Tramadol Hydrochloride is a known synthetic analogue of codeine. This drug is a centrally acting analgesic with a recorded low affinity for opioid receptors. Only recently has it been shown to posses a selectivity for mu receptors partly responsible for its analgesic effects. This is the main reason why it is compared to morphine, hydrocodone and other such drugs. And because of its agonistic actions in the opioid receptors it has been described as “narcotic-like.” This description of the drug has attracted recreational users.
Its M1 metabolite, as produced by liver O-demethylation, shows a significantly higher affinity to opioid receptors than its original form. This is characteristic of a prodrug. A prodrug is any pharmacologic substance that is administered in an inactive form. Only after administration and being metabolized shall the prodrug be termed active. This process is called bioactivation. The reason behind the use of prodrugs is generally to optimize absorption, distribution, metabolism, and excretion, otherwise known as ADME. Besides this, prodrugs have increase selectivity for its intended target. The enhanced selectivity of Tramadol HCl enables it to target the mu opioid receptors, and the mu opioid receptors only. By doing so, it does not produce the effects caused by an affinity with the other receptors like delta, kappa and sigma. If at all, these effects are rare and hardly noticeable.
Even with its established affinity to mu receptors of the central nervous system, the degree is exponentially low compared to morphine by 6000 times. In contrast to other opioids, the painkilling action of the drug is only partly inhibited by naloxone, which is a known opioid antagonist and overdose antidote. This strongly suggests that there exists another mechanism of action for its analgesic effects. The notion was proven by the detection of the monoaminergic activity inhibiting norepinephrine and serotonin reuptake. Its effect is a significant increase in analgesic function by stopping nociceptive signals at the spinal level.
As a recreational drug, users take about 150mg to produce euphoric effects. However, the euphoria is a very subjective feeling and some people who have reported to take up to an unbelievable 600-6500mg (single dose) of the drug and miraculously lived to tell about it say it eventually fades away due to tolerance. Others who have taken Tramadol for pain and went beyond their prescribed dosages and taken up to 350mg (also as a single dose) claimed to have felt no euphoria or any feeling of being high at all. Then again, the feeling is subjective and depends from person to person.
The value and demand of Tramadol in the streets is not as high as other recreational drugs. It can also be acquired easily in the internet without prescription from a doctor. Even from a medical provider, the drug can be easily procured as it is not a Scheduled, or considered as a controlled drug.
Tramadol’s selectivity and chemical composition limits the euphoria and high felt from the drug. This is the reason why it is not Scheduled. Taking it at very large doses to accumulate the high is not a very bright idea. Overdose will occur and users can die a horrible death.