Flutoprazepam

Flutoprazepam (Restas, KB-509) is a drug which is a benzodiazepine derivative. It was invented in Japan, and this is the main country in which it has been used medically. It has sedative, hypnotic, anxiolytic and anticonvulsant effects around 4 times more potent than those of diazepam, but is about the same potency as a muscle relaxant.^[1] It is however longer acting than diazepam due to producing long-acting active metabolites,^[2] which contribute significantly to its effects.^[3]

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Flutoprazepam is used for the treatment of insomnia and anxiety, and also for treating stomach ulcers.^[4]

References

1. ^ Sukamoto T, Aikawa K, Itoh K, Nose T. Psycopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509). Nippon Yakurigaku Zasshi. 1980 Sep;76(6):447-68. (Japanese).
2. ^ Ueki S, Sukamoto T, Watanabe S, Yamamoto T, Kataoka Y, Shibata S, Suwandi D, Shibata K, Takano M, Sato Y. Behavioral effects of flutoprazepam (KB-509) and its metabolites. Nippon Yakurigaku Zasshi. 1982 Jul;80(1):15-30. (Japanese).
3. ^ Barzaghi N, Leone L, Monteleone M, Tomasini G, Perucca E. Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. European Journal of Drug Metabolism and Pharmacokinetics. 1989 Oct-Dec;14(4):293-8.
4. ^ Fukuda T, Itoh K, Nose T. Antiulcerogenic action of 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one (KB-509), a new benzodiazepine derivative. Nippon Yakurigaku Zasshi. 1981 Mar;77(3):273-80. (Japanese).