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.
[Studies on the effects of intravenous administration of glucose, fructose, invertose and sorbitol on various blood constituents of blood plasma (monosaccharides, insulin, lactate, pyruvate and free fatty acids as well as glutamate-oxaloacetate transaminase) in the horse]. Horses were examined for the behaviour of various blood constituents prior to and following infusions of solutions of glucose, fructose, invertose, and sorbitol. Infusion of 0.5 g/kg live weight glucose to six horses was followed by half-life variation between eleven and 23 minutes. Subsequent infusion of invertose to the same animals usually caused prolongation of glucose half-life. Half-life values were between 17 and 33 minutes for fructose and between 21 and 80 minutes for glucose. Infusion of 0.5 g/kg live weight fructose to two horses was followed by half-life values between 17 and 18 mi...
Drug interactions in the horse: effects of chloramphenicol, quinidine, and oxyphenbutazone on phenylbutazone metabolism. The plasma half-life of phenylbutazone in horses was not increased after pretreatment with chloramphenicol or quinidine, but was increased after oxyphenbutazone. This increased plasma half-life after oxyphenbutazone is consistent with observations in other species and suggests that oxyphenbutazone inhibits the metabolism of phenylbutazone in horses. Lack of inhibition of phenylbutazone metabolism in the horse by chloramphenicol and quinidine is inconsistent with results obtained in other species.
Drug interactions in the horse: effect of furosemide on plasma and urinary levels of phenylbutazone. Horses pretreated with 6.6 mg/kg of phenylbutazone were injected with 1 mg/kg of furosemide intravenously. Furosemide had no clinically significant effect on either plasma levels or plasma half-life of phenylbutazone. Furosemide reduced urinary levels of phenylbutazone 18-fold to concentrations which may result in inconsistent drug detection in routine screening tests. The results show that it is not possible to monitor compliance with phenylbutazone medication rules by means of urinalysis alone if the use of furosemide is permitted. Furosemide treatment, however, does not interfere with monit...
The excretion of ibuprofen by the horse – a preliminary report. The anti-inflammatory drug Ibuprofen [(+/-)-2-(p-isobutylphenyl) propionic acid] was estimated in the blood and urine of a horse using gas-liquid chromatography of the silylated derivative. Levels of the drug in the two body fluids were measured over a period of about 24 hours after administering a 12 gm dose of Ibuprofen. Plasma peak levels were observed within 30 to 60 min, and the drug was no longer detectable in the plasma by 8 hr. Urinary peak levels were observed 200 to 300 min after dosing, and the drug was no longer detectable in the urine by about 28 hr. It was observed that only 2% t...
Pharmacology of procaine in the horse: procaine esterase properties of equine plasma and synovial fluid. Procaine added to whole equine blood or diluted plasma was hydrolyzed with half times of approximately 9 and 12 minutes, respectively, at 37 C. This hydrolytic activity was sensitive to heating and physostigmine, but did not affect procainamide. At pharmacologic concentrations of procaine, the rate of the hydrolytic reaction depended directly on the concentrations of plasma or procaine in the system and was less in whole blood than in plasma. These properties are consistent with hydrolysis being due to plasma esterases operating at less than saturating procaine concentrations. These esterases ...
A review of the pharmacology, pharmacokinetics and behavioral effects of procaine in thoroughbred horses. Since procaine has both local anaesthetic and central stimulant actions its presence in the blood or urine of racing horses is forbidden. After rapid intravenous injection of procaine HC1 (2.5 mg/Kg) in thoroughbred mares plasma levels of this drug fell rapidly (t 1/2 alpha = 5 min) and then more slowly (t 1/2 beta = 50.2 min). These kinetics were well fitted by a two compartment open model (Model I). This model gave an apparent Vdbeta for procaine in the horse of about 3,500 litres. Since procaine was about 45% bound to equine plasma protein this gives a true Vdbeta for procaine of about 6,50...
Pharmacology of procaine in the horse: a preliminary report. Rapid intravenous injection of 1 g of procaine hydrochloride in Thoroughbred mares produced variable signs of central nervous system excitation for as long as 4 minutes. Plasma concentrations of procaine were similarly variable and transient, decreasing with a half-life of approximately 25 minutes. In vitro, plasma from freshly collected equine blood hydrolyzed procaine with a half-life of approximately 7.5 minutes. This hydrolysis was apparently due to plasma esterases. Penicillin, when added free or complexed as procaine-penicillin, did not protect procaine against hydrolysis by these plasma...
Mefanamic acid blood and urine levels in the horse determined by derivative gas-liquid chromatography-electron capture. Mefenamic acid is extracted from biological fluids and is acylated with pentafluoropropionic anhydride to form a derivative possessing high electron affinity. The derivative is analyzed by gas-liquid chromatography with an electron capture detector. The method is particularly valuable for determining drug levels in blood where small sample and/or drug concentrations are available.
Studies on metabolism and effects of estrogen on pituitary prolactin and LH secretion. The effect of a subcutaneous injection of estradiol on the secretion of pituitary prolactin in the rat and the relationship between serum estradiol level and luteinizing hormone (LH) secretion in mare were reviewed. In addition, the effect of estradiol injection on LH secretion and the metabolism of [14C] estradiol in intact and bile duct fistulated pony mares were studied. Low (0.1 mug/day/rat) to moderate dose (5 mug/day/rat) of estradiol benzoate injected subcutaneously to mature or immature rats significantly increased pituitary content of prolactin and serum prolactin level five- to tenfo...
Comparison of the pharmacokinetics of penicillin G and ampicillin in the horse. The affinity and the binding capacity of horse serum proteins for ampicillin and penicillin G were measured by equilibrium dialysis or ultrafiltration technique. From the figures thus obtained it may be concluded that in the range of therapeutic concentrations the protein-bound fraction accounts for 6 X 8-8 per cent of the total ampicillin concentration and for 52-54 per cent of the total penicillin G concentration in serum. The rate of elimination of ampicillin and penicillin G in horses was assessed by following serum concentrations after a single intravenous injection. The biological half l...
Muscle structure and function–an explanation. The structure of vertebrate skeletal muscle is reviewed. The mechanism of muscular contraction and its control is then discussed from the point of view of molecular structure. Contraction takes place by a sliding filament mechanism produced by cross-bridges which form between thick and thin filaments. Control is exercised by tropomyosin and troponin. When the calcium concentration is low, these proteins interfere with the formation of cross-bridges and prevent contraction, but when the calcium concentration is increased, they no longer interfere and contraction proceeds.
Pharmacological experiments as a basis for the administration of digoxin in the horse. It is shown that the concentration of ouabain necessary for 50 per cent inhibition of the Na+K activated membrane ATPase of red cells is similar in man and horse. This is taken to indicate that the two species have similar sensitivity towards cardiac glycosides in general. In five adult healthy horses plasma digoxin concentration was measured with a radioimmunoassay technique after a single intravenous injection of 1 mg/100 kg body weight digoxin. The half time of elimination was 23 h and the apparent volume of distribution 7.3 litres/kg. An approximate estimate of plasma protein binding of di...
Plasma concentrations, plasma protein binding and residues of sulfamonomethoxine in pigs, horses and cattle. The protein binding, the plasma half-life and the residue depletion of sulfamonomethoxine (SMM) after intramuscular administration were investigated in pigs, horses and cattle. Protein binding was weakly concentration-dependent. The bound fraction in plasma in the therapeutic range amounted to approximately 45, 40 and 50% for pigs, horses and cattle respectively, and the plasma half-lives were approximately 5.1, 5.7 and 3.1 hours respectively. SMM levels were less than 1 mug/g in muscle tissue after 36, 20 and 12 hours in pigs, horses and cattle respectively. In the kidney SMM levels were not ...
Effect of exogenous progesterone on its endogenous levels: biological half-life of progesterone and lack of progesterone binding in mares. The disappearance rate of progesterone from blood plasma of an ovariectomized mare was rapid and occurred in three phases. The half-life of the first component was 2-5 min and that of the second was 20 min; the half-life of the much slower third component was not measured. Progesterone, administered to ovariectomized and deeply anoestrous mares at the rate of 150 or 300 mg/day, maintained maximal peripheral levels of 6 to 8 ng/ml. Physiological levels were reached in 21 days using a dose of 150 mg and in 11 days with 300 mg daily. After withdrawal, circulating levels dropped rapidly. Blood pla...
Relationship between luteal function and metabolic clearance and production rates of progesterone in the mare. The functional activity of the equine CL was measured by its ability to convert [4-14C]3beta-hydroxy-5-en-20-one to [4-14C]pregn-4-en-3,20-dione. The capacity of homogenates of CL of different ages followed the temporal pattern of plasma progestagen concentrations. In ten mares which ovulated twice at intervals of 0 to 9 days in the same cycle, the conversion capacity of the CL from the second ovulation was similar to that from the first ovulation. After adjusting for age, the CL from the first of two ovulations had a similar conversion capacity as that resulting from a single ovulation. Plasm...
Immunoglobulin metabolism in the neonatal foal. The proteins IgG and IgG(T) are the predominant immunoglobulins in equine colostrum. Their distribution and catabolism were studied in the newborn foal using an isotopic tracer technique. More precise quantitation of the absorption of these immunoglobulins from colostrum is now possible.
Plasma LH levels in the mare during the oestrous cycle. Plasma levels of LH were determined by heterologous radioimmunoassay utilizing highly purified equine LH as standard. Samples were taken regularly from eleven mares for twenty-six oestrous cycles over a period of 10 weeks. The mean cycle length was 20-5 +/- 3-1 (S.D.) days, and ovulation occurred on average 4-3 +/- 1-6 (S.D.) days from the time heat was first detected. Levels of LH were persistently low from Days 5 to 16 of the cycle (ovulation = Day 0). They then increased slowly over a number of days and continued to rise beyond the levels observed at any time during the immediate preovulato...
Bile acid kinetics and bile secretion in the pony. Bile acid pool size and synthesis rate were determined by both isotope-dilution and washout methods in ponies with chronic external biliary fistulas. Bile acid pool size (10.9 mumol/kg) and synthesis rate (11.2 mumol/day per kg) estimated by the isotope-dilution method did not differ significantly from pool size (9.4 mumol/kg) and synthesis rate (9.5 mumol/day per kg) estimated by washout method. Bile acid-dependent and -independent fractions of bile flow, determined by a method that circumvents any inevitable correlation of flow to bile acid secretion due to common factors in both parameters,...
The kinetics of hematopoiesis in the light horse II. The hematological response to hemorrhagic anemia. Hemorrhagic anemia was experimentally produced in three Standardbred horses by removing approximately 63% of the red cell mass and the accompanying plasma during a three day interval. Red cell parameters were examined daily for 45 days and then weekly until termination of the experiment 250 days after production of the anemia. Leukocytes, platelets and bone marrow aspirates were examined at regular intervals for 25 days after the final phlebotomy. At 24 hours after the last bleeding, 75-selenomethionine was injected intravenously to measure the lifespan of the newly produced erythrocytes. The ...
Pregnant mare serum gonadotrophin: rate of clearance from the circulation of sheep. The process involved in the disappearance of PMSG from the blood of sheep, following a single intravenous injection, has been separated into two exponential components. Values (mean plus or minus S.E.) calculated from experiments on five animals were: metabolic clearance rate (37.8 plus or minus 1.6 ml hr-minus 1); rate constant of disposal (0.0315 plus or minus 0.0016 hr-minus 1); half-time of disposal (21.2 plus or minus 1.1 hr). The stage of the oestrous cycle, ovariectomy and the dose of PMSG used had no apparent effect on these values.
Nitrite and nitrate pharmacokinetics in the dog, sheep, and pony. Elimination kinetics of nitrite and nitrate in the dog, sheep, and pony were determined. The elimination half-lives of nitrite were 0.499, 0.475, and 0.566 hours in the dog, sheep, and pony, respectively; those of nitrate were 44.681, 4.233, and 4.821 hours. Apparent specific volumes of distribution (V'd) of nitrite were variable among the 3 species--1,623.7 ml/kg in the dog, 278.0 ml/kg in the sheep, and 191.6 ml/kg in the pony. The V'd of nitrate were less varied--dog, 238.5 ml/kg; sheep, 291.1 ml/kg; and pony, 209.3 ml/kg. In the in vitro studies on protein binding in canine plasma, the ext...
Recovery of procaine from biological fluids. A published method for the recovery of procaine from human plasma using 5M NaOH gave very poor recoveries. Investigation showed that under the recommended extraction conditions procaine was rapidly hydrolysed. Extraction into benzene of samples buffered to pH 9.0 with borate buffer allowed essentially 100% recovery of procaine from equine plasma and urine.
A pharmacological study of chloramphenicol in horses. Pharmacological disposition of chloramphenicol was studied in horses. Minimum levels of the antibiotic (greater than or equal to 5 mu g/ml) in blood or plasma recommended to combat infections could not be achieved by 4.4 and 8.8 mg/kg I.V. or 30 and 50 mg/kg I.M. or 30 mg/kg oral (as palmitate salt) doses of chloramphenicol. Increasing the dose to 19.8 and 26.4 mg/kg I.V. provided such levels for about two and three hours respectively. A combination of 20 mg/kg I.V. and 30 mg/kg I.M. administered simultaneously did not provide more prolonged levels than 26.4 mg/kg I.V. alone. Chloramphenicol s...