Fosazepam

Drugbox
IUPAC_name = 7-chloro-1-(dimethylphosphorylmethyl)-5-phenyl-3H-1,4-benzodiazepin-2-one

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CAS_number=35322-07-7
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PubChem=37114
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C=18 | H=18 | Cl=1 | N=2 | O=2 | P=1
molecular_weight = 360.774
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Fosazepam is a drug which is a benzodiazepine derivative. It has sedative and anxiolytic effects, [Allen S, Oswald I. Anxiety and sleep after fosazepam. "British Journal of Clinical Pharmacology". 1976 Feb;3(1):165-8.] and is a derivative of diazepam which has been substituted with a dimethylphosphoryl group to improve solubility in water. [Nicholson AN, Wright CM. Activity of fosazepam, a soluble analogue of diazepam. "British Journal of Clinical Pharmacology". 1977 Aug;4(4):494-6.]

Fosazepam is of relatively low potency compared to other benzodiazepine derivatives, with a 100mg dose of fosazepam equivalent to 10mg of nitrazepam. [Risberg AM, Henricsson S, Ingvar DH. Evaulation of the effect of fosazepam (a new benzodiazepine), nitrazepam and placebo on sleep patterns in normal subjects. "European Journal of Clinical Pharmacology". 1977 Oct 14;12(2):105-9.] Fosazepam has similar effects to nitrazepam, but with a shorter duration of action and less tendency to cause rebound insomnia. [Viukari M, Linnoila M, Aalto U. Efficacy and side effects of flurazepam, fosazepam, and nitrazepam as sleeping aids in psychogeriatric patients. "Acta Psychiatrica Scandinavica". 1978 Jan;57(1):27-35.] However fosazepam does produce the long-acting active metabolite nordazepam which might cause extended sedative effects at high doses or with prolonged use, and may produce residual sedation upon awakening. [Breimer DD, Jochemsen R, von Albert HH. Pharmacokinetics of benzodiazepines. Short-acting versus long-acting. "Arzneimittelforschung". 1980;30(5a):875-81.]

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