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

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Showing 801 - 810 of 1722 results

Status:
US Previously Marketed
First approved in 1991

Class (Stereo):
CHEMICAL (ABSOLUTE)



Didanosine was developed by Bristol-Myers Squibb in collaboration with the NIH for the treatment of HIV-1 infections. Upon administration the drug is metabolized to the active metabolite which inhibits HIV-1 reverse transcriptase both by competing with deoxyadenosine 5'-triphosphate and by its incorporation into viral DNA. Didanosine was approved by FDA under the name Videx (among the other names).
Status:
US Previously Marketed
Source:
Synarel by Syntex
(1990)
Source URL:
First approved in 1990
Source:
Synarel by Syntex
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levamisole (the trade name Ergamisol), an anthelminthic drug with immunological properties. It also has antitumor activity when administered with 5-fluorouracil in patients with Duke's C colorectal carcinoma; however, this use was discontinued. The mechanism of the antitumor effect is unknown but has been postulated to be related to levamisole's immunomodulatory properties. Levamisole can stimulate antibody formation to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis, chemotaxis and increases motility, adherence, and chemotaxis. Levamisole inhibits alkaline phosphatase and possesses cholinergic activity. The mechanism of action of levamisole as an antiparasitic agent, for example, to treat ascariasis, relates to its agonistic activity to L-subtype nicotinic acetylcholine receptors in nematode muscles. In addition, levamisole was studied for preventing relapses of the steroid-sensitive idiopathic nephrotic syndrome (SSINS). It was shown, that alone or in combination with steroids, the drug can prolong the time to relapse and prevented recurrence during one year of treatment. However, these studies also were also discontinued.
Status:
US Previously Marketed
First approved in 1985

Class (Stereo):
CHEMICAL (RACEMIC)



Nabilone is a synthetic cannabinoid approved under the brand name cesamet for treatment of severe nausea and vomiting associated with cancer chemotherapy. Nabilone is an orally active which, like other cannabinoids, has complex effects on the central nervous system (CNS). It has been suggested that the antiemetic effect of nabilone is caused by interaction with the cannabinoid receptor system, i.e. the CB (1) receptor, which has been discovered in neural tissues.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(22)(iv) antifungal:scalp or nails camphorated metacresol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Metacresol (m-cresol or 3-methylphenol) is colorless, yellowish liquid. It is used as a bactericide for control of crown gall and olive knot on certain fruit and nut trees and ornamentals and the genetic/physiological disorder burr knot on apples. Currently, one product is registered which contains both m-cresol and xylenol. Used as disinfectant/bacteriocide/germicide for animal pathogenic bacteria (G- and G+ vegetative) in households, sickrooms, hospitals, veterinary clinics, and veterinary hospitals; on surgical instruments, diagnostic instruments/equipment and on hospital critical rubber/plastic items. Used as an insecticide and miticide on dogs for treatment of lice and fleas. It is also used for making synthetic resins; in photographic developers, explosives. Additionally, m-cresol is chemical intermediate for thymol used in cough/cold medicinals, synthetic pyrethroid insecticides, 3-methyl-6-t-butylphenol, trinitro-m-cresol for explosives, and phenolic resins; disinfectant ingredient; ore flotation agent; solvent. m-Cresol, either pure or mixed with p-cresol, is important in the production of contact herbicides. m-Cresol is also a precursor to the pyrethroid insecticides. Furthermore, many flavor and fragrance compounds, such as (-)-methanol and musk ambrette, are derived from m-cresol. Several important antioxidants including synthetic vitamin E are produced from m-cresol. m-cresol is used as a topical dental antiseptic. m-cresol is an effective antimicrobial preservative and is used at low levels (0.3%) in multi-dose peptide and protein formulations. m-cresol has been shown to cause protein aggregation.
Status:
US Previously Marketed
Source:
MAPROTILINE HYDROCHLORIDE by WATSON LABS
(1988)
Source URL:
First approved in 1980

Class (Stereo):
CHEMICAL (ACHIRAL)



Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TCAs in that it does not appear to block serotonin reuptake. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder (depressive neurosis) and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression. The mechanism of action of maprotiline is not precisely known. It does not act primarily by stimulation of the central nervous system and is not a monoamine oxidase inhibitor. The postulated mechanism of maprotiline is that it acts primarily by potentiation of central adrenergic synapses by blocking reuptake of norepinephrine at nerve endings. This pharmacologic action is thought to be responsible for the drug’s antidepressant and anxiolytic effects. The mean time to peak is 12 hours. The half-life of elimination averages 51 hours.
Status:
US Previously Marketed
Source:
21 CFR 310.532(a) benign prostatic hypertrophy alanine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Alanine is a non-essential aminoacid encoded by GCU, GCC, GCA, and GCG codons. Besides being a building block of proteins, alanine plays a key role in glucose-alanine cycle. Alanine is medically used as a dietary supplement for conditions such as fructose intolerance, muscle atrophy, low birth weight.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control valine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Valine is an α-amino acid that is used in the biosynthesis of proteins. It is essential in humans, meaning the body cannot synthesize it and thus it must be obtained from the diet. There is a mixed scientivic evidence that as a dietary supplement valine improves training efficacy, delays central fatigue.
Denatonium, usually available as denatonium benzoate (trade names Bitrex) is the most bitter chemical compound known, with bitterness thresholds of 0.05 ppm for the benzoate and 0.01 ppm for the saccharide. Scientists at Macfarlan Smith, Ltd. of Edinburgh, Scotland discovered Bitrex during research on derivatives of the anesthetic lidocaine. The extremely bitter taste proved effective in reducing ingestion by humans and animals. Denatonium is commonly included in placebo medications used in clinical trials to match the bitter taste of certain medications. Denatonium activates bitter taste receptor, mainly, TAS2R4, TAS2R8, TAS2R10, TAS2R13 on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ABSOLUTE)



Paramethasone acetate (a derivative of paramethasone) is a glucocorticoid with the general properties of corticosteroids. It has been used by mouth in the treatment of all conditions in which corticosteroid therapy is indicated except adrenal-deficiency states for which its lack of sodium-retaining properties makes it less suitable than hydrocortisone with supplementary fludrocortisone.