View source for Talk:Brorphine

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{{SubstanceBox/Brorphine}}

'''Brorphine''' is a recently emerging, highly potent synthetic [[psychoactive class::opioid]] of the [[chemical class::piperidine]] and [[chemical class::benzimidazolone]] chemical class that produces [[pain relief|analgesic]], [[muscle relaxation|relaxing]], [[sedation|sedating]] and [[euphoria|euphoric]] effects when [[Routes of administration|administered]]. It has been seen in an increasing number of detections in seized drug samples since 2019.<ref name="UNODC2020">{{cite web|url=https://www.unodc.org/LSS/Announcement/Details/21380025-9afb-494f-ad1f-d4a371489a65|archive-url=https://webcache.googleusercontent.com/search?q=cache:T4EanAh1pLEJ:https://www.unodc.org/LSS/Announcement/Details/21380025-9afb-494f-ad1f-d4a371489a65+&cd=5&hl=de&ct=clnk&gl=de&client=firefox-b-d|archive-date=October 23, 2020|date=August 2020|title=UNODC EWA: Brorphine, a newly emerging synthetic opioid detected in post-mortem cases|publisher=United Nations Office on Drugs and Crime (UNODC)}}</ref> 

Very little is known about the toxicity of brorphine and it has very little history of human usage. It is currently available as a gray-area [[research chemical]] in many countries. It is strongly advised to use [[responsible drug use|harm reduction practices]] if choosing to use this substance.

==History and culture==
{{historyStub}}
Brorphine was first described in the scientific literature as a μ-opioid receptor agonist in 2018.<ref name="DEA2020"/> It was reported to the UNODC Early Warning Advisory on NPS in 2019.<ref name="UNODC2020"/> In mid-2019 brorphine
emerged in the United States’ drug market.<ref name="DEA2020"/> After the temporarily scheduling of isotonitazene in June 2020 by the Drug Enforcement Administration, detections of brorphine in the U.S. began to increase, appearing as similar gray drug powders and an apparent
replacement for isotonitazene.<ref name="CFSRE2020">{{cite web|title=The Rise of Brorphine — A Potent New Synthetic Opioid Identified in the Midwestern United States|date=July 2020|first1=A. J.|last1=Krotulski|first2=D. M.|last2=Papsun|first3=C.|last3=Noble|first4=S. L.|last4=Kacinko|first5=L.|last5=Nelson|first6=B. K.|last6=Logan|publisher=Center for Forensic Science Research and Education (CFSRE)|url=https://www.npsdiscovery.org/wp-content/uploads/2020/07/Public-Alert_Brorphine_NPS-Discovery_072720.pdf}}</ref>

==Chemistry==
{{chemistry}}
Brorphine is an atypical opioid of the [[piperidine]] and benzimidazolone class which has some structural similarities with [[fentanyl]].<ref name="UNODC2020"/><ref name="CFSRE2020"/> It is comprised of three main units: A 4-bromophenethyl group, a piperidine ring, and a 1,3-dihydro-2H-benzoimidzole-2-one group. Brorphine is being trafficked as its hydrochloride salt which would be water-soluble.<ref name="DEA2020">{{cite web|date=August 2020|title=Brorphine|url=https://www.deadiversion.usdoj.gov/drug_chem_info/brorphine.pdf|publisher=Drug Enforcement Administration (DEA)}}</ref>

==Pharmacology==
{{pharmacology}}
[[Opioids]] exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endorphins which are naturally found in the body and also work with the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. 

''In vitro'' pharmacological data show brorphine exhibits potency similar to [[fentanyl]]<ref name="CFSRE2020"/> and activation of mu-opioid receptors involves recruitment of beta-arrestin-2, a regulatory protein<ref name="DEA2020"/>

==Subjective effects==
{{EffectStub}}
{{Preamble/SubjectiveEffects}}
{{effects/base

|{{effects/physical|


*'''[[Effect::Pain relief]]'''<ref name="DEA2020"/>
*'''[[Effect::Physical euphoria]]'''<ref name="DEA2020"/>
*'''[[Effect::Itchiness]]''' - This compound, like most opioids, tends to cause strong histamine reactions which cause the skin to feel itchy.
*'''[[Effect::Respiratory depression]]'''<ref name="DEA2020"/> 
*'''[[Effect::Sedation]]''' 
*'''[[Effect::Constipation]]'''
*'''[[Effect::Cough suppression]]'''
*'''[[Effect::Difficulty urinating]]'''
*'''[[Effect::Pupil constriction]]'''
*'''[[Effect::Decreased libido]]'''
*'''[[Effect::Appetite suppression]]'''

}}
|{{effects/cognitive|

*'''[[Effect::Cognitive euphoria]]'''<ref name="DEA2020"/>
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Compulsive redosing]]''' 

}}
{{effects/aftereffects|

*'''[[Effect::Cognitive fatigue]]'''
*'''[[Effect::Thought deceleration]]''' 
*'''[[Effect::Anxiety]]'''
*'''[[Effect::Depression]]'''
*'''[[Effect::Irritability]]'''

}}
}}
===Experience reports===
Anecdotal reports which describe the effects of this compound within our [[experience index]] include:
{{#ask: [[Category:Brorphine]][[Category:Experience]]|format=ul|Columns=1}}

==Toxicity and harm potential==
{{toxicity}}
{{Further|Research chemicals#Toxicity and harm potential}}
Brorphine has a [[Toxicity::high toxicity relative to its dose due to its extreme potency]]. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. It is also [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[benzodiazepines]]]].

Recent detections in drug related deaths leads to the conclusion that brorphine has the potential to cause widespread harm.<ref name="CFSRE2020"/> There are no published studies on safety for human use as of August 2020.<ref name="DEA2020"/>

It is strongly recommended that one use [[responsible drug use|harm reduction practices]], and take extreme caution when using this substance.

===Tolerance and addiction potential===
As with other [[opioids]], the chronic use of brorphine can be considered [[Addiction potential::moderately addictive with a high potential for abuse]] and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and [[Opioids#Discontinuation|withdrawal symptoms]] may occur if a person suddenly stops their usage.

Brorphine presents cross-tolerance with [[Cross-tolerance::all other [[opioids]]]], meaning that after the consumption of brorphine all [[opioid]]s will have a reduced effect.

The risk of fatal opioid overdoses rise sharply after a period of cessation and [[relapse]], largely because of reduced tolerance.<ref>Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2</ref> To account for this lack of tolerance, it is safer to only dose a fraction of one's usual [[dosage]] if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.<ref>Siegel, S., Hinson, R., Krank, M., & McCully, J. (1982). Heroin “overdose” death: contribution of drug-associated environmental cues. Science, 216(4544), 436–437. https://doi.org/10.1126/science.7200260</ref>

===Dangerous interactions===
{{DangerousInteractions}}
{{DangerousInteractions/Intro}}
{{DangerousInteractions/Opioids}}

==Legal status==
{{LegalStub}}
Brorphine is not under international control.<ref name="UNODC2020"/>

*'''Turkey:''' Metonitazene is a classed as drug and is illegal to possess, produce, supply, or import.<ref>https://resmigazete.gov.tr/eskiler/2020/10/20201007-8.pdf</ref>
*'''United States''': As of August 2020, brorphine is not controlled under the Controlled Substances Act.<ref name="DEA2020"/>

==See also==
*[[Responsible use]]
*[[Research chemical]]
*[[Depressants]]
*[[Opioid]]

==External links==
*[https://en.wikipedia.org/wiki/Brorphine Brorphine (Wikipedia)]

=References=
{{reflist|2}}

[[Category:Opioid]]
[[Category:Piperidine]] 
[[Category:Benzimidazolone]]
[[Category:Research chemical]]

[[Category:Approval]]
[[Category:Articles in talk page]]

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