Purpose:

What is the purpose of cannabinoid information?

• The purpose of the Endocannabinoid System is to maintain balance in the body (Homeostasis). The ECS modulates almost every physiological process in the body including:
  • Memory
  • Cognition
  • Pain
  • Rest
  • Appetite (hunger)
  • Relaxation
  • Mood
  • Digestive Motility
  • Emotion
  • Anxiety
  • Reproduction
  • Depression
  • Thermogenesis
• All of these processes are influenced by Genetics and Epi-genetics (environmental factors) and are modulated by the ECS
• ECS fine-tunes cellular processes
• Acts in a retrograde (opposite) manner compared to all other neurotransmitters, thus helping to put the brakes on overly aggressive neurotransmission (i.e., pain/inflammatory response)

Components

Three Main Components including cannabinoid information:

1. The Ligands (chemicals that activate receptors) These neurotransmitters are NOT stored, they are made on-demand (unlike all other neurotransmitters that are stored)!
   1. Anandamide in the Brain
   2. 2-ArachadonylGlycerol (2AG) in the peripheral tissue
2. The Receptors (CB1 & CB2)
3. Enzymes that make or brake the Ligands (Fatty Acid Amide Hydrolase) FAAH breaks down Anandamide

Features:

• The largest neurotransmitter system in the body
• Activated by Phyto-Cannabinoids (Cannabidiol – CBD), Cannabigerol (CBG), Tetrahydrocannabinol (THC) which may help establish/maintain balance (Homeostasis)
• Endocannabinoids are made by the body on demand
• Show specificity (act in the area of need)
• Numerous studies have been, and are being conducted showing that a deficiency in the overall functioning of the ECS (called Endocannabinoid TONE) MAY be responsible for, or contribute to chronic illnesses
• A decrease in functionality is commonly referred to as the Endocannabinoid Deficiency Syndrome

What are Terpenes

Terpenes are fragrant oils produced by plants and are believed to function as a way to attract pollinators and/or repel pests. Terpenes are fragile, volatile compounds that are easily lost during the extraction process.

Carbon Dioxide (CO2) extraction separates Terpenes from cannabinoids. In order to return the end product to its natural state, the terpenes must be added back. Terpene manufacturers are able to create products that closely mimic those of the original plant. There are three main sources of Tterpenes used in this process:

1. Terpenes from cannabis
2. Terpenes from Other plants
3. Synthetic terpenes (Petroleum Distillate Based)

The cannabis plant produces a wide variety of different terpenes (over 200), yet NONE are specific to the cannabis plant. The most common being:

• Myrcene
• Terpinolene
• Caryophyllene
• Linalool
• Limonene
• Humulene
• Pinene
• Ocimene

Terpenes are by far, the most underrated compounds in cannabis. They seem to take a backseat to the more popular Phyto-Cannabinoids in popularity when discussing therapeutic potential.

However, recently, worldwide attention has focused on efforts to determine if the terpene profile of a particular cultivar is equally (if not more important) than the cannabinoid profile when determining its potential therapeutic effect(s).

What are the Benefits of Terpenes

Terpenes in cannabis are rapidly becoming recognized as the biggest determining factor for the effects (both physical and psychoactive), of specific cannabis cultivars (aka strains). Research into the medical benefits of terpenes is in the beginning stages.

All of the published data pertains to the effects of isolated terpenes in pre-clinical (non-human) rodent studies. Ultimately, the belief that the greatest therapeutic outcomes will only be achieved when we understand the properties of various cannabinoid and terpene profiles. The activities attributable to these combinations along with the other cannabis constituents (i.e., Flavonoids) account for the overall effects of various cannabis cultivars. This is called the “Entourage Effect.”

As of today, the following benefits have been shown in RODENTS but there are NO robust human trials showing these benefits…

• Myrcene may provide relaxing effects,
• Limonene may alleviate stress and anxiety,
• Caryophyllene is known to relieve inflammation,
• Pinene may help with pain, anxiety, and inflammation.

The “Entourage Effect” describes how the various molecules of the cannabis plant interact with each other to produce the unique effects of various cultivars. Cannabis constituents include:

• 100+ Cannabinoids
• 200+ Terpenes
• 23 Polyphenols
• 7 Alcohols
• 12 Aldehydes
• 13 Ketones

The Entourage Effects differ from those obtained from any of the constituents in isolation. Many researchers who work closely with cannabis believe the entourage effect can dramatically increase the medicinal utility of the Phyto-Cannabinoids THC and CBD, either by magnifying their known effects or by expanding their menu of therapeutic applications.

Laboratory studies may one day establish the existence of the entourage effect beyond a reasonable doubt. That day has not yet arrived, but the research that strongly suggests the effect is real is starting to accumulate, along with ample anecdotal evidence from users whose experiences with medicinal cannabis vary based on the chemical composition of the products they’ve been consuming.

General Information:

• Product effectiveness depends upon more than the amount of drug in a dosage form.
• Effectiveness is directly related to a drugs Bioavailability (How much active drug gets into the body)
• Bioavailability of a drug is dependent upon its “Pharmacokinetic Parameters”
  • Absorption – Amount of drug up taken by the body
  • Distribution – Where the drug goes in the body. Expressed as Volume of Distribution [Vd]
  • Metabolism – All features of how a drug is broken down.
  • Elimination – How a drug and its breakdown products are removed from the body, most commonly through the Liver and Kidneys. This is the “Elimination Rate Constant” [Kel]
• Bioavailability is the amount of active drug getting into the body
• Bioavailability is initially related to Dosage Form, which further relates to onset and duration of action.
  • Intravenous
  • Intramuscular
  • Inhaled
  • Rectal
  • Oral
  • Topical

Liposomes are molecules consisting of an outer Lipid (Fat) Bilayer (Houses Oil-soluble Drugs])and an inner area that (Houses Solid or Water-Soluble Drugs) PRISMM Earth’s topical/transdermal creams use a Liposomal base to carry active drugs through ALL layers of the skin for maximum concentration at the site of application. This means that the topical/transdermal products produced by PRISMM Earth have the greatest Bioavailability (amount of drug reaching the target areas) in the world!

Extended-Release Cannabinoid Information:

The Doctors at PRISMM Earth understand the need for some products to be long-acting. Our Compounding Pharmacists achieve this by adding ingredients that delay the absorption of active ingredients. Delayed absorption translates into an extended duration of action.

Our sleep and pain capsules can be made to have an extended duration of action by incorporating the active ingredients into a Methylcellulose (Organic Cellulose) matrix. The uniform release is achieved by combining the Methylcellulose within a polymeric matrix (E4M) which provides a consistent release into the body.

This dosage form can help decrease the number of doses needed during a day (or night), thus improving compliance, and saving our patients money.

Troches (Lozenges) and Oral (Sublingual) Spray

The PRISMM Earth Troches are placed under the tongue for Sublingual (S.L.) absorption. A significant amount of the active ingredients is absorbed directly into the blood stream through the mucosal lining of the mouth. Under normal circumstances, only a small amount of a drug is swallowed and absorbed through the Gastro-intestinal Tract.

The benefits of this delivery system include a more rapid onset of action than through the oral route, and S.L. absorption bypasses the GI Tract thus eliminating the effects of First Pass Metabolism.

First Pass Metabolism occurs only when a drug is taken orally. The drug goes from the GI Tract directly to the Liver where it is broken down by Liver Enzymes thus reducing the amount of “active” drug up taken by the body.

Our oral spray products also have the features of:

• Sublingual absorption
• Rapid onset of action
• Bypassing “First Pass Metabolism” by the Liver
• Greater amount of active ingredients reaching the site(s) of action
• Provides a STANDARD dosing concentration (mg per spray)

In some cases, the Liver breaks down a drug into metabolites that are also active. When delta-9 Tetrahydrocannabinol (THC) is taken orally, not only is the absorption (and resulting onset of action) delayed for up to 1-2 hours, but some of the THC is metabolized from delta-9 THC to 11-OH THC (known as 11 Hydroxy THC). 11-OH THC has greater intoxicating properties than delta-9 THC!!