Phytocannabinoids

Question 1

What are the constitutive ingredients in phytocannabinoids

Answer 1

Psychoactive ingredient:
- Tetrahydrocannabinol (THC) identified in 1964
- THC binds and activates receptors
 Non-psychoactive ingredient:
- Cannabidiol (CBD) identified in 1934
- Binds but doesn’t activate receptors
 Different plants have different levels of these two components which can affect their
us
- Cannabis Sativa: THC > CBD
- Cannabis Indica: CBD < THC

Question 2

What are the different types of cannabinoids

Answer 2

Plant-derived cannabinoids/phytocannabinoids = naturally occurring and found in
plants
 Synthetic cannabinoids = not found in nature
 Endogenous cannabinoids = naturally occurring and produced by our body

Question 3

What are the cannabinoid receptors

Answer 3

CB 1 /CB 2 RECEPTORS
 GPCR receptors = both Gi/o coupled
 The two receptors have 44% homology = quite different
 CB 1 is one of the most highly expressed GPCRs in the brain
 CB 2 is mostly found in the periphery
 Distinctive pharmacology depending on the binding of an agonist or antagonist

Question 4

Describe CB1 signalling

Answer 4

• Inhibits adenylyl cyclase
• Inhibits voltage gated Ca2+ channels
• Activates inwardly rectifying K+ channels
• Activates MAP kinases

 CB1 is predominantly in pre-synaptic neurones and its activation will reduce
neurotransmitter release
 If those short-term responses took place in a
glutaminergic neurone there would be different
effects to a GABA neurone = glutamate is
excitatory, and GABA is inhibitory = not just one
mechanism for all neurones

Question 5

What neurotransmitters are involved in CB1 neurotransmission

Answer 5

Certain pathways have a lot of CB1 receptors, for
example the reward pathway
 Involve a range of neurotransmitters
- Glutamate
- GABA
- Dopamine
- Acetylcholine
- Noradrenaline
- CGRP
 Evidence from brain slices and animals/tissues with intact innervation
 Modulate functions in the brain, cardiovascular and respiratory system, gut motility

Question 6

What are the effects of Cannabis through CB2

Answer 6

CANNABIS EFFECTS THROUGH CB2
 THC is also a partial agonist at CB2
 Anti-inflammatory effect
 Immunosuppressive effect
 Analgesic
 Peripheral vs central CB2
- Atherosclerosis
- Microglia; neuroinflammation; neurodegeneration

Question 7

Describe the medicinal use of cannabinoids

Answer 7

Mismatch of bodies of evidence that discuss the medicinal benefits of cannabis
 Synthetic partial agonists of CB1 and CB2 are 100 times more potent than THC
 Some of these agonists can be found in (il)legal highs

Question 8

What is Nabilone

Answer 8

Nabilone is a synthetic analogue of THC
- Marketed since 1983
- Suppression of nausea and vomiting during chemotherapy
- And anorexia in AIDS patients = makes individual feel hungry (munchies)

Question 9

Whatt is Sativex

Answer 9

first purified standardised cannabis medicinal extract = THC: CBD at equal
ratio = used for pain management but does have side effects

Question 10

what is Cannabidiol

Answer 10

Cannabidiol could be used in some specific forms of epilepsy

Question 11

what is Epidiolex

Answer 11

Epidiolex used for seizures associated with Lennox-Gastaut syndrome or Dravet
syndrome

Question 12

LEGISLATION AND REGULATION of cannbinoids

Answer 12

Cannabis is a controlled drug under Misuse of Drugs Act 1971

 Cannabis oil with less than 0.2% THC can be licensed and may be prescribed by a
specialist hospital doctor
 Cannabidiol products, if advertised for medical purposes, are regulated by Medicines
and Healthcare products (regulatory agency)
 Epidiolex (cannabidiol) for seizures associated with Lennox-Gastaut syndrome or
Dravet syndrome