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Cannabidiol (CBD)

CBD is one of more than 100 compounds in recreational cannabis.

It does not have potent psychoactive effects of its chemical cousin delta-9-tetrahydrocannabinols (THC).

It’s only FDA-improved indication is to treat intractable seizures in patients with Lennox-Gestaut syndrome or the Dravet syndrome.

More Americans use products infused with cannabidiol (CBD) than use marijuana or other illegal drugs.

CBD, one of marijuana’s active ingredients, has risen in prominence despite a lack of scientific understanding or careful regulation of the substance.

Gallup poll found that 14 percent of U.S. adults, roughly one in seven, personally use CBD products.

CBD is more popular than all the major illicit drugs combined, outpaced only by past-month use of cigarettes and alcohol.

That popularity is driven in large part by young people.

CBD is one of the active ingredients in marijuana; tetrahydrocannabinol, also known as THC, is the other main one.

It is derived from hemp.

The 2018 Farm Bill legalized the cultivation of hemp and removed it from the schedule of controlled substances, thereby permitting the production of CBD goods.

Importantly, the actual sale of CBD products for therapeutic purposes is still basically illegal unless approved by the Food and Drug Administration, which has only signed off on a single CBD-derived drug.

CBD in non-medical applications, like food, is legal.

Has been approved for treatment of epilepsy.

CBD  bioavailability from smoked product may be around 31%.

Trials have identified liver abnormalities, diarrhea, fatigue, vomiting, and somnolence as side effects.

Animal studies have found side effects including: hypotension, central nervous system toxicity, and harms to the male reproductive system.

It may be beneficial for anxiety, insomnia and chronic pain.

Cannabidiol (CBD) is a phytocannabinoid.

It is one of some 113 identified cannabinoids in cannabis plants and accounts for up to 40% of the plant’s extract.

Routes ofadministration:

Inhalation (smoking, vaping), buccal (aerosol spray), oral (solution).

Hemp-derived.

Bioavailability

• Oral: 13–19%

• Inhaled: 31%

Elimination half-life 18–32 hours.

Can be taken in multiple ways, including: inhalation of smoke or vapor, as an aerosol spray into the cheek, and by mouth.

It may be supplied as CBD oil containing only CBD as the active ingredient.

It does not have the same psychoactivity as THC.

If taken with THC it may change the effects of THC.

Cannabidiol may reduce THC clearance, increasing plasma concentrations which may raise THC availability to receptors and enhance its effect in a dose-dependent manner.

Its mechanism of action for its biological effects has not been determined.

As of 2019 the cannabidiol drug Epidiolex has been approved for the treatment of 2 types of epilepsy.

Side effects include: somnolence, decreased appetite, diarrhea, fatigue, malaise, weakness, and sleeping problems.

As of July 2019 it is a Schedule I controlled substance that is illegal for use in human foods, dietary supplements, other consumer products, or pet foods.

For refractory epilepsy, limited research has shown some efficacy in combination with conventional anti seizure medications.

Combination medication did not eliminate seizures.

Its use in other neurological disorders, research has not established clinical usefulness.

It may inhibit receptors affecting the activity of voltage-dependent sodium and potassium channels, which may affect neural activity.

Little is known about potential drug interactions, but it decreases clobazam metabolism.

Cannabidiol has low affinity for the cannabinoid CB1 and CB2 receptors.

Cannabidiol can act as an antagonist of CB1/CB2 agonists despite their low affinity.

Cannabidiol may be an antagonist of GPR55, a G protein-coupled receptor and cannabinoid receptor that is expressed in the caudate nucleus and putamen in the brain.

It may act as an inverse agonist of GPR3, GPR6, and GPR12, and as a serotonin 5-HT1A receptor partial agonist.

It is an allosteric modulator of the μ- and δ-opioid receptors.

Its pharmacological effects may involve PPARγ agonism and
intracellular calcium release.

The elimination half-life of CBD is 18–32 hours.

It is metabolized in the liver as well as in the intestines by CYP2C19 and CYP3A4 enzymes, and UGT1A7, UGT1A9, and UGT2B7 isoforms.

Epidiolex is an orally administered cannabidiol solution approved in 2018 by the US Food and Drug Administration for treatment of two rare forms of childhood epilepsy, Lennox-Gastaut syndrome and Dravet syndrome.

Numerous products are marketed as containing CBD, but in reality contain little or none.

In the US, hemp is classified by the federal government as cannabis containing no more than 0.3% THC by dry weight.

Does not appear to have any psychotropic effects such as those caused by ∆9-THC in marijuana.

It may have anti-anxiety and anti-psychotic effects.

In September 2018, following its approval by the FDA for rare types of childhood epilepsy, Epidiolex was rescheduled as a Schedule V drug to allow for its prescription use.

All other CBD-containing products remain Schedule I drugs.

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