Rilmazafone
Also called Rhythmy
Part of the metabolic pathway of Rilmazafone. See the timeline on the metabolic highway.
Dosage
Oral
TripSit dose text
TripSit's factsheet also states its doses as text.
Light: .5-1mg Common: 1-2mg Strong: 2-4mg+ TS
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Duration
TripSit factsheet
Mixing
For best safety practice, don't mix this drug with other depressants.
Why: respiratory depression. PsychonautWiki says:
- “Respiratory depression (also known as hypoventilation) can be described as a reduced urge to breathe that can be fatal depending on its intensity.” (PsychonautWiki, Respiratory depression, revision 150612)
- “... otherwise safe dosages of these compounds can become fatal when combined with even small amounts of other classes of depressant. For example, benzodiazepines combined with opioids are an extremely common cause of fatal respiratory depression. It is therefore strongly discouraged to combine these depressants at any dosage range.” (PsychonautWiki, Respiratory depression, revision 150612)
- “The most common cause of substance-related deaths is the combination of depressants (such as opiates, benzodiazepines, or alcohol) with other depressants.” (PsychonautWiki, Responsible drug use, revision 168206)
- “This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration.” (PsychonautWiki, dangerous interactions table, "Depressants" row, revision 156847)
Quotes from PsychonautWiki, CC BY-SA 4.0.
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
Backed by medical journals
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart; TripSit's own notes are on combo.tripsit.me.
Caution
Risks and toxicity
Testing
Effects
Overview
Unique to Japan, this drug, also known as Rhythmy, is a benzodiazepine pro-drug which while inactive itself, is metabolised into the active compound in-vivo. Soluble in water. TS
Rilmazafone (リスミー, brand name Rhythmy; developmental code 450191-S) is a water-soluble prodrug developed by Shionogi and approved in Japan for the treatment of insomnia and as a pre-anesthetic agent. It is not a benzodiazepine in the pharmacological or structural sense — the parent compound contains no diazepine ring and has no affinity for benzodiazepine receptors — but is converted inside the body into several active benzodiazepine metabolites, principally rilmazolam, which produce sedative and hypnotic effects. Outside Japan, rilmazafone has appeared as a new psychoactive substance (NPS) and has been implicated in fatal overdoses in Europe and North America.[1–4] WP
History
Legal status
Legal status
Rilmazafone is approved as a prescription medication in Japan (Rx-only). It is not approved for medical use and is not scheduled as a controlled substance in the United States, Canada, or most European jurisdictions as of mid-2026, though early-warning monitoring is ongoing in several countries. WP⚠ Wikipedia itself has flagged this text: citation needed.
Pharmacology
Pharmacology
Rilmazafone itself has negligible affinity for GABAA receptors and produces no psychoactive effects prior to metabolism. Its pharmacological activity is mediated entirely through its metabolites, particularly rilmazolam, which acts as a positive allosteric modulator of the GABAA receptor, enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) in the central nervous system. This produces sedative, hypnotic, anxiolytic, and muscle-relaxant effects characteristic of the benzodiazepine class.[2]
Because rilmazafone's prodrug structure bypasses direct receptor interaction until after intestinal metabolism, it was developed partly with the intention of reducing the abuse potential and side-effect profile associated with direct-acting benzodiazepines, though its metabolites retain the full pharmacodynamic profile of the class. WP
Chemistry
- Formula
- C21H20Cl2N6O3 PC
- CAS number
- 99593-25-6 PC
- Molar mass (g/mol)
- 475.3 PC
- IUPAC name (computed by PubChem)
- 5-
[[(2- PCaminoacetyl) amino] methyl] - 1- [4- chloro- 2- (2- chlorobenzoyl) phenyl] - N, N- dimethyl- 1, 2, 4- triazole- 3- carboxamide - SMILES
- CN(C)
C(=O) PCC1=NN(C(=N1) CNC(=O) CN) C2=C(C=C(C=C2) Cl) C(=O) C3=CC=CC=C3Cl - InChIKey
- KYHFRCPLIGODFH-
UHFFFAOYSA- PCN - PubChem CID
- 5069
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ListingsPop culture
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References
- Other 1-PHENYL-1H-1,2,4-TRIAZOL-DERIVATE, IHRE Salze mit Saeuren, Verfahren zu Ihrer Herstellung und Diese Verbindungen Enthaltende Arzneimittel
- Journal / agency Yamamoto K, Hirose K, Matsushita A, Yoshimura K, Sawada T, Eigyo M, Jyoyama H, Fujita A, Matsubara K, Tsukinoki Y. Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. July 1984. doi:10.1254/fpj.84.109 · PMID 6149174
- Journal / agency Yamamoto K, Matsushita A, Sawada T, Naito Y, Yoshimura K, Takesue H, Utsumi S, Kawasaki K, Hirono S, Koshida H. 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. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. July 1984. doi:10.1254/fpj.84.25 · PMID 6149175
- Journal / agency Kronstrand R, Roman M, Johansson A, Wu X, Green H, Truver MT. Rilmazafone: A designer benzodiazepine pro-drug involved in fatal intoxications. Journal of Analytical Toxicology. 15 September 2023. doi:10.1093/jat/bkad041 · PMID 37348041
- Journal / agency 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. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. August 1984. doi:10.1254/fpj.84.155 · PMID 6149177
- Journal / agency Yasui M, Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes. Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology. June 2005. PMID 16045197
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), TripSit factsheets, PubChem (public domain). Each value links to the exact revision it came from.