Ethyl loflazepate

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	US: Schedule IV
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[[]]

Ethyl loflazepate (marketed under the brand names Meilax, Ronlax and Victan) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. 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. Its elimination half life is 51 hours - 103 hours. It's mechanism of action is similar to other benzodiazepines. Ethyl loflazepate also produces an active metabolite which is stronger than the parent compound. 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. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-hydroxydescarbethoxyloflazepate. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. 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. 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. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.

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

• Anxiety
• Post-trauma anxiety
• Anxiety associated with severe neuropathic pain.
• Generalized anxiety disorder (GAD)
• Anxiety "crisis"
• Delirium tremens

See also

• Benzodiazepine

External links

• (Japanese) Meilax Fine Granules

ja:ロフラゼプ酸エチル pt:Loflazepato de etilo