Physiological effects of kratom and role in treatment of addiction

Addiction of any type (alcohol, Opioids, Cannabis, Tobacco, Cocaine, Prescription drugs, Amphetamines…) is usually accompanied by serious common symptoms as Fatigue, nausea, headache, constipation, etc. as mentioned before.

Kratom suggested to help in relieving symptoms of addiction, may complement the existing treatments and help in the treatment process through its distinct effects as analgesic, anti-inflamatory action and detoxification effect. Detoxification as known is the initial step of treatment of addiction.

According to recent sources, Mitragyna alkaloids have the ability to alleviate or delay symptoms of opioid withdrawal through its interaction with both adrenergic and opioid receptors.

A. Antinociceptive action:

Intracellularly, when mitraginine binds to the opioid receptor this activates G protein and in turn decreases the activity of adenylyl cyclase and the production of cyclic adenosine monophosphate (cAMP). This leads to increase of potassium efflux, cellular hyperpolarization, a decrease in the influx of Ca2+ by partly blocking of Ca2+ channels and lowering intracellular concentrations of free Ca2+. The net result is a decrease in the release of neurotransmitters thus reduces neuronal excitability and results in analgesia.

Antinociceptive activity of Mitragynine is found to involve the activation of descending noradrenergic and serotonergic pathways in the spinal cord. Through animal studies it was found that mitragynine may stimulate postsynaptic α2-adrenergic receptors and may block 5-hydroxytryptamine2A receptors and this has shown to be inhibited by α2R blocker idazoxan and the non-selective 5-HT antagonist cyproheptadine.

Studies have demonstrated that the minor constituent 7-hydroxymitragynine in Kratom is more potent than mitragynine, even after oral administration as it passes the blood brain barrier and has better oral bioavailability than mitragynine, suggesting it the predominant mediator in exerting the analgesic effects of kratom.

The antinociceptive actions of mitragynine and 7-HM in animal experiments are also inhibited by naloxone.

B. Anti-inflammatory effects

Mitragyna speciosa extract shows strong anti-inflammatory properties in experimental animals and this was recently found to be through mitragynine inhibition of COX-2 mRNA and protein expression as well as PG E2 production in a dose-dependent manner.

C. Detoxification and antibacterial action

A case study reported detoxification in patient after using kratom. The Kratom extracts show antioxidant properties due to a significant increase in glutathione transferase (GST) which is an enzyme plays an important role in detoxifying xenobiotics within the body and protects against toxic injuries.

Traditionally Kratom preparations are used for its antibacterial effects to treat gastrointestinal infections. Recent studies found an antibacterial activity against Salmonella typhi and Bacillus subtilis.

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