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J Zürcher

Publications and source records attributed to J Zürcher.

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Distribution kinetics of enoxacin and its metabolite oxoenoxacin in excretory fluids of healthy volunteers.

The distribution kinetics of enoxacin and its main metabolite oxoenoxacin in excretory fluids was investigated in 11 healthy volunteers. A single intravenous dose of 428 mg of enoxacin was given as a 1-h infusion. Serial samples of plasma, urine, saliva, nasal secretions, tears, and sweat were drawn and analyzed for enoxacin and oxoenoxacin by reversed-phase high-pressure liquid chromatography. Large differences in the concentration-time profiles of the excretory fluids analyzed were observed. Nasal secretions exhibited the highest enoxacin exposure, as assessed by the area under the concentration-time curve. Excretory fluid/plasma area under the concentration-time curve ratios were found to be 1.67 +/- 0.36 for nasal secretions, 0.76 +/- 0.28 for saliva, 0.25 +/- 0.07 for sweat, and 0.23 +/- 0.11 for tears. The elimination half-life of enoxacin from sweat (8.27 +/- 2.63 h) was significantly longer than that for plasma (5.10 +/- 0.46 h). Oxoenoxacin was detected in urine and saliva and exhibited a higher renal clearance and a lower saliva exposure than the parent compound. In contrast to that of the metabolite, distribution of enoxacin in saliva was found to be time and pH dependent. In conclusion, our study revealed considerable differences in the distribution kinetics of enoxacin among various excretory sites. Because of distinct acidic and basic properties, the anionic oxometabolite significantly differs from the zwitterionic parent compound in its distribution characteristics.

Adult↗

[Enoxacin concentrations in lung tissue].

For successful treatment of bacterial lung infections the administered antibiotic must reach sufficiently high concentrations in lung tissue. Therefore, the concentrations of enoxacin in this tissue were measured in ten patients requiring pulmonary surgery. In order to prevent postoperative infection, the patients received 400 mg enoxacin b.i.d. for three days. Eight h after the final dose samples of venous blood were drawn and a sample of lung tissue was removed. Using a microbiological assay, we found the following concentrations (mean +/- S.D.):serum 2.36 (+/- 0.65) mg/l, lung 6.48 (+/- 1.54) mg/kg. With the HPLC-technique the corresponding values method were 2.37 (+/- 0.80) mg/l and 7.41 (+/- 3.01) mg/kg. Thus concentrations of enoxacin in lung tissue are about three times higher than the corresponding serum concentrations.

Aged↗

[Enoxacin concentration in bone tissue].

For successful treatment of bacterial osteomyelitis the administered antibiotic must reach sufficiently high concentrations in bone tissues. Therefore concentrations of enoxacin in bone in ten patients requiring hip surgery were measured. To prevent a postoperative infection, 400 mg enoxacin b.i.d. for two days were administered. On an average 120 (90-210) min after the final dose samples of venous blood and bone tissue were taken. The bone pieces were divided into corticalis and spongiosa. Using a bio-assay-method the following concentrations were found: (mean +/- S.D.): serum 2.88 ( +/- 0.90) mg/l, corticalis 5.90 ( +/- 0.79) mg/kg, spongiosa 3.95 ( +/- 1.01) mg/kg. Thus enoxacin reaches higher levels in bone tissue than in serum.

Aged↗

[Enoxacin concentration in seminal fluid, in prostate secretions and in prostatic adenoma tissue following oral administration or intravenous infusion].

In eleven volunteers and 39 patients undergoing transurethral resection of the prostate or bladder tumor, concentrations of enoxacin were measured in seminal fluid (volunteers), in prostatic fluid (volunteers, patients) and in prostatic adenoma tissue (patients) after oral (400 mg) administration and intravenous (428 mg) infusion (60 min) of enoxacin. Simultaneously 2.534 g of iothalamic acid was i.v. injected to identify possible urinary contamination. The concentrations of enoxacin in seminal fluid after 2-4 h and in prostatic tissue after about 1-4 h and 14-16 h exceeded plasma concentrations more than two-fold. The concentrations in prostatic fluid after 1-4 h were about half the plasma concentrations. Venous blood samples were taken after intravenous infusion at intervals of up to 24 h in a total of 14 patients. The mean plasma concentration of enoxacin decreased from its maximum of 6.9 mg/l at the end of infusion to 0.5 mg/l at 12 h after administration. A terminal half life of 6.65 h was calculated according to an open two-compartment model.

Administration, Oral↗