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Pharmacology - Exam 2 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

define narcotic

A

“sleep-inducing”

better legal than medical term

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2
Q

define opiate

A

derived from opium

ie) morphine or codeine

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3
Q

define opioid

A

compound with pharmacology similar to morphine

ie) synthetic drugs or endogenous opioid ligands

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4
Q

define analgesic

A

pain-relieving

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5
Q

define endogenous opioids

A

naturally occurring opioids that mimic the actions of exogenous opiates in the brain and periphery

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6
Q

what three genes are endogenous opioids made from

A

POMC (pro-opio-melano-cortin gene)
Pro-enkephalin gene
Pro-dynorphin gene

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7
Q

what active opioid product does the POMC gene make

A

B-endorphin

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8
Q

what active opioid product does the pro-enkephalin gene make

A

met-enkephalin and leu-enkephalin

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9
Q

what active opioid product does the pro-dynorphin gene make

A

dynorphin-A (also dynorphin-B, neo-endorphins, and leu-enkephalin)

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10
Q

what endogenous opioid binds Mu opioid receptor

A

B-endorphin and enkephalins

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11
Q

what endogenous opioid binds Delta opioid receptor

A

mostly enkephalins and some B-endorphin

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12
Q

what endogenous opioid binds Kappa opioid receptor

A

dynorphin

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13
Q

where are the endogenous opioids working

A

at descending inhibitory pathway

have inhibitory effect on C pain fibers

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14
Q

what type of receptors are the opioid receptors? ionotropic? muscarinic/metabotropic?

A

muscarinic/metabotropic

ALL G-PROTEIN-COUPLED

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15
Q

of the three opioid receptors which is the major one and what are its effects

A

Mu opioid receptor

analgesia, respiratory depression, euphoria, dependence ie) drug addiction

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16
Q

what is an important non-opioid receptor

A

DM receptor

mediates antitussive effects (anti-cough)

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17
Q

therapeutic effects of opioids

A

analgesia
antitussive
antidiarrheal
(also mood enhancement and relief of acute pulmonary edema)

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18
Q

Of the three types of pain which does opioids not work well on

A

neuropathic pain

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19
Q

what is a problem with the antidiarrheal therapeutic effect of opioids

A

constipation

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20
Q

general effects of opioid analgesia

A

inc pain threshold (discriminative)
inc pain tolerance (affective/emotional)
selective for analgesia

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21
Q

what general effects of opioid analgesia is unique compared to local anesthetics

A

inc pain tolerance (local anesthetics don’t do that, they just do the discriminative inc pain threshold) and selective for analgesia (local anesthetics are not selective, they affect other somatosensory modalities as well)

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22
Q

sites of action for opioid analgesia

A

opioid receptors at C fibers/ascending pain pathways and descending pain inhibitory pathways and cerebral cortex

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23
Q

major receptor of analgesic action

A

Mu opioid receptor with contribution from Delta opioid receptor

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24
Q

how does the analgesic action if opioids work at the ascending pathway

A

1) activate Mu opioid receptors on C fibers which blocks opening of Ca channels so NTs/sub P not released
2) activate Mu opioid receptors on spinothalamic neuron enhancing the opening of K+ channels leading to hyperpolarization
(slide 15)

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25
Q

what type of pain does opioid analgesia work on

A

best agains slow pain/C fiber pain (dull, burning, aching, constant) less effective against fast pain/A-delta fibers (sharp, intense, stinging intermittent pain)

  • *good against nociceptive and inflammatory pain
  • **bad against neuropathic pain
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26
Q

what is an example of neuropathic pain

A

postherpetic neuralgia resulting from shingles

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27
Q

how does the analgesic action if opioids work at the descending pain inhibitory pathway

A

Mu receptors activated in brain to activate descending pain inhibitory pathway that activates enkephalin containing interneurons that synapse onto the terminal end of C-fibers so Mu receptors on C-fibers activated which blocks the opening of Ca channels so NTs/sub P not released and enkephalins also work on spinothalamic neuron by opening K+ channels causing hyperpolarization
RESULT inhibition of pain ascending pathways
(slide 18)

28
Q

pathway of the descending pain inhibitory pathway

A

descending serotonergic neurons from Raphe Nucleus
synapse onto enkephalin containing interneurons
synapse onto terminal end of C-fibers and have inhibitory effect on the release of NTs at this terminal end of C-fibers (C-fiber synapses onto spinothalamic neuron to thalamus)
RESULT is inhibition of ascending pain pathway

29
Q

opioid use in anesthetic settings include

A

1) as premedication (act as sedative, anxiolytic, analgesic) prior to general anesthetic
2) intraoperatively as adjunct to general anesthetic or as primary general anesthetic
3) spinal anesthesia for thoracic or abdominal surgery or in labor

30
Q

T/F antitussive effects are not mediated by opioid receptors

A

true

31
Q

what receptor mediates antitussive effects

A

DM receptor

32
Q

is the DM receptor stereoselective

A

no

not selective for l or d form of stereoisomer

33
Q

is the Mu opioid receptor stereoselective

A

yes

selective for l form of stereoisomer (so no d form)

34
Q

examples of opioids/opiates in l isomer so levy form so have antitussive and analgesic effect

A

natural opioids like B-endorphin and opiates like morphine

35
Q

example of opioids/opiates in d isomer so dextro form so have antitussive but no analgesic activity

A

dextromethorphan

36
Q

why might the dextro d form be a good

A

has antitussive effect but not analgesic so no respiratory depression, euphoria, nausea, or addiction

37
Q

result of anti-diarrheal effects mediated by opioid receptors

A

delayed gastric emptying
inc transit time in GI tract
inc water absorption in GI tract
constipation

38
Q

is there tolerance for the anti-diarrheal effects of opioids

A

little to no tolerance

39
Q

common adverse effects of opioids (mostly Mu/MOR mediated)

A 
constipation (#1 complaint)
nausea/vomiting
sedation
miosis (construction of pupils)
pruritus
40
Q

less common adverse effects of opioids (mostly MOR/Mu mediated)

A

respiratory depression (cause of death from opioid therapy)
urinary retention
cardiovascular effects are indirect (meperidine)
truncal rigidity
dysphoria
physical dependence and addiction

41
Q

triad of opioid overdose

A

pinpoint pupils (miosis)
respiratory depression
dec consciousness

42
Q

direct effect on heart by Meperidine

A

antimuscarinic activity leading to tachycardia

43
Q

can tolerance occur with opioids

A

yes, can occur with continued use

44
Q

is tolerance to opioids unsafe

A

generally does not affect safety

45
Q

is there cross-tolerance among opioids

A

yes but it can be incomplete

46
Q

major opioid cautions and contraindications

A

substance abuse history

drug interactions with SSRIs and sedative hypnotics/anti-psychotics

47
Q

what to do if substance abuse history

A

still require pain relief so do not withhold opioids when patient is experiencing severe pain but look for possible analgesic tolerance and prescribe carefully/limit prescription

48
Q

Drug interactions of opioids with SSRIs

A

SSRIs combined with certain opioids like meperidine and propoxyphene can can lead to life threatening serotonin syndrome (tachycardia, hypertension, hypertherm, seizures)

49
Q

drug interactions of opioids with sedative hypnotics/anti-psychotics

A

sedative hypnotics/anti-psychotics combined with opioids can lead to increased respiratory depression

50
Q

other possible opioid cautions and contraindications

A 
head injuries
pregnancy
impaired pulmonary function
impaired renal function
impaired hepatic function
Addison's or hypothyroidism
partial agonists (pentazocine) with full agonists (morphine) can precipitate withdrawal
51
Q

administration routes of opioids

A 
oral
buccal
sublingual
transdermal
nasal
suppository
parenteral (intramuscular, subcutaneous, IV, intrathecal)
52
Q

what to use with neuropathic pain

A

antidepressants and anticonvulsants

so atypical analgesics

53
Q

therapeutic considerations

A 
acute vs chronic pain
type of pain
goals for onset and duration
opioid naive vs opioid dependent
GI motility
hepatic or renal impairment
ability to tolerate oral delivery
54
Q

first line high efficacy opioid analgesics/agonists AKA strong agonists AKA full agonists

A

morphine
methadone
fentanyl

55
Q

second line high efficacy opioid analgesics/agonists AKA strong agonists AKA full agonists

A

meperidine

56
Q

low-medium efficacy oral opioid analgesics/agonists AKA mild to moderate agonists

A

codeine
oxycodone
hydrocodone

57
Q

characteristics of low-medium oral opioid analgesics/agonists AKA mild to moderate agonists

A

only available in oral preparations
some drugs have mild to moderate agonists combined with acetaminophen- FDA recommends not using these drugs due to liver toxicity with chronic acetaminophen, also contraindicated in patients with liver impairment/compromised function (i.e. Vicodin, Percocet, Lortab, Roxicet, etc)

58
Q

mixed kappa agonist-mu antagonists

A

pentazocine

59
Q

mixed partial mu agonist-kappa antagonists

A

buprenorphine

60
Q

non-analgesic opioids

A

dextromethorphan aka dextrorphan

antitussive

61
Q

antagonists

A

naloxone

competitive antagonists at all opioid receptors but not at non-opioid receptors like DM

62
Q

primary use of naloxone

A

treatment for opioid overdose

because of short duration must monitor overdose patient closely and be prepared to administer multiple doses

63
Q

examples of neuropathic pain

A

diabetic neuropathy
postherpetic neuralgia
fibromyalgia
phantom limb pain

64
Q

drugs to use for neuropathic pain

A

atypical analgesics because don’t always respond to opioids (antidepressants and anticonvulsants)

65
Q

what to use for treatment of mild pain

A

aspirin/NSAIDS

acetaminophen

66
Q

what to use for treatment of moderate pain

A

aspirin/NSAIDS
acetaminophen
combine above with low to medium efficacy oral opioids

67
Q

what to use for treatment of severe pain

A

high efficacy opioids

alone or with adjuncts

Pharmacology - Exam 2 (14 decks)

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