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37 Cards in this Set

  • Front
  • Back
Where does Opium come from?
papaver somniferum "poppy that causes sleep"
most grow between SE Europe and SE Asia
comes as a milky juice
Laudanum
"dream wine"
opium, saffron, cinnamon and cloves dissolved in canary wine
Harrison Narcotic Act (1914)
outlawed cocaine and morphine
fueled by racist journalism
many physicians were incarcerated b/c they prescribed the drug to relieve withdrawl symptoms
Morphine
the active ingredient in opium
named after the Roman God of dreams "Morpheus"
Other active compounds similar to morhpine
codeine, percodan, heroin, vicodin
How much morhpine crosses BBB?
only 10%, it has a hard time crossing lipid membranes.
70% is excreted whole...
Half Lives of common opiates
IV Morphine - 1-3 hours
IV Heroine - 10-20 min
oral codeine - 2-3 hours
oral Vicoden 1.5-3 hours
What are the opiate receptors?
Mu receptors
Delta Receptors
Kappa Receptors
Mechanism of action is similar to marijuana?
Mu Receptors
involved in analgesia, pain relief
opiates reduce neurotransmitter release
Delta Receptors
involved in the euphoric effects
opiates reduce neurotransmitter release
Kappa Receptors
opiates don't bind well here
do the opposite of Mu and K
When opiates bind to these receptors, they reduce the affinity of Mu and K receptors, desensitizing them (so they have the opposite effects)
Where are these receptors found?
highest conc in forebrain, ventral striatum, midbrain, and hindbrain
Endogenous Opioids
large molecule neurotransmitters - peptides
synthesized and packaged in the soma and then carried down the axon into the cleft
along the way enzymes break them down into 3 groups: endorphins, enkephalins, and dynorphins
How do they work
inhibitory
they increase dopamine release indirectly by inhibiting the inhibitor (GABA)
Effects of Opiates
hypothermia
decreased BP
Flushed skin
constricted pupils
constipation
respiratory depression
cough suppression
reduced sex drive
less anxiety
analgesia
3 parts to opiate addiction
1. incentive motivation pathway - wanting of drug
2. intense euphoria - liking of drug
3. intense withdrawl syndrom
Incentive motivation pathway
increased dopamine release
makes you over motivated to get the drug
intense euphoria
post-ingestive effect of euphoria
similar to the first experience of a new food you like
comes before the wanting
most other drugs do not do as good of a job with this part of the reward
naloxone
opioid antagonist
short half-life
give if someone ODs
VERY lipid soluble so ineffective orally
naltrexone
given orally, half life up to 3 days
both can induce withdrawl sypmtoms
Methadone Maintenance
taken orally
half life is 20 hours
occupies the receptor for a long time, internalizes the receptor protein inside the membrane
heroine cannot bind
Suboxone
buprenorphine and naloxone
opiod agonist
half life of 36 hours
better at inducing euphoria
taken sublingual
naloxon is broken down by salivary enzymes before it can be absorbed, prevents people from injecting it.
Where does cocaine come from?
found in South America
from the Erythroxolon Coca Shrub in the Andes
Vin Mariani Wine
cocaine and red wine
actually promoted by the pope
cocaethylene
very toxic byproduct of cocaine and alcohol
John Pemberton
made a beverage with cocaine from coca leaf and caffeine from kola nuts
became very popular during temperance movement
originally a hangover cure
oultawed in Harris Narcotic Act
Powdered (salt) cocaine
water soluble and somewhat lipid soluble, so it will stay in your blood AND cross lipid membranes
cannot vaporize
Free Base Cocaine
separated from the salt
much more lipid soluble so it can cross membranes well, but wont stay in blood so cannot be injected
smoked
Why is free base dangerous?
because you can get pockets of pure ethyl ether which could explode when lighted
Crack Cocaine
safer form that can be smoked
2 parts cocaine, 1 part baking soda
heat gently with a candle
Ephedra
Ma Huang
purified form is a very powerful bronchodilator
treated asthma and narcolepsy
Bioavailablity of cocaine
metabolized rapidly
half life is .5 to 1.5 hours
Bioavailablity of Amphetamine
MUCH slower than cocaine
can take up to 30 min to reach perceivalbe brain conc.
elimination is also much slower
half life 7 to 10 hours
can be extended up to 30 hours depending on urinary pH
How much is excreted whole?
75%
Urinary pH effects
amphetamine is a weak base
Urine pH is around 7 so it ionizes in the urine, making it hard to cross lipid membranes and will NOT be reabsorbed by the body
if you drink basic solutions, it will not be ionized as much
Cocaine mechanism of action
blocks reuptake of neurotransmitter by blocking several transporter proteins:
prefers 5HTT (serotonin transporter) - leads to increased confidence
NET (norepinephrine)
DAT (dopamine)
Amphetamine mech of action
blocks reuptake by blocking trasporter
prefers NET (norepinephrine transporter)
DAT (dopamine)
5HTT (seratonin)