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Topic:Drug

The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
[The concentration changes of different phenylbutazone formulations in horse plasma].
DTW. Deutsche tierarztliche Wochenschrift    June 1, 1996   Volume 103, Issue 6 224-230 
Keller H, Hashem A.In a study in the horse, the disposition, the pharmacokinetic parameters and the absorption rates of 3 formulations of phenylbutazone (injection solution, powder and paste suspension) have been determined. After i.v. injection, the half-life time of phenylbutazone has been determined to be 6.6-6.7 h. After oral administration, the absorption of phenylbutazone was found to be faster after administration via stomach tube than after direct application into the mouth. The absorption rat constant of the paste suspension was found to be higher than that of the powder (1.797-2.304 h-1 vs. 0.656-1.197...
Detection of quinine and its metabolites in horse urine by gas chromatography-mass spectrometry.
The Analyst    May 1, 1996   Volume 121, Issue 5 651-662 doi: 10.1039/an9962100651
Demir C, Brereton RG, Dumasia MC.After oral administration of quinine sulfate to a thoroughbred mare, seven urine samples were obtained over a 45.5 h period. Using gas chromatography -electron impact ionization and positive-ion chemical ionization mass spectrometry, quinine and five putative metabolites were detected and tentatively identified in enzyme-hydrolysed post-administration urine; all metabolites involved some form of oxidation. The parent drug could be detected for about 16 h and some phase I biotransformation products for up to 40 h post-administration.
Effects of U-74389G, a novel 21-aminosteroid, on small intestinal ischemia and reperfusion injury in horses.
American journal of veterinary research    May 1, 1996   Volume 57, Issue 5 762-770 
Vatistas NJ, Snyder JR, Hildebrand SV, Harmon FA, Woliner MJ, Barry SJ, Nieto J, Henry P, Enos LR, Magliano D, Brown SA, Drake C.To determine the effects of the 21-aminosteroid, U-74389G, on reperfusion of the equine jejunum, using total (TVO) and partial (PVO) vascular occlusion during the ischemic period. Methods: TVO: 16 healthy horses were randomly allotted to 3 groups-4 horses received the vehicle alone, 6 horses received a low dosage (3 mg/kg o body weight), and 6 horses a high dosage (10 mg/kg) of U-7438G. PVO: 10 healthy horses were randomly allotted to 2 groups--5 horses received the vehicle alone, and 5 horses received the low dosage (3 mg/kg) of U-74389G. Methods: TVO was induced for 1 hour followed by 2 hour...
Serum can inhibit reversal of multidrug resistance by chemosensitisers.
European journal of cancer (Oxford, England : 1990)    May 1, 1996   Volume 32A, Issue 5 862-867 doi: 10.1016/0959-8049(96)00004-4
Lehnert M, de Giuli R, Kunke K, Emerson S, Dalton WS, Salmon SE.The purpose of this study was to evaluate to what extent the ability of various chemosensitisers (CS) to reverse P-glycoprotein-associated multidrug resistance (MDR) is reduced when tested in physiological serum protein concentrations. Utilising drug sensitivity and accumulation assays, the CS were tested in medium containing 10% fetal bovine serum and in 100% horse or human serum. Two RPMI 8226 human myeloma sublines were used which express different levels of P-glycoprotein. The CS were tested at various concentrations, including clinically achievable blood levels. When using the CS at high ...
Determination of phenylbutazone and oxyphenbutazone in plasma and urine samples of horses by high-performance liquid chromatography and gas chromatography-mass spectrometry.
Journal of chromatography. B, Biomedical applications    April 12, 1996   Volume 678, Issue 2 211-218 doi: 10.1016/0378-4347(95)00508-0
Neto LM, Andraus MH, Salvadori MC.A method is described for the qualitative and quantitative determination of phenylbutazone and oxyphenbutazone in horse urine and plasma samples viewing antidoping control. A horse was administered intravenously with 3 g of phenylbutazone. For the qualitative determination, a screening by HPLC was performed after acidic extraction of the urine samples and the confirmation process was realized by GC-MS. Using the proposed method it was possible to detect phenylbutazone and oxyphenbutazone in urine for up to 48 and 120 h, respectively. For the quantitation of these drugs the plasma was deprotein...
Ultrasonographic renal changes associated with phenylbutazone administration in three foals.
The Canadian veterinary journal = La revue veterinaire canadienne    April 1, 1996   Volume 37, Issue 4 235-236 
Léveillé R, Miyabayashi T, Weisbrode SE, Biller DS, Takiguchi M, Williams JF.No abstract available
Adverse drug reactions: report of the Australian Veterinary Association Adverse Drug Reaction Subcommittee, 1994.
Australian veterinary journal    April 1, 1996   Volume 73, Issue 4 132-136 doi: 10.1111/j.1751-0813.1996.tb10005.x
Maddison JE.Seventy-seven reports of suspected adverse drug reactions (ADRs) were received by the Adverse Drug Reaction Subcommittee (ADRSc) of the Australian Veterinary Association from April 1993 to December 1994 inclusive. The number of reports received/number of animals involved per species were: dogs (32/44), cats (18/31), horses (17/48), and cattle (10/21). Of these, 49 (64%) were classified as definite ADRs and 9 (12%) as probable ADRs. In 11 (14%) reports an ADR could not be substantiated or there was insufficient information available to make a decision. Eight reports were not classified because ...
Prothipendyl: detection and elimination in the horse–a case report.
DTW. Deutsche tierarztliche Wochenschrift    April 1, 1996   Volume 103, Issue 4 125-127 
Hagedorn HW, Zuck S, Schulz R.The azaphenothiazine neuroleptic prothipendyl (Dominal) is suspected to be administered illegally at low doses to race-horses to improve their performance. Since for this species pharmacokinetic data of the drug are missing we studied its elimination from blood and urine in a standard-bred mare. At a low (subtherapeutic) dose (i.v., 0.24 mg/kg) the horse is described to be less excited while locomotor activity and attention remain unaffected. In contrast, sedation and ataxia are brought about at 1 mg/kg (therapeutic dose). Identification of prothipendyl given i.v. at subtherapeutic doses was a...
Evaluation of propofol for general anesthesia in premedicated horses.
American journal of veterinary research    April 1, 1996   Volume 57, Issue 4 512-516 
Mama KR, Steffey EP, Pascoe PJ.To evaluate selected hemodynamic, respiratory, and behavioral responses to propofol in horses premedicated with xylazine or detomidine. Methods: Xylazine (0.5 and 1.0 mg/kg of body weight) was administered IV on different days to each of 6 horses prior to IV administration of propofol (2 mg/kg). In a second group of 6 horses, detomidine (15 and 30 micrograms/kg) was similarly studied. Methods: 2 groups of 6 mature healthy horses. Methods: Rectal temperature, heart and respiratory rates, arterial blood gas tensions, and direct arterial blood pressures were recorded before and at fixed intervals...
Regulatory significance of procaine residues in plasma and urine samples: preliminary communication.
Equine veterinary journal    March 1, 1996   Volume 28, Issue 2 121-125 doi: 10.1111/j.2042-3306.1996.tb01603.x
Harkins JD, Mundy GD, Stanley S, Woods WE, Boyles J, Arthur RA, Sams RA, Tobin T.Plasma and urinary concentrations of procaine and the duration of response to procaine after its administration as a local anaesthetic to horses were studied. Following injection of a clinical dose of procaine HCl (80 mg), the concentration of procaine in plasma was less than the lower limit of quantitation and unsuitable for threshold determination. Therefore, the urinary concentration of procaine was determined after injection of a dose of 5 mg procaine HCl, the highest no-effect dose (HNED) of this agent. Free unconjugated procaine in equine urine reached a peak concentration of 23.7 ng/mL,...
Effects of sodium bicarbonate and sodium chloride on the elimination of etorphine in equine urine.
Journal of analytical toxicology    March 1, 1996   Volume 20, Issue 2 81-88 doi: 10.1093/jat/20.2.81
Lloyd DR, Rose RJ, Duffield AM, Suann CJ.The combination of large doses of sodium bicarbonate and the potent narcotic, etorphine, has reportedly been given to racehorses in attempts to improve their performance and also to "mask" the presence of etorphine in urine samples. The increased urinary output and pH associated with sodium bicarbonate (approximately 500 g) administration may reduce the urinary concentration of etorphine, making it more difficult to detect. Our experiment was designed to examine the effects of this combination. Six Thoroughbred horses were used in a latin-square design with three horse pairs and three treatmen...
Tissue and serum concentrations of amikacin after intramuscular and intrauterine administration to mares in estrus.
The Canadian veterinary journal = La revue veterinaire canadienne    March 1, 1996   Volume 37, Issue 3 157-160 
Orsini JA, Park MI, Spencer PA.Concentrations of amikacin in endometrial tissue and plasma were studied in mares in estrus after intrauterine infusion of 1.0 or 2.0 g once a day for 3 consecutive d, and after 9.7 or 14.5 mg/kg body weight (BW) had been injected intramuscularly once a day for 3 consecutive d to determine concentrations of amikacin sulfate in plasma and endometrial tissues, and whether parenteral administration provides any advantages over intramuscular infusion. No amikacin was detected in serum at the 1.0 g dose. At the infusion dose of 2.0 g once a day, very low levels of serum amikacin were detected at 1 ...
Pharmacokinetics of lignocaine in Icelandic horses after infiltration anaesthesia.
The Veterinary record    February 3, 1996   Volume 138, Issue 5 111-112 doi: 10.1136/vr.138.5.111
Kristinsson J, Thordarson TH, Johannesson T.The pharmacokinetics of lignocaine was studied in four Icelandic horses after infiltration anaesthesia. A total of 240 mg of the drug was injected on either side of the left foreleg, over the medial and lateral branches of the palmar nerve. Blood samples were collected up to seven hours after injection and the concentrations of the drug in plasma were determined by gas chromatography/mass spectrometry. The results showed that lignocaine was rapidly absorbed. A mean maximum concentration of 232 ng/ml was observed after 20 minutes. In three of the horses the decline in the plasma concentration o...
The pharmacokinetics of dexamethasone in the thoroughbred racehorse.
Journal of veterinary pharmacology and therapeutics    February 1, 1996   Volume 19, Issue 1 68-71 doi: 10.1111/j.1365-2885.1996.tb00011.x
Cunningham FE, Rogers S, Fischer JH, Jensen RC.No abstract available
Plasma, urine, and synovial fluid disposition of methylprednisolone acetate and isoflupredone acetate after intra-articular administration in horses.
American journal of veterinary research    February 1, 1996   Volume 57, Issue 2 187-192 
Lillich JD, Bertone AL, Schmall LM, Ruggles AJ, Sams RA.OBJECTIVE--To document plasma, urine, and synovial fluid disposition of 2 common intra-articularly administered steroid preparations, methylprednisolone acetate (MPA) and isoflupredone acetate (IPA). DESIGN--Descriptive investigation. SAMPLE POPULATION--100 mg of MPA or 4 mg of IPA was administered to 2 groups of 4 healthy sound radiographically normal female horses. PROCEDURE--Blood samples were collected at time 0 (before) and 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours after administration of the designated steroid. Complete urine collection for measurement of designated steroid was ac...
Pharmacokinetics of cefoperazone in horses.
Journal of veterinary pharmacology and therapeutics    February 1, 1996   Volume 19, Issue 1 39-43 doi: 10.1111/j.1365-2885.1996.tb00006.x
Soraci AL, Mestorino ON, Errecalde JO.The pharmacokinetics and bioavailability of cefoperazone (CPZ) were studied following intravenous (IV) and intramuscular (IM) administration of single doses (30 mg/kg) to horses. Concentrations in serum, urine and synovial fluid samples were measured following IV administration. CPZ concentrations in serum, synovial fluid and spongy bone samples were measured following IM administration. After IV administration a rapid distribution phase (t1/2 (alpha): 4.22 +/- 2.73 min) was followed by a slower elimination phase (t1/2(beta) 0.77 +/- 0.19 h). The apparent volume of distribution was 0.68 +/- 0....
Use of enzyme-linked immunosorbent assay and radioimmunoassay to determine serum and urine dexamethasone concentrations in thoroughbreds after intravenous administration of the steroid.
American journal of veterinary research    February 1, 1996   Volume 57, Issue 2 182-186 
Chen CL, Zhu D, Gillis KD, Meleka-Boules M.To develop a simple and sensitive ELISA for detection of dexamethasone in horse serum and urine. Methods: Blood and urine samples from 3 thoroughbred mares. Methods: A dexamethasone oxime was prepared and conjugated to hemocyanin, bovine serum albumin and to horseradish peroxidase. One- and two-step double-antibody ELISA methods, as well as a radioimmunoassay method, were performed. The one-step ELISA was used to test urine from 3 Thoroughbred mares injected with 5 mg of dexamethasone, IV. Results: The ELISA could detect dexamethasone in the range of 0.01 to 50 ng/ml, with intra- and interassa...
Detection of non-steroidal anti-inflammatory drugs in equine plasma and urine by gas chromatography-mass spectrometry.
Journal of chromatography. A    January 5, 1996   Volume 719, Issue 1 251-264 doi: 10.1016/0021-9673(95)00370-3
González G, Ventura R, Smith AK, de la Torre R, Segura J.A gas chromatographic-mass spectrometric (GC-MS) procedure for the detection of seventeen non-steroidal anti-inflammatory drugs (NSAIDs) in equine plasma and urine samples is described. The extraction of the compounds from the biological matrix was performed at acidic pH (2-3) with diethyl ether. Ethereal extracts were washed with a saturated solution of sodium hydrogencarbonate (urine) or treated with a solid mixture of sodium carbonate and sodium hydrogencarbonate (plasma). The ethereal extracts were dried and derivatized by incubation at 60 degrees C with methyl iodide in acetone in the pre...
Drug use and misuse: frontiers between biological science, bureaucracy and clinical pragmatism.
Equine veterinary journal    January 1, 1996   Volume 28, Issue 1 7-8 doi: 10.1111/j.2042-3306.1996.tb01581.x
Rossdale PD.No abstract available
Determination of highest no effect dose (HNED) for local anaesthetic responses to procaine, cocaine, bupivacaine and benzocaine.
Equine veterinary journal    January 1, 1996   Volume 28, Issue 1 30-37 doi: 10.1111/j.2042-3306.1996.tb01587.x
Harkins JD, Mundy GD, Stanley S, Woods WE, Rees WA, Thompson KN, Tobin T.The highest no effect doses (HNEDs) for the local anaesthetic (LA) effects of procaine, cocaine, bupivacaine and benzocaine were determined using the heat lamp/hoof withdrawal model of Kamerling et al. (1985b) and the abaxial sesamoid block model of local anaesthesia. The heat lamp rapidly (4 or 5 s) increased the temperature of the superficial skin layers of the pastern to about 90 degrees C, at which point the animal sharply withdrew its hoof. Effective LA blockade precluded this response and superficial skin temperatures exceeded 120 degrees C. Thermal stimulus experiments were routinely te...
A comparison of N-butylscopolammonium bromide and butorphanol tartrate for analgesia using a balloon model of abdominal pain in ponies. Boatwright CE, Fubini SL, Grohn YT, Goossens L.The analgesic effect of N-butylscopolammonium bromide (0.3 mg/kg) using a balloon-induced model of colic in ponies was evaluated and compared with butorphanol tartrate (0.1 mg/kg). Eight adult ponies were used and each received both treatments during the two different trials. The order in which the treatment was received was randomly assigned. At the start of each trial, moderate abdominal pain was induced by inflation of a balloon placed in the lumen of the caecum. The ponies were evaluated every 5 minutes, and a cumulative pain score (CPS) was assigned. Two baseline measurements were recorde...
A partially automated pretreatment module for routine analyses for seventeen non-steroid antiinflammatory drugs in race horses using gas chromatography/mass spectrometry.
Analytical chemistry    January 1, 1996   Volume 68, Issue 1 118-123 doi: 10.1021/ac950566j
Cárdenas S, Gallego M, Valcárcel M, Ventura R, Segura J.A partially automated module for the routine determination of illicit non-steroid antiinflammatory drugs (NSAIDs) in biological fluids from race horses was built, tested, refined, and shown to work. This pretreatment module retains 17 NSAIDs on an Amberlite XAD-2 column before back-elution derivatization with methyl iodide in acetonitrile. Methylated derivatives are manually injected into a gas chromatograph connected to a mass spectrometer. The quantification limits thus achieved are 50-100 ng/mL in 1 mL of urine or plasma. The proposed method is more expeditious than its manual liquid-liquid...
Establishing the cut-off concentration for the detection of etorphine in horse urine.
The Analyst    January 1, 1996   Volume 121, Issue 1 67-69 doi: 10.1039/an9962100067
Smith RF, Jackson LS, Moore A.An 125I radioimmunoassay to determine the pattern of urinary excretion of etorphine (a semisynthetic opiate agonist) after its administration to horses is described. Three thoroughbred horses were each given 5, 15, 30 and 100 micrograms of etorphine intramuscularly. Urine was collected for up to 72 after administration. The maximum etorphine concentration after administration of a dose of 5 micrograms was 711 pg ml-1 (concentrations were greater than 100 pg ml-1 after 23 h in all three horses); a 15 micrograms gave 2661 pg ml-1 (levels remained above 100 pg ml-1 for more than 44 h in each hors...
Desflurane in equine anaesthesia: a preliminary trial.
The Veterinary record    December 9, 1995   Volume 137, Issue 24 618-620 
Jones NY, Clarke KW, Clegg PD.No abstract available
A review of the pharmacology, pharmacokinetics, and regulatory control in the US of local anaesthetics in the horse.
Journal of veterinary pharmacology and therapeutics    December 1, 1995   Volume 18, Issue 6 397-406 doi: 10.1111/j.1365-2885.1995.tb00616.x
Harkins JD, Stanley S, Mundy GD, Sams RA, Woods WE, Tobin T.No abstract available
Drugs coordinating and restoring gastrointestinal motility and their effect on selected hypodynamic gastrointestinal disorders in horses and cattle.
Zentralblatt fur Veterinarmedizin. Reihe A    December 1, 1995   Volume 42, Issue 10 613-631 doi: 10.1111/j.1439-0442.1995.tb00416.x
Steiner A, Roussel AJ.Hypodynamic gastrointestinal disorders in horses and cattle that are thought to benefit from treatment with drugs restoring and coordinating gastrointestinal motility include postoperative ileus and large colon impaction in the horse and displacement of the abomasum and dilatation of the cecum in cattle. Important physiologic, pathophysiologic and pharmacologic mechanisms involved in the intrinsic control of gastrointestinal motility include cholinergic, adrenergic, dopaminergic, serotoninergic, and opioid-mediated pathways. Preliminary results suggest that cisapride, acting on 5-Hydroxytrypta...
The pharmacokinetics or oral and intravenous allopurinol and intravenous oxypurinol in the horse.
Journal of veterinary pharmacology and therapeutics    December 1, 1995   Volume 18, Issue 6 451-456 doi: 10.1111/j.1365-2885.1995.tb00625.x
Mills PC, Dunnett M, Smith NC.The pharmacokinetics of oral and intravenous allopurinol was studied in five horses and compared with intravenous oxypurinol. The plasma concentration vs. time curves, following intravenous administration of 5 mg/kg, were best described by the biexponential equations Cp = 106.58e(-25.14t) + 159.93e(-10.96t) for allopurinol and Cp = 321.09e(-9.72t) + 82.39e(-0.44t) for oxypurinol, with an elimination half-life (t1/2 beta) of 0.09 h and an area under the curve (AUC) of 19.8 mumol.h/L after intravenous administration, while the t1/2 beta and AUC of oxypurinol were 1.09 h and 231 mumol.h/L, respec...
The dose-related effects of phenylbutazone and a methylprednisolone acetate formulation (Depo-Medrol) on cultured explants of equine carpal articular cartilage.
Journal of veterinary pharmacology and therapeutics    December 1, 1995   Volume 18, Issue 6 429-437 doi: 10.1111/j.1365-2885.1995.tb00621.x
Jolly WT, Whittem T, Jolly AC, Firth EC.The dose-related effects of phenylbutazone and Depo-Medrol on chondrocyte viability and chondrocyte-mediated synthesis and depletion of proteoglycans were investigated using cultured explants of equine middle carpal joint articular cartilage. Explants from 12 horses (941 x 3 mm diameter) were cultured for a total of 5 days, which included 3 days' exposure to either phenylbutazone (0, 2, 20, 200 or 2000 micrograms/mL) or Depo-Medrol (0, 20, 200 or 2000 micrograms/mL). For each explant, amino sugar content was used as a measure of proteoglycan content, 35S incorporation as a measure of the rate ...
Influence of formulation on the pharmacokinetics and bioavailability of racemic ketoprofen in horses.
Journal of veterinary pharmacology and therapeutics    December 1, 1995   Volume 18, Issue 6 446-450 doi: 10.1111/j.1365-2885.1995.tb00624.x
Landoni MF, Lees P.The bioavailability of S(+) and R(-) ketoprofen (KTP) in six horses was investigated after oral administration of the racemic (rac) mixture. Two oral formulations were studied, an oil-based paste containing micronised rac-KTP and powder from the same source in hard gelatin capsules, each at a dose rate of 2.2 mg/kg. For the oil-based paste two feeding schedules were used; horses were either allowed free access to food or access to food was restricted for 4 h before and 5 h after dosing. The drug in hard gelatin capsules was administered to horses with restricted access to food. After intraveno...
Pharmacokinetics and therapeutic potential for repeated oral doses of trimethoprim/sulphachlorpyridazine in horses.
The Veterinary record    November 4, 1995   Volume 137, Issue 19 483-486 doi: 10.1136/vr.137.19.483
van Duijkeren E, Sloet van Oldruitenborgh-Oosterbaan MM, Vulto AG, Kessels BG, van Miert AS, Breukink HJ.The pharmacokinetic parameters of a powder formulation of trimethoprim/sulphachlorpyridazine were studied in eight healthy horses which received 5 mg/kg trimethoprim and 25 mg/kg sulphachlorpyridazine 12-hourly with concentrate for five days. The intake of the medicated concentrate by the horses was variable during the first two days, but after they became accustomed to the taste the intake by all the horses during the last three days was good. Faecal samples taken before and on the last day of the drug administrations were negative when cultured for salmonella. Compared with the results of a ...
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