Heroin: Difference between revisions

==Pharmacology==

Heroin itself is an inactive drug, but it is metabolized into [[morphine]] when inserted into the body.<ref name="Sawynok1986">{{cite journal | vauthors=((Sawynok, J.)) | journal=Canadian Journal of Physiology and Pharmacology | title=The therapeutic use of heroin: a review of the pharmacological literature | volume=64 | issue=1 | pages=1–6 | date=1 January 1986 | url=http://www.nrcresearchpress.com/doi/10.1139/y86-001 | issn=0008-4212 | doi=10.1139/y86-001}}</ref> When taken orally, heroin undergoes extensive first-pass metabolism via deacetylation, making it a prodrug for the systemic delivery of morphine.<ref name="Sawynok1986" /> 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.<ref>{{cite journal | vauthors=((Klous, M. G.)), ((Brink, W. V. den)), ((Ree, J. M. V.)), ((Beijnen, J. H.)) | journal=Drug and Alcohol Dependence | title=Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients | volume=80 | issue=3 | pages=283–295 | date=12 December 2005 | url=https://www.sciencedirect.com/science/article/pii/S0376871605001511 | issn=0376-8716 | doi=10.1016/j.drugalcdep.2005.04.008}}</ref>  

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 commercially 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.<ref>{{cite journal | vauthors=((Inturrisi, C. E.)), ((Schultz, M.)), ((Shin, S.)), ((Umans, J. G.)), ((Angel, L.)), ((Simon, E. J.)) | journal=Life Sciences | title=Evidence from opiate binding studies that heroin acts through its metabolites | volume=33 Suppl 1 | pages=773–776 | date= 1983 | issn=0024-3205 | doi=10.1016/0024-3205(83)90616-1}}</ref>

==Subjective effects==

{{Preamble/SubjectiveEffects}}

{{effects/base

====Hallucinatory states====

*'''[[Effect::Internal hallucination]]''' - One may experience a state of semi-consciousness and [[hypnagogia]] during heavy dosage nodding which results in dream-like states and up to level 3 [[Lucid_dreaming#Internally_sourced_sensory_input|imagery]]. This is often accompanied by ill-defined [[geometry]].

}}

===Experience reports===

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

====Black tar heroin====

[[File:Tar.jpeg - Copy.jpg|thumbnail|200px|Above is "black tar" heroin as commonly seen on the west coast of the U.S..]]

==Toxicity and harm potential==

[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of heroin<ref>{{cite journal | vauthors=((Nutt, D.)), ((King, L. A.)), ((Saulsbury, W.)), ((Blakemore, C.)) | journal=The Lancet | title=Development of a rational scale to assess the harm of drugs of potential misuse | volume=369 | issue=9566 | pages=1047–1053 | date=24 March 2007 | url=https://www.sciencedirect.com/science/article/pii/S0140673607604644 | issn=0140-6736 | doi=10.1016/S0140-6736(07)60464-4}}</ref>]]

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 [[responsible use|the necessary precautions]] in regards to [[injected|its administration]], [[dosage|overdosing]] and using impure heroin products that contain harmful additives.  

It is strongly recommended that one use [[responsible drug 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 an overdose this substance presents.)

===Dependence and abuse potential===

Tolerance to many of the effects of heroin [[Time to full tolerance::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 [[Time to half tolerance::3 - 7 days]] for the tolerance to be reduced to half and [[Time to zero tolerance::1 - 2 weeks]] to be back at baseline (in the absence of further consumption). Heroin presents cross-tolerance with [[Cross-tolerance::all other [[opioids]]]], meaning that after the consumption of heroin all [[opioid]]s will have a reduced effect.

==Legal status==

*'''Austria:''' Diacetylmorphine is illegal to possess, produce and sell under the SMG (Suchtmittelgesetz Österreich).{{citation needed}}

*'''Brazil:''' Heroin is listed as a controlled substance, making the production, distribution, or possession illegal. {{citation needed}}

*[http://en.wikipedia.org/wiki/Heroin Heroin (Wikipedia)]

*[https://www.erowid.org/chemicals/heroin/heroin.shtml Heroin (Erowid Vault)]

==Literature==