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Psilocybin mushrooms, also known as traditional psychedelics, function similarly to LSD by acting as a serotonin 5-HT2A receptor agonist. Currently, research is being conducted on their potential use in therapy for mental health issues, including anxiety, major depression, emotional distress, cluster headaches, and migraines.

Understanding how shrooms can help with these conditions requires a closer look at how they are metabolized in the body. This knowledge enables both researchers and users to grasp how the active compound produces its psychological and therapeutic effects. This article offers a basic overview of the pharmacology and pharmacokinetics of psilocybin.

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Key Takeaways:

  • When consumed orally, half of the psychedelic fungi is absorbed and distributed in the body.
  • The compound in the fungi undergoes dephosphorylation through the action of an enzyme called alkaline phosphatase, primarily in the liver.
  • Within 24 hours, approximately 3.4% of the compound is expelled in its original form, while the majority is eliminated as a stable metabolite.

What Does Pharmacokinetics Mean?

Pharmacokinetics (PK) is a field of study that explores how substances, such as drugs, are processed once they enter the body. While it’s related to pharmacodynamics, which analyses how a substance interacts with the body, PK focuses primarily on four aspects: absorption, distribution, metabolism, and excretion (ADME).

By understanding these processes, healthcare providers can prescribe the most effective medications with the least amount of risk. This knowledge also allows them to customize treatments based on each patient’s individual physiology and lifestyle.

How Does Pharmacokinetics Relate to Psilocybin?

Psilocybin and psilocin, the primary active compounds in certain types of magic mushrooms, have garnered significant attention from researchers and users. Pharmacokinetics provides insights into how the body processes mushrooms containing psilocybin, aiding in understanding their potential effects, whether therapeutic or recreational.

These compounds, often referred to as “magic,” “psychedelic,” “medicinal,” or “sacred,” are found in consumed fungi. The types of mushrooms, their place of origin, size, growing and drying conditions, along with their age, can drastically affect their potency.

Although these mushrooms are naturally occurring, scientists have mastered techniques to create synthetic versions in the laboratory. Both natural and lab-made variants demonstrate low toxicity, though they may induce minor side effects such as nausea or vomiting.

Despite these mild physical reactions, the compounds in these mushrooms have demonstrated potential therapeutic benefits due to their safety and non-habit forming characteristics. This has prompted researchers to explore their use in psychotherapy, particularly as a treatment for anxiety and depression.

The 4 Phases of Pharmacokinetics

Psilocybin, the compound found in these mushrooms, is inactive in its raw state and acts as a prodrug, converting into its active form, psilocin. Enzymes such as alkaline phosphatase facilitate this transformation, allowing psilocin to be assimilated and distributed throughout the body, reaching various tissues. However, after oral ingestion, psilocybin is undetectable in the circulatory system, feces, or urine.

Absorption

Absorption refers to the process where the compound enters the bloodstream from the site of administration. It determines the rate and efficiency at which the compound arrives at its target, such as the plasma. The most common route of administration is oral. Inhalation has been tested, but it does not prove as effective as oral intake.

The absorption process also includes the liberation of the compound from the dosage form during oral ingestion. Aspects like a delay in the throat or esophagus can affect this, potentially delaying effects or causing discomfort. Once the compound reaches the stomach, the acidic environment may start to degrade it before it enters the bloodstream.

Studies on animals suggest that only around 50% of the orally administered psychedelics are absorbed and dispersed throughout the body.

Factors Affecting the Absorption Process

A number of factors can affect the absorption process, leading to variations in the onset, intensity, and duration:

  1. Stomach Contents: Consuming the compound on a full stomach can delay the process as it slows the onset of effects. Absorption occurs faster when the stomach is empty.

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