Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Sulbactam”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 235 records · Page 13Linked to original sources
PubMedDate not supplied

[Sulbactam-ampicillin monotherapy in the ambulatory treatment of pneumonia. Results of mono-administration].

Since ampicillin, the parent drug of aminopenicillins, is hydrolyzed by penicillinase, it is normally used in association with sulbactam, a sodium penicillinate sulfone with potent inhibiting activity on type II, III, IV, and V beta-lactamases. The combination ampicillin-sulbactam has been found remarkably useful for the treatment of severe community pneumonia caused by bacteria resistant to ampicillin alone. Approximately 300 patients with community pneumonia of various degrees of severity have been treated with a single dose of 3-4 g ampicillin-sulbactam either diluted in normal saline or in dextrose solution, usually associated with methylprednisolone 20 mg or betametasone 8 mg (tapered). As assessed by clinical and radiological findings, recovery has been obtained all cases.

Ambulatory Care↗
PubMed1998

Microbiological assay of ampicillin in serum and aqueous humor of patients given ampicillin-sulbactam injection.

The aim of this study was to determine the bacterial growth inhibitory activities of ampicillin in aqueous humor and serum of patients administered ampicillin-sulbactam combination intramuscularly prior to cataract surgery. 43 patients received a combination of both antibiotics intramuscularly at varying periods (60-140 minutes) prior to surgery. Aqueous humor and venous blood were collected at the beginning of the surgery. For microbiological assay, spores of Bacillus subtilis were incorporated in the agar. The test sample and the standard solutions (calibrators) of ampicillin and ampicillin-sulbactam combination were placed in 3 mm wells in the agar. The diameter zones of growth inhibitory activities of ampicillin of the calibrators and the test samples measured in mm were extrapolated to the standard curve and were recorded as ampicillin activity in micrograms/ml. The results of the assay were placed in 5 groups according to the time intervals between injection and collection of serum and aqueous humor (< or = 70, 75, 80, 90, > 90 minutes). Ampicillin activities in sera and aqueous humor of group 5 (> 90 minutes) were significantly higher than the others (p < 0.001). The ratio of ampicillin activities of sera and aqueous humor in group 5 patients was significantly lower indicating higher concentration of ampicillin activity in aqueous humor during this period. Bacterial growth inhibitory activities of ampicillin-sulbactam combination were adequate in aqueous humor of all patients with highest activity being 90 minutes after intramuscular administration indicating the potential usefulness of this antibiotic combination as chemoprophylaxis prior to cataract surgery.

Adult↗
PubMed2006

Triple, standard quadruple and ampicillin-sulbactam-based quadruple therapies for H. pylori eradication: a comparative three-armed randomized clinical trial.

AIM: To compare the effectiveness of triple, standard quadruple and ampicillin-sulbactam-based quadruple therapies for H. pylori eradication in a comparative three-armed randomized clinical trial. METHODS: A total of 360 H. pylori-positive patients suffering from dyspepsia and aging 24-79 years with a median age of 42 years were enrolled in the study and randomly allocated into the following three groups: group A (n = 120) received a standard 1-wk triple therapy (20 mg omeprazole b.i.d., 1000 mg amoxicillin b.i.d., 500 mg clarithromycin b.i.d.); group B (n = 120) received a 10-d standard quadruple therapy (20 mg omeprazole b.i.d., 1000 mg amoxicillin b.i.d., 240 mg colloidal bismuth subcitrate b.i.d., and 500 mg metronidazole b.i.d.); group C (n = 120) received the new protocol, i.e. 375 mg sultamicillin (225 mg ampicillin plus 150 mg sulbactam) b.i.d. (before breakfast and dinner), instead of amoxicillin in the standard quadruple therapy for the same duration. Chi-square test with the consideration of P<0.05 as significant was used to compare the eradication rates by intention-to-treat and per-protocol analyses in the three groups. RESULTS: The per-protocol eradication rate was 91.81% (101 patients from a total of 110) in group A, 85.84% (97 patients from a total of 113) in group B, and 92.85% (104 patients from a total of 112) in group C. The intention-to-treat eradication rate was 84.17% in group A, 80.83% in group B, and 86.67% in group C. The new protocol yielded the highest eradication rates by both per-protocol and intention-to-treat analyses followed by the standard triple and quadruple regimens, respectively. However, the differences were not statistically significant between the three groups. CONCLUSION: The results of this study provide further support for the equivalence of triple and quadruple therapies in terms of effectiveness, compliance and side-effect profile when administered as first-line treatment for H. pylori infection. Moreover, the new protocol using ampicillin-sulbactam instead of amoxicillin in the quadruple regimen is a suitable first-line alternative to be used in regions with amoxicillin-resistant H. pylori strains.

Adult↗
PubMedDate not supplied

Ampicillin and ampicillin-sulbactam dilution tests with mixed cultures of Bacteroides fragilis, Escherichia coli and Enterococcus.

Bacterial interactions in mixed infections may compromise antimicrobial therapy. The in vitro bactericidal activity of ampicillin and ampicillin-sulbactam against aerobic/anaerobic mixed cultures of Bacteroides fragilis, Escherichia coli and Enterococcus spp. was studied by means of broth dilution tests. The MBC of ampicillin for Enterococcus faecalis 6 was 0.25 mg/l when tested singly; in association with B. fragilis 1, however, the MBC for E. faecalis 6 was 16 mg/l. When tested singly E. coli 9 and B. fragilis 1 were both killed by ampicillin at a concentration of 4 mg/l in combination with 1 mg/l sulbactam. When both strains were associated, the MBC for B. fragilis 1 rose to > 256 mg/l. Results obtained indicate that the behaviour of bacteria as determined in pure cultures is not necessarily identical with the antibiotic susceptibility present in mixed cultures. It was shown that, besides beta-lactamase production by involved bacteria, other factors contribute to the alteration of bacterial susceptibility in mixed cultures. Synergistic and antagonistic effects between associated organisms were observed. For example, it was found that two moderately sensitive bacterial strains were resistant in mixed culture.

Ampicillin↗
PubMedDate not supplied

Pharmacokinetics of ampicillin, sulbactam and cefotiam in patients undergoing orthopedic surgery.

As perioperative prophylaxis for major orthopedic operations 81 patients were given the fixed combination of ampicillin (1 g)/sulbactam (0.5 g) or cefotiam (2 g) as short infusions. The three beta-lactams were rapidly distributed into the different tissues and their pharmacokinetic profiles were found to be very similar. It was noteworthy that ampicillin, sulbactam and cefotiam penetrated within minutes, not only into skin, fat and muscles, but also into bone. Thus 0.25 h after starting the infusion the following mean concentrations were measured in bone: 21.8 +/- 10.5 mg/kg ampicillin, 4.9 +/- 2.2 mg/kg sulbactam and 19.4 +/- 10.6 mg/kg cefotiam. For a period of at least 2 h the concentrations measured in serum and in the different tissues affected by the operation (skin, fat, muscle, bone) were above the MICs for pathogens which are involved in postoperative wound infections. On the basis of pharmacokinetic data, ampicillin/sulbactam and cefotiam seem about equally suitable for perioperative prophylaxis in major orthopedic operations.

Adult↗
PubMed1992

Error rates in cefoperazone and cefoperazone-sulbactam disk tests with Enterobacteriaceae and Pseudomonas aeruginosa.

In a collaborative study involving five medical centers, 6% of 2,440 consecutive isolates of Enterobacteriaceae were resistant to cefoperazone; resistance to cefoperazone was reduced to < 1% by the addition of sulbactam. Susceptibility to cefoperazone and cefoperazone-sulbactam was accurately predicted by disk diffusion tests. Resistance to cefoperazone, however, was not as reliably detected by disk tests and results of dilution tests were not always consistent. The prevalence of resistance to cefoperazone and/or the ability to detect resistance had a significant influence on very major error rates for individual laboratories.

Agar↗
PubMed1989

In vitro activity of cefoperazone-sulbactam combinations against cefoperazone-resistant clinical bacterial isolates.

From July 1987 to January 1988, 452 cefoperazone-resistant bacterial isolates were identified among strains subjected to routine susceptibility testing in a clinical microbiology laboratory. The 452 isolates were tested for susceptibility to cefoperazone, sulbactam, and a 2:1 combination of these drugs by agar dilution techniques. The greatest benefit of the cefoperazone-sulbactam combination was noted against Bacteroides spp. and Acinetobacter spp. The combination demonstrated clinically significant synergism against approximately 20% of strains of Pseudomonas aeruginosa.

Acinetobacter↗
PubMed1995

Rapid determination of sulbactam and tazobactam in human serum by high-performance liquid chromatography.

A simple and rapid HPLC method for the determination of tazobactam and sulbactam, two beta-lactamase inhibitors, in serum for the therapeutic follow-up of patients is described. The effect of the pH of the aqueous mobile phase and column temperature on column efficiency and retention were examined and equations for their dependences were derived. The use of a chromatographic response function showed that methanol-buffer (5:95, v/v) (pH 6.3) as the mobile phase and a 45 degrees C column temperature were optimum values for chromatographic separation. The analytical method was linear from 10 to 200 micrograms/ml. This assay limit range is sufficient for the analysis of human serum. The limit of detection was 10 micrograms/ml for sulbactam and 5 micrograms/ml for tazobactam. The coefficient of variation was less than 5%. The speed at which this assay can be performed makes it especially useful for estimating the levels of these drugs in human serum.

Chromatography, High Pressure Liquid↗
PubMedDate not supplied

Mechanism of beta-lactamase inhibition: differences between sulbactam and other inhibitors.

Three different types of beta-lactamases--TEM-2 type penicillinase, a typical cephalosporinase of Citrobacter freundii, and a Proteus vulgaris cephalosporinase with broad substrate range--were studied to determine the inactivation and reactivation kinetics for beta-lactamase inhibitors of these enzymes. Sulbactam, cloxacillin sulfone, clavulanic acid, imipenem, and aztreonam were evaluated. On the basis of the kinetic parameters a minimum scheme for the inactivation of these beta-lactamases by each compound was proposed, and the difference in the features of each of these as progressive and competitive inhibitors were evaluated. The relationship between the kinetic parameters and the synergistic effects of the inhibitors in combination with traditional beta-lactam antibiotics on the bacterial strains producing these beta-lactamases was examined. A close relationship between the synergistic effect, expressed as the FIC index, and a proposed parameter, TN x Ki/Km, was demonstrated. The results of this analysis suggest that sulbactam is a beta-lactamase inhibitor applicable to a wide range of beta-lactamase types.

Anti-Bacterial Agents↗
PubMedDate not supplied

Broth-disk elution tests to predict the susceptibility of anaerobic bacteria to the ampicillin-sulbactam combination.

The ampicillin-sulbactam Wilkins-Chalgren agar dilution MICs (2 ratios) were compared with the results of broth-disk elution (BDE) tests using various numbers of disks corresponding to elution breakpoints of less than or equal to 8:8 micrograms/ml, less than or equal to 16:8 micrograms/ml, and less than or equal to 16:16 micrograms/ml. This study showed that a 2:1 ratio MIC test and a 16:8 micrograms/ml BDE breakpoint were best for anaerobic organisms; a recommendation consistent with susceptibility testing criteria for rapidly growing aerobic species. The addition of four ampicillin disks (10 micrograms) and four ampicillin-sulbactam discs (10:10 micrograms) to 5 ml of thioglycolate broth was recommended. This test would achieve greater than 99% comparative accuracy to MICs determined with the reference National Committee for Clinical Laboratory Standards agar dilution method.

Ampicillin↗
PubMed2004

In vitro activities of beta-lactam antibiotics alone and in combination with sulbactam against Gram-negative bacteria.

The resistance rates of ampicillin/sulbactam 2:1 against imipenem-susceptible and -resistant Acinetobacter baumannii were 23.5 and 30%, respectively. Ceftazidime/sulbactam combination showed significant reduction of resistant rates against Enterobacter cloacae, A. baumannii, ESBL Klebsiella pneumoniae. MIC90 of cefoperazone against E. cloacae, Serratia marcescens, A. baumannii and ESBL K. pneumoniae were > 128 mg/l. Addition of sulbactam enhanced the antimicrobial activities significantly. When imipenem was combined with sulbactam, the resistant rates against imipenem-resistant A. baumanni were significantly reduced. Cefepime/sulbactam combination was active against imipenem-resistant A. baumanni. The resistance rates of aztreonam/sulbactam combination against E. cloacae, imipenem-sensitive and resistant A. baumannii, ESBL K. pneumoniae were lowered significantly. The cefotaxime/sulbactam combination showed a significant improvement of activities against E. cloacae, S. marcescens, A. baumannii and ESBL K. pneumoniae.

Acinetobacter baumannii↗
PubMed2004

A liquid chromatographic method for simultaneous determination of amoxicillin sodium and sulbactam sodium in a combination formulation.

An isocratic liquid chromatographic method with UV detection at 210nm is described for simultaneous determination of amoxicillin sodium and sulbactam sodium in a new combination formulation. Chromatographic separation of the two drugs was achieved on a Hypersil C(18) column using a mobile phase consisting of a binary mixture of methanol and 0.01mol/l sodium acetate (5:95, v/v). The commonly used paired-ion aqueous mobile phase for the determination of penicillins was avoided in this study. The developed LC method offers symmetric peak shape, good resolution and reasonable retention time for both drugs. Linearity, accuracy and precision were found to be acceptable over the concentration ranges of 155.3-1553.0microg/ml for amoxicillin sodium and 45.0-450.0microg/ml for sulbactam sodium. The proposed LC method can be used for the quality control of formulated products containing these two drugs.

Amoxicillin↗
PubMed1988

Placental transfer of cefoperazone and sulbactam in the isolated in vitro perfused human placenta.

The transfer of cefoperazone and sulbactam across the human placenta was studied qualitatively and quantitatively with the isolated in vitro bidirectionally perfused human placental lobule. Clearance indexes for both cefoperazone and sulbactam were derived. The absence of active transport and facilitated diffusion were documented, implying simple diffusion as the mechanism of placental transfer for both drugs. Placental tissue levels were also studied.

Biological Transport↗
PubMed1987

Perioperative prophylaxis with sulbactam and ampicillin compared with metronidazole and cefotaxime in the prevention of wound infection in children undergoing appendectomy.

Sulbactam is a beta-lactamase inhibitor, which when administered with ampicillin, increases the latter agents antibacterial activity against beta-lactamase producing organisms. One hundred children between the ages of 5 and 14 undergoing emergency appendectomy were entered into a prospective randomized trial comparing sulbactam and ampicillin (SA) with metronidazole and cefotaxime (MC) as prophylaxis against postoperative wound infection. Patients in whom the appendix was perforated or gangrenous received a 72-hour course of antibiotics, others received a single dose only. The overall wound infection rate was 8% (14% in patients with perforation or gangrene and 4% in those without). There was no difference in infection rate between the two antibiotic groups; there were three wound infections and one subphrenic abscess in patients receiving SA and four wound infections in patients receiving MC. SA, therefore, appears to be a suitable antibiotic combination for use as prophylaxis in appendicitis in children.

Adolescent↗
PubMed1996

In-vitro activity of penicillin G plus sulbactam in comparison with other beta-lactamase inhibitor combinations and oxacillin against staphylococci.

The in-vitro activity of penicillin G in combination with the beta-lactamase inhibitor, sulbactam, against penicillin-sensitive S. aureus (n = 10) and penicillin-resistant, methicillin-sensitive S. aureus (n = 69) and S. epidermidis (n = 20) was tested in comparison with ampicillin/sulbactam, amoxicillin/clavulanic acid, piperacillin/tazobactam and oxacillin. The combination of penicillin G plus sulbactam was found to lead to MIC values for beta-lactamase producing staphylococci comparable to those for penicillin-sensitive staphylococci, with MIC90 values between < or = 0,03 mg/L and 0.06 mg/L.

Humans↗
PubMed2005

High resolution crystal structures of the trans-enamine intermediates formed by sulbactam and clavulanic acid and E166A SHV-1 {beta}-lactamase.

Antibiotic resistance mediated by constantly evolving beta-lactamases is a serious threat to human health. The mechanism of inhibition of these enzymes by therapeutic beta-lactamase inhibitors is probed using a novel approach involving Raman microscopy and x-ray crystallography. We have presented here the high resolution crystal structures of the beta-lactamase inhibitors sulbactam and clavulanic acid bound to the deacylation-deficient E166A variant of SHV-1 beta-lactamase. Our previous Raman measurements have identified the trans-enamine species for both inhibitors and were used to guide the soaking time and concentration to achieve full occupancy of the active sites. The two inhibitor-bound x-ray structures revealed a linear trans-enamine intermediate covalently attached to the active site Ser-70 residue. This intermediate was thought to play a key role in the transient inhibition of class A beta-lactamases. Both the Raman and x-ray data indicated that the clavulanic acid intermediate is decarboxylated. When compared with our previously determined tazobactam-bound inhibitor structure, our new inhibitor-bound structures revealed an increased disorder in the tail region of the inhibitors as well as in the enamine skeleton. The x-ray crystallographic observations correlated with the broadening of the O-C=C-N (enamine) symmetric stretch Raman band near 1595 cm(-1). Band broadening in the sulbactam and clavulanic acid inter-mediates reflected a heterogeneous conformational population that results from variations of torsional angles in the O-(C=O)-C=C=NH-C skeleton. These observations led us to conclude that the conformational stability of the trans-enamine form is critical for their transient inhibitory efficacy.

Anti-Bacterial Agents↗
PubMed1989

Antibacterial activity of the sulbactam-ampicillin combination.

The in vitro antibacterial activity of ampicillin combined with sulbactam 2:1 was evaluated on 257 aerobic Gram-positive and Gram-negative bacteria, and on 174 anaerobic bacteria from isolated hospital strains by evaluating the minimum inhibitory concentration (MIC). The results obtained show a synergic effect which was able to significantly decrease the MIC90 of the tested beta-lactamase producing bacteria. Among the Gram-positive aerobic strains, we underline the efficacy of sulbactam/ampicillin on resistant Staphylococci, including those methicillin-resistant. The activity on the Gram-negative strains was particularly evident against enterobacteria and haemophilus. The combination of sulbactam and ampicillin provides increased activity against anaerobic strains, including Bacteroides fragilis.

Ampicillin↗
PubMed2002

Comparison of ampicillin-sulbactam and imipenem-cilastatin for the treatment of acinetobacter ventilator-associated pneumonia.

Acinetobacter organisms, which are a common cause of ventilator-associated pneumonia (VAP) in some health care centers, are becoming more resistant to such first-line agents as imipenem-cilastatin (Imi-Cil). Sulbactam has good in vitro activity against Acinetobacter organisms; thus, ampicillin-sulbactam (Amp-Sulb) may be a viable treatment alternative. The outcomes for critically ill trauma patients with Acinetobacter VAP treated with either Amp-Sulb or Imi-Cil were compared retrospectively. A total of 77 episodes in 75 patients were studied. Fourteen patients were treated with Amp-Sulb, and 63 patients were treated with Imi-Cil. Treatment efficacy was similar in the Amp-Sulb and Imi-Cil groups (93% vs. 83%, respectively; P>.05). No statistically significant differences between groups were noted with regard to associated mortality, duration of mechanical ventilation, or length of stay in the intensive care unit or hospital. However, adjunctive aminoglycoside therapy was used more often in the Amp-Sulb group. Patients generally received Amp-Sulb because of imipenem resistance. Amp-Sulb was effective in treating a small number of patients with Acinetobacter VAP; however, more data are needed.

Acinetobacter↗