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

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Showing 151 - 160 of 244 results

Midecamycin (Acetate) is a macrolide antibiotic with actions and uses similar to those of erythromycin but somewhat less active. It is synthesized from Streptomyces mycarofaciens. It has been given by mouth to treat variety of bacterial infections like respiratory tract, ear, skin infections etc. Antibiotics require constant drug level in body for therapeutic effect. This is achieved by taking the drug at regular interval of time throughout the day and night as prescribed. Midecamycin (Acetate) is primarily indicated in conditions like Bronchitis, Laryngopharyngitis, Otitis media, Periodontitis, Pneumonia, Respiratory tract infections, Skin infections, Subcutaneous abscess, Tonsillitis. Midecamycin inhibits bacterial growth by targeting the 50S ribosomal subunit preventing peptide bond formation and translocation during protein synthesis. Resistance to midecamycin is commonly attributed to mutations in 50S rRNA preventing midecamycin binding allowing the cell to synthesize proteins free of error.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (EPIMERIC)

Clometocillin, one of the forms of penicillin, was active against pen-I or pen-R pneumococci and was used in children. The modern information about its application is not available.
Status:
Possibly Marketed Outside US
Source:
HABEKACIN by Kondo, S.et al.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Arbekacin is a broad-spectrum aminoglycoside used to treat methicillin-resistant Staphylococcus aureus (MRSA). Arbekacin has antibacterial activities against high-level gentamicin-resistant Enterococci, multidrug-resistant Pseudomonas aeruginosa, and Acinetobacter baumannii et al. In a cell-free system, habekacin (arbekacin) interfered with polypeptide synthesis, caused codon misreading, and inhibited translocation of N-acetylphenylalanyl-tRNA from the acceptor site to the donor site on ribosomes. Arbekacin bound to both 50S and 30S ribosomal subunits. Arbekacin has been approved as an injectable formulation in Japan since 1990, under the trade name Habekacin, for the treatment of patients with pneumonia and sepsis caused by MRSA. Meiji Seika Pharma is developing an inhaled aerosol formulation of arbekacin for the treatment of hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia. Nobelpharma is developing an intravenous formulation of arbekacin sulfate, known as nonsense readthrough compound or NPC 14, for the treatment of Duchenne muscular dystrophy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefodizime is a third-generation cephalosporin with a broad spectrum of antibacterial activity. Administered intravenously or intramuscularly 1 to 4 g of cefodizime daily for an average of 7 to 10 days produces a clinical cure in 80 to 100% of patients (adults, elderly or children) with upper or lower respiratory tract infections or urinary tract infections. In comparative trials cefodizime was as effective as other third generation cephalosporins. A single dose of cefodizime (1 or 2 g) is also useful in treating lower urinary tract infections. Urogenital gonorrhoea, whether caused by beta-lactamase producing or non-beta-lactamase producing Neisseria gonorrhoeae, is very effectively treated by single dose therapy with intramuscular cefodizime. Preliminary data from a small number of patients indicates that cefodizime may also be useful in the treatment of otitis media, sinusitis and gynaecological infections, and for the prophylaxis or treatment of surgical infections. The clinical efficacy of cefodizime compared to other third generation cephalosporins is superior to that predicted from in vitro results. This superior activity of cefodizime may be related to the relatively long elimination half-life of the drug or its ability to modify some functions of the immune system--a potentially important finding awaiting further investigation. Cefodizime is well tolerated and has a tolerability profile similar to other members of its class with systemic adverse events being primarily gastrointestinal or dermatological. Cefodizime may be more convenient to administer than some other agents of its class as it may be given once or twice daily. While there are no trials comparing cefodizime to other third generation cephalosporins in immunosuppressed populations, preliminary information indicates cefodizime may be useful in this group. Cefodizime targets penicillin-binding proteins (PBPs) 1A/B, 2, and 3 resulting in the eventual death of the bacterial cell. In vivo experimental models of infection showed that bacterial clearance by this drug is at least as effective compared with other 3rd generation cephalosporins. It has a similar adverse effect profile to other 3rd generation cephalosporins which is mainly being limited to gastrointestinal or dermatological side effects. It is not currently approved by the FDA for use in the United States.
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:
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

Class (Stereo):
CHEMICAL (ACHIRAL)

Nifurtoinol, a nitrofuran-derivative, is an antibacterial drug. Nifurtoinol (Urfadyn PL) is used for the treatment of urinary tract infections. Nifurtoinol-associated hepatic injury cases were reported in Netherlands.
Status:
Possibly Marketed Outside US
Source:
Carbenin by Daiichi Sankyo
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Panipenem is a parenteral carbapenem antibacterial agent with a broad spectrum of in vitro activity covering a wide range of Gram-negative and Gram-positive aerobic and anaerobic bacteria, including Streptococcus pneumoniae and species producing β-lactamases. Panipenem is coadministered with betamipron (Carbenin, Daiichi Sankyo Company) to inhibit panipenem uptake into the renal tubule and prevent nephrotoxicity. In large, randomised clinical trials, panipenem/betamipron demonstrated good clinical and bacteriological efficacy (similar to that of imipenem/cilastatin) in adults with respiratory tract or urinary tract infections.
Status:
Possibly Marketed Outside US
Source:
Ibaflin by 3M Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ibafloxacin is a fluoroquinolone antibiotic drug used in veterinary medicine. Ibafloxacin, a fluorinated 4-quinolone, is a broad spectrum antibiotic with bactericidal action against Gram-positive and Gram-negative bacteria. Ibafloxacin is presented in the form of a tablet/oral gel containing a racemic mixture of S- and R-ibafloxacin. The antimicrobial activity of the racemate originates mainly from the S-enantiomer. Ibafloxacin was marketed under the brand name Ibaflin. Ibaflin tablets were intended for use in dogs for treatment of respiratory tract infections, urinary tract infections and dermal infections caused by ibafloxacin susceptible pathogens. Ibafloxacin, is an antibiotic belonging to the class ‘fluoroquinolones’. It works by blocking an enzyme called ‘DNA gyrase’, which is important in allowing bacteria to make copies of their DNA. This enzyme is only found in bacterial cells, and does not have a similar function in animal cells. By blocking DNA gyrase, ibafloxacin prevents the bacteria from making DNA and stops them making proteins and growing, resulting in their death.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (EPIMERIC)



The phthalidyl thiazolidine carboxylic ester of ampicillin, talampicillin (Talpen, Beecham), has been introduced recently to improve absorption and to reduce these side effects. After oral administration talampicillin is rapidly absorbed and hydrolysed by tissue esterases in the intestinal wall to release into the circulation ampicillin and the ester moiety, mainly 2-hydroxymethyl-benzoic acid. No unchanged talampicillin is detectable in the peripheral blood. It is not approved by the FDA for use in the United States

Showing 151 - 160 of 244 results