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

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Showing 1331 - 1340 of 4002 results

Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAO) of the hydrazine class. It was originally developed for the treatment of Tuberculosis, but in 1952, its antidepressant properties were discovered when researchers noted that patients given isoniazid became inappropriately happy. Iproniazid is no longer clinically prescribed and has been withdrawn due to incidences of hepatotoxicity.
Status:
US Previously Marketed
Source:
MERATRAN 1MG by MERRELL
(1961)
Source URL:
First approved in 1955
Source:
Meratran by Merrell (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Pipradrol (Meratran) is a psychoactive agent and a central nervous system stimulant useful in the field of psychiatry. In vitro study has shown that pipradrol inhibits the reuptake of and stimulates the release of dopamine and norepinephrine. In these pharmacodynamic actions it is less potent than d-amphetamine. It was shown that pipradrol conditioned place preference (CPP) was blocked by selective D1 dopamine antagonist SCH23390 suggesting that a rewarding effect of pipradrol establishment of a CPP may involve activation of D1 dopamine receptors. Pipradrol was initially used as an adjunct in the dietary management of obesity as well as for the treatment of dementia. There have been a number of reports on the properties of pipradrol showing its favorable effects in the treatment of depression and fatigue status as well as a variety of other conditions including narcolepsy, spasmodic torticollis, schizophrenia and in geriatric practice. Pipradrol has a definite cerebral stimulating effect without affecting the blood pressure or respiration and has been used to counteract post-anasthetic and chlorpromazine depression in man. Structurally related to -phenylmethylamphetamine, a potent stimulant with a long half-life, pipradrol differs from amphetamine in that its action is more intense at higher centres, it lacks pressor activity, there is no post-excitement depression, and it does not depress the desire for food as occurs with amphetamine. The drug however is enhancing the existing pathologic behavior such as exacerbating pre-existing anxiety and is considered the drug of abuse. Meratran has certain indications and contraindications. Indications are schizophrenics without delusions having restriction of interest and activity and with depressant features, psycho-motor retardation and/or blocking of communication, long-term hospitalized schizophrenics with severe deterioration while contraindications are patients with delusions, anxiety, disturbed patients with cerebral arteriosclerosis. Pipradrol was made illegal in many countries in 1970s due to its abuse potential. It is classified under the Misuse of Drugs Act as a Class C substance. The combination of pipradrol with multivitamins and minerals marketed as Alertonic Elixir is used as adjunctive therapy in combating fatigue resulting from emotional or nutritional causes.
Status:
US Previously Marketed
First approved in 1955

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Methyprylon (brand name Noludar) is a sedative agent, which used to treat insomnia. But then the drug was replaced in the market by another drugs with less side effects. The precise mechanism of action is not known, but was made suggestion, that methyprylon increases the effects of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the brain.
Status:
US Previously Marketed
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
(1955)
Source URL:
First approved in 1955
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


DEXTROAMPHETAMINE TANNATE is a salt of dextroamphetamine, amphetamine enantiomer. It is used as CNS stimulant in the treatment of attention deficit hyperactivity disorder.
Status:
US Previously Marketed
Source:
Frenquel by Merrell (MerrellNational)
(1955)
Source URL:
First approved in 1955
Source:
Frenquel by Merrell (MerrellNational)
Source URL:

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
Source:
Medomin by Geigy
(1955)
Source URL:
First approved in 1954
Source:
Heptabarbital by Ciba-Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

HEPTABARBITAL is an intermediate or short term barbiturate. It binds to the GABAA receptor at either the alpha or the beta subunit. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. HEPTABARBITAL was formerly used as a sedative and hypnotic drug.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



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.
Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
Source:
Fluoromar by Ohio Medical Products
(1961)
Source URL:
First approved in 1954
Source:
FLUOROMAR by OHIO CHEM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

FLUROXENE (Fluoromar®) is a colorless, volatile liquid, which was used as an inhalational anesthetic.
Status:
US Previously Marketed
First approved in 1953

Class (Stereo):
CHEMICAL (RACEMIC)



CYCRIMINE is an antispasmodic drug used for the treatment of Parkinson's disease (PD). It binds the muscarinic acetylcholine receptor M1, effectively reducing levels of acetylcholine. This decrease in acetylcholine restores the normal dopamine-acetylcholine balance and relieves the symptoms of PD.

Showing 1331 - 1340 of 4002 results