Methadone Synthesis
Dolophine, the trade name of methadone, is notable as being one of the first fully synthetic opiates. It was developed during the second world war when Germany was facing a shortage of opiates due to trade restrictions and embargoes. It turned out to be much cheaper and simpler to synthesize methadone than grow opium.
Methadone consumption by the oral route does not create the huge, massive and intense wave of euphoria that opiates when taken parenterally do. However, it does create an initial opiate buzz, especially in the intolerant user. After continued use, as tolerance builds up, the ability of methadone to create a high is lessened and lessened, until it’s consumption does not so much create a high, but prevents the low of opiate withdrawal. An explanation for why continuous methadone dosing decreasing the euphoriant effect is due to the long duration of action of methadone. Whereas heroin, morphine, and oxycodone all begin to wear off within 4 to 6 hours, the duration of effect of methadone used chronically is about 24 to 36 hours. Thus, a person using parenteral illicit opiates achieves a larger high, followed by a much lower low, the person on methadone does not experience these great changes in opiate activity. It is probable that the continued opiate stimulation is no longer recognized as a high when there is no low to compare it to, and it is the relative difference between on and off that creates the subjective feelings of getting high.
Methadone, when used at appropriate doses in persons addicted to opiates, blocks the craving and hunger for opiates, thus effectively reducing the drive for an addict to inject illicit opiates.. At high doses, it also has the effect of being an opiate blocker (not opiate antagonist). The theory behind this concept is that, at the correct (high) dose, there is so much opiate receptor activation and methadone occupies such a high fraction of opiate receptors, that the addition of more opiates ( such as the injection of heroin or morphine, does not produce any real initial effect. This lack of effect will thus dissuade the user from continuing to supplement his does.
This blockade of supplemental opiates however can lead to attempts at polypharmacy. It is not uncommon for former heroin addicts, when place on methadone maintainance, to try and achieve the previous drug induced euphoria by starting to use stimulants, especially IV cocaine, or crack cocaine.
It also does not wear of as quickly, producing a long lasting, steady, consistent and constant level of activity. The mellow and sedate state that one slips into is like a semi-nod, at least for the first while, until tolerance starts to spoil the party. The fact that it is able to satiate the opiate hunger while still leaving the individual coherent and relatively sober
