Detail of "70458-95-6"

CAS Number:
70458-95-6
Name:
Pefloxacin mesylate
Molecular Structure:
Formula:
C₁₇H₂₀FN₃O₃^.CH₄O₃S
Molecular Weight:
429.46
Synonyms:
1-Ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, monomethanesulfonate;Pefloxacin methanesulfonate;
EINECS:
274-613-9
Boiling Point:
529.1 °C at 760 mmHg
Flash Point:
273.8 °C
Hazard Symbols:
F, C
Risk Codes:
11-34
Safety:
16-26-36/37/39-45 Details

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Reference

Activities of pefloxacin and ciprofloxacin in experimentally induced Pseudomonas pneumonia in neutropenic guinea pigs: Activities of pefloxacin and ciprofloxacin in experimentally induced Pseudomonas pneumonia in neutropenic guinea pigs. Gordin, Fred M.; Hackbarth, Corinne J.; Scott, Kenyon G.; Sande, Merle A. (Dep. Med., Univ. California, San Francisco, CA 94110, USA). Antimicrob. Agents Chemother., 27(4), 452-4 (English) 1985. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Pefloxacin mesylate (I) [70458-95-6] and ciprofloxacin [85721-33-1] are two new quinoline carboxylic acid derivs. that have activity in vitro against a wide range of gram-neg. bacteria, including Pseudomonas aeruginosa. In a well-standardized model of Pseudomonas pneumonia in neutropenic guinea pigs, both drugs were highly effective in increasing survival and decreasing bacterial counts in the lungs of surviving animals. Pefloxacin and ciprofloxacin were significantly better than aminoglycosides or b-lactams tested in prior studies with this model, and they were as effective as combination therapy with aminoglycosides and b-lactams. Resistance to either ciprofloxacin or pefloxacin did not emerge during the study period. Further studies with these drugs in the therapy of Pseudomonas infections are warranted.

Absorption, distribution, metabolic fate, and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys, and humans: Absorption, distribution, metabolic fate, and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys, and humans. Montay, G.; Goueffon, Y.; Roquet, F. (Cent. Rech. Lab. Roger Bellon, Alfortville 94140, Fr.). Antimicrob. Agents Chemother., 25(4), 463-72 (English) 1984. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10 Pefloxacin mesylate (I) [70458-95-6] was well absorbed by the oral route. The antimicrobial activity in dog, monkey, and human plasma was essentially due to the unchanged drug which resp. accounted for 64, 94, and 84% of the total activity (ratios derived from relative area under the curve [AUC] values). Half-lives ranged from 1.9 h in mice to 8.6 h in humans. Protein binding was weak, about 20% in plasma. Except in the brain, drug concns. in most of the organs and tissues tested in rats and dogs were higher than the plasma levels. Microbiol. activity of the drug in urine was mainly due to pefloxacin [70458-92-3] and norfloxacin [70458-96-7], the N-desmethyl metabolite. The norfloxacin-pefloxacin ratios were 0 in mice, 1 in rats and dogs, 1.6 in monkeys, and 2.3 in humans. The principal urinary compds. were unchanged drug in mice, pefloxacin glucuronide [90352-18-4] and pefloxacin N-oxide [85145-21-7] in rats and dogs, norfloxacin and pefloxacin in monkeys, and pefloxacin N-oxide and norfloxacin in humans. The urinary recovery of the identified metabolites was 29.5% of the dose in mice, 37.8% in rats, 36.3% in dogs, 26.5% in monkeys, and 58.9% in humans. Biliary excretion occurred and was extensive in rats and dogs, mainly as a glucuronide conjugate of the drug. In rat and human bile, the main active compd. was unchanged pefloxacin.

Detail of "70458-95-6"

Pefloxacin mesylate

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CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

CAS No.70458-95-6 Pefloxacin mesylate

Reference