Overload

Heroin

Category: Medicines

Type

Involuntary and voluntary

Introduction and description

Heroin  - also known as Diamorphine, Diacetylmorphine, Acetomorphine, (Dual) Acetylated morphine, or Morphine diacetate -  is a semi-synthetic opioid drug synthesised from morphine, a derivative of the opium poppy.

Heroin is used by doctors to treat us.  When used in medicine heroin is used to treat severe pain, such as that resulting from a heart attack or a severe injury. The name "heroin" is only used when being discussed in its illegal form. When it is used in a medical environment, it is referred to as diamorphine.

Background

Heroin binds to not just the mu and delta opioid receptors but also the kappa receptors. Heroin itself exhibits relatively low affinity for the μ receptor, which normally would give it less of a ‘euphoric’ effect, however, administered intravenously, it creates a larger histamine release, giving the illusion of a ‘high’.

It was originally developed as a morphine substitute for use in cough suppressants in the belief that it did not have morphine's addictive side-effects.  In fact, this acetylated form of morphine is one and a half to two times more potent than morphine itself.  It was even marketed as a cure for morphine addiction, before it was discovered that it rapidly metabolises into morphine. When the drug is injected,  it rapidly crosses the blood-brain barrier because of the presence of the acetyl groups. Once in the brain, it is then deacetylated variously until eventually becoming morphine.  Diacetylmorphine is essentially a quicker acting form of morphine. 

It  is used both clinically as an analgesic and a  ‘recreational drug’.  Its popularity with recreational drug users, was believed to stem from the effects whilst it is being metabolised into morphine.  Heroin supposedly produces more euphoria than other opioids.   However, this perception is not supported by the results of clinical studies comparing the effects of injected heroin and morphine –people showed no preference for one drug over the other. Equipotent injected doses had comparable effects, with no difference in each persons self-rated feelings of euphoria, nervousness, relaxation, drowsiness, or sleepiness. 

Like all opioids it is addictive and regular administration leads to tolerance and physical dependence. Tolerance quickly develops, and users need increasingly more of the drug to achieve the same effects. 

As with all opioids it causes respiratory depression and large doses of heroin can cause fatal respiratory depression.  Death from overdose can take anywhere from several minutes to several hours and is caused by anoxia resulting from the breathing reflex being suppressed by µ-opioids [anoxia means a total decrease in the level of oxygen, it is a very  extreme form of hypoxia].  Fatalities are also caused by interactions with other depressant drugs like alcohol or benzodiazepines, and by aspiration of vomit by an unconscious victim. The drug has been used for both suicide and  murder. Quite a number of well known people have died from heroin overdose, for example, Sid Vicious, Janis Joplin, Tim Buckley, and River Phoenix.

The diagram on the left from Wikipedia show the relative position of heroin in relation to drugs like ketamine or the amphetamines, in terms of dependence and the physical harm done. 

 

As you can see, it is literally ‘off the scale’ – though I am sure whoever compiled the chart did not realise he or she was providing this analogy.

One of the so called ‘cutting agents’ of heroin is quinine or quinidine.  There are studies [which were made for clinical reasons connected with Lomotil and Immodium which are both opiates] that both these products help opiates cross the blood brain barrier.  For over-the-counter medicines like Immodium, this is of importance, as the side effects of respiratory depression plus sedation could be dangerous.  There also appears to be some kind of a booster effect with heroin, as a number of deaths have been caused by heroin ‘cut’ with quinine.

Cocaine is a stimulant and there also appears to be a belief that by using cocaine and heroin together you will help to both intensify the high and counteract both the respiratory depression of heroin and the hypertension of cocaine in some sort of magical balancing act whose logic defies me [the combination is known as a  speedball when injected,  or moonrocks when smoked].  Unfortunately for the user it doesn’t work this way, the effects of the cocaine wear off far more quickly than those of heroin and you get both the side effects.

The Health Committee of the League of Nations banned heroin as far back as 1925.  It is now illegal in many countries including the USA and countries in Europe, as well as places like Iran, India, Australia, Canada, Pakistan, Hong Kong  and even countries in Africa. As heroin is illegal, iIllicit or ‘street’ heroin  can be  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.  Some fatalities are attributable to this problem.

Worldwide, the United Nations estimates there are more than 50 million regular users of diacetylmorphine, cocaine and synthetic drugs. Global users of diacetylmorphine are estimated at between 15.16 million and 21.13 million people aged 15–64.

The diagram on the left from Wikipedia show the relative position of heroin in relation to drugs like ketamine or the amphetamines, in terms of dependence and the physical harm done. As you can see, it is literally ‘off the scale’ – though I am sure whoever compiled the chart did not realise he or she was providing this analogy.

References and further reading

EROWID's entry on Heroin

I also enjoyed Dale Pendell’s description of Heroin in his book Pharmako Poeia

Dr Timothy Leary – High Priest
Junk gives peace, relief from pain and a shattering cosmic detachment.  But the relief is so brief and detachment so ruthlessly physical that the very weak and the very selfish get hooked.

Related observations