Opiates Flashcards

1
Q

what plant is opium derived from?

A

poppy flower

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2
Q

Name 3 opiates that are strictly mu receptor agonists

A

codeine, oxycodone, hydrocodone

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3
Q

name 3 opiates that can activate both mu and kappa receptors

A

nalbuphine, butorphanol, buprenorphine

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4
Q

Name the phenanthrenes

A

natural: codeine, morphine, semisynthetic: hydrocodone, hydromorphone, oxycodone, oxymorphone

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5
Q

name the phenylpiperidines

A

meperidine, fentanyl

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6
Q

name the phenylheptylamines

A

methadone (+propoxyphene)

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7
Q

are opiates narcotics?

A

no - don’t refer to opiates as narcotics

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8
Q

if a phenanthrene isn’t effective for a pt, name 2 drugs you could switch to

A

meperidine, fentanyl

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9
Q

if fentanyl isn’t effective for the pt, name a drug you could switch to

A

methadone

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10
Q

True or false: opiates are used as backup therapy, first line depends on the type of pain

A

TRUE - opiates are backup therapy

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11
Q

according to WHO, mild pain can be treated with

A

non-opiate analgesics with or without adjuvant medications

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12
Q

according to WHO, mild to moderate pain can be treated with

A

weak opiate + non-opiate analgesic with or without adjuvant meds

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13
Q

according to WHO, moderate to severe pain can be treated with

A

strong opiates with our without non-opioid analgesic medication with or without adjuvant medications

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14
Q

NRS

A

numeric rating scale - should be included on scripts

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15
Q

what is the name of the faces scale for pain?

A

Wong baker faces rating scale

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16
Q

what are examples of nociceptive pain?

A

tissue injury, joints, MSK, burns, incisions

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17
Q

what are examples of neuropathic pain?

A

carpal tunnel, DM, CA, shingles

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18
Q

does neuropathic pain respond well to opiates?

A

no

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19
Q

where do opiates work in the brain?

A

site of action is the PAG and it blocks GABA. From the PAG it moves to the medulla which mediates NE and serotonin. MOR blocks Ca2+ and opens K+ channels causing hyperpolarization. Also acts at post-synaptic and K1 receptors

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20
Q

MOA of opiates

A

inhibition of painful stimuli in the substantia gelatinosa of the spinal cord, brainstem, reticular activating system, thalamus, and th elimbic system

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21
Q

effects of opiates

A

sedation, euphoria, mental clouding, respiratory depression, miosis, decreased peristaltic motility, depression of the cough reflex and orthostatic HOTN

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22
Q

ADR of opiates

A

increased esophageal reflux, N/v in the CTZ, peripheral vasodilation, increased histamine, prolongs labor, decreased urinary void reflex

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23
Q

which mu receptor is best known?

A

mu1

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24
Q

where are mu receptors found?

A

primarily supraspinal than spinal - all over: PAG, superficial dorsal horn, amygdala

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25
Q

what type of pain do mu receptors relieve

A

somatic pain more than visceral pain

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26
Q

ADR of mu receptor agonists

A

respiratory depression, euphoria, dependence, decreased GI motility, miosis

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27
Q

where are kappa receptors mostly located?

A

spinal more than suprespinal

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28
Q

what type of pain is relieved by kappa receptor agonists?

A

visceral pain

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29
Q

ADR of kappa receptor agonists?

A

sedation, miosis, dysphoria

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30
Q

primary location of delta receptors

A

spinal more than supraspinal

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31
Q

ADR of delta agonists

A

tachycardia, tachypnea, dysphoria, hallucinations, mydriasis, hypertonia

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32
Q

what is the “relative” of oxycodone with a longer T1/2?

A

oxycontin

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33
Q

what are opiates used for?

A

pain relief

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34
Q

are opiates susceptible to first pass effect?

A

yes

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35
Q

how are opiates metabolised?

A

CYP450/2D6 (genetic variability in metabolism)

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36
Q

how are opiates excreted?

A

in the urine, small amount in the feces (watch with renal impairment - may build up opiates)

37
Q

what drugs will decrease opiates in the system by stimulating 3A4?

A

st. john’s wart, antiseizure drugs

38
Q

what drugs will increase opiates in the system by inhibiting 3A4?

A

azoles, macrolides

39
Q

what drugs will increase opiates in the system by inhibiting 2D6?

A

fluoxetine, paroxetine, wellbutrin, rionavir

40
Q

what other drugs will increase CNS effects of opiates?

A

alcohol, sedatives, muscle relaxants, phenothiazines (falling, falling asleep may occur)

41
Q

what drugs can be a PCA?

A

fentanyl, morphine

42
Q

are parenteral opiate doses lower or higher than po?

A

lower

43
Q

Name all the dosage forms for opiates

A

oral, IM, IV, topically (patch), buccallu, sublingual, nasal

44
Q

contraindications for opiate use

A

allergy to opiates, acute bronchial asthma/upper airway obstruction, MAOi use in the last 14 days

45
Q

cautions for opiate use

A

history of intolerance, serioud adverse effects, lack of efficacy of opioid therapy, pt with sleep apnea not on CPAP, COPD pts, arrhythmias

46
Q

if a pt has an opiate allergy is it safe to move to a different group?

A

yes

47
Q

how should you take someone off of an opiate?

A

taper it for a few days or weeks

48
Q

what is addiction defined as?

A

increased feedback from the VTA

49
Q

true or false: start at the lowest possible dose for opiate rx

A

TRUE

50
Q

what is opiate ceiling dose dependant on?

A

side effect profiles

51
Q

how are opiates dosed for routine use?

A

treat pts for 48 hours with immediate release opioids and then convert 2/3 of the estimated daily dosing to a sustained-release regimen

52
Q

how is constipation prevented with opiate use?

A

treat empirically with docusate sodium 100mg bid

53
Q

what is a rescue dose of opiates

A

5-15% the daily dose

54
Q

what is the time of onset and peak effect of opiates?

A

onset: 45mins, peak effect: 60mins

55
Q

how do you treat an opiate user who is already constipated?

A

milk of magnesia

56
Q

what other therapy should you provide for your opiate using pts besides docusate sodium?

A

anti-emetics and diphenydramine

57
Q

what are some ways to monitor opiate therapy?

A

use standard pain assessment tools, assess of adverse events, dependency and interference with ADLs, VS (orthostatic BP), resp. function, cardiac sounds, abdominal sounds, bowel/urinary fxn

58
Q

how do you convert from one opiate to another?

A

equipotent doses - look them up

59
Q

what should elderly pts avoid when treating pain?

A

NSAIDs (GI bleed, MI, stroke, HTN, decreased kidney function) use acetaminophen!

60
Q

ADR of opiates in the elderly

A

use short term only, increased fx risk, death, CV risk (codeinde, oxycodone)

61
Q

what are ebenfits of using tramadol?

A

decreased fx risk

62
Q

MC opiates used in peds

A

oxycodone, hydrocodone, codeine (avoid!)

63
Q

are opiates safe to use in peds?

A

yes - risks are not much greater in children than in adults

64
Q

what is hydrocodone usually paired with?

A

acetaminophen

65
Q

what determines the ceiling dose of vicodin

A

the acetaminophen - not the hydrocodone

66
Q

what can vicodin treat?

A

moderate to severe pain

67
Q

is vicodin more or less constipating than codeine?

A

less

68
Q

what is the #1 prescribed drug in the US?

A

vicodin

69
Q

is hydromorphone mor or less strong than morphine

A

7-10 times the analgesic activity of morphine

70
Q

benefits of using hydromorphone?

A

less histamine release and no active metabolites, better tolerated in renal impairment and hemodynamic instability, less n/v, less sedation and constipation

71
Q

ADR of hydromorphone?

A

increased respiratory depression

72
Q

what is “hillbilly heroine”

A

oxycodone (oxycontin)

73
Q

Whaich drug is 100x more potent than morphine?

A

fentanyl

74
Q

benefits of using fentanyl?

A

less sedation, less constipation, less histamine release, safest in renal failure, no active metabolites, lower ADR

75
Q

why are IM/IV effects seen sooner than po?

A

lipphilic drug so fast effects, short duratino of action

76
Q

Nonopiate actions of methadone

A

inhibition and reuptake of monoamines (serotonin and NE), inhibition of NMDA receptors (decreases pain threshold)

77
Q

benefits of methadone

A

long acting, ess sedation and euphoria, longest T1/2 (12-190hrs), opiate detox use

78
Q

how is methadone dosed?

A

every 4-8 hours then once pt is stable q8-12 hours

79
Q

ADR of methadone

A

QT prolongation

80
Q

what is codeine?

A

less potent than morphine, prodrug converted by 2D6 into morphine

81
Q

codeine is more likely to cause

A

constipation and nausea than other opiates

82
Q

30mg of codeine = how many mg of morphine

A

1mg

83
Q

if you cant convert codeine what does that mean?

A

no morphine!

84
Q

75mg of demerol = how many mg of morphin

A

5-7.5 (1/10 potency)

85
Q

ADR of demerol

A

seizure, delerium, tremors (d/t metabolite)

86
Q

is demerol use reversible with naloxone?

A

no

87
Q

max dose of demerol

A

less than 48 hours with max of 600mg every 24 hours with normal renal functioning

88
Q

What are the 2 metabolites of morphine - compare them

A

M3G (myclonus, confusion, hyperalgesia), M6G (2-4x more potent than morphine