Lomefloxacin

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H302：삼키면 유해함

  H312：피부와 접촉하면 유해함

  H332：흡입하면 유해함

• 예방조치문구

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

Lomefloxacin MSDS

• 1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid

Lomefloxacin 화학적 특성, 용도, 생산

• 개요

  Lomefloxacin is a once-daily, third-generation quinolone antibiotic useful in the treatment of bacterial infections. The new fluorinated quinolone does not interfere with the metabolism of theophylline; it is efficacious against pathogens resistant to cephalosporins, penicillins and aminoglycosides.

• 화학적 성질

  colorless Needles

• 용도

  Anti bacterial.

• 정의

  ChEBI: A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.

• Pharmaceutical Applications

  A difluoropiperazinyl quinolone formulated as the hydrochloride salt for oral administration. The in-vitro activity is very similar to that of norfloxacin . It is active against Enterobacteriaceae and fastidious Gram-negative bacilli, including L. pneumophila. Activity against Campylobacter spp., Ps. aeruginosa, Acinetobacter and Chlamydia spp. is poor. It has reduced activity against staphylococci and poor activity against streptococci, L. monocytogenes, anaerobes and Mycobacterium spp.
  A 400 mg oral dose achieves a concentration of 3–5 mg/L after 1–1.5 h. In escalating oral doses of 100, 400 and 800 mg to volunteers, the AUC was essentially proportional to the dosage, the mean plasma concentrations following 100, 400 and 800 mg doses being approximately 1.1, 4.7 and 7.5 mg/L, respectively.
  Several metabolites have been described, accounting for <5% of the oral dose. Elimination occurs principally via the kidneys and 50–70% of a dose appears in the urine over 24 h. In patients with impaired renal function given 400 mg orally, the apparent elimination half-life ranged from 8 to 44 h, depending on the degree of renal failure. Non-renal clearance was also impaired, but there was no significant change in other pharmacokinetic parameters. The daily dosage (400 mg) should be reduced to 280 mg when the creatinine clearance falls below 30 mL/min. Hemodialysis has no effect on the plasma concentration. The effect of lomefloxacin on the plasma concentration of theophylline is clinically insignificant and no dosage adjustment is required.
  The main adverse event is phototoxicity; other adverse events (mainly diarrhea, abdominal pain, skin reactions, dizziness, headache and insomnia) occur in about 10% of patients.
  It is chiefly used in urinary tract infection, but is no longer widely available.

• Clinical Use

  1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid (Maxaquin) is adifluorinated quinolone with a longer elimination half-life(7–8 hours) than other members of its class. It is the onlyquinolone for which once-daily oral dosing suffices. The oralbioavailability of lomefloxacin is estimated to be 95% to98%. Food slows, but does not prevent, its oral absorption.The extent of biotransformation of lomefloxacin is only about5%, and high concentrations of unchanged drug, rangingfrom 60% to 80%, are excreted in the urine. The comparativelylong half-life of lomefloxacin is apparently because ofits excellent tissue distribution and renal reabsorption and not because of plasma protein binding (only ～10%) or enterohepaticrecycling (biliary excretion is estimated to be ～10%).
  Lomefloxacin has been approved for two primary indications. First, it is indicated for acute bacterial exacerbations of chronic bronchitis caused by H. influenzae or Moraxella (Branhamella) catarrhalis, but not if Streptococcus pneumoniae is the causative organism. Second, it is used for prophylaxis of infection following transurethral surgery. Lomefloxacin also finds application in the treatment of acute cystitis and chronic urinary tract infections caused by Gram-negative bacilli.

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