Cefpodoxime

Bezeichnung:Cefpodoxime

CAS-Nr80210-62-4

Englisch Name:Cefpodoxime

CBNumberCB9511604

SummenformelC15H17N5O6S2

Molgewicht427.46

MOL-Datei80210-62-4.mol

Cefpodoxime physikalisch-chemischer Eigenschaften

Schmelzpunkt	200-202°C
Dichte	1.78±0.1 g/cm3(Predicted)
RTECS-Nr.	XI0367365
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Soluble in DMSO
pka	2.77±0.50(Predicted)
Aggregatzustand	Solid
Farbe	White to off-white
Sensitive	Light Sensitive
BRN	6021381
Stabilität	Hygroscopic

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	42/43
S-Sätze:	22-36/37-45
WGK Germany	3

Gefahreninformationscode (GHS)

Cefpodoxime Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Off-White Solid
Verwenden
Cefpodoxime Proxetil metabolite antibiotic
Verwenden
A metabolite of Cefpodoxime Proxetil. An antibacterial.
Verwenden
A metabolite of Cefpodoxime Proxetil (C243860). An antibacterial.
Definition
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.
Trademarks
Vantin (Pharmacia & Upjohn).
Antimicrobial activity
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.
Biologische Aktivität
cefpodoxime, as known as r 3763, is a metabolite of cefpodoxime proxetil. it is demonstrated that cefpodoxime, as an oral third generation cephalosporin antibiotic, is active against most gram-positive and gram-negative bacteria.cefpodoxime suppresses bacterial septum and cell wall synthesis by binding to penicillin-binding proteins (pbps) located in the bacterial cytoplasmic membrane.
Pharmakokinetik
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.
Clinical Use
Cefpodoxime has been used principally for the treatment of upper and lower respiratory tract infections in children and adults.
Nebenwirkungen
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.
in vitro
cefpodoxime showed antibacterial activities against obligatory anaerobes and salmonella spp., shigella spp. and neisseria meningitides. the activity of cefpodoxime was less active than r95867, an active form of cs-834, against gram-negative bacteria [1]. cefpodoxime was quite stable to hydrolysis by β-lactamases produced from b. cereus and e. coli hb101/pbr322 [2].
in vivo
male ddy mice were administered orally in a volume of 0.2 ml of 0.5% carboxymethyl cellulose sodium salt. after 7 days, it was shown that cefpodoxime had good efficacy against streptococcus spp. and k. pneumoniae infection in mice [1].
Einzelnachweise
[1]. sakagawa, e., otsuki, m., oh, t., & nishino, t. in-vitro and in-vivo antibacterial activities of cs-834, a new oral carbapenem. journal of antimicrobial chemotherapy, 1998; 42: 426-437.
[2]. fukuoka, t., ohya, s., utsui, y., domon, h., takenouchi, t., koga, t., … kuwahara, s. in vitro and in vivo antibacterial activities of cs-834, a novel oral carbapenem. antimicrobial agents and chemotherapy, 1997; 41(12): 2652–2663.

Cefpodoxime Upstream-Materialien And Downstream Produkte

Cefpodoxime Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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