PubMed Health⌕ Search

Biomedical subjects

M R Lockley

Publications and source records attributed to M R Lockley.

9 recordsLinked to original sources

The pharmacokinetics of ofloxacin and a review of its tissue penetration.

The pharmacokinetics of ofloxacin were studied in six healthy volunteers following a 600 mg oral dose. The concentration of the compound was measured in serum, inflammatory fluid and urine. Ofloxacin was rapidly absorbed, the mean maximum concentration of ofloxacin being 10.7 mg/l at 1.2 h. The mean serum elimination half-life was 7 h and 80.3% of the administered compound was recovered in the urine by 48 h. Ofloxacin penetrated the inflammatory fluid well, the mean peak level being 5.2 mg/l at 5.3 h. A review of the tissue penetration is presented which indicates that the high volume of distribution of ofloxacin is associated with good tissue penetration.

Adult↗

The pharmacokinetics and tissue penetration of imipenem.

Two studies were performed to investigate the penetration of imipenem into chemically induced inflammatory exudate and into peritoneal fluid. In the first study six volunteers received 500 mg of imipenem, alone and with 500 mg cilastatin. Little difference was noted in the pharmacokinetics or inflammatory fluid penetration of imipenem when given with or without cilastatin. The only significant alteration was the urine recovery (an increase from a mean of 14.7% to 55.6% in the presence of the enzyme inhibitor). The mean inflammatory fluid level of imipenem at 30 min was 6.2 mg/l (or 35% of the plasma level). The inflammatory fluid levels exceeded the plasma levels after 2 h. The overall penetration of imipenem/cilastatin into inflammatory fluid was 67.8% (+/- 13.8) and imipenem alone 73.2% (+/- 13.9). The mean elimination half-life of imipenem from plasma was 1.1 h and from inflammatory fluid 1.4 h (with or without cilastatin). In the second study, 29 patients received 1 g imipenem plus cilastatin before elective surgery and plasma and peritoneal levels were measured over 4 h. There was considerable penetration of the peritoneum, imipenem levels in excess of 30 mg/l being found 15 min after administration declining to 5-7 mg/l by 3-4 h. The mean percentage penetration was 73.4% (+/- 22.1). A brief review of the literature on imipenem tissue penetration is included.

Adult↗

Pharmacokinetics and tissue penetration of temocillin.

The pharmacokinetics of intravenous (bolus) temocillin 1 g were studied in 6 healthy male volunteers, and a cantharides blister method was used to estimate tissue penetration of the antibiotic. The mean elimination half-life was 4.5 hours. Temocillin penetrated blister fluid rapidly and reached concentrations of about 50% of those in serum by 2 to 3 hours after administration. Over an 8-hour period, the serum and blister fluid concentrations exceeded the MIC90 of susceptible bacteria by 2-fold or greater, suggesting that twice or even once daily dosing with temocillin may be sufficient.

Blister↗

The pharmacokinetics and tissue penetration of ofloxacin.

The pharmacokinetics of the 4-quinolone agent, ofloxacin, were studied in six healthy volunteers, following a 600 mg oral dose. The levels of the compound were measured by a microbiological assay in serum, blister fluid and urine. The compound was rapidly absorbed, the mean maximum concentration of ofloxacin being 10.7 mg/l at 1.2 h. The mean serum elimination half-life was 7 h and 80.3% of the administered compound was recovered in the urine by 48 h. Ofloxacin penetrated the blister fluid well, the mean peak level being 5.2 mg/l at 5.3 h.

Adult↗