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1.
Spirals of endothelially denuded equine saphenous vein were used to study the pre- and post-junctional effects of medetomidine in vitro . The pD2 values were calculated for noradrenaline (6.7 /pm 0.1), phenylephrine (5.6 /pm 0.1), BHT 920 (6.2 /pm 0.2) and UK 14304 (5.7 /pm 0.2). Medetomidine produced a biphasic response, with a pD21 of 8.2 /pm 0.1 and a pD22 of 5.7 /pm 0.1 in the equine saphenous vein ( n = 6 ). Prazosin (10−7 m) significantly shifted the second phase of the medetomidine concentration-response curve to the right (pD21 was 8.1 /pm 0.2 and pD22 was 5.0 /pm 0.2, P < 0.05). Rings of equine saphenous vein were electrically stimulated to investigate the pre-junctional effects of medetomidine. Increasing concentrations of the α2-adrenoceptor agonist BHT 920 reduced the response to electrical stimulation in a concentration dependent manner to a maximum of 40 /pm 5%. whereas medetomidine (0.1-100 nm) caused a concentration dependent enhancement to a maximum of 490 /pm 150%. These results suggest α1- and α2-adrenoceptors are functional in the equine saphenous vein, but that medetomidine is not acting exclusively as an α2-adrenoceptor agonist.  相似文献   

2.
Beta2-adrenoceptor agonists are used as bronchodilators in both humans and horses. Of these drugs, clenbuterol is the one most frequently used when treating chronic obstructive pulmonary disease in the horse, while salbutamol and terbutaline are used in the treatment of human asthma. Little is known of the properties of the latter two drugs in equine medicine.
  We have compared salbutamol and terbutaline with clenbuterol in relation to their ability to relax muscle strips from equine tracheal muscle, pre- contracted with 40 n m carbachol, in tissue chambers. The affinities of these drugs to the β2-adrenoceptors in homogenates of the same muscle tissue were also examined. These experiments were performed with radioligand binding studies using the very potent β-adrenoceptor antagonist 125I-cyanopindolol.
  The three drugs were almost equipotent in relaxing the muscle strips. The EC50-values for salbutamol, terbutaline and clenbuterol were 5.6, 13.8 and 2.1 n m , respectively, and all three drugs relaxed the preparations completely. In the competitive binding study, however, the Kd-value of clenbuterol was much lower (24 n m ) than that of salbutamol and terbutaline (1100 n m and 3900 n m , respectively). The amount of receptors bound at the EC50-value of clenbuterol was 8% compared to less than 1% for salbutamol and terbutaline. This indicates a lower intrinsic efficacy of clenbuterol than of the other two drugs. The β-adrenoceptor density was 45 ± 14.3 fmol/mg protein (mean ± SD) and the Kd-value of 125I-cyanopindolol was 11.4 ± 3.3 p m .  相似文献   

3.
We examined the functional role of adrenergic receptor subtypes (ARs) in bovine intra-mammary arteries (IMAs), 1.5–2.5 mm internal diameter. Norepinephrine (NE) and phenylephrine (PE) produced concentration-dependent increases in tone in segments maintained at a previously determined optimal basal tension in vitro . The sensitivity of the tissue to NE and PE, based on -log molar ED50s was 6.87 ± 0.17 and 7.05 ± 0.35, respectively. In addition a Schild analysis yielded antagonist affinities for the receptor mediating contractile responses to NE (pA2 value) of 10.46 ± 0.85 for prazosin and 6.29 ± 0.18 for yohimbine. These data indicate a dominance of functional alpha 1 (α1) over alpha 2 (α2)-ARs in this tissue. Based on the inhibitory effects of chloroethylclonidine (CEC) on PE responses and the further reduction in sensitivity when nifedipine was added to the CEC, also in the presence of PE, we conclude that there is more than one α1-AR subtype, with a predominant role for α1B-ARs in phenylephrine responses. Stimulation of beta (β)-ARs, resulted in relatively small reductions in tone (the highest magnitude of response was 25.94 ± 6.46% of the papaverine maximum at 3×10−6 M isoproterenol); in addition, propranolol did not significantly alter tissue sensitivity to NE. Additional characterization of functional autonomic receptor populations in this circulatory bed will form a basis for future studies on circulatory dynamics in the mammary gland.  相似文献   

4.
Strips of tracheal smooth muscle from 12 horses were contracted by carbachol in tissue baths under isometric conditions. This contraction (≅50% of maximum: EC50) was relaxed completely with adrenoceptor drugs. The only exception was clenbuterol, where the degree of relaxation was ≅90%. In all horses the EC50-value for isoprenaline (mean 1.6 × 10−8M) was less than that for adrenaline (mean 9.6 × 10− 8M) and noradrenaline (mean 1. 8 × 10- 6M). The potency ratio was 1 < 6 < 110 which indicates that the β2-subtype dominates among the β-adrenoceptors of equine airways. All preparations were also very sensitive to the specific and potent β2-receptor agonists clenbuterol (mean 5.7 × 10− 9M) and procaterol (mean 3.6 × 10−10M). No differences in EC50-values due to age, sex and breed were observed in this material. The standard deviation of the mean EC50-values seems to be larger for the specific β2-adrenoceptor agonists than for the unspecific. A reason for this could be differences in the pattern of the β-adrenoceptor population.  相似文献   

5.
The effect of xylazine on the isolated sheep trachea and its possible interactions with the α2-adrenergic antagonist, atipamezole, and the anticholinergic agent, atropine, was studied. The mechanical responses of the tracheal preparations were recorded after exposing each one to cumulatively increasing concentrations of xylazine alone or in the presence of atipamezole or atropine.
Xylazine exerted a concentration-dependent contractile effect, with a threshold concentration of 10--7M while the maximum activity was produced at a concentration of 10--5M (EC50= 2.3 × 10--7). This xylazine-induced contractile effect was inhibited by atipamezole, but not significantly modified by atropine. Thus, it is concluded that α2-adrenoceptors exist in the sheep trachea and it is suggested that α2-adrenoceptor agonists may act on airways in sheep directly through stimulation of peripheral α2-adrenergic receptors and indirectly via central α2-adrenergic receptor activation of parasympathetic tone.  相似文献   

6.
α2-Adrenergic receptor agonists are widely used in veterinary medicine as sedative/hypnotic agents. Four pharmacological subtypes of the α2-adrenergic receptor (A, B, C and D) have been identified based primarily on differences in affinity for several drugs. The purpose of this study was to examine the affinities of the sedative agents, xylazine, detomidine and medetomidine at the four α2-adrenergic receptor subtypes. Saturation and inhibition binding curves were performed in membranes of tissues containing only one subtype of a2-adrenergic receptor. The KD for the α2-adrenergic receptor radioligand, [3H]-MK-912, in HT29 cells (α2A-), neonatal rat lung (α2B-), OK cells (α2C-) and PC12 cells transfected with RG20 (α2D-) were 0.38 ± 0.08 n m , 0.70 ± 0.5 n m , 0.07 ± 0.02 n m and 0.87 ± 0.03 n m , respectively. Detomidine and medetomidine had approximately a 100 fold higher affinity for all the α2-adrenergic receptors compared to xylazine but neither agonist displayed selectivity for the α2-adrenergic receptor subtypes. These data suggest that available sedative/hypnotic α2-adrenergic receptor agonists can not discriminate between the four known α2-adrenergic receptor subtypes.  相似文献   

7.
Acetylcholine interacts with endothelial muscarinic receptors releasing nitric oxide and causing vasodilatation. To identify the receptor subtype responsible for acetylcholine-induced relaxation in canine uterine artery, the usual organ bath method for in vitro investigation on isolated blood vessels was applied. Using a range of muscarinic receptor antagonists such as atropine (nonselective), pirenzepine (M1-selective), methoctramine (M2-selective) and p -fluoro-hexahydro-sila-difenidol ( p -FHHSiD) (M1/M3) and determining pA2 value of those antagonists through Shild analysis, we aimed at establishing a precise receptor mechanism underlying acetylcholine-induced relaxation in isolated canine uterine artery. The relaxation of uterine arterial rings in response to acetylcholine in the presence or absence of selective muscarinic receptors antagonists was calculated using concentration response curves. Acetylcholine induced concentration-dependent and endothelium-dependent relaxation of arterial rings precontracted with phenylephrine (pEC50 = 6.90 ± 0.02). Muscarinic receptors antagonists atropine, pirenzepine, methoctramine and p -FHHSiD competitively antagonized the response to acetylcholine and obtained pA2 values were 9.91 ± 0.06, 6.60 ± 0.04, 6.21 ± 0.08 and 8.05 ± 0.1, respectively. This study showed that acetylcholine induced endothelium-dependent relaxation of canine uterine artery by stimulation of muscarinic receptors localized on the endothelial cells. On the basis of differential antagonist affinity, we suggest that the muscarinic receptors involved in the acetylcholine-induced relaxation of canine uterine artery are predominantly of M3 subtype.  相似文献   

8.
The aim of the current study was to investigate whether multiple oral dosing of valacyclovir could result in plasma concentrations exceeding the EC50-value of acyclovir against equine herpesvirus 1 (EHV1) during the majority of the treatment period. Additionally, we wanted to determine the concentration of acyclovir in nasal mucus and cerebrospinal fluid (CSF). Valacyclovir was administered to four horses and two ponies, three times daily, at a dosage of 40 mg/kg, for four consecutive days. Blood was collected prior to each administration and 1 h after dosing. Nasal mucus samples and CSF were collected once during treatment; 1 h after the last administration. This dosage regimen resulted in plasma concentrations that were higher than the EC50-value of 1.7 μg/mL, i.e. EC50 of an isolate highly susceptible to acyclovir, for 80% of the treatment period; and higher than the EC50-value of 3.0 μg/mL, i.e. EC50 of an isolate less susceptible to acyclovir, for 60% of the treatment period. Concentration in nasal mucus samples and CSF was 0.36–1.17 μg/mL and 0.11–0.23 μg/mL, respectively. This study illustrates that multiple dosing of valacyclovir may result in a therapeutic benefit as plasma concentrations could be maintained above the EC50-value of acyclovir against EHV1 for more than 50% of the treatment period. Acyclovir could be detected in both nasal mucus samples and CSF. However, these concentrations were lower than the EC50.  相似文献   

9.
The serum 25-OH-D3, Ca, P, and Mg concentrations in thirty-seven cows that had calved in March April were studied in this trial. Twenty-three had puerperal paresis. Values observed in this group were Ca, 1.27 ± 0.3 mmol/l, P, 1.63 ± 0.82 mmol/l, Mg, 1.14 ± 0.27 mmol/l, and 25-OH-D3, 32.7 ± 22 μg/l. In the fourteen age-matched healthy control cows from the same herd values were Ca, 1.93 ± 0.5 mmol/l, P, 3.09 ± 1.28 mmol/l, Mg, 1.01 ± 0.3 mmol/l and 25-OH-D3, 31.5 ± 19.7 μg/l. The range of values for the cows serum 25-OH-D3 concentration was l't; 3.2 to 76 μg/l. No differences could be established in terms of 25-OH-D3 concentrations between the groups.  相似文献   

10.
The vasoconstrictor effects of phenylephrine and histamine were investigated in isolated strips of pulmonary arteries in pigs during ageing. Interactions between phenylephrine-induced responses and arachidonic acid derivatives were also studied by incubating the blood-vessels with indomethacin. Potency (pD2 values) and maximal effects (Emaxx) recorded in 5-week-old piglets (group I, n = 5) with phenylephrine [5.71 ± 0.17 and 0.76 ± 0.22 g/mg of dry tissue respectively (mean ± SEM)] were similar to values found in 12-week-old animals (group 2, n = 5) (5.49 ± 0.30 and 1.06 ± 0.27 g/mg of dry tissue respectively). The sensitivity and responsiveness of tissues to this agonist were significantly reduced in 26-week-old mature pigs (group 3, n = 6) as indicated by the decrease in pD2 (3.91 ± 0.23; P < 0.01) and Emax (0.27 ± 0.13 g/mg of dry tissue; P < 0.05) values observed in this group. Histamine (10_3M)-induced maximal responses (Emax) were significantly higher in group 2 (2.23 ± 0.49 g/mg) than in group 1 (0.85 ± 0.11 g/mg; P < 0.05) and in group 3 (0.48 ± 0.10 g/mg; P < 0.01). In 5-week-old animals, indomethacin (3.10˜5M) significantly ( P < 0.05) shifted the concentration-response curve to phenylephrine to the right (0.28 log. units) and depressed contractions to this drug as shown by the significant decrease of 39.5% ( P < 0.05) in Emax. This cyclo-oxygenase inhibitor had no effect in other groups. These data indicate that phenylephrine is a potent and effective vasoconstrictor agent for the main pulmonary arteries in 5-week-old piglets and that alpha-1-adrenergic-induced contractions are enhanced by cyclo-oxygenase products. These findings can be related with the high reactivity of pulmonary vascular smooth muscles in these animals.  相似文献   

11.
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 F1α 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 15 min after bolus injection and were 9.2± 1.4 and 7.8± 4.3 μg/mL, respectively. The half-life of elimination ( t ½β) of pentoxifylline was 1.44 h and volume of distribution ( V darea) was 0.94 L/kg. The mean plasma concentration of 6-keto-prostaglandin F1α increased over time, with a significant increase occurring 30 min after the bolus administration. Ex vivo plasma endotoxin-induced tumour necrosis factor activity was significantly decreased at 1.5 and 3 h of infusion. These results indicate that infusion of pentoxifylline will increase 6-keto-prostaglandin F1α and significantly suppress endotoxin-induced tumour necrosis factor activity in horses during the period of infusion.  相似文献   

12.
The present experiments were designed to study the effect of adding the detergent Equex-STM® to freezing extender, and of straw volume (0.25 ml vs 0.5 ml), on boar sperm quality after cryopreservation. Three ejaculates from each of four purebred boars (three Landrace and one Yorkshire) were collected and frozen with a lactose-egg yolk extender containing glycerol with or without 1.5% Equex-STM®. The extended semen was loaded into either 0.25- or 0.5-ml straws. The straws were placed in liquid nitrogen (LN2) vapour approximately 3 cm above the level of LN2 for 20 min and then were plunged into LN2. Thawing was achieved in warm water at 50°C for 12 s and then was incubated in a 38°C water-bath for 30 min before evaluating sperm quality. Results showed that the individual motility, viability and acrosomal normal apical ridge (NAR) were improved (p < 0.001) when Equex-STM® was added to the freezing extender. There was no difference (p   =   0.48) in sperm motility between 0.25- and 0.5-ml straws when Equex-STM® was added. The percentages of viable and of NAR sperm in 0.5-ml straws were higher than those in 0.25-ml straws (p   =   0.02, p   =   0.0003 respectively). The percentages of membrane intact sperm evaluated using the short hypo-osmotic swelling test were not affected by straw volume or the adding of Equex-STM® (p   >   0.05). The results of these investigations suggested that Equex-STM® exerts a beneficial effect on the quality of cryopreserved boar semen and this cryopreservation protocol was favourable for a 0.5-ml straw.  相似文献   

13.
Simultaneous pharmacokinetic-pharmacodynamic (PK-PD) models of meperidine in Soats were established by utilizing the P3 wave of the cerebral evoked potentials as an analgesic measurement. An effect compartment linked to the central compartment was postulated in the models. The hypothetical drug amount in the effect compartment was related to the observed analgesia through the Hill equation. After intramuscular (i. m., n = 16) and intravenous (i. v., n = 13) dosing (5 mg/kg), the elimination rate constants of meperidine in the effect compartment ( K eO) were 0.3744 ± 0.2546 and 0.1123 ± 0.0428 min-1, drug concentrations in the effect compartment generating half maximal analgesia (EC(50)) were 0.70 ± 0.33 and 0.41 ± 0.26 μg/ml, the maximal effects (Emax) were 89.63 ± 15.63 and 85.92 ± 9.64%, and the Hill coefficients (S) were 2.61 ± 1.21 and 2.37 ± 1.15, respectively. K eO and EC(50) with i.m. dosing were significantly greater than with i.v. injection. However, administration route had no influence on S, Emax and the total amount of effect ( AUE ). The predicted peak effect (Emax^) of 64.44 ± 14.64 and 66.02 ± 11.51% were achieved at 14.7 ± 7.4 and 8.5 ± 2.2 min after i.m. and i.v. dosing, respectively. Peak analgesia appeared much later than peak plasma concentration, but simultaneously with peak CSF level both after i.m. and i.v. dosing. An obvious hysteresis was demonstrated between plasma concentration and analgesic effect. This study demonstrates that meperidine analgesia can be predicted using a PK-PD model, but not by PK data alone. Both i.m. and i.v. administration routes were evaluated kinetically and dynamically.  相似文献   

14.
The objective of this study was to determine the kinetic parameters of a new formulation that contained 2.25% ivermectin combined with 1.25% abamectin in bovine plasma. The results for 2.25% ivermectin: C max (37.11 ng/mL ± 7.42), T max (16 days ± 5.29), T 1/2 (44.62 days ± 53.89), AUC (928.2 ng·day/mL ± 153.83) and MRT (36.73 days ± 33.64), and for 1.25% abamectin: C max (28.70 ng/mL ± 9.54), T max (14 days ± 4.04), T 1/2 (15.40 days ± 11.43), AUC (618.05 ng·day/mL ± 80.27) and MRT (20.79 days ± 8.43) suggest that this combination of 2.25% ivermectin + 1.25% abamectin possesses properties that give this pharmaceutical formula a longer activity time than two of the commercial products tested (1% ivermectin and 1% abamectin), and showed similarity to 3.15% ivermectin.  相似文献   

15.
Palmar digital arteries and veins removed surgically from healthy horses under general anesthesia were cut into 4 mm vascular rings, suspended in tissue baths, and attached to force displacement transducers for continuous measurement of vascular tension. In vitro vascular responses were determined for acetylcholine, acepromazine, isoxsuprine hydrochloride (isoxsuprine), prostaglandin E2 (PGE2), and prostaglandin I2 (prostacyclin). After preconstriction with norepinephrine hydrochloride (norepinephrine), or prostaglandin F2 alpha (PGF2 alpha), the concentrations needed to produce 50% maximum relaxation (EC50) and the maximum percentage of relaxation were determined for each drug.
Acetylcholine was the most potent arterial vasodilator (smallest EC50 value) and PGE2 was the least potent. Prostacyclin was the least potent venodilator (highest EC50 value); there were no differences between acetylcholine, acepromazine, isoxsuprine, and PGE2. Isoxsuprine produced greater arterial relaxation than all other agents. Isoxsuprine and acepromazine produced significantly greater venous relaxation than did acetylcholine and PGE2. Prostacyclin produced minimal vasodilation of arteries or veins. Acepromazine and isoxsuprine relaxed the veins significantly more than the arteries. When PGF2 alpha was used instead of norepinephrine to preconstrict the arteries and veins, the potency and effectiveness of acepromazine and isoxsuprine to produce vasodilation were significantly decreased. Results indicate that acepromazine and isoxsuprine can relax the equine digital vasculature but their effectiveness varies depending on the origin of the constriction.  相似文献   

16.
The pharmacokinetics and pharmacodynamics of the non-steroidal antiinflammatory drug, oxindanac, were assessed simultaneously in calves after intravenous (i.v.) administration at dose rates of 0.5, 1, 2, 4 and 8 mg/kg. Plasma pharmacokinetic data were fitted to either two or three compartment open models. The elimination t 1/2 was constant in the dose range 0.5 to 4 mg/kg (20.2–22.8 h) and shorter at 8 mg/kg (14.7 h). The pharmacodynamics of oxindanac were assessed by its inhibition of serum TxB2, an index of platelet cyclo-oxygenase activity. Plots of total plasma oxindanac concentration vs. inhibition of serum TxB2 fitted in all cases a sigmoidal Emax equation. There were no significant differences in the estimates for ED 50 (1.6-1.9 μg/ml), Hill constant (1.3-2.7) or Emax between the doses used in the in vivo studies or when blood was spiked with oxindanac in vitro. Plots of inhibition of serum TxB2 vs. time were prepared from the pharmacokinetic model equations in each calf in combination with a single sigmoidal Emax plot generated in vitro. These data were not significantly different from the results produced in vivo. It is concluded that oxindanac causes reversible inhibition of platelet cyclo-oxygenase in calves. Its inhibition of serum TxB2 can be predicted from total plasma drug concentration, as described by a multicompartmental model, and sigmoidal Emax enzyme kinetics. It was not necessary to take into account factors such as drug equilibration between plasma and its target site, free vs. total drug concentration or chirality. This simple model may be useful for predicting the pharmacodynamics of oxindanac in other species.  相似文献   

17.
The purpose of this sutdy was to determine the clinical utility of 111 In-labeled transferrin ( 111 In-TF) scintigraphy for evaluating dogs suspected of having protein-losing enteropathies. Four dogs were injected intravenoulsy with autologous 111In-TF after 30 min incubation (at 37°C) of 18.5 MBq (0.5mCi) 111In CI3 with one ml of autologous plasma, Serial right lateral, left lateral and dorsal images were obtained 2, 4, and 24 hours post 111 In-TF administration, Images were subjectively evaluated for the presence or absence of 111 within the gastrointestinal tract. The results of total protein, albumin and globulin legels and results form gastrointestinal tract. the results of total protein, albumin and globulin levels and results from gastrointestinal biopsies were recorded. In one dog, a follow-up scientigraphic study was done six months after initial evaluation and initiation of treatment for plasmocytic-lymphocytic enteritis. Gastrointestinal activity was noted by two hours in two dogs, while all four dogs had gastrointestinal activity on the 24 hour images. The mean (±std dev) plasma protein, albumin and globulin levels were 3.5 (±0.9), 1.7 (±1) and 1.8 (±0.3) respectively at the time of initial presentation. In the one dog that was evaluated after therapy, faint visualization of radioactivity within the colon was noted on the 24 hour image. Based on this study, 111In-TF appears to be a viable scientigraphic method for evaluating dogs with suspected dogs withfd suspected protein-losing enteropathies, Potential limitations of tjis radiopharmaceutical include cost and prolonged isolation of the animal prior to release to the client due to the long physical half-life (T½= 2.82 days).  相似文献   

18.
Objective  To evaluate and to validate the accuracy of the Perkins® handheld applanation tonometer in the measurement of IOP in dogs and cats.
Animals  Twenty eyes from 10 dogs and 10 cats immediately after sacrifice were used for the postmortem study and 20 eyes from 10 clinically normal and anesthetized dogs and cats were used for the in vivo study. Both eyes of 20 conscious dogs and cats were also evaluated.
Procedure  Readings of IOP postmortem and in vivo were taken using manometry (measured with a mercury column manometer) and tonometry (measured with a Perkins® handheld applanation tonometer). The IOP measurement with Perkins® tonometer in anesthetized and conscious dogs and cats was accomplished by instillation of proxymetacaine 0.5% and of 1% fluorescein eye drops.
Results  The correlation coefficient ( r 2) between the manometry and the Perkins® tonometer were 0.982 (dogs) and 0.988 (cats), and the corresponding linear regression equation were y  = 0.0893 x  + 0.1105 (dogs) and y  = 0.0899 x  + 0.1145 (cats) in the postmortem study. The mean IOP readings with the Perkins® tonometer after calibration curve correction were 14.9 ± 1.6 mmHg (range 12.2–17.2 mmHg) in conscious dogs, and were 15.1 ± 1.7 mmHg (range 12.1–18.7 mmHg) in conscious cats.
Conclusion  There was an excellent correlation between the IOP values obtained from direct ocular manometry and the Perkins® tonometer in dogs and cats. The Perkins® handheld tonometer could be in the future a new alternative for the diagnosis of glaucoma in veterinary ophthalmology.  相似文献   

19.
α2-adrenoceptor agonist drugs can cause respiratory changes leading to a short period of hypoxaemia in sheep. It has been suggested that this is due to transient platelet aggregation and pulmonary microembolism. If platelet aggregation were to follow platelet activation in response to the administration of α2 agonists, plasma thromboxane levels would be expected to rise. This study was carried out to measure plasma thromboxane B2 concentrations before and after the intravenous administration of the α2-agonist drug xylazine at a dose of 0.1 mg/kg. It was found that the plasma thromboxane concentration rose by 320% and, furthermore, the rise was prevented by the prior administration of atipamezole hydrochloride (0.125 mg/kg), an α2-adrenoceptor antagonist.  相似文献   

20.
Target-controlled infusion (TCI) anesthesia using target effect-site concentration rather than plasma concentration provides less drug consumption, safer anesthesia, less undesired side effects and improved animal welfare. The aim of this study was to calculate the constant that converts propofol plasma into effect-site concentration ( k e0) in dogs, and to implement it in a TCI system and compare it with the effect on the central nervous system (CNS). All dogs were subjected to general anesthesia using propofol. Fourteen dogs were used as the pilot group to calculate k e0, using the t peak method. Fourteen dogs were used as the test group to test and validate the model. R ugloop ii ® software was used to drive the propofol syringe pump and to collect data from S/5 Datex monitor and cerebral state monitor. The calculated k e0 was incorporated in an existing pharmacokinetic model (Beths Model). The relationship between propofol effect site concentrations and anesthetic planes, and propofol plasma and effect-site concentrations was compared using Pearson's correlation analysis. Average t peak was 3.1 min resulting in a k e0 of 0.7230 min−1. The test group showed a positive correlation between anesthetic planes and propofol effect-site concentration ( R  = 0.69; P <  0.0001). This study proposes a k e0 for propofol with results that demonstrated a good adequacy for the pharmacokinetic model and the measured effect. The use of this k e0 will allow an easier propofol titration according to the anesthetic depth, which may lead to a reduction in propofol consumption and less undesired side effects usually associated to high propofol concentrations in dogs.  相似文献   

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