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1.
The penetration of penicillin into tissue cage fluid (TCF) in calves was studied after intravenous and intramuscular injection. The penicillin concentrations in TCF were lower than in serum and maximum was reached much later. Intravenous injection of benzyl-penicillin gave significantly higher levels in TCF than intramuscular injection. The penetration after procaine penicillin was very slow. The results showed that the serum peak rather than the area under curve determines the penetration of penicillin. Repeated intramuscular injections of benzylpenicillin and procaine penicillin caused an accumulation of penicillin in TCF. Similar levels were however reached by one single intravenous injection. The clinical counterparts to the used tissue cage model are abscesses. It was concluded that if high penicillin concentration are desireable in such foci, the drug must be given in a way that gives as high serum peaks as possible.  相似文献   

2.
A pilot study in two ponies showed that the plasma concentrations of intramuscularly administered procaine penicillin were higher if phenylbutazone was administered concurrently. In two other trials, each involving five horses, intravenous sodium penicillin was administered with and without concurrent intravenously injected phenylbutazone, and procaine penicillin was injected intramuscularly with and without oral phenylbutazone. In both cases the plasma concentrations of penicillin were higher when phenylbutazone was given. The pharmacokinetic parameters indicated that the effect was probably due to a lower peripheral distribution because the penetration of penicillin into the tissues was greatly reduced.  相似文献   

3.
Following concomitant intravenous administration of Tomanol and sodium penicillin G to six Dutch Friesian dairy cows a significant decrease in total body clearance of penicillin (34.7%) and a prolongation of the elimination half-life of penicillin (17.2%) was observed. Tomanol did not affect other pharmacokinetic parameters such as rate constants of drug transfer (k12/k21, alpha en beta), distribution volume of the central compartment (V1), and extrapolated serum drug levels. Intravenous or intramuscular administration of Tomanol had no effect on the tissue distribution of penicillin G, because neither a change in the ratios of muscle to serum and of kidney cortex to serum nor a change in an induced steady state level of low penicilline G serum concentrations was observed. From the data obtained it is concluded that concomitant Tomanol administration with penicillin induces an elevation of the serum penicillin concentration and prolongs the persistence of penicillin residues in carcass meat and organs.  相似文献   

4.
The affinity and the binding capacity of horse serum proteins for ampicillin and penicillin G were measured by equilibrium dialysis or ultrafiltration technique. From the figures thus obtained it may be concluded that in the range of therapeutic concentrations the protein-bound fraction accounts for 6 X 8-8 per cent of the total ampicillin concentration and for 52-54 per cent of the total penicillin G concentration in serum. The rate of elimination of ampicillin and penicillin G in horses was assessed by following serum concentrations after a single intravenous injection. The biological half life of ampicillin was found to be 93 min and that of penicillin G 53 min in adult horses with unimpaired circulation and intact kidney and liver function.  相似文献   

5.
Sodium penicillin, sodium cefazolin, and sodium citrate were administered to six adult horses on separate occasions, when awake and during anesthesia. The order of administration was randomized and studies were separated by a minimum of 7 days. Arterial blood pressure decreased significantly (less than 0.05) from control 5 minutes after intravenous (IV) sodium penicillin in awake and anesthetized horses. Systolic arterial blood pressure remained significantly (less than 0.05) decreased 10 minutes after IV sodium penicillin in anesthetized horses. Sodium cefazolin and sodium citrate did not significantly affect any of the measured cardiovascular variables. Although the changes in arterial blood pressure were small (8-15 mm Hg), monitoring of arterial blood pressure is advised when sodium penicillin is administered IV to anesthetized horses.  相似文献   

6.
Acute, severe hemolytic anemia occurred in a horse being treated for tetanus with intravenous penicillin and tetanus antitoxin. During treatment, the horse developed a positive direct antiglobulin test and a high titer (maximum 1:1024) of IgG anti-penicillin antibody. The horse recovered from the tetanus and penicillin induced hemolytic anemia, but later developed acute hepatic failure, probably resulting from the administration of equine origin tetanus antitoxin.  相似文献   

7.
健康长白猪7头,按拉丁方试验设计,进行单剂量静脉注射青霉素(20 000单位/kg体重)钠、硫酸双氢链霉素(20 000单位/kg体重)及肌肉注射普鲁卡因青霉素-硫酸双氢链霉素混悬剂(20 000单位/kg体重)的药物动力学研究。HPLC法和HPLC-MS/MS法分别测定血浆中的青霉素和双氢链霉素浓度,WinNonlin软件处理血药浓度-时间数据。静脉注射青霉素钠、硫酸双氢链霉素的药时数据最佳模型为三室开放模型。肌肉注射混悬剂后青霉素G的药时数据符合一级吸收一室模型。主要药物动力学参数:t1/2ka为0.66 h,t1/2β为5.80 h,t(max)为2.3 h,C(max)为1.66 mg/L,AUC为17.65,CL为0.69 L/h.kg,F为70.57%;肌肉注射混悬剂后双氢链霉素数据符合一级吸收二室开放模型,主要药动参数:t1/2ka为0.21 h;t1/2α为2.06 h;t1/2β为8.22 h,t(max)为0.8 h,C(max)为51.42 mg/L,AUC为280.74,F为101.96%。肌肉注射混悬液药物动力学特征为青霉素G吸收迅速,消除缓慢;双氢链霉素吸收迅速完全,消除缓慢,生物利用度高。  相似文献   

8.
Summary

Following concomitant intravenous administration of Tomanol® and sodium penicillin G to six Dutch Friesian dairy cows a significant decrease in total body clearance of penicillin (34.7%) and a prolongation of the elimination half‐life of penicillin (17.2%) was observed. Tomanol® did not affect other pharmacokinetic parameters such as rate constants of drug transfer (k12/k21, α en β), distribution volume of the central compartment (V1), and extrapolated serum drug levels. Intravenous or intramuscular administration of Tomanol® had no effect on the tissue distribution of penicillin G, because neither a change in the ratios of muscle to serum and of kidney cortex to serum nor a change in an induced steady state level of low penicilline G serum concentrations was observed. From the data obtained it is concluded that concomitant Tomanol® administration with penicillin induces an elevation of the serum penicillin concentration and prolongs the persistence of penicillin residues in carcass meat and organs.  相似文献   

9.
Tissue chambers, implanted subcutaneously on both sides of the neck in eight ponies, were inoculated with Streptococcus equi subsp. zooepidemicus in order to compare the clinical efficacy of trimethoprim/sulfadiazine (TMP/SDZ) and penicillin G treatment in a purulent infection. The TMP/SDZ treatment consisted of one intravenous (i.v.) injection of 5 mg/kg TMP and 25 mg/kg SDZ and the same dose of TMP/SDZ per os (p.o.), both given 20 h after inoculation. The oral dose was then repeated every 12 h for 21 days. The penicillin treatment consisted of one i.v. injection of 20 000 IU/kg sodium penicillin G and intramuscular (i.m.) injection of 20 000 IU/kg procaine penicillin G, both given 20 h after infection. The i.m. dose was then repeated every 24 h for 21 days. Eight ponies, each with two tissue chambers, were used in a cross over design; in the first experiment the left tissue chamber (TC) was infected and in the second experiment the right. TMP/SDZ treatment resulted in a limited reduction of viable bacteria in the TC but did not eliminate the infection, resulting in abscessation in 10-42 days in all eight ponies. However, penicillin treatment eliminated the streptococci in seven of eight ponies, and only one pony suffered abscessation on day 10. This constitutes a significantly better efficacy of the penicillin treatment in this model. The most probable cause of the failure of TMP/SDZ to eliminate the streptococci is inhibition of the action of TMP/SDZ in the purulent TCF. Therefore, TMP/SDZ should not be used to treat purulent infections in secluded sites in horses.  相似文献   

10.
We present a literature review on current techniques of intravenous regional anesthesia and intravenous regional antibiosis of the distal limb in cattle. Our own experiences performing a combined procedure of intravenous anesthesia and antibiosis (10 million I.U. benzylpenicillin sodium dissolved in 15-20 ml 2%-lidocaine hydrochloride) are discussed in detail. Complete anesthesia of the treated limb was achieved in 22 out of 23 cases (96%). The successfully treated animals did not express any symptoms of pain for the entire surgical procedure. In 2 out of 15 patients (13%) we observed serious post-surgical complications. The reason of which was extensive thrombosis of all veins distal of the tourniquet. The age of the clots at the time of slaughtering of the cows was determined histologically. A direct cause effect relationship between intravenous anesthesia/antibiosis and complication is indicated. We conclude that direct toxicity of the 2000-fold overdose of benzylpenicillin (as compared to generally accepted therapeutic levels) most likely caused the problem. We recommend to reduce the dose of penicillin in regional intravenous antibiosis to maximally 100,000 I.U., even in the case of local sepsis.  相似文献   

11.
Perioperative antimicrobial administration practices were evaluated retrospectively in 97 horses undergoing elective arthroscopy, and antimicrobial use was compared with standard recommendations for perioperative prophylaxis. Parenteral antimicrobials were administered perioperatively to 95/97 (98%) horses, 88 of which received intravenous sodium penicillin. Time from 1st dose until 1st incision ranged from 30 to 390 min [142 ± 55.6 min, mean ± standard deviation (s), median 135 min], and the first incision was performed greater than 2 half-lives after administration of sodium penicillin in 86/95 (91%) cases. Overall duration of therapy was 30.8 ± 24.2 h (mean ± s). Six (6.3%) horses received only a single preoperative dose, while 63 (66%) horses were treated for 24 h or less. While objective data regarding optimal perioperative antimicrobial prophylaxis are limited, the antimicrobial use practices observed here commonly deviated from standard recommendations for perioperative prophylaxis.  相似文献   

12.
Tissue chambers, implanted subcutaneously in ponies, were inoculated with Streptococcus zooepidemicus. The animals received either no antibiotics or one of the following treatments: pivampicillin per os (19.9 mg/kg, equivalent to 15 mg/kg ampicillin, every 12 h) for 7 or 21 days (7 and 5 ponies, respectively), procaine penicillin G intramuscularly (12 mg/kg = 12,000 IU/kg, every 24 h) for 7 days (7 ponies), or ampicillin sodium intravenously (equivalent to 15 mg/kg ampicillin, every 8 h) for 1 day (5 ponies). Only intravenous administration was started before infection (prophylactically), the other treatments were started 20 h after infection (curatively). A total of 7 ponies received no antibiotics. In untreated controls, the infection led to abscessation of the tissue chamber in 4 to 10 days. Curative treatment with either pivampicillin or procaine penicillin G for 7 days resulted in a reduction of viable bacteria in the tissue chamber but did not eliminate the infection, resulting in abscessation in 5 to 14 days. However, administration of pivampicillin for 21 days eliminated the streptococci in five out of five ponies and prophylactic administration of ampicillin was successful in three out of five ponies.  相似文献   

13.
Oral prophylactic medication with either procaine penicillin G or a mixture of chlortetracycline, sulphadimidine and procaine penicillin G reduced the incidence of streptococcal meningitis in a herd of pigs with a high recorded prevalence of the disease, but to a significant extent (P less than 0.01) only in those pigs receiving procaine penicillin G. Subsequent studies showed that after oral administration of procaine penicillin G, benzylpenicillin was detectable in plasma only at very low concentration and similar results were obtained using the potassium salt of penicillin G. However, phenoxymethyl penicillin administered orally provided high plasma concentrations of this drug. A further investigation demonstrated that despite the low plasma concentrations of penicillin after oral administration of the procaine salt, gastrointestinal and urinary concentrations of the drug were relatively high for up to five hours.  相似文献   

14.
The plasma penicillin concentrations were determined in 5 horses given an IV injection of sodium penicillin G; plasma penicillin concentrations were also determined in a crossover experiment, where animals were given procaine penicillin G subcutaneously at 1 site and IM at 4 sites. The mean penicillin plasma peak concentration and bioavailability were highest after the drug was injected in the neck and biceps musculature. Injections in the gluteal muscle and in the subcutaneous sites resulted in similar, but lower, more persistent penicillin plasma concentrations and a lower bioavailability than were obtained with injection in the neck and biceps musculature. The pharmacokinetic data obtained after penicillin was administered via the pectoral muscle route exhibited an intermediate position. Therapeutic implications of the routes of administration with respect to hemolytic streptococcal infections are discussed.  相似文献   

15.
The bioavailability of penicillin and dihydrostreptomycin from three penicillin/ aminoglycoside fixed combination products for intramuscular injection was investigated in a four-way, randomized, crossover experiment in rabbits. Attention is focused on bioequivalence based on plasma concentration vs. time profiles to study whether the rabbit is a good model to detect differences in in vivo delivery of penicillin and/or dihydrostreptomycin after intramuscular administration of different products. In all products, penicillin was present as a suspension. Although the extent of absorption of penicillin did not differ between the three products, large differences in the rates of absorption were observed. With respect to dihydrostreptomycin, no significant differences were observed between the products. The results from this study demonstrate that the rabbit is a good model to detect differences in bioavailability of suspended penicillin from penicillin/dihydrostreptomycin fixed combination products for intramuscular injection. A study with the same products is presently being carried out in calves to investigate whether bioequivalence studies in rabbits could replace studies in the target animals.  相似文献   

16.
OBJECTIVE: To compare the pharmacokinetics of penicillin G and procaine in racehorses following i.m. administration of penicillin G procaine (PGP) with pharmacokinetics following i.m. administration of penicillin G potassium and procaine hydrochloride (PH). ANIMALS: 6 healthy adult mares. PROCEDURE: Horses were treated with PGP (22,000 units of penicillin G/kg of body weight, i.m.) and with penicillin G potassium (22,000 U/kg, i.m.) and PH (1.55 mg/kg, i.m.). A minimum of 3 weeks was allowed to elapse between drug treatments. Plasma and urine penicillin G and procaine concentrations were measured by use of high-pressure liquid chromatography. RESULTS: Median elimination phase half-lives of penicillin G were 24.7 and 12.9 hours, respectively, after administration of PGP and penicillin G potassium. Plasma penicillin G concentration 24 hours after administration of penicillin G potassium and PH was not significantly different from concentration 24 hours after administration of PGP. Median elimination phase half-life of procaine following administration of PGP (15.6 hours) was significantly longer than value obtained after administration of penicillin G potassium and PH (1 hour). CONCLUSIONS AND CLINICAL RELEVANCE: Results suggest that i.m. administration of penicillin G potassium will result in plasma penicillin G concentrations for 24 hours after drug administration comparable to those obtained with administration of PGP Clearance of procaine from plasma following administration of penicillin G potassium and PH was rapid, compared with clearance following administration of PGP.  相似文献   

17.
The efficacy of intramammary treatments containing procaine penicillin G alone (treatment A) or a combination of procaine penicillin G and neomycin (treatment B) was compared in treating clinical bovine mastitis caused by gram-positive bacteria susceptible in vitro to penicillin G. Both treatments were supplemented with a single intramuscular injection of procaine penicillin G on the first day of treatment. The study was carried out using a double blind design on commercial dairy farms in Southern Finland. A total of 56 quarters were treated with treatment A and 61 with treatment B. The cure rates for both treatments were equal, which suggests that the use of the penicillin G-aminoglycoside combination does not increase the efficacy of the treatment over that achieved by using penicillin G alone in bovine clinical mastitis caused by penicillin-susceptible, gram-positive bacteria.  相似文献   

18.
The veterinarian in clinical practice is often confronted with cases of mastitis that require systemic antibacterial treatment in addition to local treatment. This paper reviews the suitability of drugs available in New Zealand, taking into account their anti-staphylococcal activity, routes of administration, and their ability to attain and maintain therapeutic levels in the udder following systemic administration. The drugs considered include the more common penicillins, aminoglycosides and macrolides; oxytetracyline, chloramphenicol, trimethoprim, and several sulphonamides.

The success of systemic therapy against mastitis depends to a large extent on the concentration of antibacterial drug achieved at foci of infection. Passage of drugs across the blood-milk barrier takes place by passive diffusion, and the factors influencing this diffusion are discussed.

Whe mastitis is associated with sensitive organisms, penicillin is recommended, although, as with all other antibacterials discussed, the dose used must be higher than normal. For penicillin, doses of the order of 16,500 iu/kg are recommended.

The intramuscular injection of oxytetracycline will not produce therapeutic levels in milk but, after intravenous injection of high doses (10 mg/kg), this antibiotic is likely to maintain therapeutic levels in milk over a 24-hour period.

As a first choice for the systemic treatment of mastitis, either tylosin or erythromycin is recommended. At a dose rate of 12.5 mg/kg, either will maintain for 24 hours milk levels in excess of the average MICs for staphylococci.

Of the sulphonamides, sulphanilamide and sulphadimidine produce the highest milk levels. After intravenous administration at a dose rate of 200 mg/kg, sulphadimidine will maintain therapeutic levels in milk for 12 hours.

Although trimethoprim has a very short half-life in cattle which limits its usefulness, it readily enters the milk and a combination of trimethoprim (as a suspension) with sulphadiazine, at a dose rate of 48 mg/kg, might be expected to maintain therapeutic levels in the milk for 12 hours.

It is concluded that dihydrostreptomycin, neomycin, chloramphenicol, and the combination sulphadoxine/trimethoprim, are not suitable for the systemic treatment of bovine mastitis.  相似文献   

19.
It has been reported that antibiotics of the penicillin family impair the functional response of human, canine and lapine platelets to a broad range of agonists. In contrast, we have shown that the bovine platelet retained full functional responses to stimulation by adenosine diphosphate (ADP) or platelet activating factor (PAF) following administration of penicillin G to clinically normal cattle at 20,000 IU/kg for three days. The aggregation response to collagen was transiently reduced to approximately 50% of pretreatment values, but only while the drug was detectable in the circulation. When penicillin was added to platelet rich plasma suspensions, ADP-induced aggregation was similar to that of the control untreated platelets, while the PAF-induced aggregation response was reduced by not more than 25%. Only collagen-induced aggregation exhibited a modest dose-dependent inhibitory response in the presence of penicillin. It is postulated that the relative insensitivity of the bovine platelet to penicillin may be related to differences in postreceptor biochemical events compared to the human platelet.  相似文献   

20.
A profile off the penicillin concentration in bovine conjunctival sac fluid (CF) was determined after a single subconjunctival injection of procaine penicillin (6 x 10(5) iu in 2ml). When the injection was made through the skin of the upper eye lid, the duration of therapeutic concentration was significantly greater (P<0.01) than when the injection had been given by the perconjunctival route: approximately 68 hours or 40 hours respectively. These findings support the clinical use of subconjunctivally administered procaine penicillin in the treatment of infectious bovine keratoconjunctivitis. A single application of an equivalent dose of either procaine penicillin or benethamine penicillin, applied topically in a simple occulentum base, produced a therapeutic duration in CF of 37 +/- 4 hr and 56 +/- 4.5 hr respectively.  相似文献   

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