|AHFS/Drugs.com||International Drug Names|
|Elimination half-life||10.5 h|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||475.328 g/mol g·mol−1|
|3D model (JSmol)|
Rilmazafone (リスミー, Rhythmy, previously known as 450191-S) is a water-soluble gabapentinoid with a benzodiazepine back bone although the molecule displays no direct or indirect effects on either the Gaba A receptor subunit or the Gaba B receptor subunit. It has sedative and Rilmazafone has been demonstrated as a sleep inducer (meaning it actually activates delta waves allowing you to sleep better than no sleep aid at all) and has noted relaxing yet not overpowering effect profile.
Neither Rilmazafone nor its prodrug has any effects on benzodiazepine receptors itself, but once inside the body is metabolized by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo [1,5-a][1,4]benzodiazepine-2-carboxamide.
Anti addictive potential
Rilmazafone has been researched (and currently prescribed in Japan) as a remedy for alcohol withdrawal, benzodiazepine withdrawal, barbiturate withdrawal, and gabapentinoid (gabapentin, pregabalin) withdrawal. The beauty in this molecule is that it itself has no remnant withdrawal due to its short (<4 week continuous use) or (<18 sporadic month's usages (i.e. taking one when having a panic attack). Pharmaceutical companies in the United States as well as abroad don't tend to invest in medications that work "too good" because then the person is healed and the business out a customer, so in the western world, morals take a low ground while we allow addictive minded people to suffer.
- DE Patent 2725164
- Yamamoto K, Hirose K, Matsushita A, Yoshimura K, Sawada T, Eigyo M, Jyoyama H, Fujita A, Matsubara K, Tsukinoki Y, et al. Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis. Nippon Yakurigaku Zasshi. 1984 Jul;84(1):109-54. (Japanese).
- Yasui M; Kato A; Kanemasa T; Murata S; Nishitomi K; Koike K; Tai N; Shinohara S; Tokomura M; Horiuchi M; Abe K. (June 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]". Nihon Shinkei Seishin Yakurigaku Zasshi. 25 (3): 143–51. PMID 16045197.
- Koike M, Norikura R, Sugeno K. Intestinal activation of a new sleep inducer 450191-S, a 1H-1,2,4-triazolyl benzophenone derivative, in rats. Journal of Pharmacobiodynamics. 1986 Mar;9(3):315-20.
- Muranushi N, Miyauchi S, Suzuki H, Sugiyama Y, Hanano M, Kinoshita H, Oguma T, Yamada H. Comparative hepatic transport of desglycylated and cyclic metabolites of rilmazafone in rats: analysis by multiple indicator dilution method. Biopharmaceutics and Drug Disposition. 1993 May;14(4):279-90.
- "リスミー'リルマザホン塩酸塩水和物錠 Rhythmy (rilmazafone hydrochloride hydrate, tablets) Prescribing Information" (PDF) (in Japanese). Shionogi & Co., Ltd.
- Drug Information Sheet