Cefpiramide sodium - CAS 74849-93-7
Catalog number: 74849-93-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Cefpiramide sodium is a new Pseudomonas-active cephalosporin with a broad spectrum of antibacterial activity. It was more active against Acinetobacter spp. and Pseudomonas spp. It inhibited many Pseudomonas aeruginosa resistant to carbenicillin, piperacillin, and cefotaxime, but it was less active than ceftazidime and cefsulodin. It also inhibited staphylococci and streptococci and had appreciable activity against Streptococcus faecalis and Listeria moncytogenes.
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SM-1652; Wy-44635
1.Quantitative evaluation of capacity-limited hepatobiliary transport based on hepatocellular diffusion model by MULTI(FEM).
Higashimori M1, Yamaoka K, Fujitani S, Nakagawa T. J Pharmacokinet Pharmacodyn. 2001 Oct;28(5):415-44.
The dose-dependency of hepatic uptake and hepatobiliary transport of a drug was evaluated by means of a nonlinear least square program incorporating the finite element method, MULTI(FEM). A perfusion experiment using isolated rat livers following a pulse input (i.e., under nonsteady-state conditions) was performed at three dose levels of cefpiramide as a model drug. The hepatic extraction ratio (E(H)) of cefpiramide decreased with an increase in dose, which demonstrates that the hepatic uptake is capacity-limited. The outflow time-profiles from the liver were represented by a two-compartment dispersion model with central Michaelis-Menten elimination, and the maximal elimination rate per central compartment volume (Vmax) and the Michaelis constant (Km) were estimated to be 1420 microg/ml/min and 235 microg/ml, respectively. The biliary mean transit time (t(bile)) increased slightly with an increase in dose. The hepatocellular diffusion model under non-steady-state conditions considering nonlinear transport across the bile canalicular membrane was adopted to evaluate dose-dependency in the biliary excretion of cefpiramide.
2.Biliary excretion of phenolphthalein glucuronide in the rat.
Ogasawara T1, Takikawa H. Hepatol Res. 2001 Jun;20(2):221-231.
To examine the substrate specificity of an ATP-dependent organic anion transporter, the multidrug resistance protein 2, we examined the effects of various bile acid conjugates and organic anions on the biliary excretion of phenolphthalein glucuronide, a hydrophilic glucuronide conjugate, in rats. Biliary phenolphthalein glucuronide excretion was markedly inhibited by taurolithocholate-3-sulfate and ursodeoxycholate-3-O-glucuronide. In contrast, ursodeoxycholate-3,7-disulfate and pravastatin only slightly inhibited and cefpiramide did not inhibit biliary phenolphthalein glucuronide excretion. Biliary excretion of sulfobromophthalein, leukotriene C(4) and pravastatin was inhibited by phenolphthalein glucuronide infusion to some extent. These findings suggest that phenolphthalein glucuronide is a relatively low affinity substrate for the multidrug resistance protein 2.
3.Biliary excretion of olmesartan, an anigotensin II receptor antagonist, in the rat.
Takayanagi M1, Sano N, Takikawa H. J Gastroenterol Hepatol. 2005 May;20(5):784-8.
BACKGROUND AND AIM: Olmesartan (RNH-6270) is a newly developed anigotensin II receptor antagonist, and has been reported to be excreted into feces. To examine the mechanism of the biliary excretion of olmesartan, we studied its biliary excretion in rats.
4.In-vitro antibacterial activities of cefpiramide and other broad-spectrum antibiotics against 440 clinical isolates in China.
Wang H1, Yu Y, Xie X, Wang C, Zhang Y, Yuan Y, Zhang X, Liu J, Wang P, Chen M. J Infect Chemother. 2000 Jun;6(2):81-5.
The in-vitro antibacterial activity of cefpiramide was compared with those of 15 other broad-spectrum cephalosporins. A total of 440 clinical strains of bacteria, including 9 bacterial species, were isolated from our hospital in 1998. The minimum inhibitory concentrations (MICs) of cefpiramide and five other antibiotics were determined for each species, using the agar-dilution method. The MIC of cefpiramide for Escherichia coli and Klebsiella pneumoniae was higher than those of three other third-generation cephalosporins, (ie, cefoperazone, ceftazidime, and ceftriaxone). Fifty-one percent (26/51) of Enterobacter cloacae isolates were resistant to cefpiramide. Cefoperazone/sulbactam and cefepime had greater activity against E. cloacae (resistance, 3.9% and 19.6%, respectively) than cefpiramide. Cefpiramide was more active against Pseudomonas aeruginosa (resistance rates, 12%) than cefoperazone, ceftazidime, ceftriaxone, aztreonam, and cefepime.
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CAS 74849-93-7 Cefpiramide sodium

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