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

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Showing 111 - 120 of 174 results

Norgestomet is a synthetic derivative of progesterone with improved oral activity due to its 17α-acetate side chain. In veterinary medicine norgestomet is used for the synchronisation of oestrus in cattle. It is administered as a subcutaneous ear implant (containing 3 mg norgestomet; to be removed after 9 to 10 days), in combination with a single intramuscular injection containing 3 mg norgestomet and 5 mg oestradiol valerate. The injection is to be given immediately after application of the implant. Norgestomet is not used in human medicine. It is a steroidal progestin of the 19-norprogesterone group.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Diflucortolone (used in the form of valerate prodrug) is a corticosteroid developed for the treatment of inflammatory skin diseases. It is supposed that Diflucortolone acts by inducing Annexin A1, a phospholipase A2 inhibitory protein, and thus controls the biosynthesis of prostagladins and leukotrienes. The drug is marketed as a cream under the tradename Nerisone.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Trometamol is an organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer.
Status:
Possibly Marketed Outside US
Source:
Japan:Hydrocortisone Caproate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Hydrocortisone caproate is a synthetic steroid hormone and 21-O-hexanoyl derivative of hydrocortisone. Hydroxyprogesterone caproate was previously marketed under the trade name Delalutin by Squibb, which was approved by the U.S. Food and Drug Administration (FDA) in 1956 and withdrawn from marketing in 1999. Hydrocortisone caproate acts by binding to progesterone receptors in the uterus, ovaries, breasts and in the central nervous system. These receptors exist in 2 isoforms, PR-A and PR-B. Hydrocortisone caproate binding to these receptors ultimately leads to regulation of gene transcription. This results in an anti-inflammatory effect which blunts the proinflammatory state that occurs with the initiation of labor and maintains uterine quiescence by stabilizing progesterone acting on the myometrium. Following intramuscular injection, approximately 50% of hydroxyprogesterone caproate metabolites are eliminated in the feces, while approximately 30% of metabolites are eliminated in the urine. Injection site pain is the most common adverse effect associated with hydroxyprogesterone caproate. Other commonly reported adverse effects include injection site swelling, urticaria, pruritus, injection site pruritus, nausea, injection site nodule, and diarrhea.
Status:
Possibly Marketed Outside US
Source:
Japan:Dexamethasone Palmitate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dexamethasone palmitate (a derivative of Dexamethasone), anti-inflammatory, antirheumatic, glucocorticoid receptor agonist, is reported as an ingredient of Limethason in Japan and Lipotalon in Germany. Limethason (Dexamethasone palmitate) inhibits the function of leukocytes and tissue macrophages. It restricts the migration of leukocytes in the area of inflammation. Limethason (Dexamethasone palmitate) decreases capillary permeability caused by histamine release. It inhibits the activity of fibroblasts and collagen formation. Limethason inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Limethason (Dexamethasone palmitate) is indicated for rheumatoid arthritis.
Testosterone valerate, or testosterone pentanoate, is a synthetic, steroidal androgen. It is a short-to-medium duration C17β valerate ester of testosterone, with a terminal half-life of approximately twice that of the short-acting testosterone propionate. Testosterone valerate is available exclusively as a component of the veterinary drug Deposterona developed by Syntex Animal Health Company, which is marketed in Mexico. Deposterona also contains testosterone acetate and testosterone undecanoate and is used to treat impotence, weakness, fatigue and hypogonadism in male breeding animals (cows, pigs, canines, sheep), as well as a general protein-sparing anabolic. It is administered via intramuscular injection and acts as a long-lasting prodrug of testosterone. Esterified forms of testosterone are designed to prolong the window of therapeutic effect following administration, allowing for less frequent injection schedule compared to injections of unesterified steroid. Deposterona is also used for bodybuilding purposes in men and not recommended for women performance-enhancing purposes due to its strong androgenic nature, side effects, and slow-acting characteristics (making blood levels difficult to control). Deposterona is only known to be manufactured in Mexico. Because it contains a low concentration of steroid,this product is not in high demand, and not readily diverted for illicit sale.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Bendacort is an ester of glucocorticosteroid hydrocortisone and non-steroidal anti-inflammatory drug bendazac. In vivo studies demonstrated that bendacort has a wider spectrum of anti-inflammatory effects than bendazac or hydrocortisone alone: bendacort acts on responses with a necrotic evolution where tissue damage predominates, and in cases where the reaction of tissue defense predominates, as for example in the healing of wounds. Bendacort was marketed in Italy under tradename Versacort for the treatment of sensitive steroid dermatoses, contact eczema, dyshidrosis, insect bites.
Status:
Possibly Marketed Outside US
Source:
Kanamycin, amphomycin, and hydrocortisone ointment
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)


Amphomycin is a natural antibacterial lipopeptide initially reported by researchers at Bristol-Myers in 1953 from Streptomyces canus. Lipopeptides are cyclic depsipeptides with a peptidyl side chain capped with a saturated alkyl tail. They preferentially target Gram-positive bacteria and may be useful against drug resistant strains. Amphomycin is closely related to a number of "lost" antibiotics, such as aspartocin, crystallomycin, glumamycin, friulimicin, laspartocin, tsushimycin and zaomycin. Interest in amphomycin was re-awakened with the discovery of friulimicin activity against antibiotic resistant strains. Whole cell analysis by solid-state NMR indicates that in vivo mode of action for amphomycin is complex. While the downstream effect of purine biosynthesis inhibition by amphomycin is unknown, presumably it would directly alter the overall metabolism of bacteria.
Status:
Possibly Marketed Outside US
Source:
Benylin Antiseptic Throat Lozenges by Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amylmetacresol (AMC) is an antiseptic used to treat infections of the mouth and throat. It is used as an active pharmaceutical ingredient in Strepsils, Gorpils and Lorsept throat lozenges. It was shown that the presence of amylmetacresol, dichloro-benzylalcohol and lidocaine block of inward sodium current.
mixture
Status:
US Approved OTC
Source:
21 CFR 333.110(d) first aid antibiotic:ointment neomycin sulfate
Source URL:
First approved in 1951
Source:
Mycifradin by Upjohn
Source URL:

Class:
MIXTURE



Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eye drops. In vitro tests have demonstrated that neomycin is bactericidal and acts by inhibiting the synthesis of protein in susceptible bacterial cells. It is effective primarily against gram-negative bacilli but does have some activity against gram-positive organisms. Neomycin is active in vitro against Escherichia coli and the Klebsiella-Entero. Topical uses include treatment for superficial eye infections caused by susceptible bacteria (used in combination with other anti-infective), treatment of otitis externa caused by susceptible bacteria, treatment or prevention of bacterial infections in skin lesions, and use as a continuous short-term irrigant or rinse to prevent bacteriuria and gram negative rod bacteremia in bacteriuria patients with indwelling catheters. May be used orally to treat hepatic encephalopathy, as a perioperative prophylactic agent, and as an adjunct to fluid and electrolyte replacement in the treatment of diarrhea caused to enter pathogenic E. coli (EPEC). Neomycin sulfate has been shown to be effective adjunctive therapy in hepatic coma by reduction of the ammonia forming bacteria in the intestinal tract. The subsequent reduction in blood ammonia has resulted in neurologic improvement. To reduce the development of drug-resistant bacteria and maintain the effectiveness of Neomycin Sulfate Oral Solution and other antibacterial drugs, susceptible bacteria should use Neomycin Sulfate Oral Solution only to treat or prevent infections that are proven or strongly suspected to be caused. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Neomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site near nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes

Showing 111 - 120 of 174 results