Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Clavulanic Acids”

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 775 records · Page 43Linked to original sources
PubMed1990

Amoxicillin/clavulanic acid. An update of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Clavulanic acid enhances the antibacterial spectrum of amoxicillin by rendering most beta-lactamase-producing isolates susceptible to the drug. In clinical trials amoxicillin/clavulanic acid is clinically and bacteriologically superior to amoxicillin alone and at least as effective as numerous other comparative agents, such as orally administered cephalosporins, cotrimoxazole, doxycycline and bacampicillin, in the treatment of adults and children with the most common forms of infection encountered in general practice, i.e. urinary tract infections, upper and lower respiratory tract infections, otorhinolaryngological infections, and skin and soft tissue infections. It may also provide effective treatment for uncomplicated gonorrhoea, chancroid and gynaecological infections as well as acting as a prophylactic agent against surgical infection. Thus, in general practice environments where beta-lactamase production has restricted the effectiveness of amoxicillin, the combination of clavulanic acid with amoxicillin has clearly extended the usefulness of a tried and proven first-line antibacterial agent.

Amoxicillin↗
PubMed1984

Parenteral augmentin: pharmacokinetics.

The pharmacokinetics of intravenous Augmentin have been investigated and the data found to fit a two compartment model. In the first study, to a crossover design, a bolus injection of 1.2 g Augmentin was given to 8 healthy volunteers with and without probenecid. It was found that the serum concentrations of amoxycillin were increased in the presence of probenecid, but those of clavulanic acid were unaffected. In a second study a further 8 volunteers received an infusion over 30 min of 2.2 g Augmentin. At the end of the infusion, peak concentrations in excess of 100 micrograms/ml were recorded for amoxycillin and 14 micrograms/ml for clavulanic acid. In both studies the serum and urinary concentrations of amoxycillin and clavulanic acid obtained were well above those considered necessary to achieve a therapeutic effect.

Adult↗
PubMed1990

Lack of influence of beta-lactamase-producing flora on recovery of group A streptococci after treatment of acute pharyngitis.

Because production of beta-lactamase by normal pharyngeal flora could account for penicillin treatment failure, we studied the effect of anaerobic and aerobic beta-lactamase-producing bacteria on bacteriologic outcome in acute group A beta-hemolytic streptococcal (GABHS) pharyngitis. We compared 10-day courses of orally administered phenoxymethyl penicillin and amoxicillin-clavulanic acid, using a randomized, single-blind treatment protocol. Eligible patients were 2 to 16 years of age and had culture-proven acute GABHS pharyngitis; 89 patients (43 penicillin, 46 amoxicillin-clavulanic acid) were compliant with therapy. beta-Lactamase-producing organisms were isolated before therapy from the throats of 67% of patients treated with penicillin and 63% treated with amoxicillin-clavulanic acid. Throat cultures after completion of therapy were positive for GABHS in 7 (7.9%) of 89 patients. The initial GABHS T type persisted (treatment failure) in only 4 (4.5%) of 89 patients, including 3 (6.5%) of 46 who received amoxicillin-clavulanic acid and in 1 (2.3%) of 43 who received penicillin (not statistically significant). Bacteriologic treatment failure was unrelated to recovery of beta-lactamase-producing bacteria at the time of enrollment or after treatment. We conclude that beta-lactamase production by normal pharyngeal flora does not fully explain the failure of penicillin therapy for acute streptococcal pharyngitis. Using an antibiotic effective against beta-lactamase-producing bacteria will not eliminate the problem of bacteriologic treatment failure.

Adolescent↗
PubMed1984

Effects of hemodialysis on the pharmacokinetics of amoxicillin/clavulanic acid combination.

The effects that renal disease and hemodialysis have on the pharmacokinetics of amoxicillin/clavulanic acid combination were studied in a patient receiving this combination for the treatment of a Nocardia asteroides infection. Hemodialysis increased the clearance of both substances as evidenced by lower serum concentrations during the on-dialysis day, i.e., 2.3 +/- 0.8 vs. 5.9 +/- 1.2 micrograms/ml for clavulanic acid and 8.0 +/- 1.8 vs. 12.4 +/- 0.9 micrograms/ml for amoxicillin. Clavulanic acid appeared to be influenced to a greater extent as compared to amoxicillin because of its higher extraction ratio (0.74 vs. 0.44) as well as a higher observed ratio of amoxicillin to clavulanic acid during the on-dialysis day (3.59 +/- 1.27 vs. 2.28 +/- 0.65; p less than 0.05). Comparison of the area under the serum concentration-time (AUC) during the off-dialysis day with published AUC values suggested accumulation of amoxicillin/clavulanic acid. These data indicate that dosage adjustments for amoxicillin/clavulanic acid may be required in patients with chronic renal failure who are on hemodialysis. Further studies in this patient population are needed before specific dosing guidelines can be provided.

Amoxicillin↗
PubMed1999

Penetration of beta-lactamase inhibitors into the periplasm of gram-negative bacteria.

The effectiveness of a beta-lactamase inhibitor/beta-lactam combination against Gram-negative pathogens depends on many interplaying factors, one of which is the penetration of the inhibitor across the outer membrane. In this work we have measured the relative penetrations of clavulanic acid, sulbactam, tazobactam and BRL 42715 into two strains of Escherichia coli producing TEM-1 beta-lactamase, two strains of Klebsiella pneumoniae producing either TEM-1 or K-1, and two strains of Enterobacter cloacae each producing a Class C beta-lactamase. It was shown that clavulanic acid penetrated the outer membranes of all these strains more readily than the other beta-lactamase inhibitors. For the strains of E. coli and K. pneumoniae clavulanic acid penetrated approximately 6 to 19 times more effectively than tazobactam, 2 to 9 times more effectively than sulbactam and 4 to 25 times more effectively than BRL 42715. The superior penetration of clavulanic acid observed in this study is likely to contribute to the efficacy of clavulanic acid/beta-lactam combinations in combating beta-lactam resistant bacterial pathogens.

Anti-Bacterial Agents↗
PubMed1987

Intraperitoneal penetration of ticarcillin/clavulanic acid (Timentin).

Thirty-eight patients undergoing elective abdominal surgery were given 3.0 g ticarcillin plus 0.2 g clavulanic acid as a single intravenous injection at varying times prior to the operation. Sterile assay discs were placed on the peritoneal surface in order to measure peritoneal fluid levels of each agent. Simultaneous serum levels were also measured. A total of 38 serum and peritoneal samples were analysed. There was rapid penetration of both agents into peritoneal fluid. The mean peritoneal fluid levels of ticarcillin were 70% (S.D. 13) of the serum level and 67% (S.D. 4) for clavulanic acid. The peritoneal levels of both agents declined in parallel to the serum levels (the half-lives being about 1 h) and the ratio of ticarcillin-clavulanic acid in serum and peritoneal fluid did not vary significantly with time.

Abdomen↗
PubMed1995

Antimicrobial susceptibility of subgingival bacterial flora in dogs with gingivitis.

The aerobic and anaerobic flora from gingival pockets of 49 dogs with severe gingivitis and periodontitis were cultured. The susceptibility of each isolate to four antimicrobial agents currently approved for veterinary use in the USA (amoxicillin-clavulanic acid; clindamycin; cefadroxil; and enrofloxacin) was determined. Amoxicillin-clavulanic acid (Clavamox Pfizer Animal Health) had the highest in-vitro susceptibility against all isolates (96%), all aerobes (94%) and all anaerobes (100%) tested. For gram-negative aerobes, enrofloxacin (Baytril, Bayer Corp.) had the highest in-vitro susceptibility activity. For bacteria associated with treatment of gingivitis, which typically are mixed aerobic/anaerobic and gram-positive/gram-negative organisms, the antimicrobial of choice for clinical use based on these susceptibility tests is amoxicillin-clavulanic acid.

Amoxicillin-Potassium Clavulanate Combination↗
PubMed2004

Streptomyces clavuligerus has a second copy of the proclavaminate amidinohydrolase gene.

Past genetic studies have indicated that the genes encoding early enzymes of clavulanic acid biosynthesis may be duplicated in Streptomyces clavuligerus. We observed cross-hybridizing bands upon Southern analyses of proclavaminate amidinohydrolase (pah)-defective mutant strains of S. clavuligerus screened with a pah-specific probe. The DNA fragment responsible for this cross hybridization was cloned and sequenced and shown to encode a second copy of the pah gene. The new pah gene (pah1) was 1,056 bp in length, and its sequence was 72% identical to that of the original pah gene (pah2). Disruption mutants with defects in pah1 showed no significant effects on production of clavulanic acid or any of the clavam metabolites with stereochemistries opposite that of clavulanic acid (5S clavams) produced by S. clavuligerus when they were grown on starch asparagine or soy medium. However, double mutants with defects in both pah1 and pah2 were defective in the production of both clavulanic acid and all of the 5S clavam metabolites.

Amino Acid Sequence↗
PubMed1987

[Bronchial superinfection. Clinical trial of clavulanic acid-amoxicillin against josamycin].

Authors report a prospective clinical an bacteriological study in 32 patients, almost with a chronic bronchopulmonary disease. A group of 16 patients was treated with the association clavulanic acid-amoxicillin (ACA) and the 16 others with josamycin (J) for an acute exacerbation of bronchitis. Pus and numeration of bacteria in expectorations were the criteria of efficacity. Better results of ACA group were assessed with 14 cures (87%) against 4 (25%) (p less than 0.001) and no failure against 4 in J group (p less than 0.05). They conclude therapy with ACA is more effective and recommended in serious acute exacerbations in chronic bronchopulmonary diseases.

Aged↗
PubMed1996

In vitro activity of cefdinir against respiratory pathogens isolated in Sicily with reference to beta-lactamase production.

The in vitro activity of cefdinir (CI-983, FK-482), an orally absorbed aminothiazolyl cephalosporin, was evaluated against all 287 strains of Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Streptococcus pneumoniae and Streptococcus pyogenes in comparison with cefaclor, cefuroxime, amoxicillin, amoxicillin-clavulanic acid, erythromycin and cotrimoxazole. The bactericidal activity of cefdinir, cotrimoxazole, amoxicillin-clavulanic acid and erythromycin was determined against H. influenzae, M. catarrhalis and S. pneumoniae. With the exception of one beta-lactamase negative ampicillin-resistant strain of H. influenzae (resistant to all antibiotics tested), no resistance to cefdinir was observed (MIC < or = 1 mg/l). Cefdinir was active against H. influenzae, H. parainfluenzae and M. catarrhalis regardless of whether or not they produced beta-lactamase. In general, the inhibitory concentrations of cefdinir against H. influenzae, H. parainfluenzae and M. catarrhalis were similar to those of amoxicillin/clavulanic acid, one or two dilutions lower than those of cefuroxime and four dilutions lower than those of cefaclor and cotrimoxazole. Against S. pneumoniae and S. pyogenes cefdinir had the same activity as cefuroxime and amoxicillin but was more effective than the other antibiotics tested. Kinetic studies showed that cefdinir was rapidly bactericidal at concentrations 2 and 4 times the minimum inhibitory concentration (MIC): a reduction of 99.9% in CFU values was generally observed after 6-8 h.

Administration, Oral↗
PubMed1990

In-vitro sensitivity of amoxicillin/clavulanic acid (Augmentin) to isolated beta-lactamases and in-vitro antibacterial activity.

The in vitro sensitivity of amoxicillin alone and combined with clavulanic acid (ratio 4:1) as been studied by a spectrophotometric method utilizing crude extract of the following enzymes: TEM1, TEM2, SHV1, SHV2, TLE1, HMS1, LXA, P99, ENT208. The in-vitro antibacterial activity of ampicillin, amoxicillin alone and associated with clavulanic acid was also determined by an agar dilution method. Clavulanate protects amoxicillin from the hydrolytic activity of plasmid mediated beta-lactamase, conferring a stability on the beta-lactam comparable with that of cefotaxime. The protection of amoxicillin by means of clavulanic acid reduces the minimal concentration of antibiotic necessary to inhibit most bacterial species and allows bacteria to remain sensitive to the drug which might otherwise be resistant.

Amoxicillin↗
PubMed1999

Antibiotic efficacy in small intestinal bacterial overgrowth-related chronic diarrhea: a crossover, randomized trial.

BACKGROUND & AIMS: No controlled trial has examined the clinical efficacy of antibiotics in small bowel bacterial overgrowth. METHODS: Ten patients with bacterial overgrowth-related diarrhea underwent the following five 7-day treatment periods: untreated (control period), then placebo, and subsequently, in random order and blinded fashion, norfloxacin (800 mg/day), amoxicillin-clavulanic acid (1500 mg/day), and Saccharomyces boulardii (1500 mg/day). A hydrogen breath test was performed on the first and last day of each period. RESULTS: Daily stool frequency was similar during the control and placebo periods (4.2 +/- 0.6 vs. 3.9 +/- 0.6 [mean +/- SEM], respectively). Norfloxacin and amoxicillin-clavulanic acid led to a significant reduction in daily stool frequency (2.3 +/- 0.4 and 3.0 +/- 0.5, respectively; P < 0.01 vs. placebo period) after 2.0 +/- 1.4 and 1.2 +/- 0.4 days, which was maintained for 6.1 +/- 3.7 and 6.0 +/- 9.6 days, respectively. Breath-expired H(2) volume decreased with norfloxacin (37 +/- 8 to 12 +/- 5 mL per 2 hours; P < 0.01) and amoxicillin-clavulanic acid (24 +/- 6 to 8 +/- 4 mL per 2 hours, respectively; P = 0.01), but H(2) breath test result was negative in only 3 and 5 patients. CONCLUSIONS: Norfloxacin and amoxicillin-clavulanic acid are effective in the treatment of bacterial overgrowth-related diarrhea.

Adult↗
PubMed1980

Synergistic activity of piperacillin in combination with beta-lactamase inhibitors.

Clavulanic acid and a penicillanic acid sulfone, when combined individually with piperacillin, synergistically inhibited various Enterobacteriaceae, Staphylococcus aureus, and Bacteroides fragilis. Clavulanic acid and piperacillin synergistically inhibited 91 of 170 (55%) isolates tested. Synergy was most often found against piperacillin-resistant bacteria: 65 of 69 isolates (94%). Although the penicillanic acid sulfone acted synergistically with piperacillin, inhibiting 62 of 170 strains (33%), the concentration of clavulanic acid required for synergy generally was less than that of penicillanic acid sulfone. Combination of piperacillin and cefotaxime, an inhibitor of type 1 beta-lactamases, rarely was synergistic and was antagonistic for several species. The combination of piperacillin with potent beta-lactamase inhibitors made piperacillin active against those isolates of Escherichia coli and Klebsiella and Bacteroides species, as well as selected other species, that are resistant to piperacillin by virtue of their production of beta-lactamases.

Anti-Bacterial Agents↗
PubMed2002

CE versus LC for simultaneous determination of amoxicillin/clavulanic acid and ampicillin/sulbactam in pharmaceutical formulations for injections.

A rapid, capillary electrophoresis method was evaluated for determination of amoxicillin and clavulanic acid in Augmentin as well as ampicillin and sulbactam in Unasyn preparations for injections. Phosphate-borate buffer at pH 8.66 containing 14.4% sodium dodecyl sulfate was used as a mobile phase. The method was validated. Reproducibility, precision, accuracy and assay linearity in concentration of amoxicillin 0.05-3.03 mg/ml and ampicillin 0.05-3.08 mg/ml, as well as clavulanic acid 0.02-2.02 mg/ml and sulbactam 0.05-2.08 mg/ml were established. This new method is fast, inexpensive and limits consumption of organic solvents when compared with alternative high performance liquid chromatography (HPLC) method, used for drug analysis. Statistical analysis by Student's t-test showed no significant differences between the results obtained by the two methods t(calculated) 0.32 and 1.69 for amoxicillin and clavulanic acid and 0.67 and 1.93 for ampicillin and sulbactam were smaller than t(tabulated).

Amoxicillin-Potassium Clavulanate Combination↗
PubMed1986

In vitro activity of an orally administered cephalosporin, LY164846, against potentially pathogenic respiratory and dermal bacterial isolates.

The antibacterial activity of LY164846, a new orally administered semisynthetic cephalosporin, was compared with that of amoxicillin-clavulanic acid against 492 potentially pathogenic respiratory tract and dermal isolates. Against groups A, B, and G streptococci; pneumococci; staphylococci (other than methicillin resistant); Haemophilus influenzae; Branhamella catarrhalis; and meningococci, the MICs for 90% of strains tested of LY164846 and amoxicillin-clavulanic acid were less than or equal to 4 and less than or equal to 1 microgram/ml, respectively. LY164846 was equally active against beta-lactamase-positive and -negative strains of Haemophilus and Staphylococcus. MBC to MIC ratios of LY164846 versus H. influenzae were less than or equal to 2, while those with Staphylococcus aureus were more difficult to determine because of skipped tubes or paradoxic effects. There were minimal inoculum, pH, or serum effects on LY164846 activity against H. influenzae and S. aureus. In time-kill studies, LY164846 and amoxicillin-clavulanic acid at double MICs were 99.9 to 100% bactericidal to H. influenzae in 24 h; two times the MIC of LY164846 and four times the MIC of cephalexin were 99.9 to 100% bactericidal to S. aureus in 24 h. Based on error-rate-bounded analysis, the following interpretative guidelines for 30-micrograms LY164846 disk diffusion test diameters are suggested: greater than or equal to 19 mm, susceptible (MIC, less than or equal to 4 micrograms/ml); 16 to 18 mm, intermediate (MIC, greater than 4 but less than or equal to 8 micrograms/ml); less than or equal to 15 mm, resistant (MIC, greater than 8 micrograms/ml).

Amoxicillin↗
PubMed2001

Amoxicillin/clavulanate in chronic rhinosinusitis: tissue and serum distribution.

UNLABELLED: Amoxicillin/clavulanate in chronic rhinosinusitis: tissue and serum distribution. OBJECTIVE: The aim of the present study is to determine the concentrations of coamoxiclav in the sinusal mucosa of patients undergoing surgery for chronic sinusitis in comparison to serum levels after single oral administration. METHODOLOGY: 24 patients affected by chronic sinusitis, undergoing sinus surgery, were divided into three groups receiving an oral dose of 1 g of coamoxiclav (875 mg amoxicillin, 125 g of clavulanic acid, 7:1 ratio) at 2 h (first group), 4 h (second group) and 6 h (third group) before surgery. The mean concentration of amoxicillin and clavulanic acid were determined biologically in serum and in tissues. RESULTS: The highest concentrations of coamoxiclav both in serum and tissues were observed in the group which received the antibiotic 2 hours before surgery. However the tissue levels of both amoxicillin and clavulanic acid in the time period within 2-6 h after administration were higher than the Minimum Inhibitory Concentration (MIC) for the most frequent causative pathogens of sinus bacterial infections. CONCLUSIONS: Since penicillins need to maintain concentrations above the MIC for at least 40 to 60% of the interval time between administrations to be potentially effective, the Authors concluded that since both amoxicillin and clavulanic acid spread well in the ENT tissues, 1 g twice a day of the combination seems to be clinically effective even in patients suffering from acute episodes of chronic rhinosinusitis.

Adolescent↗
PubMed2001

Bioequivalence study of a novel Solutab tablet formulation of amoxicillin/clavulanic acid versus the originator film-coated tablet.

With amoxicillin/clavulanic acid Solutab tablet, a new tablet formulation of amoxicillin/clavulanic acid (500/125), was developed. The aim of the present study was to demonstrate bioequivalence between the new tablet formulation, taken as an intact tablet and after prior dispersal, versus the originator product viz. Augmentan film-coated tablet. The study was performed in 48 healthy volunteers, according to an open, single-dose three-period, crossover design. Blood samples were taken prior to each administration and at 10 time points after dosing. Plasma concentrations of amoxicillin and clavulanic acid were determined by validated high performance liquid chromatography with UV detection. With regard to amoxicillin, the results were within the preset bioequivalence range of 0.8 to 1.25 for the ratios of the primary parameters AUC(0-t) and Cmax. In terms of clavulanic acid the 90% confidence intervals of the ratios for AUC(0-t) and Cmax versus the reference lay outside the predefined bioequivalence range of 0.75 to 1.33. This result, however, was mainly due to the large variability of the reference formulation compared to the amoxicillin/clavulanic acid Solutab tablet. Based on statistical indications that 3/48 subjects with extremely low levels on the reference formulation could be regarded as "outliers" and after excluding these subjects' data from the statistical analysis, results for clavulanic acid were within the predefined bioequivalence range of 0.75 to 1.33. Overall, the amoxicillin/clavulanic acid Solutab tablet provided, in comparison to the reference tablet, less variable levels of clavulanic acid, thus giving more appropriate protection to the available amoxicillin. Thirteen adverse events were reported post dosing by 7 subjects. There were no differences in incidence of adverse events between amoxicillin/clavulanic acid Solutab tablet taken intact or dispersed and Augmentan.

Adolescent↗
PubMed1983

[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) in the field of otorhinolaryngology].

We studied BRL 25000, (amoxicillin trihydrate and potassium clavulanate a beta-lactamase inhibitor in ratio of 2: 1), in the otorhinolaryngological field in terms of its basic and clinical utility. Pharmacokinetics The distribution of BRL 25000 in mucous membrane of maxillary sinus and retaining liquid of maxillary sinus after administration of 1 tablet (375 mg) was favorable and the good transitional properties were obtained. It was similar to chephems. Clinical results BRL 25000 was administered to 26 patients (6 cases with otitis media, 9 cases with tonsillitis, 2 cases with sinusitis, 1 case with laryngitis, 5 cases with pharyngitis, 1 case with epipharyngitis and 2 cases with pharyngolaryngitis). The overall clinical effective response was obtained in 88.5% of patients. Bacteriological effects BRL 25000 was effective against amoxicillin-resistant S. aureus and K. rhinoscleromatis. Side effects No adverse reactions were seen.

Adult↗