Clinical data | |
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Trade names | Victan, Meilax, Ronlax |
AHFS/ Drugs.com | International Drug Names |
Pregnancy category |
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Routes of administration | Oral |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Bioavailability | ? |
Metabolism | Hepatic |
Elimination half-life | 51-103 h |
Excretion | Renal |
Identifiers | |
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CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
ECHA InfoCard | 100.044.976 |
Chemical and physical data | |
Formula | C18H14ClFN2O3 |
Molar mass | 360.77 g·mol−1 |
3D model ( JSmol) | |
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(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]
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 |
Chemical and physical data | |
Formula | C18H14ClFN2O3 |
Molar mass | 360.77 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(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]