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

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Showing 11 - 20 of 33 results

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
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.
Status:
US Previously Marketed
First approved in 1960
Source:
Striatran by Merck Sharp & Dohme
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


EMYLCAMATE (STRIATRAN®), the carbamate ester of the tertiary alcohol methylpentanol, is a tranquilizing and muscle relaxant agent used for the treatment of anxiety and tension.
Status:
First approved in 1958
Source:
Suvren by Ayerst
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

CAPTODIAME, also known as captodiamine, is a diphenylmethane derivative. It is a 5-HT2c receptor antagonist and agonist at sigma-1 and D3 dopamine receptors. It is an antihistamine which is used as a sedative and anxiolytic. CAPTODIAME is probably useful in preventing benzodiazepine withdrawal syndrome.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Adinazolam, a benzodiazepine agonist, is an effective anxiolytic agent with antidepressant properties. It was shown, that adinazolam by itself had relatively weak benzodiazepine agonist activity, and much of the pharmacological activity belonged to its active metabolite N-desmethyladinazolam (NDMAD). Adinazolam has never been FDA approved, but it is sold as a research chemical.
Status:
Possibly Marketed Outside US
Source:
Madar by Sternbach, L.H.|Reeder, E.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nordazepam (INN; marketed under brand names Nordaz, Stilny, Madar, Vegesan, and Calmday) is a 1,4-benzodiazepine derivative with amnesic, anticonvulsant, anxiolytic, muscle relaxant, and sedative properties. Nordazepam is an active metabolite of diazepam, chlordiazepoxide, clorazepate, prazepam, pinazepam, and medazepam, used primarily in the treatment of anxiety disorders. Nordazepam is a partial agonist at the GABAA receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle-relaxing effects. Nordazepam’s elimination half-life is between 36 and 200 hours, with wide variation among individuals; factors such as age and gender are known to impact it. The variation of reported half-life are attributed to differences in nordazepam metabolism and that of its metabolites as nordazepam is hydroxylated to active metabolites such as oxazepam, before finally being glucuronidated and excreted in the urine. Common side effects of nordazepam include somnolence, which is more common in elderly patients and/or people on high-dose regimens. Hypotonia, which is much less common, is also associated with high doses and/or old age.
Medazepam is a benzodiazepine drug with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. Marketed in Russia. Indicated for the treatment of neurotic disorders and states, accompanied with sense of fear, anxiety, intension, raised irritability, insomnia, vegetative lability.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzoctamine (Tacitin), a psychotropic drug, known to exert in man an anti-anxiety effect. Its action also was studied when given as a hypnotic or sedative in patients with respiratory failure. Benzoctamine decreases 5-HT turnover in the brain and this action may play a role in the anti-anxiety effect of the drug.
Status:
Possibly Marketed Outside US
Source:
NEUROVAL
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clotiazepam is a compound of the benzodiazepine class. The drug was developed in Japan and approved for the treatment of insomnia, anxiety and before anesthesia. Clotiazepam was marketed worlwide under different names, however, currently it is available only in South America under the name Neuroval and presumably in Japan. Clotiazepam exerts its action by binding and activating GABA-A receptors.

Showing 11 - 20 of 33 results