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PubMed1992

Structure of the extracellular polysaccharide from slime-forming Lactococcus lactis subsp. cremoris SBT 0495.

The extracellular polysaccharide obtained from slime-forming Lactococcus lactis subsp. cremoris SBT 0495 is composed of D-glucose, D-galactose, L-rhamnose, and phosphate. Methylation analysis of the native and dephosphorylated polysaccharides provided information on the linkage of the sugar residues and the location of the phosphate group. N.m.r. spectroscopy confirmed the structure of the polysaccharide, which is assigned the following repeating-unit: [formula: see text]

Carbohydrate Sequence↗
PubMed1989

[Pharmacokinetic, bacteriological and clinical studies of sulbactam/ampicillin in pediatric patients].

Plasma and urine concentrations of sulbactam (SBT) and ampicillin (ABPC) were determined following bolus administration of injectable SBT/ABPC combined in a fixed ratio of 1:2 to 6 pediatric patients, 3 at a dose of 30 mg/kg and the other 3 at 60 mg/kg. Clinical and bacteriological efficacies of SBT/ABPC were evaluated in a total of 65 patients composed of 45 cases with pneumonia, 3 cases each with bronchitis, urinary tract infections, staphylococcal scalded skin syndrome, purulent lymphadenitis, 2 cases each with tonsillitis, pleuropneumonia, phlegmon and 1 case each with pyothorax, submaxillitis. The dosage used was 101.2 mg/kg daily given in 3 or 4 divided doses (t.i.d. in 24 patients and q.i.d. in 41 patients) by bolus intravenous injection for 7 days on an average. Side effects and effects on clinical laboratory parameters were monitored in the 65 patients. The results of these evaluations are summarized as follows. 1. Mean serum concentrations of SBT and ABPC in 3 children each given an intravenous bolus injection of 30 mg/kg and other 3 each given 60 mg/kg reached peak levels at 5 minutes after administration with values of 49.8 and 90.3 micrograms/ml, respectively, for SBT and 99.8 and 189.7 micrograms/ml, respectively, for ABPC. The latter values were about twice as high as SBT, and both were dose-related. Mean half-lives were 0.889 hour for SBT and 0.857 hour for ABPC in the 30 mg/kg group and 0.882 hour for SBT and 0.834 hour of ABPC in the 60 mg/kg group, showing similarities between the 2 dosage groups as well as between SBT and ABPC. 2. Mean urine concentrations in the 2 groups mentioned above were the highest for both SBT and ABPC during the first 2 hours after administration, with values of 1,677 micrograms/ml for SBT and 2,730 micrograms/ml for ABPC in the 30 mg/kg group and 2,693 micrograms/ml and 3,623 micrograms/ml, respectively, in the 60 mg/kg group. Mean recovery rates in urine in the first 6 hours were 72.4% for SBT and 56.8% for ABPC in the low dosage group and 72.7% and 52.0%, respectively, in the high dosage group. In the 2 groups, the amounts of ABPC recovered were less than those of SBT. 3. Clinical efficacies of SBT/ABPC in 65 patients with various bacterial infections were excellent or good in 62 (95.4%) patients. 4. The bacteriological efficacy was evaluable with 10 patients. The pathogenic bacteria were eradicated in 9 patients and the efficacy rate was 90%.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗
PubMed1984

[Bacteriological, pharmacokinetic and clinical studies on sulbactam/cefoperazone in the pediatric field].

Bacteriological and clinical effect of a newly developed SBT/CPZ in the treatment for pediatric patients was assessed by a study group consisting of 15 institutions. The results were as follows. Antibacterial effect Susceptibility studies were performed with 93 clinical isolates. The MIC of SBT/CPZ was one-tube inferior or almost similar to that of CPZ in susceptible organisms. In CPZ-resistant organisms at the inoculum of 10(8) cells/ml, however, SBT/CPZ was much superior to CPZ on the basis of the MIC. When the MIC of SBT/CPZ was compared to that of CPZ in 27 strains which have high beta-lactamase-producing activity, it was found that many of CPZ-resistant organisms were susceptible to SBT/CPZ. Serum concentration and urinary excretion The serum concentrations of SBT and CPZ were 33.2 micrograms/ml, respectively at 15 minutes after 20 mg/kg SBT/CPZ was administered by intravenous bolus injection, and those of SBT and CPZ, 51.0 micrograms/ml and 108.3 micrograms/ml, respectively following 40 mg/kg SBT/CPZ therapy. The serum concentrations of CPZ were 2.1-2.4 times as high as those of SBT. The concentrations were dose-related. The half-lives of SBT and CPZ following 20 mg/kg SBT/CPZ administration were 0.94 hour and 1.50 hours, respectively, and those following 40 mg/kg SBT/CPZ were 0.95 hour and 1.53 hours, respectively. There was no significant difference between 20 mg/kg and 40 mg/kg administrations. When compared between SBT and CPZ, CPZ had slightly longer half-lives. At the termination of 1 hour drip infusion of 20 mg/kg SBT/CPZ, the serum concentrations of SBT and CPZ were 16.7 micrograms/ml and 40.1 micrograms/ml, respectively. In the case of 40 mg/kg, the levels of SBT and CPZ were 38.6 micrograms/ml and 94.9 micrograms/ml, respectively. The concentrations were found to be dose-related as were following intravenous bolus injections. The SBT half-lives obtained after 20 mg/kg and 40 mg/kg SBT/CPZ administrations were 1.39 hours and 0.89 hour, respectively; those of CPZ, 2.00 hours and 1.44 hours, respectively. The highest urinary concentration occurred 0-2 hours after intravenous bolus injections of 20 mg/kg or 40 mg/kg SBT/CPZ. Urinary excretion of SBT over 6 hours was 60.0% and 67.7%, and that of CPZ, 21.2% and 25.0%, indicating higher urinary excretion for SBT. When 20 mg/kg SBT/CPZ or 40 mg/kg was administered over 1 hour by drip infusion, urinary excretion became the highest at 1-3 hours after administration. Urinary excretion of SBT over 7 hours following 20 mg/kg and 40 mg/kg SBT/CPZ was 68.8% and 80.3%, respectively, and that of CPZ, 24.4% and 27.3%. The results were similar to those observed following intravenous bolus injections.

Adolescent↗
PubMed1984

[Fundamental and clinical studies of sulbactam/cefoperazone in the pediatric field].

Fundamental and clinical studies were carried out on sulbactam/cefoperazone (SBT/CPZ) in the field of pediatrics. The following results were obtained: A total of 185 clinical isolates that had been stocked at our department was employed to determine the minimum inhibitory concentrations (MICs) of SBT/CPZ against various bacterial species. SBT/CPZ showed strong antibacterial potency against E. coli, Salmonella, Klebsiella and P. mirabilis, and relatively strong potency against S. marcescens, P. aeruginosa and S. aureus. Antibacterial potency of SBT/CPZ was stronger than that of CPZ alone against E. coli, and it also showed strong activity against strains of Salmonella, S. marcescens and S. aureus, moderately or highly resistant to CPZ. SBT/CPZ was administered by intravenous bolus infusion to pediatric patients to determine the serum concentrations of SBT and CPZ. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were as follows; 17.8 micrograms/ml, 40.7 micrograms/ml at 15 minutes and 0.3 microgram/ml at 6 hours, respectively. The half-lives of SBT and CPZ in the serum were 1.05 hours and 1.76 hours, respectively. Similarly, at a dose of 20 mg/kg the mean serum levels of SBT and CPZ were; 31.9 micrograms/ml, 81.0 micrograms/ml at 15 minutes and 0.5 microgram/ml, 6.1 micrograms/ml at 6 hours, and the half-lives were 1.00 hour and 1.72 hours, respectively. At a dose of 40 mg/kg, only 1 case was determined. The serum levels of SBT and CPZ were 34.4 micrograms/ml, 74.8 micrograms/ml at 30 minutes and 0.2 microgram/ml at 6 hours, and the half-lives were 0.78 hour and 1.38 hours, respectively. SBT/CPZ was drip-infused intravenously over a period of 1 hour, and the serum concentrations of SBT and CPZ were determined. At the dose of 10 mg/kg or 20 mg/kg, the peak serum levels of SBT and CPZ were observed at 1 hour or at the end of drip infusion. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were 14.4 micrograms/ml, 33.7 micrograms/ml at 1 hour and 1.4 micrograms/ml, 4.6 micrograms/ml at 7 hours, respectively. The half-lives was 1.86 hours for SBT and 2.23 hours for CPZ, respectively. Similarly at a dose of 20 mg/kg, the mean serum levels of SBT and CPZ were, 22.2 micrograms/ml, 34.6 micrograms/ml at 1 hour and 0.5 microgram/ml, 2.8 micrograms/ml at 7 hours, and the half-lives was 1.17 hours and 1.75 hours, respectively. The urinary recovery rate was determined for the 6 hours period after administration.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗
PubMed1992

[Long-term medication with acetylsalicylic acid--a problem in regional anesthesia?].

In patients medicated with acetylsalicylic acid (ASA) and undergoing regional anaesthesia there is a risk of traumatically induced haematoma, particularly near the spinal cord. The increased bleeding tendency following aspirin administration is due to a change in thrombocyte aggregation caused by irreversible inhibition of prostaglandin synthesis. In order to assess the bleeding risk, it was investigated whether and how much subaqueous bleeding time (SBT) and aggregation inhibition (AGI) change under low-dose medication, and when these values return to normal after the end of administration. RESULTS. 1. SBT increased significantly with daily ASA medication of 100 mg or of 300 mg. However, only 4.5% of the values measured were within a pathologic range. After discontinuation of the medication SBT significantly dropped on the 2nd day, reaching the initial level on the 4th day at the latest. 2. AGI was significantly reduced, to 20% of the normal value. Depending on the dosage, the 100-mg group reached full aggregation capacity on the 4th day and the 300-mg group on the 7th day following discontinuation of medication. 3. AGI returned to normal 2-3 days later than SBT. CONCLUSIONS. 1. In the case of pathologically increased values (greater than 6 min), the determination of SBT may indicate an increased bleeding risk. 2. If SBT is within the normal range during or shortly after ASA administration, thrombocytic function is still disturbed. Whether there is a correlation between inhibition of thrombocyte aggregation and the occurrence of spinal haematomas is not yet known. 3. In view of these results, the effect of ASA should be investigated by determining SBT prior to scheduled regional anaesthetic procedures near the spinal cord. 4. If SBT is increased (greater than 6 min) and regional anaesthesia near the spinal cord is indicated, the procedure involving the slightest trauma (spinal anaesthesia) should be chosen [31]. Careful postoperative follow-up (1-2 days) should be guaranteed with regard to neurological disorders.

Adult↗
PubMed1989

[Effects of sulbactam on the activity of cefoperazone against various clinical isolates].

Sulbactam/Cefoperazone (SBT/CPZ) have been used in clinical infusion at ratios of 1:1 and 1:2 in Japan and U.S.A., respectively. After an administration of these drugs as a 1:1 parenteral formulation, the ratio of levels of CPZ and SBT in blood was 1:1/4 to 1:1/5 for 1 to 2 hours, whereas the ratio of free, unbound drug levels was 1:1.4 to 1:1.5. In urine these drugs were excreted at a ratio between 1:1 and 1:4 during 6 hours after the infusion. Antimicrobial interaction studies using various combinations of CPZ and SBT were performed to obtain information with respect to the effect of SBT on the antimicrobial activity of CPZ in vivo and the most appropriate ratio of these drugs for the in vitro test system. Antimicrobial activities were determined using the agar dilution method and the disk diffusion susceptibility test. SBT increased the activity of CPZ against various clinical isolates tested except Enterococcus faecalis. CPZ-SBT at a fixed ratio of 1:1/5 significantly increased the antimicrobial activity of CPZ, resulting in decreases in MIC values and increases in disk inhibitory zone diameters. These drugs at ratios 1:1 to 1:3 maximized the synergistic enhancement of the activity. Therefore, a fixed ratio between 1:1/5 and 1:1 would be appropriate for the in vitro antimicrobial test system using either the agar dilution method or the disk susceptibility test. Based on pharmacokinetic data for CPZ and SBT, results of the present study on antimicrobial activity would support that the parenteral formulation of CPZ-SBT at the fixed ratios of 1:1 and 2:1 for the intravenous infusion used in Japan and U.S.A., respectively, are appropriate. The effect of SBT on the activity of CPZ was more marked against clinical isolates with greater production abilities of beta-lactamase than against those with less production abilities. SBT/CPZ, however, exerted a synergistic effect against methicillin-resistant Staphylococcus aureus without beta-lactamase production. The MIC80 of SBT/CPZ (1:1) against various clinical isolates with 10(6) CFU/ml inoculum size were as follows: S. aureus 12.5 micrograms/ml, Staphylococcus epidermis 3.13 micrograms/ml, and E. faecalis 50 micrograms/ml. Those of Gram-negative bacilli were: Escherichia coli 0.20 microgram/ml, Klebsiella pneumoniae 0.20 micrograms/ml, Proteus mirabilis 0.78 microgram/ml, Proteus vulgaris 0.78 microgram/ml, Pseudomonas aeruginosa 12.5 micrograms/ml, Serratia marcescens 25 micrograms/ml, Enterobacter spp. 3.13 micrograms/ml, Citrobacter spp. 12.5 micrograms/ml and Acinetobacter spp. 0.78 microgram/ml.

Bacteria↗
PubMed1988

[Pharmacokinetic and clinical studies of sultamicillin granule in the pediatric field].

Sultamicillin (SBTPC) is a combined drug of ampicillin (ABPC) and sulbactam (SBT) which is an inhibitor of beta-lactamase, in a clinical form of tosylate with equivalent molecules in ester linkages. A tablet form of this combined drug has been released since July, 1987 in Japan and now a granular form for pediatric patients has been developed. Hence, the granular form of SBTPC was administered to 6 boys (age: 8 years 5 months-11 years 5 months) to determine plasma and urinary concentrations of the drug and its urinary recovery-rates. The dose of 10 mg/kg or 15 mg/kg was given orally just after meal to 3 boys. To study clinical and bacteriological effects of this drug, a mean daily dose of 27.1 mg/kg divided 2-4 times a day was administered for 9 days on the average to a total of 57 cases with pharyngitis (5), tonsillitis (5), laryngitis (1), bronchitis (1), pneumonia (8), scarlet fever (1), typhoid fever (1), impetigo (16), furuncle (2), abscess (6), lymphadenitis (1) and urinary tract infection (10) except 2 cases which were unevaluable for clinical effects. MICs of 7 drugs (SBTPC, ABPC, SBT, methicillin (DMPPC), cloxacillin (MCIPC), cephalexin and cefaclor) against 12 of 22 strains isolated from patients with infections of skin and soft tissue were determined with inoculum-sizes of 10(8) and 10(8) CFU/ml to study beta-lactamase producing activities. Adverse reactions and abnormal effects on laboratory test values attributable to this drug were studied in patients including dropped-out cases. The results obtained are summarized as follows. 1. Mean plasma peak levels of ABPC and SBT were observed at 1 hour after administration in both of the 10 mg/kg and the 15 mg/kg groups with values of 2.34 and 5.57 micrograms/ml for ABPC and 1.87 and 4.66 micrograms/ml for SBT, respectively. Mean concentrations of SBT were lower than those of ABPC in both groups and individuals. Dose-responses in plasma levels and AUCs were observed in both groups. Mean half-life values of ABPC and SBT in the 2 groups were 1.93 and 1.12 hours for ABPC and 1.97 and 1.22 for SBT, respectively. Mean half-life values for ABPC and SBT were similar in each group and this tendency was also seen among individuals.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

[Basic and clinical evaluation of sulbactam/cefoperazone in the field of pediatrics].

Sulbactam (SBT) in a novel beta-lactamase inhibitor from Pfizer and combined with cefoperazone (CPZ) ina 1:1 ratio (SBT/CPZ). Fundamental and clinical studies on SBT/CPZ were executed. The antibacterial activity of SBT/CPZ was compared with those of SBT, CPZ and CEZ against clinical isolates of S. aureus and E. coli which were not susceptible to CEZ. SBT alone did not show any activity against S. aureus, MICs against all strains were over than 100 micrograms/ml on the inoculations of undiluted and 100-fold diluted specimen. CPZ showed MICs over than 100 micrograms/ml against approximately 70% of the isolates on the undiluted inoculation, and on the 100-fold diluted inoculation, the MIC50 and MIC70 were 12.5 micrograms/ml and 100 micrograms/ml, respectively. SBT/CPZ showed better activity than CPZ by 2-8 folds against the strains highly resistant to CPZ; the MIC50 on the undiluted inoculation was 50 micrograms/ml. Against E. coli, the characteristic of SBT/CPZ was shown more clearly. The MICs of CPZ were over than 100 micrograms/ml against approximately 70% of the isolates on the undiluted inoculation, but SBT/CPZ showed MIC50 at 25 micrograms/ml. On the 100-fold diluted inoculation, SBT/CPZ was 4 approximately 8-fold superior than CPZ against strains on which MICs of CPZ were over than 12.5 micrograms/ml. Serum levels were determined by a bolus intravenous injection and by intravenous drip infusion of 10, 20, 40 mg/kg of SBT/CPZ. When administered by a bolus injection, the peak level was seen at 30 minutes in most patients: 8.7, 14.7 or 27.0 micrograms/ml of SBT and 30.1, 42.5 or 76.4 micrograms/ml of CPZ were detected with the 3 different doses. These levels were dose-dependent, and decreased slowly to 0.3, 0.3 or 0.3 micrograms/ml of SBT and 2.9, 2.8 or 3.3 micrograms/ml of CPZ at 6 hours after administration. Half-lives were 1.39, 1.20 or 0.98 hour for SBT and 1.77, 1.59 or 1.42 hours for CPZ. The same 3 doses were given by intravenous drip infusion. The peak levels obtained at the end of infusion (1 hour after initiation of infusion) were 15.3, 14.4 or 43.2 micrograms/ml for SBT and 33.4, 38.2 or 104.2 micrograms/ml for CPZ, respectively. The levels were somewhat low in 20 mg/kg group. After the end of infusion, these levels decreased fairly rapidly, and after 6 hours almost the same levels of 0.4, 0.5 or 0.3 micrograms/ml for SBT and 1.4, 3.9 or 3.3 micrograms/ml for CPZ were detected.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗
PubMed1990

[Synergy between sulbactam and ampicillin or cefoperazone in antimicrobial activity against beta-lactamase producing microorganisms. Results with the use of microdilution broth method].

Antimicrobial activities of sulbactam (SBT) with ampicillin (ABPC) or with cefoperazone (CPZ), in other words, the effects of SBT, an beta-lactamase inhibitor, against beta-lactamase producing strains of clinical isolates, were studied using microdilution broth method. 1. beta-Lactamase producing strains such as Staphylococcus aureus, Branhamella catarrhalis, Haemophilus influenzae, Escherichia coli and Klebsiella pneumoniae decompose benzylpenicillin (PCG) which is one of substrates of the acid-metry disc method and show a strong reaction, while they do not decompose cefazolin (CEZ), another substrate, showing no or weak reaction. Thus, it is suspected that beta-lactamases produced by these organisms are mainly penicillinase (PCase). MIC-distributions of ABPC and CPZ against these clinical isolates which seemed to produce PCase shifted to lower MIC ranges with MIC's reduced to 1/4 or below when 0.025 to 0.39 microgram/ml of SBT was added. 2. It appears that beta-lactamase produced by Proteus vulgaris may be oxyiminocephalosporinase (CXase), because P. vulgaris showed strong reaction on CEZ, but moderate reaction on PCG in the acid-metry disc method. MIC-distribution of ABPC and CPZ against P. vulgaris shifted to a lower range with MIC's of 1/4 or below when 0.20 to 0.39 microgram/ml of SBT was added. 3. All the test strains of Pseudomonas aeruginosa showed strong reaction on CEZ but only 56% of the test strains showed reaction on PCG. It appears that the beta-lactamases which showed strong reaction on CEZ is cephalosporinase and is encoded in chromosome, while those beta-lactamase that showed strong reaction on PCG is encoded in a plasmid which was acquired secondarily by P. aeruginosa. MIC-distribution of CPZ against P. aeruginosa shifted to a lower range with MIC values of 1/2 or below with the addition of SBT at 1.56 micrograms/ml. 4. It appears that the synergy of SBT with ABPC or with CPZ against the PCase or CXase producing strains may occur in the presence of SBT at a concentration far less than that reported previously.

Ampicillin↗
PubMed1989

[Cerebrospinal fluid levels of sulbactam/ampicillin in rabbits with staphylococcal meningitis].

Concentrations of sulbactam (SBT) and ampicillin (ABPC) in the blood and cerebrospinal fluid (CSF) following an intravenous administration of SBT/ABPC at a dose of 150 mg/kg (SBT/ABPC = 1:2) were determined in 12 rabbits with staphylococcal meningitis. Drug concentrations were measured 9 times, 6 times each with intervals of 15 minutes and thereafter with intervals of 30 minutes. The results were compared with those of a group of 9 rabbits given 100 mg/kg of ABPC alone. 1. The maximum concentration of SBT in the CSF and the percentages of both the maximum concentration and the area under the concentration-time curve (AUC) of SBT in CSF vs. those in serum of the SBT/ABPC group were higher than those of ABPC and the half-life of SBT in the CSF was also longer than that of ABPC, all with significant difference. When these parameters for SBT of SBT/ABPC groups were compared with those of ABPC of the ABPC group, not much differences existed between the 2 groups except that the CSF half-life of SBT was much longer than that of ABPC. 2. The percentages of both the maximum concentration and AUC of ABPC in CSF vs. those in serum of the SBT/ABPC group were significantly lower than those of ABPC of the ABPC group. The CSF half-life of ABPC of the former group was longer than that of the latter. 3. The above results suggest that when SBT and ABPC are administered simultaneously, the penetration of ABPC into the CSF is inhibited.

Ampicillin↗
PubMed1987

A radiographic comparison of prehospital cervical immobilization methods.

Three methods of prehospital cervical immobilization were studied radiographically and compared to the short board technique (SBT). The methods were California Stif-Neck Immobilizing Collar (CSC), Kendrick Extrication Device (KED), and Extrication Plus-One (XP-One). Forty-five volunteers were immobilized in the short board (SB) and one of the test devices studied. Cervical movement in the sagittal and frontal planes was measured radiographically. Movement in the horizontal plane was measured directly. Two-tailed, paired t test analysis was performed comparing test devices to the SBT. The SBT proved to be significantly better (P less than .05) in the following comparisons: the CSC in extension and lateral bending; the KED in lateral bending; and the XP-One in extension. We confirm the SBT as the standard of comparison against which newer prehospital devices can be compared objectively. Of the three devices compared against the SBT, the factory-fabricated short board devices (KED and XP-One) provided the greatest degree of immobilization, in addition to logistical advantages over the SBT.

Adolescent↗
PubMed1989

A practical radiographic comparison of short board technique and Kendrick Extrication Device.

Cervical spine immobilization is necessary during the prehospital care of most trauma patients. Earlier studies performed in controlled, indoor settings suggested short board technique (SBT) was the standard against which other methods of cervical stabilization should be measured. Our study approximated the prehospital setting by comparing the use of tape, SBT, and Philadelphia collar (PC) with tape, the Kendrick Extrication Device (KED), and PC after immobilization in and extrication from a compact car. Seven men were immobilized with KED and SBT in addition to PCs and tape. These subjects were extricated and then taken by ambulance stretcher across a 50-yd length of concrete to the radiology suite. Flexion, extension, lateral bending, and rotation were measured. KED-PC (16 degrees +/- 8 degrees) was statistically superior to SBT-PC (41 degrees +/- 5 degrees) in limiting rotation (P less than .001). KED-PC and SBT-PC were similar in their abilities to limit extension (8 degrees +/- 4 degrees vs 6 degrees +/- 5 degrees), flexion (4 degrees +/- 2 degrees vs 4 degrees +/- 4 degrees), and lateral bending (13 degrees +/- 5 degrees vs 17 degrees +/- 6 degrees). In an approximation of the prehospital setting, tape, a PC, and either KED or SBT substantially limit extension, flexion, and lateral bending of the normal cervical spine. KED-PC is more beneficial in rotation.

Adolescent↗
PubMedDate not supplied

The serum bactericidal test.

The serum bactericidal test (SBT) has been used for almost 40 years to monitor therapy in patients with bacterial endocarditis, osteomyelitis, and other serious infections. The SBT is basically a variation of the broth dilution test adapted to assess the activity of a treated patient's own serum against the infecting microorganism. Only recently, however, have rigorous attempts been made to standardize all the relevant variables that affect results of the SBT. The widely recommended goal of a peak bactericidal titer of 1:8 in the therapy for infective endocarditis may be inadequate for the treatment of some patients. Peak titers of 1:64 or greater in the microdilution SBT should be sought if they can be achieved without toxicity. Titers of less than 1:8 may be acceptable, although they are less often successful, if serious toxicity would result from increased dosage. Peak SBT titers of 1:8 or greater yield high cure rates for acute osteomyelitis in children; data are limited in adults. A defined SBT method is necessary for additional multicenter clinical trials on which firmer recommendations for its future use can be made.

Anti-Bacterial Agents↗
PubMed1988

[Transfer of injected sulbactam/cefoperazone into burn blister fluid].

Transfer of sulbactam/cefoperazone (SBT/CPZ) into the burn blister fluid was studied in 10 burn patients after one shot intravenous injection of 50 mg/kg SBT/CPZ (CPZ 25 mg/kg, SBT 25 mg/kg). CPZ and SBT concentrations in serum and burn blister fluid were determined using bioassay and high performance liquid chromatography (HPLC). The concentration of CPZ in serum reached 109.5 +/- 9.2 micrograms/ml (mean +/- S.E.) at 0.25 hour after injection, and decreased to 6.8 +/- 2.3 micrograms/ml after 8 hours. The concentration of CPZ in burn blister fluid peaked at 4 hours and reached 28.2 +/- 8.0 micrograms/ml. The concentration of SBT in serum reached 75.7 +/- 8.3 micrograms/ml at 0.25 hour after injection, and decreased to 2.3 +/- 0.7 micrograms/ml after 8 hours. The peak concentration of SBT in burn blister fluid was 13.5 +/- 1.8 micrograms/ml at 3 hours. The data obtained were analysed pharmacokinetically. Cmax of CPZ and SBT levels in burn blister fluid were calculated to be 30.4 micrograms/ml and 13.6 micrograms/ml, respectively. The AUC0-8 hrs. (area under the burn blister fluid concentration of drug-time curve between 0 and 8 hours after injection), absorption rate constant (ka) and therapeutic AUC (AUC where drug concentrations were above minimum effective concentration) of CPZ were calculated to be 194.0 micrograms.hr/ml, 1.52 hr-1 and 97.1 micrograms.hr/ml (0.3-11.1 hours), respectively. The AUC0-8 hrs. and ka of SBT were also calculated as 68.3 micrograms.hr/ml and 0.62 hr-1, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Blister↗
PubMed1988

[Clinical and pharmacokinetic studies on sultamicillin fine granules in pediatrics].

Sultamicillin (SBTPC) is a mutual prodrug of sulbactam (SBT) and ampicillin (ABPC). A study has been performed to evaluate pharmacokinetic properties and clinical usefulness of SBTPC fine granules in the treatment of pediatric infections. After an oral dose of 5-15 mg/kg of SBTPC fine granules, peak serum concentrations of ABPC and SBT were 1.18-3.26 micrograms/ml and 0.97-3.05 micrograms/ml, respectively at 1 hour. Serum half-lives for elimination (T 1/2 (beta] of ABPC and SBT were 0.83-1.83 hours and 0.94-1.71 hours, respectively. Serum concentrations of ABPC at 1-6 hours after an oral administration of SBTPC fine granules were similar to those of SBT. Serum concentrations of ABPC and SBT were proportional to dose levels of SBTPC fine granules. Following oral administrations of 5-15 mg/kg, 33.9-64.8% of ABPC and 38.1-76.6% of SBT were recovered in urine in 6 hours. SBTPC fine granules were administered in a daily dose of approximately 30 mg/kg divided into 3 doses to 14 pediatric patients with bacterial infections. All 14 were cured with 11 excellent and 3 good clinical response to this drug. Microbiological eradication was obtained in 85.7%. beta-Lactamase-producing ABPC-resistant strains were eradicated. Adverse effects including laboratory test values that may be attributed to the administration of SBTPC fine granules were not observed except a treatment episode of diarrhea in 1 patient.

Adolescent↗