U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 531 - 540 of 576 results

Status:
Possibly Marketed Outside US
Source:
ORASPOR by Ciba-Geigy
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cefroxadine is an antibiotic developed for the treatment of bacterial infectious diseases caused by gram-negative and gram-positive organisms. The information about drug status is unavailable and is supposed to be "discontinued", however it may be manufactured in Italy by Novartis.
Status:
Possibly Marketed Outside US
Source:
TOMIRON by Toyama
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefteram is a semisynthetic cephalosporin formulated for oral administration as the prodrug ester, cefteram pivoxil. The mechanism of action of cefteram is inhibition of bacterial cell wall synthesis. Cefteram exerts its bactericidal activity by strongly binding to penicillin-binding protein (PBP) 3, 1A, and 1Bs. The drug is available in Japan and is used for the treatment of bacterial infections.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefozopran Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefozopran hydrochloride is a third-generation cephalosporin that was launched for the treatment of severe infections in immunocompromised patients caused by staphylococci and enterococci. While it shows a very broad antibacterial spectrum against Gram-positive and Gram-negative organisms, it is particularly potent against S. aureus, Enterococcus faecalis, P. aeruginosa, and Citrobacter freundii. It is resistant to hydrolysis by most chromosomal and plasmid mediated β-lactamases and is reported to be active against respiratory, urinary tract, obstetrical, gynecological, soft tissue, and surgical infections. Similar to β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases.
Cefatrizine is a broad-spectrum, semisynthetic, first-generation cephalosporin with antibacterial activity. Cefatrizine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Cefatrizine is used to treat a large variety of bacterial infections, such as respiratory tract, ear, skin and urinary tract infections. Cefatrizine is less effective against gram positive bacteria than first generation drugs. Antibiotics require constant drug level in body for therapeutic effect.
Cefuzoname (CZON, L-105) is a second-generation cephalosporin antibiotic, has broad spectrum on Gram-positive or -negative bacteria and may also be effective against Staphylococcus aureus against which third generation cephalosporins are largely ineffective.
Cefbuperazone (cefalosporin antibiotic) is marketed under the brand name Keiperazon by Kaken, and Tomiproan by Toyama, Japan. It is powder for injection 0.5 and 1 g/ampoule. It is indicated to treat infections with susceptible microorganisms. It has been proposed especially against Pseudomonas infections. Cefbuperazone binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.
Status:
Possibly Marketed Outside US
Source:
Ceftezole sodium for injection by Fujisawa Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or GU tract, skin and skin structure, endocarditis. Surgical prophylaxis.
Status:
Possibly Marketed Outside US
Source:
NCT04664803: Phase 4 Interventional Terminated Acute Sinusitis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefetamet pivoxil is an oral third-generation cephalosporin which is hydrolysed to form the active agent, cefetamet. Cefetamet has excellent in vitro activity against the major respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci; it is active against beta-lactamase-producing strains of H. influenzae and M. catarrhalis, but has poor activity against penicillin-resistant S. pneumoniae. Cefetamet has marked activity against Neisseria gonorrhoeae and possesses a broad spectrum of activity against Enterobacteriaceae. Both staphylococci and Pseudomonas spp. are resistant to cefetamet. Cefetamet pivoxil has been investigated in the treatment of both upper and lower community-acquired respiratory tract infections and has demonstrated equivalent efficacy to a number of more established agents, namely cefaclor, amoxicillin and cefixime. In complicated urinary tract infections, cefetamet pivoxil showed similar efficacy to cefadroxil, cefaclor and cefuroxime axetil. Cefetamet pivoxil was effective in the treatment of otitis media, pneumonia, pharyngotonsillitis and urinary tract infections in children. Cefetamet is not extensively bound to plasma proteins. Cefetamet has a relatively small apparent volume of distribution consistent with that of other beta-lactam antibiotics. The absorption and disposition of cefetamet in human subpopulations [i.e. children, elderly (< 75 years of age), renal impairment, liver disease and patients taking concomitant drugs] have been studied extensively. Only impaired renal function appears to significantly alter the elimination of this drug. Cefetamet pivoxil exerts its bactericidal action by inhibition the final transpeptidation step of peptidoglycan synthesis in the bacterial cell wall by binding to one or more of the Penicillin-binding Proteins (PBPs).
Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
Possibly Marketed Outside US
Source:
NCT04664803: Phase 4 Interventional Terminated Acute Sinusitis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefetamet pivoxil is an oral third-generation cephalosporin which is hydrolysed to form the active agent, cefetamet. Cefetamet has excellent in vitro activity against the major respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci; it is active against beta-lactamase-producing strains of H. influenzae and M. catarrhalis, but has poor activity against penicillin-resistant S. pneumoniae. Cefetamet has marked activity against Neisseria gonorrhoeae and possesses a broad spectrum of activity against Enterobacteriaceae. Both staphylococci and Pseudomonas spp. are resistant to cefetamet. Cefetamet pivoxil has been investigated in the treatment of both upper and lower community-acquired respiratory tract infections and has demonstrated equivalent efficacy to a number of more established agents, namely cefaclor, amoxicillin and cefixime. In complicated urinary tract infections, cefetamet pivoxil showed similar efficacy to cefadroxil, cefaclor and cefuroxime axetil. Cefetamet pivoxil was effective in the treatment of otitis media, pneumonia, pharyngotonsillitis and urinary tract infections in children. Cefetamet is not extensively bound to plasma proteins. Cefetamet has a relatively small apparent volume of distribution consistent with that of other beta-lactam antibiotics. The absorption and disposition of cefetamet in human subpopulations [i.e. children, elderly (< 75 years of age), renal impairment, liver disease and patients taking concomitant drugs] have been studied extensively. Only impaired renal function appears to significantly alter the elimination of this drug. Cefetamet pivoxil exerts its bactericidal action by inhibition the final transpeptidation step of peptidoglycan synthesis in the bacterial cell wall by binding to one or more of the Penicillin-binding Proteins (PBPs).

Showing 531 - 540 of 576 results