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Search results for "ATC|NERVOUS SYSTEM|PSYCHOLEPTICS|ANXIOLYTICS|Benzodiazepine derivatives" in comments (approximate match)
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Bentazepam (also known as Thiadipone, Tiadipona) is a benzodiazepine analog, used as a short-action anxiolytic. Bentazepam a thienodiazepine with the same main mechanism of action as the classic 1,4-benzodiazepines, is a short-action anxiolytic, with an elimination-half-life of 3 to 5 hours in healthy volunteers. Bentazepam possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. A severe benzodiazepine overdose with bentazepam may result in coma and respiratory failure. Adverse effects include dry mouth, somnolence, asthenia, dyspepsia, constipation, nausea and drug-induced lymphocytic colitis has been associated with bentazepam. Severe liver damage and hepatitis has also been associated with bentazepam. Whilst liver failure from bentazepam is considered to be rare, liver function monitoring has been recommended for all patients taking bentazepam.
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.
Status:
Possibly Marketed Outside US
Source:
Nobrium by Hoffman-La Roche
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
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)
Conditions:
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.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine derivative that is marketed in several European countries as the anxiolytic drug. Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with the highest affinity to PDE-4A1 followed by PDE-10A1, PDE-3, and PDE-2A3. Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines, it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin). Tofisopam is not approved for sale in the United States or Canada. However, Vela Pharmaceuticals of New Jersey is developing the D-enantiomer (dextofisopam) as a treatment for irritable bowel syndrome, with moderate efficacy demonstrated in clinical trials so far.
Status:
Possibly Marketed Outside US
Source:
Limpidon
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Changes in sleep with camazepam were minimal. However, non-anxious subjects reported being more relaxed the next day. Camazepam may cause skin disorders.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.
Status:
Possibly Marketed Outside US
Source:
DEPAS by Yoshitomi Pharmaceutical Industries
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Etizolam is an analogue of benzodiazepine that contains thienotriazolodiazepine group. The drug was developed and approved in Japan and now is used in Japan, Italy and India for the treatment of anxiety disorders. Etizolam exerts its action through activation of GABA A receptors, moreover, the agonistic behavior was shown on isolated neurons. There are several cases when etizolam dependence was reported. In many countries the drug is recognized as a psychoactive substance and its distribution is illegal there.
Status:
Possibly Marketed Outside US
Source:
NCT01574313: Phase 4 Interventional Completed Vertigo
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fludiazepam is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s. Fludiazepam is marketed in Japan and Taiwan under the brand name Erispan. Fludiazepam exerts its pharmacological properties via enhancement of GABAergic inhibition. Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam. Fludiazepam possesses anxiolytic, anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Cloxazolam is an agonist of GABA-A receptor that was developed in Japan for the treatment of anxiety-disorders. The drug was marketed in Europe under the names Sepazon, Olcadil, Akton and Lubalix.