Opioids Flashcards

1
Q

what are the four steps in feeling pain?

A

transduction
transmission
modulation
perception

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2
Q

what two places in four steps of feeling pain do opioids work?

A

modulation and transmission

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3
Q

where doe descending and ascneding pain sensations summate in the SC?

A

dorsal horn…good spot for opioid action

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4
Q

where else are mu opioid receptors found in body other than brain and SC?

A

peripheral nociceptor neurons and GI

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5
Q

name the full agonists opioids

A
codeine
morphine
hydrocodone
oxycodone
heroin
methadone
meperidine
fentanyl 
remifentanil 
carfentanil
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6
Q

what is most potent full agonist?

A

carfentanil

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7
Q

what opioid is used to compare potency?

A

morphine set as 1

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8
Q

what are oral opiods subject to?

A

first pass effect

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9
Q

where are opioids mainly cleared

A

kidneys

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10
Q

what are opiods broken down into before clearance?

A

polar metabolites

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11
Q

what three drugs are broken down into more potent drugs?

A

codeine
hydrocodone
oxycodone

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12
Q

what is secondary effect of increased morphine metabolites in system?

A

seizures

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13
Q

what is codeine broken down into?

A

morphine

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14
Q

what is hydrocodone broken down into?

A

hydromorphone

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15
Q

what is oxycodone broken down into?

A

oxymorphone

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16
Q

what is secondary effect of increased hydromorhpone metabolites in system?

A

neurotoxicity

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17
Q

name the foursafe opioids to give with renal failure

A

fentanyl
hydromorhpone
methadone
buprenorphine

18
Q

what do opioids do to pre synaptic neuron in ascending path?

A

inhibit voltage gates Ca2+ entry

19
Q

what do opioids do to post synaptic neuron in ascending path?

A

increase K+ efflux…hyperpolarize cell

20
Q

what is opioids MoA in descending path?

A

inhibits GABA so GABA cannot inhibit the pathway anymore

21
Q

how do opioids inhibit GABA in descending path?

A

inhib Ca2+ influx in presynaptic terminal to release GABA…so decreases GABA release

22
Q

what are three adverse affects with acut opioid use?

A

respiratory depression
constipation
sedation

23
Q

what are three adverse opioid effects with chronic use?

A

hyperalgesia
tolerance
withdrawal

24
Q

where are there mu opioid receptors that contribute to respiratory depression?

A

respiratory center of the pons

25
Q

how do opioids cause constipation?

A

target mu opioid receptors in GI and lead to less contraction of SM there

26
Q

what opiods is used to treat diarrhea?

A

fentanyl and eluxadoline

27
Q

what drug class treats opioid induced constipation?

A

PAMORAs

28
Q

what are PAMORAS

A

peripherally acting mu opiod receptor antagonsits

29
Q

what is the PAMORA to know?

A

methylnaltrexone

30
Q

if patient builds up tolerance to opioid what can you do? but what can be issue with this?

A

can switch to other opioid…but often has cross tolerance

31
Q

how do opioids lead to euphoria/addiction?

A

stimulate the mesolimbic dopaminergic pathway by inhibiting GABA release so dopamine is uninhibited

32
Q

when is peak opioid withdrawal?

A

72 hours after last dose

33
Q

what are symptoms of opioid withdrawal?

A

chills, fever, body ache, msucle pain, nausea, dilated pupils

34
Q

what type of opioid is methadone?

A

full agonist

35
Q

what is unique about methadone in treating opioid addiction?

A

has very long halflife and can satisfy cravings…and does not lead to withdrawal symptoms

36
Q

what class of opioids is buprenorphine?

A

partial agonist

37
Q

how does buprenorphine treat addiction?

A

partially substitutes full agonist opiods…so reduces withdrawal symptoms and eases detox

38
Q

what two meds are used in acute overdose? why?

A

naloxone and naltrexone …because they are antagonist and inverse agonist

39
Q

what does it mean for naloxone/naltrexone to be inverse agonist?

A

take away the basal level of firing of the mu opioid receptor

40
Q

what does it mean for naloxone/naltrexone to be antagonist?

A

inhibit binding of other opioids to mu receptor

41
Q

what is suboxone?

A

combo of buprenorphine and naloxone