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PHRM 845 > L? Pharm of opiates - Barker > Flashcards

L? Pharm of opiates - Barker Flashcards

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
Q

Morphine:
MOA (kinda):
Phen or nonphen:
Receptor:
NMDA activity?
Kappa activity?

A

full agonist
phen
mu
no nmda
no kappy

26
Q

Nociceptin receptor endogenous opioid

A

nociceptin duh

27
Q

which 3 opioids are prodrugs with an active metabolite? *

A

heroin
codeine
tramadol

28
Q

T or F: Fentanyl and methadone produce active metabolites

A

False

29
Q

High lipophilicity
A. Morphine
B. Fentanyl

A

b

30
Q

CYP3A4 makes opioids starting with?

A

NOR
oxycodone -> noroxycodone
oxymorphone -> noroxymorphone

31
Q

PM (poor metabolizer) (of CYP2D6) phenotype is more common in what group?

A

white people somehow

32
Q

__ phenotype is of high relevance worldwide.
A. PM (poor)
B. IM (intermediate)
C. EM (extensive)
D. UM (ultra-rapid)

A

D

33
Q

fentanyl is how much more potent than:
morphine
heroin

A

100 x
50 x

34
Q

which opioid is typically used in palliative care

A

fentanyl

35
Q

which 3 opioids are broken down by plasma esterases due to ester linkage?

A

3 synthetic ones: sufentanil, remifentanil, alfentanil

36
Q

which opioid has snri properties?

A

tramadol

37
Q

which opioid has the toxic active metabolite normeperidine?

A

meperidine (demerol) lol

38
Q

Methadone: **
- Primarily used for ______ ________
- ________ __ (unwanted effect)
- ______ antagonist *

A

opioid dependence
prolonged QTc
NMDA

39
Q

2 opioids that can be used for cough

A

codeine and dextromethorphan

40
Q

2 opioid agonists used as anti-diarrheal

A

Diphenoxylate w/ atropine (lomotil)
and
loperamide (imodium)

41
Q

Pentazocine and Butorphanol MOA

A

Kappa agonist, partial agonist/antagonism at mu

42
Q

3 side effects for pentazocine and butorphanol

A

less dysphoria
hallucinations
increase in BP/HR

43
Q

Nalbuphine (nubain) MOA

A

Full agonist at kappa
antagonist at mu
antagonism produces withdrawal

44
Q

buprenorphine MOA and primary use

A

Partial mu agonist, weak kappa agonist and delta antagonist (damn)
primary use in opioid replacement therapy

45
Q

3 meds used for preventative and acute mgmt of ileus and constipatino

A

senna -> colonic contraction** (so pick this one if it comes up)
miralax
docusate

46
Q

Methadone MOA

A

FULL mu agonist

47
Q

T or F: Methadone is frequently used in medication assisted treatment for opioid dependence

A

true.

48
Q

T or F: Methadone is fast acting and has less accumulation

A

False, slow acting and accumulates with repeated dose

49
Q

what is the buprenorphine and naloxone combo called?

A

suboxone

50
Q

T or F: Subutex has abuse potential.

A

true

51
Q

T or F: Naltrexone has decent oral bioavailability

A

true

52
Q

2 opioid antagonists

A

naloxone and naltrexone

53
Q

which opioid antagonist is typically given IV or intranasal

A

naloxone

54
Q

short half life (30-90 min)
A. Naloxone
B. Naltrexone

A

A

55
Q

how long after the first narcan (naloxon) dose should you give the second?

A

2-5 minutes IF NOT CONSCIOUS

56
Q

4 sxs of neonatal abstinence syndrome

A

tremors
yawning
poor feeding
sweating

57
Q

T or F: Heroin, methadone, and other opiates can cause serious withdrawal in babies when born

A

true

58
Q

Seizures may also be a sx of neonatal abstinence syndrome in babies born to _____ users *

A

methadone

59
Q

5 options for non-pharm tx of neonatal abstinence syndrome *

A

swaddling
hypercaloric formula
frequent feedings
observation
rehydration
(all easy i guess)

60
Q

Pharmacological tx of neonatal abstinence syndrome (3.5)

A

morphine sulfate
sublingual buprenorphine
methadone
maybe clon?

61
Q

Which 2 tx options are linked to a shorter hospital stay than methadone in the tx of neonatal abstinence syndrome?

A

morphine and buprenorphine

PHRM 845 (34 decks)

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