Know Your Nose Candy
Crack or Cocaine
Legal and Illicit Compounds
And
How They Work
Outline
Axons (the hardware)
Neurotransmitters (the software)
Drugs (the virus)
Axons – The Hardware
Dendrites at one end
receive stimuli.
Depolarize and allow
charges to cross the
cell membrane
starting an action
potential.
Release stored
chemical messengers
into the synaptic gap.
The Synapse
At the presynaptic
axon,
neurotransmitters are
made and stored.
When released, they
diffuse across a gap,
and bind at a specific
receptor (protein).
The receptor changes
shape and allows for
depolarization.
The Synapse
Binding is reversible.
The neurotransmitter
lets go
Metabolized or taken
back into the original
axon.
Can happen more
than 400 times per
second.
Two Basic States
Excitement
– Axons in this state
release
neurotransmitters that
stimulate other
neurons.
Inhibition
– Axons in this state
release
neurotransmitters that
inhibit other neurons.
Therefore the chemical messengers often occur in
pairs to both stimulate and inhibit various functions.
A sample pair would be GABA and Glutamate
Important Point # 1
Neurotransmitters are small molecules,
whose presence in the synaptic gap
stimulates a response in other axons,
tissues, etc.
Neurotransmitters are removed from the
synaptic gap to end transmission of the
signal.
They can either excite or inhibit activity.
Modes of Action
Agonism
– A compound that
produces more of a
compound, or does
the job of a natural
substance.
– Does not effect the
rate of an enzyme
catalyzed reaction.
Antagonism
– A compound inhibits
an enzyme from doing
its job.
– Slows down an
enzymatically
catalyzed reaction.
– May chemically
appear like a normal
analate.
Important Point #2
Agonists – drugs that create an artificial
stimulus and ‘trick’ the body into doing
something that it would normally do in the
presence of the actual stimulus.
Antagonists – drugs that keep something
in the body from doing its normal job.
Generally this inhibits the reuptake of
neurotransmitters.
Drug Philosophy
Act as either an agonist or an antagonist
for something in the body.
Any psychoactive drug that is
administered plays on the use of
neurotransmitters to do its job.
The drug is not always necessary.
A coach isn’t always necessary either, but
it helps.
Birth Control Medication
Agonist
Basic steroid structure.
Progesterone naturally
released after fertilization
of an egg to limit further
ovulation events.
Original use of
progesterone analogs –
pregnancy promoters.
Enovid – approved for
sale in 1960. GD Searle.
Birth Control Medication
This progesterone
analogs mimics the
natural steroid that is
produced during
pregnancy.
The pill tricks the body
into thinking it is pregnant
to stop ovulation events.
Male version of the pill
developed and tested in
2000.
Caffeine
Basic Information
– The most widely used and abused legal
stimulant in the world.
– Coffee Beans were originally chewed
– Hot extract drinks (coffee) were produced
around 1000 A.D.
– Currently present in soda and coffee
beverages.
Caffeine
Caffeine blocks adenosine receptors.
There is enough caffeine in 2-3 cups of
coffee to block 50% of the adenosine
receptors.
Effects
– Heart stimulation
– Diuresis (excess urination or urine volume)
Caffeine Function
Caffeine blocks adenosine receptors.
Adenosine acts as a neural inhibitor for
CNS activity.
Adenosine is not a neurotransmitter, it is a
neuromodulator.
As caffeine blocks the receptors it acts as
a stimulant.
Caffeine in Excess
Too much caffeine
(6 cups or
more/day)
increases the
number of
adenosine
receptors on axons.
Sluggishness in the
absence of caffeine.
Physiological and
Psychological
addiction.
Where to go to get your fix.
The Illegal Stuff
So lets look at less
than legal stuff.
Agonists, antagonists
Effects on other parts
of the body.
Mode of action.
Ways in which they
are used.
Cocaine
Schedule II
compound. Used for
pain relief for some
procedures.
Cocaine
hydrochloride
Quaternary amine,
charged, white
powder.
CH3
O
H
N
O
OCH 3
O
Crack
Tertiary amine
No formal charge
Fat soluble
Must be smoked
CH3
O
N
O
OCH 3
O
Cocaine - Origins
Found in leaves of
various plants.
Sold in tonics.
Part of the original
Coca-Cola recipe.
Coca leaves chewed
by indigenous
peoples to increase
alertness.
Taking Cocaine
Smoking – (Crack)
Gets to the brain the
fastest (Peak in 1-2
minutes)
Snorting – Cocaine
(Peak in 30 minutes)
Ingestion (Tonic, Leaf
chewing) Low levels
maintained over long
time.
Cocaine Effects
Cocaine is an
antagonist for the
dopamine
reuptake enzyme.
Quickly
metabolized. Half
of the original
dose gone in an
hour.
Blocks reuptake of
norepinephrine,
serotonin, and
dopamine.
Dopamine - Rewards
Since dopamine deals
with rewards, excess
levels leads to
stimulus addiction.
Cocaine is a quick
high so people will
take enough cocaine
to kill themselves,
whereas they would
not choose that with
alcohol.
Amphetamines /
Methylamphetamines
Amphetamines are chiral
compounds.
Levoamphetamine affects
nasal passages.
Dextroamphetamine
enters the brain.
Once given to soldiers in
WWII to promote
alertness and delay
sleep, hunger, etc.
Methylamphetamines
These cause a rapid
release of stored
serotonin and dopamine.
Are not easily
metabolized by the body.
Readsorbed by axons.
Very long effectiveness 810 hours.
Full body effects of
amphetamines
Simulates the fight or flight response.
Basically makes you ready for a fast
response for several hours.
Your heart rate increases, brain function
speeds up.
You are in constant motion.
Other portions of the nervous system get
sensitive to invisible stimuli. ‘Picking’
Detection
THC is metabolized to
another compound.
Detection of 15ng/mL is
legal limit for proof of
exposure to significant
amount. (More than
being passively
surrounded.)
Single use detectable for
up to 3 days. 10 days in
a simple urine analysis.
Continual use detectable
for 28 days or more.
SSRI
Selective Serotonin Reuptake Inhibitors
Serotonin effects mood and appetite in the brain.
Blocks the enzymes that take them up.
Artificially elevates serotonin levels.
Prozac, Celexa, Zoloft, Paxil
Prescription
Since 1986 more than
50 million people
have taken Prozac for
treatment for anything
from anorexia to
panic disorder.
Zoloft is prescribed
for SAD, PTSD, OCD,
PMDD (all entries to
the DSM)
Diagnostic and
Statistical Manual of
Mental Disorders
Arbitrary entries, like
homosexuality.
Easier to obtain an
entry than make a
new drug.
Easier to make a
disease than a cure.
Fin
Vote well.
Be well informed in all of
your choices.
These substances have
effect while you take
them, and after.
Especially for drugs, the
laws are very confusing.
For prescription
medication, know the
rules of how you can be
marketed to.
Mark it 8 dude.