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

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Showing 121 - 130 of 170 results

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:
Limethason by Ammo, T.|Sakai, T.|Aizawa, T.|Fujihira, E.|Naganuma, A.
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
Source:
Canada:AMYLMETACRESOL
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 Rx (2013)
Source:
BLA125416
(2013)
Source URL:
First approved in 1958
Source:
BLA101140
Source URL:

Class:
MIXTURE

Epoprostenol (marketed as FLOLAN, VELETRI) is a prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. Epoprostenol (PGI2, PGX, prostacyclin), a metabolite of arachidonic acid, is a naturally occurring prostaglandin with potent vasodilatory activity and inhibitory activity of platelet aggregation. FLOLAN (epoprostenol sodium) for Injection is a sterile sodium salt formulated for intravenous (IV) administration. Epoprostenol has two major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. The effect of epoprostenol on heart rate in animals varies with dose. At low doses, there is vagally mediated brudycardia, but at higher doses, epoprostenol causes reflex tachycardia in response to direct vasodilation and hypotension. No major effects on cardiac conduction have been observed. Additional pharmacologic effects of epoprostenol in animals include bronchodilation, inhibition of gastric acid secretion, and decreased gastric emptying. No available chemical assay is sufficiently sensitive and specific to assess the in vivo human pharmacokinetics of epoprostenol. FLOLAN is indicated for the long-term intravenous treatment of primary pulmonary hypertension and pulmonary hypertension associated with the scleroderma spectrum of disease in NYHA Class III and Class IV patients who do not respond adequately to conventional therapy.
Status:
First approved in 1985

Class (Stereo):
CHEMICAL (ABSOLUTE)



CLOBETASOL, a derivative of prednisolone with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than fluocinonide, it is used topically in the treatment of psoriasis but may cause marked adrenocortical suppression. For short-term topical treatment of the inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp. Like other topical corticosteroids, clobetasol has anti-inflammatory, antipruritic, and vasoconstrictive properties. It is a very high potency topical corticosteroid that should not be used with occlusive dressings. Topical corticosteroids share anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of topical steroids is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Initially, however, clobetasol, like other corticosteroids, bind to the glucocorticoid receptor, which complexes, enters the cell nucleus and modifies genetic transcription (transrepression/transactivation).

Showing 121 - 130 of 170 results