The penetration of ticarcillin and clavulanate into cartilage was investigated in 20 subjects undergoing funnel chest correction. Cartilage samples, obtained 120 or 180 min after administration of ticarcillin/clavulanate (mean dose: ticarcillin 70.0 mg/kg, clavulanate 4.7 mg/kg), were divided into core samples and outer covering portions. After 120 min, the mean ticarcillin in the outer portion was 11.0 mg/kg and that in the core sample was 0.81 mg/kg; at 180 min the mean concentration in the outer portion was 6.47 mg/kg and ticarcillin was undetectable in all but two core samples. Clavulanate was shown to decline with time in spiked cartilage preparations and the results in this investigation may underestimate penetration. Clavulanate was undetectable in most core samples. In the outer portion the mean concentration was 1.30 mg/kg at 120 min and 0.62 mg/kg at 180 min. The penetration gradient requires further elucidation and should be considered when chemotherapy for infection in cartilage is discussed.

Adolescent↗

PubMed1989

Penetration of amoxycillin/clavulanate into human bone.

Twenty patients undergoing orthopaedic surgery for total hip replacement received a single prophylactic intravenous dose of 2.2 g Augmentin (2 g amoxycillin + 200 mg clavulanate). Bone samples removed during the operation were saved for amoxycillin and clavulanate assay. The proportion of inorganic matter in the bone samples was determined to calculate the concentrations of the drugs in their distribution volume. The cortical and cancellous bone were penetrated to a comparable extent by both compounds yielding maximum concentrations at one hour after the end of the infusion. The mean concentrations of amoxycillin in the cortex and spongy layer were 26.0 and 18.2 mg/kg within 1 h, 23.8 and 19.8 mg/kg in the interval from 1 to 2 h after infusion, and 9.2 and 5.9 mg/kg between 2 and 5 h. The corresponding values for clavulanate were 2.3 and 1.6 mg/kg, 2.5 and 1.6 mg/kg, and 1.0 and 0.7 mg/kg, respectively. No postoperative wound infections occurred in these patients.

Aged↗

PubMed1987

Concentrations of ticarcillin and clavulanic acid in human bone after prophylactic administration of 5.2 g of timentin.

The penetration of ticarcillin and clavulanate into their distribution space within human bone was determined after prophylactic administration of 5.2 g of timentin (5 g of ticarcillin plus 0.2 g of clavulanic acid) to 20 patients undergoing hip surgery. All samples were taken 45 to 85 min postadministration. The mean concentrations of ticarcillin in spongiosa and corticalis bone were 57.1 and 70.5 mg/kg, respectively; those of clavulanic acid were 17.8 and 32.5 mg/kg, respectively. No infections occurred in these patients.

Aged↗

PubMed1987

Therapeutic experience with ticarcillin disodium plus potassium clavulanate in the Federal Republic of Germany--results of a multicentre-study.

Three hundred and eighty protocols of a multicentre study of ticarcillin plus clavulanic acid were evaluated. Patients with a multitude of severe infections were treated. Therapy with the drug combination was successful in 89% of the cases. The drug was tolerated very well. No severe adverse reactions were attributable to the test drug.

Adolescent↗

PubMed1985

A survey of temocillin sensitivity of strains resistant to newer beta-lactam antibiotics.

The susceptibility of a total of 2014 Gram-negative clinical isolates (except Pseudomonas aeruginosa) to a number of antibiotics, including temocillin, was investigated in 2 geographically distinct areas. Overall, more strains were sensitive to temocillin than to mezlocillin, piperacillin, amoxycillin plus clavulanic acid, cefotaxime, cephazolin, latamoxef (moxalactam), cefoxitin, or netilmicin. Susceptibility to temocillin of multiple-resistant strains was studied.

Bacterial Infections↗

PubMed1985

Treatment of severe infections with temocillin. Clinical and bacteriological evaluation.

Included in a study of the clinical efficacy of temocillin were 20 hospitalised female patients suffering from infections of the respiratory or urinary tract, septicaemia or an abscess. Clinical evaluation revealed fully effective treatment in all patients, and all pathogens identified were eliminated during therapy with no adverse reactions being observed.

Abscess↗

PubMed1984

In-vitro activity of augmentin against clinically important gram-positive and gram-negative bacteria in comparison with other antibiotics.

The susceptibility to Augmentin of a total of 1,417 bacterial isolates was investigated. Augmentin is a new formulation of the broad-spectrum beta-lactam-antibiotic amoxicillin together with the beta-lactamase-inhibitor clavulanic acid. It was demonstrated that 88% of all isolates tested were sensitive to Augmentin, 9% were resistant. 88% of all Pseudomonas aeruginosa strains fell in the "resistant" category. Only 1/71 anaerobes and 15/286 staphylococci were classified as resistant to Augmentin.

Amoxicillin↗

PubMed1981

The spatial organization of the active sites of the bifunctional oligomeric enzyme tryptophan synthase: cross-linking by a novel method.

Explore the source record for details and available documents.

Bacterial Proteins↗

PubMed1981

Dependency on serine concentration of the activity of tryptophan synthase. Cooperative properties.

The activity of the enzyme tryptophan synthase from Escherichia coli was tested as a function of the concentration of L-serine which serves as a substrate in the indole to tryptophan reaction as well as for the L-serine deaminase activity. L-Serine binding was found to follow the pattern of negative cooperativity both by kinetic and by equilibrium methods. The enzyme kinetic data support the view that a rapid equilibration model for the enzyme . substrates complex formation is not strictly obeyed.

Escherichia coli↗

PubMed1978

On the mechanism of action of Escherichia coli tryptophan synthase. Steady-state investigations.

Tryptophan synthase from Escherichia coli (L-serine hydro-lyase (adding indole), EC 4.2.1.20) synthesizes L-trypotophan from indoleglycerol phosphate and L-serine, releasing glyceraldehyde 3-phosphate, or from indole and L-serine. The latter reaction (B reaction), catalyzed either by the beta2 species or by the (alpha2 beta2) complex, has been studied by steady-state methods. A sequential mechanism is indicated. Inhibition experiments with the substrate analogue benzimidazole were carried out in order to distinguish between random and ordered mechanisms. The results are compatible with a random sequential mechanism. The dissociation constants of the enzyme-substrate complexes are evaluated. When catalyzed by the tetrameric complex (alpha2 beta2) the B reaction is inhibited by higher concentrations of the substrate indole. This inhibition does not follow the usual substrate inhibition pattern. The question whether the binding of indole to the alpha-subunit exerts an inhibitory effect on the beta2 species, possibly by reversing the activation by the alpha subunit of the beta2 species, is discussed.

Benzimidazoles↗

PubMed1974