pharmacology of opioids Flashcards

1
Q

what are the chemical classes of opioids?

A

phenathrenes
phenylpiperidines
benzomorphans
dipheylheptanes

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2
Q

what are the functional classes or opioids

A

opioid agonists

mixed agonists/antagonists

opioid antagonist

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3
Q

give a classic example of opioid agonists (5)

A

morphine
methadone
fentanyl
codeine
hydrocodone

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4
Q

give an example of a mixed opioid agonist/antagonist (2)

A

pentazocine
buprenorphine

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5
Q

given an example of opioid antagonists (2)

A

naloxone and naltrexone

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6
Q

opioid drugs MOA

A

bind to the opioid receptors in the CNS and inhibit pain pathways giving a generalized CNS depression

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7
Q

onset of action of an opioid is dependent on what

A

patient

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8
Q

duration of pain relief in opioids

immediate release
extended release
epidural/intrathecal
suppository

A

immediate release: 3-5 hrs

extended release: 8-24 hrs.

epidural/intrathecal- up to 24 hrs

suppository - 3 to 7 hrs

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9
Q

when do we use opioid therapy

A

in acute/chronic pain and pain management

MI, sickle cell crisis, back pain, cancer, post operative procedures, adjunct to anesthesia, antitussive*
antidiarrheal

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10
Q

opined drug side effects

A

CNS depression

Respiratory depression-BBW

constipation

hypotension

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11
Q

what is the black box warning associated with using opioids?

A

respiratory depression (can be fatal) monitor closely especially during initiation or dose escalation.

*carbon dioxide retention from opioid induced respiratory depression can exacerbate the sedating effects of opioids

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12
Q

acute effects of opioids

A

sedation, euphoria, loss of cough reflex (antitussive), slowed CNS and heart

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13
Q

chronic effects of opioids

A

tolerance, hepatic and brain damage, dependance and addiction, loss of appetite, loss of libido

hepC from sharing needles

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14
Q

how do sedatives/hypnotics interact with opioid drugs

A

they increase the central nervous system depression (respiratory depression)

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15
Q

how to antipsychotics interact with opioids?

A

increase sedation and cardiovascular effects

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16
Q

how do monamine oxidase inhibitors interact with opioids?

A

they are contraindicated because they can cause hyper pyrexic coma

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17
Q

fentanyl is _ times more potent than morphine

A

100

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18
Q

lower doses of opioids before analgesic effects are

A

antidiarrheal
antitussive
euphoria
nausea

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19
Q

higher doses of opioids after analgesic effects are?

A

mitosis/vomiting
sedation
respiratory depression
coma/death

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20
Q

what is the function of the mu receptor

and what is its endogenous opioid peptide affinity

A

supraspinal and spinal analgesia

INHIBITION OF RESPIRATION

slowed GI transit

modulation of hormone and NT release

**ENDORPHINS

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21
Q

what is the function of the delta receptor

and what is the endogenous opioid peptide affinity

A

supra spinal/spinal analgesia

modulation of hormone and NT release

ENKEPHALINS

22
Q

what is the function of the kappa receptor

and what is the endogenous opioid peptide affinity

A

supra spinal and spinal analgesia

PSYCHOMIMETIC EFFECTS

slower GI transit

DYNORPHINS

23
Q

which drug is an agonist at the mu, delta, and kappa receptors

A

morphine!

24
Q

which drug is an agonist at the mu receptor

A

methadone

25
Q

what drug is a partial agonist at the mu, delta, and kappa receptor

A

buprenorphine

26
Q

what drug is an antagonist at the mu and delta receptor

A

naloxone

27
Q

_ is an opioid agonist that is indicated for the management of pain not reponsive to non-narcotic analgesics

do not use if there is sulfa allergy, bronchial asthma, or respiratory depression

A

morphine

28
Q

what opioid is indicated management of persistent moderate to severe chronic pain that requires continuous around the clock opioid administration for an extended period of time

**pain is not controlled with non-narcotic anaglesics, combination opioids, all option exhausted

A

fentanyl

29
Q

which opioid is most appropriate to manage abstinence symptoms and treat opioid use disorder in an outpatient rehabilitation setting (withdrawal acute and active)- full agonist

A

methadone

(clinics)

detoxification and maintence

30
Q

which opioid is used for moderately to severe pain that is a semi synthetic narcotic with antitussive qualities (anti cough)

very common and highly prescribed

A

hydrocodone

31
Q

hydrocodone is frequently combined with ?

A

acetaminophen

32
Q

what opioid is a mixed agonist/antagonist that is used in the management of severe pain that alternative treatments have failed to treat

A

pentazocine

33
Q

pentazocine is used when?

addiction?

A

used as a preoperative or preanaethesia medication and as a supplement

does not work for addiction

34
Q

concomitant use of opioids with _ or another other CNS depressants including alcohol can result in sedation, depression, coma and death

A

benzodiazepines

35
Q

prolonged used of _ during pregnancy can result in neonatal opioid withdrawal syndrome

A

pentazocine

36
Q

which opioid is used in the management of severe pain that was not mitigated by other option and CANNOT be mixed with a mixed agonist/antagonist analgesics because it can precipitate withdrawal symptoms

A

meperidine

37
Q

what opioid is an analgesic, antitussive and contains the least opioid analgesic activity

A

codeine

38
Q

which opioid exposed patients and users to the risks of opioid addiction, abuse and tissues

A

codeine

39
Q

uses of codeine

A

mild pain, cough, diarrhea

40
Q

when discontinuing chronic opioid therapy the dose should be

A

gradually tapered down

41
Q

which opioid is used to treat diarrhea and decrease the amount of drainage in patients with ostomies

patient with addiction can take this to minimize withdrawal effects (OTC)

A

loperamide

42
Q

which opioid is indicated in the treatment of pain, addiction to opioids (withdrawal - acute and maintenance) it is a partial agonist and can be abused in similar ways to opioids

A

buprenorphine

43
Q

what should you be monitoring in patients if you start them on buprenorphine

A

monitor for overdosing or underusing since it is a CYP3A4 inhibitor and inducers

44
Q

MOA of naloxone

A

opioid antagonist at all sites

45
Q

use of naloxone

A

opioid overdose (reversal of opioid reversal )

give even in opioid overdose is SUSPECTED

46
Q

side effects of opioid antagonists

A

release of catecholamines that can cause acute withdrawal and cause pain

47
Q

what is the MOA of naltrexone

A

opioid antagonist that is a competitive inhibitor at the mu receptors

(opioid addiction - maintenance)

48
Q

use of naltrexone

A

alcohol disorder
opioid dependence

49
Q

what is the concern surrounding naltrexone in opioid overdose

A

people treated with naltrexone may response to lower opioid doses than used before which can lead to intoxication (life threatening)

50
Q

what is the concern surrounding naltrexone in opioid withdrawal

A

may precipitate symptoms of acute withdrawal in the opioid dependence in patients

51
Q

acute withdrawal of opioids in neonates

A

naltrexone - shrill cry

52
Q

can opioids exacerbate OTC pain relievers

A

yes

aspirin
ibuprofen
bismuth
naproxen
diphenhydramine