Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
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) |