Description

Simple

A medication derived from cannabis that is used for various medical conditions, such as seizures, certain conditions of severe pain, and muscle spasms in certain disorders affecting the brain and spinal cord.

Clinical

An active cannabinoid used as an adjunctive treatment for the management of seizures associated with Lennox-Gastaut syndrome or Dravet syndrome and symptomatic relief of moderate to severe neuropathic pain or other painful conditions, like cancer.

Overview

Cannabidiol, or CBD, is one of at least 85 active cannabinoids identified within the Cannabis plant. It is a major phytocannabinoid, accounting for up to 40% of the Cannabis plant's extract, that binds to a wide variety of physiological targets of the endocannabinoid system within the body. Although the exact medical implications are currently being investigated, CBD has shown promise as a therapeutic and pharmaceutical drug target. In particular, CBD has shown promise as an analgesic, anticonvulsant, muscle relaxant, anxiolytic, antipsychotic and has shown neuroprotective, anti-inflammatory, and antioxidant activity, among other currently investigated uses [6, 5]. CBD's exact place within medical practice is still currently hotly debated, however as the body of evidence grows and legislation changes to reflect its wide-spread use, public and medical opinion have changed significantly with re... Read more

Pharmacology

Indication

When used in combination with delta-9-tetrahydrocannabinol as the product Sativex, cannabidiol was given a standard marketing authorization (ie. a Notice of Compliance (NOC)) by Health Canada for the following indications:
1) as adjunctive treatment for symptomatic relief of spasticity in adult pa... Read more

Pharmacodynamic

Although the exact mechanism and magnitude of effects of THC and CBD are not fully understood, CBD has been shown to have analgesic, anticonvulsant, muscle relaxant, anxiolytic, neuroprotective, anti-oxidant, and anti-psychotic activity. This wide variety of effects is likely due to it's complex pha... Read more

Mechanism of action

The exact mechanism of action of CBD and THC is not currently fully understood. However, it is known that CBD acts on cannabinoid (CB) receptors of the endocannabinoid system, which are found in numerous areas of the body, including the peripheral and central nervous systems, including the brain. Th... Read more

Absorption

Following a single buccal administration, maximum plasma concentrations of both CBD and THC typically occur within two to four hours. When administered buccally,
blood levels of THC and other cannabinoids are lower compared with inhalation of smoked cannabis. The resultant concentrations in the blo... Read more

Protein binding

Information currently not available.

Volume of distribution

Cannabinoids are distributed throughout the body; they are highly lipid soluble and accumulate in fatty tissue. The release of cannabinoids from fatty tissue is responsible for the prolonged terminal elimination half-life.

Clearance

Information currently not available.

Half life

The CBD component of sublingual Sativex was found to have a half life (t1/2) of 1.44hr, while buccal Sativex was found to have a half life (t1/2) of 1.81hr.

Route of elimination

Elimination from plasma is bi-exponential with an initial half-life of one to two hours. The terminal elimination half-lives are of the order of 24 to 36 hours or longer. Sativex is excreted in the urine and faeces.

Toxicity

Information currently not available.

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type

Contraindications

Information currently not available.

Food Interactions

Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of sedation.

Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of cannabidiol, which may increase its serum concentration. Cannabidiol dose reduction may be necessary if used together.

Avoid St. John's Wort. This herb induces the CYP3A metabolism of cannabidiol and may reduce its serum concentration. The dose of cannabidiol may need to be increased if used together.

Take with food. Taking cannabidiol with food (particularly high-fat food) increases its bioavailability. The absorption of cannabidiol is more consistent when meal macronutrients remain the same.