Ethyl loflazepate

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Ethyl loflazepate
File:Ethyl loflazepate.svg
File:EtLoflazepate3d.png
Systematic (IUPAC) name
ethyl- 9-chloro- 6-(2-fluorophenyl)- 3-oxo- 2,5-diazabicyclo [5.4.0]undeca- 5,8,10,12- tetraene- 4-carboxylate
Clinical data
Pregnancy
category
  •  ?
Routes of
administration
Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life ?
Excretion Renal
Identifiers
CAS Number 28911-01-5
ATC code N05BA18 (WHO)
PubChem CID 3299
DrugBank ?
Chemical data
Formula C18H14ClFN2O3
Molar mass 360.7[[Script error: No such module "String".]]
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Ethyl loflazepate (marketed under the brand names Meilax, Ronlax and Victan)[1][2][3] is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.[4] 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.[5] Its elimination half life is 51 hours - 103 hours.[6] It's mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound.[7] Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, it's active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate.[8] The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate.[9] Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment.[10] 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.[11] 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.[12] High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.[13]

Ethyl loflazeplate is commercialized in Mexico, although is not very used, under the trade name Victan. It's officially approved for the following conditions:[14][15]

See also

References

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External links

ja:ロフラゼプ酸エチル pt:Loflazepato de etilo
  1. Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. Ba, BB; Iliadis, A; Cano, JP (1989). "Pharmacokinetic modeling of ethyl loflazepate (Victan) and its main active metabolites". Annals of biomedical engineering. 17 (6): 633–46. doi:10.1007/BF02367467. ISSN 0090-6964. PMID 2574017. 
  3. "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2009-04-05. 
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  8. Chambon, JP; Perio, A; Demarne, H; Hallot, A; Dantzer, R; Roncucci, R; Bizière, K (1985). "Ethyl loflazepate: a prodrug from the benzodiazepine series designed to dissociate anxiolytic and sedative activities". Arzneimittel-Forschung. 35 (10): 1573–7. ISSN 0004-4172. PMID 2866771. 
  9. Davi, H; Guyonnet, J; Sales, Y; Cautreels, W (1985). "Metabolism of ethyl loflazepate in the rat, the dog, the baboon and in man". Arzneimittel-Forschung. 35 (7): 1061–5. ISSN 0004-4172. PMID 2864933. 
  10. Ba, BB; Iliadis, A; Durand, A; Berger, Y; Necciari, J; Cano, JP (1989). "Effect of renal failure on the pharmacokinetics of ethyl loflazepate (Victan) in man". Fundamental & clinical pharmacology. 3 (1): 11–7. doi:10.1111/j.1472-8206.1989.tb00025.x. ISSN 0767-3981. PMID 2714728. 
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  14. "Victan". saludzac.gob.mx/. Retrieved 2009-12-25. 
  15. "VICTAN". Farmacia Guerra. Retrieved 2009-12-25.