A new tricyclic fluoroquinolone, rufloxacin (MF-934), with interesting antibacterial and pharmacokinetic characteristics.
The kinetics of a new fluoroquinolone, rufloxacin (MF-934), have been studied in rats, dogs and monkeys. The drug is characterized by a long half-life, which is equal to 24, 12 and 15 h in the three species, respectively. A high tissue plasma ratio is observed in rats. In these animals the bioavailability is equal to 60%. The drug does not appear to enter the brain in rats and in monkeys, even after repeated administration (90 days). No accumulation is seen in rats and in monkeys after repeated daily administration for 90 days. The urinary excretion of unmodified drug is equal to about 27 and 40% of the dose in the rat and in the monkey, respectively.
Segre
G
G
Institute of Pharmacology, University of Siena, Italy.
Cerretani
D
D
Cerri
D
D
Moltoni
L
L
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000032:analysis / Q000493:pharmacokinetics / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D005260:Female; D024841:Fluoroquinolones; D008252:Macaca fascicularis; D008297:Male; D015363:Quinolones; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity; D014018:Tissue Distribution
D042462:4-Quinolones; D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; C060328:rufloxacin