Pharmacokinetics of Brodimoprim in Serum and Skin Blister Fluid

Abstract

Following 400 mg brodimoprim given orally to 8 volunteers, the peaks of the mean concentration curves were 3.2 ± 1.0 mg/1 in serum and 1.0 ± 0.2 mg/1 ( ± SEM) in skin blister fluid. The terminal half-lives were 25.9 ± 2.2 h and 42.2 ± 6.5 h in serum and blister fluid, respectively. The area under the concentration-versus-time curve for blister fluid was 73 % of serum value, and the mean recovery of bioactive drug in urine during 24 h was 3.4%. Considering the minimal inhibitory concentrations of potential target organisms and the slow elimination, the results suggest that brodimoprim may be useful in the treatment of infections, and that dosage once a day may be sufficient.

Correlations between theophylline concentrations in plasma, erythrocytes and cantharides-induced blister fluid and peak expiratory flow in asthma patients

“…In recent years tissue fluid penetration has been demonstrated for antibiotics such as timentin [Walstad et al 1986], brodimoprim [Kalager et al 1985], ceftriaxone [Lebel et al 1985], ceflizoxime [Korting et al 1984], ofloxacin [Lockley et al 1984], griseofulvin [Schafer- , cardiotonics such as digoxin [Schafer-Korting et al 1987], and anti-inflammatory drugs, such as ketoprofen [Netter et al 1990]. Those studies showed that BF allows direct experimental access to the peripheral compartment.…”

“…The efficacy of a number of drugs, including antibiotics [Korting et al 1984;Lockley et al 1984;Kalager et al 1985;Lebel et al 1985;Schafer-Korting et al 1985;Walstad et al 1986], cardiotonics such as digoxin [Schafer-Korting et al 1987], and anti-inflammatory agents [Netter et al 1990] have been evaluated on the basis of their penetration into tissue fluids. Few works have actually documented the assumed correlation between tissue fluid concentration and pharmacodynamic effect.…”