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

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Showing 41 - 50 of 118 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Imolamine is a coronary vasodilator, which is used in the treatment of angina pectoris and as a local anesthetic. Imolamine has been shown to produce in animals coronary vasodilation, local anaesthesia, analgesia and a papaverine like action in duodenal preparations. Imolamine increased the tone of uterus and ileum and this was accompanied by a reduction in amplitude of contraction. The response of the stomach tissue to imolamine was similar to that of butalamine and aminophylline, i.e. a relaxant action on smooth muscle. Imolamine has a variable action on tone, producing an increase in ileum and uterus and a decrease in stomach. Imolamine is able to cause severe cytolytic hepatitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefteram Pivoxil
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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Glyconiazide is an antibacterial drug with high antitubercular activity in vitro as well as in vivo. The drug was reported to cause sensitive polyneuritis upon administration.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluazacort is a synthetic glucocorticoid. It was marketed under tradename Azacortid for the treatment of eczema and psoriasis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Xibornol [6-(isoborn-2-yl)-3,4 xylenol] is a highly lipophilic and poorly soluble drug used as spray mouthwash for the local treatment of infection and inflammation of the throat and in the dental care, due to both its bacteriostatic activity, mainly against Gram positive micro-organisms and its antiviral properties. The drug concentration required for the therapeutic activity is 3% (w/v). Its poor water solubility makes difficult to set up drug formulations based on aqueous solvents, so xibornol is at present commercially available only as spray aqueous suspension. The self-microemulsifying approach was found to be effective to formulate stable and pharmaceutically acceptable liquid spray formulations of xibornol. The minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of xibornol against 100 strains of Staphylococcus aureus, clinically isolated have been evaluated in range between 2 ug/ml and 8 ug/ml. In the patients treated with xibornol (500 mg every 8 h for 7 days) any modification in phagocytosis frequency (PMF), phagocytosis index (PHI), nitroblue tetrazolium (NBT), reduction frequency (NRF), microbicidal activity and neutrophil mobility of PML, before, during and after the end of therapy wasn’t found.
S-Adenosylmethionine (often referred to as SAMe) is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. SAM is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma (HCC), HepG2 cells and colon cancer cells. Because of structural instability, stable salt forms of SAM are required for its use as an oral drug. The commonly used salts: tosylate, butanedisulfonate, disulfate tosylate, disulfate ditosylate, and disulfate monotosylate. SAMe has been marketed in some European countries since the mid-1980s for the treatment of depression and for other medical conditions such as osteoarthritis (joint disease that causes joint pain and stiffness), fibromyalgia (widespread pain and stiffness). In addition, it is used to treat liver disease and migraine headaches. However, it is not formally approved in the UK for the treatment of depression, and in the USA, it is classified only as a dietary supplement. Some research suggests that it is more effective than placebo in treating mild-to-moderate depression and is just as effective as antidepressant medications without the side effects (headaches, sleeplessness, and sexual dysfunction). In addition, antidepressants tend to take 6 to 8 weeks to begin working, while It seems to begin more quickly. Researchers are not sure how SAMe works to relieve depression. But they speculate it might increase the amount of serotonin in the brain just as some antidepressants do. Many studies have examined injectable forms of SAMe, not oral supplements.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxolamine under brand names Symphocal, Perebron is used in some countries as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Oxolamine possesses anti-inflammatory activity, which causes a reduction in the irritation of the nervous receptors of the respiratory tract.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Ornipressin (ornithine-8-vasopressin, POR-8), is a synthetic vasopressin analogue. Ornipressin produces vasoconstriction via vasopressin V1A receptor-mediated vascular smooth muscle cell contraction. Ornipressin is used to control bleeding in surgical practice. It was introduced in 1971, and approved for use in Germany, Switzerland, New Zealand and Australia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.
Status:
Possibly Marketed Outside US
Source:
Japan:Melinamide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Melinamide is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Melinamide caused a decrease of the enhanced intestinal ACAT activity in diabetic rats, but did not affect intestinal cholesterol esterase activity. Marked improvement of hypercholesterolaemia in cholesterol-fed diabetic rats occurred concomitantly with the drug treatment. These results suggest that intestinal ACAT activity is closely related to the serum cholesterol level in diabetic rats, and show that melinamide lowers intestinal ACAT activity. Melinamide (Artes®) was the only marketed (in Japan) ACAT inhibitor. 04 Aug 2004 was withdrawn for Hypercholesterolaemia in Japan.