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
Q

spinal cord opioid R mediate

A

reciept and integration of incoming sensory

change painful afferent stimuli

26
Q

hypothalamic opioid R

A

effect neuroendocrine secretion

27
Q

limbic system opioid R

A

high density of opioid R in amygdala

28
Q

periphery opioid R

A

inhibit Ca influx and release of excitatory glutamate and pro inflammatory substanc eP

29
Q

immune cell opioid R

A

function unknown

30
Q

which opioid R is responsible for majoirty classical effects of opiods

A

mu R

analgesia, euphoria, miosis, resp depression, physio dependence, reduced GI motility (constipation)

31
Q

main action of stimulation kappa R

A

dysphoria
analgesia
psychotomimetic responses

32
Q

what occurs with respiratory depression from opioids

A

decreased response to CO2

33
Q

what drugs are used to suppress cough

A

dextromethophan and codeine

34
Q

why do opiates cause miosis

A

indirect parasympathetic actions

no tolerance develops in abusers

35
Q

when does opiate overdose cause mydriasis

A

when asphyxia develops

36
Q

opioids CI in what patients

A

with severe brain injury since increase the CSF from respiratory depression and CO2 retention

37
Q

GI complication opioid therapy

A

constipation

38
Q

why should asthmatics not be on opioids

A

can cause histamine induced bronchoconstriction

causes urticaria, sweating and vasodilation

39
Q

what do you consider when giving morphine orally

A

high first pass metabolism so oral higher dose than IV

usually 4X higher dose

40
Q

teratogenicity of opioids

A

do not use during labor

41
Q

PK fentanyl

A

highly lipophilic cross BBB quick but redistributes to fat super fast

42
Q

affinity of morphin

A

mu > delta or kappa

43
Q

warning of morphine

A

high addiction potential

44
Q

clinical uses morphine

A
analgesia
acute pulmonary edema
AcuteMI
cough suppression
diarrhea
45
Q

type of pain to attempt analgesia with morphine

A

severe

constant

46
Q

morphine and acute pulmonary edema

A

relief from dyspnea with L ventricular failure
reduced perception SOB
dec anxiety
reduce cardiac preload and afterload

47
Q

what opioids are used for diarrhea

A

loperamide (imodium OTC)
diphenoxylate + atropine (lomotil)
difenoxin and atropine (motofen)

48
Q

administration fentanyl

A

IV
epidural
intrathecal

49
Q

fentanyl is used for what

A

analgesia labor

oral transucosal for cancer patients

50
Q

which opioid has longer duration action than morphine but less euphoria

A

methadone

51
Q

methadone used for

A

controlled withdrawal of dependent heroin and morphine abusers

52
Q

what is the synthetic opioid used for acute pain

A

meperidine

“demerol”

53
Q

reaction of pupils from meperidine

A

mydriasis

dilates

54
Q

which opioid can be used in obstetrics

A

meperidine

55
Q

meperidine time use limit

A

<48 hours since toxic metabolite accumulates and can cause seizures