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部分中文Grandaxin处方资料（仅供参考）
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【中文品名】托非索泮

【药效类别】抗抑郁药，抗焦虑药

【通用药名】TOFISOPAM

【别　　名】EGYT-341, Grandaxin, Grandaxine, Mer-19, Mer-1961, Seriel, Tavor

【化学名称】 (RS)-1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine

【CA登记号】[22345-47-7]

【分 子 式】C22H26N2O4

【分 子 量】382.45

【收录药典】JP14

【开发单位】Servier

【首次上市】1974年，匈牙利

Grandaxin (tofisopam)
Grandaxin relieves various symptoms caused by tension imbalances between the sympathetic and parasympathetic nervous systems. It has proved effective in treating a variety of stress-induced ailments.

Tofisopam, an anti-anxiety agent first approved over 25 years ago and currently marketed in more than 15 countries, has a benign safety profile and a broad spectrum of clinical activity, including effects on anxiety, depression, autonomic dysfunction, IBS, and perimenopausal symptoms. In addition, tofisopam, a racemic 2,3-benzodiazepine comprised of R- and S-enantiomers, is unlike traditional 1,4-benzodiazepines, as it appears to be nonsedating, with minimal abuse liability and minimal cognitive impairment.

Clinical Observations
Although tofisopam is a clinically effective anxiolytic agent with a chemical structure similar to that of the typical benzodiazepines, its binding profile is clearly distinct from that of any known 1,4- or 1,5-benzodiazepine receptor agonist.

In addition, unlike typical benzodiazepines, tofisopam was inactive in a conventional animal model of anxiety, the elevated plus-maze test. However, the drug was active in the water-immersion stress test. This activity, consistent with an anxiolytic effect, suggests a mechanism of action that may involve stress pathways. These data indicate tofisopam has a unique preclinical neurochemical and behavioral profile, one that is clearly distinct from that of typical benzodiazepines.

Tofisopam does not bind in the CNS and neither to the 1,4-benzodiazepine, nor to the GABA receptors, but it enhances the binding of benzodiazepines and muscimol to their binding sites. Tofisopam has also mixed dopamine agonist and antagonist like properties

Any drug capable of blocking dopamine receptors is capable of inducing parkinson's and other dysfunctions. Even minute quantities of such a drug can easily damage you for life. But I'm sure the someone here will get the picture once they try it.

Grandaxin as a drug has been reported in 4 cases. Age-wise distribution is available below and gender-wise distribution of Grandaxin as a drug is available below.
 
Indications
Grandaxin is used in following indications/medical conditions : Neck Pain,Occipital Neuralgia,Vertigo,.

Side effects
The following side effects are associated with Grandaxin.
Cholelithiasis Gamma-Glutamyltransferase Pyrexia
Rash Generalised Liver Disorder Oedema
Cholelithotomy Hepatic Function Abnormal Lymphocyte Stimulation Te
Mucosal Inflammation Stomatitis

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2011年4月20日更新