Lecture 16 - Cannabinoids Flashcards
a genus of flowering plant which contains many bioactive compounds
cannabis
what are the two major bioactive compounds that come from the cannabis plant that have been studied?
tetrahydrocannabidiol (THC) and cannabidiol (CBD)
what is the primary psychoactive compound in cannabis?
THC
a class of chemical compounds that act at the cannabinoid receptors
cannabinoids
cannabis contains hundreds of non-cannabinoid constituents, including _____ which give the plant its characteristic smell
terpenoids
in vitro and in vivo studies found some terpenoids to have:
anti-inflammatory, anti-bacterial and anti anxiety effects
have any clinical studies been conducted on terpenoids?
no
why are cannabis constituents difficult to study?
there is the possibility of synergy between compounds
the fraction of an administered drug that reaches its effectors
absorption/bioavailability
what is the most rapid and efficient method of delivering THC to the body?
smoking
the bioavailability of smoked THC is _____, reaching peak plasma concentration in _____
25%, 6-10 minutes
the bioavailability of ingested THC is _____, reaching peak plasma concentration in _____
6%, 2-6 hours
why is THC so readily taken up by the body tissues (particularly those with high blood flow)?
it is highly lipophillic
true or false: tissues with low blood flow accumulate THC more slowly and release it over a long period of time
true
in frequent cannabis smokers, THC is stored in _____ and can be released into the blood for _____
fat, days
THC metabolism occurs mostly in the liver by:
cytochrome P450 2C9 (CYP 2C9)
metabolism of THC produces:
11-OH-THC and THC-COOH
within five days, ____% of a THC dose is excreted
80-90
cannabinoid receptors are:
inhibitory GPCRs (Gi coupled)
what are the two types of cannabinoid receptors?
CB1 and CB2
CB receptors lead to decreases in ______ accumulation which inhibits _______
cAMP, the influx of calcium in the firing neuron (inhibits neurotransmitter release)
overall, activating cannabinoid receptors will:
decrease synaptic transmission and inhibit neurotransmitter release
THC is a:
partial agonist at CB1
while the CBD mechanism of action is poorly understood, there is some evidence to suggest that it can act as:
a negative allosteric modulator at CB1