Ethyl loflazepate
Systematic (IUPAC) name | |
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ethyl 7-chloro-5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepine-3-carboxylate
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Clinical data | |
Trade names | Victan, Meilax, Ronlax |
AHFS/Drugs.com | International Drug Names |
Pregnancy category |
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Legal status |
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Routes of administration |
Oral |
Pharmacokinetic data | |
Bioavailability | ? |
Metabolism | Hepatic |
Biological half-life | 51-103 h |
Excretion | Renal |
Identifiers | |
CAS Number | 29177-84-2 |
ATC code | N05BA18 (WHO) |
PubChem | CID: 3299 |
DrugBank | DB01545 |
ChemSpider | 3183 |
UNII | VJB5FW9W9J |
KEGG | D01293 |
ChEMBL | CHEMBL1213460 |
Chemical data | |
Formula | C18H14ClFN2O3 |
Molecular mass | 360.7 |
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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 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]
- Anxiety
- Post-trauma anxiety
- Anxiety associated with severe neuropathic pain.
- Generalized anxiety disorder (GAD)
- Anxiety "crisis"
- Delirium tremens
See also
References
- ↑ DE Patent 2012190
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External links
- (Japanese) Meilax Fine Granules