Detail of "84880-03-5"

Reference

Pharmacokinetics of cefpimizole in normal humans after single- and multiple-dose intravenous infusions

Pharmacokinetics of cefpimizole in normal humans after single- and multiple-dose intravenous infusions. Lakings, Duane B.; Friis, Janice M.; Brown, Ronald J.; Allen, Harry R. (Upjohn Co., Kalamazoo, MI 49002, USA). Antimicrob. Agents Chemother., 26(6), 802-6 (English) 1984. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The pharmacokinetics of cefpimizole (I) [84880-03-5], a broad-spectrum cephalosporin antibiotic, were detd. after single- and multiple-dose 20-min i.v. infusions of 1, 2, and 4 g. The kinetics of single-dose administration of cefpimizole correspond to a 2-compartment model with an av. apparent vol. of distribution of 20.0 L, a distribution rate const. of 2.24 h-1, and a terminal rate const. of 0.358 h-1 (half-life, 1.9 h). The total body clearance was 118.6 mL/min. The primary route of elimination for cefpimizole was the renal route, with ~80% of the administered dose excreted as the parent compd. The elimination rate const., as calcd. from urinary excretion data, was 0.339 h-1, which is in close agreement with the terminal rate const. for plasma. Renal clearance of cefpimizole was 96.2 mL/min. Dose proportionality over the 3 dose levels was obtained from area under the plasma curve and cumulative urinary excretion data. The results of the multiple-dose study indicated that no apparent change in the distribution or elimination kinetics of cefpimizole occurred after the administration of 1-, 2-, and 4-g doses for 7 days, 3 times a day. The kinetics from the multiple-dose study were in close agreement with those from the single-dose study. No accumulation of cefpimizole occurred, and no detectable levels were obsd. 24 h after administration of the last dose. Peaks that could be attributed to metabolites of cefpimizole were not obsd. during high-pressure liq. chromatog. anal. of either plasma or urine specimens.

New cephalosporins cefotaxime, cefpimizole, BMY 28142, and HR 810 in experimental pneumococcal meningitis in rabbits

New cephalosporins cefotaxime, cefpimizole, BMY 28142, and HR 810 in experimental pneumococcal meningitis in rabbits. Tauber, Martin G.; Hackbarth, Corinne J.; Scott, Kenyon G.; Rusnak, Michael G.; Sande, Merle A. (Sch. Med., Univ. California, San Francisco, CA 94110, USA). Antimicrob. Agents Chemother., 27(3), 340-2 (English) 1985. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Four new cephalosporins, cefotaxime [63527-52-6], cefpimizole (U 63196E) [84880-03-5], BMY 28142 [88040-23-7], and HR 810 [84957-29-9] were evaluated in exptl. pneumococcal meningitis. Cefotaxime penetrated only moderately into the cerebrospinal fluid of rabbits with meningitis, whereas cefpimizole, BMY 28142, and HR 810 all exhibited unusually good penetration. The bactericidal activity in infected cerebrospinal fluid was comparable for the 4 drugs.