Controversial Kratom Growing in Popularity

The dominant alkaloid in kratom can exert somewhat selective μ-opioid receptor activity
The dominant alkaloid in kratom can exert somewhat selective μ-opioid receptor activity

A complex, poorly understood plant product, kratom, or Mitragyna speciosa, has recently burst onto the American stage in a big way and gained the attention of the US Food and Drug Administration (FDA), as well as the Drug Enforcement Administration (DEA). Mitragynine, the dominant alkaloid in the compound, has been found to have some opioid-like activity and some argue that it is useful in assisting patients who are withdrawing from either licit or illicit narcotic use. The debate about potential DEA regulation of this compound is, more than likely, just beginning.

Background

Kratom grows naturally in much of southeast Asia, more specifically, in Malaysia.1 This evergreen tree can reach a height of more than 80 feet with a trunk diameter of 3 feet.1 The large, dark glossy green leaves yield the extract that is the active component of the tree.

Kratom has been used in its native environment for centuries for purposes ranging from religious ceremonies to wound healing. Its action as an opium substitute, however, was reported in 1836.2 Official notation of this plant and its action was first made by Dutch botanist Pieter Korthals in 1839.3 Despite centuries of use in Malaysia, the compound has been relatively slow to develop a following in the United States, but that appears to be changing.

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Science

The main mechanism of action of kratom is due largely to one of the more than 25 alkaloids found in its extract.4 Mitragynine, the dominant alkaloid, has been found to exert somewhat selective μ-opioid receptor activity, especially when used in moderation.5 Proponents of this chemical argue that it is useful in assisting patients who are withdrawing from either licit or illicit narcotic use. Those against the use of kratom take the stance that, since its action is basically opioid in nature, nothing is gained.

There are no clinical trials in humans to determine either the safety or efficacy of kratom. However, a growing body of laboratory data shows some very intriguing actions of the extract. One study demonstrated both adrenergic and serotonergic actions, as well as actual opioid antagonistic functions.6 These activities are seen as promising means to ease withdrawal from narcotic dependence.

In the absence of human clinical trials based in the United States, we are forced to depend largely upon pharmacokinetic data and foreign trials. One case report highlights the differing actions of kratom based on total daily dose.7 In this report, a man in his early 40s was using escalating doses of prescribed hydromorphone for a chronic pain condition. Due to a sudden change in his personal life, he was forced to abruptly cease use of this potent drug. In order to manage his intense symptoms of withdrawal, he began ingesting a kratom tea four times a day. He found that the tea greatly alleviated his physical pain without the typical sedation from prescription medication.7