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

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Showing 81 - 90 of 194 results

Status:
US Previously Marketed
Source:
TACE 25 MG ERGONOVINE by MERRELL
(1959)
Source URL:
First approved in 1959
Source:
TACE 25 MG ERGONOVINE by MERRELL
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ergonovine (also known as ergometrine) is the active water soluble component of ergot of rye. Ergonovine is being used as a maleate salt to prevent or treate postpartum haemorrhage and postabortion haemorrhage. Ergonovine stimulates alpha-adrenergic and serotonin receptors, thus activating contractions of uterine and vascular smooth muscle. Ergonovine may have depressant effect on CNS system as it binds to dopamine receptors.
Status:
US Previously Marketed
Source:
Tricofuron by Eaton
(1957)
Source URL:
First approved in 1957
Source:
Tricofuron by Eaton
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Furazolidone is a nitrofuran derivarive with broad antibacterial, antiprotazoal properties. It was used for the treatment of bacterial or protozoal enteritis and diarrhea, but now the drug is no longer prescibed in the US. The mechanism of furazolidone action is supposed to be mediated by its binding to bacterial DNA.
Status:
US Previously Marketed
First approved in 1957
Source:
Enovid by Searle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Norethynodrel is a steroidal progestin of the 19-nortestosterone group and an isomer of norethisterone. Norethynodrel is a progesteron agonist with very weak estrogenic activiry. Noretynodrel was introduced in 1957 in Enovid, a combination formulation of noretynodrel and mestranol, for the treatment of gynecological and menstrual disorders.A few years later, in May 1960, Enovid was also approved as the first oral contraceptive.
Status:
US Previously Marketed
First approved in 1956
Source:
Sterisil by Warner/Chilcott
Source URL:

Class (Stereo):
CHEMICAL (MIXED)


Hexetidine is very safe oral antiseptic with broad antibacterial and antifungal activity in vivo and in vitro. It has local-anesthetics, astringent and deodorant activity. Also, it has very strong antiplac effects. Resistention of microorganisms on hexetidine is short and transient. These characteristics give important therapeutic role in treatment of oral infections. In the UK, hexetidine is the active ingredient in the medicated mouthwash branded Oraldene. Oraldene contains 0.1 g/100 ml of hexetidine. In Germany, hexetidine is used for vaginal antisepsis.
Status:
US Previously Marketed
First approved in 1956

Class (Stereo):
CHEMICAL (ABSOLUTE)



Fluoxymesterone, sold under the brand names Halotestin and Ultandren among others, is a synthetic, orally active androgenic-anabolic steroid (AAS) and a 17α-alkylated derivative of testosterone developed by Pharmacia & Upjohn Company LLC, approved by FDA at 1956. Fluoxymesterone is used in the treatment of hypogonadism in males and breast cancer in women. Fluoxymesterone has a relatively high ratio of androgenic to anabolic activity similarly to testosterone. Like many 17α-alkylated AAS, it has a relatively low affinity for the androgen receptor (AR). However, its actions are mediated by the AR, most likely due to its relatively long elimination half-life of approximately 9.2 hours.
Nylidrin (Buphenine, Arlidin) is a beta-adrenergic agonist. Nylidrin causes peripheral vasodilation, a positive inotropic effect, and increased gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. In peripheral vascular disorders, Arlidin (nylidrin HCl) increases walking ability and promotes healing of trophic ulcers. Nylidrin hydrochloride acts predominantly by beta-receptor stimulation. Beta stimulation with nylidrin has been demonstrated in a variety of isolated tissues from rabbits, guinea pigs and dogs. It has been shown to dilate arterioles in skeletal muscle and to increase cardiac output in the anesthetized dog and cat and in unanesthetized man. An increase in cerebral blood flow and a decrease in vascular resistance has also been reported. The result of this combination of actions is a greater blood supply to ischemic tissues, with usually minimal change in blood pressure. Arlidin may be of benefit in elderly patients with mild to moderate symptoms that are commonly associated with organic mental disorders. Short-term (3 months’ duration) and long-term (12 months’ duration) clinical studies have demonstrated a modest improvement in ability to perform general activities of daily living, self-care and in a capability for social interactions. The mechanism whereby nylidrin may provide relief of selected symptoms in some elderly patients with organic brain disorders is not known.
Status:
US Previously Marketed
Source:
Neodrol by Pfizer
(1953)
Source URL:
First approved in 1953
Source:
Neodrol by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


STANOLONE, also known as dihydrotestosterone, is a potent androgenic metabolite of testosterone and anabolic agent for systemic use. It may be used as a replacement of male sex steroids in men who have androgen deficiency, for example as a result of the loss of both testes, and also the treatment of certain rare forms of aplastic anemia which are or may be responsive to anabolic androgens.
Status:
US Previously Marketed
First approved in 1953

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

The quinoline derivative diiodohydroxyquinoline (INN) or iodoquinol (USAN), one of the halogenated 8-quinolinols widely used as an intestinal antiseptic, especially as an antiamebic agent. Iodoquinol is also used topically in other infections and may cause CNS and eye damage. It was discovered by Adco Co. and introduced as diiodohydroxyquinoline. The mechanism of action is unknown. Iodoquinol acts against the trophozoites of Entamoeba histolytica. Iodoquinol produces its amebicidal effect at the site of infection, since it is poorly absorbed from the gastrointestinal tract and can reach high concentrations in the intestinal lumen.
Status:
US Previously Marketed
Source:
Vallestril by Searle
(1952)
Source URL:
First approved in 1952
Source:
Vallestril by Searle
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


METHALLENESTRIL, an allenolic acid derivative, is a synthetic nonsteroidal estrogen used to treat menstrual issues.
Status:
US Previously Marketed
First approved in 1951
Source:
Tace by Merrell (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorotrianisene (TACE®) is a powerful synthetic, non-steroidal estrogen used to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. It may also be used to prevent breast engorgement following childbirth. Chlorotrianisene (TACE®) binds to the estrogen receptor on various estrogen receptor bearing cells. Target cells include cells in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.