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Psilocybin mushrooms, functionally similar to LSD as they both act as serotonin 5-HT2A receptor agonists, are a traditional form of psychedelic. Current research is exploring their potential role in psilocybin-assisted therapy to treat mental health disorders, such as emotional distress linked to major depression, anxiety, cluster headaches, and migraines.

To understand how shrooms alleviate these conditions, it’s essential to explore their metabolism in the body. This knowledge equips researchers and users with insights into how the active compound triggers psychological and therapeutic effects. This article offers a basic overview of psilocybin’s pharmacology and pharmacokinetics.

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Key Takeaways:

  • When psychedelic fungi are consumed orally, half is absorbed and dispersed throughout the body.
  • The fungal compound is dephosphorylated by the enzyme alkaline phosphatase, primarily in the liver.
  • Approximately 3.4% of the compound is expelled in its original form within 24 hours, while most is secreted as a stable metabolite.

What Does Pharmacokinetics Mean?

Pharmacokinetics (PK) is the scientific study of how substances, such as drugs, are processed by the body once ingested. It is related to, but different from, pharmacodynamics, which explores how a compound interacts with the body. PK primarily focuses on four aspects: absorption, distribution, metabolism, and excretion (ADME).

Understanding these processes helps healthcare professionals prescribe the most effective medications with minimal risk. It also allows them to customize treatments according to each patient’s unique physiological and lifestyle needs.

How is Pharmacokinetics Relevant to Psilocybin?

Psilocybin and psilocin, the main active ingredients present in certain types of magic mushrooms, have generated significant interest among researchers and users. Pharmacokinetics investigates how the body processes mushrooms containing psilocybin, providing insights into their potential medicinal or recreational effects.

These compounds, referred to as “magic,” “psychedelic,” “medicinal,” or “sacred,” are found in fungi that are consumed. The Mushroom species, their place of origin, size, growing and drying conditions, and age can cause substantial variations in their concentrations.

Even though these mushrooms are naturally occurring, scientists have devised methods to create them in laboratories. Both the naturally occurring and lab-made versions exhibit low toxicity, although minor side effects like nausea or vomiting might occur.

In spite of the physical effects, these mushrooms’ compounds have demonstrated potential therapeutic benefits due to their safe profile and non-addictive characteristics. These benefits have prompted further research into their use in psychotherapy, particularly in treating anxiety and depression.

The 4 Stages of Pharmacokinetics

The compound found in these mushrooms, psilocybin, is inactive in its original state and functions as a prodrug, converting into its active form, psilocin. Enzymes such as alkaline phosphatase facilitate this conversion, enabling psilocin to be absorbed and circulated throughout the body, reaching various tissues. However, psilocybin cannot be detected in the circulatory system, feces, or urine after oral administration.

Absorption

Absorption refers to how the compound enters the bloodstream from the site of administration. This process affects the pace and effectiveness of the compound reaching its intended target, such as the plasma. The most common method of administration is oral, while inhalation has been tried but is less effective.

The absorption process also entails the compound’s release from the dosage form during oral ingestion. Factors like delay in the throat or esophagus can influence this, potentially slowing down the effects or causing discomfort. Once the compound arrives at the stomach, the acidic environment might start to decompose it before it infiltrates the bloodstream.

Animal studies suggest that only around 50% of orally administered psychedelics are absorbed and distributed throughout the body.

Factors Influencing the Absorption Process

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

  1. Stomach Contents: The presence of food in the stomach can delay the process as it slows the onset of effects. Faster absorption is enabled by an empty stomach.