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Psilocybin mushrooms, similar to LSD, function as a serotonin 5-HT2A receptor agonist and are considered a classic psychedelic. Currently, these mushrooms are under investigation for their potential use in psilocybin-assisted therapy for mental health disorders, such as severe depression-related emotional distress, anxiety, cluster headaches, and migraines.

Understanding how shrooms can help with these mental conditions requires a detailed study of their metabolism in the body. This knowledge allows both researchers and users to ascertain 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:

  • Upon oral consumption, half of the psychedelic fungi is absorbed and dispersed throughout the body.
  • The fungi compound undergoes dephosphorylation by the enzyme alkaline phosphatase, predominantly in the liver.
  • Approximately 3.4% of the compound is excreted unchanged within 24 hours, with the majority being eliminated as a stable metabolite.

What is Pharmacokinetics?

Pharmacokinetics (PK) is the science of how the body deals with substances, such as drugs, once they are ingested. While similar, it’s distinct from pharmacodynamics, which focuses on how a compound interacts with your body. PK explores four main components: absorption, distribution, metabolism, and excretion (ADME).

Grasping these processes empowers healthcare providers to prescribe the most effective medications with the least risks. It also allows them to customize treatments according to each patient’s unique physiology and lifestyle.

How Pharmacokinetics Relates to Psilocybin?

Psilocybin and psilocin, the primary active compounds in specific species of magic mushrooms, have piqued the interest of researchers and users alike. Pharmacokinetics provides insights into how the body metabolizes mushrooms containing psilocybin and facilitates understanding their potential medicinal or recreational effects.

These compounds are known by various names, such as “magic,” “psychedelic,” “medicinal,” or “sacred.” Fungi containing these compounds are ingested, and the Mushroom species, their places of origin, sizes, the conditions under which they flourish and dry, plus their age, can all lead to significant fluctuations in their concentrations.

Even though these mushrooms naturally grow in the wild, scientists have discovered ways to artificially create them in laboratories. Both the natural and lab-grown versions are marked by low toxicity, but minor side effects like nausea or vomiting may still occur.

Despite these physical side effects, the compounds in these mushrooms have demonstrated potential therapeutic benefits due to their safety profile and non-addictive properties. These advantages have sparked researchers’ interest in exploring their application in psychotherapy, particularly for treating anxiety and depression.

Understanding the 4 Stages of Pharmacokinetics

Psilocybin, the compound found in these mushrooms, is dormant in its natural state and acts as a prodrug, converting into its active form, psilocin. Enzymes like alkaline phosphatase facilitate this change, enabling psilocin to be absorbed and distributed throughout the body, reaching various tissues. However, after oral administration, psilocybin is undetectable in the circulatory system, feces, or urine.

Absorption

Absorption refers to the process where the compound enters the bloodstream from its point of administration. It affects how quickly and effectively the compound reaches its target, such as the plasma. Oral ingestion is the most common administration route. Inhalation has also been tried, but it’s not as efficient as oral intake.

The absorption process also entails the release of the compound from the dosage form during oral ingestion. Factors like delays in the throat or esophagus can influence this, potentially slowing the results or causing irritation. Once the compound reaches the stomach, the acidic environment may start to degrade it before it enters the bloodstream.

Studies conducted on animals suggest that only about 50% of orally administered psychedelics are absorbed and distributed within the body.

Factors Affecting the Absorption Process

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

  1. Stomach Contents: Eating before the procedure can delay the process as it slows down the onset of effects. Conversely, an empty stomach facilitates quicker absorption.

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