Reference

Antimicrobial activity evaluations of two new quinolones, PD127391 (CI-960 and AM-1091) and PD131628

Antimicrobial activity evaluations of two new quinolones, PD127391 (CI-960 and AM-1091) and PD131628. Barrett, Mary S.Several substances are used for example 105956-97-6 and 127967-03-7 which are their cas registry numbers.; Jones, Ronald N.; Erwin, Meridith E.; Johnson, David M.; Briggs, Beth M. (Coll. Med., Univ. Iowa, Iowa City, IA 52242, USA). Diagn. Microbiol. Infect. Dis., 14(5), 389-401 (English) 1991. CODEN: DMIDDZ. ISSN: 0732-8893. DOCUMENT TYPE: Journal CA Section: 10 (Microbial, Algal, and Fungal Biochemistry) The in vitro activities of PD127391 and the new fluorinated-4-quinolone, PD131628, were compared with each other and with five similar fluoroquinolones (ciprofloxacin, enoxacin, fleroxacin, norfloxacin, and ofloxacin). A total of 844 isolates mainly from recent clin. bacteremias and addnl. stock strains with well-characterized resistance mechanisms were tested. PD127391 had slightly more activity than PD131628 (90% min. inhibitory concn. [MIC90] 0.008-0.12) against the Enterobacteriaceae, but both were 2- to 4-fold more potent than ciprofloxacin. PD131628 activity was equal to or greater than PD127391 when tested against Pseudomonas aeruginosa. PD127391 showed greatest activity against Bacteroides fragilis group strains (MIC90, 2 mg/mL) when compared with PD131628 (MIC90 >8 mg/mL). Both PD127391 (MIC90s, 0.015-1.0 mg/mL) and PD131628 (MIC90s, 0.03- >8 mg/mL) were more active than ciprofloxacin against Gram-pos. organisms. Altering the medium pH, adding divalent cations (magnesium), and increasing the inoculum concn. to 106 colony-forming units per spot adversely effected the activity of both PD127391 and PD131628. Resistance selection and mutational rates to resistance were identical to previously studied drugs in their class. .

The tolerance and pharmacokinetics of clinafloxacin (CI-960) in healthy subjects

The tolerance and pharmacokinetics of clinafloxacin (CI-960) in healthy subjects. Bron, N. J.; Dorr, M. B.; Mant, T. G.; Webb, C. L.; Vassos, A. B. ( Division of Warner-Lambert Company, Department of Clinical Pharmacology, Parke-Davis Pharmaceutical Research, Eastleigh SO53 3ZQ, UK). Journal of Antimicrobial Chemotherapy, 38(6), 1023-1029 (English) 1996 Saunders. CODEN: JACHDX. ISSN: 0305-7453. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The single-dose tolerance and pharmacokinetics of clinafloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy volunteers. Single oral doses of 25, 50, 100, and 200 mg were well tolerated. Adverse events after placebo and clinafloxacin were similar, with mild drowsiness, dizziness, headache, and rash being reported most frequently. The frequency and intensity of side-effects did not increase with dose. Clinafloxacin was rapidly absorbed, with Cmax occurring at approx. 40 min postdose. Plasma concns. increased proportionately and, following 100 or 200 mg doses, remained above MIC90S required for most nosocomial pathogens for at least 12 h. Clinafloxacin elimination half-life averaged 5.2 h and renal clearance was approx. 200 mL/min.Except for chemicals metioned above, 105956-97-6 is also used. About 50% of the administered dose was excreted unchanged in the urine. .