Flutemazepam, initially first synthesized in 1965, but wasn't further developed and described until a team at Stabilimenti Chimici Farmaceutici Riuniti SpA in the mid 1970s. It is the fluorinated analogue of

temazepam Temazepam (sold under the brand names Restoril among others) is a medication of the benzodiazepine class which is generally used to treat severe or debilitating insomnia. It is taken by mouth. Temazepam is rapidly absorbed, and significant hyp ...

that has powerful hypnotic, sedative,

amnesiac Amnesia is a deficit in memory caused by brain damage or disease,Gazzaniga, M., Ivry, R., & Mangun, G. (2009) Cognitive Neuroscience: The biology of the mind. New York: W.W. Norton & Company. but it can also be caused temporarily by the use o ...

anxiolytic An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...

, anticonvulsant and

skeletal muscle relaxant A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeu ...

properties. It is most closely related in structure to

, being the fluoro instead of chloro analogue. As a result, flutemazepam has been shown to have similar pharmacological properties to temazepam and nimetazepam. It has been found to be effective for the treatment of the most severe states of anxiety,

panic attack Panic attacks are sudden periods of intense fear and discomfort that may include palpitations, sweating, chest pain or chest discomfort, shortness of breath, trembling, dizziness, numbness, confusion, or a feeling of impending doom or of losing ...

s, and severe insomnia. Furthermore, it is highly potent with 1 mg of flutemazepam being equivalent to 10 mg of diazepam. Flutemazepam is highly effective for acute psychotic states, especially stimulant psychosis, violent behaviour, and aggression. It was first synthesized and described in 1965 by Leo Sternbach. In a test which compared a series of 3-fluorobenzodiazepine compounds in 1976, one of which was the 3-hydroxy benzodiazepine, flutemazepam. Of the tested compounds (9 different 3-fluorobenzodiazepines including, a powerful compound known as ''N-Desalkyl-3-hydroxyflurazepam''). Flutemazepam was the most potent: 20x more potent than temazepam, 10x more potent than diazepam and nitrazepam, 5x more potent than nimetazepam and roughly equipotent to a related 3-hydroxy benzodiazepine,

lorazepam Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication. It is used to treat anxiety disorders, trouble sleeping, severe agitation, active seizures including status epilepticus, alcohol withdrawal, and c ...

. It was also the most rapid-acting compound of the series via oral administration, as well as the most active and powerful anxiolytic, myorelaxant, tranquilizer, motor-impairing, amnesic, sedative-hypnotic, and anti-convulsive agent at doses as low as 0.5-1 mg range.

References

{{GABAAR PAMs Benzodiazepines Chloroarenes Fluoroarenes Lactams Lactims GABAA receptor positive allosteric modulators Hydroxyketones

See also

References