Heroin
| Diacetylmorphine | |
|---|---|
noframe The skeletal formula of Diacetylmorphine. | |
| Dosage | |
| Depends on purity, tolerance and route of administration. | |
| Duration (Insufflated) | |
| Total Duration | 3 - 5 hrs |
| Initial effects | 30 mins - 120 seconds |
| Onset | 10 - 30 mins |
| Peak | 30 - 180 mins |
| Coming down | 1 - 2 hrs |
| After effects | 0 - 3 hrs |
| Duration (Intravenous) | |
| Onset | 10 - 20 seconds |
| Duration | 3 - 5 hrs |
| Duration (Smoked/Vaporized) | |
| Initial effects | 5 - 10 seconds |
| Onset | 5 - 10 mins |
| Peak | 5 - 6 mins |
| After effects | 3 - 5 hrs |
Diacetylmorphine (heroin, morphine diacetate, also known as diamorphine) and commonly known by its street names of H, smack, horse, brown, black, tar, and others,[1] is an opioid analgesic originally synthesized by C.R. Alder Wright in 1874 by adding two acetyl groups to the molecule morphine, which is found naturally in the opium poppy.
Diacetylmorphine, almost always still called by its original trade name of heroin in non-medical settings, is used as a recreational drug for the transcendent relaxation and intense euphoria it induces. As with other opioids, diacetylmorphine is used as both an analgesic and a recreational drug. Frequent and regular administration is associated with tolerance and physical dependence.
Chemistry
This compound is the 3,6-diacetyl ester of morphine.
Pharmocology
Heroin itself is an inactive drug, but when inserted into the body, it converts into morphine.[2] When taken orally, heroin undergoes extensive first-pass metabolism via deacetylation, making it a prodrug for the systemic delivery of morphine.[3] 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 than morphine itself.[4] Once in the brain, it then is deacetylated variously into the inactive 3-monoacetylmorphine and the active 6-monoacetylmorphine (6-MAM), and then to morphine, which bind to μ-opioid receptors, resulting in the drug's euphoric, analgesic (pain relief), and anxiolytic (anti-anxiety) effects; heroin itself exhibits relatively low affinity for the μ receptor.[5]
Subjective effects
The subjective effects of opioids are extremely similar across individual substances with very little variation. These usually only differ in terms of their potency, intensity and duration. In comparison to other opioids, this particular substance can be considered as extremely intense in its physical and cognitive euhoria when compared with that of other opioids such as codiene or tramadol (heroin). It also presents milder amounts of itchiness and is considerably more sedating than that of tramadol and oxycontin.
Studies have shown that the subjective pleasure of drug use (the reinforcing component of addiction) is proportional to the rate at which the blood level of the drug increases.[6] Intravenous injection is the fastest route of drug administration, causing blood concentrations to rise the most quickly, followed by smoking, suppository (anal or vaginal insertion), insufflation (snorting), and ingestion (swallowing).
Toxicity and harm potential
Like most opioids, unadulterated heroin does not cause many long-term complications other than dependence and constipation.[7] In fact outside of the extremely powerful addiction and physical dependence the harmful or toxic aspects of heroin usage are exclusively associated with not taking appropriate precautions in regards to its administration, overdosing and using impure products.
It should also be noted that since heroin can cause nausea and vomiting, a significant number of deaths attributed to heroin overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semiconscious user who is lying on their back vomits into their mouth and unknowingly suffocates as a result. It can be prevented by ensuring that one is laying on their side with their head tilted downwards so that ones airways cannot be blocked in the event of vomiting whilst unconscious.
Due to the nature of the unregulated drug market, illicit heroin is of widely varying and unpredictable purity. This means that the 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. 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 600 mg.[8]
Tolerance and addiction potential
As with other opiate-based pain killers, chronic use of diacetylmorphine can be considered as extremely addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.
Tolerance to many of the effects of diacetylmorphine develops with prolonged use, including therapeutic effects. This results in users having to administer increasingly large doses to achieve the same effects. 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.
Interactions
Diacetylmorphine is dangerous to use in combination other depressents as many fatalities reported as overdoses are in fact caused by interactions with other depressant drugs like alcohol or benzodiazepines resulting in dangerously high levels of respiratory depression.[9]
Legal issues
- Australia - Heroin is controlled in Australa, but we have found conflicting information about its exact legal status. Heroin was listed in Schedule I of the Narcotic Drugs Act of 1967, but we are unclear whether the control system has changed since then.
- Brazil - Heroin is listed as a controlled substance, making 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, if they are available.[10]
- 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. [11]
- Finland - Heroin is a controlled substance, making production, distribution, and possession illegal without a license.
- Germany (Deutschland) - in May 2009, Germany made it legal to prescribe heroin to addicts who are over 23 years old, been addicted for at least 5 years, and have tried 2 other therapies to get off heroin.
- 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, but the chemical is still Schedule I.
- Portugal - Effective July 2001, personal use of heroin was decriminalized by Law 30/2000. Possession of less than 1 g is not regarded as a criminal offense, though 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 otherwise illegal to posess.
- U.K. - Heroin is Schedule II/Class A in the U.K. It is illegal to buy, sell or possess without a license.
- U.S.A. - Heroin is Schedule I in the United States. This means it is illegal to manufacture, buy, possess, or distribute (sell, trade or give) without a DEA license.
See also
References
- ↑ Street names for heroin | http://thecyn.com/heroin-rehab/street-names/
- ↑ The therapeutic use of heroin: a review of the pharmacological literature | http://www.nrcresearchpress.com/doi/abs/10.1139/y86-001
- ↑ The therapeutic use of heroin: a review of the pharmacological literature | http://www.ncbi.nlm.nih.gov/pubmed/2420426
- ↑ Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients | http://www.sciencedirect.com/science/article/pii/S0376871605001511
- ↑ Evidence from opiate binding studies that heroin acts through its metabolites | http://www.ncbi.nlm.nih.gov/pubmed/6319928
- ↑ 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
- ↑ Merck Manual of Home Health Handbook – 2nd edition, 2003, p. 2097
- ↑ The Consumers Union Report on Licit and Illicit Drugs | http://www.druglibrary.org/schaffer/Library/studies/cu/cu12.htm
- ↑ Fatal heroin 'overdose': a review | http://www.ncbi.nlm.nih.gov/pubmed/8997759
- ↑ http://www.bbc.co.uk/news/world-us-canada-15130282, and http://scc.lexum.org/en/2011/2011scc44/2011scc44.html
- ↑ http://www.praguepost.com/news/3194-new-drug-guidelines-are-europes-most-liberal.html