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

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Showing 201 - 210 of 525 results

Status:
US Previously Marketed
First approved in 1981

Class (Stereo):
CHEMICAL (ACHIRAL)



Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Halazepam is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Halazepam (Paxipam) is no longer commercially available in the United States. Common adverse effects are: hypotension, nausea, xerostomia, confusion, headache. Alcohol should be avoided while taking Paxipam as it causes drowsiness as well. Medications that also cause drowsiness should not be taken along with Paxipam. These include: Antidepressants, Pain relievers, Seizure medications, Muscle relaxants, Antihistamines, Sleeping pills and sedatives.
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
First approved in 1976

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Prazepam is a benzodiazepine derivative and is indicated to treat symptoms of anxiety. Benzodiazepines are used to treat severe incapacitating symptoms or symptoms leading to an extreme suffering for the patient. Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation. Prazepam is a prodrug for N-desmethyl-diazepam, which is responsible for the therapeutic effects of prazepam. Prazepam was discontinued in USA.
Status:
US Previously Marketed
First approved in 1976

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Etidocaine, marketed under the trade name Duranest, is a local anesthetic given by injection during surgical procedures and labor and delivery. Etidocaine has a long duration of activity, and the main disadvantage of using during dentistry is increased bleeding during surgery. Etidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
Status:
US Previously Marketed
First approved in 1975

Class (Stereo):
CHEMICAL (RACEMIC)



Pemoline is a central nervous system stimulant. Pemoline is structurally dissimilar to the amphetamines and methylphenidate. Pemoline is generally considered dopaminergic, but its precise method of action hasn't yet been definitively determined. The interaction of pemoline with other drugs has not been studied in humans. The following are adverse reactions in decreasing order of severity within each category associated with pemoline: hepatic dysfunction, aplastic anemia, convulsive seizures, hallucinations, insomnia, anorexia and weight loss.
Status:
US Previously Marketed
First approved in 1972

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Triclofos is primarily indicated in conditions like Insomnia, and can also be given in adjunctive therapy as an alternative drug of choice in Nausea, vertigo, labyrinthine disorders. It is also used sedate people suffering from anxiety or tension before medical investigations. Triclofos is converted to Trichloroethanol in the body .This act on brain and produces sleep. Trichloroethanol decreases time taken to fall asleep and lengthen the sleep. Triclofos is most commonly used agent for sedation in neonates as well as in older infants and children in Japan.
Enflurane (2-chloro-1,1,2,-trifluoroethyl-difluoromethyl ether) is a halogenated ether structural isomer of isoflurane. Developed by Ross Terrell in 1963, it was first used clinically in 1966. It was increasingly used for inhalational anesthesia during the 1970s and 1980s but is no longer in common use. Clinically, enflurane produces a dose-related depression of myocardial contractility with an associated decrease in myocardial oxygen consumption. Between 2% and 5% of the inhaled dose is oxidized in the liver, producing fluoride ions and difluoromethoxy-difluoroacetic acid. This is significantly higher than the metabolism of its structural isomer isoflurane. The exact mechanism of the action of general anesthetics has not been delineated. Enflurane acts as a positive allosteric modulator of the GABAA, glycine, and 5-HT3 receptors, and as a negative allosteric modulator of the AMPA, kainate, and NMDA receptors, as well as of nicotinic acetylcholine receptors.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control tryptophan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tryptophan is alpha-aminoacid that is used in the biosynthesis of proteins. It is essential aminoacid in humans, meaning the body cannot synthesize and it must be obtained from the diet. Tryptophan is a precursor of serotonin, and as such is sold over the counter in many countries as a dietary supplement for use as an antidepressant, anxiolytic and sleep aid, however application of tryptophan in these indications is not approved by FDA.
Status:
US Previously Marketed
First approved in 1970

Class (Stereo):
CHEMICAL (MIXED)



Mesoridazine (brand name Serentil) is a phenothiazine antipsychotic. It was marketed in the U.S. for the treatment of schizophrenia, behavioral problems in mental deficiency and chronic brain syndrome, alcoholism and psychoneurotic symptoms, such as anxiety and tension. Due to the risk of serious cardiac events the indicated use of Serentil was limited to severely ill schizophrenic patients who fail other therapies. Based upon animal studies, mesoridazine acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. Mesoridazine shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo.
Status:
US Previously Marketed
Source:
Repoise by Robins
(1967)
Source URL:
First approved in 1967
Source:
Repoise by Robins
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Butaperazine is an antipsychotic phenothiazine. As shown in animal studies butaperazine increases striatal and mesolimbic dopamine turnover. Butaperazine is effective in the management of schizophrenia. Extrapyramidal symptoms and drowsiness are the most common adverse effects.

Showing 201 - 210 of 525 results