Routes of Administration and Dosing for Cannabinoids

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Routes of Administration and Dosing for Cannabinoids

Cannabis can be a great tool for the management of many conditions however due to its legality information is scant on proper dosing. Our trusted third party testing lab SC Laboratories references 10 mg as a standardized dose of cannabinoids, however this could be far too little or far too much depending on the individuals needs and prior cannabis experience. The goal of this article is to the help patients understand what the ideal dose is for them and the best route of administration for that dose to achieve maximum benefits.

Bioavailability and the First Pass Effect

To understand why some routes of administration produce different results one must understand the concept of bioavailability. Bioavailability is defined as the proportion of a drug or other substance that enters the circulation when introduced into the body and is able to have an active effect. Not all routes of administration are equal in terms of bioavailability due to degradation in the stomach, poor absorption, or metabolism by the liver.

Routes of administration that pass through the liver are less effective at drug delivery because of something called the first pass effect. The first pass effect occurs when a drug is transformed into its metabolite(s) via enzymes in the liver. In particular this first pass effect causes the transformation of THC into 11-hydoxy-THC which has significantly stronger psychoactive properties than THC itself. Further metabolism by the liver yields 11-nor-9-carboxy-THC, the body’s storage cannabinoid which then sequesters into the fat or is transformed into its glucoronidated form for excretion.

thc-to-thc-cooh

Routes of Administration

Buccal/Sublingual [10-25%] – A route in which the medication is held in the cheek allowing the drug to diffuse into the oral mucosa and directly into the bloodstream. This can be done between the gum and cheek or sublingually (underneath the tongue). Pure Ratios has developed extended release lozenges that utilize this route as an alternative to oral ingestion with greater bioavailability.

Inhalation [2-56%] – Vaporized or smoked cannabis can provide a rapid onset of effect and allows the patient to titrate the dosage.

Intravenous [100%] – A direct injection of medication into the blood which allows for maximum bioavailability. Not very practical and greatly increases the chance of adverse effects.

Oral [6-10%] – While this route is convenient and has a longer effect, the bioavailability is lower due to first pass metabolism in the liver.

Rectal [~13.5%] – Allows for more of the medication to bypass the liver, hence greatly increasing effect and bioavailability.

Topical [N/A] – Provides localized relief without psychoactive effects because it does not reach the bloodstream. Depending on the matrix in which the cannabinoids are delivered there may be limited penetration beyond the dermal layer and into the blood. Pure Ratios offers patches for localized relief that do not penetrate the dermal layer and hence does not produce psychoactive effects.

Transdermal [80-100%] – Allows for localized relief where the patch is applied while also penetrating into the blood stream. This route of administration greatly increases bioavailability because it bypasses the liver. Pure Ratios has also developed transdermal patches that provide extended relief.

Proper Dosing

When evaluating dosage, one must consider what the treatment goal is, a patient’s level of experience with cannabis, the route of administration used, and the ratios of cannabinoids being administered. For example, if a patient is new to cannabis it is advantageous to start with a higher CBD to THC ratio to avoid adverse effects, especially if the route of administration is inhalation. For example, in an inexperienced cannabis user this dosage could induce adverse effects, especially if administered orally for reasons mentioned above. Conversely, in cancer where the treatment goal is to saturate the body’s ECS to trigger cancer cell death this would be far too little and would have even less of an impact if administered orally due to poor bioavailability.

As mentioned, some testing labs consider a standard dose of cannabinoids as 10 mg. While this serves as a good conservative measure it is certainly not a one size fits all. Studies have demonstrated that cannabinoid receptor density can fluctuate rapidly in a short window of time making tolerance one of the most important factors in dosing [2]. Further adding to the complexity of cannabis dosing is the biphasic response of the cannabinoids. For example, at low doses THC produces and anxiety-relieving effect and induces anxiety at higher doses [3]. For these reasons, any time you are starting a new treatment it’s best to dose conservatively, taking into account parameters like body weight and previous experience with cannabis.

Why Choose Pure Ratios

Pure Ratios has developed product lines that have a treatment plan in mind. Pure Ratio’s transdermal patches and buccal lozenges allow for a controlled release of cannabinoids into the blood allowing the patient to establish a baseline of cannabinoids. Pure Ratios also offers vapor lines that allow for that baseline to be titrated with varying cannabinoid ratios. These blends are also infused with premium essential oils from a variety of healing plants for maximum therapeutic benefit.

References

1. Huestis MA. Human cannabinoid pharmacokinetics. Chem Biodivers. 2007;4(8):1770-804.
2. D’souza DC, Cortes-briones JA, Ranganathan M, et al. Rapid Changes in CB1 Receptor Availability in Cannabis Dependent Males after Abstinence from Cannabis. Biol Psychiatry Cogn Neurosci Neuroimaging. 2016;1(1):60-67.
3. Sexton, M. “Cannabis as an Adaptogenic Herb”. Patients Out of Time 2014 Presentation.

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