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PHARM 2 > Opioids > Flashcards

Opioids Flashcards

1
Q

2 opioids used for diarrhea

A

1) loperamide
2) diphenyoxylate

lack analgesic effects at usual doses

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2
Q

coanalgesic for neuropathic pain

A

imipramine

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3
Q

meperidine AE

A

large doses given in short intervals - seizures, mydriasis

meperidine = short t 1/2 BUT its metabolite = normeperidine has a t 1/2 of 15-20 hours

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4
Q

fentanyl is metabolized by

A

CYP3A4

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5
Q

which opioids are metabolized by CYP2D6

A

codeine (used CYP2D6 to convert to morphine)
oxycodone
hydrocodone

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6
Q

combination of which two opioid types can cause withdrawal sxs

A

pure agonist + weak partial agonist - risk of diminishing analgesia OR inducing withdrawal

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7
Q

what is meperidine contraindicated with

A

MAOI, serotinergic agents

- meperidine can block reuptake of serotonin

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8
Q

what is tramadol contraindicated with

A

MAOI
epileptic patients: inc risk of seizures in pt with seizure disorders and those taking medications that lower seizure threshold

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9
Q

what are opioids contraindicated with

A

1) sedatives

2) anti psychotics

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10
Q

what clinical conditions are opioids contraindicated with

A

impaired: pulmonary, renal, liver, adrenal function

pregnancy

head injuries

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11
Q

opioids for severe pain

A

1) morphine
2) heroine
3) oxycodone hydrocodone

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12
Q

methadone AE

A

QT prolong - torsades

death

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13
Q

tramadol contraindications

A

serotinergic drugs –> serotonin syndrome

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14
Q

tramadol use

A

neuropathic pain

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15
Q

tramadol MOA

A

weak mu agonist AND NE/serotonin reuptake inhib

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16
Q

methadone MOA

A

strong mu agonist, NMDA antagonist, serotonin/NE reuptake inhibitor

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17
Q

pentazocine

A

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

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18
Q

butorphanol

A

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

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19
Q

nalbuphine

A

mixed agonist and antagonist opioid

kappa agonist, mu antagonist/partial agonist

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20
Q

buprenorphine

A

mixed agonist and antagonist opioid

partial mu agonist, kappa antagonist

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21
Q

ceiling effect in which drugs

A

1) pentazocine
2) butorphanol
3) nalbuphine
4) buprenorphine

22
Q

mixed agonist and antagonist opioids AE

A

all cause psychomimetic effects except: buprenorphine

23
Q

mixed agonist and antagonist opioids use

A

to reduce addiction potential of opioids

  • potent in opioid naive pt
  • can precipitate withdrawal in pt who are already physically dependent
24
Q

buprenorphine use

A

management of opioid addiction
psychomimetic effect is uncommon
partial mu agonist and kappa antagonist

25
Q

naloxone

A

used in tx of opioid OD

opioid antagonist at mu, delta, kappa receptors

26
Q

naltrexone

A

used for opioid addiction – dec alcohol craving

opioid antagonist at mu, delta, kappa receptors

27
Q

antitussives (2)

A

dextrometorphan

codeine

28
Q

which receptors to antimotility opioids work at

A

mu and delta receptors on enteric nerves, epithelial cells, and muscle

29
Q

topical and blocks VG sodium channels

A

lidocaine

30
Q

loperamide and diphenoxylate act on which receptors

A

mu and delta on enteric nerves, epithelial cells, muscle

31
Q

which drug decreases craving for alcohol in chronic alcoholics?

A

naltrexone

32
Q

which drug is preferred for managing opioid withdrawal?

A

methadone

33
Q

what makes methadone a good drug for managing opioid withdrawal

A

long t 1/2 = abstinence syndrome is prolonged BUT less severe
less profound sedation
euphoria

34
Q

methadone vs morphine

A

equal in potency

less euphoria, longer duration

35
Q

fentanyl MOA

A

mu agonist
rapid onset/short duration

100x more potent than morphine

36
Q

meperidine MOA

A

mu receptor agonist

not recommended b/c of metabolite toxicity

37
Q

heroin MOA

A

hydrolyzes to 6-MAM –> then to morphine

38
Q

heroin vs morphine

A

heroin and its metabolite (6-MAM) more liposoluble than morphine = enter brain more readily

39
Q

morphine MOA

A

strong agonist of mu, delta, kappa
high affinity at mu
low affinity at delta and kappa

40
Q

which drugs are hydrolyzed by tissue esterases

A

heroin

remifentanil

41
Q

opioid metabolism

A

convert to glucuoronides = excretd by kidneys

42
Q

morphine conjugated

A

morphine-3-glucoronide = neuroexcitatory

also conjugates to M6G = more potent than morphine

43
Q

ingestion of toxic doses of mu agonists presents with

A

pinpoint pupils - d/t PS excitation

44
Q

where are mu receptors located

A

peripheral terminals of sensory neurons

45
Q

opioids MOA

A

close VG Ca2+ channels of PRESYNAPTIC NT and open K+ on POSTSYNAPTIC neurons

46
Q

receptors associated with supraspinal analgesia

A

mu, kappa, delta

47
Q

receptors associated with spinal analgesia

A

mu, kappa, delta

48
Q

receptors associated with respiratory depression

A

mu

49
Q

receptors associated with dec GI motility

A

mu, delta

50
Q

receptors associate with psychotomimesis

A

kappa

51
Q

receptors associated with sedation

A

mu, kappa

52
Q

G protein associated with opioid receptors

A

G(i)

PHARM 2 (18 decks)

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