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Principles Anesthesia II > Medications from Acute Pain > Flashcards

Medications from Acute Pain Flashcards

1
Q

Hydrocodone + Tylenol (3)

A

Norco, Lortab, Vicodin

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2
Q

Dolophine

A

Methadone

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3
Q

MsContin, Kadian, MSIR

A

morphine

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4
Q

Percocet

A

oxycodone + acetaminophen

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5
Q

Percodan

A

oxycodone + aspirin

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6
Q

Controlled-released oxycodone is called

A

oxycontin

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7
Q

3-Methoxymorphine is ____

A

codeine

derived from opium poppy

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8
Q

Codeine is metabolized (CYP450) into two things:

A

10% morphine (active)

the rest into inactive norcodeine

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9
Q

if children 12 years or younger receive this medication, they can experience side effects w/o analgesia dt immature enzymes in the liver

A

codeine

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10
Q

Dose: (adult)

30-60 mg q 4hrs, max 360 mg/day

A

Codeine

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11
Q

Pediatric dosing for codeine

A

0.5-1 mg/kg

max 60 mg/dose

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12
Q

What is the ceiling effect dose for codeine?

A

60 mg

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13
Q

Opioids, alcohol, and anticholinergics interact with ______

A

codeine

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14
Q

Contraindications for codeine (4)

A
  1. hypersensitivity
  2. acute/chronic ashtma
  3. respiratory depression
  4. paralytic ileus
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15
Q

codeine works on what receptors

A

mu, kappa, delta

side effects include: N/V, brady, hypotension, respiratory depression, urinary retention, constipation, dizziness, miosis

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16
Q

synthetic 4-phenylpiperidine analogue of morphine and codeine

A

Tramadol

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17
Q

Tramadol is a racemic mixture of two enantiomers + & -

+ enanatiomer is centrally acting opioid agonist with moderate affinity to ____ receptor, weak affinity to ____ & ___, and opposes _____ reuptake

A

strong affinity: mu

weak: kappa and delta

opposes serotonin reuptake

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18
Q

Tramadol is a racemic mixture of two enantiomers + & -

( — )enantiomer inhibits _____ reuptake and stimulates _____ receptors

A

inh. norepinephrine reuptake

and stimulates alpha 2 receptors

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19
Q

Tramadol is metabolized by CYP450 into ______

A

o-desmethyltramadol

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20
Q

o-desmethyltramadol 2-4x more potent or weaker than Tramadol?

A

Potent

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21
Q

What is Tramadol’s potency compared to morphine?

A

1/5- 1/10s the potent to morphine

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22
Q

Tramadol’s onset PO

A

1-2 hrs

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23
Q

Tramadol’s protein binding

A

20%

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24
Q

Tramadol is contraindicated in patients that have what?

A

seizure disorders

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25
Q

T/F:

tramadol causes respiratory depressioin

A

false: minimal

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26
Q

T/F:

Tramadol is not associated with dependence, tolerance, or addiction

A

True

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27
Q

T/F:

Tramadol causes constipation

A

F: minimal

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28
Q

T/F:

Tramadol does not cause N/V

A

F: high incidence of N/V

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29
Q

Oral dose of Morphine is about ___x higher than IM or IV

A

3

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30
Q

Morphine primarily acts on what receptors

A

Mu 1 and Mu 2

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31
Q

This drug’s primary pathway for metabolism is conjugation with glucuronic acid in hepatic and extrahepatic sites, especially the kidney

A

Morphine

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32
Q

Morphine gets metabolised into two substances

A

morphine-6-glucuronide

morphine-3-glucuronide

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33
Q

T/F:

morphine-3-glucuronide contributes to analgesia

A

F: morphine-3-glucuronide causes adverse effects such as neurotoxicity and hyperalgesia

morphine-6-glucuronide contributes to analgesia

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34
Q

Morphine’s absorption into the CNS is minimal dt 3 things:

A

1.poor lipid solubility (morphine hydrophilic)

  1. high protein binding (35%)
  2. high degree of ionization at physiologic pH
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35
Q

Morphine IM

onset: ____

peak: _____

A

onset: 15-30 mins

peak: 45-90 mins

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36
Q

Women vs men

who has a greater analgesic potency and slower speed of offset with morphine

A

women

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37
Q

Morphine is contraindicated in what patients and why?

A

renal impairment dt metabolite morphine-6-glucuronide causing respiratory depression

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38
Q

______ is a semisynthetic derivative of thebaine

A

oxycodone

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39
Q

oxycodone has recently replaced ____ as the most used opioid worldwide

A

morphine

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40
Q

oxycodone can be made alone or combined with 3 things and has many names

A

acetaminophen (Percocet), aspirin (Percodan), and ibuprofen (Combunox)

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41
Q

This drug is used to tx neuropathic pain syndrome and to treat acute/chronic pain

A

oxycodone

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42
Q

controlled release oxycodone is called?

A

Oxycotin

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43
Q

Oxycodone is mainly a prodrug and is metabolized into two forms ___ & ____

A

(active) Oxymorphone
(inactive) noroxycodone

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44
Q

What receptors do oxycodone work on

A

Mu and Kappa

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45
Q

How is oxycodone metabolized and excreted?

A

Cype 450 (2D6) and excreted in the urine

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46
Q

T/F:

Oxycodone has an extensive first pass effect

A

true

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47
Q

Oxycodone (PO)

onset:

duration: IR & CR

A

onset: < 1hr

duration: IR 3-4 hrs

duration: CR: 12 hrs

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48
Q

Oxycodone dose PO

A

10-15 mg of oxycodone is equal to 10 mg Morphine

49
Q

Protein binding of oxycodone

A

45%

50
Q

T/F

Oxycodone can only be given PO

A

F: can be giving both IV/ PO (PO most common)

51
Q

T/F: oxycodone doesn’t cause histamine release

A

F: oxycodone causes histamine release

52
Q

This drug is a synthetic broad-spectrum opioid that has become the maintenance drug for opioid addiction due to its oral bioavailability (60-95%) high potency, and long duration of action

A

Methadone

53
Q

What receptors does methadone work on?

A

weak non-competitive NMDA antagonist, serotonin reuptake inhibitor, monoamine transmitter reuptake inhibitor, and affinity for the mu- receptor

54
Q

How is methadone metabolized and does it have an active metabolites?

A

metabolized by the liver CYP450 and only has inactive metabolites

55
Q

What effect does carbamazepine have on methadone’s metabolism?

A

carbamazepine (anticonvulsant/ (Tegretol®)* ) is a CYP450 inducer, so it lowers the concentration of the drug in the bloodstream

56
Q

What effect do antiretroviral agents and grapefruit have on methadone’s metabolism?

A

inhibit CYP45, so metabolism is reduced so the concentration of the drug is higher in the bloodstream

57
Q

Does hepatic and renal impairment influence the clearance of methadone significantly?

A

No

58
Q

Steady-state of methadone may take up to ____ days, dt extensive redistribution of the drug

A

10

59
Q

The morphine/methadone equianalgesic ratio appears to be curvilinear:

3:1 at morphine doses < ___ mg/day

20:1 at morphine doses > ___ mg/day

A

3:1 at morphine doses < 100 mg/day

20:1 at morphine doses > 1000 mg/day

60
Q

Methadone dose: PO/IM/SC

A

2.5-10 mg q4-12 hrs

61
Q

Methadone has a high variable half-life pt to pt so dosing guidelines are unachievable.

Half-life range: ___ - ____

A

8-80 hours

“ * one time dose of 10 mg, you can guess about 12-24 hours of pain relief”

62
Q

ciprofloxacin, diazepam, and ethanol (acute use) have what effect of methadone?

A

increase concentration/effect

63
Q

Amprenavir, phenobarbital, phenytoin, rifampin (abx), MAOIs have what effect of methadone?

A

decrease concentration/effect

MAOIs have an unpredictable reaction with MAOIs

64
Q

Methadone S/E includes: 4

A

hypotension, respiratory depression, sedation, confusion

65
Q

This medication rarely cause these side effects:

pause-dependent dysrhythmia associated with bradycardia *, QT prolongation *, and torsades

A

methadone

66
Q

____ is a phenylpiperidine-derivative synthetic opioid agonist that is structurally related to meperidine (demeral)

A

Fentanyl

67
Q

This drug has high potency, rapid onset of action and short duration of action

A

fentanyl

68
Q

Extensively metabolized by N-demethylation and produces ____, ____, ____

A

norfentanyl

hydroxyproprionyl-fentanyl

hydroxyproprionyl-norfentanyl

69
Q

____ is the principal metabolite of fentanyl and is excreted by the kidneys

A

Norfentanyl and is structurally similar to normeperidine

70
Q

This drug’s elimination is slightly prolonged despite a short duration of action due to the _____ serving as a large inactive reservoir

A

Fentanyl

lungs: large inactive reservoir

71
Q

Why does fentanyl have a greater potency and more rapid onset compared to morphine?

A

lipid solubility

Fentanyl is lipophilic while morphine is hydrophilic

72
Q

Where does 75% of first-pass effect occur for fentanyl?

A

lungs

73
Q

what is the % protein binding for fentanyl?

A

84%

74
Q

____: is a semisynthetic drug and hydrogenated ketone of analogue of morphine and can be formed by N-demethylation of hydrocodone

A

Hydromorphone

75
Q

this drug is an effective alternative to morphine for tx of moderate to severe pain. Available in PO, IV, and rectal

A

Hydromorphone

76
Q

How much stronger is hydromorphone than morphine when administered orally?

A

3-5x stronger

77
Q

How much stronger is hydromorphone than morphine when administered parenterally?

A

8.5x stronger

78
Q

Hydromorphone is metabolized in the liver to ____

A

hydromorphone-3-glucuronide (active)

79
Q

Does hydromorphone-3-glucuronide have analgesic effects?

A

No, it lacks analgesic effects but may be an active metabolite that potentiates neurotoxic effects: allodynia, myoclonus, and seizures

luckily production of this product is low unless pt has renal insufficiency

80
Q

Hydromorphone:

Parenteral dose for postoperative pain ____ mg every ___ -___ mins, titrated to achieve a balance btw pain relief and respiratory depression

A

dose: 0.2 mg

Q 3-5 mins

81
Q

Duration of action for hydromorphone

A

3-4 hours

(same of IR of oxycodone)

82
Q

Oral dose of hydromorphone

A

2-8 mg

83
Q

____ a semi-synthetic opioid which is a codeine derivative

A

hydrocodone

84
Q

how much stronger is hydrocodone to codeine?

A

6-8x stronger

85
Q

Hydrocodone is commonly paired with ______

A

acetaminophen

86
Q

Norco concentration

A

Norco: 5mg hydrocodone w/ 325 mg tylenol

87
Q

Vicodin concentration

A

Vicodin: 5mg hydrocodone w/ 500 mg tylenol

88
Q

Lortab concentration

A

Lortab: 7.5mg hydrocodone w/ 325mg tylenol

89
Q

This drug is the second most abused prescription behind oxycodone

A

hydrocodone

90
Q

The liver metabolizes hydrocodone and produces 2 metabolites: ___ & ____

A

hydromorphone (active)

Norhydrocodone (inactive)

91
Q

30 mg of hydrocodone = ___ mg of morphine

A

10 mg of morphine

92
Q

dose range of hydrocodone:

___ -____ mg hydrocodone w/ ___-___ mg of acetaminophen q4-6 hrs

A

2.5-10 mg of hydrocodone w/

300-750 mg of acetaminophen

4g max tylenol in 24 hrs

93
Q

These side effects are for what drug:

meiosis, histamine release, pruritus, decreased hypercapnia drive/ RR, airway reflexes, bradycardia, hypotension, NV

A

hydrocodone

94
Q

____: a semi-synthetic agonist-antagonist opioid derived from the opium alkaloid thebaine

A

Buprenorphine

95
Q

Buprenorphine

partial agonist @ __ receptor

antagonist @ ___ receptor

and a weak ___ receptor agonist

A

partial agonist @ mu receptor

antagonist @ kappa receptor

and a weak delta receptor agonist

96
Q

T/F: Burprenorphine

has less respiratory depression, less immune suppression, no accumulation in patients with renal function

A

True

97
Q

What is Subutex

A

buprenorphine

98
Q

What is the metabolite of buprenorphine?

A

Norbuprenorphine

99
Q

What receptors do norbuprenorphine act on?

A

full agonist at mu, delta, and ORL-1

partial agonist at Kappa

100
Q

Does Buprenorphine’s metabolite have more or less effect on respiratory depression?

A

Norbuprenorphine has extremely little antinociceptive potency but markedly increased respiratory depression (10fold)

101
Q

Buprenorphine

____ mg = 10 mg of morphine

A

0.3 mg

102
Q

Oral administration of buprenorphine results in high first-pass metabolism and can be bypassed by sublingual

sublingual administration –> onset of _____ mins

duration of ___-___ hrs

A

sublingual

onset: 30 mins

duration 6-9 hrs

103
Q

Does renal impairment affect the elimination of buprenorphine?

A

No mainly hepatic elimination so there is little risk of accumulation with renal impairment

104
Q

This drug can be resistant to antagonism with naloxone

A

buprenorphine

105
Q

other name for phenytoin

A

Dilantin

106
Q

other name for carbamazepine

A

tegretol

107
Q

other name for Topiramate

A

Topamax

108
Q

other name for baclofen

A

lioresal

109
Q

other name for carisoprodol

A

soma

110
Q

other name for cyclobenzaprine

A

flexeril

111
Q

other name for Methocarbamol

A

robaxin

112
Q

other name for Tizanidine

A

Zanaflex

113
Q

Opioid conversion: Morphine

parenteral: 10 mg

Oral:

A

Oral: 30 mg

114
Q

Opioid conversion: Hydromorphone

parenteral: 1.5 mg

Oral:

A

Oral: 7.5 mg

115
Q

Opioid conversion: Oxycodone

Oral:

A

Oral: 20-30 mg*

parenteral: —-

116
Q

Opioid conversion: Codeine

parenteral: 130 mg

Oral:

A

Oral: 200 mg

117
Q

Opioid conversion: Hydrocodone

parenteral: —–

Oral:

A

parenteral: —–

Oral: 30 mg

118
Q

Opioid conversion: Methadone

parenteral: 1.5-2.5

Oral:

A

Oral: 3-5 mg

119
Q

Opioid conversion: Fentanyl

parenteral:

oral: —-

A

parenteral: 0.1 mg

oral: —-

Principles Anesthesia II (2 decks)

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