Heroin: Difference between revisions

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==Pharmacology==

Heroin itself is an inactive drug, but it is metabolized into [[morphine]] when inserted into the body.<ref>The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/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>The therapeutic use of heroin: a review of the pharmacological literature (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2420426</ref> 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>Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0376871605001511</ref>

Heroin itself is an inactive drug, but it is metabolized into [[morphine]] when inserted into the body.<ref>The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/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>The therapeutic use of heroin: a review of the pharmacological literature (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2420426</ref> 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>Development of pharmaceutical heroin preparations for medical co-prescription to opioid-dependent patients (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0376871605001511</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 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.<ref>Evidence from opiate binding studies that heroin acts through its metabolites (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6319928</ref>

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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 manufacturing process.

When injected into any type of tissue, this form of heroin results in an increased risk of wound botulism<ref>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 </ref>. 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<ref>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</ref> which is not advocated from a harm reduction point of view. For users who do choose to inject this substance, it is advised to follow the procedures found in the [[safer injection guide]].

When injected into any type of tissue, this form of heroin results in an increased risk of wound botulism<ref>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 </ref>. Wound botulism can be fatal and leads to amputations and death at 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<ref>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</ref> which is not advocated from a harm reduction point of view. For users who do choose to inject this substance, it is advised to follow the procedures found in the [[safer injection guide]].

==Toxicity and harm potential==

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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<ref>Drugs.com Naloxone Hydrochloride Page|https://www.drugs.com/monograph/naloxone-hydrochloride.html</ref>.

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 overdose this substance presents.)

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.)

===Tolerance and addiction potential===

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*'''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.<ref>http://www.praguepost.com/news/3194-new-drug-guidelines-are-europes-most-liberal.html</ref>

*'''Finland:''' Heroin is a controlled substance, making the production, distribution, and possession illegal without a license.{{citation needed}}

*'''Germany:''' Heroin is controlled under BtMG Anlage I, II and III, making it illegal to manufacture, import, possess, sell, or transfer it without a license. There is an exception for ~~preperations~~, that are approved for addiction treatment, which can be prescribed on a narcotic prescription form.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_i.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref>

*'''Germany:''' Heroin is controlled under BtMG Anlage I, II and III, making it illegal to manufacture, import, possess, sell, or transfer it without a license. There is an exception for preparations, that are approved for addiction treatment, which can be prescribed on a narcotic prescription form.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_i.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref>

*'''Latvia:''' Heroin is a Schedule I drug.<ref>Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (1.2. morfināna atvasinājumi) | http://likumi.lv/doc.php?id=121086</ref>

*'''New Zealand:''' Heroin is Class A in New Zealand.{{citation needed}}

*'''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.{{citation needed}}

*'''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.{{citation needed}}

*'''Portugal:''' The personal use of heroin was decriminalized by Law 30/2000 on 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.{{citation needed}}

*'''Switzerland:''' Heroin is legally available for addicts under an ongoing experiment but is otherwise illegal to possess.{{citation needed}}

*'''United Kingdom:''' Heroin is Schedule II/Class A and is illegal to buy, sell or possess without a license.{{citation needed}}

@@ Line 21: / Line 21: @@
 ==Pharmacology==
-Heroin itself is an inactive drug, but it is metabolized into [[morphine]] when inserted into the body.<ref>The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/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>The therapeutic use of heroin: a review of the pharmacological literature (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2420426</ref> 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>Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0376871605001511</ref>
+Heroin itself is an inactive drug, but it is metabolized into [[morphine]] when inserted into the body.<ref>The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/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>The therapeutic use of heroin: a review of the pharmacological literature (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2420426</ref> 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>Development of pharmaceutical heroin preparations for medical co-prescription to opioid-dependent patients (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0376871605001511</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 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.<ref>Evidence from opiate binding studies that heroin acts through its metabolites (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6319928</ref>
@@ Line 85: / Line 85: @@
 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 manufacturing process.
-When injected into any type of tissue, this form of heroin results in an increased risk of wound botulism<ref>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 </ref>. 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<ref>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</ref> which is not advocated from a harm reduction point of view. For users who do choose to inject this substance, it is advised to follow the procedures found in the [[safer injection guide]].
+When injected into any type of tissue, this form of heroin results in an increased risk of wound botulism<ref>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 </ref>. Wound botulism can be fatal and leads to amputations and death at 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<ref>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</ref> which is not advocated from a harm reduction point of view. For users who do choose to inject this substance, it is advised to follow the procedures found in the [[safer injection guide]].
 ==Toxicity and harm potential==
@@ Line 99: / Line 99: @@
 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<ref>Drugs.com Naloxone Hydrochloride Page|https://www.drugs.com/monograph/naloxone-hydrochloride.html</ref>.
-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 overdose this substance presents.)
+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.)
 ===Tolerance and addiction potential===
@@ Line 122: / Line 122: @@
 *'''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.<ref>http://www.praguepost.com/news/3194-new-drug-guidelines-are-europes-most-liberal.html</ref>
 *'''Finland:''' Heroin is a controlled substance, making the production, distribution, and possession illegal without a license.{{citation needed}}
-*'''Germany:''' Heroin is controlled under BtMG Anlage I, II and III, making it illegal to manufacture, import, possess, sell, or transfer it without a license. There is an exception for preperations, that are approved for addiction treatment, which can be prescribed on a narcotic prescription form.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_i.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref>
+*'''Germany:''' Heroin is controlled under BtMG Anlage I, II and III, making it illegal to manufacture, import, possess, sell, or transfer it without a license. There is an exception for preparations, that are approved for addiction treatment, which can be prescribed on a narcotic prescription form.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_i.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_ii.html</ref><ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref>
 *'''Latvia:''' Heroin is a Schedule I drug.<ref>Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (1.2. morfināna atvasinājumi) | http://likumi.lv/doc.php?id=121086</ref>
 *'''New Zealand:''' Heroin is Class A in New Zealand.{{citation needed}}
 *'''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.{{citation needed}}
-*'''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.{{citation needed}}
+*'''Portugal:''' The personal use of heroin was decriminalized by Law 30/2000 on 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.{{citation needed}}
 *'''Switzerland:''' Heroin is legally available for addicts under an ongoing experiment but is otherwise illegal to possess.{{citation needed}}
 *'''United Kingdom:''' Heroin is Schedule II/Class A and is illegal to buy, sell or possess without a license.{{citation needed}}