Ethyl loflazepate

Routes of
administrationOralATC codeLegal statusLegal status Pharmacokinetic dataBioavailability?MetabolismHepaticElimination half-life51-103 hExcretionRenalIdentifiersCAS NumberPubChem CIDDrugBankChemSpiderUNIIKEGGChEMBLECHA InfoCard100.044.976 Chemical and physical dataFormulaC₁₈H₁₄ClFN₂O₃Molar mass360.77 g·mol⁻¹3D model (JSmol) ^NY (what is this?)  (verify)

Ethyl loflazepate^[2] (marketed under the brand names Meilax, Ronlax and Victan)^[3][4][5] is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.^[6] 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.^[7] Its elimination half-life is 51–103 hours.^[8] Its mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound.^[9] 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.^[10] The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate.^[11] Accumulation of the active metabolites of ethyl loflazepate are not affected by those with kidney failure or impairment.^[12] 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.^[13] 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.^[14] High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.^[15]

Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions:^[16][17]

• Anxiety
• Post-trauma anxiety
• Anxiety associated with severe neuropathic pain
• Generalized anxiety disorder (GAD)
• Obsessive–compulsive disorder
• Panic attack
• Delirium tremens

See also

• Benzodiazepine

References

External links

• "Meilax Fine Granules" (PDF) (in Japanese).