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diacetylmorphine (diamorphine, heroin)

Epidemiology: - 2-fold increase in heroin overdoses 2010-2012 [2] - nonmedical use of prescription opioids is a risk factor for heroin use [4] Pharmacokinectics: - heroin (diacetylmorphine) is rapidly hydrolyzed to 6-monoacetyl morphine, which, in turn, is hydrolyzed to morphine - both heroin & 6-monoacetyl morphine are more lipid soluble than morphine & more readily cross the blood brain barrier - intravenous injection of heroin gives a "rush" due to the rapid initial flux of heroin into the brain - this "rush" is described as a warmth, taste or high with intense pleasure & may be responsible for much of the popularity of heroin & its abuse potential - after intravenous injection, effects begin in < 1 minute - an intense euphoria "rush" ensues lasting 45 seconds to several minutes - after this, there is a period of sedation & tranquility lasting up to 1 hour - the effects of heroin wear off after 3-5 hours depending upon the dose Adverse effects: - overdose, death [2] - dependence, addiction - endocarditis & other complications from contamination or non-sterile practices Laboratory: - diamorphine in specimen - diamorphine in hair - diamorphine in serum/plasma - diamorphine in urine Notes: - White house announced coordinated effort between public health & law enforcement officials to reduce heroin & prescription opioid use in certain areas of the U.S. [3] - goal is to shift the focus toward treatment, rather than punishment of drug users - large-scale heroin suppliers will be targeted for arrest [3]

Interactions

drug interactions drug adverse effects (more general classes)

Related

morphine (morphine sulfate [MS], MS Contin, Roxanol, Oramorph SR, Kadian, Avinza, DepoDur, Duromorph)

General

morphinan opiate opioid receptor agonist (narcotic)

Properties

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996 pg 536, 567
  2. Rudd RA et al Increases in Heroin Overdose Deaths- 2010-2012. Weekly. October 3, 2014 / 63(39);849-854 http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6339a1.htm
  3. The White House. Press Release. Aug. 17, 2015 White House Drug Policy Office Funds New Projects in High Intensity Drug Trafficking Areas. https://www.whitehouse.gov/the-press-office/2015/08/17/white-house-drug-policy-office-funds-new-projects-high-intensity-drug
  4. Compton WM, Jones CM, Baldwin GT Relationship between Nonmedical Prescription-Opioid Use and Heroin Use. N Engl J Med 2016; 374:154-163. January 14, 2016 PMID: 26760086 http://www.nejm.org/doi/full/10.1056/NEJMra1508490

Component-of

cocaine/diacetylmorphine (speedball)