opiods Flashcards

1
Q

Full opioid agonists

A

morphine
fentanyl
heroin
methadone

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2
Q

partial opioid agonists

A

codeine
hydrocodone
oxycodone

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3
Q

mixed agonists/antagonists

A

buprenorphine

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4
Q

antagonisits

A

naloxone

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5
Q

weak opioid agonists/reuptake inhibitors

A

tramadol

tapentadol

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6
Q

tramadol

A

serotonin uptake blocker
NE uptake blockers
weak mu-R agonist

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7
Q

tapentadol

A

weak muR agonist and NE reuptake blocker

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8
Q

narcotic

A

archaic term

more legal then medical referring to any substance that produces stupor associated with analgesia

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9
Q

opiates

A

natural products and derivatives obtained from opium poppy

  • opium
  • morphine
  • heroine
  • codeine
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10
Q

opiods

A
class of compounds that bind to opioid R 
includes agonists, antagonists, partial agonists, and mixed agonists/antagonists
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11
Q

endogenous opioid agonists

A

endorphin
enkephalines
dynorphins

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12
Q

muRs

A
endorpins>enkepalins>dynorphins
supraspinal and spinal analgesia
sedation
inhibition of respiration 
slowed GI transit
modulation of hormone and neurotransmitter release
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13
Q

kappa Rs

A

enkephalins>endorphins=dynorphins
supraspinal and spinal analgesia
modulation of hormone and neurotransmitter release

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14
Q

deltaRs

A

dynorphins>endorphins>enkephalins

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15
Q

other Rs

A

sigma
TLR-4
ORL-1

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16
Q

ORL-1

A

orphan opioid R like
cloned ‘orphan R’
similar structure to opioid R
different fnx (no effec on pain, hyperalgesia, or inflammation)
different ligands - nocipetin = orphanin FQ

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17
Q

opioid Rs

A

all GPCRs
inbitis cyclic AMP
open G-protien modulated KChS -> hyperpolarization
reduce presynaptic Ca influx inhibiting NT release

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18
Q

brain stem

A

opioid R influence respiration, cough, nausea, vomiting, BP, pupillary diameter, stomach secretion

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19
Q

medial thalamus

A

mediates deep pain that is poorly localized

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20
Q

spinal cord

A

receipt and integration of incoming sensory information, activation of these R attenuates painful afferent stimuli

21
Q

hypothalamus

A

affect neuroendocrine secretion

22
Q

limbic system

A

high density of opioid Rs in amygdala

23
Q

periphery

A

peripheral sensory nn fibers and nn terminals inhibit Ca influx and release of excitatory and pro-inflammatory substances

24
Q

immune cells

A

have opioid Rs, but fnx is unknown

25
Q

major efects of activating mu

A
analgesia
euphoria
miosis
respiratory depression
physiological dependence
reduced GI motility
26
Q

major efects of activating kappa R

A
less abuse potential and physical dependence
dysphoria
psychotomimetic 
less miosis and respiratory depression then mu
analgesia
sedation
vasodilation
increased urinary output
27
Q

miosis

A

d/t indirect parasympathetic actions
little or no tolerance develops against this
almost all other causes of coma cause mydriasis

28
Q

opioids and CV system

A

no major effects on BP or heart rate
b/d of respiratory depression and CO2 retention cerebral vessels dilate -> increased ICP therefore use is CI in severe brain injury

29
Q

opioids and Histamine

A

opioids release H2 from mast cells

CI in asthmatics

30
Q

opioids and first pass

A

variable
morphine- very high
codeine and oxycodone less

31
Q

opioids and pregnancy

A

do cross placental barrier therefore CI

32
Q

fentayl PK

A
highly lipophilic
slowly metabolized
but short acting b/c distributes to fatty tissues 
100x more potent then morphine
IV, epidural, intrathecal
33
Q

morphine

A
binds all opioid Rs
highest affinity for mu
low oral availability
high efficacy for analgesia 
high abuse potential
34
Q

uses of morphine

A

analgesic- best with severe, constant pain
acute pulmonary edema
acute MI

35
Q

morphine and acute pulmonary edema

A

reduced perception of SOB
anxiolytic effects
reduction in cardiac preload and afterload

36
Q

opioids and cough suppression

A

low doses
maybe d/t activation of sigma R
dextromethorphan
codeine

37
Q

opioids and diarrhea

A

low doses
loperamide (cannot X BBB)
diephnoxylate (+atropine)
difenoxin (+atropine)

38
Q

uses of fentanyl

A

epidural for labor

oral transumucosal and patch for CA pts

39
Q

methadone

A

synthetic, PO effectice opioid
equally potent as morphine, but induces <euphoria with longer duration of action
analgesic
control withdrawl of heroin and morphine

40
Q

meperidine

A

syntheitic opioid used for acute pain
binds both mu and kappa
respiratory depression
DILATES pupils
not useful for diarrhea or cough
less effects on smooth mm (can be used in obstetrics)
toxic metabolite causes seizures so cannot be used >48hrs

41
Q

heroin

A

schedule I
3x more potent then morphine
greater lipid solubility so more CNS effects
more exaggerated euphoria

42
Q

codeine

A

mu effects w/low doses

kappa effects w/high doses

43
Q

hydrocodone

A

relatively pure mu actiavtion

44
Q

oxycodone

A

relatively pure mu
derivative of codeine
high PO effects
sustained release product (oxycotin)

45
Q

bupreoprhine

A

mixed opioid agonist/antagonists
depends on R subtype
partial agonist at mu
major use is for opioid detox

46
Q

mixed opioid agonist/antagonists

A

can precipitate withdrawl symptoms

47
Q

naloxone

A
opioid antagonist
short acting
used to Tx opioid overdose
precipitates withdrawal syndrome
can be used to Tx drug-fee addicts
48
Q

primary symptoms of opioid overdose

A

triad:
lethargy/coma
depressed respiration
pinpoint pupils

49
Q

secondary symptoms of opioid overdose

A
hypotension
hypothermia w/cold or clammy skin
pulmonary edema
convulsions
hypoxia w/dilated pupils