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

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Showing 131 - 140 of 172 results

Status:
Possibly Marketed Outside US
Source:
Majeptil Tab 10mg by Erfa Canada 2012 Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Thioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma.
Zotepine is a potent antipsychotic and antidepressive drug, which was developed in Japan and used in many countries for the treatment of schizophrenia. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity.The drug is still available in Asia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Pinazepam, a benzodiazepine derivative, differs from other drugs of its class by the presence of an unsaturated bond, the propargyl group, at the N-1 position. In animals, pinazepam controls anxiety and aggressiveness and exerts anticonvulsant activity. In clinical trials with open or controlled design, pinazepam, compared with diazepam, showed significant and purely anxiolytic action in patients suffering from anxiety with or without somatic manifestations, particularly in gastrointestinal disorders. Even though it is not a specific hypnotic drug, it seems to help patients in whom the physiological course of the sleep is disturbed. Pinazepam is used in the treatment of anxiety and insomnia associated with anxiety.
Status:
Possibly Marketed Outside US
Source:
Japan:Sultopride Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Sultopride (trade names Barnetil, Barnotil, Topral) is an atypical antipsychotic of the benzamide chemical class used in Europe, Japan, and Hong Kong for the treatment of schizophrenia. It was launched by Sanofi-Aventis in 1976. Sultopride acts as a selective D2 and D3 receptor antagonist. It has also been shown to have clinically relevant affinity for the GHB receptor as well, a property it shares in common with amisulpride and sulpiride.
Chloral hydrate was discovered in 1832, and was used as a sedative in late 19th century. Chloral hydrate has not been approved by the FDA or the EMA, and is on the list of unapproved drugs that are prescribed for postoperative pain control, sedation and to prevent alcohol withdrawal and reduce anxiety associated with withdrawal of opiates or barbiturates. Mechanism of action of chloral hydrate is not known. It is generally believed that the central depressant effects are due to the principal pharmacologically active metabolite trichloroethanol, which has a plasma half- life of 8 to 10 hours, and acts by potentiating GABA-activated Cl currents.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Lormetazepam
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Lormetazepam (or methyl-lorazepam), possesses hypnotic, anxiolytic, sedative and skeletal muscle relaxant properties. Lormetazepam is not approved for sale in the United States or Canada, though it is licensed in the Netherlands as 1 and 2 mg tablets, under the brand names Loramet and Noctamid and as generic, available from several different manufacturers. Lormetazepam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or falling asleep. Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the omega 1 receptor which is responsible for sedation. Changes in electroencephalography can therefore be used to measure the sedative sleep promoting properties of lormetazepam.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

KETAZOLAM, a benzodiazepine with an additional d-face-fused heterocyclic ring, possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used for the treatment of anxiety and spasticity.
Status:
Possibly Marketed Outside US
Source:
Canada:DIPHENHYDRAMINE HYDROCHLORIDE
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Bromisoval (INN; aka bromvalerylurea) is a hypnotic and sedative compound of the bromoureide group discovered by Knoll in 1907 and patented in 1909. It is marketed over the counter in Asia under various trade names (such as Brovarin) usually in combination with non-steroidal anti-inflammatory drugs. Chronic use of bromisoval has been associated with bromine poisoning. Bromovisal can be prepared by bromination of isovaleric acid by the Hell-Volhard-Zelinsky reaction followed by reaction with urea. Bromvalerylurea (BU) can suppress expression of many kinds of pro- and anti-inflammatory mediators in LPS- or interferon-γ activated alveolar and peritoneal macrophages. Bromisoval was found to ameliorate sepsis in rats. It also prevents elevated serum-IL-6 level as well as IL-6 mRNA expression in septic rats. Bromisoval was also found useful for inflammatory skin disorders. The compound is able to suppress the TLR ligands-induced proinflammatory response similar to the steroid DEX without the side effects often associated with the steroid usage.
Status:
Possibly Marketed Outside US
Source:
Japan:Brotizolam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short-term treatment of severe or debilitating insomnia and in a dose of 0.25 mg can be used as a premedication prior to surgery, this dose was found to be comparable in efficacy to 2 mg flunitrazepam as a premedicant prior to surgery. The drug was developed by a team led by T Nishiyama while working for Takeda Chemical Industries in 1976 in Japan. Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Spain, Belgium, Luxembourg, Austria, Portugal, Israel, Italy, Taiwan and Japan. Insomnia. Brotizolam is prescribed for the short-term treatment, 2–4 weeks only of severe or debilitating insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Brotizolam inhibits the hypothalamus and cerebral limbic system controlling emotion through GABA, a typical inhibitory transmitter of central nervous system. As a result, unnecessary stimulation from the autonomic nervous system and other sites is blocked, demonstrating central nervous action including hypnosis, sedation and anti-anxiety
Status:
Possibly Marketed Outside US
Source:
Neuleptil by Erfa Canada 2012 Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Periciazine (INN), also known as pericyazine (BAN) or Propericiazine, is a drug that belongs to the phenothiazine class of typical antipsychotics. Pericyazine is not approved for sale in the United States. It is commonly sold in Canada and Russia under the tradename Neuleptil and in the United Kingdom and Australia under the tradename Neulactil. The primary uses of pericyazine include the short-term treatment of severe anxiety or tension and in the maintenance treatment of psychotic disorders such as schizophrenia. There is insufficient evidence to determine whether periciazine is more or less effective than other antipsychotics. Pericyazine is a rather sedating and anticholinergic antipsychotic, and despite being classed with the typical antipsychotics, its risk of extrapyramidal side effects is comparatively low. It has a relatively high risk of causing hyperprolactinemia and a moderate risk of causing weight gain and orthostatic hypotension.

Showing 131 - 140 of 172 results