Pharmacokinetics and Pharmacodynamics of Cannabis Pastilles

Understanding the pharmacokinetics and pharmacodynamics of cannabis pastilles, is an important first step in offering Blüm patients the best guidance and treatment possible. This article offers an insightful look into how pastilles are metabolised and absorbed, and how this process compares to other cannabis consumption methods.

With this knowledge in hand, you can offer more thoughtful advice on using cannabis pastilles, helping your patients achieve the best outcomes.
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Edible metabolism and absorption

Cannabis pastilles undergo a complex process of metabolism and absorption that sets them apart from other medicinal cannabis consumption methods. Understanding this process can help healthcare professionals predict the onset, intensity, and duration of edible effects.

When medicinal cannabis pastilles are consumed, it travels through the gastrointestinal (GI) tract where it is broken down by stomach acids and digestive enzymes. The cannabinoids within the edible are absorbed through the intestinal lining into the bloodstream.

Once in the bloodstream, cannabinoids are transported to the liver via the portal vein. In the liver, cannabinoids undergo first-pass metabolism, where they are converted into various metabolites, including 11-hydroxy-THC. This metabolite is notably more potent than THC, which can significantly enhance the psychoactive effects of pastilles. 

Edibles vs Inhalation metabolism and absorption

Inhalation methods, such as smoking or vaping, deliver cannabinoids directly to the bloodstream via the pulmonary system. This direct absorption into the blood allows for a rapid onset of effects, typically within minutes, as the cannabinoids bypass the gastrointestinal tract and hepatic metabolism. Consequently, the duration of these effects is relatively short, generally lasting only a few hours.

In contrast, cannabis edibles (including pastille formats) involve a more complex metabolic process. Upon ingestion, cannabinoids are absorbed through the digestive system and then metabolised in the liver. This digestive and hepatic processing results in a delayed onset of effects, typically occurring 30 to 60 minutes post-ingestion.

During hepatic metabolism, tetrahydrocannabinol (THC) is converted into 11-hydroxy-THC, a metabolite that can produce a more potent and prolonged psychoactive experience compared to cannabinoids administered via inhalation.

Factors that can affect edible metabolism and absorption

• Digestion Speed: The rate at which the digestive system processes the edible can influence the onset of effects. Consuming pastilles on an empty stomach may result in faster onset compared to eating them with a meal, as food can slow down digestion.
  
• Liver Function: The efficiency of liver metabolism varies among individuals due to genetic factors, age, and overall liver health. Variations in liver enzyme activity can affect how quickly and effectively cannabinoids are processed.
  
• Food Intake: The presence of food in the stomach can impact cannabinoid absorption. High-fat meals can enhance the absorption of cannabinoids, as cannabinoids are lipophilic and dissolve better in fats. This may lead to a more pronounced effect compared to when pastilles are consumed without food.

Understanding these aspects of metabolism and absorption can help you predict the effects of cannabis pastilles and tailor your advice to individual patient needs.

Onset, duration, and intensity of edible effects

The effects of cannabis pastilles are distinct from other consumption methods due to the unique metabolic processes involved. Understanding the onset, duration, and intensity of these effects can help you guide patients beginning medicinal cannabis edible treatment plans. 

Onset of Effects

As mentioned, the onset of effects from cannabis pastilles is generally slower compared to inhalation methods. After ingestion, cannabinoids must be digested and absorbed through the gastrointestinal tract before reaching the bloodstream. This process typically takes between 30 to 60 minutes.

However, the exact onset time can vary based on several factors, including individual metabolic rates and food intake. 
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Duration of Effects

The duration of effects from cannabis pastilles is typically extended. These effects can last from 4 to 8 hours or even longer, influenced by several factors:

• Cannabinoid Metabolism: The liver's enzymatic activity, particularly involving cytochrome P450 enzymes, converts THC into 11-hydroxy-THC. This metabolite has a longer half-life and exhibits enhanced psychoactive potency compared to THC, contributing to a more prolonged duration of effects. The variability in individual enzyme activity can further affect the rate and extent of this conversion.
  
• Dosage and Potency: Higher doses and pastilles with elevated THC concentrations generally lead to extended effects. The potency and cannabinoid content of the edible directly impact the duration and intensity of its psychoactive impact, with greater concentrations resulting in longer-lasting effects.
  
• Individual Variability: Variations in liver enzyme activity, such as differences in cytochrome P450 enzyme levels, can also play a significant role in determining the overall duration of the effects. 

Intensity of Effects

The intensity of effects from pastilles can be more pronounced than inhalation due to the presence of 11-hydroxy-THC. This metabolite can produce stronger psychoactive effects and a more intense high. Other factors that may influence the intensity include:

• Dosage: The amount of cannabinoids consumed directly impacts the intensity of effects. Higher doses generally lead to more intense experiences.
  
• Individual Sensitivity: Personal sensitivity to cannabinoids varies. Some patients may experience more pronounced effects, while others might find the effects less intense.

Variability in Effects

The variability in onset, duration, and intensity of effects can be influenced by several additional factors:

• Body Weight and Composition: Cannabinoids are lipophilic and can accumulate in body fat. Individuals with higher body fat may experience a more gradual release and longer-lasting effects.
  
• Liver Health: Variations in liver function and enzyme activity can affect how cannabinoids are metabolised, influencing both the onset and duration of effects.
  
• Interactions with Other Substances: Cannabis pastilles may interact with other medications, which can impact cannabinoid metabolism and alter their effects. Moreover, the consumption of alcohol or other substances can influence how cannabis pastilles affect the body, potentially intensifying or modifying their impact.
  
• Dosage Variability: Inconsistencies in edible formulations can lead to variability in cannabinoid content, impacting the predictability of effects.
  
• Mood, Setting, and Mindset: The environment, emotional state, and patient expectations play crucial roles in the overall experience of pastilles.

Additionally, the consistency and quality of the edible formulation also plays a role in the variability of therapeutic effects, for example:

• Formulation variability: Differing formulation, such as the distribution of cannabinoids, can affect the predictability of effects. Highly-regulated products like Blüm ensure consistent cannabinoid distribution and reliable dosing, enhancing therapeutic reliability.
  
• Quality variability: Products from reputable manufacturers with rigorous quality control measures offer more accurate dosing and reliable effects. Blüm pastilles, for instance, are produced with precise quality control, helping maintain cannabinoid potency and consistency, reducing variability seen in other formats.

Unique Pharmacokinetics and Pharmacodynamics of Blüm Pastilles

Here’s a look at what makes Blüm pastilles distinct in terms of how they are metabolised and how they interact with the body:

Innovative Emulsion and Its Impact

Blüm pastilles incorporate unique emulsion formulas featuring natural emulsifiers derived from Quillaja saponaria, a native Chilean plant, and high oleic sunflower oil. This formulation is designed to enhance cannabinoid absorption, solubility, and bioavailability, leading to a more effective therapeutic experience.

Quillaja Saponaria Extract:

• Saponins: Quillaja saponaria, commonly known as the soap bark tree, contains saponins—natural surfactants that reduce the surface tension of cannabinoids. This reduction facilitates the formation of a stable emulsion, allowing cannabinoids to mix more effectively with the digestive fluids and improving their absorption through the gastrointestinal tract.
  
  Research has demonstrated that saponins can enhance the solubility of lipophilic compounds, such as cannabinoids, by forming micelles. These micelles encapsulate the cannabinoids, making them more readily absorbed across the intestinal lining.

High Oleic Sunflower Oil:

• High oleic sunflower oil is rich in monounsaturated fats, which are beneficial for improving the solubility of cannabinoids. Cannabinoids are lipophilic and dissolve more effectively in fats, leading to better absorption when combined with high oleic sunflower oil.

Studies have shown that fatty acids from oils can enhance the permeability of the intestinal mucosa, which may suggest improved transport of cannabinoids into the bloodstream. This mechanism supports the rapid and efficient absorption of cannabinoids, resulting in a significant increase of bioavailability.

By improving cannabinoid solubility and absorption, the emulsion used in Blüm pastilles may enhance the bioavailability of cannabinoids. This means a greater proportion of the active compounds reach the bloodstream, potentially improving the overall therapeutic efficacy of the product.

The unique emulsion formula may also lead to a more rapid onset of effects compared to traditional pastilles. Faster absorption through the enhanced emulsion can reduce the time it takes for patients to experience the therapeutic benefits of the pastilles.

Pharmacokinetics and Pharmacodynamics of Cannabis Pastilles — In Summary

Understanding the pharmacokinetics and pharmacodynamics of cannabis pastilles is essential for delivering optimal patient care with Blüm products. Pastilles have a unique metabolic process, including conversion to potent metabolites like 11-hydroxy-THC, which sets them apart from other consumption methods such as inhalation.

By considering factors such as digestion speed, liver function, and food intake, healthcare professionals can better anticipate and manage the effects of cannabis pastilles. Blüm’s diverse range of pastilles, with varying THC, CBD, CBN and CBG ratios, allows for tailored treatment plans that meet individual patient needs and support personalised advice.