レボフロキサシン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H302：飲み込むと有害

  H317：アレルギー性皮膚反応を起こすおそれ

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

レボフロキサシン 価格

レボフロキサシン 化学特性,用途語,生産方法

• 外観

  うすい黄赤色～黄色～緑色粉末～結晶

• 効能

  抗菌薬, 核酸合成阻害薬

• 説明

  Levofloxacin, the optically active S-isomer of the fluoroquinolone antibiotic ofloxacin, is two to four times more potent than ofloxacin with reportedly less side effects in treating infections of the lower respiratory and urinary tract, prostate infections and sexually transmitted diseases. It has broad and potent antibacterial activity over common Grampositive and -negative aerobic pathogens and obligate anaerobes. Different from the cephem antibiotics, levofloxacin is unique in its marked selectivity against members of the family Enterobacteriaceae and its negligible effect on predominant anaerobes. Levofloxacin also exhibits satisfactory antimicrobial effects in surgical infections and it may be used for treatment of gastrointestinal infections such as traveler’s diarrhea associated with the pathogenic Enterobacteriaceae.

• 化学的特性

  Slight yellow powder

• 使用

  Antibacterial.

• 抗菌性

  Levofloxacin is the active component of ofloxacin; d-ofloxacin is without significant antibacterial activity. It exhibits good activity in vitro against Gram-positive cocci (including Str. pneumoniae), Enterobacteriaceae, some fastidious Gram-negative bacilli and Ps. aeruginosa as well as chlamydiae, Mycoplasma pneumoniae, L. pneumophila and M. tuberculosis. MICs for Acinetobacter spp. and Sten. maltophilia are 0.06–0.25 and 0.5–2.0 mg/L, respectively. Activity against anaerobes is moderate to low.

• 一般的な説明

  Chemical structure: quinolone

• 応用例（製薬）

  For molecular weight and structure, see ofloxacin . Levofloxacin is the l-isomer of ofloxacin.

• 薬物動態学

  Oral absorption: >95%
  C_max 500 mg oral: c. 5 mg/L after 1.5–2 h
  750 mg oral: c. 8 mg/L after 1.5–2 h
  500 mg intravenous (90-min infusion): c. 6 mg/L end infusion
  750 mg intravenous (90-min infusion) ：c. 12 mg/L end infusion
  Plasma half-life ：6–8 h
  Volume of distribution：0.6–0.8 L/kg
  Plasma protein binding： <25%
  Co-administration with antacids, calcium, sucralfate and heavy metals decreases bioavailability and AUC. No interactions with warfarin or theophylline have been observed. Co-administration of a non-steroidal anti-inflammatory drug may increase the risk of convulsions. It undergoes limited metabolism and is primarily eliminated unchanged in urine by both glomerular filtration and tubular secretion. The free AUC:MIC ratio for Str. pneumoniae increases from about 55 to 70 when the daily dosage is raised from 500 mg to 750 mg.
  It is stable in plasma and does not revert to d-ofloxacin. It undergoes limited metabolism and is primarily eliminated unchanged in the urine. Renal clearance in excess of the glomerular filtration rate suggests that tubular secretion also occurs. Concomitant administration of either cimetidine or probenecid reduces renal clearance by approximately onethird. Clearance is reduced and half-life is prolonged in patients with impaired renal function (creatinine clearance <50 mL/min) requiring dosage adjustment in such patients.

• 臨床応用

  Acute bacterial sinusitis
  Acute bacterial exacerbations of chronic bronchitis, community-acquired pneumonia
  Uncomplicated and complicated skin and skin structure infections
  Uncomplicated and complicated urinary infections including acute pyelonephritis
  Chronic bacterial prostatitis

• 副作用

  Side effects have been reported in 6–7% of patients and include fever, rash and other events common to the group. Elderly patients are at increased risk of developing severe tendon disorders including rupture, a risk increased by concomitant corticosteroid therapy.

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