“Thou hast the keys of Paradise; oh just, subtle and mighty opium!”
Thomas De Quincey, Confessions of an English Opium-Eater
, the sleep-bringing poppy, was cultivated in Mesopotamia (modern-day Iraq) as farback as 3,400 BC. The narcotic and analgesic properties of opium, the dried latex procured from the plant,were recognised in ancient times, when it was used for anaesthetic and ritualistic purposes. Recreationaluse of opium began in China in the 15
Century, and by the 17
Century its addictive properties werewell recognised.
The “opium dens” of this time
provide the earliest historical accounts of opioiddependence.Opium contains up to 12% morphine, the narcotic alkaloid which is responsible for most of its activityand which forms the precursor for the synthesis of diacetylmorphine, a drug which is twice as potent asmorphine itself. Diacetylmorphine was first mass-produced in 1898 and was sold under the trademark
“Heroin” by the Bayer pharmaceutical company. Ironically, it was first marketed as a non
-addictivemorphine substitute and even as a cure for morphine addiction. Diacetylmorphine is still referred to asheroin in non-medical settings.
Heroin’s abuse potential stems from the intense euphoric “rush” and state of transcendent relaxation that
Recreational users prefer heroin to other opioids because of this “rush”, which heroin
exhibits as it crosses the blood-brain barrier more rapidly due to its acetyl groups, which render it morelipophilic. Once in the brain, it is de-acetylated into monoacetylmorphine and then to morphine. Both 6-MAM and morphine bind to µ-opioid receptors, resulting in its euphoric effect. It can be injectedintravenously, insufflated or smoked.Heroin addiction is a chronic, relapsing disease, characterised by preoccupation with a strong desire totake the drug and persistent drug-seeking behaviour, as well as meeting other criteria for substancedependence, such as physiological withdrawal and tolerance, primacy of heroin use over alternativeinterests, and continued use despite awareness of the harmful consequences. The determinants of opioiddependence are multifactorial, comprising a complex interplay of biology, psychology and social issues.The addictive potential of the drug is a major factor and, according to a study published in
comparing the addictive potential of 20 different drugs, heroin poses the highest risk for bothpsychological and physical dependence. Tolerance to heroin occurs with repeated use, requiringincreasingly higher doses to produce the same euphoric effect as the original dose. This results fromadaptation and opioid receptor desensitisation. After approximately 3 weeks of daily heroin use, thisopioid receptor dysregulation leads to physical dependence, whereby abrupt cessation of the drug leadsto unpleasant withdrawal symptoms.The heroin withdrawal syndrome is characterised by restlessness, anxiety, insomnia, tremor, muscle andbone pain, diaphoresis, diarrhoea, lacrimation, rhinorrhoea, excessive yawning and sneezing, pruritis,fever, chills, piloerection and tachycardia. Physical dependence and fear of withdrawal are powerfulmotivating factors for continued heroin use and were once believed to be the sole underlying cause of heroin addiction. Some addicted individuals, however, will endure the withdrawal symptoms in order toreduce their tolerance to heroin so that they can experience a stronger rush. Furthermore, it is recognisedthat craving and relapse often occur weeks and months after the withdrawal symptoms are long gone.Therefore, there must factors other than physical dependence responsible for heroin misuse progressingto heroin addiction. Genetic predisposition is reported to account for 40-60% of the risk for developing adrug addiction. Self-medication with heroin for pre-existing emotional problems and psychiatricdisorders, such as depression, is another strong risk factor for addiction. Poor socio-economic status,