Ethyl loflazepate

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Ethyl loflazepate
Ethyl loflazepate.svg
EtLoflazepate3d.png
Clinical data
Trade names Victan, Meilax, Ronlax
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • ?
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Elimination half-life 51-103 h
Excretion Renal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.044.976 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C18H14ClFN2O3
Molar mass 360.7 g·mol−1
3D model (JSmol)
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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]

Contents

Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions: [15] [16]

See also

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References

  1. DE Patent 2012190
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  11. 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. S2CID   2850707.
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