Psilocybin mushrooms, which act as a serotonin 5-HT2A receptor agonist like LSD, are a traditional psychedelic. They are currently being studied in psilocybin-assisted therapy for mental health disorders, including emotional distress associated with major depression, anxiety, cluster headaches, and migraines.
To comprehend how shrooms aid in these conditions, it’s crucial to investigate how they metabolize in the body. This understanding allows researchers and users to determine how the active compound elicits psychological and therapeutic effects. This article provides a fundamental rundown of psilocybin’s pharmacology and pharmacokinetics.
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Main Points:
- Half of the psychedelic fungi consumed orally is absorbed and distributed throughout the body.
- The fungi compound undergoes dephosphorylation via the enzyme alkaline phosphatase, primarily in the liver.
- About 3.4% of the compound is excreted in its original form within 24 hours, with the majority being expelled as a stable metabolite.
What is Pharmacokinetics?
Pharmacokinetics (PK) is the study of how the body processes substances, such as drugs, once they enter the system. It’s distinct but related to pharmacodynamics, which examines how a compound interacts with your body. PK delves into four primary aspects: absorption, distribution, metabolism, and excretion (ADME).
Understanding these processes allows healthcare professionals to prescribe the most beneficial medications with minimal risk. It also enables them to tailor treatments to each patient’s unique physiology and lifestyle.
How Pharmacokinetics Applies to Psilocybin?
Psilocybin and psilocin, the dominant active compounds in certain species of magic mushrooms, have sparked considerable interest among researchers and users. Pharmacokinetics examines how the body handles mushrooms that contain psilocybin and helps to understand their potential effects, whether medicinal or recreational.
These compounds are known by several names, including “magic,” “psychedelic,” “medicinal,” or “sacred.” The fungi containing these compounds are consumed, with The species of the mushrooms, their origin, size, the conditions under which they grow and are dried, and their age can cause significant variations in their concentrations.
While these shrooms naturally occur in the wild, scientists have developed methods to synthesize them in a lab. Both natural and synthetic versions exhibit low toxicity, though minor side effects such as nausea or vomiting may occur.
Despite these physical effects, the compounds in the shrooms have shown potential therapeutic benefits due to their safe profile and non-addictive nature. These benefits have led researchers to probe their use in psychotherapy, specifically as a treatment for anxiety and depression.
The 4 Stages of Pharmacokinetics
Psilocybin, the compound found in these mushrooms, is inactive in its original form and works as a prodrug, transforming into its active form, psilocin. Enzymes like alkaline phosphatase aid this conversion, allowing psilocin to be absorbed and circulated throughout the body, reaching various tissues. However, after oral administration, psilocybin cannot be detected in the circulatory system, feces, or urine.
Absorption
Absorption is the mechanism through which the compound enters the bloodstream from its administration site. It influences the speed and efficacy at which the compound reaches its target, such as the plasma. The oral route is the most frequently used for administration. Inhalation has been attempted, but it is not as effective as oral consumption.
The absorption process also involves the release of the compound from the dosage form during oral ingestion. Factors such as a delay in the throat or esophagus can impact this, potentially slowing down results or causing irritation. Once the compound reaches the stomach, the acidic environment may begin to break it down before it enters the bloodstream.
Animal studies indicate that only about 50% of orally administered psychedelics get absorbed and distributed throughout the body.
Factors Influencing the Absorption Process
Several factors can impact the absorption process, causing differences in the onset, intensity, and duration:
- Stomach Contents: Having a full stomach can delay the procedure as it slows down the onset of effects. An empty stomach enables faster absorption.
- pH Levels: An acidic stomach environment facilitates quick dephosphorylation.
- Forms of Psilocybin Mushrooms: The rate of absorption may vary between consuming raw fungi and taking capsules or extracts. Raw fungi tends to break down more rapidly.
The phosphate group in psilocybin possesses strong polarity. Coupled with the positive charge of the amine group, this makes the molecule zwitterionic and enhances its water solubility compared to psilocin. In the absence of the phosphate group, psilocin becomes more lipid-soluble, metabolically accessible, and is more readily absorbed in the intestines.
Metabolism
Metabolism is the means by which the body processes mushroom strains into compounds that can be easily expelled. This process involves increasing the water solubility of the mushroom for effective renal clearance and is necessary for activating its effects.
The liver primarily carries out metabolism in two stages:
- Phase I (CYP450 Reactions): This phase oxidizes hallucinogenic drugs into polar metabolites.
- Phase II (UGT Reactions): This phase conjugates the metabolites to facilitate their distribution.
- These steps disable the drug and prepare it for expulsion via urine or bile.
Once absorbed, the compound undergoes metabolic conversion in the liver. The primary metabolic process is dephosphorylation, where psilocybin is transformed into psilocin by the enzyme alkaline phosphatase. This transformation mainly occurs in the liver. Additionally, secondary metabolic processes can produce various byproducts.
Psilocin is then subjected to extensive Phase I metabolism in the liver to form different metabolites:
- 4-hydroxyindole-3-acetaldehyde
- 4-hydroxytryptophol
- 4-hydroxyindole-3-acetic acid (4-HIAA)
The Phase II metabolism is catalyzed by the UDP-glucuronosyltransferase enzyme family, with UGT1A10 being the chief pathway. Psilocin-O-glucuronide is the primary metabolite found in urine, with 2% to 4% of psilocin being expelled unchanged.
Distribution
Distribution refers to the spread of psilocin throughout the body after it has entered the bloodstream. Being lipophilic, psilocin can cross the blood-brain barrier and reach the central nervous system.
system.Factors such as the size, polarity, and protein-binding ability of the product, along with an individual’s physiology—including hydration levels and body composition—play a significant role in this process.
The objective is to attain an effective concentration at the target site. For it to be effective, the product must reach the designated area, as determined by the volume of distribution, and stay unbound to proteins, enabling it to interact actively with its receptor.
What Influences the Distribution Processes?
The distribution process can be influenced by several factors:
- Body Fat: Substances have the potential to accumulate in fatty tissues, which could potentially extend their effects.
- Age: Metabolic rates and body composition tend to fluctuate with age.
The effects will typically start to appear within 20-40 minutes after consumption, peaking at approximately 80-100 minutes. The effects of magic mushrooms usually last for a duration of 4-6 hours.
How Does Distribution to the Brain Occur?
An early experimental study conducted on two species revealed that the sequence of its binding affinity is 5HT2A > 5HT1A > 5HT2B [23]. It also binds to receptors of dopamine D1, 5HT1E, 5HT5A, 5HT7, 5HT6, D3, 5HT2C, and 5HT1B.
It behaves as a partial agonist at the 5HT2A receptor, with a efficacy of approximately 40%. The psychedelic effects can be attributed to its partial agonist activity at 5HT1A autoreceptors.
The mood-enhancing and psychotomimetic experiences may be due to the observed correlation between elevated dopamine levels and feelings of depersonalization and bliss. Hallucinogens function by altering neurochemistry and receptor activity. It boosts 5HT2A agonist activity by increasing BDNF synthesis in the hippocampus, which in turn promotes neurogenesis and mitigates conditioned fear-related behaviours.
Excretion
Excretion is the process by which the body eliminates a compound, primarily through the kidneys, but also via the lungs, skin, or gastrointestinal tract. In the case of the kidneys, a naturally occurring psychedelic drug is filtered in the glomerulus or secreted in the tubules, with some reabsorption adding complexity to the process.
The main compound has a half-life of approximately 160 minutes, while psilocin’s half-life is around 50 minutes. Animal studies have shown that this is primarily excreted in the urine, accounting for about 65% within 8 After consumption, traces of the substance can still be found in smaller quantities in bile and feces.
In human bodies, approximately 3.4% of the substance is expelled in its original form within a day, while the majority is removed as psilocin-O-glucuronide, a more stable metabolite. This stability enables the compound to be detected in urine samples over an extended period.
There are two primary methods of substance excretion:
- Zero-Order Kinetics: Substance is removed at a consistent rate, independent of its concentration.
- First-Order Kinetics: The rate of elimination is proportional to the drug’s concentration.
Most psychedelic drugs follow the first-order kinetics method, attaining steady-state concentrations after four to five half-lives. Full eradication also takes place after four to five half-lives.
Explore Our Selection of Hallucinogenic Mushrooms
The metabolic process varies amongst different types of fungi. By purchasing from trusted online suppliers like Sero Canada, you can avoid accidentally consuming toxic mushrooms. Some types, such as Agaric mushrooms, may produce strong and unpleasant effects. Therefore, it’s crucial to source magic mushrooms from reputable dispensaries, rather than risky street vendors or wild foraging.
| Feature | Enigma | Full Moon Party | Gold Member |
| Strain Type | Psilocybe Cubensis OMNI | Psilocybe cubensis (Thai Koh Samui) | Psilocybe cubensis |
| Potency | Exceptionally high; 3.8% tryptamine content | Moderate to high potency | High potency |
| Visual Characteristics | Resembles a blob or cauliflower/brain-like structure | Traditional cubensis appearance; moderately sized | Thick white stems; golden caramel caps; noticeable blue bruising |
| Effects | Regarded as the most potent; produces intense effects | Strong mental high; delayed onset with pronounced visuals | Potent visuals and euphoria |
Learn About Psilocybin Mushroom Usage Online
Understanding the pharmacokinetics of shrooms is vital for medical professionals, researchers, and users. With this knowledge, you can make informed choices about dosage and timing, thereby minimizing potential risks.
Find your ideal psychedelic experience at Sero Canada. Whether you’re seeking a calming journey or a more profound exploration, our diverse product range is designed to cater to your specific needs. Experience premium, safe, and quality-controlled shrooms, eliminating concerns about uncertain sources or toxic mushrooms.
Experience the finest magic mushrooms Canada offers and elevate your psychedelic journey to unprecedented levels.
Commonly Asked Questions
Are there any known interactions between shrooms and other medications?
Our products can potentially interact with certain medications, especially those that influence serotonin levels, such as SSRIs (Selective Serotonin Reuptake Inhibitors). SSRIs and SNRIs (Serotonin and Norepinephrine Reuptake Inhibitors) tend to diminish the effects, unlike non-serotonergic antidepressants. This diminished effect can persist for up to three months after ceasing the antidepressant usage.
Do all psychedelics follow the same pathway as psilocybin?
No, each psychedelic substance possesses a unique structure that necessitates distinct metabolic processes to become active, and they bind to various receptors within the body. The method of administration also influences the absorption of each psychedelic. While the fundamental principles of absorption, metabolism, and distribution remain constant, the specific pathways and effects differ for each substance.
Can the form of the shroom influence the pharmacokinetics?
Yes, the form (whether fresh, powdered, or dried mushrooms) can impact the rate of absorption. For instance, powdered forms might be absorbed more rapidly than whole dried ones due to quicker dissolution.
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