Opioids - Opioids Flashcards
Where does opium come from?
it is sap derived from the poppy
What is the difference between an analgesic vs narcotic opium drug?
analgesic = pain relief narcotic = opium-based
What drug types fall under the following categories? Endogenous - Alkaloids - Semisynthetic - Synthetic -
Endogenous - endorphins
Alkaloids - morphine, codeine
Semisynthetic - oxycodone, heroin
Synthetic - methadone, fentanyl
_____: occurring within
_____: directly extracted
______: derivative compounds
_____: structurally different
Endogenous
Alkaloids
Semisynthetic
Synthetic
Opium exhibits ____ (stimulant) and _____ (depressant) effects, it is also used as a ______ (anti-psychotic)
euphoric
anxiolytic
medicine
What are the three intake methods for heroin and morphine?
oral, inhalation and intravenous
Taking heroin and morphine orally, by ingestion, and intravenously all have different effects. What are they?
Oral: mood alleviation, cough suppression
Inhalation: euphoria
Intravenously: euphoria, pain relief
Seeing decreased body temperature and pupil constriction is characteristic of taking heroin and morphine by which method of intake?
intravenously
During injection of heroin and morphine, what are the three stages and how long does each last?
Stage 1:
- 0-2 minutes
- “rush”, “flash”: intense euphoria
- tingling and warmth in “lower abdomen” resembling sexual orgasm
Stage 2:
- 2-3 hours
- “on the nod” : tranquil drowsiness
Stage 3:
- 4+ hours
- WITHDRAWAL
In what stage of heroin or morphine injection is there a reduction in sexual interest? What is it a result of?
stage 2: lowering testosterone levels
What is the withdrawal like from heroin and morphine?
occurs in stage 3, is very rapid - allostatic mechanisms involved don’t seem to be following through
What drug has the following street names: china white, china girl, TNT, apache, percopop
fentanyl - a lot of these names are based on where they are coming from (China, Mexico)
What Schedule are the following drugs: heroin, morphine, methadone, fentanyl, codeine, oxycodone
Schedule I: heroin
Schedule II: morphine methadone, fentanyl
Schedule III: codeine, oxycodone
Fentanyl design:
- Demerol = used as an _______
- “lollipop” = used in _____ care
- Duragesic = used for _____ pain
anesthetic
palliative care
chronic pain (analgesia)
Fentanyl is __x more potent than morphine
100
What are the three methods of intake for fentanyl?
oral
transdermal
insufflation
What is the problem with intake of fentanyl?
respiratory depression increases with faster absorption
Opium has an agonistic effect on _____ _____
endogenous neuropeptides
“separating the molecules into separate chains”
cleavage
Cleavage is an internal ______ action
internal
Enzyme CYP2D6 converts codeine to ____
morphine
Cleavage:
-active metabolite ______
morphine-6-glucuronide
What do G-protein metabotropic receptors allow for?
return neurons to resting potential sooner by allowing K+ to influx inwards
Pure Agonist: ____ relief (what drugs?)
pain relief - fentanyl and morphine
Partial Agonist: ____ relief but no ____ effect
pain
respiratory
Mixed Agonist-Antagonist: treating ___ ____
opioid addiction (naloxone, methadone, buprenorphine)
Mixed Agonist-Antagonist:
- _____ receptor, ______ drug
- ___ one receptor, _____ another
agonising; antagonizing
agonize; antagonize
How does opium have agonistic effects with regard to GABA?
it inhibits the GABA neurons so that there is an increase in dopamine levels and an increase in reinforcing effects
How is opium agonistic in the ventral tegmental area?
suppression of the inhibitory response of GABA on dopamine receptors
How is opium agonistic in the nucleus accumbens?
activation of m opioid receptors that inhibit the GABA neurons - this allows dopamine to be released in VTA and “enhancement” of the dopaminergic response
With opium, there is agonism of the ___ ___ receptor
glutamate NMDA
How does inhibition of opium effect nociception?
- A and C fibers
- Glutamate and substance P
How do A and C fibers decrease pain?
sensory pain signal from receptor to spinal cord -
these fibers are inhibited, stopping neurotransmission of the pain
How do glutamate and substance P stop pain?
it is the sensory pain signal from the spinal cord to the thalamus that is inhibited by activation of the medulla - this dulls/blunts the pain
Is there a tolerance seen with opium?
it is dose dependant
Tolerance with opium is ___ and ____ (allostatic principles) and is selective to ___, ____, and ____ ____ (conditioning effects)
accrued and relational
analgesia, euphoria, and respiratory depression
Withdrawal lasts __-__ days
5-10
When does craving intensify?
at 36-72 hours
Withdrawal: at 8-12 hours you start to get what symptoms?
flu-like
Withdrawal: at 48-72 hours you start to get what symptoms?
pupil dilation, anorexia, piloerection, spastic arm/leg movements
90% relapse after withdrawal associated with ____
environment - this is evidence for conditioning
Detoxification:
Long term is ___ days and short term is ___ days
180; 30
You can use ___ or ____ for long term/short term detoxification
methadone or buprenophrine
Using methadone or buprenorphine will prevent ___, has ____ effects, and weak/no _____
withdrawal
long-lasting
euphoria
What is the debate for using methadone or buprenorphine?
institutional control of addicts - you can get addicted to methadone so it just gets addicts addicted to the institution
Naloxone is an ___ ____ - it binds as an agonist and induces what?
inverse agonist - induces opposite pharmacological response (ie. lowers the response)
Naloxone ____ withdrawal symptoms and ____ duration
increases, decreases
Ultra-rapid detoxification (2 days) is in conjunction with _____ for the first few hours
sedation/amesthetized
