Heroin

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

It is strongly discouraged to consume moderate to heavy dosages of these substances together.

Summary sheet: Heroin
Heroin
Molecular structure of Diacetylmorphine.
Diamorphine.svg
Chemical Nomenclature
Common names Heroin, H, Smack, Junk, Brown
Substitutive name Diacetylmorphine (Diamorphine)
Systematic name (5α,6α)-7,8-Didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate
Class Membership
Psychoactive class Opioid
Chemical class Morphinan
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.


Smoked
Dosage
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation. The dosages listed are assuming that the individual is using pure heroin, because the purity of heroin can vary greatly, the actual dosages used may be substantially higher.
This dosage and duration information has been sourced from TripSit
Threshold 2 - 5 mg
Light 5 - 15 mg
Common 15 - 25 mg
Strong 25 - 50 mg
Heavy 50 mg +
Duration
Total 3 - 5 hours
Onset 5 - 10 seconds
Peak 15 - 30 minutes
Offset 15 - 30 minutes
After effects 10 - 30 minutes




Insufflated
Dosage
Threshold 5 - 7.5 mg
Light 7.5 - 20 mg
Common 20 - 35 mg
Strong 35 - 50 mg
Heavy 50 mg +
Duration
Total 3 - 7 hours
Onset 10 - 60 seconds
Peak 1 - 90 minutes
Offset 1 - 3 hours
After effects 1.5 - 3 hours





Intravenous
Dosage
Threshold mg
Common 5 - 8 mg
Strong 8 - 15 mg
Heavy 15 mg +
Duration
Total 4 - 5 hours
Onset 0 - 5 seconds

DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Diacetylmorphine (also known as Heroin, H, and colloquially as Smack, Junk, Brown, and Boy) is a semisynthetic opioid of the morphinan class that produces analgesic, relaxing, sedating and euphoric effects when administered.

Heroin was originally synthesized by C.R. Alder Wright in 1874 by adding two acetyl groups to the morphine alkaloid from the latex of the poppy plant (Papaver somniferum)[2]. Although the name heroin is a traditional trade name for a Bayer Pharmaceutical product containing diacetylmorphine, the name has since been widely adopted for all intents and purposes and may describe a recreational depressant that may or may not contain pure diacetylmorphine.

In its pure form, heroin is active at doses of 5mg and above; however, the substance is most commonly found in a preparation containing significant impurities. These impurities can result from including processing faults during synthesis, the addition of harmful or benign cutting agents, or the substitution of significantly more potent and dangerous analogous substances such as fentanyl adulterated into the end-product before distribution.[3][4][5][6][7] This makes accurate dosing is particularly difficult.

History and culture

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Diacetylmorphine was first synthesized by Alder Wright in 1874 when attempting to combine morphine with various acids. The synthesis was achieved through boiling anhydrous morphine with morphine alkaloid with acetic anhydride)[8].

Chemistry

Heroin, or diacetylmorphine, is an opioid of the morphinan class. Heroin and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called a phenanthrene. A fourth nitrogen containing ring is fused to the phenanthrene at R9 and R13, with the nitrogen member looking at R17 of the combined structure. This structure is called morphinan.

Heroin, along with other morphinans, contains an ether bridge between two of its rings, connecting R4 and R5 through an oxygen group. Heroin contains two acetate (CH3COO−) groups bonded to R3 and R6 of its structure, and a methyl group located on the nitrogen atom at R17. On the same ring containing the 6-acetyl group, heroin contains a double bond.

Heroin's chemical structure is closely related to morphine. Heroin is the 3,6-diacetyl derivative of the diol morphine, meaning it contains acetate functional groups at the same locations hydroxy groups are found in morphine (3,6). Heroin is analogous to the other morphinans including dihydrocodeine, codeine, ethylmorphine, hydrocodone, and oxycodone.

Pharmacology

Heroin itself is an inactive drug, but it is metabolized into morphine when inserted into the body.[9] When taken orally, heroin undergoes extensive first-pass metabolism via deacetylation, making it a prodrug for the systemic delivery of morphine.[10] When the drug is injected, however, it avoids this first-pass effect, very rapidly crossing the blood–brain barrier because of the presence of the acetyl groups which render it much more fat soluble, and thus more potent, than morphine itself.[11]

Once in the brain, it is deacetylated variously into the inactive 3-monoacetylmorphine and the active 6-monoacetylmorphine (6-MAM). 6-MAM is found in some commerically prepared batches of black tar heroin, often found on the west coast of the United States. It is then deacetylated into morphine, which binds to μ-opioid receptors. Heroin itself exhibits relatively low affinity for the μ receptor, suggesting that much of the psychoactive effects of the substance come from the metabolites of heroin rather than the diacetylmorphine itself.[12]

The recreational effects of this compound, including cognitive euphoria and physical euphoria, occur because opioids structurally mimic endogenous endorphins which are naturally produced within the body and are also active on the μ-opioid receptor set in the brain. The way in which synthetic opioids such as heroin structurally mimic these natural endorphins results in their euphoric, pain relief and anxiolytic effects. This is because natural endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. The endorphins can be released in response to pain, strenuous exercise, orgasm, or general excitement.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.

Physical effects
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Cognitive effects
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Visual effects
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Experience reports

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

Additional experience reports can be found here:

Forms

Above is heroin in its typical and most common form: a dusty brown powder.

Black Tar Heroin

Above is "black tar" heroin as commonly seen on the west coast of the U.S..

This form of heroin is diacetylmorphine acetate, a product of heroin production that does not require further acetylation. It differs in texture from powder heroin in that it is black, gooey, viscous, and a texture ranging from quite similar to wet asphalt and a hard rock of material. It is commonly produced in South America and is found on the western coast of the USA.

The actual chemical contents of black tar heroin can vary from the white powder form. Black tar might contain a variable mixture of morphine derivatives, predominantly 6-MAM (6-monoacetylmorphine) which is another result of crude acetylation that occurs in the clandestine production process.

When injected into any type of tissue, this form of heroin results in an increased risk of wound botulism[14]. Wound botulism can be fatal and leads to amputations and death in a higher rate of black tar heroin users. Because of the consistency of the substance (tar like), it can pose a greater risk for collapsing, damaging, or infecting veins. This damage to veins leads to a higher chance of subcutaneous and intradermal injection[15] which is not advocated from a harm reduction point of view. For users who do choose to inject this substance, it is highly recommended to follow the procedures found in the safe injection guide.

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of heroin[16]

Like many other opioids, unadulterated heroin at appropriate dosages does not cause many long-term complications other than physical and psychological dependence and constipation. Outside of the extremely powerful addiction and physical dependence, the harmful or toxic aspects of opioid usage are exclusively associated with not taking the necessary precautions in regards to its administration, overdosing and using impure heroin products that contain harmful additives.

Heavy dosages of heroin can result in severe respiratory depression which can result in dangerous or even fatal levels of anoxia (oxygen deprivation). This occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors - this effect is proportional to the dosage of the substance consumed.

Due to the nature of the unregulated drug market, illicit heroin is of widely varying and unpredictable purity. A user may prepare what they consider to be a moderate dose while actually taking far more than intended in the event of obtaining a purer product than they are used to, or may be cut unknowingly with more potent and dangerous substances such as fentanyl.[17] Depending on drug interactions and numerous other factors, death from overdose can take anywhere from several minutes to several hours and is a direct result of respiratory depression leading onto anoxia (oxygen deprivation) resulting from the breathing reflex being suppressed by agonism of µ-opioid receptors. Some sources quote the median lethal dose (for an average 75 kg opiate-naive individual) as being between 75 and 600mg.[18]

Heroin can also cause nausea and vomiting; a significant number of deaths attributed to opioid overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semi-conscious user who is lying on their back vomits into their mouth and unknowingly suffocates. It can be prevented by ensuring that one is lying on their side with their head tilted downwards so that the airways cannot be blocked in the event of vomiting while unconscious (also known as the recovery position).

In case of a suspected or known overdose, it is advised to administer a dose of naloxone intravenously, intramuscularly, or nasally to reverse the effects of opioid agonism[19].

It is strongly recommended that one use harm reduction practices such as volumetric dosing, when using this substance to ensure the administration of the intended dose (especially due to the unusually high risk of overdose this substance presents.)

Tolerance and addiction potential

As with other opioids, the chronic use of heroin can be considered extremely addictive with a high potential for abuse and is capable of causing psychological and physical dependence among certain users. When psychological or physical addiction has developed, mental and physical withdrawal symptoms and cravings may occur if a person suddenly stops their usage.

Tolerance to many of the effects of heroin develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same psychoactive effects of a previously lower dose. After heroin tolerance has developed, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Heroin presents cross-tolerance with all other opioids, meaning that after the consumption of heroin all opioids will have a reduced effect.

The risk of fatal heroin overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance.[20] When users dose their old doses, they no longer have the physical tolerance to handle the sedative effects of heroin and overdose occurs. To account for this lack of physical tolerance, it is safer to only dose a fraction of one's usual dosage if using after a prolonged period of sobriety. It has also been found that the environment one is in can play a role in 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.[21]

Studies have shown that the subjective cognitive euphoria and physical euphoria of heroin use, which is the reinforcing component of addiction, is proportional in its' intensity to the rate at which the blood level concentrations of the drug increases.[22] Intravenous injection is the fastest route of drug administration, causing blood concentrations to rise the fastest. It is followed by smoking, suppository (anal or vaginal insertion), insufflation (snorting), and ingestion (swallowing).

Dangerous interactions

Although many substances are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

  • Depressants (1,4-Butanediol, 2M2B, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Stimulants - It is dangerous to combine heroin, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants mask the sedative effect of heroin, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of heroin will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of heroin.

Legality

  • Australia: Heroin is controlled in Australia, but there is conflicting information about its exact legal status. Heroin was listed in Schedule I of the Narcotic Drugs Act of 1967; however, it is unclear whether the control system has changed since then.
  • Brazil: Heroin is listed as a controlled substance, making the production, distribution, or possession illegal.
  • Canada: Heroin is Schedule I in Canada. However, a unanimous Supreme Court decision in 2011 declared that there is a right under Section 7 of the Charter to have access to clean injection sites.[23]
  • Czech Republic: The Czech Republic has decriminalized 1.5g or less of heroin and the punishment is similar in scale to a parking ticket. Sales, production, and larger quantity possession are still crimes.[24]
  • Finland: Heroin is a controlled substance, making the production, distribution, and possession illegal without a license.
  • Germany: In May 2009, Germany made it legal to prescribe heroin to addicts who are over 23 years old, have been addicted for at least 5 years, and have tried 2 other therapies to get off heroin.
  • Latvia: Heroin is a Schedule I drug.[25]
  • New Zealand: Heroin is Class A in New Zealand.
  • Norway: Heroin is Schedule I in Norway and illegal to buy or possess without a special license. There have been some projects to establish needle rooms in Norway by the government where heroin addicts are allowed to get fresh needles for injecting heroin.
  • Portugal: The personal use of heroin was decriminalized by Law 30/2000 in July 2001. Possession of less than 1g is not regarded as a criminal offense although the substance is liable to be seized and the possessor can be referred to mandatory treatment. Sale or possession of quantities greater than the personal possession limit are criminal offenses punishable by jail time.
  • Switzerland: Heroin is legally available for addicts under an ongoing experiment but is otherwise illegal to possess.
  • United Kingdom: Heroin is Schedule II/Class A and is illegal to buy, sell or possess without a license.
  • United States: Heroin is Schedule I in the United States. This means it is illegal to manufacture, buy, possess, or distribute without a DEA license.

See also

External links

Literature

  • Schmidt, H., Vormfelde, S. V., Klinder, K., Gundert-Remy, U., Gleiter, C. H., Skopp, G., Aderjan, R. and Fuhr, U. (2002), Affinities of Dihydrocodeine and its Metabolites to Opioid Receptors. Pharmacology & Toxicology, 91: 57–63. https://doi.org/10.1034/j.1600-0773.2002.910203.x
  • Koch T, Höllt V (2008). Role of receptor internalization in opioid tolerance and dependence. Pharmacol. Ther. 117 (2): 199–206. https://doi.org/10.1016/j.pharmthera.2007.10.003
  • Pert, C. B., Pasternak, G., & Snyder, S. H. (1973). Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain. Science, 182(4119), 1359-1361. https://doi.org/10.1126/science.182.4119.1359
  • Friswell J, Phillips C, Holding J, Morgan CJ, Brandner B, Curran HV (2008). Acute effects of opioids on memory functions of healthy men and women. Psychopharmacology (Berl.). 198 (2): 243–50. https://doi.org/10.1007/s00213-008-1123-x.
  • Stefano GB, Ptáček R, Kuželová H, Kream RM (2012). Endogenous morphine: up-to-date review (2011). Folia Biol. (Praha). 58 (2): 49–56. PMID 22578954. Positive evolutionary pressure has apparently preserved the ability to synthesize chemically authentic morphine, albeit in homeopathic concentrations, throughout animal phyla.

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. Wright, C.R.A. (1874). "On the Action of Organic Acids and their Anhydrides on the Natural Alkaloids". Journal of the Chemical Society. 27: 1031–1043. doi:10.1039/js8742701031|https://web.archive.org/web/20040606103721/http://adhpage.dilaudid.net/heroin.html
  3. Much of Heroin Supply Adulterated with Fentanyl | http://mha.ohio.gov/Portals/0/assets/Research/OSAM-TRI/092015-OSAMogram-heroin-fentanyl-update.pdf
  4. InFocus: Fentanyl-Laced Heroin: A Deadly Combination (Medicine News)| http://journals.lww.com/em-news/Fulltext/2014/04000/InFocus__Fentanyl_Laced_Heroin__A_Deadly.5.aspx
  5. Illicit Version Of Painkiller Fentanyl Makes Heroin Deadlier | http://www.npr.org/sections/health-shots/2015/08/26/434618809/ilicit-version-of-painkiller-fentanyl-makes-heroin-deadlier
  6. What You Need to Know About Fentanyl-Laced Heroin | http://www.projectknow.com/what-you-need-to-know-about-fentanyl-laced-heroin/
  7. Killer batch of white heroin responsible for at least 100 deaths across the country... and rising | http://www.dailymail.co.uk/news/article-2549944/Killer-heroin-fentanyl-epidemic-responsible-100-deaths-country-rising-half-month.html
  8. Wright, C.R.A. (1874). "On the Action of Organic Acids and their Anhydrides on the Natural Alkaloids". Journal of the Chemical Society. 27: 1031–1043. doi:10.1039/js8742701031|https://web.archive.org/web/20040606103721/http://adhpage.dilaudid.net/heroin.html
  9. The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/10.1139/y86-001
  10. The therapeutic use of heroin: a review of the pharmacological literature (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2420426
  11. Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0376871605001511
  12. Evidence from opiate binding studies that heroin acts through its metabolites (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6319928
  13. Urban Dictionary: Nodding Off|http://www.urbandictionary.com/define.php?term=nodding%20off
  14. Wound Botulism Associated With Black Tar Heroin Among Injecting Drug Users (Douglas J. Passaro, MD, MPH; S. Benson Werner, MD, MPH; Jim McGee, MSPH; et al) | http://jamanetwork.com/journals/jama/fullarticle/187346
  15. Explaining the Geographical Variation of HIV Among Injection Drug Users in the United States (D. Ciccarone, M.D., M.P.H. and P. Bourgois, Ph.D.) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1343535/pdf/nihms3846.pdf
  16. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  17. 'Death pill': fentanyl disguised as other drugs linked to spike in US overdoses | https://www.theguardian.com/society/2016/may/10/fentanyl-drug-overdoses-xanax-painkillers
  18. The Consumers Union Report on Licit and Illicit Drugs | http://www.druglibrary.org/schaffer/Library/studies/cu/cu12.htm
  19. Drugs.com Naloxone Hydrochloride Page|https://www.drugs.com/monograph/naloxone-hydrochloride.html
  20. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  21. 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
  22. Relative Reinforcing Strength of Three N-Methyl-D-Aspartate Antagonists with Different Onsets of Action | http://jpet.aspetjournals.org/content/301/2/690.full.pdf
  23. http://www.bbc.co.uk/news/world-us-canada-15130282, and http://scc.lexum.org/en/2011/2011scc44/2011scc44.html
  24. http://www.praguepost.com/news/3194-new-drug-guidelines-are-europes-most-liberal.html
  25. Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (1.2. morfināna atvasinājumi) | http://likumi.lv/doc.php?id=121086