opioid 1 Flashcards
what is happening to fentanyl related accidental opioid poisoning deaths over time
they are increasing (compared to non-fentanyl opioids)
what are almost all opioid poisoning deaths caused by
fentanyl
which drugs often are laced with fentanyl
meth
cocaine
heroin
has the % of heroin that contains fentanyl increased or decreased in recent years
increased to 60% in 2017
what does opioid mean
term to describe both natural and synthetic compounds that have properties similar to opium or morphine
what is opiate
only referred to naturally occurring compounds
what makes opioids so good clinically
powerful analgesics, dramatic effect on the affective part of pain (anxiety, worry)
what is a narcotic
causes sleep
is opioid narcotic
yes seep
what are natural opiates
opium from poppies contains natural opiates
what are 2 examples of natural opiates
morphine
codeine
what are semisynthetic opiates
modified versions of naturally occurring chemicals found in poppies
what are 2 examples of semisynthetic opiates
heroin
oxycodone
what are synthetic opiates
entirely artificial but bind to opioid receptors
what is 1 examples of synthetic opiates
fentanyl
how long does opioid cause analgesia
3-5 hours
what are some feelings when you take opioids IV
euphoric rush followed by sedation, drowsy, mental cloudiness
what do opioids do to pupils and how
constrict because of agonistic effects on mu and kappa receptors (in oculomotor nucleus)
which opioid drugs dont cause constriction of pupils
meperidine
demerol
what do opioids do to nausea and how
induce nausea and vomiting via chemoreceptor trigger zone in area postrema in medulla
what do opioids do to BP and how
lowers by medulla + histamine effect
what do opioids do to sweating and how
increase due to vasodilation
what do opioids do to histamine and what does this cause
increase histamine release, causing hypotension, bronchoconstriction, itching
what do opioids do to respiration and how
depress respiration via mu activation - inhibition of respiratory rhythm generator in medulla
what is respiratory depression associated with
decrease in sensitivity to arterial pH, CO2 and O2
what do opioids do to digestion and how
constipation -increased muscular tone and less motility, mu opioid receptors in GI and CNS
what do opioids do to cough and how
suppression of cough by codeine maybe, unknown how
what part of the poppy is opium
the sap
how many days of opium poppys life cycle does it make drug and when is that
10 days between petals dropping and seed pod maturing
how do the laborers extract opium
scratch seeds in evening, white sap oozes overnight, oxidizes into brown gummy substance
is there narcotic or non-narcotic alkaloids in opium
both
what are the 2 major narcotic components in opium, and how much (%)
morphine 10%
codeine 0.5%
how much is morphine more potent than opium
10 fold
how is codeine converted into morphine and where
in liver and brain by CYP2D6
what % of what race is deficient in CYP2D6
10% caucasians
what happens in the 10% caucasians that are deficient in CYP2D6
codeine produces no effect
what % of population is overactive in CYP2D6
2%
what happens in the 2% of population that are overactive in CYP2D6 who use codeine
can get morphine intoication from codeine use
what kind of opiod is heroin
semisynthetic
how is heroin diff from morphine (structure)
2 more acetal groups
why is heroin more potent than morphine
its 10X more lipid soluble than morphine so more potent
how does heroin enter the brain vs morphine (2 things)
faster and in higher concentrations
what happens once heroin enters the brain
acetyl groups metabolically removed then converted into morphine (which can then bind to receptors)
do both acetal groups from heroin get removed at the same time
no, one at a time (still quick)
what are the 2 incomplete acetylation products of heroin
6-MAM and 3-MAM
which receptors does 6-MAM bind to
mu receptors
is 6-MAM psychoactive
yes
which receptors does 3-MAM bind to
none I think (not psychoactive)
is 3-MAM psychoactive
no
which MAM product is psychoactive
6-MAM
which MAM product binds to mu receptors
6-MAM
what happens to 3 and 6 MAM
converts into morphine
what is a way to tell if someone was on heroin (legal cases)
6-MAM (only produced from heroin)
is 6-MAM or 3-MAM only produced when you take heroin
6-MAM
how does black tar heroin get its color from
heroin mixed with 3-MAM and 6-MAM formed from incomplete acetylation reaction
where does krokodil come from
Russia
what is desomorphine
krokodil
what makes krokodil/desomorphine
codeine, red phosphorus, gasoline, iodine, HCl
is krokodil/desomorphine or morphine more potent and why
krokodil/desomorphine because it is more lipophilic
how is krokodil/desomorphine administered
IV
why does krokodil/desomorphine cause so much damage
because the final product is unfiltered
what happens to the skin when you take krokodil/desomorphine
abseccess, gangrene, large-scale necrosis
what opioid class is krokodil/desomorphine
semi-synthetic
what opioid class is oxycodone
semi-synthetic
what is one of the most abused prescription analgesics
oxycodone
what is percocet
oxycodone +acetaminophen
what is percodan
oxycodone and aspirin
what is the difference with oxycodone and oxycontin
oxycontin contained much more oxycodone, time release, could be crushed
what is the difference with oxycodone and oxyneo
a new version (from oxycontin) slow release with polyethylene oxide (polymer)
which drug replaced oxycontin and why
oxyneo
people abused oxycontin, this had a polymer in it
what was added to oxyneo to make it different
polyethylene oxide
what is polyethylene oxide (1 word)
polymer
what happens when polyethylene oxide is exposed to water
turns into a gummy gel
why couldnt people abuse oxyneo as easily as oxycontin
it forms a gummy gel when exposed to fluid
what happened to demand when oxyneo went to the market (+ explanation)
demand went down, abusers switched to heroin and other opioids (fentanyl)
where does most fentanyl in canada come from
china
where do bad guys sneak fentanyl into
“oxycontin” pills, heroin, cocaine, MDMA
how does resp depression from fentanyl compare to from other opioids
much higher depression
how is fentanyl used clinically
surgical anesthetic and analgesic, but also lollipops and patches to control pain
how much more potent is fentanyl than morphine
100X
how much more potent is fentanyl than heroin
40-50X
why is fentanyl sooooo potent
very highly lipophilic
how much more potent is carfentanyl than morphine in managing pain
10000X times
how many mg of morphine is lethal
150-200mg
how many mg of heroin is lethal
12-180mg
how many mg of fentanyl is lethal
2mg
how many mg of carfentanyl is lethal
0.02
how much more potent is carfentanyl than fentanyl
100X
how much more potent is 3-methylfentanyl than fentanyl
10-15
what happens to heroin and morphine in stomach pH wise and why
they become ionized because they are weak bases
are heroin and morphine well absorbed in stomach
no
why is heroin and morphine so bad orally
not well absorbed in GI and major first pass metabolism (liver)
which opioids have been designed to be taken orally and absorbed from GI
oxyneo
methadone
what is a specific medical issue that comes with chasing the dragon
destruction of white matter in cerebellum (leukoencephalopathy)
what is leukoencephalopathy
destruction of white matter
what kind of destruction happens with chasing the dragon / leukoencephalopathy
spongiform destruction
what is spongiform destruction
sponge like appearance of brain due to loss of tissue
what causes spongiform destruction
leukoencephalopathy from chasing the dragon
what are the symptoms of leukoencephalopathy/ spongiform destruction
ataxia, apathy, akathisia, complete inability to speak or more
what is akathisia
compulsive need to more
why does chasing the dragon cause leukoencephalopathy/ spongiform destruction
maybe the tin from the tinfoil, or contaminant - unsure
how do you chase the dragon
heat on tin foil, inhale the fumes
you can also use a pipe
how do you prep heroin for injection (3)
mix with water in spoon then add something acidic to help dissolve (like lemon juice)
then heat to help dissolve and warm to body temp
what is a stupid thing heroin users do to filter out impurities bacteria and viruses
draw it up through a cotton ball
can heroin be snorted
yes
can morphine be snorted
no
why can heroin be snorted
it crosses mucosal membranes
what causes track marks
scars left by frequent injections, especially with dull reused needles
what does multiple injections do to the vein and why
collapsed vein due to scarring
why are crushed pills especially dangerous to vein health
due to the fillers in them
what happens when veins collapse to blood flow
blood is rerouted through deeper smaller veins