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

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Showing 51 - 60 of 172 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
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 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.
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.
Status:
US Previously Marketed
First approved in 1966

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomepromazine (also known as methotrimeprazine) is a phenothiazine neuroleptic drug. It is sold in many countries under the generic name (levomepromazine) or under brand names such as Nozinan, Detenler and many more. Levomepromazine is an antipsychotic drug is commonly used as an antiemetic to alleviate nausea and vomiting in palliative care settings particularly in terminal illness. Levomepromazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. Levomepromazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, it can block 5HT2 receptors and some others, like histamine, serotonin.
Status:
US Previously Marketed
Source:
Beta-Chlor by Mead Johnson
(1963)
Source URL:
First approved in 1963
Source:
Beta-Chlor by Mead Johnson
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

CHLORAL BETAINE, a chemical complex of chloral hydrate and betaine, is a nonbarbiturate sedative and hypnotic. It is indicated for sleep induction, preoperative sedation, and daytime sedation. CHLORAL BETAINE is converted to chloral hydrate in the body and its action on the central nervous system is identical with that of chloral hydrate.
Chlorprothixene (Taractan, Tarasan, Truxal) is a thioxanthine derivative developed by Lundbeck for the treatment of psychotic disorders. The drug exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor.
Status:
US Previously Marketed
Source:
Trepidone by Lederle
(1961)
Source URL:
First approved in 1961

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Mephenoxalone is an oxazolidinone compound. It is a skeletal muscle relaxant as well as anxiolytic. Mephenoxalone is indicated for the treatment of muscle spasms.
Status:
US Previously Marketed
Source:
Capla by Wallace
(1961)
Source URL:
First approved in 1961
Source:
Capla by Wallace
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Mebutamate (Capla, Dormate) is a biscarbamate drug that has anxiolytic, sedative, and antihypertensive effects. It is marketed under many trade names, including Capla and Dormate. Its preparation was reported in a 1959 US patent to Carter Products. It is less well known that mebutamate is also hypnotic. In a 1967 study, L. Tetreault, P. Richer, and J. M. Bordeleau in Montreal found that, at a dose of 600 mg, mebutamate has hypnotic properties that “affect the duration and quality of sleep induction, and the duration and quality of sleep, without disturbing the state of the subject upon awakening and during the morning.” A higher dose (900 mg) did not change the overall effect, which was “consistently between that of secobarbital at 200 mg and 100 mg.” The authors did not observe any significant side effects. Mebutamate is one of many GABAergic drugs which act via allosteric agonism of the GABAA receptor at the β-subreceptor similar to barbiturates. In contrast, benzodiazepines act at the α-subreceptor. As such, carbamates and barbiturates, possess analgesic properties which the benzodiazepine class of drugs does not.