Ethyl loflazepate explained

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]

See also

External links

Notes and References

  1. DE . 2012190 .
  2. Ba BB, Iliadis A, Durand A, Berger Y, Cano JP . New approach in bioavailability study of two formulations of ethyl loflazepate . Arzneimittel-Forschung . 38 . 10 . 1486–1489 . October 1988 . 2904268 .
  3. Ba BB, Iliadis A, Cano JP . Pharmacokinetic modeling of ethyl loflazepate (Victan) and its main active metabolites . Annals of Biomedical Engineering . 17 . 6 . 633–646 . 1989 . 2574017 . 10.1007/BF02367467 . 31310535 .
  4. Web site: Benzodiazepine Names . 2009-04-05 . non-benzodiazepines.org.uk . dead . https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html . 2008-12-08 .
  5. Ueki S, Watanabe S, Yamamoto T, Shibata S, Shibata K, Ohta H, Ikeda K, Kiyota Y, Sato Y . 6 . [Behavioral effects of ethyl loflazepate and its metabolites] . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 82 . 5 . 395–409 . November 1983 . 6142848 . 10.1254/fpj.82.395 . free .
  6. Mazue G, Berthe J, Newmann AJ, Brunaud M . A toxicologic evaluation of ethyl fluclozepate (CM 6912) . International Journal of Clinical Pharmacology, Therapy, and Toxicology . 19 . 10 . 453–472 . October 1981 . 6116677 .
  7. 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 . 7 . 11–12 . 565–571 . November 1980 . 6112027 . 10.1002/bms.1200071124 .
  8. 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 . 37 . 4 . 373–379 . April 1985 . 2861304 . 10.1254/jjp.37.373 . free .
  9. 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 . 35 . 10 . 1573–1577 . 1985 . 2866771 .
  10. Davi H, Guyonnet J, Sales Y, Cautreels W . Metabolism of ethyl loflazepate in the rat, the dog, the baboon and in man . Arzneimittel-Forschung . 35 . 7 . 1061–1065 . 1985 . 2864933 .
  11. 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 . 3 . 1 . 11–17 . 1989 . 2714728 . 10.1111/j.1472-8206.1989.tb00025.x . 2850707 .
  12. 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 . 34 . 2 . 141–143 . April 1992 . 1354907 .
  13. 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 . 29 . 2 . 140–144 . March 2005 . 15902983 . 10.1093/jat/29.2.140 .
  14. 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 . 118 . 6 . 403–410 . December 2001 . 11778459 . 10.1254/fpj.118.403 . free .
  15. Web site: Victan. 2009-12-25. saludzac.gob.mx/. https://web.archive.org/web/20090526230611/http://www.saludzac.gob.mx/plm/prods/36557.htm. 2009-05-26. dead.
  16. Web site: VICTAN. 2009-12-25. Farmacia Guerra.

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