セフポドキシム 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
化学的特性
Off-White Solid
使用
A metabolite of Cefpodoxime Proxetil. An antibacterial.
定義
ChEBI: A third-generation cephalosporin antibiotic with methoxymethyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamino substituents at positions 3 and 7, respectively, of the cephem skeleton. Given by mouth as its proxetil ester prodrug, it is used
to treat acute otitis media, pharyngitis, and sinusitis.
抗菌性
It
is stable to a wide range of plasmid-mediated β-lactamases.
It induces the chromosomal β-lactamases of Ps. aeruginosa,
Enterobacter spp., S. marcescens and Citrobacter spp., but is a
less potent inducer than cefoxitin.
薬物動態学
Oral absorption: c. 50%
C
max 200 mg oral: 2.1 mg/L after 3 h
Plasma half-life: c. 2.2 h
Volume of distribution: c. 35 L
Plasma protein binding: 20–30%
Absorption and distribution
The ester is rapidly hydrolyzed to the parent compound in the small intestine. Bioavailability increases to 65% if taken with food, but antacids and H2-receptor antagonists reduce absorption. Unabsorbed drug is hydrolyzed and excreted in the feces.
It is well distributed and penetrates well into tissues (including lung tissue) and inflammatory exudate to achieve concentrations inhibitory to common pathogens.
Metabolism and excretion
The hydrolyzed prodrug is not subject to further metabolism. About 80% of the absorbed compound (30–40% of the original dose) appears in the urine over 24 h. Excretion is by glomerular filtration and tubular secretion; probenecid delays secretion and increases the peak plasma concentration.
Metabolism and excretion
The hydrolyzed prodrug is not subject to further metabolism. About 80% of the absorbed compound (30–40% of the original dose) appears in the urine over 24 h. Excretion is by glomerular filtration and tubular secretion; probenecid delays secretion and increases the peak plasma concentration.
臨床応用
Cefpodoxime has been used principally for the treatment of
upper and lower respiratory tract infections in children and
adults.
副作用
The drug is well tolerated, but gastrointestinal disturbance
with diarrhea is common. Pseudomembranous colitis has
been reported occasionally. Other side effects are those common
to cephalosporins.
セフポドキシム 上流と下流の製品情報
原材料
準備製品