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al atc code n05ba18 who legal status legal status br class b1 psychoactive drugs 1 ca schedule iv de anlage iii special prescription form required us schedule iv pharmacokinetic data bioavailability metabolism hepatic elimination half life 51 103 h excretion renal identifiers iupac name ethyl 7 chloro 5 2 fluorophenyl 2 oxo 1 3 dihydro 1 4 benzodiazepine 3 carboxylate cas number 29177 84 2 n pubchem cid 3299 drugbank db01545 y chemspider 3183 y unii vjb5fw9w9j kegg d01293 n chembl chembl1213460 y comptox dashboard epa dtxsid60865475 echa infocard 100 044 976 chemical and physical data formula c 18 h 14 cl f n 2 o 3 molar mass 360 77 g mol 1 3d model jsmol interactive image smiles fc1 cc cc c1c2 nc c occ o c nc3 c2c c c c3 cl o inchi 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 y key cuchjcmwnfeyom uhfffaoysa n y n y 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 belgium costa rica dominican republic el salvador france guatemala honduras mexico panama paraguay portugal and romania under the trade name victan in japan it is prescribed under the name meilax メイラックス it is officially approved for the following conditions anxiety post trauma anxiety anxiety associated with severe neuropathic pain generalized anxiety disorder gad obsessive compulsive disorder panic attack delirium tremens see also edit benzodiazepine references edit anvisa 2023 03 31 rdc nº 784 listas de substâncias entorpecentes psicotrópicas precursoras e outras sob controle especial collegiate board resolution no 784 lists of narcotic psychotropic precursor and other substances under special control in brazilian portuguese diário oficial da união published 2023 04 04 archived from the original on 2023 08 03 retrieved 2023 08 16 de 2012190 ba bb iliadis a durand a berger y cano jp october 1988 new approach in bioavailability study of two formulations of ethyl loflazepate arzneimittel forschung 38 10 1486 1489 pmid 2904268 ba bb iliadis a cano jp 1989 pharmacokinetic modeling of ethyl loflazepate victan and its main active metabolites annals of biomedical engineering 17 6 633 646 doi 10 1007 bf02367467 pmid 2574017 s2cid 31310535 benzodiazepine names non benzodiazepines org uk archived from the original on 2008 12 08 retrieved 2009 04 05 ueki s watanabe s yamamoto t shibata s shibata k ohta h et al november 1983 behavioral effects of ethyl loflazepate and its metabolites nihon yakurigaku zasshi folia pharmacologica japonica 82 5 395 409 doi 10 1254 fpj 82 395 pmid 6142848 mazue g berthe j newmann aj brunaud m october 1981 a toxicologic evaluation of ethyl fluclozepate cm 6912 international journal of clinical pharmacology therapy and toxicology 19 10 453 472 pmid 6116677 cautreels w jeanniot jp november 1980 quantitative analysis of cm 6912 ethyl loflazepate and its metabolites in plasma and urine by chemical ionization gas chromatography mass spectrometry application to pharmacokinetic studies in man biomedical mass spectrometry 7 11 12 565 571 doi 10 1002 bms 1200071124 pmid 6112027 sakai y namima m april 1985 inhibitory effect on 3h diazepam binding and potentiating action on gaba of ethyl loflazepate a new minor tranquilizer japanese journal of pharmacology 37 4 373 379 doi 10 1254 jjp 37 373 pmid 2861304 chambon jp perio a demarne h hallot a dantzer r roncucci r bizière k 1985 ethyl loflazepate a prodrug from the benzodiazepine series designed to dissociate anxiolytic and sedative activities arzneimittel forschung 35 10 1573 1577 pmid 2866771 davi h guyonnet j sales y cautreels w 1985 metabolism of ethyl loflazepate in the rat the dog the baboon and in man arzneimittel forschung 35 7 1061 1065 pmid 2864933 ba bb iliadis a durand a berger y necciari j cano jp 1989 effect of renal failure on the pharmacokinetics of ethyl loflazepate victan in man fundamental clinical pharmacology 3 1 11 17 doi 10 1111 j 1472 8206 1989 tb00025 x pmid 2714728 s2cid 2850707 pulce c mollon p pham e frantz p descotes j april 1992 acute poisonings with ethyle loflazepate flunitrazepam prazepam and triazolam in children veterinary and human toxicology 34 2 141 143 pmid 1354907 kamijo y hayashi i nishikawa t yoshimura k soma k march 2005 pharmacokinetics of the active metabolites of ethyl loflazepate in elderly patients who died of asphyxia associated with benzodiazepine related toxicity journal of analytical toxicology 29 2 140 144 doi 10 1093 jat 29 2 140 pmid 15902983 imanishi t onozawa k hayashi a baba j december 2001 effects of fluvoxamine on both the desired anxiolytic effect and the adverse motor incoordination and amnesia induced by benzodiazepines nihon yakurigaku zasshi folia pharmacologica japonica 118 6 403 410 doi 10 1254 fpj 118 403 pmid 11778459 external links edit meilax fine granules pdf in japanese v t e benzodiazepines 1 4 benzodiazepines 2 oxoquazepam 3 hydroxyphenazepam bromazepam bromonordiazepam bms 906024 camazepam carburazepam chlordiazepoxide cinazepam cinolazepam clonazepam cloniprazepam clorazepate cyprazepam delorazepam demoxepam desmethylflunitrazepam devazepide diazepam diclazepam difludiazepam doxefazepam elfazepam ethyl carfluzepate ethyl dirazepate ethyl loflazepate flubromazepam fletazepam fludiazepam flunitrazepam flurazepam flutemazepam flutoprazepam fosazepam gidazepam halazepam iclazepam irazepine kenazepine ketazolam lorazepam lormetazepam lufuradom meclonazepam medazepam menitrazepam metaclazepam motrazepam n desalkylflurazepam nifoxipam nimetazepam nitemazepam nitrazepam nitrazepate nordazepam nortetrazepam oxazepam phenazepam pinazepam pivoxazepam prazepam proflazepam quazepam qh ii 66 reclazepam ro4491533 ro05 4082 ro5 4864 ro07 5220 ro07 9749 ro20 8065 ro20 8552 sh i 048a sulazepam temazepam tetrazepam tifluadom timelotem tolufazepam triflunordazepam tuclazepam uldazepam 1 5 benzodiazepines arfendazam clobazam cp 1414s lofendazam triflubazam 2 3 benzodiazepines girisopam gyki 52466 gyki 52895 nerisopam talampanel tofisopam triazolobenzodiazepines adinazolam alprazolam bromazolam clonazolam estazolam ethylbromazolam fluadinazolam flualprazolam flubromazolam flunitrazolam nitrazolam phenazolam pyrazolam rilmazolam active metabolite of rilmazafone triazolam imidazobenzodiazepines bretazenil climazolam evt 201 fg 8205 flumazenil gl ii 73 imidazenil 123 i iomazenil l 655 708 loprazolam midazolam pwz 029 remimazolam ro15 4513 ro48 6791 ro48 8684 ro4938581 sarmazenil sh 053 r ch3 2 f oxazolobenzodiazepines cloxazolam flutazolam haloxazolam mexazolam oxazolam thienodiazepines bentazepam clotiazepam ro09 9212 thienotriazolodiazepines α hydroxyetizolam apafant brotizolam ciclotizolam clotizolam deschloroclotizolam deschloroetizolam etizolam flubrotizolam fluclotizolam fluetizolam israpafant jq1 metizolam thienobenzodiazepines olanzapine telenzepine pyridodiazepines lopirazepam pyridotriazolodiazepines zapizolam pyrazolodiazepines razobazam ripazepam zolazepam zomebazam zometapine pyrrolodiazepines premazepam tetrahydroisoquinobenzodiazepines clazolam pyrrolobenzodiazepines anthramycin benzodiazepine prodrugs alprazolam triazolobenzophenone avizafone rilmazafone others unsorted ntx 1955 ro 7308480 atypical activity profile not gaba a receptor ligands v t e anxiolytics n05b 5 ht 1a r tooltip 5 ht1a receptor agonists buspirone gepirone tandospirone gaba a r tooltip gabaa receptor pams tooltip positive allosteric modulators benzodiazepines adinazolam alprazolam bromazepam camazepam chlordiazepoxide clobazam clonazepam clorazepate clotiazepam cloxazolam diazepam ethyl loflazepate etizolam fludiazepam halazepam ketazolam lorazepam medazepam nordazepam oxazepam pinazepam prazepam others alpidem barbiturates e g phenobarbital carbamates e g meprobamate carisoprodol chlormezanone ethanol alcohol etifoxine gabapentinoids α 2 δ vdcc blockers gabapentin gabapentin enacarbil phenibut baclofen pregabalin antidepressants ssris tooltip selective serotonin reuptake inhibitors e g escitalopram snris tooltip serotonin norepinephrine reuptake inhibitors e g duloxetine saris tooltip serotonin antagonist and reuptake inhibitors e g trazodone tcas tooltip tricyclic antidepressants e g clomipramine tecas tooltip tetracyclic antidepressants e g mirtazapine maois tooltip monoamine oxidase inhibitors e g phenelzine others agomelatine bupropion tianeptine vilazodone vortioxetine sympatholytics antiadrenergics alpha 1 blockers e g prazosin alpha 2 agonists e g clonidine dexmedetomidine guanfacine beta blockers e g propranolol atenolol betaxolol nadolol oxprenolol pindolol others benzoctamine cycloserine fabomotizole hydroxyzine lorpiprazole mebicar mepiprazole nicotine tobacco opipramol oxaflozane phenaglycodol phenibut picamilon selank tiagabine tofisopam validolum who em withdrawn from market clinical trials phase iii never to phase iii v t e gaba a receptor positive modulators alcohols brometone butanol chloralodol chlorobutanol cloretone ethanol alcohol alcoholic drink ethchlorvynol isobutanol isopropanol menthol methanol methylpentynol pentanol petrichloral propanol tert butanol 2m2p tert pentanol 2m2b tribromoethanol trichloroethanol triclofos trifluoroethanol barbiturates dmbb allobarbital alphenal amobarbital aprobarbital barbexaclone barbital benzobarbital benzylbutylbarbiturate brallobarbital brophebarbital butabarbital secbutabarbital butalbital buthalital butobarbital butallylonal carbubarb crotylbarbital cyclobarbital cyclopentobarbital difebarbamate enallylpropymal ethallobarbital eterobarb febarbamate heptabarb heptobarbital hexethal hexobarbital methallatal metharbital methitural methohexital methylphenobarbital narcobarbital nealbarbital pentobarbital phenallymal phenobarbital phetharbital primidone probarbital propallylonal propylbarbital proxibarbital reposal secobarbital sigmodal spirobarbital talbutal tetrabamate tetrabarbital thialbarbital thiamylal thiobarbital thiobutabarbital thiopental thiotetrabarbital valofane vinbarbital vinylbital benzodiazepines 2 oxoquazepam 3 hydroxyphenazepam adinazolam alprazolam arfendazam avizafone bentazepam bretazenil bromazepam bromazolam brotizolam camazepam carburazepam chlordiazepoxide ciclotizolam cinazepam cinolazepam clazolam climazolam clobazam clonazepam clonazolam cloniprazepam clorazepate clotiazepam cloxazolam cp 1414s cyprazepam delorazepam demoxepam diazepam diclazepam dimdazenil doxefazepam elfazepam estazolam ethyl carfluzepate ethyl dirazepate ethyl loflazepate etizolam fg 8205 fletazepam flubromazepam flubromazolam fludiazepam flunitrazepam flunitrazolam flurazepam flutazolam flutemazepam flutoprazepam fosazepam gidazepam halazepam haloxazolam iclazepam imidazenil irazepine ketazolam lofendazam lopirazepam loprazolam lorazepam lormetazepam meclonazepam medazepam menitrazepam metaclazepam mexazolam midazolam motrazepam n desalkylflurazepam nifoxipam nimetazepam nitrazepam nitrazepate nitrazolam nordazepam nortetrazepam oxazepam oxazolam phenazepam pinazepam pivoxazepam prazepam premazepam proflazepam pyrazolam qh ii 66 quazepam reclazepam remimazolam rilmazafone ripazepam ro48 6791 ro48 8684 sh 053 r ch3 2 f sulazepam temazepam tetrazepam tolufazepam triazolam triflubazam triflunordazepam ro5 2904 tuclazepam uldazepam zapizolam zolazepam zomebazam carbamates carisbamate carisoprodol clocental cyclarbamate difebarbamate emylcamate ethinamate febarbamate felbamate hexapropymate hydroxyphenamate lorbamate mebutamate meprobamate nisobamate pentabamate phenprobamate procymate styramate tetrabamate tybamate flavonoids 6 methylapigenin ampelopsin dihydromyricetin apigenin baicalein baicalin catechin egc egcg hispidulin linarin luteolin rc ome skullcap constituents e g baicalin wogonin imidazoles etomidate metomidate methoxyetomidate propoxate isopropoxate butomidate iso butomidate sec butomidate cf2 etomidate cf3 etomidate cf3 propoxate flutomidate 2 6 dichloro 3 fluoroetomidate kava constituents 10 methoxyyangonin 11 methoxyyangonin 11 hydroxyyangonin desmethoxyyangonin 11 methoxy 12 hydroxydehydrokavain 7 8 dihydroyangonin kavain 5 hydroxykavain 5 6 dihydroyangonin 7 8 dihydrokavain 5 6 7 8 tetrahydroyangonin 5 6 dehydromethysticin methysticin 7 8 dihydromethysticin yangonin monoureides acecarbromal apronal apronalide bromisoval carbromal capuride ectylurea neurosteroids acebrochol allopregnanolone brexanolone alfadolone alfaxalone 3α androstanediol androstenol androsterone certain anabolic androgenic steroids cholesterol cortisol hydrocortisone dhdoc 3α dhp 5α dhp 5β dhp dht etiocholanolone etx 155 ganaxolone hydroxydione lpcn 1154 minaxolone nora 520 org 20599 org 21465 p1 185 posovolone prax 114 pregnanolone eltanolone progesterone renanolone sage 105 sage 324 sage 516 sage 689 sage 872 testosterone thdoc zuranolone nonbenzodiazepines cyclopyrrolones eszopiclone pagoclone pazinaclone suproclone suriclone zopiclone imidazopyridines alpidem ds 1 necopidem saripidem zolpidem pyrazolopyrimidines divaplon fasiplon indiplon lorediplon ocinaplon panadiplon taniplon zaleplon others adipiplon axs 17 baer 101 azd 7325 cgs 8216 cgs 9896 cgs 13767 cgs 20625 cl 218 872 cp 615 003 ctp 354 elb 139 enx 102 tpa 023b gbld 345 imepitoin jm 1232 l 838 417 lirequinil ro41 3696 miltirone rosmariquinone ns 2664 ns 2710 ns 11394 ns 11821 pipequaline rod 188 rwj 51204 sb 205 384 sx 3228 tgsc01aa tp 003 tpa 023 tp 13 u 89843a u 90042 viqualine y 23684 phenols cipepofol fospropofol propofol pr...