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Mandie's Pharm test I > Pain & Opioids > Flashcards

Pain & Opioids Flashcards

1
Q

acute pain that is not treated promptly and properly transitions into ____ that causes _____

A

persistent pain; irreversible changes to nervous system

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2
Q

eudynia

A

symptomatic or normal pain

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3
Q

maldynia

A

pathophysiologic disease of the nervous system, “abnormal” pain

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4
Q

3 dimensions of pain

A

1) sensory-discriminative (sensation, location, quality)
2) motivational-effective (unpleasantness)
3) cognitive-evaluative (past experiences modify other 2 dimensions; negative or positively affect outcome and pain experience; based on patient beliefs, cultural background, past experience)

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5
Q

opioids affect which dimension of pain

A

motivational-effective

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6
Q

Which cells initiates the motor, sensory, and ANS responses of pain? which is inhibitory?

A

T cell; SG neuron

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7
Q

which NT release allows pain transmission?

A

Substance P (blocked by intrathecal opioids) and glutamate

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8
Q

opioid receptors on ____ are probably on Substance P terminals and block it’s release

A

substantia gelatinosa

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9
Q

non-opioid inhibitory NT

A

Endorphins (are excitatory for the descending p/ways that inhibit pain)
Serotonin (inhib in brain)
Norepi (RAS & hypothalamus)
glycine (inhibs at spinal chord by increasing Cl-)
GABA (cerebral cortex, basal ganglia, cerebellum, SC (increases cl- and hyperpolarizes)

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10
Q

Glutamate

A

excitatory NT in hippocampus, outer layer of cerebral cortex, and substantia gelatinosa (learning & memory recall, central pain transduction, excitotoxic neuronal injury)
-there are also inotropic glutamate receptors (ligand-gated channel opens, influx of cation (na+) and depolarization

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11
Q

opioids

A
  • have receptor agonist activity with morphine-like effects at mu receptors throughout body, but also at kappa and delta receptors
  • mu receptors produce analgesic and SE
  • inhib NT, block Ca influx and increase K efflux
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12
Q

analgesia

A

absence of pain without loss of consciousness

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13
Q

Which endogenous opioids affect mu receptors

A

endomorphins and endorphins

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14
Q

Which endogenous opioids affect delta receptors

A

endorphins and enkephalins

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15
Q

Which endogenous opioids affect kappa receptors

A

dynorphins

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16
Q

mu receptors

A

brain: sedation, analgesia, physical dependence
spinal cord (SG): resp depression, miosis
peripheral sensory neurons: euphoria
GI tract: reduced GI motility, vasodilation

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17
Q

kappa receptors

A

brain: analgesia, anticonvulsant effects, delirium
SC: diuresis
Peripheral: dysphoria, miosis, sedation, reduces shivering

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18
Q

delta

A

location: brain
action: analgesia, antidepressent effects, convulsant, dependence

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19
Q

generalized opioid SE

A

sedation & resp depression, N/V, CV effects (vasodilation d/t histamine release), euphoria (esp meperidine), antitussive, miosis, pruritis, biliary spasm, myoclonus/seizures with high dosage, chest wall rigidity

20
Q

morphine

A

-classic mu receptor agonist
-influences the motivational-effective aspect of pain
-analgesia in the brain mu-1 and spinal mu-2
-only 23% unionized and able to cross BBB
-lipid solubility low (1.4) slow onset
1/2 life 2-3 hours
DOA 4-6

21
Q

morphine SE

A
  • resp depression (shift to right of the CO2 response curve)
  • vent response to hypoxia decreased
  • N/V
  • large doses or rapid admin cause skeletal muscle rigidity (eliminated with GABA agonists and paralytics)
  • miosis
  • pruritis (not histamine related, but rx with antihistamines)
  • hyperalgesia with prolonged use
  • decreased cough reflex
  • decreased GI motility
  • increased biliary pressure by increasing phasic wave frequency of the sphincter of oddi
  • release of histamine
  • reduces centrally mediated SNS –> vasodilation
22
Q

morphine metabolism

A

70% metabolized in liver via glucuronidation (liver disease has minimal effect, but reduced liver blood flow reduces clearance [very old and young])
excretion of metabolites by kidney (renal disease affects)
-m3 glucuronide (75-85%) inactive metabolite, no analgesia
-m6 (5-10%) active, 10x more potent than morphine

23
Q

codeine

A

3-methyl-morphine

  • 10% converted to morphine which causes analgesia
  • less 1st pass metabolism when taken orally
24
Q

hydromorphone

A

5x more potent than morphine
onset : 5 min, peaks 10-20 min
1-2 mg dilaudid = 10-20 mg morphine

25
Q

oxycodone

A

-less first pass metabolism

26
Q

oxycontin

A

SR oxycodone, bolus high when crushed or chewed

27
Q

meperidine

A

1/10th potency of morphine but more lipid soluble –> faster onset
-less bradycardia/resp depression than equianalgesic morphine
-some local anesthetic activity
-has dysphoric and psychotomimetic effects (K receptor)
-less biliar pressure effect
-> histamine release than morphine
-liver metabolism
-active metabolite: normeperidine
T1/2 14-21 hours, can build to toxic levels–seizures/coma
-useful for post op shivering

28
Q

meperidine and serotonin syndrome

A

meperidine inhibits reuptake of serotonin, when given in conjunction with MAOI or SSRI can lead to serotonin syndrome (delirium, fever, convulsions)

29
Q

fentanyl

A

-50-100x more potent than morphine
-SE similiar at equianalgesic dose
-almost completely mu receptor agonist
-onset: 3-5 min (rapid resp depression)
context sensitive 1/2 life depends on length of admin
(1 min = 5 min; 1 hr = 20 min; 8 hour = 250 min)
-100% hepatic extraction to inactive metabolites
-clearance correlated to liver blood flow
-decreased with P450 inhibitors (cimetidine, erythromycin)
-transdermal patches

30
Q

alfentanil

A

10x more potent than morphine (1/10th -1/4 as potent as fentanyl)
-effects similar at equianalgesic dose
-mu receptor agonist
-very rapid onset (1-2 min; 90% unbound unionized at 7.4; crosses BBB)
-metabolized in the liver 30-50% (inactive metab)
context sensitive 1/2 life depends on length of admin, but less than fentanyl (1 min = 1 min; 1 hour = 30 mins, 8 hour = 50 mins)

31
Q

remifentanil

A
  • equipotent to fentanyl
  • v. rapid onset, 1 min (cannot be bolus)
  • mu receptor agonist
  • metabolism by non-specific plasma esterases
  • clearance is constant, not affected by liver flow, renal failure, length of infusion
  • great option for neurosurg
  • t1/2= 3 mins
32
Q

spinal opioids

A

preservative free
-less drug intrathecal than epidural
-spinal mu receptors are present in dorsal form
-morphine or fent admin spinally is analgesic
epidural : acute; intrathecal: acute and chronic
Morphine controls pain well, less sedation and resp depression than IV; SE: resp depression, N/V, itching
-d/t lipid solubility, morphine hangs around longer
-NO MOTOR BLOCKADE

33
Q

hydromorphone

A

IV or Po
-more lipid soluble than morphine, faster onset
-5x more potent
glucuronid metabolism (hydromorphone 6G less agonist act than morphine 6 G; 3 G inactive)

34
Q

hydrocodone

A

metabolized by CYP2D to hydromorphone

35
Q

oxycodone

A

metabolized by CYP2D6 to oxymorphone

36
Q

codeine

A

prodrug converted to morphine via demethylation by CYP2D6

37
Q

methadone

A

-ultra long active
1/2 life: 15-60 hr
-useful for addicted patient’s maintenance
-chronic pain management

38
Q

acute opioid overdose

A

sedation leads to stupor leads to coma leads to death
-rx with opioid antagonist naloxone
-abrupt reversal of all opioid effects
-may require multiple redosing due to opioid t 1/2
resp and cv support

39
Q

naloxone

A

competetive antagonist at mu, kappa, delta receptors
-given IV, IM, SQ
-onset: 1-2 mins
T1/2 60 mins (3 hours in infants)
met in liver by glucuronidation
0.4 mg per ampule
0.04 mg increments for slow/partial reversal

40
Q

naltrexone

A

oral opioid antangonist= slow active

-used for maintenance of opioid dependence

41
Q

Which effects do we not dev opioid tolerance to

A

Gi/ocular

42
Q

signs/symptoms of opioid withdrawl

A

restlessness, insomnia, perspiration, abd cramps, N/V/D, tachycardia, tachypnea, Hypertension/hypotension, hot/cold flashes

43
Q

tramadol

A

partial mu agonist (also inhibits MAO reuptake, adds to analgesic effect)

  • metabolized by CYP2D6
  • good for mild to moderate acute pain (not severe)
44
Q

tapentadol

A
  • partial mu agonist
  • less pharmacogenomic variability than tramadol
  • metabolized by CYP2C19, C19, D6
  • > mu receptor efficacy
  • good for mild to moderate acute pain (not severe)
45
Q

nalbuphine/butorphanol

A

kappa agonist; partial mu agonists; mu antagonists
nalbuphine 10x as potent as butorphanol
-chemically related to naloxone and oxymorphone
Good for ST, Acute moderate to severe pain (often L&D)
no chronic
receive benefits of opioids with fewer unwanted side effects

46
Q

petazocine

A

two isomers
+ has affinity for kappa; - does not
-often mixed with naloxone
-has ceiling effct

47
Q

buprenorphine

A
  • partial mu receptor agonist and kappa agonist
  • high affinity for mu: hard to reverse
  • useful to rx opioid addiction at higher doses
  • available as 7 day transdermal patch

Mandie's Pharm test I (10 decks)

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