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e of contents brotizolam 21 languages العربية deutsch español euskara فارسی suomi français עברית hrvatski magyar italiano 日本語 nederlands polski português română srpskohrvatski српскохрватски српски srpski svenska tiếng việt 中文 edit links article talk english read edit view history tools tools move to sidebar hide actions read edit view history general what links here related changes upload file permanent link page information cite this page get shortened url switch to legacy parser print export download as pdf printable version in other projects wikimedia commons wikidata item appearance move to sidebar hide from wikipedia the free encyclopedia thienotriazolodiazepine drug pharmaceutical compound brotizolam clinical data trade names lendormin others ahfs drugs com international drug names routes of administration oral atc code n05cd09 who legal status legal status br class b1 psychoactive drugs 1 ca schedule iv de prescription only anlage iii for higher doses uk class c us unscheduled 2 un schedule iv pharmacokinetic data bioavailability 48 95 metabolism hepatic elimination half life 4 4 hours range 2 6 6 9 h excretion renal identifiers iupac name 2 bromo 4 2 chlorophenyl 9 methyl 6 h thieno 3 2 f 1 2 4 triazolo 4 3 a 1 4 diazepine cas number 57801 81 7 n pubchem cid 2451 drugbank db09017 n chemspider 2357 y unii 5xzm1r3dkf kegg d01744 y chebi chebi 31308 chembl chembl32479 y comptox dashboard epa dtxsid0022692 echa infocard 100 055 404 chemical and physical data formula c 15 h 10 br cl n 4 s molar mass 393 69 g mol 1 3d model jsmol interactive image smiles clc1 cc cc c1c2 ncc3 nn c c n3c4 c2c c br s4 inchi inchi 1s c15h10brcln4s c1 8 19 20 13 7 18 14 9 4 2 3 5 11 9 17 10 6 12 16 22 15 10 21 8 13 h2 6h 7h2 1h3 y key umsgktjduherqw uhfffaoysa n y n y what is this verify brotizolam 3 sold under the brand name lendormin among others is a sedative hypnotic 4 thienotriazolodiazepine 5 drug which is a benzodiazepine analog 6 it possesses anxiolytic anticonvulsant hypnotic sedative and skeletal muscle relaxant properties and is considered to be similar in effect to other short acting hypnotic benzodiazepines such as triazolam or midazolam 7 it is used in the short term treatment of severe insomnia brotizolam is a highly potent and short acting hypnotic with a typical dose ranging from 0 125 to 0 25 milligrams which is rapidly eliminated with an average half life of 4 4 hours range 3 6 7 9 hours 8 it was patented in 1974 9 and came into medical use in 1984 10 brotizolam is not approved for sale in the uk united states or canada it is approved for sale in the netherlands germany spain belgium luxembourg austria portugal israel italy taiwan and japan medical uses edit brotizolam is prescribed for the short term treatment 2 4 weeks of severe or debilitating insomnia brotizolam is a short acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or getting to sleep hypnotics should only be used on a short term basis or in those with chronic insomnia on an occasional basis 11 brotizolam in a dose of 0 25 mg can be used as a premedication prior to surgery this dose was found to be comparable in efficacy to 2 mg flunitrazepam as a premedicant prior to surgery 12 side effects edit common side effects of brotizolam are typical of hypnotic benzodiazepines are related to cns depression and can include somnolence ataxia headache anterograde amnesia dizziness fatigue impairment of motor functions slurred speech confusion and clumsiness less common side effects include hypotension respiratory depression hallucinations nausea and vomiting palpitations and paradoxical reactions i e aggression anxiety violent behavior etc brotizolam can cause residual side effects the next day such as impaired cognitive and motor functions as well as drowsiness disruption of sleep patterns may also occur such as suppression of rem sleep these side effects are more likely at higher doses above 0 5 1 mg 13 in clinical trials brotizolam 0 125 to 0 5 mg improved sleep in insomniacs similarly to nitrazepam 2 5 and 5 mg flunitrazepam 2 mg and triazolam 0 25 mg whilst brotizolam 0 5 mg was shown to be superior to flurazepam 30 mg but inferior to temazepam 30 mg in some studies brotizolam at dosages below 0 5 mg at night usually produced minimal morning drowsiness no residual impairment of psychomotor performance occurs following dosages within the recommended range of 0 125 to 0 25 mg no serious side effects have been reported to date and the most frequently observed adverse experiences are drowsiness headache and dizziness mild rebound insomnia may occur in some patients when treatment is stopped 8 contraindications edit thienodiazepines and benzodiazepines require special precaution if used in the elderly during pregnancy in children alcohol or drug dependent individuals and individuals with comorbid psychiatric disorders 14 pharmacology edit brotizolam has been shown in animal studies to be a very high potency thienodiazepine the elimination half life of brotizolam is 3 6 hours it is absorbed rapidly after administration into active metabolites one of which is far less potent than brotizolam and the other is only present in very small amounts in the blood thus the metabolites of brotizolam do not have significant pharmacological effect in humans 6 brotizolam induces impairment of motor function and has hypnotic properties 15 brotizolam increases the slow wave light sleep swls in a dose dependent manner whilst suppressing deep sleep stages less time is spent in stages 3 and 4 which are the deep sleep stages when gabaergics such as brotizolam are used benzodiazepines and thienodiazepines are therefore not ideal hypnotics in the treatment of insomnia the suppression of deep sleep stages may be especially problematic in the elderly as they naturally spend less time in the deep sleep stage 16 society and culture edit abuse edit see also benzodiazepine use disorder abuse of brotizolam although not widespread was a problem in hong kong in the late 1980s and early 1990s to control benzodiazepine abuse in hong kong the government s pharmacy and poisons board reclassified benzodiazepines as dangerous drugs in october 1990 alongside formal prescriptions detailed records were required for the supply and dispensing of these drugs these regulations were applied initially only to brotizolam triazolam and flunitrazepam as they were the major benzodiazepines being abused following these regulations the sales of flunitrazepam and triazolam fell in 1991 but the sales of five unrestricted benzodiazepines increased 17 particular problems then arose with the trafficking and abuse of nimetazepam and the abuse of temazepam the regulations were then extended to include all benzodiazepines by january 1992 this appears to have curbed at least partially their abuse in hong kong there are still some problems with temazepam nimetazepam triazolam and brotizolam but they are not major brand names edit name countries bondormin brotizolam israel dormex chile lendorm austria denmark lendormin south africa belgium germany hungary italy japan netherlands portugal taiwan lendormine switzerland lindormin mexico noctilan chile sintonal spain see also edit benzodiazepine dependence benzodiazepine withdrawal syndrome bromazepam bromazolam loprazolam flubrotizolam fluclotizolam 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 dea diversion control division pdf archived from the original pdf on 2019 10 17 retrieved 2015 12 10 us 4094984 6 phenyl 8 bromo 4h s triazolo 3 4c thieno 2 3e 1 4 diazepines and salts thereof fink m irwin p september 1981 pharmacoelectroencephalographic study of brotizolam a novel hypnotic clinical pharmacology and therapeutics 30 3 336 42 doi 10 1038 clpt 1981 169 pmid 7273596 s2cid 30788171 catabay a taniguchi m jinno k pesek jj williamsen e 1 march 1998 separation of 1 4 benzodiazepines and analogues using cholesteryl 10 undecenoate bonded phase in microcolumn liquid chromatography journal of chromatographic science 36 3 113 doi 10 1093 chromsci 36 3 111 1 2 jochemsen r wesselman jg van boxtel cj hermans j breimer dd 1983 comparative pharmacokinetics of brotizolam and triazolam in healthy subjects british journal of clinical pharmacology 16 suppl 2 291s 297s doi 10 1111 j 1365 2125 1983 tb02303 x pmc 1428224 pmid 6140948 mandrioli r mercolini l raggi ma october 2008 benzodiazepine metabolism an analytical perspective current drug metabolism 9 8 827 44 doi 10 2174 138920008786049258 pmid 18855614 1 2 langley ms clissold sp february 1988 brotizolam a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic drugs 35 2 104 22 doi 10 2165 00003495 198835020 00002 pmid 3281819 s2cid 243228878 us4094984 6 phenyl 8 bromo 4h s triazolo 3 4c thieno 2 3e 1 4 diazepines and salts thereof fischer j ganellin cr 2006 analogue based drug discovery john wiley sons p 539 isbn 9783527607495 rickels k 1986 the clinical use of hypnotics indications for use and the need for a variety of hypnotics acta psychiatrica scandinavica supplementum 332 132 41 doi 10 1111 j 1600 0447 1986 tb08990 x pmid 2883820 s2cid 46560074 nishiyama t yamashita k yokoyama t imoto a manabe m 2007 effects of quazepam as a preoperative night hypnotic comparison with brotizolam journal of anesthesia 21 1 7 12 doi 10 1007 s00540 006 0445 2 pmid 17285406 s2cid 24584685 nicholson an stone bm pascoe pa july 1980 studies on sleep and performance with a triazolo 1 4 thienodiazepine brotizolam british journal of clinical pharmacology 10 1 75 81 doi 10 1111 j 1365 2125 1980 tb00504 x pmc 1430017 pmid 7397057 authier n balayssac d sautereau m zangarelli a courty p somogyi aa et al november 2009 benzodiazepine dependence focus on withdrawal syndrome benzodiazepine dependence focus on withdrawal syndrome annales pharmaceutiques françaises in french 67 6 408 13 doi 10 1016 j pharma 2009 07 001 pmid 19900604 yasui m kato a kanemasa t murata s nishitomi k koike k et al june 2005 pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes nihon shinkei seishin yakurigaku zasshi japanese journal of psychopharmacology 25 3 143 51 pmid 16045197 noguchi h kitazumi k mori m shiba t march 2004 electroencephalographic properties of zaleplon a non benzodiazepine sedative hypnotic in rats journal of pharmacological sciences 94 3 246 51 doi 10 1254 jphs 94 246 pmid 15037809 lee kk chan ty chan aw lau gs critchley ja 1995 use and abuse of benzodiazepines in hong kong 1990 1993 the impact of regulatory changes journal of toxicology clinical toxicology 33 6 597 602 doi 10 3109 15563659509010615 pmid 8523479 further reading edit greenblatt dj locniskar a shader ri 1983 pilot pharmacokinetic study of brotizolam a thienodiazepine hypnotic using electron capture gas liquid chromatography sleep 6 1 72 6 doi 10 1093 sleep 6 1 72 pmid 6844800 langley ms clissold sp february 1988 brotizolam a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic drugs 35 2 104 22 doi 10 2165 00003495 198835020 00002 pmid 3281819 s2cid 243228878 bechtel wd 1983 pharmacokinetics and metabolism of brotizolam in humans british journal of clinical pharmacology 16 suppl 2 279s 283s doi 10 1111 j 1365 2125 1983 tb02301 x pmc 1428235 pmid 6661373 jochemsen r wesselman jg hermans j van boxtel cj breimer dd 1983 pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration british journal of clinical pharmacology 16 suppl 2 285s 290s doi 10 1111 j 1365 2125 1983 tb02302 x pmc 1428208 pmid 6661374 external links edit inchem org brotizolam 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 hypnotics sedatives n05c gaba a alcohols 2m2b chloralodol ethanol alcohol diethylpropanediol ethchlorvynol methylpentynol trichloroethanol barbiturates allobarbital amobarbital aprobarbital barbital butabarbital butobarbital cyclobarbital ethallobarbital heptabarb hexobarbital mephobarbital methohexital narcobarbital pentobarbital phenallymal phenobarbital propylbarbital proxibarbal reposal secobarbital talbutal thiamylal thiopental thiotetrabarbital vinbarbital vinylbital benzodiazepines brotizolam cinolazepam climazolam clobazam clonazolam doxe...