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.

[Therapeutic effect of sulfobenzyl-penicillin (SB-PC) on the concentration of SB-PC in human bile (author's transl)].

Sulfobenzyl-penicillin (SB-PC) is currently being investigated for use in man. The purpose of this study was to evaluate effect of SB-PC on Salmonella typhosa and biliary excretion of SB-PC in disease of the biliary tract. 1) Clinically, typhoid carriers without cholelithiasis were initiated with 4.0 g/day of SB-PC. Stool and bile became negative for Salmonella typhosa 14 days after initial treatment. 2) In typhoid carriers with cholelithiasis, Salmonella typhosa were not isolated from bile, wall of the gallbladder and surface of gallstone, but were isolated from nuclei of gallstones. The treatment of typhoid carriers with cholelithiasis may belong to a most difficult problem. 3) Biliary excretion of SB-PC in the patient given a single dose of 2.0 g/day im. was markedly dependent on characteristics of the patient, situation of external drainage and volume of bile excretion. High concentration in bile in some patient was 298 mug/ml at 3 hours after administration. 4) In intravenous administration of single dose of 6.0 g. maximum concentration in bile was about 2,000 mug/ml at 2 hours after administration and bactericidal concentration was obtained for resistant bacteria (Pseudomonas, Proteus, etc.) in biliary infection. 5) As side effects, pain and redness were infrequent after im. administration. Toxicity was not experienced in the patients injected intravenously.

[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.

[Comparative clinical study of aspoxicillin and sulbenicillin in postoperative wound infections].

A well-controlled comparative study was performed to evaluate efficacy, safety and utility of aspoxicillin (ASPC) as compared with sulbenicillin (SBPC) in the treatment of postoperative wound infections. Either 2 g of ASPC or 2 g of SBPC was administered to patients by intravenous drip infusion twice a day for 7 days. The following results were obtained: Overall clinical effectiveness rates were 82.5% (66/80) in ASPC group and 77.0% (57/74) in SBPC group, with no statistically significant difference between 2 groups. Final overall clinical improvement rates were 83.8% (67/80) in ASPC group and 81.1% (60/74) in SBPC group, with no statistically significant difference between 2 groups. As to bacteriological effectiveness, eradication rates of clinical isolates were 70.4% (38/54) in ASPC group and 74.4% (32/43) in SBPC group. There was no statistically significant difference in 2 groups. Side effects and abnormal laboratory findings were observed in 6 cases (6.7%) and 11 cases (12.4%) in ASPC group (89 cases) respectively, and 4 cases (4.4%) and 7 cases (7.8%) in SBPC group (90 cases) respectively. Especially severe adverse reactions were not observed, and there was no significant difference in the incidences of side effects and abnormal laboratory findings between 2 groups. As to overall clinical utility, utility rates were 77.5% (62/80) in ASPC group and 70.3% (52/74) in SBPC group. There was no statistically significant difference between 2 groups. These results may be indicated that ASPC is as useful as SBPC in the treatment of postoperative wound infections.

Retinal toxicity of antibiotics: evaluation by electroretinogram.

Toxicity of an intravitreal injection of gentamicin sulfate, disodium sulbenicillin and cefazolin sodium on the retina was investigated by electroretinogram in albino and pigmented rabbits. Recordings were made before injection and 2 hours and 3, 7, 14, and 21 days after injection. Significant differences were found in the susceptibility of the electroretinogram components to various antibiotics as follows. Gentamicin 0.24 mg/0.1 ml irreversibly abolished all the components examined. Sulbenicillin 4.0, 8.0, or 12 mg/0.1 ml transiently suppressed the b-wave and the oscillatory potentials incrementally with increasing dose. Cefazolin 0.5, 2.0, or 5.0 mg/0.1 ml selectively reduced the oscillatory potentials, leaving the a- and b-waves almost unattenuated. The cefazolin-suppressed oscillatory potentials recovered within 14 days after injection. Judging from the most susceptible electroretinogram components to each antibiotic, we recommend intravitreal doses of these antibiotics for clinical use as follows: gentamicin 0.1 mg/0.1 ml, sulbenicillin 2 mg/0.1 ml, and cefazolin 0.25 mg/0.1 ml.