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1.
Three groups of five clinically healthy buffaloes each were injected intravenously with sulphadiazine, sulphadimidine and sulphamerazine in a dose of 100 mg/kg b. wt. (as a singly initial dose of 40 mg/kg b. wt. an subsequently the plasma level kept constant by a continuous intravenous infusion of a maintenance dose of 20 mg/kg per hour over a period of 3 hours). It was found that, 1) sulphadiazine, sulphadimidine and sulphamerazine increase the plasma glucose levels at 1, 2, 2.5 and 3.5 hours from the start of i.v. infusion. 2) The glucose concentration in urine increased in the buffaloes infused i.v. with sulphadiazine. 3) The glucose level in urine of buffaloes infused i.v. with sulphadimidine and sulphamerazine was slightly increased. 4) The concentrations of sulphadiazine, sulphadimidine and sulphamerazine in plasma reached its highest level, 2.5, 2 and 2.5 hours during the i.v. infusion, respectively, then declined rapidly. 5) The concentrations of sulphadiazine, sulphadimidine and sulphamerazine in urine reached their highest concentrations 3.5 hours after i.v. infusion.  相似文献   

2.
Hydroxylated metabolites of sulphadimidine, sulphamerazine, sulphatroxazole, sulphamethoxazole, and sulphadiazine exhibited antimicrobial activity against Escherichia coli 28 PR 271 test strain ranging from 2.5 to 39.5 per cent of that of the parent drug. Trimethoprim addition potentiated the antimicrobial activity of these metabolites. N4-acetyl sulphonamide metabolites possessed no antimicrobial activity, nor did trimethoprim potentiated them.  相似文献   

3.
Pharmacokinetic studies in broilers and layers of different sulphonamides indicate a good absorption and a long elimination half-life (of sulphaquinoxaline, sulphadimidine and to a lesser degree sulphadiazine) resulting in high plasma concentrations during drinking water medication in the recommended therapeutic doses. In contrast drinking water medication with high concentrations of trimethoprim (up to 1,320 mg/liter) resulted in a maximal mean plasma concentration of 1.2 micrograms/ml. Very good therapeutic effects were demonstrated in broilers experimentally infected with a sulphonamide-susceptible E. coli strain when treated with sulphaquinoxaline (200 mg/liter), sulphadimidine sodium (2 gram/liter), sulphachloropyridazine 30 per cent (1 gram/liter) and to a lesser degree sulphadiazine sodium (250 mg/liter). Synergism was demonstrated between trimethoprim and sulphadiazine (1:5). The combination of trimethoprim with sulphaquinoxaline (1:3) did not induce better therapeutic effects than sulphaquinoxaline in proportional doses. However, significant synergism was demonstrated between trimethoprim and both sulphonamides in treatment of experimental infection with sulphonamide-resistant E. coli. No signs resembling sulphonamide intoxication were observed during these studies.  相似文献   

4.
Summary

Hydroxylated metabolites of sulphadimidine, sulphamerazine, sulphatroxazole, sulphamethoxazole, and sulphadiazine exhibited antimicrobial activity against Escheria coli 28 PR 271 test strain ranging from 2.5 to 39.5 per cent of that of the parent drug. Trimethoprim addition potentiated the antimicrobial activity of these metabolites. N4‐acetyl sulphonamide metabolites possessed no antimicrobial activity, nor did trimethoprim potentiated them.  相似文献   

5.
Eight experiments were carried out on eight clinically healthy non-pregnant ewes. Each animal was injected intravenously with either sulphadiazine or sulphadimidine at a dose rate of 100 mg/kg body weight. A two-compartment pharmacokinetic model was developed to describe the disposition of these drugs. The elimination half-lives were 7.15 ± 0.58 h and 9.51 ± 0.59 h and the distribution half-lives were 0.56 ± 0.07 h and 0.42 ± 0.05 h for sulphadiazine and sulphadimidine, respectively. The apparent specific volumes of distribution were less than 1 litre/kg (0.410 and 0.501 litres/kg for sulphadiazine and sulphadimidine, respectively) which indicates a relatively lower distribution of these drugs to tissues than in plasma in sheep. The degree of plasma protein binding was similar for both drugs (19.15 ± 0.55% and 23.12 ± 0.32%) for sulphadiazine and sulphadimidine, respectively). Serum concentrations of ketone bodies, total lipids and calcium were significantly reduced, and blood glucose concentration significantly increased following administration of both of these sulphonamides, whilst serum total protein concentration was unaltered. The serum cholesterol concentration was significantly reduced following sulphadiazine administration, but not after sulphadimidine.  相似文献   

6.
Summary

The various sulphonamides show marked differences in disposition characteristics after administration to ruminants. For use in combination with a diaminopyrimidine derivative such as trimethoprim or baquiloprim, it is essential that a sulphonamide has similar pharmacokinetic properties in order to obtain optimal synergy. In the present study the pharmacokinetics of sulphamethoxazole, sulphatroxazole, and sulphamerazine were investigated in dwarf goats (n=6) after IV and intraruminal administration at a dose of 30 mg/kg bodyweight. In addition, the in vitro binding of sulphamerazine to ruminal contents was studied as a possible explanation for a reduced absorption rate. Sulphamethoxazole showed the most rapid absorption after intraruminal administration (mean tmax ± SD : 0.8 ± 0.2h). However, the drug was rapidly eliminated from the plasma (t1/2ß : 2.4 ± 1.5h) and the bioavailability was only 12.4 ± 4.7 %, most likely due to an extensive ‘first‐pass’ effect. The bioavailability of orally administered sulphamerazine and sulphatroxazole was much higher (67.6 ± 13.5 % and 70.2 ± 32.3 %, respectively). After intraruminal administration, sulphatroxazole showed the highest plasma peak concentration (26.1 ± 6.3 mg/I) and the longest plasma half‐life (4.7 ± 1.8h) and mean residence time (13.9 ± 4.5 h). Sulphamerazine showed considerable binding to rumen contents in vitro. Based on its pharmacokinetic properties sulphatroxazole appears to be a suitable candidate to be used in combination with the more recently developed diaminopyrimidines such as baquiloprim.  相似文献   

7.
Half the progeny in a 200-sow herd (2045 pigs) was given feed medicated with 500 g/tonne of a 1:5 trimethoprim/sulphadiazine mixture from three to nine weeks of age. The other half (1989) acted as controls. The trial lasted 12 months. No difference was observed between the two groups in the incidence of streptococcal meningitis and the morbidity and mortality from all disease causes during the growing/fattening periods did not differ significantly. The main diseases encountered were pneumonia (7.24 per cent), streptococcal meningitis (5.12 per cent), leg and foot disorders (3.34 per cent) and the after-effects of vices (1.86 per cent). The resistance of faecal coliforms to trimethoprim was studied during the six-week period of trimethoprim/sulphadiazine feeding. Faecal coliforms in both medicated and non-medicated groups developed almost 100 per cent resistance. However, resistance developed more slowly in the untreated pigs. The medicated pigs showed a small overall improvement in feed conversion rate up to 18 weeks of age mainly because of a marked improvement between three and six weeks.  相似文献   

8.
Trimethoprim (TMP) was administered in combination with either sulphadiazine or sulphadimidine to broilers, and plasma concentrations were determined simultaneously by newly developed thin-layer and/or high-performance liquid-chromatographic procedures, which also allowed quantification of the N4-acetyl metabolites of the sulphonamides. After i.v. injection of TMP (20 mg/kg body wt) and sulphadiazine (100 mg/kg body wt), both compounds were rapidly eliminated from plasma with half-lives of 1 and 2.7 h, respectively. Apparent volumes of distribution (3.3 and 0.96 l/kg, respectively) indicated that the tissue distribution of TMP was more extensive than that of the sulphonamide. After oral administration of the same dosages, elimination appeared to be slower compared to the i.v. injection, but this was obviously related to delayed absorption. Bioavailability after oral administration was approximately 100% of sulphadiazine, but only about 60% for TMP. Oral dosing of TMP in combination with sulphadimidine yielded similar maximum plasma concentrations of both compounds to those obtained with the combination of TMP with sulphadiazine, but the plasma concentration decline of sulphadimidine appeared to be more rapid than that of sulphadiazine after oral administration. During prolonged administration of different dosages of TMP-sulphadiazine combinations via drinking water, only low plasma concentrations were attained by the recommended dosage of the combination. Up to 10-fold higher dosages were tolerated by the animals without side-effects. In view of the fact that the sensitivity of bacterial strains to TMP-sulphonamide combinations differs widely, the plasma concentrations determined in the present study during prolonged drinking-water medication with different dosages of a TMP-sulphadiazine combination can be used to select effective doses for treatment of different poultry diseases.  相似文献   

9.
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10.
Resistance to 16 antimicrobial agents was monitored in 109,125 Salmonella cultures isolated from animals, their environment and feedstuffs between 1988 and 1999. The sensitivity of the 6512 isolates of Salmonella enterica enterica serotype Dublin to all the antimicrobial agents tested varied from 98.2 per cent in 1997 to 99.7 per cent in 1990 and 1996. In contrast, among 28,053 isolates of Salmonella enterica enterica serotype Typhimurium, there was a marked decrease in their sensitivity to all the antimicrobial agents tested, from 57.4 per cent in 1992 to 7.6 per cent in 1995, owing to the widespread occurrence in farm animals of S Typhimurium isolates of the definitive type DT104, resistant to ampicillin, sulphonamides, streptomycin, chloramphenicol and tetracyclines, although the percentage of sensitive isolates increased to 18.4 per cent in 1999, when the incidence of DT104 had decreased. Some isolates of DT104 also showed an increase in resistance to potentiated sulphonamides (2.4 per cent in 1989 to 19.2 per cent in 1999) and nalidixic acid (0 per cent in 1992, 3.8 per cent in 1995 to a peak of 16.9 per cent in 1998). In 1996, 5.1 per cent of 1086 isolates of S Typhimurium from cattle and 35.9 per cent of 192 isolates of S Typhimurium from poultry showed resistance to nalidixic acid. Of the other 74,528 Salmonella isolates, the percentage of strains sensitive to all the antimicrobials tested decreased slightly from 88.2 per cent in 1988 to 70.6 per cent in 1996 and then increased slightly to 73.7 per cent in 1999. The commonest of these other Salmonella serotypes was Salmonella Enteritidis (20,982), which remained predominantly susceptible (ranging from 81.4 to 97.4 per cent) during the study period. Few isolates were resistant to commonly used veterinary antimicrobials, for example, furazolidone, the use of which was banned in 1990, and the aminoglycoside, apramycin.  相似文献   

11.
The prevalence of Salmonella serovars and their antimicrobial resistance patterns were investigated among Danish turkeys between 1995 and 2000, by sampling the flocks approximately 14 days before they were slaughtered. Within the flocks, the prevalence of salmonella varied from 7.1 per cent to 25 per cent, and 24 different serovars were detected. The five most prevalent, which accounted for 58.5 per cent of the isolates were Salmonella Heidelberg (16.2 per cent of the isolates), Salmonella Agona (15.8 per cent), Salmonella Derby (12.4 per cent), Salmonella Muenster (7.3 per cent) and Salmonella Anatum (6.8 per cent). In addition, a few rough isolates and isolates belonging to the antigenically incomplete formulae 6,7:-:- and 4,12:b:- were found. The level of antimicrobial resistance was low; the highest resistance was recorded to ampicillin (13.7 per cent) and streptomycin (9.0 per cent) followed by tetracycline (8.5 per cent), sulphonamides (7.7 per cent) and spectinomycin (4.7 per cent). Resistance to quinolones was very low: four isolates were resistant to nalidixic acid, and only one was resistant to enrofloxacin. No resistance was recorded to colistin, apramycin, ceftiofur, florfenicol, or amoxycillin with clavulanic acid. Only 24 isolates were resistant to two or more compounds in various combinations of up to six compounds; one Salmonella Havana isolate was resistant to six compounds. Six isolates were serovar Typhimurium, but none of them belonged to phage type DT104.  相似文献   

12.
The effect of molecular structure on the drug disposition and protein binding in plasma, the urinary recovery, and the renal clearance of sulphamerazine (SMR), sulphadiazine (SDZ), and sulphadimidine (SDM) and their N4-acetyl and hydroxy derivatives were studied in pigs. Following IV administration of SDM, SMR and SDZ, their mean elimination half-lives were 12.4 h, 4.3 h and 4.9 h respectively. The plasma concentrations of parent sulphonamide were higher than those of the metabolites, and ran parallel. The acetylated derivatives were the main metabolites; traces of 6-hydroxymethylsulphamerazine and 4-hydroxysulphadiazine were detected in plasma. The urine recovery data showed that in pigs acetylation is the major elimination pathway of SDM, SMR and SDZ; hydroxylation became more important in case of SMR (6-hydroxymethyl and 4-hydroxy derivatives) and SDZ (4-hydroxy derivatives) than in SDM. In pigs methyl substitution of the pyrimidine side chain decreased the renal clearance of the parent drug and made the parent compound less accessible for hydroxylation. Acetylation and hydroxylation speeded up drug elimination, because their renal clearance values were higher than those of the parent drug.  相似文献   

13.
Plasma drug concentrations were measured after two commercially available potentiated sulphonamides, trimethoprim and sulfadoxine and trimethoprim and sulphadiazine, were infused daily for 2 and 3 days, respectively, into the uteri of pony mares which had been mated before ovulation. Intravenous administration of trimethoprim and sulfadoxine allowed uterine absorption of trimethoprim (23-43%) and sulfadoxine (29-34%) to be calculated. After intra-uterine administration trimethoprim and sulphadiazine were detected in the milk of a lactating mare. In order to maintain plasma concentrations likely to be required for clinical efficacy of both drugs they should be administered every 12 h. However, infusions of both preparations caused endometrial inflammation as assessed by cytological and histological examination and this may have been responsible for the low pregnancy rate.  相似文献   

14.
Aetiology of diarrhoea in young calves   总被引：9，自引：0，他引：9  
Faeces samples were collected from 302 untreated calves on the day of onset of diarrhoea and from 49 healthy calves at 32 farms experiencing outbreaks of diarrhoea. At least four diarrhoeic calves were sampled on each farm, and samples were examined for rotavirus, coronavirus, cryptosporidium, enterotoxigenic Escherichia coli and Salmonella species. Although all these enteropathogens were excreted more frequently by the diarrhoeic than by the healthy calves, the difference was significant overall only for rotavirus. Rotavirus was excreted by 18 per cent of healthy calves, coronavirus by 4 per cent, cryptosporidium by 14 per cent, and no enterotoxigenic E coli or Salmonella species were detected. The most common enteropathogen in diarrhoeic calves was rotavirus, which was excreted by more than half the diarrhoeic calves on 18 farms. Coronavirus was excreted at a similar high prevalence on one farm, cryptosporidium on five farms and enterotoxigenic E coli on three farms. Concurrent infection with two or more microorganisms occurred in 15 per cent of diarrhoeic calves. There was no difference in the isolation rate of campylobacters between diarrhoeic and healthy calves.  相似文献   

15.
Phenylbutazone, sulphadiazine and trimethoprim were administered to three horses on two occasions, recently fed and unfed, and the effect of feeding on the pharmacokinetics of the three drugs assessed. The mean peak concentrations of phenylbutazone and trimethoprim were reduced by feeding by 34 and 75 per cent, respectively. The pharmacokinetics of sulphadiazine were not significantly affected.  相似文献   

16.
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17.
Summary

The effect of molecular structure on the drug disposition and protein binding in plasma, the urinary recovery, and the renal clearance of sulphamerazine (SMR), sulphadiazine (SDZ), and sulphadimidine (SDM) and their N4‐acetyl and hydroxy derivatives were studied in pigs. Following IV administration of SDM, SMR and SDZ, their mean elimination half‐lives were 12.4 h, 4.3 h and 4.9 h respectively. The plasma concentrations of parent sulphonamide were higher than those of the metabolites, and ran parallel. The acetylated derivatives were the main metabolites; traces of 6‐hydroxymethylsulphamerazine and 4‐hydroxysulphadiazine were detected in plasma.

The urine recovery data showed that in pigs acetylation is the major elimination pathway of SDM, SMR and SDZ; hydroxylation became more important in case of SMR (6‐hydroxymethyl and 4‐hydroxy derivatives) and SDZ (4‐hydroxy derivatives) than in SDM. In pigs methyl substitution of the pyrimidine side chain decreased the renal clearance of the parent drug and made the parent compound less accessible for hydroxylation. Acetylation and hydroxylation speeded up drug elimentation, because their renal clearance values were higher than those of the parent drug.  相似文献   

18.
One hundred and thirteen finishing pig units and 74 sow units in Catalonia, Spain, were examined to determine the prevalence of salmonella infections and the factors that could be associated with them. Pooled faecal samples were taken from the finishing units, and samples of faeces were collected from individual sows. The Salmonella isolates were serotyped, phage typed and examined for their antimicrobial susceptibility to 18 common antimicrobial drugs. In addition, blood samples from pigs on 141 farms were analysed by ELISA. In both the bacteriological and serological surveys, a questionnaire with 84 questions was completed for each farm. Salmonella species were isolated from 20 per cent of the finishing units and 24 per cent of the sow units; 14 serotypes were detected in the finishing pigs and 11 in the sows. More than 30 per cent of the strains were resistant to tetracycline, sulphonamides, ampicillin or streptomycin, and 69 per cent of the strains were resistant to three or more agents up to 10 compounds. Seventy-seven per cent of the farms had at least one seropositive animal, and 26 per cent of these farms had an individual seroprevalence of 50 per cent or more. The factors associated (P<0.05) with the excretion of Salmonella species in the finishing units were the practice of raising livestock other than pigs (odds ratio [OR]=6.18), the herd size (OR=5.87), and a past history of clinical salmonellosis (OR=4.97). For the sows, the factors associated (P<0.05) with the excretion of Salmonella species were having open-flushed drainage of sewage (OR=34.48), a lack of rodent control measures (OR=0.05) and the number of sows in the unit (OR=9.26). Factors associated with seropositivity in the finishing units were a lack of bird-proof nets (OR=0.30) and the use of water from private wells (OR=3.64).  相似文献   

19.
During the kidding season between January and April 2003, 10 farms were selected and divided into two groups of five. The farms in group A had had serious diarrhoeal illness and losses in neonatal kids the previous year, and there were Cryptosporidium parvum infections in kids associated with diarrhoea during the survey. On the farms in group B, there was no history of diarrhoeal disease the previous year and neither C parvum oocysts nor diarrhoea were detected in neonatal kids during the survey. Faecal samples were collected once from 10 adult goats aged between one and seven years on each farm. To assess more accurately the pattern of output of oocysts of C parvum and cysts of Giardia duodenalis by periparturient adult goats, one farm was selected from each group, faecal samples were collected weekly before and after kidding from 12 goats on the farm in group A and from 10 goats on the farm in group B. There was no significant difference in the prevalence of G duodenalis cysts between the group A farms (14 per cent) and the group B farms (12 per cent), and the numbers of cysts excreted ranged from 143 to 400 cysts per gram of faeces (cpg) on the group A farms and 72 to 334 cpg on the group B farms. There was a significant difference (P=0.03) in the prevalence of C parvum oocysts at the group level between the group A farms (20 per cent) and the group B farms (6 per cent). All the adult goats excreted cysts and oocysts at some date around the kidding period; the number of animals excreting cysts of G duodenalis or oocysts of C parvum increased when they gave birth, and seven to 10 times more cysts and oocysts were shed in the three weeks around kidding than in the period more than three weeks from kidding (P<0.001).  相似文献   

20.
Tissue residues of sulphadiazine (SDZ), sulphadimidine (SDD) and sulphquinoxaline (SQ) were studied in healthy and E. stiedai infected rabbits following oral administration of 0.5 g/l drinking water for 5 days. The solid-phase extraction and HPLC was used to determine the concentration of the three sulphonamides in a single tissue sample. SDZ was detected in the liver and kidney in concentrations below the tolerance levels at day 5 and no residues could be detected at day 7 after drug withdrawal. SDD and SQ were detected in all of the tested organs of healthy rabbits up to day 5, where the highest concentration was reported in the liver (0.08 +/- 0.02 and 0.09 +/- 0.02 g/g respectively). In infected rabbits, the three sulphonamides were detected up to day 7 in concentrations higher than the tolerance limits (> 0.1 g/g) in the liver and kidney and lower levels in other tissues. A withdrawal period of 4 days for SDZ and 5 days for SDD and SQ in healthy rabbits and 7 days for SDZ and 8 days for SDD and SQ in E. stiedai infected rabbits is suggested.  相似文献   

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