Pharm Pain, Martin I Flashcards

1
Q

What are the full agonists for opioid R

A

morphine
fentanyl
heroin
methadone

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2
Q

what are the partial agonists for opioid R

A

codeine, hydrocondone, oxycodone

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3
Q

what are the mixed agonists/antagonists

A

buprenorphine

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4
Q

opioid antagonists

A

naloxone

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5
Q

what are the weak opioid antonists or reuptake inhibitors

A

tramadol

tapentadol

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6
Q

what are the non opioid analgesics

A

acetaminphen, aspirin, other NSAIDs and selective COX2 inhibitors

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7
Q

what is analgesia

A

attenuation of pain perception without loss of consciousness

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8
Q

how is analgeisa accomplised

A

raising pain threshold at level of spinal cord and altering brains perception of pain

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9
Q

sensory component of pain

A

perceived as result of direct stimulatino of pain R

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10
Q

reactive component of pain

A

intensity of pain dramatically altered by lvel of anxiety and stress response related to original insult

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11
Q

narcotic

A

substance producing stupor associated with analgesia

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12
Q

opiates

A

natural products and dervatives obtained from opium poppy

opium, morphine, heroin, codeine

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13
Q

opioids

A

bind to opioid R

includes agonists, antagonists, partial agonists and mixed agonists/antagonists

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14
Q

endogenous opioid agonists

A

endorphin enkephalin, dynorphin and others

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15
Q

where are endogenous opioid peptides made

A

in nucleus and transported down

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16
Q

endogenous opioid peptide precursoe

A

pro-opiomelanocortin POMC

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17
Q

opioid effect in peraqueductal gray

A

inhibit GABA release which increase inhibitory nerve activity regulating projections to medulla that alter dorsal horn excitability

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18
Q

how do opiates work on spinal cord

A

presynaptically to block Ca influx and NT release
or
postsynaptically to open K Ch causing hyeprpolarization

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19
Q

mu opiod R

A
endorphins>enkephalins>dynorphins
supraspinal and spinal analgesia
sedation
inhibition respiration
slowed GI
modulation hormone and NT release
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20
Q

kappa opioid R

A

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

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21
Q

delta opioid R

A

dynorphins>endorphins>enkephalins
supraspinal and spinal analgesia
psychomimetic effects and slowed GI transit

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22
Q

principle signal mech of opioid R

A

GPCR

  • inhbiit cAMP
  • open K Channels allowing efflux and hyperpolarization
  • reduce presynaptic Ca influx inhibiting NT release
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23
Q

brainstem opiod R influence

A

respiration, cough, nausea, vomiting, BP, pupillary diameter, stomach secretions

24
Q

medial thalamus opioid R mediate

A

deep pain that is poorly localized

25
spinal cord opioid R mediate
reciept and integration of incoming sensory | change painful afferent stimuli
26
hypothalamic opioid R
effect neuroendocrine secretion
27
limbic system opioid R
high density of opioid R in amygdala
28
periphery opioid R
inhibit Ca influx and release of excitatory glutamate and pro inflammatory substanc eP
29
immune cell opioid R
function unknown
30
which opioid R is responsible for majoirty classical effects of opiods
mu R | analgesia, euphoria, miosis, resp depression, physio dependence, reduced GI motility (constipation)
31
main action of stimulation kappa R
dysphoria analgesia psychotomimetic responses
32
what occurs with respiratory depression from opioids
decreased response to CO2
33
what drugs are used to suppress cough
dextromethophan and codeine
34
why do opiates cause miosis
indirect parasympathetic actions | no tolerance develops in abusers
35
when does opiate overdose cause mydriasis
when asphyxia develops
36
opioids CI in what patients
with severe brain injury since increase the CSF from respiratory depression and CO2 retention
37
GI complication opioid therapy
constipation
38
why should asthmatics not be on opioids
can cause histamine induced bronchoconstriction | causes urticaria, sweating and vasodilation
39
what do you consider when giving morphine orally
high first pass metabolism so oral higher dose than IV | usually 4X higher dose
40
teratogenicity of opioids
do not use during labor
41
PK fentanyl
highly lipophilic cross BBB quick but redistributes to fat super fast
42
affinity of morphin
mu > delta or kappa
43
warning of morphine
high addiction potential
44
clinical uses morphine
``` analgesia acute pulmonary edema AcuteMI cough suppression diarrhea ```
45
type of pain to attempt analgesia with morphine
severe | constant
46
morphine and acute pulmonary edema
relief from dyspnea with L ventricular failure reduced perception SOB dec anxiety reduce cardiac preload and afterload
47
what opioids are used for diarrhea
loperamide (imodium OTC) diphenoxylate + atropine (lomotil) difenoxin and atropine (motofen)
48
administration fentanyl
IV epidural intrathecal
49
fentanyl is used for what
analgesia labor | oral transucosal for cancer patients
50
which opioid has longer duration action than morphine but less euphoria
methadone
51
methadone used for
controlled withdrawal of dependent heroin and morphine abusers
52
what is the synthetic opioid used for acute pain
meperidine | "demerol"
53
reaction of pupils from meperidine
mydriasis | dilates
54
which opioid can be used in obstetrics
meperidine
55
meperidine time use limit
<48 hours since toxic metabolite accumulates and can cause seizures