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ANPH 510 pharm 2 mccarver > opioid agonists > Flashcards

opioid agonists Flashcards

0
Q

name some morphine derivatives

A

dilaudid (morphine with a hydroxyl group added)

heroin (morphine with two acetyl groups added)

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1
Q

how do opioid agonists produce miosis?

A

opioids cause miosis (pupillary constriction) by acting on mu and kappa receptors to stimulate the Edinger Westphal nucleus of the oculomotor cranial nerve (CN3) to constrict pupils

“The Edinger–Westphal nucleus is the accessory parasympathetic cranial nerve nucleus of the oculomotor nerve (cranial nerve III), supplying the constricting muscles of the Iris.” - wikipedia

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2
Q

name some phenylpiperidine derivatives

A

demerol
anything with fentanyl like sufenta, remi, etc.

most commonly used opioid agonists in anesthesia

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3
Q

why can’t you use opioids as the sole anesthetic?

two reasons

A

respiratory depression

not reliable as anesthetics

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4
Q

phenylpiperidines vary widely in potency, from the least potent __ to the most potent __

A

least - demerol (50mg to stop shivering)

most - sufenta (0.4 mcg/kg/min as an infusion)

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5
Q

where do opioid agonists work?

A

STEREOSPECIFIC receptors sites at pre and post synaptic sites in the CNS, also outside the CNS in peripheral tissues

NON-ionized and LEVOrotary

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6
Q

what is the prototypical opioid agonist?

A

morphine

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7
Q

where do neuraxial opioids exert their effect?

A

mu receptors of the substantia gelatinosa in the spinal cord

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8
Q

the epidural dose is usually __x greater than the subarachnoid dose

A

5-10x

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9
Q

remember, neuraxial opioids are specific for __, not somatic pain

A

visceral

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10
Q

epidural opioids work via mu spinal cord receptors AND __

A

systemic action

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11
Q

which way do neuraxial opioids move?

is the movement greater with more or less lipid soluble opioids?

A

they move cephalad

movement is greater with LESS lipid solubles like morphine

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12
Q

what’s the most common side effect of neuraxial opioids?

A

pruritis

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13
Q

what is poikothermia?

A

when the body temp equilibrates with room temp

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14
Q

is pruritis from histamine release?

A

NOPE, it’s due to cephalad migration in the CSF to trigeminal nucleus

treatment is narcan, antihistamines

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15
Q

four main side effects of neuraxial opioids

A

pruritis, urinary retention, ventilatory depression, sedation

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16
Q

how do neuraxial opioids cause urinary retention and what is the treatment?

A

opioid receptor activation in sacral spinal cord inhibits sacral parasympathetic outflow causing detrusor muscle relaxation and greater bladder capacity

reversed with narcan

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17
Q

what is the MOST SERIOUS side effect of neuraxial opioids?

A

respiratory depression, 2 hours think cephalad migration in CSF interacting with ventral medulla

occurs most often with morphine, coughing, ongoing use

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18
Q

sedation after neuraxial opioid is most common with __

A

sufentanil

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19
Q

should you use morphine WITH preservatives in epidural/SAB?

A

no

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20
Q

how do neuraxial opioids cause water retention?

A

release vasopressin

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21
Q

since neuraxial opioids delay gastric emptying, if your epidural patient becomes a crash c-section, besides the fact they are a full stomach, hold ___ !

A

cricoid

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22
Q

analgesia with morphine is best when given __ pain starts

A

before

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23
Q

morphine has a slower peak than fentanyl due to slower penetration of the __

A

BBB

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24
Q

morphine has poor CNS penetration due to high ionization, poor lipid solubility, and rapid conjugation via __ acid

A

glucuronic acid

25
Q

where and how is morphine metabolized?

A

glucuronic acid conjugation in liver and kidney, 75% changed to morphine-3 which is INACTIVE, 25% changed to morphine-6 which is GREATER analgesic than morphine

26
Q

morphine is eliminated in the __ so it has a cumulative effect in end stage renal patients

A

urine

27
Q

how does morphine drop your BP?

A
  • decreased SNS tone to capacitance vessels = decr venous return
  • bradycardia from stimulation of vagal nuclei in medulla = decr cardiac output
  • histamine release
28
Q

give morphine no faster than __ mg/min

A

5 mg/min

29
Q

how do people breathe on morphine?

A

like a hibernating bear, big tidal but slow rate, net increased PaCO2

could be bad for neuro patients d/t incr ICP from incr CO2

30
Q

how to correct angina like pain caused by morphine induced spasm of biliary smooth muscle?

A

narcan, glucagon, ntg

31
Q

signs your CRNA friend may be going through morphine withdrawal

A

yawning, sweating, can’t sleep, restless, cramps, N/V, diarrhea

32
Q

what was the first synthetic opioid agonist? what receptors does it work on?

synthesized by Nazi chemists using cyanide and methylamine

A

meperidine/demerol

33
Q

where and how is meperidine metabolized? any metabolites?

A

hepatic metabolism, urine excretion, metabolite = nor-meperidine, has half the potency

34
Q

you’re not allergic to meperidine, you’re allergic to __-meperidine

A

nor-meperidine

35
Q

meperidine is 60% protein bound so has greater effects in __, __, and __ failure patients

A

elderly, malnourished, liver failure

36
Q

what opioid has the narrowest therapeutic index of all?

A

meperidine

37
Q

how does meperidine decrease post-op shivering?

A

kappa agonism

38
Q

meperidine for cough? diarrhea? cardiac?

A

no, no, no
has similar structure to atropine so increases HR and heart O2 req’s
produces MYDRIASIS, not miosis

39
Q

fentanyl can rapidly redistribute to inactive tissues like fat and muscle, but the __ can store up to 75% of the initial dose

A

lungs

40
Q

fentanyl metabolism and metabolite

A

metabolized to nor-fentanyl - minimally analgesic

urine excretion

41
Q

fentanyl dosages and responses
1-2 mcg/kg
2-20 mcg/kg
50-150 mcg/kg

A

1-2 analgesia
2-20 adjuvant to inhaled
50-150 sole anesthetic

42
Q

what are the disadvantages to using fentanyl as the sole anesthetic?

A

not reliable amnesia, post op ventilatory depression, sympathetic breakthrough, absorbed by CPB circuit

43
Q

what are the advantages to fentanyl?

A

not a myocardial depressant (but does cause bradycardia by depressing carotid sinus - could be dangerous to neonates)
no histamine release
supression of stress response
it comes in a lollypop

44
Q

fentanyl and ICP

A

increased ICP

45
Q

sufenta is __ to __ more potent than fentanyl

A

5-10x

46
Q

sufenta metabolism and metabolite

A

dealkylation into inactive metabolites

47
Q

sufenta excretion

A

equal urine and GI

48
Q

sufenta can cause prolonged vent depression in __

A

ESRD

49
Q

how is sufenta better than fentanyl?

A

greater analgesia and less vent depression, more rapid induction, earlier emergence and extubation, minimal hemodynamic changes

50
Q

sufenta is NOT better than fentanyl in these areas

A

not perfect in blunting BP and stress response to surg, may cause chest wall rigidity, bradycardia

51
Q

remifentanyl is unique due to its __ linkage

A

ester

52
Q

how is remi metabolized?

A

ester hydrolysis

53
Q

which is more potent, remi or fentanyl?

A

equal

54
Q

how fast can steady state be reached with a remi infusion?

A

10 minutes

55
Q

does remi have active metabolites?

A

no, otherwise it would not have such a short action

56
Q

does remi last longer in pt’s with liver or kidney failure?

A

nope, go ahead and use it.

57
Q

what receptor for remi?

A

mu

58
Q

what if your patient has a plasma cholinesterase difficiency, should you use remi??

A

not a problem, use it.

59
Q

your patient may develop chest wall rigidity and be unable to ventilate with remi. what should you do?

A

hypnotics or NMB

60
Q

does remi cause histamine release?

any problems with giving remi to a ESRD or liver?

A

no

no

61
Q

narcan is a pure antagonist

A

reverses opioids

ANPH 510 pharm 2 mccarver (7 decks)

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