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Topic:Pharmacokinetics

Pharmacokinetics in horses involves the study of how drugs are absorbed, distributed, metabolized, and excreted in equine species. This field of study provides insights into the time course of drug concentrations within the horse's body and helps in understanding the effects of various pharmaceuticals. Key parameters in equine pharmacokinetics include absorption rates, bioavailability, half-life, and clearance. These parameters can vary significantly due to factors such as age, breed, and health status of the horse. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetic profiles of different drugs in horses, aiming to optimize dosing regimens and improve therapeutic outcomes in equine medicine.
Bioavailability of ‘bute’.
The Veterinary record    June 25, 1983   Volume 112, Issue 26 595 doi: 10.1136/vr.112.26.595
No abstract available
Studies on a new paste preparation of phenylbutazone.
The Veterinary record    June 25, 1983   Volume 112, Issue 26 602-607 doi: 10.1136/vr.112.26.602
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...
Influence of acepromazine maleate on the equine haematocrit.
Journal of veterinary pharmacology and therapeutics    June 1, 1983   Volume 6, Issue 2 121-126 doi: 10.1111/j.1365-2885.1983.tb00388.x
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.
Diuretic effect of high-ceiling diuretics in ponies.
Journal of veterinary pharmacology and therapeutics    June 1, 1983   Volume 6, Issue 2 157-158 doi: 10.1111/j.1365-2885.1983.tb00394.x
Frey HH.No abstract available
Pharmacokinetics of phenytoin (diphenylhydantoin) in horses.
Journal of veterinary pharmacology and therapeutics    June 1, 1983   Volume 6, Issue 2 133-140 doi: 10.1111/j.1365-2885.1983.tb00390.x
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...
Effect of spasmolytic analgesic drugs on the motility patterns of the equine small intestine.
Research in veterinary science    May 1, 1983   Volume 34, Issue 3 334-339 
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...
The pharmacology of furosemide in the horse. V. Pharmacokinetics and blood levels of furosemide after intravenous administration.
Drug metabolism and disposition: the biological fate of chemicals    May 1, 1983   Volume 11, Issue 3 226-231 
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...
Pharmacokinetics and protein binding of morphine in horses.
American journal of veterinary research    May 1, 1983   Volume 44, Issue 5 870-874 
Combie JD, Nugent TE, Tobin T.Morphine could be detected in horses dosed with 0.1 mg of drug/kg of body weight for up to 48 hours in blood and 144 hours in urine. This dose of morphine elicited no observable effects and is a suggested analgesic dose. Computer analysis revealed that a 3-compartment open system was the best fitting model with a serum half life (t1/2(beta)) of 87.9 minutes and a urine t1/2(beta) of 101.1 minutes. Binding to equine serum proteins was linear over a drug concentration range of 3.88 X 10(-5)M to 3.50 X 10(-8)M and averaged 31.6%. In RBC-partitioning experiments, 78.1% of the drug was found in the...
The metabolism of fenclofenac in the horse.
Xenobiotica; the fate of foreign compounds in biological systems    April 1, 1983   Volume 13, Issue 4 233-240 doi: 10.3109/00498258309052259
Marsh MV, Caldwell J, Sloan TP, Smith RL, Horner M, Moss MS.14C-Fenclofenac (2-(2'-4'-dichlorophenoxy)-phenylacetic acid) was administered orally to horses, and urinary metabolites investigated by chromatography. Fenclofenac was rapidly absorbed and eliminated, with a plasma half-life (t1/2) of 2.3 h, with 83.2 and 85.8% of the dose being recovered in the urine in 0-24 h. The major urinary metabolite was the ester glucuronide (58.8, 70.0% dose), and evidence is presented that this metabolite undergoes a structural rearrangement to give beta-glucuronidase-resistant isomers. The other 14C-labelled components in horse urine were unchanged fenclofenac (13....
Trimethoprim-sulfadiazine in the horse: serum, synovial, peritoneal, and urine concentrations after single-dose intravenous administration.
American journal of veterinary research    April 1, 1983   Volume 44, Issue 4 540-543 
Brown MP, Kelly RH, Stover SM, Gronwall R.Six healthy adult mares were given a single IV injection of trimethoprim (TMP)-sulfadiazine (SDZ) at a dosage rate of 2.5 mg of TMP/kg of body weight and 12.5 mg of SDZ/kg. Serum, synovial, peritoneal, and urine TMP-SDZ concentrations were measured serially over a 48-hour period. The highest measured mean concentrations of TMP and SDZ were found in the first (0.5 hour) sample of serum, synovial fluid, and peritoneal fluid. The mean peak concentrations of TMP and SDZ averaged 4.37 micrograms/ml and 21.81 micrograms/ml for serum, 2.95 micrograms/ml and 15.31 micrograms/ml for synovial fluid, and...
Practical equine injectable anesthesia.
Journal of the American Veterinary Medical Association    March 15, 1983   Volume 182, Issue 6 574-577 
Geiser DR.No abstract available
The pharmacokinetics, plasma protein binding and time response relationships of 2-amino-5-phenyl-2-oxazolin-4-one (pemoline) in the horse.
Drug metabolism and disposition: the biological fate of chemicals    March 1, 1983   Volume 11, Issue 2 120-125 
Igwe OJ, Blake JW.The disposition kinetics of pemoline after iv and oral administration of 2.4 mg/kg of the drug were studied. The elimination half-life was 39.4 hr. The mean volume of distribution was 1.5 liters/kg indicating extensive tissue distribution and sequestration for an amphoteric drug. Plasma protein binding determined by in vitro equilibrium dialysis was concentration dependent. The mean binding capacity was found to be 0.80 mu-mol/g, an apparent dissociation constant of 3.73 X 10(-5) molar, and a total plasma protein concentration of 64.7 g/liter. The mean systemic availability by oral administrat...
Pharmacokinetics of erythromycin in foals and in adult horses.
Journal of veterinary pharmacology and therapeutics    March 1, 1983   Volume 6, Issue 1 67-73 doi: 10.1111/j.1365-2885.1983.tb00456.x
Prescott JF, Hoover DJ, Dohoo IR.The pharmacokinetic parameters of erythromycin in foals were determined following intravenous administration of 5.0 mg/kg to animals aged 1, 3, 5 and 7 weeks. The distribution of the drug was described by a two-compartment open model, and no significant differences were observed between coefficients on which the parameters were based. Pharmacokinetic values were also determined for four mares given 5.0 mg/kg intravenously and for six 10-12-week-old foals given 20.0 mg/kg intravenously. The half-life of erythromycin for all groups of animals (foals less than 7 weeks, mares, foals 10-12 weeks) w...
Gastrointestinal complications associated with the use of atropine in horses.
Journal of the American Veterinary Medical Association    February 1, 1983   Volume 182, Issue 3 229-231 
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...
Cortisol (hydrocortisone) disappearance rate and pathophysiologic changes after bilateral adrenalectomy in equids.
American journal of veterinary research    February 1, 1983   Volume 44, Issue 2 276-279 
Slone DE, Ganjam VK, Purohit RC, Ravis WR.Six ponies and 1 horse were bilaterally adrenalectomized (BADX). The survival time of 2 of the 7 animals after BADX was 24 and 72 hours without supplemental corticosteroids. The cause of death was not related to the surgical technique. The biological half-life of cortisol (hydrocortisone) was estimated to be 2.1 +/- 0.6 hours. The disappearance of cortisol in the horse was found to be biphasic, composed of redistribution and elimination phases. Pathophysiologic changes (ie, increased serum sodium and chloride, increased PCV, and decreased serum potassium) similar to those seen in other species...
Sodium retention and cortisol (hydrocortisone) suppression caused by dexamethasone and triamcinolone in equids.
American journal of veterinary research    February 1, 1983   Volume 44, Issue 2 280-283 
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...
Ticarcillin administration to the equine: Intrauterine and intramuscular.
Theriogenology    February 1, 1983   Volume 19, Issue 2 169-179 doi: 10.1016/0093-691x(83)90003-1
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...
Studies on the strongyle egg output of horses after treatment with oxfendazole (Synanthic vet. Syntex).
Nordisk veterinaermedicin    February 1, 1983   Volume 35, Issue 2 69-73 
Nilsson O, Klingborn B.The effect of oxfendazole (Synanthic vet. Syntex) on the strongyle egg output of naturally infected horses was evaluated. It was demonstrated that the compound, administered orally as an 18,5% paste or as 6,48% pellets mixed in feed (46.3 grams per 300 kg bodyweight) at a dose-rate of 10 mg per kg bodyweight, markedly reduced the strongyle egg output over a 10 week period. As this period to egg reappearance is considerably longer than for most other anthelmintics at recommended dose levels, oxfendazole may be considered a valuable compound for the control of strongylosis in horses.
Critical tests in equids with fenbendazole alone or combined with piperazine: particular reference to activity on benzimidazole-resistant small strongyles.
Veterinary parasitology    February 1, 1983   Volume 12, Issue 1 91-98 doi: 10.1016/0304-4017(83)90092-4
Lyons ET, Tolliver SC, Drudge JH.Seven critical tests in equids were conducted with single doses of fenbendazole (5 mg kg-1) alone (Panacur--American Hoechst, Somerville, NJ); (2 tests with paste and 1 with suspension formulation) or in combination with piperazine (American Hoechst); (40 mg base kg-1); (4 tests with paste formulation). The main purpose of the tests was evaluation of activity against benzimidazole-resistant small strongyles (Cyathostomum catinatum, Cyathostomum coronatum, Cylicocyclus nassatus, Cylicostephanus goldi, and Cylicostephanus longibursatus). Natural infections of 2 populations of benzimidazole-resis...
Thermographic evaluation of corticosteroid efficacy in amphotericin B-induced arthritis in ponies.
American journal of veterinary research    January 1, 1983   Volume 44, Issue 1 51-56 
Bowman KF, Purohit RC, Ganjam VK, Pechman RD, Vaughan JT.No abstract available
Pharmacology, pharmacokinetics, and behavioral effects of caffeine in horses.
American journal of veterinary research    January 1, 1983   Volume 44, Issue 1 57-63 
Greene EW, Woods WE, Tobin T.Caffeine (4 mg/kg) was given by rapid IV injection to 4 horses. Plasma concentrations of the drug peaked at 10 micrograms/ml and decreased rapidly at first, and then more slowly, with an apparent beta-phase half-life of 18.2 hours. Urinary concentrations of caffeine were remarkably consistent at about 3 times plasma values of the drug. Caffeine was detectable in both plasma and urine of the horses for up to 9 days after dosing. After oral administration, caffeine was absorbed poorly with an apparent bioavailability of 39%. Although blood concentrations of caffeine peaked rapidly after oral adm...
Serum concentrations of penicillin in the horse after administration of a variety of penicillin preparations.
Equine veterinary journal    January 1, 1983   Volume 15, Issue 1 43-48 doi: 10.1111/j.2042-3306.1983.tb01700.x
Love DN, Rose RJ, Martin IC, Bailey M.Twelve geldings were used to evaluate serum levels of penicillin following the intravenous (iv) and intramuscular (im) injection of benzylpenicillin, im procaine penicillin and im fortified benzathine penicillin, at a variety of dose rates. Blood samples were collected up to 7 h after iv and im benzylpenicillin, up to benzathine penicillin. Results were analysed using an analysis of variance and regression analyses were used to calculate the time taken for the serum penicillin concentration to decline to 0.5 micrograms/ml. As a result of the experiments the following dosage regimes could be re...
Serum protein binding of furosemide in several species.
Journal of veterinary pharmacology and therapeutics    December 1, 1982   Volume 5, Issue 4 293-294 doi: 10.1111/j.1365-2885.1982.tb00446.x
Neff-Davis CA, Davis LE.No abstract available
Pulmonary effects of intravenous histamine in the conscious pony: dose-response relationships and reproducibility.
American journal of veterinary research    December 1, 1982   Volume 43, Issue 12 2134-2137 
Derksen FJ, Slocombe RF, Robinson NE.In standing sedated ponies, we measured dynamic lung compliance (Cdyn) and pulmonary resistance (RL) during IV infusion of various doses of histamine; this was done in a given pony 3 times at 1-week intervals between experiments. Histamine doses causing a decrease in Cdyn of 50% and 75% and an increase in RL of 300% and 600% (ED50Cdyn, ED75Cdyn, ED300RL and ED600RL, respectively) were interpolated from the histamine dose-response curves. We also measured respiratory frequency, tidal volume, minute ventilation, functional residual capacity, arterial oxygen tension, arterial carbon dioxide tensi...
The uptake of mepacrine by horse polymorphonuclear leucocytes in vitro.
The Journal of pharmacy and pharmacology    November 1, 1982   Volume 34, Issue 11 711-714 doi: 10.1111/j.2042-7158.1982.tb06205.x
Read NG, Trist DG.The uptake of mepacrine by isolated horse polymorphonuclear leucocytes (PMN) was measured using spectrophotofluorimetry. Two phases of uptake were observed, the first, rapid fraction, essentially complete by 10 min, and a second, slow fraction, which was still proceeding after 60 min. The appearance of mepacrine within the PMN was also visualized by fluorescence microscopy. Discrete yellow points of fluorescence were observed in the cytoplasm of PMN within 30 s. These discrete points corresponded both in size and number to the PMN granules. After 5 min, the nuclei showed faint fluorescence whi...
Hypotension in the horse induced by acepromazine maleate.
Australian veterinary journal    November 1, 1982   Volume 59, Issue 5 148-152 doi: 10.1111/j.1751-0813.1982.tb02761.x
Parry BW, Anderson GA, Gay CC.The hypotensive effect of acepromazine maleate was related to both the dose and route of administration. The degree and duration of hypotension varied between individual horses. In general, intravenous administration produced a more rapid maximum effect than intramuscular injection and the larger the dose the longer blood pressure remained at low levels. Average systolic pressure (of 6 horses) remained significantly below control values for more than 6 h after an intramuscular injection of 0.05 mg acepromazine maleate/kg body weight. Respiratory rate was markedly decreased, with the duration, ...
Paste formulation of phenylbutazone.
The Veterinary record    October 9, 1982   Volume 111, Issue 15 353 doi: 10.1136/vr.111.15.353-a
Snow DH.No abstract available
Effect of experimental uterine tube occlusion on plasma penicillin concentrations following intrauterine instillation in pony mares.
Equine veterinary journal    October 1, 1982   Volume 14, Issue 4 336-337 doi: 10.1111/j.2042-3306.1982.tb02449.x
Ayliffe TR, Allen WE.PREVIOUS studies have shown that instillation of sodium benzylpenicillin into the uterine lumen of ponies in small volumes is followed by peak plasma concentrations of the antibiotic in 10to 15 mins (Allen 1978; Allen and Clarke 1978). However, the assumption that the circulating penicillin is absorbed only through the endometrium is questionable because Allen, Kessy and Noakes (1979) concluded that the intrauterine instillation of phenolsulphonphthalein was followed by absorption of the dye from the peritoneal cavity, after passage along the uterine tubes. The present investigation was carri...
Pharmacodynamic and pharmacokinetic properties of diazepam in horses.
American journal of veterinary research    October 1, 1982   Volume 43, Issue 10 1756-1762 
Muir WW, Sams RA, Huffman RH, Noonan JS.The cardiopulmonary, behavioral, and pharmacokinetic properties of diazepam were determined in horses. Heart rate, cardiac output, mean pulmonary artery, aortic and right atrial blood pressures, respiratory rate, and arterial pH and blood gas values did not change after IV diazepam (0.05, 0.1, 0.2, 0.4 mg/kg) administration. Increasing doses of diazepam resulted in signs of muscle weakness including fixed stance, muscle fasciculations of the head, neck, and thorax muscles, ataxia, and then recumbency. Dosages of diazepam exceeding 0.2 mg/kg produced mild sedation. Behavioral changes persisted ...
[Radioimmunologic determination of triamcinolone acetonide levels in equine plasma].
Berliner und Munchener tierarztliche Wochenschrift    September 1, 1982   Volume 95, Issue 17 325-330 
Gylstorff B, Hegner D.No abstract available
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