セフチブテン 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
Ceftibuten is a new, once daily, orally active cephalosporin introduced as a treatment of
Gram-negative bacteria-related urinarylrespiratory tract and gynecological infections.
In vitro studies of 359 strains of Gram-negative bacteria demonstrated that ceftibuten
was superior to cefaclor and as active or slightly more active than cefixime and
cefteram.
使用
anorexic, antidepressant, inhibitor of 5HT, norepinephrine & dopamine uptake
定義
ChEBI: A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to tre
t urinary-tract and respiratory-tract infections.
抗菌性
A semisynthetic cephalosporin formulated as the dihydrate
for oral administration.
It exhibits good activity against many Gram-negative bacilli,
but its activity against Gram-positive cocci is very poor. It
is stable to hydrolysis by the common plasmid-mediated
β-lactamases, but not derepressed chromosomal enzymes .
It is rapidly and almost completely absorbed by mouth and
is excreted in the urine with a half-life of 1.5–3 h. An oral dose
of 400 mg achieves a peak plasma concentration of around
15 mg/L. Binding to plasma proteins is 65–77%.
Side effects mostly consist of mild gastrointestinal symptoms
and mild liver function test changes. Clinical trials have
mainly been conducted in urinary tract and respiratory tract
infections which, despite the poor in-vitro activity against
Str. pneumoniae, have shown ceftibuten to be as efficacious as
comparator agents.
一般的な説明
Chemical structure: ?-lactam
薬物動態学
Ceftibuten is highly (75–90%) absorbed on oral administration,
but this is decreased significantly by food. Being lipophilic and acidic, it is significantly (65%) serum protein
bound. Some isomerization of the geometry of the olefinic linkage appears to take place in vivo before
excretion.
臨床応用
Ceftibuten (Cedax) is a recently introduced, chemicallynovel analog of the oximino cephalosporins in which anolefinic methylene group (C＝CHCH
2-) with Z stereochemistryhas replaced the syn oximino (CBNO-) group.
This isosteric replacement yields a compound that retainsresistance to hydrolysis catalyzed by many β-lactamases,has enhanced chemical stability, and is orally active. Oralabsorption is rapid and nearly complete. It has the highestoral bioavailability of the third-generation cephalosporins.Ceftibuten is excreted largely unchanged in the urine andhas a half-life of about 2.5 hours. Plasma protein binding ofthis cephalosporin is estimated to be 63%.
Ceftibuten possesses excellent potency against mostmembers of the Enterobacteriaceae family, H. influenzae,Neisseria spp., and M. catarrhalis. It is not active against S.aureus or P. aeruginosa and exhibits modest antistreptococcal activity. Ceftibuten is recommended in the managementof community-acquired respiratory tract, urinary tract, andgynecological infections.
セフチブテン 上流と下流の製品情報
原材料
準備製品