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Status:
US Previously Marketed
Source:
ARLIDIN NYLIDRIN HYDROCHLORIDE by USV
(1961)
Source URL:
First approved in 1955
Class (Stereo):
CHEMICAL (MIXED)
Targets:
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:
TERGEMIST SODIUM ETHASULFATE by ABBOTT
(1955)
Source URL:
First approved in 1955
Source:
TERGEMIST SODIUM ETHASULFATE by ABBOTT
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Sodium ethasulfate is a clear, colorless, viscous, and nonflammable liquid that belongs to the sodium sulfate chemical group. Sodium ethasulfate is usually stable; however, it is incompatible with strong oxidizing agents. Due to its unique solubility and penetrating action, it is widely used in various end-user industries such as textile, chemical production, pharmaceuticals, agrochemicals, metal working, and food processing. Sodium ethasulfate is used as wetting agent in the textile industry. The product is used along with calcium hypochlorite as a bleaching agent. The product is used as mercerizing agent for cotton processing in the chemical industry. Sodium ethasulfate is employed as intermediate in anoinic surfactants that are used for dishwashing detergents. It is also used as surfactant in lye washing and peeling process. In the pharmaceutical industry, it is used to enhance the bactericidal properties of generic antiseptics that are more acidic. It is also employed as surfactant in penicillin production for breaking undesired reaction conditions.
Status:
US Previously Marketed
Source:
POVAN by PARKE DAVIS
(1959)
Source URL:
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
First approved in 1955
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
HYDROXYDIONE is a neuroactive steroid used formerly as a general anesthetic. It was discontinued due to a high incidence of post-anesthetic thrombophlebitis, delayed onset of anesthesia and an unacceptably long duration of action.
Status:
US Previously Marketed
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Azacyclonol (aka gamma-pipradrol) is an ataractive agent; a compound which diminished hallucinations in psychotic individuals. It is sometimes referred to as a tranquilizer or antipsychotic, though it does not actually possess these properties. It was used in Europe during the 1950's for treatment of schizophrenia; likely to reduce the psychedelic effects of LSD and mescaline. However, it had mixed clinical effectiveness and did not gain widespread adoption and was eventually discontinued. Azacyclonol was sold under several trade names: Ataractan, Calmeran, Frenoton, Frenquel and Psychosan.
Status:
US Previously Marketed
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Hexafluorenium inhibits the enzyme cholinesterase in the plasms, but apparently not at the neuromuscular juntion. It also has some nondepolarizing activity (tubocurarine-like) at the postjunctional membrane. In man hexafluorenium potentiates the muscle relaxant effects of succinylcholine. As such, smaller doses of succinylcholine are required and fewer side effects like fasciculations, twitching and postoperative muscle pain are experienced.
Status:
US Previously Marketed
Source:
POVAN by PARKE DAVIS
(1959)
Source URL:
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
US Previously Marketed
Source:
POVAN by PARKE DAVIS
(1959)
Source URL:
First approved in 1955
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
US Previously Marketed
Source:
PATHILON by LEDERLE
(1982)
Source URL:
First approved in 1954
Source:
PATHILON by LEDERLE
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Tridihexethyl is a synthetic anticholinergic agent which was marketed under the brand name Pathilon as an adjunct in the treatment of peptic ulcer disease. However, it is no longer available in the US market. Tridihexethyl may block all three types of muscarinic receptors including M-1 receptors in the CNS and ganglia, M-2 receptors in the heart, and M-3 receptors. The muscarinic acetylcholine receptors mediate various cellular responses including inhibition of adenylate cyclase, the breakdown of phosphoinositides, and modulation of potassium channels through the action of G proteins. Tridihexethyl inhibits vagally mediated reflexes by antagonizing the action of acetylcholine. This, in turn, reduces the secretion of gastric acids in the stomach. Tridihexethyl was also examined for effect on patients with acquired nystagmus where four out of six patients showed improvement, but due to the profile usage of Tridihexethyl to treat nystagmus was limited.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954
Source:
SERPASIL by NOVARTIS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.