Cefprozil

Cefprozil 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  Pale Yellow Solid

• 용도

  Semisynthetic oral cephalosporin consisting of approx. 90:10 Z/E isomeric mixture. Antibacterial

• 정의

  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.

• Antimicrobial activity

  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 .

• 위험도

  Moderately toxic by ingestion. Human sys- temic effects.

• Pharmacokinetics

  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.

• Clinical Use

  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.

• 부작용

  It is well tolerated. Diarrhea and gastrointestinal discomfort may occur. There have been a few reports of pseudomembranous colitis and serum sickness-like reactions.

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