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PubMed1988

Evaluation of in vitro methods for testing susceptibility of anaerobes to ampicillin-sulbactam and amoxicillin-clavulanic acid.

A total of 97 anaerobic bacteria were tested for susceptibility to ampicillin, ampicillin-sulbactam, and amoxicillin-clavulanic acid by broth microdilution and disk elution methods, the results of which were compared with those of the reference agar dilution method. With the broth microdilution method, approximately 95% of MICs were within 1 dilution of those of the reference agar method, with a definite (0.6 to 0.7 dilution) trend toward lower MICs. The disk elution test performed satisfactorily, but additional anaerobic isolates resistant to ampicillin-sulbactam and/or amoxicillin-clavulanic acid (currently rare) are needed to assure the predictability of resistance by the disk elution test.

Amoxicillin↗
PubMedDate not supplied

Piperacillin tazobactam compared with co-amoxiclav, ampicillin plus sulbactam and timentin against beta-lactamase-producing clinical isolates of Escherichia coli, Klebsiella pneumoniae and Klebsiella oxytoca.

A total of 266 enterobacterial isolates (Escherichia coli = 190, Klebsiella pneumoniae = 49, K. oxytoca = 27) were tested for susceptibility (Bauer-Kirby agar disk diffusion test and agar dilution procedure) to ampicillin, ampicillin in 10 micrograms/ml of sulbactam, amoxicillin in 4 micrograms/ml of clavulanic acid, piperacillin, piperacillin plus tazobactam (8:1 ratio), ticarcillin and timentin (ticarcillin in 4 micrograms/ml of clavulanic acid). Discrepant results between the two methods of susceptibility testing were categorized as follows: category I = very major [minimal inhibitory concentration (MIC) = resistant, disk diffusion = susceptible] category II = major (MIC = susceptible, disk diffusion = resistant), category III = minor (MIC = intermediate susceptibility, disk diffusion = susceptible), category IV = slight (MIC = resistant, disk diffusion = intermediate), category V = minimal (MIC = susceptible, disk diffusion = intermediate) and category VI = negligible (MIC = intermediate, disk diffusion = resistant). The antibiotics, or combinations with beta-lactamase inhibitors, yielded the following discrepant results: ampicillin (II = 2, V = 1 and VI = 3), co-amoxiclav (I = 5, III = 25, IV = 1 and V = 3), ampicillin plus sulbactam (I = 5, II = 3, III = 1, V = 19 and VI = 1), piperacillin (II = 15, III = 1, V = 15 and VI = 85), piperacillin plus tazobactam (III = 16, IV = 2, V = 1 and VI = 5) and timentin (I = 2, III = 48 and IV = 1).(ABSTRACT TRUNCATED AT 250 WORDS)

Amoxicillin↗
PubMedDate not supplied

Oral bioavailability of ampicillin and amoxycillin alone and bound in fixed proportions to sulbactam and clavulanic acid.

Oral bioavailability of ampicillin when bound to sulbactam (sultamicillin) compared with ampicillin alone and that of amoxycillin with a ligand of clavulanic acid versus amoxycillin alone were assessed in 16 healthy subjects using an open label, multiple crossover study. After a single administration of the drugs, the bioavailability of ampicillin released from sultamicillin was more than twice (2.17) that of ampicillin administered alone, whereas that of amoxycillin was increased by a factor of 1.64 by the presence of clavulanic acid. Higher peak concentrations and areas under the curves, along with shorter lag times, were observed in both cases. The increased oral bioavailability of these aminopenicillins when associated with a beta-lactamase inhibitor was well demonstrated in this study, the bioavailability of ampicillin being more enhanced by sulbactam than that of amoxycillin by clavulanic acid.

Administration, Oral↗
PubMed2002

Nontraditional dosing of ampicillin-sulbactam for multidrug-resistant Acinetobacter baumannii meningitis.

A 52-year-old man was admitted to a local hospital with headache, nausea, vomiting, dizziness, photophobia, and confusion after a sudden fall. Progressive changes in neurologic function were noted despite neurosurgical intervention and broad-spectrum antimicrobial coverage. Cerebral spinal fluid (CSF) culture identified Acinetobacter baumannii that was resistant to traditionally recommended therapies of amikacin and imipenem-cilastatin. The organism demonstrated minimum inhibitory concentrations of greater than 32 microg/ml and 8 microg/ml, respectively, for these two agents. Ampicillin 2 g-sulbactam 1 g every 3 hours was administered based on history of therapeutic failure of traditional dosing in our thermal injury population. Repeat CSF cultures after 12 days of ampicillin-sulbactam therapy were negative. After 35 days, the patient's A. baumannii infection was completely resolved. The patient experienced no adverse drug events or toxicity with this high-dosage regimen.

Acinetobacter↗
PubMed1986

Alterations in the human oropharyngeal microflora related to therapy with aztreonam, moxalactam and ampicillin plus sulbactam.

33 patients undergoing colorectal surgery were treated prophylactically with aztreonam (19 patients), moxalactam (10 patients) and ampicillin plus sulbactam (4 patients). The effect on the normal oropharyngeal microflora and new colonization of oropharynx were studied during and after the treatment. Aztreonam had minor effect on the normal flora but induced colonization with staphylococci. Moxalactam suppressed gram-negative aerobic and anaerobic bacteria and promoted colonization with Candida albicans. Ampicillin plus sulbactam had marked effect on the normal flora and suppressed aerobic as well as anaerobic bacteria. New colonization with enteric gram-negative rods or fungi was observed in all patients.

Adult↗
PubMedDate not supplied

Sepsis and multiple brain abscesses caused by Salmonella paratyphi B in an infant: successful treatment with sulbactam-ampicillin and surgical drainage.

Abscess formation by Salmonella species is an uncommon but significant manifestation of salmonellosis, because this type of infection has high morbidity and mortality rates and is a potential nosocomial hazard. In infants, history of consumption of contaminated water should be especially quired. We report a case who had sepsis and multiple brain abscesses due to Salmonella paratyphi B and who responded to sulbactam-ampicillin (SAM) therapy. Sulbactam-ampicillin combination may be preferable due to its immunomodulator effect.

Ampicillin↗
PubMed2000

[Simultaneous determination of sulbactam sodium and cefoperazone sodium in sulperazon by high performance liquid chromatography].

A reversed-phase, isocratic high performance liquid chromatographic method with acid mobile phase can separate sulbactam and cafoperazone within 12 minutes. Column packed with Hypersil ODS2(250 mm x 4.6 mm i.d., 5 microns) was manufactured by Dalian Elite Company. Mobile phase is composed of water (adjusted to pH 4.0 with 1% phosphoric acid) and acetonitrile (80:20, V/V). The detection was performed at 210 nm and the injection volume was 2 microL. Cefoperazone and sulbactam have good linearity in the ranges of 100 mg/L to 800 mg/L and 100 mg/L to 1,000 mg/L with the correlation coefficients of 0.9991 and 0.9997 respectively. This method is easily to be operated and can be applied for manufacturing and medicinal study.

Anti-Infective Agents, Urinary↗
PubMed2003

Urine inhibitory titers against resistant Escherichia coli isolates after oral amoxicillin-sulbactam.

UNLABELLED: It has been previously shown that following the oral administration of amoxicillin-sulbactam (AXS) the urinary activity against Escherichia coli (Ec) is due to beta-lactamase inhibition (i.e. TEM-1) as well as to the intrinsic activity of sulbactam (SB). Similarly, it has been previously demonstrated in volunteers that a single oral dose of AXS 500/500 mg allows high urine inhibitory titers (UITs) against resistant Ec isolates. In this in vitro and ex vivo study we assessed the urinary activity of a new AXS proportion: 875/125 mg. Urine was collected from 12 volunteers at 0-2; 2-4; 4-6 h after a single oral dose of AXS 875/125 mg. Previous studies had shown that pooled urine from 12 volunteers did not differ significantly in the UIT as compared to the mean individual values. Urine pools for each period were prepared. Each pool was tested for UIT against 60 Ec isolates received from 10 different laboratories in South American countries: 10 susceptible (S) to AXS; 10 intermediate (I) and 40 resistant (R); the latter ranging 32/16-256/128 mg/l. Amoxicillin (AX) and SB urine concentrations were determined in all the samples. UIT ranged from 1/4 to > 1/32 for S and I strains and from 1/1 to 1/4 for R strains. For one strain (AXS, MIC 256/128 mg/l) the UIT titer was 1/1 at 2 and 4 h but it was not inhibited at 6 h. AX mean levels ranged from 1872 (2 h) to 522 mg/l (6 h) while SB ranged from 1075 (2 h) to 334 (6 h) mg/l. It is noteworthy that 59/60 strains were inhibited by 128 mg/l SB alone. IN CONCLUSION: The AXS 875/125 proportion has a remarkable in vitro and ex vivo activity against Ec urinary isolates.

Administration, Oral↗
PubMed1992

[Sulbactam-ampicillin in surgery. Our experience].

The bacterial infections constitute a serious problem for the surgeon: the choice of antibiotic drugs is really important and, as often as possible, should be guided by antibiotic sensitivity tests. In this study we used sulbactam-ampicillin (Unasyn) who is an antibiotic combination between sulbactam, inhibitor of beta lactam and ampicillin. The preliminary results were as follows: Unasyn was administered to 21 hospitalized selected patients, 16 women and 5 man, who had clinical signs of intraabdominal infection, wound infection and subphrenic abscess after digestive surgery. In these patients were isolated the following organisms: Staphylococcus epidermidis (8), Staphylococcus aureus (11), serratia (1), streptococcus (3), E. coli (3). The daily dosage of Unasyn was 3-12 g/die administered in three to four divided doses, and was determined by the severity of infection, the antibiotic susceptibility of the causative organism(s) and the condition of the patient. Each dose was given by slow i.v. infusion in 15-30 minutes. Our success rate was 100%, and neither systemic nor local side effects were recorded.

Adult↗
PubMed1992

[Study of general toxic and organotropic properties of ampicillin combined with sulbactam].

The effect of sulacillin, a combination of sulbactam and ampicillin (1:2), on the functions of the liver and kidneys, peripheral blood count, cardiovascular and central nervous systems was studied in acute and chronic experiments on animals of various species. The allergenic and local irritating properties of the combination were also studied. It was shown that the combination was low toxic and the interaction of sulbactam and ampicillin by the lethal effect was additive. When the combination was administered intravenously to mice, its LD50 amounted to 6 g/kg. In chronic experiments on rats parenterally given the combination in doses equivalent to the therapeutic ones there were no changes in the examined systems and organs. When used in the doses exceeding the therapeutic ones, sulacillin used during long periods induced a transitory elevation of blood levels of transaminases and alkaline phosphatases, an increase in the relative weight of the liver and kidneys, elongation the typhlon and an increase in glycogen levels in the hepatocytes without morphological changes. The combination had no significant effect of sulacillin and the painful injections alleviated by local anesthesia were recorded. The allergenic properties of the combination were moderate and did not differ from those of ampicillin. The data indicate that the combined sulacillin preparation greatly resembles its foreign analogue.

Ampicillin↗
PubMed2004

[Comparison of efficacy between ceftriaxone and cefoperazone plus sulbactam in peri-operative treatment of acute suppurative cholangitis].

OBJECTIVE: To compare the efficacy of ceftriaxone and that of cefoperazone plus sulbactam (sulperazon) in controlling infection, in scavenging bacteria from bile, and in their costs when treating acute suppurative cholangitis with choledochostomy. METHODS: Patients were randomly assigned to two groups: the ceftriaxone group (R-group, n=95) and sulperazon group (S-group, n=95). Before choledochostomy, both groups received one intravenous dose of the corresponding antibiotics: and 2 g ceftriaxnoe for the R-group, 2 g sulperazon, containing 1 g cefoperazone and 1 g sulbactam, for the S-group. After the operation, the patients in the R-group received ceftriaxone 2 g i.v. q.d.; the patients in the S-group received sulperazon 2 g i.v. b.i.d.. In addition, all patients in both groups received metronidazole 0.5 g daily before and after the operation. The efficacy was evaluated by efficiency in controlling infection and the persisting days of symptoms due to infection, fever and leukocytosis; the persisting days was compared using the life table method to calculate the "cumulative probability of persistence of symptoms (CPPS)". The two groups were also compared in regards to their biliary bacterial clearance rates and the costs directly attributable to the antibiotics. RESULTS: The efficiency in controlling infection was 98.9% (94/95) in both groups. However, the CPPS of the R-group decreased more rapidly than that of the S-group, Log-Rankchi2=6.7901, P=0.0092. Biliary bacterial clearance rate on post-operative day 3 was 72.0% (36/50) for the R-group, 41.3% (19/46) for the S-group, P=0.0037. Cost directly attributable to the antibiotics were (1788.29 +/- 518.46) yuan (RMB) for the R-group, and (3768.74 +/- 820.55) yuan for the S-group, F=395.51, P=0.0000. CONCLUSION: Both ceftriaxone and sulperazon are effective in treating acute suppurative cholangitis when used before and after choledochostomy. Ceftriaxone is superior in expediting symptom relief and bacterial clearance from bile, and is more cost-effective.

Acute Disease↗
PubMed1990

Comparative efficacy of cefoperazone, cefoperazone plus sulbactam, ciprofloxacin, clindamycin, metronidazole, and penicillin G against anaerobic bacteria in an animal model.

Treatment efficacy of various antimicrobial regimens against anaerobes was studied in semipermeable chambers simulating a closed-space, locally neutropenic infection site in rabbits. Bacteroides fragilis, Bacteroides melaninogenicus, Clostridium perfringens, and Peptostreptococcus anaerobius were inoculated (at a mean of 5.3 log10 CFU/ml in prereduced pooled rabbit serum) into the chambers (one isolate per chamber) in triplicate. Antimicrobial therapy consisted of cefoperazone, cefoperazone plus sulbactam, ciprofloxacin, clindamycin, metronidazole (against the gram-negative anaerobes), or penicillin G (against the gram-positive anaerobes), beginning 4 hours after organism inoculation and continuing every 6 hours for 16 doses. With the use of anaerobic techniques for specimen acquisition, transport, and culture, quantitative bacterial findings were measured at the start of therapy and at various time points thereafter. Antibiotic concentrations were measured in blood and chamber fluid by liquid chromatography or bioassay methods. At the end of the study in vivo organisms were reduced by at least 3 log10 CFU/ml from drug-free growth control chambers by all the antimicrobial regimens tested except for cefoperazone against B. fragilis and ciprofloxacin against the three isolates tested. The addition of sulbactam to cefoperazone inhibited B. fragilis beta-lactamase activity and eradicated B. fragilis in vivo. In vivo results with this model confirmed in vitro susceptibilities of all tested antimicrobials except ciprofloxacin and should provide useful indications of the potential clinical efficacy of other new agents against anaerobes.

Animals↗
PubMed1990

Sulbactam-induced hyperpyrexia.

We describe a patient who experienced hyperpyrexia after the administration of ampicillin sodium-sulbactam sodium. This previously unreported complication did not occur with administration of ampicillin alone and could not be attributed to other medications, to diluents, or to an allergic reaction. Because of the evidence in this case, we believe that the sulbactam component of this antibiotic combination should be considered in the pathogenesis of drug-induced hyperpyrexia.

Adult↗
PubMed1990

Increase in the activity of third-generation cephalosporins in combination with clavulanic acid and Sulbactam against Bacteroides fragilis.

We studied the sensitivity of 160 strains of Bacteroides fragilis (74 beta-lactamase-positive and 86 beta-lactamase-negative) to four third-generation cephalosporins, alone as well as in combination with clavulanic acid and Sulbactam. For susceptibility testing we used a dilution method in agar. Detection of beta-lactamase production by this micro-organism was performed using chromogenic cephalosporin (Nitrocefin). There was a substantial improvement in cephalosporin activity with both positive and negative strains when they were combined with the inhibitors, although this was more significant in beta-lactamase-producing organisms. Generally, the results achieved in combination with clavulanic acid were better than those with Sulbactam, the highest increase in activity being obtained with Ceftizoxime in combination with any one of the inhibitors.

Bacteroides fragilis↗
PubMed1989

[In vitro activity of ampicillin and ampicillin-sulbactam on diverse bacteria].

A foremost mechanism of bacterial resistance to penicillin and its derivatives is the chromosomal or plasmid mediated production of B-lactamase. Inhibitors of these enzymes like sulbactam may help overcome this problem. We tested the in vitro activity of ampicillin alone or in association with sulbactam (1:1 ratio) against enterobacteriaceae, aeromonae, Hemophilus influenzae, staphylococci and Streptococcus fecalis, isolated from patients suffering different infectious diseases. The Kirby-Bauer method was used to evaluate susceptibility and MIC was determined by agar dilution techniques. Most enterobacteriaceae and aeromonae were resistant to ampicillin. The association was effective against shigellae and Yersinia enterocolitica. 28% of H. influenzae strains were resistant to ampicillin alone but were susceptible to the association. 30% of resistant staphylococci became sensitive to the association.

Ampicillin↗
PubMed1989

[Bactericidal effect of cefotaxime-sulbactam and imipenem combined with gentamicin and/or ciprofloxacin against CTX-1 producing Klebsiella pneumoniae].

Bactericidal activity of gentamicin, imipenem, ciprofloxacin and cefotaxime associated with sulbactam are studied on 36 beta lactamase CTX-1 (TEM-3) producing Klebsiella pneumoniae strains isolated of sputum samples and urines, among patients of intensive care units, in Rangueil hospital (Toulouse). Gentamicin, imipenem, cefotaxime associated with sulbactam have a bactericidal activity at serum levels, obtained with usual therapeutic doses. Ciprofloxacin has a bactericidal activity at concentrations obtained in urine and into lung tissue. Killing curve method was used to study bactericidal activity of these antibiotics alone and in combination, on a representative sample. Alone gentamicin showed the most rapid bactericidal activity (2 hours). The associations with gentamicin are also rapidly bactericidal. The associations with ciprofloxacin and imipenem, ciprofloxacin and cefotaxime/sulbactam are synergistic.

Cefotaxime↗
PubMed1989

[Comparison of the in vitro activity of amoxycillin + clavulanic acid and ampicillin + sulbactam combinations against 50 Haemophilus influenzae strains producing beta lactamase].

We compared the ability of two beta lactamase inhibitors, clavulanic acid and sulbactam, to reduce the minimal inhibitory concentrations (MICs) respectively of amoxycillin and ampicillin against fifty strains of Haemophilus influenzae producing a beta lactamase. The reduction of MICs of aminopenicillins was studied using low concentrations of beta lactamase inhibitors (0.125 to 0.5 mg/l). Moreover, the synergic effect of each association was evaluated against a heavy bacterial inoculum (10(8) cfu/ml). The combination of amoxycillin + clavulanic acid was more synergic on these strains than the association of ampicillin + sulbactam.

Amoxicillin↗