セフプロジル 化学特性,用途語,生産方法
効能
抗生物質, 細胞壁合成阻害薬
説明
Cefprozil is a new orally active cephalosporin useful in the treatment of otitis media,
uncomplicated skin and skin structure infections plus upper/lower respiratory tract
infections. Although structurally similar to cefadroxil, its spectrum of antibacterial
activity is comparable to cefaclor, but exhibits greater activity against S.aureus, S.
epidermidis, Listeria monocytogenes, Streptococci, H. influenzae, Propionibacterium
acnes. Clostridium perfringens and difficile.
化学的特性
Pale Yellow Solid
使用
Semisynthetic oral cephalosporin consisting of approx. 90:10 Z/E isomeric mixture. Antibacterial
定義
ChEBI: A semisynthetic, second-generation cephalosporin, with prop-1-enyl and (R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is used to treat bronchitis as well as ear, skin and other bacterial infec
ions.
抗菌性
Activity against Gram-positive cocci and Gram-negative
bacilli is better than that of cefadroxil (which it structurally
resembles) but is not as good as that of group 5 agents
. It is moderately stable to hydrolysis
by the common plasmid-mediated β-lactamases, but is hydrolyzed
by the chromosomal enzymes of Gram-negative bacilli
.
危険性
Moderately toxic by ingestion. Human sys-
temic effects.
薬物動態学
Oral absorption: >90%
C
max 250 mg oral: 5–7 mg/L after 1 h
500 mg oral: 10 mg/L after 1
Plasma half-life: 1–1.4 h
Volume of distribution: 15–201
Plasma protein binding: 35–45%
Absorption and distribution
It is almost completely absorbed and well distributed, penetrating
well into tonsillar and other tissues and inflammatory
exudate. Absorption is unaffected by food or
antacids and there is no accumulation on multiple dosing
regimens.
Metabolism and excretion
Most of the dose is excreted unchanged in urine, though
about 20% is found in feces. Urinary concentrations after a
500 mg oral dose usually exceed 1 g/L. The elimination halflife
is prolonged in patients with renal impairment, reaching
6 h in anuric patients. About half the drug is removed in 3 h
by hemodialysis.
臨床応用
Cefprozil (Cefzil) is an orally active second-generationcephalosporin that is similar in structure and antibacterialspectrum to cefadroxil. Oral absorption is excellent (oralbioavailability is about 95%) and is not affected by antacidsor histamine H2-antagonists. Cefprozil exhibits greater invitro activity against streptococci, Neisseria spp., and S. aureusthan does cefadroxil. It is also more active than thefirst-generation cephalosporins against members of theEnterobacteriaceae family, such as E. coli, Klebsiella spp., P. mirabilis, and Citrobacter spp. The plasma half-life of1.2 to 1.4 hours permits twice-a-day dosing for the treatmentof most community-acquired respiratory and urinary tractinfections caused by susceptible organisms.
副作用
It is well tolerated. Diarrhea and gastrointestinal discomfort
may occur. There have been a few reports of pseudomembranous
colitis and serum sickness-like reactions.
セフプロジル 上流と下流の製品情報
原材料
準備製品