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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
what type of pain does opioid analgesia work on
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
26
what is an example of neuropathic pain
postherpetic neuralgia resulting from shingles
27
how does the analgesic action if opioids work at the descending pain inhibitory pathway
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
pathway of the descending pain inhibitory pathway
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
opioid use in anesthetic settings include
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
T/F antitussive effects are not mediated by opioid receptors
true
31
what receptor mediates antitussive effects
DM receptor
32
is the DM receptor stereoselective
no | not selective for l or d form of stereoisomer
33
is the Mu opioid receptor stereoselective
yes | selective for l form of stereoisomer (so no d form)
34
examples of opioids/opiates in l isomer so levy form so have antitussive and analgesic effect
natural opioids like B-endorphin and opiates like morphine
35
example of opioids/opiates in d isomer so dextro form so have antitussive but no analgesic activity
dextromethorphan
36
why might the dextro d form be a good
has antitussive effect but not analgesic so no respiratory depression, euphoria, nausea, or addiction
37
result of anti-diarrheal effects mediated by opioid receptors
delayed gastric emptying inc transit time in GI tract inc water absorption in GI tract constipation
38
is there tolerance for the anti-diarrheal effects of opioids
little to no tolerance
39
common adverse effects of opioids (mostly Mu/MOR mediated)
``` constipation (#1 complaint) nausea/vomiting sedation miosis (construction of pupils) pruritus ```
40
less common adverse effects of opioids (mostly MOR/Mu mediated)
respiratory depression (cause of death from opioid therapy) urinary retention cardiovascular effects are indirect (meperidine) truncal rigidity dysphoria physical dependence and addiction
41
triad of opioid overdose
pinpoint pupils (miosis) respiratory depression dec consciousness
42
direct effect on heart by Meperidine
antimuscarinic activity leading to tachycardia
43
can tolerance occur with opioids
yes, can occur with continued use
44
is tolerance to opioids unsafe
generally does not affect safety
45
is there cross-tolerance among opioids
yes but it can be incomplete
46
major opioid cautions and contraindications
substance abuse history | drug interactions with SSRIs and sedative hypnotics/anti-psychotics
47
what to do if substance abuse history
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
Drug interactions of opioids with SSRIs
SSRIs combined with certain opioids like meperidine and propoxyphene can can lead to life threatening serotonin syndrome (tachycardia, hypertension, hypertherm, seizures)
49
drug interactions of opioids with sedative hypnotics/anti-psychotics
sedative hypnotics/anti-psychotics combined with opioids can lead to increased respiratory depression
50
other possible opioid cautions and contraindications
``` 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
administration routes of opioids
``` oral buccal sublingual transdermal nasal suppository parenteral (intramuscular, subcutaneous, IV, intrathecal) ```
52
what to use with neuropathic pain
antidepressants and anticonvulsants | so atypical analgesics
53
therapeutic considerations
``` 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
first line high efficacy opioid analgesics/agonists AKA strong agonists AKA full agonists
morphine methadone fentanyl
55
second line high efficacy opioid analgesics/agonists AKA strong agonists AKA full agonists
meperidine
56
low-medium efficacy oral opioid analgesics/agonists AKA mild to moderate agonists
codeine oxycodone hydrocodone
57
characteristics of low-medium oral opioid analgesics/agonists AKA mild to moderate agonists
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
mixed kappa agonist-mu antagonists
pentazocine
59
mixed partial mu agonist-kappa antagonists
buprenorphine
60
non-analgesic opioids
dextromethorphan aka dextrorphan | antitussive
61
antagonists
naloxone | competitive antagonists at all opioid receptors but not at non-opioid receptors like DM
62
primary use of naloxone
treatment for opioid overdose | because of short duration must monitor overdose patient closely and be prepared to administer multiple doses
63
examples of neuropathic pain
diabetic neuropathy postherpetic neuralgia fibromyalgia phantom limb pain
64
drugs to use for neuropathic pain
atypical analgesics because don't always respond to opioids (antidepressants and anticonvulsants)
65
what to use for treatment of mild pain
aspirin/NSAIDS | acetaminophen
66
what to use for treatment of moderate pain
aspirin/NSAIDS acetaminophen combine above with low to medium efficacy oral opioids
67
what to use for treatment of severe pain
high efficacy opioids | alone or with adjuncts

Pharmacology - Exam 2 (14 decks)

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