mg doses given 13 d apart. Because of the apparently large variability in the pharmaco...
Effect of diet on gentamicin-induced nephrotoxicosis in horses. Gentamicin sulfate-induced nephrotoxicosis was compared in 2 groups of horses fed different rations. Four horses were fed only alfalfa hay, and 4 other horses were fed only whole oats. Seven days after initiation of the diet, all horses were given gentamicin IV (5 mg/kg of body weight) every 12 hours for 22 days. Urinary gamma-glutamyl-transferase to urinary creatinine (UGGT:UCr) ratio was calculated daily, and serum concentration of gentamicin was measured at 1 and 12 hours after drug administration. Results indicated that horses fed oats had greater renal tubular damage than did horses fed a...
Biological and immunoactive substances resembling chorionic gonadotropin are present in full-term horse and zebra placentas. This study describes the presence of immunoactive and bioactive eCG-like material in full-term placentas of both domestic horses and zebras. Term placental extracts were immunoreactive in an LH monoclonal antibody RIA, and methods successfully used previously for the purification of eCG and eLH were employed to further concentrate the immunoreactive materials to the point where additional characterization studies could be performed. Sufficient equine material was obtained to perform a final fractionation on a concanavalin A Sepharose column yielding an unadsorbed fraction, e17A, and an adsorbe...
Equine follicle-stimulating hormone action in cultured Sertoli cells from rat, sheep and pig. Using a suspension of seminiferous tubule cells, we had previously shown that equine FSH is superactive in the male rat, i.e. that it exhibits a higher biological potency than expected from its binding activity. In this work we investigated equine FSH superactivity in rat, pig and sheep, by comparing in each species the equine FSH with the homologous FSH, both for their binding activities (in a radioreceptor assay using a testicular membrane fraction) and for their in vitro biological potencies (in a plasminogen activator assay using a Sertoli cell-enriched population cultured on plastic). In ...
Assessment of the potential toxicity of a poison for rabbits, pindone (2-pivalyl 1, 3 indandione), to domestic animals. The toxicity of pindone, a rabbit poison, to horses, cattle, goats, chickens, dogs and cats was investigated, using extension of prothrombin time (PT) as an index of poisoning. The daily dose of pindone, administered for 5 days, ranged from 0.3 mg/kg for dogs to 2.5 mg/kg for chickens. This range of dose rates was considered to be indicative of the worst possible case that could arise following a campaign of baiting for rabbits. Although significant elevations in PT (more than double baseline values) were noted in all species other than horses, clinical signs of anticoagulant poisoning were no...
Maternal antibodies against equine influenza virus in foals and their interference with vaccination. Foals that were born to mares vaccinated twice a year against influenza had moderate to high haemagglutination-inhibition antibody titers at 24 hours after birth. The foals were vaccinated at six and ten weeks of age, and again at three to five months after birth. Four months after the third vaccination no antibodies against A/H7N7 and A/H3N8 influenza viruses were detected in these foals. Thus, maternal antibodies probably prevented the development of antibodies against equine influenza virus after vaccination. Foals born to the same mares one year later were monitored to determine the rate o...
Eltenac, a new anti-inflammatory and analgesic drug for horses: clinical aspects. Two controlled studies to determine efficacy in the horse were performed with eltenac, a new injectable, non-steroidal anti-inflammatory drug (NSAID). Clinical trials were carried out with a dose rate of 1 mg/kg body weight in a randomized, placebo-controlled, double-blind design to assess therapeutic efficacy in acute inflammatory disorders and in animals with orthopaedic conditions. In a preliminary pharmacokinetic investigation in six horses mean elimination half-life was 1.7 h after i.v. administration. In the first clinical study, analgesic activity on pain-related lameness was determined...
Disposition of human drug preparations in the horse. I. Rectally administered indomethacin. A high-performance liquid chromatographic method to measure urinary indomethacin levels is described. In 0.5 ml urine, 1 micrograms/ml of indomethacin could be detected. Alkaline hydrolysis of urine resulted in the decomposition of indomethacin. When two suppositories of Indocid corresponding to 200 mg indomethacin were administered rectally to four horses the drug was rapidly absorbed and remained detectable in urine from 1 to 12 h. The excretion rate peaked after 2-3 h while the maximal concentration ranged from 18.5 to 80.6 micrograms/ml. Only 8 to 16% of the indomethacin dose was eliminate...
Immunohistolocalization of the carbonic anhydrase isozymes I, II and III in equine salivary glands. The immunolocalization of carbonic anhydrase isozymes in equine salivary glands was investigated for assessment of their biologic functions. In parotid glands, duct segments showed reactivity with CA-I and CA-III. CA-III was selectively located in duct segments, particularly in the basal cells of the interlobular duct. Serous acinar cells were positive for CA-I and CA-II. In submandibular glands, CA-I and CA-II were present in serous demilune and duct segments. CA-II was selectively located in the duct segments, as also noted in the parotid gland. In sublingual glands, CA-I and CA-II were loca...
A study of bovine and equine immunoglobulin levels in pony foals fed bovine colostrum. As part of a project to raise specific pathogen free (SPF) Welsh Mountain Pony foals, free from exposure to Equid herpesvirus type 1, foals were removed from their dams at birth and fed bovine colostrum. This study characterises the uptake of bovine colostral immunoglobulin and production of endogenous immunoglobulin, in 10 SPF foals. An enzyme-linked immunoadsorbent assay was developed to measure serum concentrations of bovine IgG1 (boIgG1) to assess the efficiency of transfer, and rate of elimination of boIgG1 by the foal. The endogenous production of equine IgG was studied using a single ra...
Equine chorionic gonadotropin. Cells from the chorionic girdle of the equine trophoblast invade the maternal endometrium at day 36 of gestation and become established as secretory elements known as the endometrial cups. These structures, which persist for 40-60 days, produce a gonadotropin which can be found in circulation until about day 130 of gestation. This glycoprotein has been identified in the horse and the donkey, with the former having received much better characterization. It consists of 2 noncovalently linked peptide chains; an alpha-subunit of 96 amino acids, which is common to that found in other horse glycopro...
Chloramphenicol 3. Clinical pharmacology of systemic use in the horse. The use of chloramphenicol in the horse is now prohibited as horses are classified as food-producing animals. However, chloramphenicol has until recently been widely available for oral, intramuscular or intravenous administration. A critical appraisal of the published literature on the use of chloramphenicol in the horse clearly demonstrates that there are sound pharmacokinetic and microbiological reasons for concluding that chloramphenicol is not an appropriate antibiotic for systemic use. The short half-life of chloramphenicol in the horse, together with the broad range of minimum inhibitory...
Effect of interval between doses on response of the pony to sodium bicarbonate. Three pony geldings were given sodium bicarbonate orally in order to study the effect on blood pH and bicarbonate and to determine if frequency of dosing influences the response. In a preliminary study, it appeared that a carry-over effect might occur if the interval between dosing was only 2 days. The ponies received 2 doses of sodium bicarbonate (400 mg/kg) 7 days apart in trial one and then in trial two they received 2 doses of sodium bicarbonate 4 days apart. The sodium bicarbonate was mixed with 2 liters of warm water and given through a nasogastric tube on each trial day. Blood samples w...
Low dose calcium heparin in horses: plasma heparin concentrations, effects on red blood cell mass and on coagulation variables. Low dose calcium heparin was administered subcutaneously at 12 hourly intervals to six healthy horses at an initial dose of 150 iu of heparin/kg bodyweight (bwt) and at a maintenance dose of 120 iu/kg bwt. All injections were given at 0900 and 2100 h. Blood samples for monitoring plasma heparin concentrations were obtained prior to, at 2 hourly intervals for 84 h (treatment period), and at Hours 24, 32, 48 and 96 of the control period. Blood samples for monitoring red blood cell (RBC) mass, plasma antithrombin III activity (AT III), activated partial thromboplastin time (APTT), and thrombin ti...
Changes in luteinizing hormone bioactivity associated with gonadotrophin pulses in the cycling mare. Equine plasma luteinizing hormone (LH) possesses both biological (in vitro bioassay, B) and immunological (radioimmunoassay, I) activities and the ratio of B:I varies with stage of the oestrous cycle. To estimate the contribution made by pituitary secretion and peripheral metabolism to changes in the B:I ratio, pituitary venous effluent and circulating plasma from 5 dioestrous and 2 oestrous mares were analyzed using both an in vitro bioassay and a radioimmunoassay. During dioestrus, LH was released in a pulsatile fashion with a frequency of 1.4 pulses/24 h and a pulse duration of 20-40 min (c...
Pharmacokinetics of gentamicin in newborn to 30-day-old foals. Gentamicin sulfate, equivalent to 4 mg of gentamicin base/kg of body weight, was administered IV to 6 Thoroughbred foals on day 1 (12 to 24 hours of age) and at 5, 10, 15, and 30 days after birth. On day 40 after parturition, gentamicin was given to the mares at a dosage similar to that used in foals. Decay of serum gentamicin concentrations was best described by a 2-compartment model. Among foals, the overall elimination rate constant at 30 days of age was significantly (P less than 0.05) greater than at days 1, 10, and 15. There was, however, no difference in the overall elimination rate con...
[Detection of dexamethasone in horses]. Due to their marked antiinflammatory effect, synthetic corticosteroids are used to mask illness, especially lameness in horses. The detection of these drugs in equine body fluids requires accurate methods, particularly where misuse of corticosteroids is suspected. Gas chromatography/mass spectrometry (GC/MS) is well established as a reliable technique for the identification of drugs in biological fluids. Using GC/MS, we determined dexamethasone levels in horse urine and serum after intravenous application of a therapeutic dose. Dexamethasone was detectable, in serum for up to six hours, and in...
Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse. Hordenine is an alkaloid occurring naturally in grains, sprouting barley, and certain grasses. It is occasionally found in post race urine samples, and therefore we investigated its pharmacological actions in the horse. Hordenine (2.0 mg/kg bodyweight [bwt]) was administered by rapid intravenous (iv) injection to 10 horses. Typically, dosed horses showed a flehmen response and defecated within 60 secs. All horses showed substantial respiratory distress. Respiratory rates increased about 250 per cent and heart rates were approximately double that of resting values. All animals broke out in a sw...
