Chemistry:Ethyl loflazepate
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| Trade names | Victan, Meilax, Ronlax |
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| Routes of administration | Oral |
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| Bioavailability | ? |
| Metabolism | Hepatic |
| Elimination half-life | 51-103 h |
| Excretion | Renal |
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| Formula | C18H14ClFN2O3 |
| Molar mass | 360.7 g·mol−1 |
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Ethyl loflazepate[1] (marketed under the brand names Meilax, Ronlax and Victan)[2][3][4] is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.[5] 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.[6] Its elimination half-life is 51–103 hours.[7] Its mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound.[8] 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.[9] The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate.[10] Accumulation of the active metabolites of ethyl loflazepate are not affected by those with kidney failure or impairment.[11] 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.[12] 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.[13] High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.[14]
Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions:[15][16]
- Anxiety
- Post-trauma anxiety
- Anxiety associated with severe neuropathic pain
- Generalized anxiety disorder (GAD)
- Obsessive–compulsive disorder
- Panic attack
- Delirium tremens
See also
References
- ↑ DE patent 2012190
- ↑ "New approach in bioavailability study of two formulations of ethyl loflazepate". Arzneimittel-Forschung 38 (10): 1486–1489. October 1988. PMID 2904268.
- ↑ "Pharmacokinetic modeling of ethyl loflazepate (Victan) and its main active metabolites". Annals of Biomedical Engineering 17 (6): 633–646. 1989. doi:10.1007/BF02367467. PMID 2574017.
- ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html.
- ↑ "[Behavioral effects of ethyl loflazepate and its metabolites]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 82 (5): 395–409. November 1983. doi:10.1254/fpj.82.395. PMID 6142848.
- ↑ "A toxicologic evaluation of ethyl fluclozepate (CM 6912)". International Journal of Clinical Pharmacology, Therapy, and Toxicology 19 (10): 453–472. October 1981. PMID 6116677.
- ↑ "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 7 (11–12): 565–571. November 1980. doi:10.1002/bms.1200071124. PMID 6112027.
- ↑ "Inhibitory effect on 3H-diazepam binding and potentiating action on GABA of ethyl loflazepate, a new minor tranquilizer". Japanese Journal of Pharmacology 37 (4): 373–379. April 1985. doi:10.1254/jjp.37.373. PMID 2861304.
- ↑ "Ethyl loflazepate: a prodrug from the benzodiazepine series designed to dissociate anxiolytic and sedative activities". Arzneimittel-Forschung 35 (10): 1573–1577. 1985. PMID 2866771.
- ↑ "Metabolism of ethyl loflazepate in the rat, the dog, the baboon and in man". Arzneimittel-Forschung 35 (7): 1061–1065. 1985. PMID 2864933.
- ↑ "Effect of renal failure on the pharmacokinetics of ethyl loflazepate (Victan) in man". Fundamental & Clinical Pharmacology 3 (1): 11–17. 1989. doi:10.1111/j.1472-8206.1989.tb00025.x. PMID 2714728.
- ↑ "Acute poisonings with ethyle loflazepate, flunitrazepam, prazepam and triazolam in children". Veterinary and Human Toxicology 34 (2): 141–143. April 1992. PMID 1354907.
- ↑ "Pharmacokinetics of the active metabolites of ethyl loflazepate in elderly patients who died of asphyxia associated with benzodiazepine-related toxicity". Journal of Analytical Toxicology 29 (2): 140–144. March 2005. doi:10.1093/jat/29.2.140. PMID 15902983.
- ↑ "[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 118 (6): 403–410. December 2001. doi:10.1254/fpj.118.403. PMID 11778459.
- ↑ "Victan". saludzac.gob.mx/. http://www.saludzac.gob.mx/plm/prods/36557.htm.
- ↑ "VICTAN". Farmacia Guerra. http://www.famguerra.com/Meds/Search/Meds.cfm?pagina=36557.htm.
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