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

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Showing 161 - 170 of 244 results

Ribostamycin sulfate is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete. It is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit (some work by binding to the 50S subunit), inhibiting the translocation of the peptidyl-tRNA from the A-site to the P-site and also causing misreading of mRNA, leaving the bacterium unable to synthesize proteins vital to its growth. Ribostamycin is usually used to treat sepsis, superficial skin infection, deep skin infection, lymphangitis/lymphadenitis, chronic pyoderma, osteomyelitis, pharyngitis/laryngitis, tonsillitis, acute bronchitis, pneumonia, pulmonary abscess, pyothorax, secondary infection in chronic respiratory lesions, cystitis, pyelonephritis, gonococcal infection, peritonitis, cholecystitis, dacryocystitis, keratitis (including corneal ulcer), otitis media, sinusitis and gnathitis. The most commonly reported adverse reactions include renal dysfunction, liver disorder and rash.
Propicillin (Baycillin Mega) is this semisynthetic penicillin, analogous to penicillin V, was introduced in the early 1960s. Although it is better absorbed from the gastrointestinal tract, overall it is inferior to phenoxymethylpenicillin and phenoxyethylpenicillin because of its lower antibacterial activity. Propicillin is used by propicillin-susceptible pathogens in adults and adolescents from 14 years to treat mild to moderate bacterial infections. These include skin infections, ear, nose and throat infections (such as otitis media, sinusitis, tonsillitis, pharyngitis) and infections of the bronchi andlung inflammation. Moreover propicillin can for prevention and treatment of scarlet fever or against rheumatic fever are used (bacterial infection of the nose and throat). Even with tooth or jaw surgery the drug is used to treat an endocarditis endocarditis prevent. Its mechanism of action could be due to binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, thus propicillin may inhibit the third and last stage of bacterial cell wall synthesis
Status:
Possibly Marketed Outside US
Source:
Apravet by Aventis Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Apramycin is a broad-spectrum aminocyclitol antibiotic produced by a strain of Streptomyces tenebrarius. It has a bactericidal action against many gram-negative bacteria. Apramycin is a structurally unique antibiotic that contains a bicyclic sugar moiety and a monosubstituted deoxystreptamine. It is not approved for use in humans. Apramycin is registered for use in more than twenty countries in cattle, pigs and chickens. The drug exerts its antibacterial effect by inhibiting protein synthesis at the level of peptidyl translocation. It is mostly used for treating gastrointestinal infections. Apramycin is available in soluble powder and feed premix formulations.
Carumonam is a monobactam antibacterial agent. It was highly active in vitro against members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae and weakly active against Streptococcus pneumoniae, but it was not active against Staphylococcus aureus. The excellent activity of carumonam against Gram-negative bacteria is related to its high affinity for their penicillin-binding proteins. It is indicated for the treatment of urinary tract infections, chronic respiratory infections, biliary tract infections, peritonitis, sepsis. Another factor that contributes to the excellent activity of carumonam against Gram-negative bacteria is its resistance to beta-lactamases. Adverse effects of the carumonam were limited to phlebitis at the intravenous infusion site; bloody diarrhea.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Clomocycline is the approved name of a methylol derivative of chlortetracycline. Clomocycline is a tetracycline antibiotic that is commonly prescribed by medical doctors for infections and to treat acne. It may also be used to treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia. Clomocycline is also used commonly as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria and is also prescribed for the treatment of Lyme disease. Clomocycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Clomocycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. This drug has been reported to be noticeably free of side-effects such as nausea, vomiting, and diarrhea.
Cefquinome is a 4th generation cephalosporin which is active against a broad spectrum of Gram positive and Gram negative bacteria. As many cephalosporin it acts by binding to bacterial PBP and thus inhibiting the cell wall synthesis. Cefquinome is approved for veterinary use in cattles with respiratory tract infections, skin infections, bacterial mastitis and septicaemia.
Status:
Possibly Marketed Outside US
Source:
NCT00280514: Phase 4 Interventional Completed Abscess
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefpirome is a semisynthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity. Cefpirome 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. Cefpirome is an injectable extended-spectrum or 'fourth generation' cephalosporin. Its antibacterial activity encompasses many of the pathogens involved in hospital-acquired infections such as Enterobacteriaceae, methicillin-susceptible Staphylococcus aureus, coagulase-negative staphylococci and viridans group streptococci. Cefpirome also has in vitro activity against Streptococcus pneumoniae regardless of penicillin susceptibility. It is stable against most plasmid- and chromosome-mediated beta-lactamases, with the exception of the extended-spectrum plasmid-mediated SHV enzymes. Intravenous cefpirome 2g twice daily has shown clinical efficacy comparable to that of ceftazidime 2g 3 times daily in the treatment of hospitalised patients with moderate to severe infections. Clinical response and bacteriological eradication rates were similar in patients with severe pneumonia or septicaemia treated with either cefpirome or ceftazidime. Cefpirome appeared more effective than ceftazidime in the eradication of bacteria in patients with febrile neutropenia in 1 study; however, clinical response rates were similar in the 2 treatment groups. The tolerability of cefpirome appears similar to that of ceftazidime and other third generation cephalosporins, diarrhoea being the most frequently observed event. Thus, cefpirome is likely to be a valuable extended-spectrum agent for the treatment of severe infections. Cefpirome offers improved coverage against some Gram-positive pathogens and Enterobacteriaceae producing class I beta-lactamases compared with the third generation cephalosporins, although this has yet to be demonstrated in clinical trials.
Status:
Possibly Marketed Outside US
Source:
Japan:Piromidic Acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Piromidic acid, a quinolone antibiotic has an inhibitory effect against hepatic stages of P. falciparum and P. yoelii yoelii, and has a potential for treatment or prevention of malaria through their unique antiparasitic effect against erythrocytic and hepatic stages of Plasmodium.
Status:
Possibly Marketed Outside US
Source:
DIBEKACIN MEIJI by Umezawa, H. et al.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dibekacin is a semisynthetic aminoglycoside antibiotic useful in the treatment of severe gram-negative bacterial infections. The drug is marketed in Japan.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Rufloxacin (MF-934) is a fluoroquinolone antibacterial drug. It acts as a DNA gyrase inhibitor. Rufloxacin shows in vitro antibacterial activity against E. coli, Salmonella, Klebsiella, Proteus and Staphylococcus spp. Lower in vitro activity was observed with Pseudomonas, Serratia, Enterobacter and the streptococci group D. Rufloxacin is indicated for the treatment of lower respiratory tract and urinary tract infections caused by germs sensitive to rufloxacin.

Showing 161 - 170 of 244 results