Ethyl loflazepate

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Ethyl loflazepate
Ethyl loflazepate.svg
EtLoflazepate3d.png
Systematic (IUPAC) name
ethyl 7-chloro-5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepine-3-carboxylate
Clinical data
Trade names Victan, Meilax, Ronlax
AHFS/Drugs.com International Drug Names
Pregnancy
category
  •  ?
Legal status
Routes of
administration		 Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life 51-103 h
Excretion Renal
Identifiers
CAS Number 29177-84-2 N
ATC code N05BA18 (WHO)
PubChem CID: 3299
DrugBank DB01545 YesY
ChemSpider 3183 YesY
UNII VJB5FW9W9J N
KEGG D01293 N
ChEMBL CHEMBL1213460 YesY
Chemical data
Formula C18H14ClFN2O3
Molecular mass 360.7
  • FC1=CC=CC=C1C2=NC(C(OCC)=O)C(NC3=C2C=C(C=C3)Cl)=O
  • InChI=1S/C18H14ClFN2O3/c1-2-25-18(24)16-17(23)21-14-8-7-10(19)9-12(14)15(22-16)11-5-3-4-6-13(11)20/h3-9,16H,2H2,1H3,(H,21,23) YesY
  • Key:CUCHJCMWNFEYOM-UHFFFAOYSA-N YesY
 NYesY (what is this?)  (verify)

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 renal 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

References

  1. ↑ DE Patent 2012190
  2. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  8. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  9. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  10. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  11. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  12. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  13. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  14. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  15. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  16. ↑ Lua error in package.lua at line 80: module 'strict' not found.

External links

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