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Heroin

Heroin molecule structureHeroin molecule structure
Diacetylmorphine
Diamorphine, H, Smack, Junk, Brown
Psychoactive Class
Chemical Class

Heroin (diacetylmorphinecitation needed) is a semi-synthetic opioid of the morphinan class derived from morphine, a natural product of the opium poppy. First synthesized by a British chemist in 1874 and later commercialized by Bayer in 1898, it is among the most notorious substances of abuse worldwide. Heroin is highly addictive and exists in forms ranging from white or brown powder to black tar1, with street purity varying dramatically from as low as 5% to as high as 95%.

Dosage & Duration

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~5 mg
Light5-20 mg
Moderate20-35 mg
Strong35-50 mg
Heavy50+ mg

Duration

Onset10-60 seconds
Come Up10-60 seconds
Peak1-90 minutes
Offset1-3 hours
After Effects1.5-3 hours
Total3-7 hours

Subjective Effects

Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.

Effects vary widely by individual, dose, and context.

Physical

The physical effects of heroin can be broken down into several components which progressively intensify proportional to dosage.

Cognitive

The cognitive effects of heroin can be broken down into several components which progressively intensify proportional to dosage.

Visual

Forked from Subjective Effect Documentation byJosie Kins July 2015.

Reagent Testing

Expected colorimetric results for common reagent tests. Colors show reaction change over 1–2 minutes.

Marquis(MQ)
white → brown2 → purple2
Mecke(ME)
white → blue2 → green2
Mandelin(MD)
yellow2 → black3
Liebermann(LB)
white → purple2 → black3
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Pharmacology

Pharmacodynamics

Heroin (diamorphine) itself exhibits relatively low affinity for the μ-opioid receptor and functions primarily as a prodrug.citation needed Its pharmacological effects are mediated through its active metabolites morphine and 6-monoacetylmorphine (6-MAM), both of which are μ-opioid receptor agonists. Morphine additionally binds to δ- and κ-opioid receptors.2 These opioid metabolites also decrease the inhibitory activity of GABAergic interneurons, resulting in increased dopamine release.citation needed There is evidence that 6-MAM may bind to a distinct μ-opioid receptor subtype (mu-3), though the contribution of this receptor to heroin's overall pharmacology remains unknown.

Pharmacokinetics

Heroin undergoes rapid deacetylation by esterase enzymes, with a parent compound half-life of approximately two to three minutes.citation needed When taken orally, it is subject to extensive first-pass metabolism, yielding oral bioavailability below 35%. Deacetylation produces the active metabolites 6-monoacetylmorphine (6-MAM) and morphine, along with the inactive 3-monoacetylmorphine. When injected, the acetyl groups confer lipophilicity that allows rapid crossing of the blood-brain barrier before central deacetylation occurs. The majority of the drug is excreted renally as glucuronides, with approximately 7 to 10% eliminated via the biliary system.3

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholBenzodiazepinesCocaineDXMGHB/GBLKetamineMXEPregabalinTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

AmphetaminesMAOIsMephedroneNitrous oxidePCP
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Tolerance

Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.

Full Tolerance
With sustained repeated heroin use, many effects become less responsive. Tolerance does not develop at the same pace for every effect; constipation-related tolerance is especially slow compared with other effects. As a result, users may need progressively higher doses to obtain effects that previously occurred at lower doses.
Baseline Reset
1-2 weeks
Half Tolerance
3-7 days
Cross Tolerance

Opioids (all other opioid receptor agonists will have reduced effect after heroin consumption)

Harm Potential

Addiction & Dependence

Psychological

Extremely High

Heroin is considered extremely addictive with a high potential for abuse.citation needed The combination of powerful euphoric effects and rapid tolerance development leads many users to compulsive redosing and difficulty controlling their use. Psychological dependence can develop quickly, often accompanied by cravings and loss of interest in other activities.

Physical

High

Profound physical dependence develops with repeated use. Withdrawal symptoms may begin within 2-6 hours of the last dose and include sweating, anxiety, severe muscle and bone aches, nausea, vomiting, diarrhea, insomnia, and involuntary muscle spasms.citation needed While extremely unpleasant, opioid withdrawal is generally not life-threatening.4 Tolerance decreases significantly after periods of abstinence, making relapse particularly dangerous.citation needed

Toxicity

Respiratory

Respiratory depression is the primary mechanism of overdose death; heavy doses suppress breathing proportionally to the amount consumed, potentially reducing breathing rate to 2-4 breaths per minute.

Central Nervous System

Repeated use alters brain structure and physiology, with studies showing some deterioration of white matter in chronic users; these changes may affect decision-making, behavior regulation, and stress responses.citation needed

Auditory

Heroin is known to be ototoxic, causing hearing loss, tinnitus, and balance issues; effects may persist long after use.citation needed

Gastrointestinal

Constipation is a common and persistent effect with regular use, representing one of the few direct long-term complications of unadulterated heroin.

Urinary

Urinary retention and difficulty urinating can occur with chronic and repeated use.

Cardiovascular

Decreased heart rate and hypotension occur during intoxication; heroin use has been associated with myocardial infarction.5

Renal

Decreased kidney function (nephropathy) has been reported in intravenous users.citation needed

Pulmonary

Heroin inhalation has rarely caused toxic leukoencephalopathycitation needed and has been documented to cause severe acute asthma attacks or exacerbation of underlying asthma, potentially resulting in death.

History & Culture

Discovery and Synthesis

Diamorphine was first synthesized in 1874 by C.R. Alder Wright, an English chemist working at St. Mary's Hospital Medical School in London.citation needed Wright had been experimenting with combining morphine with various acids, achieving the synthesis by boiling anhydrous morphine alkaloid with

Legality

International

1961 Convention: Schedule I.

1971 Convention: not internationally scheduled.

1988 Convention: not internationally scheduled.

By Country

Illegal19
United States flagUnited StatesIllegal
Australia flagAustraliaSchedule I (Narcotic Drugs Act)
Austria flagAustriaIllegal
Brazil flagBrazilIllegal
Colombia flagColombiaIllegal
Finland flagFinlandIllegal
India flagIndiaIllegal
Italy flagItalyIllegal
Japan flagJapanIllegal
Latvia flagLatviaIllegal
Mexico flagMexicoIllegal
Netherlands flagNetherlandsIllegal
New Zealand flagNew ZealandIllegal
Norway flagNorwayIllegal
Poland flagPolandIllegal
Russia flagRussiaIllegal
Singapore flagSingaporeIllegal
South Africa flagSouth AfricaIllegal
Ukraine flagUkraineIllegal
Prescription5
Canada flagCanadaPrescription only
Germany flagGermanyPrescription only
Spain flagSpainPrescription only
Switzerland flagSwitzerlandPrescription only
United Kingdom flagUnited KingdomPrescription only
Legal / decriminalized2
Czech Republic flagCzech RepublicDecriminalized
Portugal flagPortugalDecriminalized

References

Source Pages

  1. Drug Users Bible by Dominic Milton Trott
  2. DrugBank
  3. DrugBank: Diamorphine Category
  4. DrugBank: Diamorphine Salt
  5. DrugBank: Oral Diacetylmorphine Study
  6. DrugBank: Swiss Medical Use
  7. Erowid
  8. Erowid: Heroin Basics
  9. Erowid: Heroin Dosage
  10. Isomer Design (TiHKAL/PiHKAL)
  11. PsychonautWiki
  12. TripSit Factsheets
  13. TripSit Wiki
  14. TripSit: Combo Chart
  15. Wikipedia

Citations

  1. Heroin. National Institute on Drug Abuse (n.d.). https://nida.nih.gov/research-topics/heroin1
  2. Milella MS, D'Ottavio G, De Pirro S, Barra M, Caprioli D, & Badiani A. (2023-04-08). Heroin and its metabolites: relevance to heroin use disorder. Translational Psychiatry, 13, 120. https://doi.org/10.1038/s41398-023-02406-51
  3. Diamorphine Hydrochloride 10mg for Injection. electronic medicines compendium (emc) (6 May 2020). https://www.medicines.org.uk/emc/product/1466/smpc12
  4. Fred K. Berger, MD. (n.d.). Opiate and opioid withdrawal: MedlinePlus Medical Encyclopedia. medlineplus.gov. https://medlineplus.gov/ency/article/000949.htm1
  5. Ritu Karoli, J. Fatima, Pushker Singh, & Khursheed I. Kazmi. (July 2012). Acute myocardial involvement after heroin inhalation. Journal of Pharmacology & Pharmacotherapeutics, 3(3), 282–4. https://doi.org/10.4103/0976-500x.994481
  6. When Heroin Hit Jazz. City Journal (n.d.). https://www.city-journal.org/article/when-heroin-hit-jazz1
  7. Decriminalisation of low-level drug possession in the ACT. Hugo Law Group (n.d.). https://hugolawgroup.com.au/insights/decriminalisation-of-low-level-drug-possession-in-the-act/1
  8. Suchtmittelgesetz. ris.bka.gv.at (n.d.). https://www.ris.bka.gv.at/GeltendeFassung.wxe?Abfrage=Bundesnormen&Gesetzesnummer=100110401
  9. Narcotic Substances Act in Austria: Overview of Rules and Penalties. MPW Rechtsanwaelte (n.d.). https://mpw-rechtsanwaelte.com/en/narcotic-substances-act-austria/1
  10. Portaria SVS/MS 344/1998. bvsms.saude.gov.br (n.d.). https://bvsms.saude.gov.br/bvs/saudelegis/svs/1998/prt0344_12_05_1998_rep.html1

Further Reading

  1. EUDA: Heroin Drug Profile
  2. Siegel et al. 1982: Heroin Overdose Death and Environmental Cues
  3. Wright 1874: Synthesis of Diacetylmorphine

Article Status

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    An autonomous workflow built by Josie Kins compiled this article's foundation from information published across the web.

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Recent changes8 human edits · latest

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