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Therapeutics III > Exam 5 (final) - Barker's lectures > Flashcards

Exam 5 (final) - Barker's lectures Flashcards

(69 cards)

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1
Q

describe opioid induced hyperalgesia

A

worsened pain due to chronic opioid use

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2
Q

pain is an ________ and impacts mood because of this

A

emotion

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3
Q

pain begins with stimulus in _______ and signals to the _____

A

periphery, brain/CNS

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4
Q

temperature sensitive receptors and channels involved in pain

A

TRP (transient receptor potential cation channel)
TRPV (vanniloid) = heat (and spice like capsaicin)
TRPM (melastatin) = cold (like menthol)

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5
Q

glutamates’ role in pain

A

glutamate in the major excitatory neuron in brain
-plays a role in conduction in spinal cord

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6
Q

A beta fibers

A

non-noxious (non-pain producing)
faster (35-75m/s)

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7
Q

A gamma fibers

A

pain, cold receptors
fast (2-35m/s)
respond to “first pain” such as sharp object

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8
Q

C-fibers

A

respond to pain, temp, touch, pressure, itch
-“second pain” (dull, aching)
slow (0.5-2m/s)

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9
Q

what is substance P

A

neuropeptide released when there is an injury causing a chain of events

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10
Q

substance P chain of events (4 steps)

A
  1. vasodilation
  2. degranulation of mast cells
  3. release of histamine
  4. inflammation and prostaglandins
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11
Q

neuropathic pain sensitization description (spinal)

A

neuropeptides (CGRP and substance P) –> PLC –> PKC –> more excitable AMPA and NMDA receptors, and more expression and sensitivity
-possibly leads to ectopic action potentials

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12
Q

where does NSAID inhibition occur along signaling pathway

A

on afferent neuron just after injury signal is starting to be sent down afferent neuron

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13
Q

mu opioid receptor expression in the brain leads to what effects of opioids

A

altered mood
sedation
reduction in emotional reaction

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14
Q

morphine, codeine and thebaine are part of what structural class

A

phenanthrenes

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15
Q

3 position substitutions lead to _____

A

decreased potency - codeine

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16
Q

6 position substitutions lead to ______

A

increased activity - hydromorphone or hydrocodone (from codeine)

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17
Q

14 position OH leads to _______

A

increased potency - oxycodone

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18
Q

N-allyl substitutions leads to _____

A

antagonist activity - nalaxone or naltrexone

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19
Q

buprenorphine has substitution on which spot of the opioid structure to allow for partial agonism

A

N-allyl

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20
Q

what 3 opioid receptors are responsible for analgesia effects and side effects of opioids

A

mu
kappa
delta

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21
Q

presynaptically, mu agonists (opioid agonists) bind to ______ receptors causing an inhibition of _____ channels and a ______ in neurotransmitter release

A

mu opioid, calcium, decrease

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22
Q

postsynaptically, mu agonists (opioid agonists) bind to ______ receptors causing activation of ______ so that _____ can leave the neuron, preventing conduction to CNS

A

mu opioid, GIRK channel, potassium

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23
Q

efflux of K+ by GIRK is called ________

A

hyperpolarization

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24
Q

opioid induced side effects are mostly ____ effects (on-target or off-target)

A

on target

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25
opioid induced side effects include (6)
-respiratory depression -constipation -pruritis (itch - note this is not allergic rxn but can be -bad enough to where pts must switch opioids) -addiciton -urinary retention -NV
26
would you use opioids as an anti-diarrheal?
yes, you can, and some have been designed to stay out of the CNS so no analgesic effects occur (act only in GI tract to slow motility)
27
role of kappa opioid receptor
-reduce DA release, meaning reduction in abuse potential -counterbalance mu opioid receptor effects
28
role of delta opioid receptor
reduce anxiety and depression treat alcoholism side effects: seizures no FDA approved drugs for this yet
29
depressants (just like stimulants) can cause DA release. How?
1. opioid drug binds presynaptic mu receptor 2. less GABA to activate GABA-A 3. shuts off inhibition of DA neuron activity 4. increased DA release and therefore activation of DA receptors
30
in general, IV dosing looks like what on a conc./half life graph?
quick initial peak in about 6 minutes, then drops off quick
31
in general, IM/SQ dosing looks like what on a conc./half life graph?
high initial peak (not as high as IV) in about 30 minutes, then drops off (slower than IV)
32
in general, PO/PR dosing looks like what on a conc./half life graph?
lower initial peak in about 60 minutes, drops off slower than other forms
33
morphine bioavailability is ____%
25
34
morphine is metabolized by CYP _____ and _____
2D6 and 3A4
35
what three opioids are prodrugs
heroin codeine tramadol
36
codeine is metabolized to _________
hydrocodone morphine
37
heroin is metabolized to _________
morphine
38
CYP3A4 makes opioids starting with ______
nor -norhydrocodone -noroxycodone -noroxymorphone
39
when UM of codeine is given normal dose, they will have _______ serum concentrations of morphine
increased (by ~50%) (most common in north africa)
40
when PM of codeine is given normal dose, they will have _______ serum concentrations of morphine
decreased (most common in caucasian) -no effect
41
tramadol may have properties similar to what other drug class?
SNRIs
42
meperidine has a toxic metabolite that leads to neurotoxicity (nervousness, tremors, twitching, seizures). which metabolite is it and what is it metabolized by?
normeperidine, 3A4
43
blocking of NMDA does what? what drug is this effect seen in?
blocks conduction of pain signals methadone
44
3 drugs used to prevent constipation with opioids
Senna -colonic contraction/increased fluid secretion PEG (MiraLAX) -stool softener docusate -stool softener
45
difference between opioid tolerance and opioid induced hyperalgesia
tolerance = needs increased dose to have effect on pain induced hyperalgesia = due to prolonged opioid use, increased dose with have no effect on pain
46
methadone is a _____ _______
full agonist
47
methadone is a ______ antagonist
NMDA
48
methadone action is _____ and _____
slow and long
49
buprenorphine is a ______ ______
partial agonist
50
naltrexone is a ________
antagonist
51
effects on baby if mother was on opioids during pregnancy
baby has withdrawal up to 4-6 months after birth -seizures seen in methadone users -opioids present in breast milk
52
treatment of neonatal abstinence syndrome
non-pharm: -more calories -observe temp, weight (gain or loss), sleep -rehydrate pharm: -morphine 0.4mg/mL -SL buprenorphine -methadone 0.05-0.1mg/kg/dose q6h
53
NSAIDs are COX inhibitors by what pathway
arachadonic acid pathway
54
COX-1 or COX-2 selective NSAIDs show fewer GI side effects
COX-2 -reduce ulcers -reduce GI bleed
55
aspirin MOA
irreversibly inhibits COX-1/2 by acetylation
56
other NSAIDs MOA
competitive (reversible) inhibition of COX-1/2
57
which has longer half life ibuprofen or naproxen?
naproxen (14hr) ibuprofen (2hr)
58
NSAID CI
CKD PUD Hx of GI bleed increase CV risk -also known to cause asthma exacerbations
59
opioids receptors
mu, kappa, delta
60
LSD, mushrooms receptors
5HT2a, 5HT2c
61
marijuana, K2, spice receptors
CB1
62
GHB receptors
GABA-B
63
caffeine receptors
adenosine
64
cocaine, amphetamine receptors
DAT -NE, 5HT secondary
65
MDMA, ecstasy receptors
monoamine transporters
66
alcohol receptors
dirty (lots of them) -GABA -5HT
67
nicotine receptors (ion channels)
Ach R -agonist
68
PCP, ketamine receptors (ion channels)
NMDA R -antagonist
69
benzos, barbiturates receptors (ion channels)
GABA-A -positive allosteric modulators

Therapeutics III (22 decks)

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