関: rilmazafone hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/18 13:09:25」(JST)

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Rilmazafone^[1] (リスミー, Rhythmy, previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan.^[2] It has sedative and hypnotic effects.^[3]^[4] Rilmazafone induces impairment of motor function and has hypnotic properties.^[5]

Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised 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.^[6]^[7]

Rilmazafone active metabolite

References

^ 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).
^ Yamamoto K, Matsushita A, Sawada T, Naito Y, Yoshimura K, Takesue H, Utsumi S, Kawasaki K, Hirono S, Koshida H, et al. Pharmacology of a new sleep inducer, 1H-1,2,4-triazolyl benzophenone derivative, 450191-S (II). Sleep-inducing activity and effect on the motor system. Nippon Yakurigaku Zasshi. 1984 Jul;84(1):25-89. (Japanese).
^ Ibii N, Horiuchi M, Yamamoto K. Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III). Behavioral study on interactions of 450191-S and other drugs in mice. Nippon Yakurigaku Zasshi. 1984 Aug;84(2):155-73. (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.

External links

(Japanese) "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). Shionogi & Co., Ltd.

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English Journal

Induced next-day somnolence in an elderly patient taking suvorexant concomitantly with diltiazem.

Shihyakugari A, Hori S, Miki A, Sawada Y.
International journal of clinical pharmacology and therapeutics.Int J Clin Pharmacol Ther.2016 Aug;54(8):645-8. doi: 10.5414/CP202624.
OBJECTIVE: To present the first case of induced next-day somnolence in a patient taking suvorexant concomitantly with diltiazem.CASE SUMMARY: The patient was an 88-year-old female who had suffered from insomnia and anorexia, for which a psychiatric clinic had prescribed 1.5 mg/day aripiprazole and 1
PMID 27191770

Pressure ulcers induced by drug administration: A new concept and report of four cases in elderly patients.

Mizokami F1, Takahashi Y2, Hasegawa K3, Hattori H4, Nishihara K5, Endo H6, Furuta K1, Isogai Z3.
The Journal of dermatology.J Dermatol.2016 Apr;43(4):436-8. doi: 10.1111/1346-8138.13093. Epub 2015 Sep 14.
Drug-induced akinesia is a potential cause of pressure ulcers. However, pressure ulcers that are caused by drug-induced akinesia are not considered an adverse drug reaction (ADR). We propose that drug-induced pressure ulcers (DIPU) are pressure ulcers that are caused by an external force that is exp
PMID 26364579

Residual effects of zolpidem, triazolam, rilmazafone and placebo in healthy elderly subjects: a randomized double-blind study.

Uemura SI1, Kanbayashi T2, Wakasa M3, Satake M3, Ito W4, Shimizu K4, Shioya T3, Shimizu T2, Nishino S5.
Sleep medicine.Sleep Med.2015 Nov;16(11):1395-402. doi: 10.1016/j.sleep.2015.05.021. Epub 2015 Jul 9.
With current hypnotic agents, next-day residual effects are a common problem. The purpose of the present study was to evaluate the residual effects of the commercially available hypnotics - zolpidem, triazolam, and rilmazafone - on the physical and cognitive functions of healthy elderly people in th
PMID 26498242

Japanese Journal

THE EFFECTS OF TRIAZOLAM AND RILMAZAFONE ON THE PHYSICAL AND COGNITIVE FUNCTIONS IN HEALTHY ELDERLY PERSONS

秋田医学 38(2), 63-69, 2011-12
NAID 110008752362

向精神薬と転倒·転落の関係に関する研究

医療薬学 37(1), 49-55, 2011
NAID 130004502652

Hypnotic and Sleep Quality-Enhancing Properties of Kavain in Sleep-Disturbed Rats

Journal of pharmacological sciences 111(3), 293-298, 2009-11-20
NAID 10026154277

「リルマザホン」

Rilmazafone
Systematic (IUPAC) name
	1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide
Clinical data
Trade names	Rhythmy
AHFS/Drugs.com	International Drug Names
Legal status	℞-only (JP);
Routes of; administration	Oral (tablets)
Pharmacokinetic data
Biological half-life	10.5 h
Excretion	Urine
Identifiers
CAS Number	99593-25-6
ATC code	None
PubChem	CID 5069
ChemSpider	4891
UNII	CU3H37T766
KEGG	D08481
Synonyms	5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide
Chemical data
Formula	C21H20Cl2N6O3
Molar mass	475.328 g/mol
	SMILES ClC1=C(C(C2=CC(Cl)=CC=C2N3C(CNC(CN)=O)=NC(C(N(C)C)=O)=N3)=O)C=CC=C1 ;
	InChI InChI=1S/C21H20Cl2N6O3/c1-28(2)21(32)20-26-17(11-25-18(30)10-24)29(27-20)16-8-7-12(22)9-14(16)19(31)13-5-3-4-6-15(13)23/h3-9H,10-11,24H2,1-2H3,(H,25,30) ; Key:KYHFRCPLIGODFH-UHFFFAOYSA-N ;
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