Products
In many countries, there are currently no medicines approved that contain only cannabidiol. However, the active ingredient is a component of the cannabis oral spray Sativex, which is registered as a drug for MS treatment in many countries and also contains THC. The oral solution Epidiolex or Epidyolex was approved as a drug in the U.S. in 2018 and is also pending approval in the EU. Cannabidiol can be used for the preparation of extemporaneous preparations in many countries (source: Swissmedic, 2018). Unlike tetrahydrocannabinol, cannabidiol is not an anesthetic. Since many countries allow the sale of hemp with a THC content of less than 1%, hemp flowers with a high content of CBD and a low THC content are sold as tobacco substitutes. Other products such as dietary supplements, cosmetics, drops, and chewing gum are available. see also under cannabidiol hemp
Structure and properties
Cannabidiol (C21H30O2, Mr = 314.5 g/mol) is a natural cannabinoid from hemp (, ) that is found in high concentrations in the female plant. Cannabidiol is a lipophilic molecule and is therefore well distributed throughout the body and into the central nervous system.
Effects
Cannabidiol has antiepileptic (anticonvulsant), antianxiety, neuroprotective, antipsychotic, anti-inflammatory, antiemetic, and antioxidant properties. Unlike Δ9-tetrahydrocannabinol (THC), it is not psychoactive (euphoric) and does not bind as an agonist to the CB1 and CB2 receptors. Cannabidiol is a multi-target drug. Its effects are attributed to its interaction with various systems. These include the ENT transporter, the GPR55 receptor, serotonin receptors (5HT1A), PPAR receptors, and the TRPM8 channel.
Indications for use
- For the treatment of epilepsies in children: Dravet syndrome, Lennox-Gastaut syndrome, tuberous sclerosis, infantile spasms (epidiolex, epidyolex).
- Other indications for use are being investigated. These include, for example, psychotic disorders and neurodegenerative diseases.
- Hemp flowers with high CBD and low THC content are smoked as a stimulant and intoxicant.
- As a dietary supplement, CBD is used, among other things, as a sedative and against sleep disorders.
Dosage
According to the SmPC. CBD can be administered perorally, topically, buccally and by inhalation, among others. It is recommended that the drops be held slightly in the mouth so that the active ingredient is absorbed through the oral mucosa. This may bypass first-pass metabolism.
Contraindications
Refer to the drug label for complete precautions.
Interactions
Cannabidiol is a substrate of CYP450 isozymes and corresponding drug-drug interactions are possible (CYP3A, CYP2C). Cannabidiol undergoes high first-pass metabolism, producing the metabolite 7-OH-CBD.
Adverse effects
During administration of the epilepsy drug Epidiolex, adverse effects included diarrhea, drowsiness, poor appetite, fever, and vomiting.