Leo Sher, M.D.

Heroin (diacetylmorphine, (5a,6a)-7,8-Didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate (ester), diamorphine, or Diagesil®) is a semi-synthetic morphine derivative and a powerful opioid analgesic (1). Heroin was created in 1874 by Dr. Charles Romley Alder Wright, a British chemistry and physics researcher who worked at St. Mary’s Hospital Medical School in London (2). Heroin was first marketed in 1898 as an antitussive for patients with asthma and tuberculosis.

The blood brain permeability of heroin is about 10 times that of morphine (1,3).  When heroin crosses the blood brain barrier, it is hydrolyzed into 6-acetyl morphine and morphine, which then bind to opioid receptors.There are multiple effects of heroin including euphoria and indifference to an anticipated distress.

Heroin is a very popular opioid among individuals with substance use disorders (4,5). The United Nations estimates that there are currently between 13 and 22 million opioid dependent people worldwide (4). In Europe and North America, there are an estimated two to four million illicit heroin users (5). Heroin dependence creates tremendous social and health costs (6,7). These include crime, diseases such as HIV and Hepatitis C and unemployment.

Methadone and buprenorphine maintenance are good treatments with moderate effect sizes, but a substantial part of heroin dependent individuals do not respond to these treatments (1,7,8). In order to create better outcomes for these treatment refractory patients, heroin-assisted treatment was developed. Heroin-assisted treatment was developed in the 1990s and tested in the last two decades (1,7,8). In this treatment, patients are given pharmaceutical grade heroin three times per day in a special clinic under a close supervision to prevent abuse or diversion. A psychosocial support is also provided. It is important to note that heroin-assisted treatment does not promote the legalization of heroin. It is a tool to reduce the problems caused by the use of illegal heroin.

Prof. Wim van den Brink, one of the pioneers of heroin-assisted treatment wrote in his Editorial in the British Medical Journal that “heroin assisted treatment is generally safe and more effective than standard oral methadone maintenance treatment in chronic relapsing heroin dependent patients” (8). Indeed, the effectiveness of heroin-assisted treatment has been demonstrated in randomized trials in Switzerland, the Netherlands, Spain, Germany, Canada and the U.K. (7).

A relatively recent Cochrane review concluded that “The available evidence suggests an added value of heroin prescribed alongside flexible doses of methadone for long-term, treatment refractory, opioid users, to reach a decrease in the use of illicit substances, involvement in criminal activity and incarceration, a possible reduction in mortality; and an increase in retention in treatment” (9). It looks like heroin-assisted treatment may improve public safety. At the same time, the Cochrane review noted that “Due to the higher rate of serious adverse events, heroin prescription should remain a treatment for people who are currently or have in the past failed maintenance treatment.” The Cochrane study included 8 randomized controlled trials of heroin maintenance treatment (alone or combined with methadone).
 
Heroin-assisted maintenance treatment is currently available in the Netherlands, Switzerland, U.K., Germany and Denmark for patients who suffered from severe heroin dependency for many years and where other treatments like methadone maintenance therapy have failed. It appears that this treatment results in significant cost savings to society from reduced crime and health expenditures.

References
1.    Rook EJ, Huitema AD, van den Brink W, van Ree JM, Beijnen JH. Pharmacokinetics and pharmacokinetic variability of heroin and its metabolites: review of the literature. Curr Clin Pharmacol 2006;1(1):109-18.
2.    Sneader W. The discovery of heroin. Lancet 1998; 352: 1697-9.
3.    Bao G, Kang L, Li H, Li Y, Pu L, Xia P, Ma L, Pei G. Morphine and heroin differentially modulate in vivo hippocampal LTP in opiate-dependent rat. Neuropsychopharmacology 2007;32(8):1738-49.
4.    UNODC, World Drug Report 2010 (United Nations Publication, Sales No. E.10.XI.13).
5.    EMCDDA. Annual Report 2005: The State of the Drugs Problem in Europe. Lisbon: European Monitoring Centre for Drugs and Drug Addiction; 2005.
6.    Mark T, Woody G, Juday T, Kleber H. The economic costs of heroin addiction in the United States. Drug Alcohol Depend. 2001;61:195–206.
7.    Fischer B, Oviedo-Joekes E, Blanken P, Haasen C, Rehm J, Schechter MT, Strang J, van den Brink W. Heroin-assisted treatment (HAT) a decade later: a brief update on science and politics. J Urban Health. 2007;84(4):552-62.
8.    van den Brink W. Heroin assisted treatment. British Medical Journal 2009;339:b4545.
9.    Ferri M, Davoli M, Perucci CA. Heroin maintenance for chronic heroin-dependent individuals. Cochrane Database Syst Rev. 2011 Dec 7;(12):CD003410.