Flutoprazepam: Difference between revisions
Content deleted Content added
++ |
No edit summary |
||
| Line 20: | Line 20: | ||
}} |
}} |
||
'''Flutoprazepam''' (Restas, KB-509) is a drug which is a [[benzodiazepine]] derivative. It was invented in Japan in [[1972]], and its medical use remains mostly confined to that country. Its [[muscle relaxant]] properties are approximately equivalent to those of [[diazepam]] - however, it has powerful [[sedative]], [[hypnotic]], [[anxiolytic]] and [[anticonvulsant]] effects and is around four times more potent by weight compared to diazepam. <ref>Sukamoto T, Aikawa K, Itoh K, Nose T. Psychopharmacological 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).</ref> It is longer acting than diazepam due to its long-acting active metabolites,<ref>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).</ref> which contribute significantly to its effects.<ref>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.</ref> |
'''Flutoprazepam''' (Restas, KB-509) is a drug which is a [[benzodiazepine]] derivative. It was invented in [[Japan]] in [[1972]], and its medical use remains mostly confined to that country. Its [[muscle relaxant]] properties are approximately equivalent to those of [[diazepam]] - however, it has powerful [[sedative]], [[hypnotic]], [[anxiolytic]] and [[anticonvulsant]] effects and is around four times more potent by weight compared to diazepam. <ref>Sukamoto T, Aikawa K, Itoh K, Nose T. Psychopharmacological 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).</ref> It is longer acting than diazepam due to its long-acting active metabolites,<ref>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).</ref> which contribute significantly to its effects.<ref>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.</ref> |
||
Flutoprazepam is used for the treatment of [[insomnia]] and may also be used for treating [[Stomach ulcer|stomach ulcers]].<ref>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).</ref> |
Flutoprazepam is used for the treatment of [[insomnia]] and may also be used for treating [[Stomach ulcer|stomach ulcers]].<ref>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).</ref> |
||
Abuse of benzodiazepines in Japan is extremely common, with flutoprazepam being one of the most commonly abused |
Abuse of benzodiazepines in Japan is extremely common, with flutoprazepam being one of the most commonly abused, along with the benzodiazepines of abuse [[nimetazepam]] and [[temazepam]]. As of late [[2007]], the Japanese government is considering placing nimetazepam and temazepam into a more restrictive drug schedule. It is unknown as of yet whether flutoprazepam will be subject to the same controls. [[Triazolam]], [[oxazepam]], and [[nitrazepam]] are also very common benzodiazepines of abuse in Japan. {{fact}} |
||
{{sedative-stub}} |
{{sedative-stub}} |
||
Revision as of 00:01, 17 March 2008
 | |
| Clinical data | |
|---|---|
| Routes of administration | Oral, Intravenous |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 80-90% |
| Metabolism | Hepatic |
| Elimination half-life | 60-90 hours |
| Excretion | Renal |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C19H16ClFN2O |
| Molar mass | 342.795 g·mol−1 |
Flutoprazepam (Restas, KB-509) is a drug which is a benzodiazepine derivative. It was invented in Japan in 1972, and its medical use remains mostly confined to that country. Its muscle relaxant properties are approximately equivalent to those of diazepam - however, it has powerful sedative, hypnotic, anxiolytic and anticonvulsant effects and is around four times more potent by weight compared to diazepam. [1] It is longer acting than diazepam due to its long-acting active metabolites,[2] which contribute significantly to its effects.[3]
Flutoprazepam is used for the treatment of insomnia and may also be used for treating stomach ulcers.[4]
Abuse of benzodiazepines in Japan is extremely common, with flutoprazepam being one of the most commonly abused, along with the benzodiazepines of abuse nimetazepam and temazepam. As of late 2007, the Japanese government is considering placing nimetazepam and temazepam into a more restrictive drug schedule. It is unknown as of yet whether flutoprazepam will be subject to the same controls. Triazolam, oxazepam, and nitrazepam are also very common benzodiazepines of abuse in Japan. [citation needed]
 | This sedative-related article is a stub. You can help Wikipedia by expanding it. |
References
- ^ Sukamoto T, Aikawa K, Itoh K, Nose T. Psychopharmacological 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).
- ^ 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).
- ^ 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.
- ^ 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).