L? Pharm of opiates - Barker Flashcards

(61 cards)

1
Q

two types of alkaloids that opium contains

A

phenanthrenes
benzylisoquinolines

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2
Q

what are the 3 non-phenanthrene opioids ***

A

tramadol
meperidine
fentanyl
(all others are phenanthrenes im pretty sure)

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3
Q

T or F: sigma receptors are opioid receptors

A

false

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4
Q

Opioid receptor signal transduction:
Presynaptic: inhibit _____ channel (Gi), decrease in ________ releas

A

calcium
neurotransmitter

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5
Q

Opioid receptor signal transduction:
Postsynaptic: Activate ______ channel (GBy) -> Efflux of ___ leading to hyperpolarization

A

GIRK
K+

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6
Q

T or F: Opioid induced side effects are mostly on-target effects **

A

True

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7
Q

T or F: Pruritus is an allergic response due to opioids, not a side effect

A

false, other way around

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8
Q

7 side effects induced by opioids

A

resp depression
constipation
Pruritus
Addiction
urinary retention
N/V
Miosis

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9
Q

T or F: Kappa opioid receptor has potential use for treatment of addiction due to its increase in dopamine release

A

false, reduction

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10
Q

3 therapeutic uses of mu opioid receptor *

A

analgesia (not as effective for chronic pain)
sedation
antitussive (cool)

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11
Q

Endogenous opioid for mu opioid receptor ***

A

endorphin
M-morphine

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12
Q

Which opioid receptor some verb counterbalance mu opioid receptor effects

A

kappa

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13
Q

which opioid receptor?
Dynorphins natural ligand
- preprodynorphin

A

kappa

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14
Q

natural ligand for delta opioid receptor

A

Enkephalins
- preprronekphalin

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15
Q

T or F: Delta opioid receptors are extracellular

A

false, intracellular

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16
Q

Which opioid receptor has a role in hypoxia/ischemia/stroke ?

A

delta

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17
Q

Which opioid receptor reduces anxiety and depression?

A

delta

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18
Q

which of the opioid receptors can treat alcoholism?

A

delta.

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19
Q

one listed side effect on delta opioid receptor slide

A

seizures

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20
Q

T or F: There are no FDA approved Kappa opioids

A

False, its no delta

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21
Q

Opioid site of action:
_______ -> _________

A

ventral tegmental area -> nucleus accumbens

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22
Q

make sure you actually look at the MOA on slide 16

A

okay please do it cole i beg you

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23
Q

which opioid has first pass metabolism with a bioavailability of 25%?

A

morphine

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24
Q

Morphine CYP(s)

A

2d6 and 3a4

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25
Morphine: MOA (kinda): Phen or nonphen: Receptor: NMDA activity? Kappa activity?
full agonist phen mu no nmda no kappy
26
Nociceptin receptor endogenous opioid
nociceptin duh
27
which 3 opioids are prodrugs with an active metabolite? *
heroin codeine tramadol
28
T or F: Fentanyl and methadone produce active metabolites
False
29
High lipophilicity A. Morphine B. Fentanyl
b
30
CYP3A4 makes opioids starting with?
NOR oxycodone -> noroxycodone oxymorphone -> noroxymorphone
31
PM (poor metabolizer) (of CYP2D6) phenotype is more common in what group?
white people somehow
32
__ phenotype is of high relevance worldwide. A. PM (poor) B. IM (intermediate) C. EM (extensive) D. UM (ultra-rapid)
D
33
fentanyl is how much more potent than: morphine heroin
100 x 50 x
34
which opioid is typically used in palliative care
fentanyl
35
which 3 opioids are broken down by plasma esterases due to ester linkage?
3 synthetic ones: sufentanil, remifentanil, alfentanil
36
which opioid has snri properties?
tramadol
37
which opioid has the toxic active metabolite normeperidine?
meperidine (demerol) lol
38
Methadone: ** - Primarily used for ______ ________ - ________ __ (unwanted effect) - ______ antagonist *
opioid dependence prolonged QTc NMDA
39
2 opioids that can be used for cough
codeine and dextromethorphan
40
2 opioid agonists used as anti-diarrheal
Diphenoxylate w/ atropine (lomotil) and loperamide (imodium)
41
Pentazocine and Butorphanol MOA
Kappa agonist, partial agonist/antagonism at mu
42
3 side effects for pentazocine and butorphanol
less dysphoria hallucinations increase in BP/HR
43
Nalbuphine (nubain) MOA
Full agonist at kappa antagonist at mu antagonism produces withdrawal
44
buprenorphine MOA and primary use
Partial mu agonist, weak kappa agonist and delta antagonist (damn) primary use in opioid replacement therapy
45
3 meds used for preventative and acute mgmt of ileus and constipatino
senna -> colonic contraction** (so pick this one if it comes up) miralax docusate
46
Methadone MOA
FULL mu agonist
47
T or F: Methadone is frequently used in medication assisted treatment for opioid dependence
true.
48
T or F: Methadone is fast acting and has less accumulation
False, slow acting and accumulates with repeated dose
49
what is the buprenorphine and naloxone combo called?
suboxone
50
T or F: Subutex has abuse potential.
true
51
T or F: Naltrexone has decent oral bioavailability
true
52
2 opioid antagonists
naloxone and naltrexone
53
which opioid antagonist is typically given IV or intranasal
naloxone
54
short half life (30-90 min) A. Naloxone B. Naltrexone
A
55
how long after the first narcan (naloxon) dose should you give the second?
2-5 minutes IF NOT CONSCIOUS
56
4 sxs of neonatal abstinence syndrome
tremors yawning poor feeding sweating
57
T or F: Heroin, methadone, and other opiates can cause serious withdrawal in babies when born
true
58
Seizures may also be a sx of neonatal abstinence syndrome in babies born to _____ users *
methadone
59
5 options for non-pharm tx of neonatal abstinence syndrome *
swaddling hypercaloric formula frequent feedings observation rehydration (all easy i guess)
60
Pharmacological tx of neonatal abstinence syndrome (3.5)
morphine sulfate sublingual buprenorphine methadone maybe clon?
61
Which 2 tx options are linked to a shorter hospital stay than methadone in the tx of neonatal abstinence syndrome?
morphine and buprenorphine