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.
レボフロキサシン 上流と下流の製品情報
原材料
準備製品