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

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Showing 1 - 10 of 31 results

Prednisolone hemisuccinate is a prodrug of a glucocorticoid agonist prednisolone, which is marketed under trade name Prednisolut in Germany and Austria. Prednisolone hemisuccinate is used in emergency medicine to treate shock due to allergic reaction, insect and snake bites, in neurology to treat brain edema and meningitis, in transplantation medicine to reduce risk of organ refection after kidney transplane, in pneumology to treat acute asthma attack, pulmonary edema, in severe or life-threatening situation in rheumatic diseases.
Status:
Investigational
Source:
INN:darbufelone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Darbufelone mesylate is a dual inhibitor of cellular prostaglandin and leukotriene production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 uM) but is much less potent with PGHS-1 (IC50= 20 uM). Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. Darbufelone mesylate was in phase III clinical trials by Pfizer and Zhuhai United Laboratories for the treatment of rheumatoid arthritis.
Status:
Investigational
Source:
NCT02194023: Phase 2 Interventional Completed Dental Plaque
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Fenamole is a muscle relaxant. It is effectively inhibits muscle spasms at good levels for a four hours and at significant levels for six hours. Clinical benefits were derived in patients with spasticity-spasm for periods up to 24 hours after a single oral dose. Fenamole is relatively free of adverse side effects particularly in the central nervous system. It is a potent copper chelator. It was once investigated as a potential antirheumatic agent in man.
Status:
US Previously Marketed
Source:
Betapar by Parke-Davis
(1970)
Source URL:
First approved in 1970
Source:
Betapar by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Meprednisone, also known as NSC-63278 and Betapar, is a glucocorticoid receptor agonist.It has anti-inflammatory and immunosuppressive activity. It was approved since 1978, but its marketing in USA was discontinied since. Meprednisone is marketed in Argentina under trade name Copytren for treatment of rheumatic diseases, diseases of collagen, dermatological, gastrointestinal, respiratory and ophtalmological diseases.
Cortisone is a hormone that is FDA approved for the treatment of primary and secondary adrenocortical deficiency, rheumatic disorders, psoriasis, exfoliative dermatitis, bronchial asthma, allergic conjunctivitis, hemolytic anemia, enteritis, tuberculosis, trichnosis. Cortisone acetate binds to the cytosolic glucocorticoid receptor. After binding the receptor, the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. Common adverse reactions include convulsions, increased intracranial pressure with papilledema, vertigo, headache, psychic disturbances, hirsuitism, glaucoma, exophthalmos. Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression. Co-administration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports. Cortisone is a natural steroid hormone. Its sulfate analog has been detected in in umbilical vein blood fetus plasma between 19 and 32 weeks of gestation with a significant increase at 29-30 weeks and in amniotic fluid. Base on the experiments with rats it was suggested that cortisone sulfate in mammals could be hydrolyzed enzymatically liberating sulfate ions from cortisone. Cortisone sulfate has been proposed for use as one of the glycosaminoglycan compound materials in a cartilage prosthesis and biological nasal bridge implant manufacture as well as auxiliary agent in powder aerosol composition for use in baby powder, dry shampoo, water-eczema remedy and antiperspirant.
Status:
Possibly Marketed Outside US
Source:
PERMALON by Hangarter, W.|Reiser
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Cupric salicylate is an anti-inflammatory agent which was used as pain relief for patients with osteoarthritis, rheumatoid and other degenerative diseases (as a copper-salicylate complex). The preparation seem to be discontinued for now.
Prednisolone hemisuccinate is a prodrug of a glucocorticoid agonist prednisolone, which is marketed under trade name Prednisolut in Germany and Austria. Prednisolone hemisuccinate is used in emergency medicine to treate shock due to allergic reaction, insect and snake bites, in neurology to treat brain edema and meningitis, in transplantation medicine to reduce risk of organ refection after kidney transplane, in pneumology to treat acute asthma attack, pulmonary edema, in severe or life-threatening situation in rheumatic diseases.
Prednisolone hemisuccinate is a prodrug of a glucocorticoid agonist prednisolone, which is marketed under trade name Prednisolut in Germany and Austria. Prednisolone hemisuccinate is used in emergency medicine to treate shock due to allergic reaction, insect and snake bites, in neurology to treat brain edema and meningitis, in transplantation medicine to reduce risk of organ refection after kidney transplane, in pneumology to treat acute asthma attack, pulmonary edema, in severe or life-threatening situation in rheumatic diseases.
Prednisolone hemisuccinate is a prodrug of a glucocorticoid agonist prednisolone, which is marketed under trade name Prednisolut in Germany and Austria. Prednisolone hemisuccinate is used in emergency medicine to treate shock due to allergic reaction, insect and snake bites, in neurology to treat brain edema and meningitis, in transplantation medicine to reduce risk of organ refection after kidney transplane, in pneumology to treat acute asthma attack, pulmonary edema, in severe or life-threatening situation in rheumatic diseases.
Prednisolone hemisuccinate is a prodrug of a glucocorticoid agonist prednisolone, which is marketed under trade name Prednisolut in Germany and Austria. Prednisolone hemisuccinate is used in emergency medicine to treate shock due to allergic reaction, insect and snake bites, in neurology to treat brain edema and meningitis, in transplantation medicine to reduce risk of organ refection after kidney transplane, in pneumology to treat acute asthma attack, pulmonary edema, in severe or life-threatening situation in rheumatic diseases.