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

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Showing 301 - 310 of 657 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Adimolol is an antihypertensive agent with a potent antagonist of central beta-adrenoceptors and has a weaker alpha 1-adrenolytic action. The central alpha 2-antagonistic effect is either very weak or absent. The reduction in beta-adrenoceptor number following adimolol suggests that this prolonged effect may not be solely due to competitive antagonism but may additionally depend upon non-competitive antagonism at beta-adrenoceptors. Adimolol reduced supine, standing and exercise heart rates in a dose dependent manner.
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.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Temocillin sodium
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Temocillin was marketed by Beecham Pharmaceuticals in the UK in the 1980s but achieved little commercial success and was withdrawn, though it remained available via the manufacturer’s medical department. Presently licensed to Eumedica, temocillin is being re-launched in the UK and Belgium for treating UTI, sepsis, and respiratory infections by ESBL (Extended-spectrum beta-lactamases) and AmpC-producing Enterobacteriaceae. It acts by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls. It irreversibly binds to the active site of specific transpeptidases and carboxypeptidases known as Penicillin Binding Proteins (PBP), preventing peptidoglycan production.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefalonium is a 1st generation cephalosporin with a broad spectrum of actvity against Gram-positive and Gram-negative bacterias. The drug inhibits the bacterial cell wall synthesis by binding to penicillin binding proteins. Cefalonium is approved for routine dry cow therapy to treat existing sub-clinical infections and to prevent new infections which occur during the dry period.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metampicillin is the approved name for the penicillin resulting from the reaction of ampicillin with formaldehyde. Metampicillin is hydrolysed in aqueous solution with the formation of ampicillin. Metampicillin has broad spectrum of activity coupled with a marked degree of stability to bacterial penicillinase. Furthermore, metampicillin is reported to be absorbed to a greater extent than ampicillin, resulting in superior blood levels in human subjects, and also giving high levels of antibiotic in bile following parenteral administration. Metampicillin showed a spectrum and level of activity similar to that of ampicillin in vitro, and both compounds were inactive against penicillinase-producing strains of bacteria. The activity of metampicillin was markedly reduced by human serum, and the compound was less active than ampicillin in the presence of human serum. Following the oral administration of metampicillin to man, metampicillin was not detected in the blood stream nor in urine, and ampicillin alone was demonstrated in these subjects. The serum concentrations of ampicillin that were produced following the oral administration of metampicillin were somewhat lower than those obtained with equivalent doses of ampicillin. Adminstration of metampicillin by the intramuscular (i.m.) route to volunteers resulted in the appearance of both ampicillin and metampicillin in the blood, and of ampicillin alone in the urine of these subjects. When parenteraly administered, metampicillin appeared to be a particularly suitable penicillin for the treatment of biliary tract infections. Metampicillin is a cell wall biosynthesis inhibitor.
Status:
Possibly Marketed Outside US
Source:
Japan:Bunitrolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bunitrolol is a beta-adrenergic antagonist that can be used for treatment of coronary heart disease. It improves cardiac performance after beta-blockade in patients with coronary artery disease. Bunitrolol was found to have a greater beta 1 than beta 2 adrenergic activity and a weak alpha 1 blocking action.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Bornaprolol is norbornyl derivative. It is the beta-adrenoceptor blocking agent. The prolonged beta-blocking action of bornaprolol was related to a tight irreversible binding to beta-receptors rather than to pharmacokinetic properties of this drug. In vitro, bornaprolol inhibits isoproterenol-induced stimulation of adenylate cyclase in rat heart homogenate. A dose-related inhibition of the rise in heart rate and blood pressure on sub-maximal exercise 2 h after single doses of bornaprolol. Bornaprolol eliminated mainly by metabolism with a bioavailability that decreases inversely with oral dose. Bornaprolol has a more prolonged action and may prove to be of therapeutic value in situations, such as angina and certain arrhythmias, where sustained high degrees of beta-adrenergic receptor blockade are beneficial. Bornaprolol behaved in man as a non-cardioselective drug.
Status:
Possibly Marketed Outside US
Source:
Japan:Oxyfedrine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.
Status:
Possibly Marketed Outside US
Source:
Japan:Arotinolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It is used in the treatment of high blood pressure and essential tremor. The recommended dosage is 10–30 mg per day.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefminox Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefminox is a broad-spectrum, bactericidal cephalosporin antibiotic. It is especially effective against Gram-negative and anaerobic bacteria. It is indicated in treatment of the following infections caused by sensitive bacteria: 1. Respiratory infections: Amygdalitis, circumtonsillar abscess, bronchitis, bronchiolitis, bronchiectasis (in fection), secondary infections of chronic respiratory diseases, pneumonia, and pulmonary suppuration; 2. Infection in urinary system: Nephropyelitis, cystitis; 3. Infections in abdominal cavity: Cholecystitis' angiocholitis'peritonitis; 4. Infections in pelvic cavity: Pelvic peritonitis, adnexitis, intrauterine infection, inflammation in pelvic dead space, and parametritis; 5. Septicaemia.

Showing 301 - 310 of 657 results