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nesia hong kong and singapore prescriptions for the drug have decreased dramatically since 2005 due to rampant misuse and addiction it is primarily used as an anticonvulsant in children it is also still used in the most severe and debilitating cases of insomnia in an inpatient setting or in short term outpatient treatment hypnotic benzodiazepines estazolam and nitrazepam are used more frequently than nimetazepam for this purpose antidepressants such as trazodone and mirtazapine or z drugs like zopiclone and zolpidem are first line treatment for insomnia although prescriptions for nimetazepam have decreased abuse of the drug is still significant in brunei singapore malaysia and the philippines it is commonly used in combination with methamphetamine and mdma ecstasy and opiates especially heroin or morphine the strict legal restrictions nimetazepam is subject to in malaysia has made the drug scarce but many pills sold as nimetazepam in the black market are counterfeit diazepam and nitrazepam are among the most commonly prescribed benzodiazepines in the region and as a result they are commonly diverted and sold on the black market often as nimetazepam illicit manufacturing of nimetazepam sold as erimin 5 is prevalent in the region abuse of nimetazepam continued to rise throughout the 2010s seizures of illicitly manufactured erimin 5 tablets paralleled the seizures of methamphetamine seizures in malaysia a small seizure of 46 illicit erimin 5 tablets were tested for their physical and chemical characteristics the active ingredient adulterant major diluent and dyes make up the chemical characteristics of a tablet the results indicated that nimetazepam was the most common active ingredient in the vast majority of the tablets seized lactose was detected as a major diluent in the majority of the samples followed by mannitol and then calcium phosphate dibasic dihydrate sunset yellow was found in most of the tablet samples either alone or in combination with other dyes such as tartrazine and ponceau 4r to give the tablets a peach orange colour green tablets in the samples contained brilliant blue and tartrazine dyes diazepam which is primarily an anxiolytic was the active ingredient in only one tablet out of the 46 nitrazepam a powerful sedative hypnotic which is also nimetazepams parent drug was found to be a minor compound together with a caffeine as a major compound in three of the tablets 4 in 2003 94 200 erimin 5 tablets were seized in singapore the central narcotics bureau s cnb laboratory tested the tablets with results that confirmed the tablets were indeed nimetazepam pharmacokinetics edit taken orally nimetazepam has very good bioavailability with nearly 100 being absorbed from the gut it is among the most rapidly absorbed and quickest acting oral benzodiazepines and hypnotic effects are typically felt within 15 30 minutes after oral ingestion the blood level decline of the parent drug was biphasic with the short half life ranging from 0 5 0 7 hours and the terminal half life from 8 to 26 5 hours mean 17 25 hours citation needed it is the n methylated analogue of nitrazepam mogadon alodorm to which it is partially metabolized nitrazepam has a long elimination half life so effects of repeated dosage tend to be cumulative recreational use edit see also benzodiazepine drug misuse there is a risk of misuse and dependence in both patients and non medical users of nimetazepam the pharmacological properties of nimetazepam such as high affinity binding high potency being short to intermediate acting and having a rapid onset of action increase the abuse potential of nimetazepam the physical dependence and withdrawal syndrome of nimetazepam also adds to the addictive nature of nimetazepam nimetazepam has a particular reputation in south east asia for recreational use at around usd 7 per tab and is particularly popular among persons addicted to amphetamines or opioids 5 6 in addition nimetazepam has an anti depressant and muscle relaxant effect 7 nimetazepam also has withdrawal suppression effect and lower drug seeking versus nitrazepam in rhesus monkey macaca mulatta 8 which might help stimulant addicts to overcome withdrawal symptoms drug misuse edit nimetazepam has a reputation for being particularly subject to abuse known as happy 5 sold as an ecstasy replacement without a hangover although is still a significant drug of abuse in some asian countries such as japan and malaysia nimetazepam is subject to legal restrictions in malaysia and due to its scarcity many tablets sold on the black market are in fact counterfeits containing other benzodiazepines such as diazepam or nitrazepam instead 9 10 11 legal status edit in the united states nimetazepam is categorized schedule iv fda and dea nimetazepam is currently a schedule iv drug under the international convention on psychotropic substances of 1971 12 in singapore nimetazepam is a physician prescribed drug and is regulated under the misuse of drugs act 13 the illegal possession or consumption of nimetazepam is punishable by up to 10 years of imprisonment a fine of 20 000 singapore dollars or both importing or exporting nimetazepam is punishable by up to 20 years of imprisonment and or caning in hong kong nimetazepam is regulated under schedule 1 of hong kong s chapter 134 dangerous drugs ordinance nimetazepam can only be used legally by health professionals and for university research purposes the substance can be given by pharmacists under a prescription anyone who supplies the substance without prescription can be fined 10000 hkd the penalty for trafficking or manufacturing the substance is a 5 000 000 hkd fine and life imprisonment possession of the substance for consumption without license from the department of health is illegal with a 1 000 000 hkd fine and or 7 years of jail time 14 similarly in taiwan and indonesia nimetazepam is also regulated as a controlled prescribed substance in victoria australia nimetazepam is regulated under schedule 11 of drugs poisons and controlled substances act 1981 it is deemed to fall under the category of 7 nitro 1 4 benzodiazepines not included elsewhere in this part 15 toxicity edit in a rat study nimetazepam showed greater damage to the fetus as did nitrazepam when compared against other benzodiazepines all at a dosage of 100 mg kg diazepam however showed relatively weak fetal toxicities 16 the same fetotoxicity of nitrazepam could not be observed in mice and is likely due to the particular metabolism of the drug in the rat 17 in a rat study nimetazepam showed slight enlargement of the liver and adrenals and atrophy of the testes and ovaries were found in high dose groups of both drugs at the 4th and 12th week however in histopathological examination there were no change in the liver adrenals and ovaries degenerative changes of seminiferous epithelium in the testes were observed but these atrophic change returned to normal by withdrawal of the drugs for 12 weeks 18 see also edit benzodiazepines flunitrazepam fluorinated derivative nifoxipam fluorinated 3 hydroxylated desmethyl derivative nitemazepam 3 hydroxy derivative nitrazepam desmethyl derivative temazepam related hypnotic with similar side effects profile 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 us patent 3109843 reeder e sternbach lh process for preparing 5 phenyl 1 2 dihydro 3h 1 4 benzodiazepines issued 1963 11 05 assigned to hoffmann la roche fukinaga m ishizawa k kamei c november 1998 anticonvulsant properties of 1 4 benzodiazepine derivatives in amygdaloid kindled seizures and their chemical structure related anticonvulsant action pharmacology 57 5 233 41 doi 10 1159 000028247 pmid 9742288 s2cid 25773207 kunalan v 2012 forensic drug profiling of erimin 5 using tlc and gc ms malaysian journal of forensic sciences 3 1 14 via researchgate chong yk kaprawi mm chan kb 2004 the quantitation of nimetazepam in erimin 5 tablets and powders by reverse phase hplc microgram journal 2 1 4 27 33 archived from the original on 2011 08 10 retrieved 2011 12 07 devaney m reid g baldwin s 2005 situational analysis of illicit drug issues and responses in the asia pacific region pdf ancd research paper 12 canberra australian national council on drugs sakai s kitagawa s yamamoto h march 1972 pharmacological studies on 1 methyl 7 nitro 5 phenyl 1 3 dihydro 2h 1 4 benzodiazepin 2 one s 1530 arzneimittel forschung 22 3 534 9 pmid 5067925 yanagita t takahashi s oinuma n drug dependence liability of nimetazepam evaluated in the rhesus monkey cite journal cite journal requires journal help abdullah af abraham aa sulaiman m kunalan v 2012 forensic drug profiling of erimin 5 using tlc and gc ms malaysian journal of forensic sciences 3 1 12 15 binti abdul rahim rusdiyah profiling of illicit erimin 5 tablet seized in malaysia a research project report submitted to the department of chemistry faculty of science university of malaya erimin 5 tablets in singapore the centre for forensic science hsa singapore 2006 list of psychotropic substances under international control pdf green list annex to the annual statistical report on psychotropic substances form p 23rd ed international narcotics control board august 2003 archived from the original pdf on 2012 08 31 retrieved 2011 12 06 misuse of drugs act chapter 185 archived from the original on 2012 02 15 retrieved 2011 09 08 bilingual laws information system the government of the hong kong special administrative region of the people s republic of china victorian legislation and parliamentary documents the state government victoria saito h kobayashi h takeno s sakai t december 1984 fetal toxicity of benzodiazepines in rats research communications in chemical pathology and pharmacology 46 3 437 47 pmid 6151222 takeno s hirano y kitamura a sakai t august 1993 comparative developmental toxicity and metabolism of nitrazepam in rats and mice toxicology and applied pharmacology 121 2 233 8 bibcode 1993toxap 121 233t doi 10 1006 taap 1993 1150 pmid 8346540 yamamoto t kato t wada h kerata y 1972 chronic toxicity of 1 methyl 7 nitro 5 phenyl 1 3 dihydro 2h 1 4 benzodiazepin 2 one nimetazepam in rats chronic toxicity 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 doxefazepam estazolam flubromazolam flunitrazolam flunitrazepam flurazepam flutemazepam flutoprazepam loprazolam lormetazepam midazolam nimetazepam nitemazepam nitrazepam nitrazolam quazepam temazepam triazolam carbamates carisoprodol emylcamate ethinamate hexapropymate meprobamate methocarbamol phenprobamate procymate tybamate imidazoles etomidate metomidate propoxate monoureides acecarbromal apronal apronalide bromisoval capuride carbromal ectylurea neurosteroids acebrochol alfadolone alfaxolone brexanolone allopregnanolone eltanolone pregnanolone ganaxolone hydroxydione minaxolone progesterone renanolone zuranolone nonbenzodiazepines eszopiclone indiplon lirequinil necopidem pagoclone pazinaclone saripidem suproclone suriclone zaleplon zolpidem zopiclone phenols cipepofol ciprofol fospropofol propofol propofol hemisuccinate piperidinediones glutethimide methyprylon piperidione pyrithyldione quinazolinones afloqualone cloroqualone diproqualone etaqualone mebroqualone mecloqualone methaqualone methylmethaqualone nitromethaqualone sl 164 others acetophenone acetylglycinamide chloral hydrate bromide compounds lithium bromide potassium bromide sodium bromide centalun chloral betaine chloral hydrate chloralose clomethiazole dichloralphenazone gaboxadol thip ibotenic acid amanita muscaria kavalactones loreclezole muscimol amanita muscaria paraldehyde petrichloral sesquiterpene isovaleramide isovaleric acid valerenic acid sulfonylalkanes sulfonmethane sulfonal tetronal trional triclofos gaba b 1 4 butaned...