Ethyl loflazepate
Also called Ronlax, Meilax, Victan
Part of the metabolic pathway of Ronlax. See the timeline on the metabolic highway.
Dosage
Oral
TripSit dose text
TripSit's factsheet also states its doses as text.
Oral Light: 0.5-1mg Common: 1-2mg Strong: 2-4mg. TS
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Duration
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Mixing
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
Risks and toxicity
TripSit factsheet
- Avoid
- All CNS depressants. Also if using the antidepressant Fluvoxamine may potentiate the adverse effects. TS
Testing
Effects
Overview
A benzodiazepine derivative that posses the standard benzodiazepine effects. It has a very long half life (51-103 hours) it metabolizes into an active compound. (Descarboxyloflazepate) Is sold in Mexico. TS
Ethyl loflazepate (marketed under the brand names Meilax, Ronlax and Victan) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. In animal studies it was found to have low toxicity, although in rats evidence of pulmonary phospholipidosis occurred with pulmonary foam cells developing with long-term use of very high doses. Its elimination half-life is 51–103 hours. Its mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with kidney failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. Death from therapeutic maintenance doses of ethyl loflazepate taken for 2 – 3 weeks has been reported in 3 elderly patients. The cause of death was asphyxia due to benzodiazepine toxicity. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.[1–13] WP
Ethyl loflazeplate is commercialized in Belgium, Costa Rica, Dominican Republic, El Salvador, France, Guatemala, Honduras, Mexico, Panama, Paraguay, Portugal and Romania, under the trade name Victan. In Japan, it is prescribed under the name Meilax (メイラックス). It is officially approved for the following conditions: WP
Anxiety WP
Post-trauma anxiety WP
Anxiety associated with severe neuropathic pain WP
Generalized anxiety disorder (GAD) WP
Obsessive–compulsive disorder WP
Panic attack WP
Delirium tremens WP
History
Legal status
Pharmacology
Chemistry
- Formula
- C18H14ClFN2O3 PC
- CAS number
- 29177-84-2 PC
- Molar mass (g/mol)
- 360.8 PC
- IUPAC name (computed by PubChem)
- ethyl 7-
chloro- PC5- (2- fluorophenyl) - 2- oxo- 1, 3- dihydro- 1, 4- benzodiazepine- 3- carboxylate - SMILES
- CCOC(=O)
C1C(=O) PCNC2=C(C=C(C=C2) Cl) C(=N1) C3=CC=CC=C3F - InChIKey
- CUCHJCMWNFEYOM-
UHFFFAOYSA- PCN - PubChem CID
- 3299
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References
- Journal / agency Ba BB, Iliadis A, Durand A, Berger Y, Cano JP. New approach in bioavailability study of two formulations of ethyl loflazepate. Arzneimittel-Forschung. October 1988. PMID 2904268
- Journal / agency Ba BB, Iliadis A, Cano JP. Pharmacokinetic modeling of ethyl loflazepate (Victan) and its main active metabolites. Annals of Biomedical Engineering. 1989. doi:10.1007/BF02367467 · PMID 2574017
- Other Benzodiazepine Names
- Journal / agency Ueki S, Watanabe S, Yamamoto T, Shibata S, Shibata K, Ohta H, Ikeda K, Kiyota Y, Sato Y. Behavioral effects of ethyl loflazepate and its metabolites. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. November 1983. doi:10.1254/fpj.82.395 · PMID 6142848
- Journal / agency Mazue G, Berthe J, Newmann AJ, Brunaud M. A toxicologic evaluation of ethyl fluclozepate (CM 6912). International Journal of Clinical Pharmacology, Therapy, and Toxicology. October 1981. PMID 6116677
- Journal / agency Cautreels W, Jeanniot JP. Quantitative analysis of CM 6912 (ethyl loflazepate) and its metabolites in plasma and urine by chemical ionization gas chromatography mass spectrometry. Application to pharmacokinetic studies in man. Biomedical Mass Spectrometry. November 1980. doi:10.1002/bms.1200071124 · PMID 6112027
- Journal / agency Sakai Y, Namima M. Inhibitory effect on 3H-diazepam binding and potentiating action on GABA of ethyl loflazepate, a new minor tranquilizer. Japanese Journal of Pharmacology. April 1985. doi:10.1254/jjp.37.373 · PMID 2861304
- Journal / agency Chambon JP, Perio A, Demarne H, Hallot A, Dantzer R, Roncucci R, Bizière K. Ethyl loflazepate: a prodrug from the benzodiazepine series designed to dissociate anxiolytic and sedative activities. Arzneimittel-Forschung. 1985. PMID 2866771
- Journal / agency Davi H, Guyonnet J, Sales Y, Cautreels W. Metabolism of ethyl loflazepate in the rat, the dog, the baboon and in man. Arzneimittel-Forschung. 1985. PMID 2864933
- Journal / agency Ba BB, Iliadis A, Durand A, Berger Y, Necciari J, Cano JP. Effect of renal failure on the pharmacokinetics of ethyl loflazepate (Victan) in man. Fundamental & Clinical Pharmacology. 1989. doi:10.1111/j.1472-8206.1989.tb00025.x · PMID 2714728
- Journal / agency Pulce C, Mollon P, Pham E, Frantz P, Descotes J. Acute poisonings with ethyle loflazepate, flunitrazepam, prazepam and triazolam in children. Veterinary and Human Toxicology. April 1992. PMID 1354907
- Journal / agency Kamijo Y, Hayashi I, Nishikawa T, Yoshimura K, Soma K. Pharmacokinetics of the active metabolites of ethyl loflazepate in elderly patients who died of asphyxia associated with benzodiazepine-related toxicity. Journal of Analytical Toxicology. March 2005. doi:10.1093/jat/29.2.140 · PMID 15902983
- Journal / agency Imanishi T, Onozawa K, Hayashi A, Baba J. Effects of fluvoxamine on both the desired anxiolytic effect and the adverse motor incoordination and amnesia induced by benzodiazepines. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica. December 2001. doi:10.1254/fpj.118.403 · PMID 11778459
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