Heroin
Heroin (diacetylmorphine1) is a semi-synthetic opioid of the morphinan class derived from morphine1, a natural product of the opium poppy1. First synthesized by a British chemist in 18741 and later commercialized by Bayer in 18982, it is among the most notorious substances of abuse worldwide. Heroin is highly addictive3 and exists in forms ranging from white or brown powder to black tar4, with street purity varying dramatically from as low as 5% to as high as 95%.
Contents
Dosage & Duration
Dosage
Duration
Subjective Effects
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
Reagent Testing
Loading reagent data
Pharmacology
Pharmacodynamics
Heroin (diamorphine) itself exhibits relatively low affinity for the μ-opioid receptor and functions primarily as a prodrug.1 Its pharmacological effects are mediated through its active metabolites morphine and 6-monoacetylmorphine (6-MAM), both of which are μ-opioid receptor agonists.1 Morphine additionally binds to δ- and κ-opioid receptors.1 These opioid metabolites also decrease the inhibitory activity of GABAergic interneurons, resulting in increased dopamine release.1 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.51 When taken orally, it is subject to extensive first-pass metabolism, yielding oral bioavailability below 35%.6 Deacetylation produces the active metabolites 6-monoacetylmorphine (6-MAM) and morphine, along with the inactive 3-monoacetylmorphine.1 When injected, the acetyl groups confer lipophilicity that allows rapid crossing of the blood-brain barrier before central deacetylation occurs.51 The majority of the drug is excreted renally as glucuronides, with approximately 7 to 10% eliminated via the biliary system.5
Dangerous
Highest riskThese 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.
Unsafe
AvoidThere is considerable risk of physical harm when taking these combinations, they should be avoided where possible.
Caution
Use cautionThese 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.
Tolerance
Opioids (all other opioid receptor agonists will have reduced effect after heroin consumption)
Harm Potential
Addiction & Dependence
Psychological
Extremely HighHeroin is considered extremely addictive with a high potential for abuse.7 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
HighProfound 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.8 While extremely unpleasant, opioid withdrawal is generally not life-threatening.8 Tolerance decreases significantly after periods of abstinence, making relapse particularly dangerous.8
Toxicity
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.
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.11
Heroin is known to be ototoxic, causing hearing loss, tinnitus, and balance issues; effects may persist long after use.12
Constipation is a common and persistent effect with regular use, representing one of the few direct long-term complications of unadulterated heroin.
Urinary retention and difficulty urinating can occur with chronic and repeated use.
Decreased heart rate and hypotension occur during intoxication; heroin use has been associated with myocardial infarction.13
Decreased kidney function (nephropathy) has been reported in intravenous users.15
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.20 Wright had been experimenting with combining morphine with various acids, achieving the synthesis by boiling anhydrous…
Legality
International
1961 Convention: Schedule I.
1971 Convention: not internationally scheduled.
1988 Convention: not internationally scheduled.
By Country
References
Source Pages
Drug Users Bible by Dominic Milton Trott
DrugBank
DrugBank: Diamorphine Category
DrugBank: Diamorphine Salt
DrugBank: Oral Diacetylmorphine Study
DrugBank: Swiss Medical Use
Erowid
Erowid: Heroin Basics
Erowid: Heroin Dosage
Isomer Design (TiHKAL/PiHKAL)
PsychonautWiki
TripSit Factsheets
TripSit Wiki
TripSit: Combo Chart
Wikipedia
Citations
- 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/s41398-023-02406-51234567891011
- (n.d.). Heroin Bottle. DEA Museum. https://museum.dea.gov/museum-collection/collection-spotlight/artifact/heroin-bottle1
- (n.d.). Heroin. Drug Enforcement Administration. https://www.dea.gov/factsheets/heroin1
- (n.d.). Heroin. National Institute on Drug Abuse. https://nida.nih.gov/research-topics/heroin1
- (6 May 2020). Diamorphine Hydrochloride 10mg for Injection. electronic medicines compendium (emc). https://www.medicines.org.uk/emc/product/1466/smpc1234
- (December 2008). Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure. British Journal of Clinical Pharmacology, 66(6), 781–91. https://doi.org/10.1111/j.1365-2125.2008.03286.x12
- (October 2014). DrugFacts—Heroin. National Institute on Drug Abuse. https://www.drugabuse.gov/publications/drugfacts/heroin1
- (n.d.). Opiate and opioid withdrawal: MedlinePlus Medical Encyclopedia. medlineplus.gov. https://medlineplus.gov/ency/article/000949.htm123
- (n.d.). Opioid overdose. World Health Organization. https://www.who.int/news-room/fact-sheets/detail/opioid-overdose1
- (December 1996). Fatal heroin 'overdose': a review. Addiction, 91(12), 1765–72. https://doi.org/10.1046/j.1360-0443.1996.911217652.x1
- (2019). [Substance Abuse and White Matter: Findings, Limitations, and Future of Diffusion Tensor Imaging Research]. Drug and Alcohol Dependence, 197(4), 288–298. https://doi.org/10.1016/j.drugalcdep.2019.02.0051
- Mozeika AM, Ruck BE, Nelson LS, & Calello DP. (2020). Opioid-Associated Hearing Loss: A 20-Year Review from the New Jersey Poison Center. Journal of Medical Toxicology. https://doi.org/10.1007/s13181-020-00785-51
- (July 2012). Acute myocardial involvement after heroin inhalation. Journal of Pharmacology & Pharmacotherapeutics, 3(3), 282–4. https://doi.org/10.4103/0976-500x.994481
- Miro JM, del Rio A, & Mestres CA. (2003). Infective endocarditis in intravenous drug abusers. Current Infectious Disease Reports. https://doi.org/10.1007/s11908-003-0012-91
- (January 2005). Heroin-associated nephropathy. Expert Opinion on Drug Safety, 4(1), 19–28. https://doi.org/10.1517/14740338.4.1.1912
- (February 2008). Heroin-induced leukoencephalopathy: characterization using MRI, diffusion-weighted imaging, and MR spectroscopy. Clinical Radiology, 63(2), 146–152. https://doi.org/10.1016/j.crad.2007.07.0211
- (2011). Chasing the dragon - characterizing cases of leukoencephalopathy associated with heroin inhalation in British Columbia. Harm Reduction Journal, 8(1), 3. https://doi.org/10.1186/1477-7517-8-31
- (10 December 1988). Heroin inhalation and asthma.. BMJ, 297(6662), 1511–1512. https://doi.org/10.1136/bmj.297.6662.15111
- (February 2003). Heroin Insufflation as a Trigger for Patients With Life-Threatening Asthma. Chest, 123(2), 510–517. https://doi.org/10.1378/chest.123.2.5101
- (2023-05-30). From poppy to morphine and heroin. Hektoen International. https://hekint.org/2023/05/30/from-poppy-to-morphine-and-heroin/1
- (n.d.). Felix Hoffmann. Science History Institute. https://www.sciencehistory.org/education/scientific-biographies/felix-hoffmann/123
- (n.d.). Pharmacy's Past: Chemist Discovers Aspirin and Heroin. Pharmacy Times. https://www.pharmacytimes.com/view/pharmacys-past-chemist-discovers-aspirin-and-heroin1
- (n.d.). The Pharmaceutical Company Bayer Coined the Name "Heroin" and Marketed the Drug as a Non-Addictive Cough Medicine. Today I Found Out. http://www.todayifoundout.com/index.php/2012/02/the-pharmaceutical-company-bayer-coined-the-name-heroin-and-marketed-the-drug-as-a-non-addictive-cough-medicine/1234
- (n.d.). 1911 Encyclopædia Britannica/Morphine. Wikisource. https://en.wikisource.org/wiki/1911_Encyclop%C3%A6dia_Britannica/Morphine1
- (n.d.). A History of Opiate opioid Laws in the United States. NAABT. https://www.naabt.org/laws.cfm12
- (n.d.). Tracing France's History in the Heroin Trade. Vice. https://www.vice.com/en/article/french-connection-kevin-perry-marseille/1
- (n.d.). Perspectives on drugs: opioid trafficking routes from Asia to Europe. European Union Drugs Agency (EUDA). https://www.euda.europa.eu/topics/pods/opioid-trafficking-routes_en1
- (n.d.). When Heroin Hit Jazz. City Journal. https://www.city-journal.org/article/when-heroin-hit-jazz1
- (n.d.). Decriminalisation of low-level drug possession in the ACT. Hugo Law Group. https://hugolawgroup.com.au/insights/decriminalisation-of-low-level-drug-possession-in-the-act/1
- (n.d.). Suchtmittelgesetz. ris.bka.gv.at. https://www.ris.bka.gv.at/GeltendeFassung.wxe?Abfrage=Bundesnormen&Gesetzesnummer=100110401
- (n.d.). Narcotic Substances Act in Austria: Overview of Rules and Penalties. MPW Rechtsanwaelte. https://mpw-rechtsanwaelte.com/en/narcotic-substances-act-austria/1
- (n.d.). Portaria SVS/MS 344/1998. bvsms.saude.gov.br. https://bvsms.saude.gov.br/bvs/saudelegis/svs/1998/prt0344_12_05_1998_rep.html1
- (n.d.). Portaria SVS/MS 344/1998. planalto.gov.br. https://www.planalto.gov.br/ccivil_03/_ato2004-2006/2006/lei/l11343.htm1
- (n.d.). Controlled Drugs and Substances Act. laws-lois.justice.gc.ca. https://laws-lois.justice.gc.ca/eng/acts/C-38.8/FullText.html1
- (n.d.). Controlled Drugs and Substances Act (SC 1996, c. 19) — Schedule I. Justice Laws Website (Canada). https://laws-lois.justice.gc.ca/eng/acts/c-38.8/page-9.html1
- (n.d.). Canada Gazette: Regulations Amending Certain Regulations Made Under the Controlled Drugs and Substances Act (Access to Diacetylmorphine for Emergency Treatment) SOR/2016-239. Canada Gazette. https://gazette.gc.ca/rp-pr/p2/2016/2016-09-07/html/sor-dors239-eng.html1
- (n.d.). Canada (Attorney General) v. PHS Community Services Society, 2011 SCC 44. Supreme Court of Canada / CanLII. https://www.canlii.org/en/ca/scc/doc/2011/2011scc44/2011scc44.html1
- (n.d.). Decreto 1019 de 1990. suin-juriscol.gov.co. https://www.suin-juriscol.gov.co/viewDocument.asp?id=12081591
- (n.d.). Government Regulation No. 463/2013. zakonyprolidi.cz. https://www.zakonyprolidi.cz/cs/2013-4631
- (n.d.). Government Regulation No. 463/2013. zakonyprolidi.cz. https://www.zakonyprolidi.cz/cs/2009-401
- (n.d.). Government Decree 543/2008. finlex.fi. https://www.finlex.fi/fi/laki/ajantasa/2008/200805431
- (n.d.). Government Decree 543/2008. finlex.fi. https://www.finlex.fi/fi/laki/ajantasa/2008/200803731
- (n.d.). Betäubungsmittelgesetz. gesetze-im-internet.de. https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html1
- (n.d.). Betäubungsmittelgesetz. gesetze-im-internet.de. https://www.gesetze-im-internet.de/btmg_1981/__13.html1
- (n.d.). Betäubungsmittelgesetz. gesetze-im-internet.de. https://www.gesetze-im-internet.de/btmg_1981/__29.html1
- (n.d.). Betäubungsmittelgesetz. gesetze-im-internet.de. https://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html1
- (n.d.). Narcotic Drugs and Psychotropic Substances Act, 1985. indiacode.nic.in. https://www.indiacode.nic.in/bitstream/123456789/6834/1/narcotic-drugs-and-psychotropic-substances-act-1985.pdf1
- (n.d.). DPR 309/1990. normattiva.it. https://www.normattiva.it/uri-res/N2Ls?urn:nir:stato:decreto.del.presidente.della.repubblica:1990-10-09;3091
- (n.d.). DPR 309/1990. salute.gov.it. https://www.salute.gov.it/portale/droga/dettaglioContenutiDroga.jsp?lingua=italiano&id=615&area=sostanzeStupefacenti&menu=vuoto1
- (n.d.). Narcotics and Psychotropics Control Act. laws.e-gov.go.jp. https://laws.e-gov.go.jp/law/328AC0000000014?occasion_date=202404161
- (n.d.). Regulations No. 847. likumi.lv. https://likumi.lv/ta/en/en/id/40283-regulations-regarding-narcotic-substances-psychotropic-substances-and-precursors-to-be-controlled-in-latvia1
- (n.d.). Ley General de Salud. diputados.gob.mx. https://www.diputados.gob.mx/LeyesBiblio/pdf/LGS.pdf1
- (n.d.). Opium Act. wetten.overheid.nl. https://wetten.overheid.nl/BWBR0001941/1
- (n.d.). Misuse of Drugs Act 1975. legislation.govt.nz. https://www.legislation.govt.nz/act/public/1975/0116/latest/DLM436101.html1
- (n.d.). Narkotikaforskriften. lovdata.no. https://lovdata.no/dokument/SF/forskrift/2013-02-14-1991
- (n.d.). Act on Counteracting Drug Addiction. isap.sejm.gov.pl. https://isap.sejm.gov.pl/isap.nsf/DocDetails.xsp?id=WDU202200016651
- (n.d.). Law No. 30/2000. diariodarepublica.pt. https://diariodarepublica.pt/dr/detalhe/lei/30-2000-3231811
- (n.d.). Law No. 30/2000. diariodarepublica.pt. https://diariodarepublica.pt/dr/detalhe/decreto-lei/15-1993-5853941
- (n.d.). Drug Decriminalization in Portugal: Challenges and Limitations. Office of National Drug Control Policy (White House Archives). https://obamawhitehouse.archives.gov/ondcp/ondcp-fact-sheets/drug-decriminalization-in-portugal-challenges-and-limitations1
- (n.d.). Government Resolution No. 681. pravo.gov.ru. http://pravo.gov.ru/proxy/ips/?docbody=&nd=1020547921
- (n.d.). Misuse of Drugs Act 1973. sso.agc.gov.sg. https://sso.agc.gov.sg/Act/MDA1973?ProvIds=Sc1-1
- (n.d.). Misuse of Drugs Act 1973. sso.agc.gov.sg. https://sso.agc.gov.sg/Act/MDA19731
- (n.d.). Drugs and Drug Trafficking Act 140 of 1992. justice.gov.za. https://www.justice.gov.za/legislation/acts/1992-140.pdf1
- (n.d.). Drugs and Drug Trafficking Act 140 of 1992. gov.za. https://www.gov.za/sites/default/files/gcis_document/202212/47736drugsanddrugtraffickingamendmentact14of2022.pdf1
- (n.d.). Instrumento de Ratificación del Convenio Único de 1961 sobre Estupefacientes. boe.es. https://www.boe.es/buscar/doc.php?id=BOE-A-1966-53731
- (n.d.). Betäubungsmittelverzeichnisverordnung. fedlex.admin.ch. https://www.fedlex.admin.ch/eli/cc/2011/364/de1
- (n.d.). Betäubungsmittelverzeichnisverordnung. fedlex.admin.ch. https://www.fedlex.admin.ch/eli/cc/1952/241_241_241/de1
- (n.d.). Diacetylmorphine-assisted (heroin-assisted) treatment. Federal Office of Public Health (Switzerland). https://www.bag.admin.ch/en/diacetylmorphine-assisted-heroin-assisted-treatment1
- (n.d.). Cabinet of Ministers Resolution No. 770 of 6 May 2000. zakon.rada.gov.ua. https://zakon.rada.gov.ua/laws/show/770-2000-%D0%BF1
- (n.d.). Misuse of Drugs Act 1971, Schedule 2 — Class A Drugs. legislation.gov.uk. https://www.legislation.gov.uk/ukpga/1971/38/schedule/212
- (n.d.). Misuse of Drugs Act 1971. legislation.gov.uk. https://www.legislation.gov.uk/uksi/2001/3998/schedule/21
- (n.d.). Controlled Substances Act. govinfo.gov. https://www.govinfo.gov/content/pkg/USCODE-2023-title21/html/USCODE-2023-title21-sec812.htm1
- (n.d.). Controlled Substances Act. govinfo.gov. https://www.govinfo.gov/content/pkg/USCODE-2023-title21/html/USCODE-2023-title21-sec841.htm1
- (n.d.). Controlled Substances Act. govinfo.gov. https://www.govinfo.gov/content/pkg/USCODE-2023-title21/html/USCODE-2023-title21-sec844.htm1
- (n.d.). 21 U.S. Code § 812 — Schedules of controlled substances. Legal Information Institute, Cornell Law School. https://www.law.cornell.edu/uscode/text/21/8121
Further Reading
Automated synthesisInformation aggregated and synthesized using an autonomous workflow built by Josie Kins.
Suggest an edit
Spotted a mistake, an outdated claim, or something missing from the Heroin article? Send the editors a private note. Feedback lands in a moderation queue and is never shown on the site.