Comparative activity of BRL 25.000 with amoxycillin against resistant clinical isolates

Landuyt, H. W. Van; Pyckavet, Monique; Lambert, A

doi:10.1093/jac/7.1.65

Cited by 14 publications

(5 citation statements)

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“…These compounds act as suicide inactivators of the bacterial enzymes, meaning that both drug and enzyme are destroyed subsequent to their interaction (25). Combination of potassium clavulanate with amoxicillin extends the spectrum of the latter to include many beta-lactamase-producing strains of Staphylococcus aureus, Haemophilus influenzae, Bacteroides fragilis, K. pneumoniae, and some other members of the Enterobacteriaceae (70,174). Combined with ticarcillin, the inhibitor increased the proportion of the Enterobacteriaceae susceptible to the former from 72 to 91% (14).…”

Section: Enzyme Inhibitorsmentioning

confidence: 99%

Antibiotic combinations: should they be tested?

1988

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When antibiotic combinations are used to provide a broader spectrum of antimicrobial activity or in an attempt to prevent the emergence of resistant organisms, it is rarely necessary or practical to perform tests of drug interactions in vitro. In vitro testing of combinations may be useful when combinations are used in an attempt to attain synergistic interactions. In some cases, screening methods can be used as substitutes for formal synergy testing. This paper examines the mechanisms of antibiotic interaction leading to synergism or antagonism, surveys attempts to correlate in vitro observations with efficacy in animal models, and reviews clinical data providing evidence for or against a useful role of synergistic antibiotic interactions in the treatment of human infections.

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Section: Enzyme Inhibitorsmentioning

confidence: 99%

Antibiotic combinations: should they be tested?

1988

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“…It has been shown in vitro that this agent will render an ampicillin-resistant organism susceptible to ampicillin if resistance is due to production of a P-lactamase which is inhibited by clavulanic acid (1,5,10,12). This in vitro effect has been confirmed in vivo in several trials of a combination of amoxicillin with clavulanic acid in the treatment of urinary tract infections (1,3,4,6 Growth from this specimen was regarded as significant if it yielded more than 105 CFU/ml of a single species.…”

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confidence: 93%

Comparative study of amoxicillin-clavulanic acid and cephalexin in the treatment of bacteriuria during pregnancy

Pedler¹,

Bint²

1985

Antimicrob Agents Chemother

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A comparative clinical trial of amoxicillin-clavulanic acid and cephalexin was carried out in 80 women with bacteriuria of pregnancy. Treatment was randomly aUlocated and consisted of either one tablet of amoxicillin plus clavulanic acid (250 and 125 mg, respectively) three times daily or cephalexin (250 mg) three times daily for 7 days. Overall bacteriological cure rates at 2 weeks were 77% in the amoxicillin-clavulanic acid group and 74% in the cephalexin group. At 6 weeks the respective rates were 76 and 60%. Twenty-five episodes of infection were with ampicillin-resistant strains; cure rates were 82% (2 weeks) and 80% (6 weeks) in the amoxicillin-clavulanic acid group and 85 and 64%, respectively, in the cephalexin group. Differences in cure rates were not statistically significant. No significant difference in the rate of side effects was found. In particular, no toxicity to the fetus was seen which could be ascribed to either drug. Amoxiciflin-clavulanic acid would appear to be a safe and effective treatment for bacteriuria of pregnancy.Ampicillin and amoxicillin are popular choices for the treatment of bacteriuria of pregnancy. They are active against the majority of commonly isolated infecting organisms and enjoy a low incidence of unwanted effects in the mother, with the further advantage that there is no evidence of toxicity to the developing fetus. Resistance to ampicillin, however, is increasing both in hospitals and in the community; in the main, this is due to plasmid-directed production of P-lactamase. There is therefore a need for antimicrobial agents possessing the same properties as ampicillin and amoxicillin but with activity against 3-lactamase-producing organisms resistant to these antibiotics.Clavulanic acid is an inhibitor of several of the more usual plasmid-mediated P-lactamases (7,8). It has been shown in vitro that this agent will render an ampicillin-resistant organism susceptible to ampicillin if resistance is due to production of a P-lactamase which is inhibited by clavulanic acid (1,5,10,12). This in vitro effect has been confirmed in vivo in several trials of a combination of amoxicillin with clavulanic acid in the treatment of urinary tract infections (1,3,4,6 Growth from this specimen was regarded as significant if it yielded more than 105 CFU/ml of a single species. Significant pyuria was defined as -20 pus cells per ,ul. Patients with significant growth from this specimen were entered into the trial, but a second MSU was taken before treatment was started; only if the result of this specimen confirmed that of the first were data from that patient used in assessing efficacy. Patients were excluded from the trial if they were known to be hypersensitive to the penicillins or cephalosporins, if the infection was caused by an organism resistant to one of the trial drugs, or if the patient was already taking an antibiotic or had taken one since the first MSU was collected.Sensitivity testing to cephalexin was carried out by the breakpoint method (11), using diagnostic sensitivity te...

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“…A very potent 3-lactamase inhibitor is clavulanic acid, a fermentation product of Streptomyces clavuligerus (14,15). Although its intrinsic antibacterial activity is comparatively weak, it irreversibly inhibits a wide range of ,B-lactamases of Richmond types II through V (12), protecting the P-lactam antibiotics administered simultaneously (e.g., amoxicillin from inactivation) and rendering the lactamase-producing organisms susceptible to the action of the antibiotic (8,18). A new formulation of amoxicillin plus clavulanic acid (4:1 by weight) exploits this strongly synergistic effect by combining the two components for oral application (see [1,7,13]).…”

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Pharmacokinetics of amoxicillin and clavulanic acid administered alone and in combination

Adam¹,

Visser²,

Koeppe³

1982

Antimicrob Agents Chemother

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The pharmacokinetics of amoxicillin and clavulanic acid, administered alone and in combination, were studied in six male and six female normal human volunteers. Each ingested 500 mg of amoxicillin or 125 mg of clavulanic acid or the above agents in combination in randomized sequences. The results indicate that most of the parameters tested for either substance are essentially independent of the presence of the other one.Microorganisms which are resistant to certain antibiotics are increasingly posing problems in the therapy of bacterial infections. The preponderant reason for this resistance against P-lactam antibiotics is the spread of ,-lactamase genes among pathogenic strains (9). One modem concept of coping with these problems is the inhibition of P-lactamase activities concomitant with the antibiotic attack on the bacterial cell. A very potent 3-lactamase inhibitor is clavulanic acid, a fermentation product of Streptomyces clavuligerus (14,15). Although its intrinsic antibacterial activity is comparatively weak, it irreversibly inhibits a wide range of ,B-lactamases of Richmond types II through V (12), protecting the P-lactam antibiotics administered simultaneously (e.g., amoxicillin from inactivation) and rendering the lactamase-producing organisms susceptible to the action of the antibiotic (8, 18). A new formulation of amoxicillin plus clavulanic acid (4:1 by weight) exploits this strongly synergistic effect by combining the two components for oral application (see [1,7,13]).The purpose of the study presented here was to investigate the mutual influence of either one of the components on the pharmacokinetic data of the other. For this purpose, urine excretion and serum drug levels were measured in volunteers after oral administration of amoxicillin, clavulanic acid, or a combination of both drugs.MATERIALS AND METHODS Substances. The substances administered were amoxicillin trihydrate (corresponding to 500 mg of amoxicillin), potassium clavulanate (corresponding to 125 mg offree acid), and a combination (corresponding to 500 mg of amoxicillin + 125 mg of clavulanic acid) called "the combination" throughout this paper. All substances were supplied by Beecham-Wulfing, Neuss, West Germany.Experimental design. The investigation was carried out in the randomized crossover mode, with 12 healthy volunteers (6 females and 6 males). Their average age was 26.1 years (standard deviation [SD] = 2.4 years), the average weights were 58.0 kg (SD = 7.3 kg) for the females and 69.0 kg (SD = 8.7 kg) for the males, the average heights were 166.5 cm (SD = 4.6 cm) for the females and 177.7 cm (SD = 7.9 cm) for the males. Tests carried out before the study revealed that all of the volunteers were healthy; their renal functions, serum enzyme levels, and blood analysis data were normal. Each subject was given 500 mg of amoxicillin orally in course a, 125 mg of clavulanic acid in course b, and 625 mg of the combination in course c. All six possible sequences of courses a, b, and c were realized with one female and one male test...

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Comparative activity of BRL 25.000 with amoxycillin against resistant clinical isolates

Cited by 14 publications

References 0 publications

Antibiotic combinations: should they be tested?

Antibiotic combinations: should they be tested?

Comparative study of amoxicillin-clavulanic acid and cephalexin in the treatment of bacteriuria during pregnancy

Pharmacokinetics of amoxicillin and clavulanic acid administered alone and in combination

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