Opioids

Question 1

opiate

Answer 1

the “natural” opioids
heroin, morphine & codeine

Question 2

opioids

Answer 2

natural, semisynthetic & synthetic

Question 3

papaver somniferum

Answer 3

(species of poppy plant)
native to the Middle East
Now cultivated throughout Asia & Middle East

Question 4

after the poppy blooms

Answer 4

petals fall off, leaving a seed pod
extract sap from seed pod & allow sap to dry
dried sap
consumed orally or by smoking

Question 5

from opium to morphine

Answer 5

1803- F.W. Serturner
Separated the morphine from opium
morphine is 10x more potent
named morphine after Morpheus (the Greek God of dreams)
widely available in the mid 1800s

Question 6

injected via hypodermic syringe

Answer 6

was used recreationally
but also used to recover from injuries, severe wounds, surgery
often withdrawal from morphine was worse than recovery from the wounds
used widely during the Civil War
dependence called “soldier’s disease”

Question 7

heroin

Answer 7

produced as a new alteration of morphine- diacetylmorphine
unnoticed until 1898- until pharmacologist rediscovered

Question 8

heroin capabilities

Answer 8

twice as potent as morphine
reaches the brain faster
had “heroic” treatment possibilities
used as cough suppressant and pain reliever
MUCH more likely to produce dependence

Question 9

1914 Harrison Narcotics Act

Answer 9

Physicians controlled opiate. drug access
later laws placed further restrictions on who can be prescribed/how much/under what circumstances
created a market for illegal opioids
changed the demographics for addiction
before Harrison act- people of all classes could use the drug purchased at the drugstore
after- large cities (where organized crime provided the supply)
more likely to be young, poorly educated

Question 10

heroin addiction

Answer 10

highly addictive- terrible for you in the long term
followed 581 heroin addicts over 33 year period- 1/2 of participants died (50-100 times the death rate in general population)
20% still using heroin (10% refused to be tested)
14% were in prison
addicts are at a higher risk of HIV/AIDS, hepatitis, and death by overdose

Question 11

opioid epidemic

Answer 11

medical uses- treating pain after the Harrison Act- these drugs were generally only used for severe and acute pain- post surgery, trauma only used for a few days at a time
in 1970s- synthetic opiates- hydrocodone (vicodin), oxycodone (percodan)- were still used prescribed carefully

Question 12

1999-2011 opioid epidemic

Answer 12

prescriptions quadrupled
physicians began prescribing opioids for chronic pain, driven by a belief (based on a small study) suggesting that opiate drugs were non addictive
pharmaceutical industry developed more opioids to treat

Question 13

oxycontin (1996)

Answer 13

designed to treat severe & chronic pain, higher dose of oxycodone, time release form (*~12 hours)
people found that you could crush and snort- delivering a LARGE dose quickly

Question 14

opioid epidemic 2000s

Answer 14

doctors felt increasing pressure to prescribe opioid drugs
by mid-2000s death rate due to opioid overdose>automobile accidents as the leading cause of death
nearly 10% of US adolescents (aged 12-17) reported use of illicit prescription drugs
no differences between African Americans, Hispanics, Asian, & Non-hispanic white populations
often crack-down on one opioid will lead to an uptick in use of others
as prescriptions for opioids go down, heroin and fentanyl are smuggled at an alarming rate
heroin deaths are now increasing substantially

Question 15

misuse of opioids

Answer 15

more than 20% of people prescribed opioids for chronic pain- misuse the drug
8-12% of people prescribed opioids develop a use disorder
2014- more than 2 million people have substance use disorder related to prescription opioid medication
1999-2011- 280,000 people have died in US from prescription opioid overdose
2021- almost 71,000 people died from overdose involving synthetic opioids

Question 16

fentanyl

Answer 16

most powerful opiate drug ever developed
about 100 times more potent than morphine
shorter duration of action
main use was surgical anesthesi
NOT new- available in 1960s
overdose deaths started to spike when fentanyl shows up on the street- sometimes combined with heroin
fentanyl is also being combined with other illicit drugs - making it even more deadly

Question 17

pharmacokinetics of opiods

Answer 17

absorption - into the bloodstream

Question 18

absorption

Answer 18

taken orally, injected intravenously, can also be absorbed through nasal mucosa & lungs

Question 19

once in the bloodstream

Answer 19

distributed throughout the body and accumulate in kidneys, lungs, liver and muscles (as well as the brain)
some penetrate the blood brain barrier better than others
heroin is more lipid soluble and enters the brain faster than morphine
most drugs are rapidly metabolized and 90% is excreted within a day- some traces can be found 2-4 days later

Question 20

mechanisms of opiate action

Answer 20

1970s- scientists discovered endorphins- and opioid receptors
function as neurotransmitters
endorphins function as the brain’s natural painkillers
opioid drugs produce their effects by triggering activity in the endorphin system
also trigger a large release of dopamine in the nucleus accumbens

Question 21

when opioids enter the brain they bind to opioid receptors

Answer 21

mu, kappa, delta
excitation of these receptors send signals to the VTA
results in the activation of the mesocorticolimbic pathways
large release of dopamine in NA
tolerance develops (quickly)

Question 22

opioids and the brain

Answer 22

opioid receptors are distributed throughout the CNS
regions associated w/ sensorimotor functions, perception of pain, stress, learning & motivation
distribution of mu & kappa overlap

Question 23

mesocortical and mesolimbic regions

Answer 23

both receptor types are found in VTA, NA, prefrontal cortex, anterior cingulate cortex, & amygdala
likely mediates the rewarding and motivating aspects of these drugs

Question 24

mu receptors

Answer 24

the primary target of (almost) all opiod drugs
largely responsible for analgesic, sedating effects, rewarding effects, respiratory depression, stomach problems
also responsible for dependence and withdrawal

Question 25

naloxone

Answer 25

opiate antagonist- doesn’t produce any effects of the drug
has a high quality for opiate receptor site
blocks effect of opioid- if take naloxone before taking opiate- the effects are blocked
if someone has overdosed on opiate drugs- naloxone rapidly reverses the effects
now all first responders are trained to administer- many people who are likely to encounter overdoses also receive training

Question 25

medical uses

Answer 25

obvious pain relieving effects
most potent and effective pain relievers known to medicine
make surgery possible
more liberal uses of these drugs-> the epidemic but, denying people the use of these drugs also has consequences

Question 26

partial opiate agonists

Answer 26

partial opiate agonists
bind to the same receptors but produce lower levels of activity
less effective as well- produce analgesia- but have much lower potential for abuse
3 are on the market- approved for moderate to severe pain, thought to be safer- but can still produce dependence

Question 27

what is a pipe dream?

Answer 27

fair game for exam
- referring to vivid experiences you have on opioids

Question 28

psychological and physiological effects

Answer 28

in addition to analgesia- euphoria, drowsiness, heavy feeling in the limbs, relaxation “like lying in warm salt water”
interference with other interests- reduced sex drive, impair social interactions, vivid dream-like experiences (pipe dreams)
respiratory depression, constriction of the pupils

Question 29

withdrawal from opioids

Answer 29

withdrawal symptoms can appear after only 1-2 weeks of use
begin 8-12 hours after last use
flu-like symptoms- snotty nose, chills, tearing, sweating
over time-more severe symptoms- anorexia, goosebumps
48-72 hours after last dose- severe flu-like symptoms- nausea, diarrhea, sneezing, pain in the bones, joints
depression and anxiety

Question 30

quitting opioids

Answer 30

total abstinence- not particularly humane or effective
use of an opioid antagonist- shorten duration of withdrawal-but intensify the symptoms
maintenance therapy drug- methadone or buprenorphine- slowly taper off the drug

Question 31

methadone

Answer 31

available as early as 1947
recognized for its ability to alleviate withdrawal
prevents withdrawal for 24 hours (*or more)
selective agent that binds to mu
blocks the action of heroin- fewer cravings, no euphoria if relapse occurs
must be distributed in a clinic

Question 32

buprenorphine

Answer 32

first line treatment for opioid addiction
sublingual tablet or transdermally through a patch
dos NOT have to be administered at a clinic
longer half life than methadone
less sedation than methadone
partial agonist at mu receptors
fully antagonizes kappa and delta receptors**
more withdrawal than methadone
suppresses stress-related responses

Question 33

recovery

Answer 33

after detoxification procedures- 80-90% relapse within 2 years most occur within 6 months- thought to be due to returning to environment of use- CS-> craving
soldiers returning from Vietnam- approx. 21% of soldiers returning were addicted to heroin- after returning home-detox-> relapse rate was less than 15%
change to environment is critical to success