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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.
Pharmacokinetics of cisapride in the horse. The purpose of this study was to determine the pharmacokinetics and absolute bioavailability of cisapride after intravenous (i.v.) and intragastric (i.g.) administration in healthy, adult horses. Five animals received single doses of 0.1 mg/kg, 0.2 mg/kg and 0.4 mg/kg cisapride by the i.g. route in an open, randomized fashion on different occasions separated by a washout period of at least 48 h. Four of these horses were also given a single i.v. dose of 0.1 mg/kg cisapride. Jugular venous blood was collected periodically up to 24 h after dosing. Plasma cisapride concentrations were measured by...
Pharmacokinetics of a high dose of gentamicin administered intravenously or intramuscularly to horses. To evaluate pharmacokinetics of a high dose of gentamicin administered i.v. or i.m. to horses. Methods: Repeated-measures study. Methods: 6 clinically normal female adult stock-type horses. Methods: All horses were given gentamicin (6.6 mg/kg [3 mg/lb] of body weight), i.v. and i.m., in a two-way cross-over design. Serum gentamicin concentrations were measured during a 24-hour period. Results: Plasma concentration curves were consistent with a two-compartment model. Maximum plasma gentamicin concentrations were 71.9 +/- 15.7 micrograms/ml (0 hours after injection) and 22.0 +/- 4.9 micrograms/m...
Passive transfer, rate of decay, and protein specificity of antibodies against equine arteritis virus in horses from a Standardbred herd with high seroprevalence. To determine rate of decay of passively acquired antibodies in Standardbred foals on a farm with a high seroprevalence to equine arteritis virus (EAV) and to determine whether vertical or horizontal transmission of the virus was responsible for infection on the farm. Methods: Repeated-measures study. Methods: 46 Standardbred horses (15 brood mares and their foals, 5 stallions, and 11 young horses). Methods: Serum samples obtained from horses on the farm were evaluated by serum neutralization and western immunoblot analysis to detect EAV-specific antibodies. The half-life of passively acquired ...
The pharmacokinetics of furosemide in anaesthetized horses after bilateral ureteral ligation. The pharmacokinetics of furosemide were investigated in anaesthetized horses with bilateral ureteral ligation (BUL) with (n = 5) or without (n = 5) premedication with phenylbutazone. Horses were administered an intravenous (i.v.) bolus dose of furosemide (1 mg/kg) approximately 60-90 min after BUL. Plasma samples collected up to 3 h after drug administration were analysed by a validated high performance liquid chromatography method. Median plasma clearance (CLp) of furosemide in anaesthetized horses with BUL was 1.4 mL/min/kg. Apparent steady state volume of distribution (Vd(ss)) ranged from 1...
Effect of sodium methyl arsinate and imidocarb dipropionate antiprotozoal drugs on the pharmacokinetic of gentamicin in equines. The pharmacokinetic behaviour of gentamicin sulphate (3.4 mg/kg bwt) was studied following its intramuscular injection to a group of horses and to another group of horses premedicated with sodium methyl arsinate (2 mg/kg bwt) or imidocarb dipropionate (4.8 mg/kg bwt). Considerable differences were observed in the pharmacokinetics of gentamicin in pre-medicated horses and in horses which had received the antibiotic alone. Peak serum concentration of gentamicin (9.85 +/- 0.05 and 11.15 +/- 0.15 micrograms/ml) were attained within 1.45 +/- 0.05 and 0.92 +/- 0.04 h in arsinate and imidocarb-medica...
Pharmacokinetics of sulfonamides and trimethoprim in the donkey (Equus asinus). The body disposition of sulfadimidine (SDM), sulfadiazine (SDZ), sulfamethoxypyridazine (SMPZ) and a trimethoprim-sulfadimethoxine combination (TMP-SDMX) was investigated in the donkey. The four sulfonamides and TMP were injected intravenously at doses of 20 mg/kg (SDM, SDZ, SMPZ), 12.5 mg/kg (SDMX) and 2.5 mg/kg (TMP). The body clearance (ClB) of SDZ (1.70 +/- 0.14 ml/min/kg) was significantly higher than those of SDM (1.13 +/- 0.18 ml/min/kg), SMPZ (1.10 +/- 0.09 ml/min/kg) and SDMX (0.75 +/- 0.04 ml/min/kg). In contrast, the volume of distribution at steady state (Vss) was similar for the f...
The activity of mixed function oxidases, estimated by in vivo antipyrine clearance, is similar in horses and camels. The activity of hepatic mixed function oxidases was compared in horses and camels (Camelus dromedarius) by studying the pharmacokinetics of antipyrine in seven camels and five horses following intravenous administration of a single dose of antipyrine (25 mg/kg). The data obtained (mean +/- SEM and median in brackets) in camels and horses, respectively, were as follows: the elimination half-lives were 3.25 +/- 0.23 (3.19) and 3.09 +/- 0.25 (2.90) hr; the apparent volumes of distribution (area method) were 0.691 +/- 0.045 (0.648) and 0.642 +/- 0.034 (0.676) l/kg; the volumes of distribution at s...
Cumulus expansion, chromatin configuration and meiotic competence in horse oocytes: a new hypothesis. When recovered from the follicle, horse oocytes may be categorised as having either a compact or an expanded cumulus. Cumulus expansion is strongly associated with follicle atresia. Oocytes with expanded and compact cumuli have similar proportions in the germinal vesicle stage when recovered from the follicle. However, during in vitro culture, a higher proportion of oocytes with expanded cumuli mature, and they do so more quickly, than do oocytes with compact cumuli. Using Hoechst 33258 to label chromatin, in the germinal-vesicle stage horse oocytes can be divided into those in which the nucle...
Pharmacokinetics of ketoprofen in healthy foals less than twenty-four hours old. To determine pharmacokinetic variables that describe disposition of ketoprofen after its i.v. administration to foals < 24 hours old. Methods: 6 healthy foals (1 male and 5 females); mean age, 12.5 (range, 8.5 to 17) hours at time of dose administration. Methods: Ketoprofen was administered i.v. to foals at a dosage of 2.2 mg/kg of body weight. Ketoprofen concentration in plasma samples was analyzed, using high-performance liquid chromatography. Concentration versus time profiles were analyzed according to standard pharmacokinetic techniques. Blood samples were obtained from foals by jugula...
Disposition of human drug preparations in the horse. VI. Tiaprofenic acid. Urinary and plasma concentrations of the nonsteroidal anti-inflammatory drug tiaprofenic acid were determined following oral and intramuscular administration of a dose of 1 g to five fasted horses. Quantitation was performed by high-performance liquid chromatography (HPLC). The limit of quantitation (LOQ) was 0.1 microg/ml and 0.5 microg/ml in 2 ml plasma and 1 ml urine, respectively. Assay precision and extraction recovery were between acceptable values. Tiaprofenic acid pharmacokinetics were described by non-compartment analysis of the data. Absorption was faster after oral administration as...
A microtiter plate assay for the determination of uronic acids. The amount of uronic acid residues in samples containing glycosaminoglycans or pectin is an important parameter in the quantitative and structural analysis of these complex carbohydrates. This paper describes a method to determine the content of uronic acids in biological samples, using conventional polystyrene microtiter plates and microtiter plate-reading equipment with standard interference filters (i.e., 540 or 492 nm). This assay is a modification of a commonly used procedure, viz. hydrolysis of uronic acid containing carbohydrate polymers in 80% sulfuric acid containing tetraborate ions ...
Duration of effects of phenylbutazone on serum total thyroxine and free thyroxine concentrations in horses. The objectives of this study were to determine if phenylbutazone decreased serum thyroxine (TT4) and free thyroxine (FT4) concentrations using radioimmunoassay and equilibrium dialysis techniques in horses, and, if so, an additional objective was to determine the duration of this decreased concentration once phenylbutazone administration was discontinued. Serum TT4 and FT4 concentrations were determined before and after administration of 4.4 mg/kg of phenylbutazone i.v. bid for 5 days. Treatment with phenylbutazone caused a significant decrease in TT4 and FT4 concentrations (P < .05). Serum...
Plasma pharmacokinetics of ranitidine HCl in foals. Plasma pharmacokinetics of ranitidine HCl were investigated after intravenous (i.v.) and oral (p.o.) administration of drug to six healthy foals. Twelve- to sixteen-week-old foals received 2.2 mg ranitidine/kg i.v. and 4.4 mg ranitidine/kg p.o. Concentrations of ranitidine were determined using normal phase high performance liquid chromatography. Plasma concentrations of ranitidine HCl declined from a mean of 3266 ng/mL at 5 min to 11 ng/mL at 720 min after administration. The profile of the plot of concentrations of ranitidine HCl vs. time was best described by a two-exponent equation for two...
The pharmacokinetics of cefadroxil over a range of oral doses and animal ages in the foal. To evaluate the effect of foal age on the pharmacokinetics of cefadroxil, five foals were administered cefadroxil in a single intravenous dose (5 mg/kg) and a single oral dose (10 or 20 mg/kg) at ages of 0.5, 1, 2, 3 and 5 months. Pharmacokinetic parameters of terminal elimination rate constant (beta(po)), oral mean residence time (MRTpo), mean absorption time (MAT), rate constant for oral absorption (Ka), bioavailability F, peak serum concentrations (Cmax) and time of peak concentration (tmax), were evaluated in a repeated measures analysis over dose. Across animal ages, parameters for the in...
The effects of pentoxifylline infusion on plasma 6-keto-prostaglandin F1 alpha and ex vivo endotoxin-induced tumour necrosis factor activity in horses. Pentoxifylline (7.5 mg/kg) was bolused intravenously to eight healthy horses and was immediately followed by infusion (1.5 mg/kg/h) for 3 h. Clinical parameters were recorded and blood samples were collected for 24 h. Plasma was separated and concentrations of pentoxifylline, its reduced metabolite I, and 6-keto-prostaglandin F1 alpha were determined. Heparinized whole blood was also incubated ex vivo with 1 ng Escherichi coli endotoxin/mL blood for 6 h before determination of plasma tumour necrosis factor activity. The peak plasma concentrations of pentoxifylline and metabolite I occurred at ...
Role of oligosaccharides in the pharmacokinetics of tissue-derived and genetically engineered cholinesterases. To understand the role of glycosylation in the circulation of cholinesterases, we compared the mean residence time of five tissue-derived and two recombinant cholinesterases (injected intravenously in mice) with their oligosaccharide profiles. Monosaccharide composition analysis revealed differences in the total carbohydrate, galactose, and sialic acid contents. The molar ratio of sialic acid to galactose residues on tetrameric human serum butyrylcholinesterase, recombinant human butyrylcholinesterase, and recombinant mouse acetylcholinesterase was found to be approximately 1.0. For Torpedo ca...
Pharmacokinetics of cisapride in horses after intravenous and rectal administration. To determine the i.v. pharmacokinetics of cisapride and measure systemic absorption after rectal administration. Methods: 5 healthy adult mares (380 to 610 kg). Methods: Cisapride was administered, i.v., at a dosage of 0.1 mg/kg of body weight. In the same horses, after a 1-week washout period, cisapride was administered rectally at a dosage of 1 mg/kg by mixing crushed tablets with propylene glycol and administering the mixture into the rectum. After each drug administration, a series of blood samples were collected. Plasma was obtained and analyzed by high-performance liquid chromatography t...
Pharmacokinetics of intravenous and intragastric cimetidine in horses. I. Effects of intravenous cimetidine on pharmacokinetics of intravenous phenylbutazone. Cimetidine was administered intravenously and by the intragastric route to six mares at a dose of 4.0 mg/kg of body weight (bw). Specific and sensitive high performance liquid chromatographic methods for the determination of cimetidine in horse plasma and urine and cimetidine sulfoxide in urine are described. Plasma cimetidine concentration vs. time data were analysed by non-linear least squares regression analysis to determine pharmacokinetic parameter estimates. The median (range) plasma clearance (Cl) was 8.20 (4.96-10.2) mL/min.kg of body weight, that of the steady-state volume of distribu...
Pharmacokinetics of enrofloxacin in horses after single intravenous and intramuscular administration. Pharmacokinetic behaviour of enrofloxacin was studied in 6 horses after intravenous (i.v.) or intramuscular (i.m.) administration of enrofloxacin (5 mg/kg bwt). Concentration of enrofloxacin and ciproflaxin were measured by high performance liquid chromatography in serum. Antimicrobial activity of the samples was determined with an agar-diffusion technique. Reactions at the site of i.m. injection were monitored clinically and by determination of serum creatine kinase (CK) activity. After i.v. administration, elimination half-life of enrofloxacin was 4.4 h and volume of distribution was 2.3 1/k...
Age-related changes in the pharmacokinetic disposition of diazepam in foals. To evaluate changes in the pharmacokinetic disposition of diazepam in foals from 4 to 84 days of age. Methods: 4 male and 2 female full-term mixed-breed foals. Methods: Diazepam terminal half-life, volume of distribution, clearance, free fraction, unbound volume of distribution, free clearance, peak desmethyldiazepam concentration, and area under the desmethyldiazepam concentration-time curve were determined after i.v. administration of 0.25 mg of diazepam/kg of body weight to foals at 4, 21, 42, and 84 days of age. Results: Disposition of diazepam was best described using a two-compartment mo...
Pharmacokinetic study of dipyrone metabolite 4-MAA in the horse and possible implications for doping control. The pharmacokinetic behaviour of dipyrone metabolite 4-MAA in serum was determined in seven horses of different breeds after a single intravenous dose administration. A biexponential formula was fitted to the serum concentration vs. time data. The median half-life of the elimination phase (t1/2 beta) was 4.85 h (range 5.04 h), the median volume of distribution (Vd(area)) was 1.85 L/kg (range 3.2 L/kg) and median of total clearance was 4.0 mL/min/kg (range 2.3 mL/min/kg).
Plasma pharmacokinetics of ranitidine HCl in adult horses. Plasma pharmacokinetics of ranitidine HCl were investigated after intravenous (i.v.) and oral (p.o.) administration of 2.2 mg/kg drug to six healthy adult horses. Concentrations of ranitidine were determined using normal-phase, high-performance liquid chromatography. Plasma concentrations of ranitidine HCl declined from a mean of 5175 ng/mL at 5 min to 37 ng/mL at 720 min after i.v. administration. A three-exponent equation, Cp = A1 x e-k1t + A2 x e-k2t + A3 x e-k3t, best described data for all horses. Mean values for model-independent values calculated from the last quantifiable time point we...
High-performance liquid chromatographic determination of N-alpha-acetyl-L-carnosine in equine plasma. N-alpha-Acetyl-L-carnosine (NAcCAR) in perchloric acid extracts of equine plasma was assayed by high-performance liquid chromatography on a 3 microns Hypersil ODS (150 x 4.6 mm I.D.) column eluted with 5 mM phosphoric acid-1 mM triethylamine, pH 2.58. NAcCAR was isolated by solid-phase extraction on Isolute PRS (propylsulphonyl) columns. The HPLC mean retention time for NAcCAR was 5.9 +/- 0.2 min. The recovery from plasma by solid-phase extraction was 93.9-99.7% and lower limit of detection in plasma was 0.18 microM. The normal NAcCAR concentration in equine plasma was 2.4 +/- 0.3 microM. The ...
[Kinetics of elimination of diazepam after intravenous injection in horses]. Diazepam is used in veterinary medicine as sedative and pre-anaesthetic agent. This publication describes the plasma-concentration time curve for diazepam and its metabolite in horses suffering from colic after intravenous application as pre-anaesthetic agent. Elimination half-life (t1/2 beta) after a dose of 0.05-0.08 mg/kg (30-50 mg Diazepam per horse) was 7.5 to 13.2 h. Total clearance (Cltot) between 1.86 and 3.44 ml/min/kg was detected and apparent volume of distribution in steady state (Vdiss) was 1.98 to 2.25 l/kg. Diazepam was still found in serum after 24 h. The metabolite oxazepam co...
Plasma von Willebrand factor in thoroughbreds in response to high-intensity treadmill exercise. To determine whether plasma von Willebrand factor (vWf) concentration changes in horses during and after treadmill exercise. Methods: 5 mature, fit Thoroughbreds. Methods: A blood sampling catheter was placed in the right jugular vein. A warm-up period was followed by a 3-minute rest period. Horses were galloped at racing pace until fatigued (about 2 minutes). Blood samples were collected prior to warm-up, during the postwarm-up rest period, 1 minute into the run, at cessation of the run, and 5 to 120 minutes after cessation of the run. vWf activity was measured by ELISA and corrected for plas...
Pharmacokinetics of flunixin meglumine in healthy foals less than twenty-four hours old. To determine pharmacokinetic variables that describe the disposition of flunixin after i.v. administration of flunixin meglumine to foals < 24 hours old. Methods: 6 healthy foals, 2 males and 4 females (mean age, 11.6 hours; range, 6 to 22.5 hours). Methods: Flunixin (as flunixin meglumine) was administered to foals at a dosage of 1.1 mg/kg of body weight. Flunixin concentration in plasma samples was analyzed, using gas chromatography/mass spectroscopy. Concentration versus time profiles were analyzed according to standard pharmacokinetic techniques. Blood samples were obtained from foals b...
