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

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Showing 1 - 10 of 33 results

Omega-hydroxyemodin a naturally occurring anthraquinone derivative isolated from Polygoni cuspidati radix. It has anti-bacterial and phytoestrogen activity. Omega-hydroxyemodin demonstrated topoisomerases I and II inhibition activity. Omega-hydroxyemodin significantly attenuated the DNA binding of activator protein (AP)-1 that regulates COX-2 expression through the reduction of the phosphorylation of c-Jun. Moreover, inhibition of PGD2 generation by Omega-hydroxyemodin was accompanied by a decrease in phosphorylation of cytosolic phospholipase A2α. Taken together, these data suggest that Omega-hydroxyemodin represents a potential therapeutic approach for the treatment of inflammatory diseases. Omega-hydroxyemodin was efficacious in a mouse model of S. aureus skin and soft tissue infections.
Cefmetazole is a semisynthetic cephamycin antibiotic. It has a broad spectrum of activity comparable to that of the second-generation cephalosporins, covering gram-positive, gram-negative, and anaerobic bacteria. Its bactericidal action results from inhibition of cell wall synthesis. It effectively treats abdominal and respiratory tract infections, pelvic inflammatory disease, urinary tract infections, skin and soft tissue infections and used for surgical prophylaxis, reducing or eliminating signs and symptoms of infection. Cefmetazole has a low frequency of adverse effects, and a side effect profile similar to that of other cephamycins. Adverse effects following overdosage have included nausea, vomiting, epigastric distress, diarrhea, and convulsions.
Ticarcillin (also known as Ticar) is a semisynthetic antibiotic with a broad spectrum of bactericidal activity against many gram-positive and gram-negative aerobic and anaerobic bacteria. Ticarcillin is not absorbed orally; therefore, it must be given intravenously or intramuscularly. Ticarcillin's antibiotic properties arise from its ability to prevent cross-linking of peptidoglycan during cell wall synthesis when the bacteria tries to divide, causing death. Usage of ticar was discontinued.
Cloxacillin is a derivative of penicillin for the treatment of broad spectrum of bacterial infections. The drug exerts its action by inhiiting bacterial beta-lactamase (penicillin-binding proteins).
Cephalothin is a first generation, semisynthetic analogue of natural cephalosporin antibiotic. The in-vitro bactericidal action of Cephalothin results from inhibition of cell-wall synthesis. In general, Cephalothin has higher activity against Gram positive than Gram negative organisms. Cephalothin is primarily indicated in conditions like bone and joint infection, genitourinary tract infections, respiratory tract infections, soft tissue and skin infections and others. The severe or irreversible adverse effects of Cephalothin, which give rise to further complications, include nephrotoxicity, hemolytic anemia. Cephalothin produces potentially life-threatening effects, which include anaphylaxis, serum sickness syndrome. The symptomatic adverse reactions produced by Cephalothin are: rashes, urticaria, allergic reactions, thrombophlebitis, pain at injection site. Co-administration of diuretics, such as furanthril, ethacrynic acid and nephrotoxic antibiotics may increase the risk of renal damage. Reciprocal inactivation could be observed during in vitro mixing of Cephalothin with aminoglycosides.
Status:
US Previously Marketed
Source:
Syncillin by Bristol
(1959)
Source URL:
First approved in 1959
Source:
Syncillin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Pheneticillin (phenoxyethylpenicillin) is an oral penicillin used for the treatment of upper respiratory tract infections; lower respiratory tract infections; skin and soft tissue infections. Pheneticillin inhibits the synthesis of the cell wall by inhibiting the penicillin binding proteins (PBPs) function. It is well absorbed from the gastrointestinal tract. It reaches the pleural and peritoneal cavities but doesn’t cross the blood-brain barrier. Diarrhea has sometimes occurred with therapeutic doses in man.
Orbifloxacin (brand name Orbax) is a fluoroquinolone antibiotic which is approved for use in dogs and cats, abd marketed by Schering-Plough Animal Health. Orbifloxacin is a synthetic broad-spectrum antibacterial agent from the class of fluoroquinolone carboxylic acid derivatives. Orbifloxacin is the international nonproprietary name for 1-cyclopropyl-5,6,8-trifluoro-1,4-dihydro-7-(cis-3,5-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid. ORBAX® Oral Suspension is a malt flavored antibiotic suspension containing 30 mg/mL of orbifloxacin and sorbic acid as a preservative. ORBAX® Oral Suspension is indicated for the treatment of urinary tract infections (cystitis) and also for skin and soft tissue infections (wounds and abscesses). Orbifloxacin is bactericidal against a wide range of gram-negative and gram-positive organisms and exerts its antibacterial effect through interference with the bacterial enzyme DNA gyrase which is needed for the maintenance and synthesis of bacterial DNA.
Status:
Possibly Marketed Outside US
Source:
NCT01876628: Phase 4 Interventional Completed Cellulitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flucloxacillin is an isoxazolyl penicillin of the β-lactam group of antibiotics, which exerts a bactericidal effect upon many Gram-positive organisms including β-lactamase-producing staphylococci and streptococci. While no longer used in the United States, Flucloxacillin is supplied under a variety of trade names in other countries, including Floxapen, Flopen, Staphylex. Floxapen is indicated for the treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; other infections caused by floxapen-sensitive organisms, like example, osteomyelitis, urinary tract infection, septicaemia, endocarditis. Floxapen is also indicated for use as a prophylactic agent during major surgical procedures when appropriate; for example cardiothoracic and orthopaedic surgery. Flucloxacillin, by its action on the synthesis of the bacterial wall, exerts a bactericidal effect on streptococci except those of group D (Enterococcus faecalis) staphylococci. It is not active against methicillin-resistant staphylococci. There is evidence that the risk of flucloxacillin induced liver injury is increased in subjects carrying the HLA-B*5701 allele. Despite this strong association, only 1 in 500-1000 carriers will develop liver injury. Consequently, the positive predictive value of testing the HLA-B*5701 allele for liver injury is very low (0.12%) and routine screening for this allele is not recommended. Flucloxacillin diffuses well into most tissue. Specifically, active concentrations of flucloxacillin have been recovered in bones: 11.6 mg/L (compact bone) and 15.6 mg/L (spongy bone), with a mean serum level of 8.9 mg/L. Flucloxacillin diffuses in only small proportion into the cerebrospinal fluid of subjects whose meninges are not inflamed. It is also excreted in small quantities in mother's milk. In normal subjects approximately 10% of the flucloxacillin administered is metabolised to penicilloic acid. The elimination half-life of flucloxacillin is in the order of 53 minutes.
Status:
Possibly Marketed Outside US
Source:
Targocid by Gruppo Lepetit
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



TEICOPLANIN A2-5 is a component of a teicoplanin complex antibiotic, which consist of six closely related glycopeptide subcomponents. TEICOPLANIN A2-5 being the most lipophilic in protein binding. Bacteria treated with the drug failed to incorporate GlcNAc, a peptidoglycan precursor, whereas they continued to synthesize DNA, RNA, and protein. The cell wall inhibition was accompanied by an accumulation of UDP-MurNAc-pentapeptide, thus indicating that the antibiotic interferes with the polymerization of the peptidoglycan but not with the synthesis of soluble precursors. Teicoplanin is indicated in adults and in children from birth for the parenteral treatment of the following infections: complicated skin and soft tissue infections; bone and joint infections; complicated urinary tract infections; infective endocarditis; bacteraemia that occurs in association with any of the indications listed above. The following side-effects may occur: nausea, vomiting, diarrhea and stomach pain, skin rash and pruritus, bronchospasm, renal impairment. Teicoplanin should be administrated with caution in patients receiving concurrent nephrotoxic or ototoxic drugs, such as aminoglycosides, amphotericin B, cyclosporine and frusemide.
Teicoplanin A2-3 is a major component of the teicoplanin complex, a glycopeptide antibiotic produced by A. teichomyceticus that is broadly effective against Gram-positive bacteria in vitro. Bacteria treated with the drug failed to incorporate GlcNAc, a peptidoglycan precursor, whereas they continued to synthesize DNA, RNA, and protein. The cell wall inhibition was accompanied by an accumulation of UDP-MurNAc-pentapeptide, thus indicating that the antibiotic interferes with the polymerization of the peptidoglycan but not with the synthesis of soluble precursors. Teicoplanin is indicated in adults and in children from birth for the parenteral treatment of the following infections: complicated skin and soft tissue infections; bone and joint infections; complicated urinary tract infections; infective endocarditis; bacteremia that occurs in association with any of the indications listed above. The following side-effects may occur -- nausea, vomiting, diarrhea and stomach pain, skin rash and pruritus, bronchospasm, renal impairment. Teicoplanin should be administrated with caution in patients receiving concurrent nephrotoxic or ototoxic drugs, such as aminoglycosides, amphotericin B, cyclosporine, and frusemide.