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At least 19 recordsLinked to original sources
PubMed1982

[Evaluation of clinical efficacy of sulbenicillin following surgery of malignant maxillary tumors. Transport of sulbenicillin to the exudates from the surgical wound of the maxilla and its therapeutic effects].

In order to know the amount of sulbenicillin (SB-PC) transported to the maxillary sinus through the blood supply after injecting by intravenous drip infusion, the authors measured SB-PC content of the exudate which was gathered from the exploratory operative maxillary sinus. This measurement was performed 3 times at 2, 4 and 6 hours after injecting 5 g of SB-PC by intravenous drip infusion. From results of these measurements, it became obvious that the SB-PC content reached to the maximum value (24.5 +/- 16.69 mcg/ml) at 2--4 hours after the injection. Next, the preventive and therapeutic effect on the postoperative maxillary infection was evaluated for 13 patients of maxillary cancer. The effect was excellent in 2 cases (16.7%), good in 8 cases (66.7%) and fair in 2 cases (16.7%). So, the ratio of effectiveness was 83.3%. The side effect of SB-PC was observed only in 1 patient who complained of palpitation, but it was not severe.

Adult↗
PubMed1987

Electron microscopy of Pseudomonas aeruginosa treated with sulbenicillin and dibekacin.

A possible mechanism responsible for the combined effects of sulbenicillin and dibekacin on Pseudomonas aeruginosa IAM 1007 was investigated. The bactericidal activity of the above two drugs in combination was very strong. The regrowth of test strains after removal of the drugs was suppressed markedly, even when they were exposed to sulbenicillin plus dibekacin at a subinhibitory concentration of individual drugs. Sulbenicillin caused elongation of the bacterial cells. At the early stage of elongation, no demonstrable changes of ultrastructure of the cell wall were observed. At the late stage, lysis of the peptidoglycan layer occurred and spheroplast was formed. However, most of the outer membrane of the cell wall remained intact. Sulbenicillin acts upon the peptidoglycan layer, but not on the outer membrane. Thus it is difficult for sulbenicillin alone to cause cell lysis. On the other hand, dibekacin caused destruction of ribosomes and lysis of the outer membrane of the cell wall. Both sulbenicillin and dibekacin act on the cell wall, the former on the peptidoglycan layer (the inner membrane) and the latter on the outer membrane. The combined use of sulbenicillin and dibekacin caused elongation of bacilli and severe destruction of the inner and outer membranes of the cell wall. These morphological changes occurred even when the concentration of the individual drug was lower than its minimum inhibitory concentration (MIC). Furthermore, the cells elongated by sulbenicillin were ruptured easily when treated with dibekacin subsequently. The bacilli treated with dibekacin at a concentration lower than MIC and then treated with sulbenicillin at a concentration lower than MIC showed a marked elongation of the cells, which indicated that the effects of sulbenicillin was enhanced by dibekacin. These findings suggested strongly that sulbenicillin and dibekacin act on cell wall constituents and that their effects were complementary and synergistic.

Cell Wall↗
PubMed1978

Bacteriological and clinical studies of sulbenicillin.

A new semi-synthetic penicillin, sulbenicillin, was evaluated with regard to clinical effect on infections caused by Pseudomonas aeruginosa and other bacteria, serum concentrations obtained after intravenous administration and antibacterial spectrum, in comparison with the closely related antibiotic carbenicillin. The antibacterial spectra of sulbenicillin and carbenicillin were similar but the MIC values were lower for sulbenicillin against most of the bacterial strains tested. The serum concentrations obtained after administration of 5 g sulbenicillin were significantly higher than those obtained after 5 g carbenicillin although no significant differences in serum half-lives were observed. The clinical effect of sulbenicillin--alone or alternating with carbenicillin--on pseudomonas infections with varying localisation was found to be good in 11 and fair in 3 of 16 treated patients. Two treatment failures were cases of chronic wound infection. In addition to the pseudomonas infections, 9 of the patients also had concurrent infections with other bacteria, e.g. pencillinase-producing staphylococci and Klebsiella, and in all these cases bacterial growth was eliminated during therapy. No serious side effects were observed during sulbenicillin treatment but some of the patients developed massive growth of fungi in the urine, which disappeared after the treatment was stopped.

Aged↗
PubMed1978

Comparative in vitro activities of SCE-129, sulbenicillin, gentamicin, and dibekacin against Pseudomonas.

Against sulbenicillin- and gentamicin-susceptible strains of Pseudomonas aeruginosa, SCE-129 was about 10 times more active than sulbenicillin and had a similar activity to gentamicin and dibekacin. Sulbenicillin-resistant strains of P. aeruginosa were moderately resistant to SCE-129, whether these strains were gentamicin-resistant or not. Gentamicin-resistant strains of P. aeruginosa were resistant to dibekacin but not to SCE-129. Against P. maltophilia, the minimum inhibitory concentration of SCE-129 resembled those of sulbenicillin, gentamicin, and dibekacin. Most strains of P. cepacia were moderately resistant to SCE-129 and sulbenicillin and highly resistant to gentamicin and dibekacin.

Cefsulodin↗
PubMed1978

Comparative in vivo activities of cefsulodin, sulbenicillin, and gentamicin against Pseudomonas aeruginosa.

The in vivo activities of cefsulodin, sulbenicillin, and gentamicin were compared in mice infected intraperitoneally with Pseudomonas aeruginosa. In mice infected with sulbenicillin- and gentamicin-susceptible strains, cefsulodin was about 12 to 60 times more active than sulbenicillin and had an activity similar to gentamicin. In mice, the activity of cefsulodin was independent whether the strains were resistant to gentamicin or not, but it was considerably affected by resistance of the strains to sulbenicillin.

Animals↗
PubMed1982

Placental transfer of disodium sulbenicillin.

The concentrations of sulbenicillin in maternal and fetal blood and in the amniotic fluid compartment were measured in 27 women at parturition. With an intramuscular injection of 2,000 mg of sulbenicillin, the highest concentration of sulbenicillin in maternal blood (109.0 micrograms/ml) was attained at 55 min. The highest concentrations in umbilical cord blood (approximately 25 micrograms/ml) were attained between 1 and 3 h after dosage. The peak concentration in amniotic fluid (27.1 micrograms/ml) was attained approximately 7.5 h after sulbenicillin administration.

Adult↗
PubMed1988

Effect of ursodeoxycholate on the biliary excretion of cefotiam and sulbenicillin in patients with percutaneous transhepatic biliary drainage.

The effects of ursodeoxycholate administration on the biliary excretion of the antibiotics cefotiam and sulbenicillin were studied in five patients with stable hepatic function receiving percutaneous transhepatic biliary drainage for obstructive jaundice. Cefotiam (I g) and sulbenicillin (2 g) were administered intravenously before and after ursodeoxycholate administration, and the maximum concentrations of the antibiotics in the bile and total amounts excreted in the bile during the 4 h after administration were determined. After ursodeoxycholate administration, both the maximum concentration of cefotiam in the bile and the amount excreted increased significantly. Ursodeoxycholate also increased the peak concentration and total excretion of sulbenicillin. For both cefotiam and sulbenicillin, the amount of antibiotic excreted in the bile during the 4 h after administration showed a significant correlation with the amount of bile acids excreted in the bile. This strongly suggests a common mechanism for the biliary excretion of these antibiotics and bile acids. Ursodeoxycholate administration is a benign way to increase both the concentration and the total amount of antibiotic excreted in the bile. Therefore, it may be useful in the treatment of serious biliary tract infections, especially in patients receiving biliary drainage.

Aged↗
PubMed1987

Sulbenicillin: pharmacokinetics and penetration into bronchial secretion in elderly patients.

This study evaluates the pharmacokinetics of sulbenicillin (alpha-sulfobenzylpenicillin) in elderly subjects after single and multiple doses and the penetration into bronchial secretion in elderly patients with chronically superinfected bronchial pathology. Peak plasma levels were 53.34 micrograms/ml (group I); 55.80 and 57.82 micrograms/ml (group II) after 1 h. The half-life (t 1/2 beta) was 1.47 h (group I); 1.49 and 1.62 h (group II). Renal clearance was 6.68 l/h; 6.25 and 5.44 l/h; whereas the volume of distribution was 18.02 l; 17.84 and 17.21 l for groups I and II respectively. The mean percentage of the recovered active drug in urine over 12 h was 77.72% of dose. The mean peak reaching the bronchial secretion was 3.60 micrograms/ml at the 4th hour. The results of the multiple dose study indicated that there was no apparent change in the distribution or elimination kinetics of sulbenicillin after 2 g i.m. administration. Thus, the kinetics from the multiple dose study were in close agreement with those from the single dose study and no accumulation of sulbenicillin was observed. This study provided satisfactory results and confirmed the significant presence of sulbenicillin into bronchial secretions.

Absorption↗
PubMed1982

[Concentration of sulbenicillin in human serum and myocardial tissue].

The concentration of sulbenicillin in the serum and myocardial tissue of 13 patients were determined at cardiac surgery. About 100 mg/kg of sulbenicillin were administered intravenously for 60 minutes. Right auricle resected at the vena caval cannuration was examined for myocardial tissue. The serum concentration was also examined every 30 minutes after injection, 30 minutes, 60 minutes, 90 minutes, 120 minutes and 150 minutes. Mean values of serum concentration were 213.6 micrograms/ml, 432.5 micrograms/ml, 181.6 micrograms/ml, 236.3 micrograms/ml and 101 micrograms/ml, respectively. The values determined in myocardial tissue were 146.5 micrograms/g (60 minutes), 39.2 micrograms/g (90 minutes), 66.0 micrograms/g (120 minutes) and 23.5 micrograms/g (150 minutes). The mean value of concentration ratio of sulbenicillin in myocardial tissue was 0.23 of serum concentration. The high myocardial tissue levels of sulbenicillin suggests that its use at cardiovascular surgery would protect the myocardial tissue from the bacterial infections.

Adolescent↗
PubMed1978

Inhibition of platelet function by sulbenicillin and its metabolite.

The effect of sulbenicillin and its major metabolite, alpha-sulfobenzylpenicilloic acid, on platelet function was investigated. Sulbenicillin caused inhibition of platelet aggregation and release reaction in the same manner as carbenicillin. alpha-Sulfobenzylpenicilloic acid was found to cause much stronger inhibition of platelet function. The results indicate that the strong inhibitory action of alpha-sulfobenzylpenicilloic acid may also take part in impaired platelet functions following administration of sulbenicillin to humans.

Blood Platelets↗
PubMedDate not supplied

[Bactericidal and potent antiadhesive activity of sulbenicillin].

Sulbenicillin, a wide broad spectrum penicillin, is active against a lot of gram positive and gram negative bacteria. The AA. studied the activity of this molecule against urinary infections causing germs, by evaluating two parameters: his antiadhesive capability and the Killing curves, in comparison with mezlocillin and piperacillin. An inhibition in adhesive capability of test-germs, due to sulbenicillin was obtained. Furthermore, resulting Killing curves showed more rapidity in action for sulbenicillin than for the two others molecules, versus resistant germs, like P. aeruginosa and S. faecalis.

Bacterial Adhesion↗
PubMed1987

Evaluation of the minimal bactericidal time (MBT) of sulbenicillin against multiresistant pathogens.

The in vitro antibacterial activity of sulbenicillin was evaluated against multiresistant strains isolated from in-patients and compared with that of carbenicillin and piperacillin. Sulbenicillin resulted in being as active as the other drugs against the strains tested, both at different pH, and at different bacterial inocula. In the time-kill tests sulbenicillin demonstrated bactericidal activity similar to that of piperacillin, and a higher killing rate when compared with that of carbenicillin.

Bacteria↗
PubMed1985

Antibacterial activity in vitro of sulbenicillin against mucoid and non-mucoid strains of Pseudomonas aeruginosa.

The in vitro antibacterial activity of sulbenicillin against a number of mucoid and non-mucoid strains of Pseudomonas aeruginosa was investigated and compared with that of some other beta-lactam antibiotics. From the data reported it is evident that sulbenicillin showed better anti-microbial activity than carbenicillin in almost all the tests run. Sulbenicillin appears to have a somewhat lower activity than piperacillin and cefotaxime; however, cefotaxime and particularly piperacillin are highly conditioned by the inoculum size and have a less favourable MBC to MIC ratio.

Ampicillin↗
PubMed1985

Clinical assessment of sulbenicillin in acute respiratory tract infection.

The effectiveness of sulbenicillin was assessed in the treatment of 15 adults, 12 suffering from bronchopneumonia and three from lobar pneumonia. Six patients had concomitant complications. At a parenteral dose of 2 g twice or thrice daily for at least seven days, all patients became afebrile by the sixth day, and chest X-rays became normal in nine patients and improved in five. It is concluded that sulbenicillin, which was well tolerated, is clinically effective in the treatment of severe respiratory tract infections, also in patients with major impairment of their immune response systems.

Adult↗
PubMed1985

Results of treatment with sodium sulbenicillin in thirty elderly patients with acute bronchopulmonary infection.

Thirty elderly patients with acute bronchopulmonary infections were treated with intravenous sodium sulbenicillin for up to 20 days at a dose of 4-6 g/day. Clinical results were excellent in 19 cases and good in 10 cases. In one case treatment had to be discontinued due to a dermal side-effect. It is concluded that sulbenicillin is a useful therapy for acute bronchopulmonary infections in the elderly.

Aged↗
PubMed1985

Multicentre clinical and bacteriological study of sulbenicillin in patients with bronchopulmonary infection.

In view of the pharmacodynamic and therapeutic properties of a broad-spectrum semisynthetic penicillin recently introduced in Italy, namely sulbenicillin, the authors conducted a multicentre clinical and bacteriological trial of the drug administered by intramuscular or intravenous injection in daily doses of 4, 6 or 8 g given in two or three administrations daily to a group of 66 patients with acute bronchopulmonary infection, mainly exacerbation of chronic infection, hospitalized in four Pneumology Centres of Sardinia. The authors assessed clinical, radiological, microbiological, and biohumoral parameters before and after treatment to provide a basis for assessing test product effectiveness and tolerability. On the strength of their findings, the authors concluded that the clinical and bacteriological activity of sulbenicillin was satisfactory and its local and general tolerability was excellent. The assembled findings indicate that the new antibiotic molecule can be used to advantage in the treatment of nontubercular bronchopulmonary infections, including severe or otherwise "difficult" cases, providing that the drug is administered at adequate dosages and for sufficiently long treatment periods.

Adolescent↗
PubMed1976

[Studies on the intravenous administration of sulbenicillin (author's transl)].

Basic and clinical investigation on the intravenous administration of sulbenicillin in moderate dose (510g daily) was carried out to evaluate its clinical effect in systemic infections due to gram-negative bacilli. The following results were obtained. (1) In human subjects received 5 g intravenous drip infusion, the peak blood levels were found at the end of infusion. In 6 cases with normal renal function (Ccr greater than or equal to 70ml/min.) the peak blood level was 181 mcg/ml on the average and the half-life 1.1 hours, while in 3 cases with impaired renal function (Ccr less than 70 ml/min.) the peak level 216 mcg/ml and the half-life longer than 2 hours. The height of the peak level seemed to be subjected to the duration of infusion. The renal excretion of sulbenicllin was 55.2% on the average both in cases with normal and impaired renal functions. (2) Sulbenicillin, 510g daily divided in 2 doses, was administered to 15 cases including 6 cases with acute pyelonephritis, 3 with acute cystitis, 3 with biliary tract infection, 2 with respiratory tract infection and 1 with acute prostatitis. All the cases except 3 cases with acute pyelonephritis had underlying diseases. Escherichia coli was isolated from 10 cases, Klebsiella from 2, Pseudomonas aeruginosa from 1, and unidentified gram-negative bacilli from 1. Eleven cases responded to the treatment, but 4 cases failed. In 11 cases with susceptible bacteria, 8 cases responded bacteriologically (2 cases recurred), and 3 cases failed to respond. A case with biliary tract infection due to E. coli did not respond to 5 g daily treatment, but responded to 5 g twice daily. Two cases due to organisms which were not inhibited by 200mcg/ml in vitro did not respond to the treatment. (3) A moderate decrease in red blood cell number and hemoglobin content was observed in one case. A transient increase in transaminase and alkaline phosphatase level was observed in other cases.

Adult↗
PubMed1976

[Studies on synergistic effect of sulbenicillin and dibekacin against gram-negative bacilli (author's transl)].

In vitro synergism of sulbenicillin and dibekacin was investigated with 19 strains of E. coli, 20 strains of Enterobacter and 20 strains of Pseudomonas aeruginosa on agar plates. As the results, sulbenicillin and dibekacin were found to be synergistically bacteriostatic against all these organisms, though the synergistic effects were somewhat less potent against E. coli. The concentrations of dibekacin required for assuming a clear synergism were 0.78 approximately 1.56 mug/ml.

Dibekacin↗