See also Frequently Asked Questions About Heroin, Morphine, and the Opiates - Heroin/Morphine FAQ

Opium (see Chapter 2.1) has been, since the beginning of the century, increasingly appreciated in medical use. The - along with 18 alkaloids- morphine and codeine containing opium is rarely prescribed by doctors in Europe and North America but is swallowed or smoked (Chandu) by addicts in Asia and Eastern Europe.

The prescription of peroral methadone to opioid addicts is a well researched method. There are many detailed, clinical reports regarding it’s use since it was first used by Dole and Nyswander (1965) (Dole 1988). Methadone was prescribed in a racemate form almost world-wide except for in Germany. A racemate is a mixture of 2 twisted, chiral forms of a molecule whereby one turns polarised light to the left, (L, Levo-), the other turns light to the right (D, Dextro-). More experiences, world-wide, have been made with the cheaper racemate of methadone. The differences have not been deeply researched but clinically they are unimportant.

In Great Britain heroin was prescribed by doctors, along with other opioids such as painkillers. The prescription of heroin for opioid addicts has been limited since 1968 and can only be prescribed by psychiatrists who have a special permit. The clinical experiences made were only marginally evaluated. Only a few psychiatrists use heroin to a larger extent; financial and other pragmatic reasons play a decisive role here.

The experiences made in Switzerland (Uchtenhagen 1995, 1996) from the Prove -experiments under the department of health, form an important base for the concept of diversified opioid prescription. The dangers of this simplified controlled, heroin dispension method are limited. Diversified drug prescription and drug dispension can be safely implemented. Over a million doses were dispensed within the Prove-experiment without any grave incidents occurring. The experiences from the Prove-experiments are not easy to interpret pharmacologically and scientific evaluations of the dosing are in part, still in the planning stages. (Kranich 1994, Hämmig 1996, Brenneisen 1997).

The therapeutic necessary blood level of 150 to 600 ng/ml is reached when 80 to 120 mg/ of methadone is consumed daily. (Dole 1988). The maximum subjective methadone-effect is reached, by opioid tolerant people, with a daily dose of 80 to120 mg (Joseph 1994). Furthermore, increases in the dose have hardly any noticeable, additional effects. Adequate doses of 80 mg/d of methadone must more than fully satisfy the hunger for opioids (Ball 1991, D'Aunno 1992). Doses under this level often lead to more illegal consumption and to an increase in stopping treatment prematurely (Christen 1996). There are still unsatisfying doses being recommended (Gölz 1995).

The maximum effect (‘ceiling effect’) from injected heroin seems to be reached with 600 mg / day (Parry 1992). The experiences made within the Prove -experiments in Switzerland confirm the figures from England. Under the direction of Seidenberg in outpatient clinic ZokL2 and in the outpatient clinic KODA-1 under the direction of Hämmig, doses and frequency of injectable heroin were chosen freely within safety measurements made. The dose of heroin is not indefinitely increased. Only rarely is more than one gram of pure heroin intravenously consumed daily, under this free choice-within safety measurements method; the maximum dose is reached, on average, after 6 weeks (Kranich 1994, Hämmig 1996, Seidenberg 1996).

Heroin fixers usually inject 3 times a day. Only a few satisfy themselves with the usual 2 injections a day. Constantly injecting more than 4 times a day is, within opioid-supported treatments with free choice, not common and in fact, illegally only seen in cocktail fixers using cocaine in excess.

The majority of patients experience a pleasant daily pace of varying vigilance and sensitivity. Many feel limited with the feeling spectrum and the dynamics of sensitivities when consuming methadone daily. Heroin fixers and heroin smokers feel this difference in feelings and report of unpleasant effects of methadone in relation to these differences. This feeling of all-always-once, of always being packed in cotton wool, living under a glass bell, corresponds to the pharmacological steady-state-opioid-consumption and is caused physiologically by the permanent occupation of the opioid receptors. Unpleasant as well as pleasant stimuli have no effect. The endogenic opioid peptides rarely reach available receptors in the rewarding system. Steady-state -opioid consumption causes, on one hand, the repression of unpleasant feelings (pain, depression) and on the other hand constant repression of euphoric highs (numbing of mania, anorgasmie etc.).

The maximum effect is reached, without a doubt, after the last heroin injection. The concentration lies far under the toxicity limit due to the full formation of tolerance

At half the concentration-effect (a half-life after the last heroin injection), the effect is still at a maximum.

Even when the amount of substance is halved, (after 2 half-life’s), there is hardly a decrease in effect noticeable

Only after a decrease, to an 1/8 of the original concentration (after 3 half-life’s, approximately after one day) does a noticeable decrease occur in the effect

The experiences made in the Prove -Project Janus in Basel show that a the majority of patients have sufficient protection against any withdrawal symptoms when they inject heroin twice a day under the one condition that the doses are high.

Doses close to the effect-maximum lead to a lasting effect which carries on long after the concentration half-life value of heroin: the concentration must only be fractionally sunk before the effect in the steepest part of the dose-effect curve, starts to fall. By administering high doses, one can ensure a reserve of heroin where even in fully tolerant heroin consumers, subjective opioid satisfaction is reached and where there is enough to keep cold-turkey at bay. The toxic concentration area is not reached.

Patients in opioid-supported treatments usually need longer to gain enough confidence to consume smaller doses of heroin. But as long as heroin is injected, these reductions in dose should not be overestimated as success on the way to abstinence. As shown in Fig.27, the flash-effect can be felt even at considerably lower levels. The injections and the flash are, without a doubt, the strongest secondary reeinforcers and encourage continuation of opioid addiction.

The most patients in the Prove-Project have never subjectively, received enough opioids in earlier substitution programmes. These earlier experiences are due to a restrictive prescriptive dosing and dispension rules and on the other hand, due to the pharmocokinetics of methadone with it’s inevitable steady-state-consumption.

It seems important for us, for therapeutic reasons, that the patients realise that the possibility to experience the biggest and best ‘flash’ is limited. 'The Flash of all flashes, the Superflash, the paradise is even with the best heroin in the world not achieveable. Either the dose is limited to three injections a day or the effect flattens out. Rules from authorities would prevent or hide the learning effect, important to know for the opioid addict, of this question because arguements about doses cover the sensible truth. The disillusion over the possibilities with drugs to have the effect of a constant comfort is a possible, achievable therapeutic effect with diversified drug dispension. Abstract pharmacological explanations concerning the course of dose-effect and maximum effects is rarely helpful for drug addicts because the perception of the effect of heroin in our patients has become something absolute and vital. Our patients need to learn and experience by themselves the course of dose-effect in order to realise how it works; it is of no use trying to force them.

Psychosomatic complaints and placebo effects are observed with surprising regularity in drug addicts. Small colour changes to different degrees were seen to relate to differences in effect in the various outpatient trial clinics of Prove. Pharmaceutical analyses though, showed only a difference in the heroin content of 1%.