ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00117.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Dorrestein, G.M.&van Miert, A.S.J.P.A.M. Pharmacotherapeutic aspects of medication of birds. J. vet. Pharmacol. Therap. 11, 33–44.This review covers current knowledge of the pharmacodynamics and pharmacokinetics of drugs in avian species. Special attention has been paid to inter‐species differences in relation to metabolic elimination, anatomy and physiology of the digestive and respiratory system, and differences in drug distribution. Intra‐species differences attributable to physicochemical aspects of the drug preparation and physiological conditions of the avian patient can also influence drug efficacy. The consequences of the choice of a particular method of drug administration on pharmacokinetics are also consi

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00118.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Laber, G. Investigation of pharmacokinetic parameters of tiamulin after intramuscular and subcutaneous administration in normal dogs.J. vet. Pharmacol. Therap.11, 45–49.Kinetic variables for tiamulin in the normal dog have been determined. Serum concentrations of tiamulin were compared after intramuscular (i.m.) and subcutaneous (s.c.) administration of a single dose of tiamulin. Following a single i.m. dose of 10 mg/kg body weight, the compound was calculated to have a Cmax= 0.61 ± 0.15 μg/ml, aTmax= 6 h and at½= 4.7 ± 1.4 h. Tiamulin showed dose‐dependent pharmacokinetics when given as a single s.c. dose of either 10 mg or 25 mg/kg body weight. For the lower dose, the values Cmax= 1.55 ± 0.11 μg/ml,Tmax= 8 h and1max= 4.28 ± 0.18 h were obtained. For the higher doseCmax= 3.14 ± 0.04 μg/ml,Tmax= 8 h andt½= 12.4 ± 3.4 h were calculated. When tiamulin was administered subcutaneously at a dose rate of 10 mg/kg body weight, higher and better maintained serum levels were achieved than those following i.m. administration. After repeated s.c. doses no significant accumulation of tiamulin occurred. Assuming that a continuous effective serum concentration is necessary throughout the course of therapy, these data would indicate that tiamulin should be gi

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00119.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Short, C.R., Flory, W., Hsieh, L.C.&Barker, S.A. The oxidative metabolism of fenbendazole: a comparative study.J, vet. Pharmacol. Therap.11, 50–55.The oxidative metabolism of fenbendazole (FBZ) was studied in hepatic fractions prepared from livers of cattle, sheep, goats, chickens, ducks, turkeys, rats, rabbits and catfish. All species produced the sulfoxide metabolite (oxfendazole; FBZ‐SO), andp‐hydroxyfenbendazole (FBZ‐OH) was produced by all species except sheep. The product of demethoxycarbonylation, fenbendazole amine (FBZ‐NH2), was not produced by liver preparations of any species. A fourth metabolite, resulting from the further oxidation of oxfendazole, fenbendazole sulfone (FBZ‐S02), was formed in all species but at highly varying rates. The chicken exhibited the highest overall rate of FBZ metabolism, followed by the duck, goat, sheep, steer, catfish, rat, rabbit, and turkey. Considerable variation was evident among avian species, the duck and turkey produced substantially less of the FBZ‐OH and FBZ‐SO2metabolites than the chicken. Catfish liver preparations formed equivalent amounts of metabolite at 25oC and 37oC incubation temperatures. The formation of the sulfone metabolite (FBZ‐SO2), however, was practically nonex

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00120.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Firth, E.C., Klein, W.R., Nouws, J.F.M.&Wensing, Th. Effect of induced synovial inflammation on pharmacokinetics and synovial concentration of sodium ampicillin and kanamycin sulfate after systemic administration in ponies. J. vet. Pharmacol. Therap. 11, 56–62.Single doses of sodium ampicillin (10 mg/kg) and kanamycin sulfate (5 mg/kg) were administered intramuscularly (i.m.) separately, and then together, to five pony mares. The plasma antibiotic concentration–time curves were constructed. The pharmacokinetic parameters of the antibiotics given separately were not altered by concurrent administration. Four of the five pony mares were then given the i.m. kanamycin/ampicillin combination 4 h after acute synovitis and fever had been induced by injection of lipopolysaccharide into the left intercarpal joint. The plasma concentration–time curves and the synovial concentration–time curves of inflamed and normal joints were constructed. The Cmaxof ampicillin in the lipopolysaccharide experiment was significantly higher than in the other experiments. The antibiotics entered the synovial fluid of the inflamed joints more quickly and attained higher concentrations than in the uninflamed joints. The ampicillin concentration exceeded 5 Jig/ml in inflamed synovial fluid for some 2.5 h after injection, and kanamycin sulfate concentration exceeded 2 μ.g/ml

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00121.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Monbaliu, J., Degryse, A.‐D., Ooms, L.A.A., Van Dijk, P., Lagerweij, E., Michiels, M., Woestenborghs, R.&Heykants, J. Hypnoanalgesia with R 8110/ fentanyl in the dog: pharmacodynamic and pharmacokinetic interactions.J. vet. Pharmacol. Therap.11, 63–70.The pharmacokinetics and clinical effects of the short‐acting hypnotic R 8110 and of the narcotic analgesic fentanyl were studied in the dog. The effects of separate intravenous (i.v.) injections of R 8110 (4 mg/kg) and fentanyl (0.015 mg/kg) and of concurrent i.v. injection of the two were studied. After administration of R 8110, induction of hypnosis occurred within 1 min, maximal depth of anaesthesia and satisfactory analgesia and muscle relaxation were obtained after 5 min. The effects had decreased within 15 min and full recovery occurred within 30 min. Fentanyl alone produced neither hypnosis nor muscle relaxation. When fentanyl and R 8110 were given simultaneously, the duration of hypnosis was doubled in comparison with R 8110 alone. Moreover, markedly improved and longer lasting analgesia and muscle relaxation were observed with the combination. When the drugs were injected together, the plasma concentrations of R 8110 were initially much higher than after separate injection of R 8110, but they became similar after 30 min. Although statistically non‐significant, fentanyl reduced the total plasma clearance of R 8110 (31.1 ± 6.9 MS. 21.9 ± 2.3 ml/kg/min) and decreased the volume of distribution (3.78 ± 1.83vs.2.23 ± 0.90 1/kg,P<0.05). Fentanyl did not alter the elimination half‐life ofR8110. R8110 had no apparent influence on the pharmacokinetic

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00122.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Dello, C.P., Belpaire, F.M., De Rick, A.&Fraeyman, N.H. Influence of inflammation of serum concentration, molecular heterogeneity and drug binding properties of canine alpha–1–acid glycoprotein.J. vet. Pharmacol. Therap.11, 71–76.The concentration and the heterogeneity of alpha–1–acid glycoprotein (α–1–AGP) and oxprenolol binding were determined in serum of healthy dogs and dogs with inflammatory disease. In inflammation, an increase in the mean a–1–AGP concentration from 0.47 to 2.85 g/1 was accompanied by a reduction in the mean free oxprenolol fraction from 25% to 6%. α–l–AGP concentration and oxprenolol binding were inversely correlated. The heterogeneity of canine a–l–AGP remained essentially unchanged in dogs with inflammation and, in both these dogs and the controls, between five and seven forms with different isoelectric points and one single concanavalin A–reactive form were detected. It is concluded that in dogs, as in humans, oxprenolol binds to serum α–l–AGP. Changes in serum binding of oxprenolol during inflammation result from a change in the serum concentration of a–l–AGP rather th

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00123.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Gerhards, H.,&Kietzmann, M. Dose‐dependent plasma elimination of subcutaneously administered calcium heparin in horses.J. vet. Pharmacol. Therap.11, 77–83.Pharmacokinetic parameters for subcutaneous low dose heparin in horses have been determined. Four groups of five and one group of eleven mature, healthy horses of various breeds were given single subcutaneous injections of 60, 80, 100, 125, and 150 units of calcium heparin/kg of body weight (U/kg) in the pectoral region. Jugular blood samples were collected prior to, and at hourly intervals for 12 h after injection. Heparin plasma concentrations were measured using a commercially available amidolytic assay. Peak concentrations 4 h after administration were 0.021 ± 0.016 (mean ± SD) units of heparin/ml of plasma (U/ml) after 60 U/kg, 0.035 ± 0.025 U/ml after 80 U/kg, 0.023 ± 0.004 U/ml after 100 U/kg, 0.034 ±0.019 U/ml after 125 U/kg, and 0.053 ±0.019 U/ml after 150 U/kg. Data from groups given 60 and 100 U/kg could not be used for kinetic calculations. Elimination constant (1/h), elimination half‐life (h), and elimination time (h) calculated to reach base‐line values after 80 U/kg were 0.182 ± 0.041 1/h, 3.8 ± 0.9 h, and 9.7 + 2.2 h. After 125 U/kg, corresponding values were 0.211 ± 0.019 1/h, 3.3 ± 0.3 h, 13.4 ± 1.2 h, and after 150 U/kg 0.098 ± 0.015 1/h, 7.1 ± 1.1 h, and 20.6 ± 3.2 h. Calculated heparin concentrations 12 h after administration of 80, 125, and 150 U/kg were 0.011 ± 0.002, 0.010 ± 0.001, and 0.027 ± 0.004 U/ml. After seven successive injections of 150 U/kg at 12 h intervals in one horse, the elimination constant decreased from 0.23/h after the first to 0.08/h after the seventh injection, and the elimination time increased from 10 h to 40 h. Reducing the dosage from 150 U/kg initially to 125 U/kg for six successive injections reduced the prolonged elimination a

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00124.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Hanna, R.M., Borchard, R.E.&Schmidt, S.L. Pharmacokinetics of ketamine HC1 and metabolite I in the cat: a comparison of i.v., i.m., and rectal administration.J. vet. Pharmacol. Therap.11, 84–93.Ketamine HC1 [2‐(o‐chlorophenyl)‐2‐(methylamino) cyclohexanone HC1] concentrations in whole blood were used to study the pharmacokinetics of i.v., i.m., and rectal administrations, at a dose of 25 mg/kg, in normal domestic cats. Absorption was rapid with both the i.m. and rectal routes. Systemic availability was 51% (SEM 10) for the i.m. dose and 43.5% (SEM 6.1) for the rectal dose. The first‐pass effect had a minimal influence on the metabolism of ketamine HC1 administered rectally. The elimination rate constant (β) of the drug was statistically similar in the i.v., i.m., and rectal groups, at a 95% level of significance (P<0.05). At the dosage rates studied, ketamine HC1 produced an anesthetic effect in the cat following i.v., i.m. and rectal ad

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00125.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY

摘要:

Nolan, A., Waterman, A.E., Livingston, A. The correlation of the thermal and mechanical antinociceptive activity of pethidine hydrochloride with plasma concentrations of the drug in sheep. J. vet. Pharmacol. Therap. 11, 94–102.The analgesic activity of pethidine was measured in eight sheep using both thermal and mechanical test systems. Pethidine, at a dose rate of 5 mg/kg body weight given intravenously, produced a significant degree of antinociception to thermal pain for 30 min (on average) but gave only a few minutes of significant analgesia when tested in the mechanical pressure system. Analgesia in both systems was abolished by pretreatment with naloxone. Pharmacokinetic analyses of plasma levels of pethidine after intravenous (i.v.) injection were carried out. Plasma concentrations of the drug exhibited a rapid biexponential pattern of decline with an average distribution half‐life of 0.99 min and an elimination half‐life of 12.8 min. Correlation of plasma levels of the drug with the presence of a significant degree of antinociception in the thermal test system enabled ‘critical’ analgesic levels of pethidine to be defined for sheep (0.

ISSN:0140-7783    

DOI:10.1111/j.1365-2885.1988.tb00126.x

出版商:Blackwell Publishing Ltd    

年代:1988

数据来源: WILEY