Talk:Brorphine

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It may contain incorrect information, particularly with respect to dosage, duration, subjective effects, toxicity and other risks.

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Fatal overdose may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: Brorphine

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Brorphine is a recently emerging, highly potent synthetic opioid of the piperidine and benzimidazolone chemical class that produces analgesic, relaxing, sedating and euphoric effects when administered. It has been seen in an increasing number of detections in seized drug samples since 2019.[2]

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 harm reduction practices if choosing to use this substance.

History and culture

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Brorphine was first described in the scientific literature as a μ-opioid receptor agonist in 2018.[3] It was reported to the UNODC Early Warning Advisory on NPS in 2019.[2] In mid-2019 brorphine emerged in the United States’ drug market.[3] 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.[4]

Chemistry

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Brorphine is an atypical opioid of the piperidine and benzimidazolone class which has some structural similarities with fentanyl.[2][4] 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.[3]

Pharmacology

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Opioids exert their effects by binding to and activating the 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 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[4] and activation of mu-opioid receptors involves recruitment of beta-arrestin-2, a regulatory protein[3]

Subjective effects

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Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy amount of skepticism. It is worth noting that these effects will not necessarily occur in a consistent or reliable manner, although higher doses are more likely to induce the full spectrum of effects. Likewise, adverse effects become much more likely with higher doses and may include serious injury or death.

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:


Toxicity and harm potential

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We also recommend that you conduct independent research and use harm reduction practices when using this substance.

Brorphine has a 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 potentially 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.[4] There are no published studies on safety for human use as of August 2020.[3]

It is strongly recommended that one 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 moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage.

Brorphine presents cross-tolerance with all other opioids, meaning that after the consumption of brorphine all opioids 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.[5] 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.[6]

Dangerous interactions

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Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The list below includes some known dangerous combinations (although it cannot be guaranteed to include all of them). Independent research (e.g. Google, DuckDuckGo) should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from TripSit.

  • Alcohol - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. Place affected patients in the recovery position to prevent vomit aspiration from excess. Memory blackouts are likely
  • Amphetamines - Stimulants increase respiration rate which allows for a higher dose of opiates than would otherwise be used. If the stimulant wears off first then the opiate may overcome the user and cause respiratory arrest.
  • Benzodiazepines - Central nervous system and/or respiratory-depressant effects may be additively or synergistically present. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position blackouts/memory loss likely.
  • Cocaine - Stimulants increase respiration rate, which allows for a higher dose of opiates than would otherwise be used. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
  • DXM - Generally considered to be toxic. CNS depression, difficulty breathing, heart issues, and liver toxicity have been observed. Additionally if one takes DXM, their tolerance of opiates goes down slightly, thus causing additional synergistic effects.
  • GHB/GBL - The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position
  • Ketamine - Both substances bring a risk of vomiting and unconsciousness. If the user falls unconscious while under the influence there is a severe risk of vomit aspiration if they are not placed in the recovery position.
  • MAOIs - Coadministration of monoamine oxidase inhibitors (MAOIs) with certain opioids has been associated with rare reports of severe adverse reactions. There appear to be two types of interaction, an excitatory and a depressive one. Symptoms of the excitatory reaction may include agitation, headache, diaphoresis, hyperpyrexia, flushing, shivering, myoclonus, rigidity, tremor, diarrhea, hypertension, tachycardia, seizures, and coma. Death has occurred in some cases.
  • MXE - MXE can potentiate the effects of opioids but also increases the risk of respiratory depression and organ toxicity.
  • Nitrous - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Memory blackouts are common.
  • PCP - PCP may reduce opioid tolerance, increasing the risk of overdose.
  • Tramadol - Increased risk of seizures. Tramadol itself is known to induce seizures and it may have additive effects on seizure threshold with other opioids. Central nervous system- and/or respiratory-depressant effects may be additively or synergistically present
  • Grapefruit - While grapefruit is not psychoactive, it may affect the metabolism of certain opioids. Tramadol, oxycodone, and fentanyl are all primarily metabolized by the enzyme CYP3A4, which is potently inhibited by grapefruit juice[7]. This may cause the drug to take longer to clear from the body. it may increase toxicity with repeated doses. Methadone may also be affected[7]. Codeine and hydrocodone are metabolized by CYP2D6. People who are on medicines that inhibit CYP2D6, or that lack the enzyme due to a genetic mutation will not respond to codeine as it can not be metabolized into its active product: morphine.

Legal status

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Brorphine is not under international control.[2]

  • United States: As of August 2020, brorphine is not controlled under the Controlled Substances Act.[3]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. 2.0 2.1 2.2 2.3 "UNODC EWA: Brorphine, a newly emerging synthetic opioid detected in post-mortem cases". United Nations Office on Drugs and Crime (UNODC). August 2020. Archived from the original on October 23, 2020. 
  3. 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 3.8 3.9 "Brorphine" (PDF). Drug Enforcement Administration (DEA). August 2020. 
  4. 4.0 4.1 4.2 4.3 Krotulski, A. J.; Papsun, D. M.; Noble, C.; Kacinko, S. L.; Nelson, L.; Logan, B. K. (July 2020). "The Rise of Brorphine — A Potent New Synthetic Opioid Identified in the Midwestern United States" (PDF). Center for Forensic Science Research and Education (CFSRE). 
  5. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  6. 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
  7. 7.0 7.1 [1]