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Principles of Anesthesia II - Fall 2024 > Acute Pain - Drugs - Exam 2 > Flashcards

Acute Pain - Drugs - Exam 2 Flashcards

1
Q
A
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2
Q

What are long-term Opioid options? (7)

A
  1. codeine (Tylenol #3)
  2. fentanyl (duragesic patch)
  3. hydrocodone (lortab, vicodin)
  4. hydromorphone (dilaudid)
  5. methadone (dolophine)
  6. morphine (MSIR, MScontin, Kadian)
  7. oxycodone (OxyIR, Percocet, Percodan, Oxycontin)
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3
Q

Codeine

What is the chemical name?
What is it derived from?

It has a substitution of ____ group for ____ group on #3 carbon of morphine.

A

3-methyloxymorphine

  • derived from opium poppy plant (papaver somniferum)
  • methyl group for hydroxyl group
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4
Q

Codeine

Receptors:

A
  • Mu opioid
  • weak kappa/delta
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5
Q

Codeine

Codeine is more reliably ________ ________ than morphine.

A

absorbed orally

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6
Q

Codeine

Codeine is admin as a ________.

It is metabolized by what enzyme? (active state)

what enzyme metabolizes codeine to the inactive state?

A
  • prodrug
  • CYP2D6 = morphine (active)
  • CYP3A4 = norcodeine (inactive)
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7
Q

Codeine

Why is there variability in analgesic effects w/ codeine?

A
  • > 50 polymorphisms in CYP enzymes
  • don’t give to children < 12y/o - they will only get the SE and no pain relief
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8
Q

Codeine

Adult dose:
max dose:
How much codeine does Tylenol # 3 have?
Tylenol # 4?

A
  • 15-60 mg q4h
  • max: 360mg/d (4-6 doses)
  • # 3 - 30mg
  • # 4 - 60mg
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9
Q

Codeine

Pedi dosing
max:

A

0.5-1mg/kg
Max: 60mg
try to avoid giving

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10
Q

Codeine

At what dose of codeine do you get the max analgesic effect?

What med & dose is this comparable to?

A

60 mg
Aspirin 650mg

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11
Q

Codeine

Half-life

A

3-3.5hrs

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12
Q

Codeine

Drug Interactions

A
  • opiods
  • alcohol
  • anticholinergics
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13
Q

Codeine

Adverse/SE (8):

A
  1. n/v
  2. brady
  3. hypotension
  4. resp. depression (lg. doses)
  5. urinary retention
  6. constipation
  7. dizziness
  8. miosis
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14
Q

Codeine

Contraindications

A
  • hypersensitivity
  • acute/severe asthma (histamine release = bronchoconstriction)
  • paralytic ileus
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15
Q

Tramadol

What is the chemical name?

  • composed of a racemic mixture w/ a ____ and ____ enantiomer.
A
  • Synthetic 4 phenylpiperidine analogue of morphine & codeine
  • + and - enantiomer
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16
Q

Tramadol

MOA of the + enantiomer:

A
  • centrally acting opioid agonsit
  • mod. affinity @ Mu
  • weak Kappa/delta
  • opposes serotonin reuptake
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17
Q

Tramadol

MOA of the - enantiomer:
what are the effects of this?

A
  • inhibits NE reuptake
  • stimulates a2 receptors
  • effects: BP issues, potentiate precedex
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18
Q

Tramadol

Metabolism:

active metabolite:

potency:

A
  • CYP2D6 & CYP3A4
  • O-desmethyltramadol
  • 2-4x potent as tramadol (less potent than morphine)
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19
Q

Tramadol

Potency compared to morphine

A

1/5-1/10 as potent as morphine

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20
Q

Tramadol

Onset:

A

1-2 hrs

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21
Q

Tramadol

Half-life:

A
  • tramadol: 6.3hrs
  • metabolite: 7.4hrs
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22
Q

Tramadol

PB:

A

20%

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23
Q

Tramadol

Vd:

A

2.6-2.9L/kg

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24
Q

Tramadol SE/Precautions

Major Contraindication:

high incidence of:

A
  • do NOT give in pts w/ seizure disorders
  • high incidence of n/v
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25
Q

Morphine

Who was morphine named after?

A

Morpheus the Greek God of Dream

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26
Q

Morphine

What preparations is Morphine available in?

A
  • immediate and sustained release
  • elixir
  • suspension
  • tablets/capsules
  • epidural/intrathecal
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27
Q

Morphine

Oral dose:IM/IV dose

A
  • oral dose 3x more
  • oral - 30 mg
  • IV/IM - 10 mg
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28
Q

Morphine

Receptor Effects:

A

Mu 1 & Mu 2

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29
Q

Morphine

Metabolism:

active metabolites and effects

A
  • conjugation (glucuronic acid) w/ hepatic & extrahepatic sites (kidneys)
  • morphine-6-glucuronide: analgesia
  • morphine-3-glucuronide: neurotoxicity & hyperalgesia
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30
Q

Morphine

What are the 3 reasons why morphine has minimal absorption into the CNS?

A
  1. poor lipid solubility
  2. high PB%
  3. high degree of ionization @ physiologic pH
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31
Q

Morphine

PO dose & onset:

A
  • PO: 30-60mg
    Onset: 30min - 1hr
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32
Q

Morphine

IV dose & onset:

A
  • IV dose: 2.5-15mg
  • IV onset: 15 min
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33
Q

Morphine

IM dose:
IM onset:

A

IM dose: 10-15 mg
IM onset: 20 min

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34
Q

Morphine

Peak:
Duration:

A
  • peak: 45-90 min
  • duration: 4-5 hrs
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35
Q

Morphine

E 1/2 time:

A

1.7-3.3 hours

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36
Q

Morphine

Does morphine have greater analgesia potency and slower offset in men or women?

A

Women

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37
Q

Morphine

% PB
Vd

A
  • % PB - 35%
  • Vd - 224L/kg
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38
Q

Morphine

What pt population should morphine be avoided in and why?

A
  • renal impairment
  • morphine-6-glucuronide accummulation = resp. depression
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39
Q

Morphine

Side Effects:

A
  • sedation
  • resp. depression
  • constipation, n/v
  • HISTAMINE RELEASE - acute use
  • euphoria
  • tolerance/dep.
40
Q

Oxycodone

What 2 formulations is it available in?

A
  • intermediate release
  • controlled release
41
Q

Oxycodone

Science:

It is a ________ derivative of ________.

Made alone or in combo with ________, ________, or ________.

A
  • semi-synthetic derivative of thebaine
  • Acetaminophen, aspirin, ibuprofen
42
Q

Oxycodone

What 2 main conditions is oxy used for?

A
  • neuropathic pain
  • chronic pain
43
Q

Oxycodone

Metabolism:

Admin as a ________.

Metabolites (2)

Oxy has an extensive ________, and is excreted in the ________.

A
  • metabolized in liver (CYP2D6)
  • admin as a prodrug
  • Metabolites:
    oxymorphone - active
    noroxycodone - inactive
  • extensive 1st pass effect
  • excreted in urine
44
Q

Oxycodone

What receptors does oxy work on?

A
  • Mu & Kappa in CNS
45
Q

Oxycodone

Dosing:
morphine equivalence:

A

5mg PO
* 10-15mg of Oxy = 10mg morphine

46
Q

Oxycodone

Onset:
Duration:

A
  • Onset: < 1 hr
  • Duration:
    IR: 3-4hrs
    CR: 12 hrs

allows pt to get to steady state and remain there

47
Q

Oxycodone

Half-life
IR:
CR:

A
  • IR: 3 hrs
  • CR: 4.5hrs
48
Q

Oxycodone

PB %
Vd

A
  • % PB - 45%
  • Vd - 2.6L/kg
49
Q

Oxycodone

Interactions/SE

A

additive effects w/ other CNS depressants
* sedation, resp. depression
* constipation, n/v
* histamine release
* euphoria
* tolerance/dep. (less)

50
Q

Methadone

Methadone is a synthetic ________ opioid and mixed ________ - ________.

A
  • synthetic broad-spectrum opioid
  • mixed agonist/antagonist
51
Q

Methadone

MOA/receptors:

A
  • weak, non-competitive NMDA receptor antagonist
  • serotonin reuptake inhibitor
  • monoamine transmitter reuptake inhibitor
  • mu receptor activity
52
Q

Methadone

what is methadone most commonly used for?

What drug properties make it ideal for this use?

A
  • maintenance drug for opioid addiction
  1. oral bioavailability (60-95%)
  2. high potency
  3. long DOA
53
Q

Methadone

Metabolism

Increased by:

Decreased by:

Excretion:

A
  • liver - CYP3A4, CYP1A2, CYP2D6
  • increased - inducers (carbamazepine)
  • decreased - antiretrovirals & grapefruit juice
  • excretion - urine & bile

safe for elderly - hepatic/renal impairment don’t influence clearance much

54
Q

Methadone Dosing

How long will it take to reach steady state?

Half-life:

A
  • up to 10 days
  • half-life variable 8-80hrs
55
Q

Methadone

Dose:
Routes:

A
  • 2.5-10mg
  • PO, IM, SQ
  • q4-12hrs

10mg go to dose = 12 to 24hrs pain control for 1 dose

56
Q

Methadone

What 3 things can increase the concentration/effects of methadone?

A
  1. ciprofloxacin
  2. diazepam
  3. ethanol (acute)
57
Q

Methadone

What 4 things can decrease the concentration/effects of methadone?

A
  1. amprenavir
  2. phenobarbital
  3. phenytoin
  4. rifampin

severe, unpredictable reactions w/ MAOIs

58
Q

Methadone

SE

A
  • similar to others
  • resp. depresison
  • hypotension
  • confusion/sedation

rare: brady, QT prolongation, torsades de point

59
Q

Fentanyl Science

A ________ derivative synthetic opioid.
Structurally r/t what drug?

A
  • pheynylpiperidine
  • Meperidine
60
Q

Fentanyl

Metabolism:

Metabolites (3)

A
  • metabolism: CYP450 - N-demethylation
  • Metabolites:
    Norfentanyl, hydroxyproprionyl-fentanyl, hydroxoyproprionyl-norfentanyl
61
Q

Fentanyl

How long can norfentanyl be detected in the urine after a single dose?

62
Q

Fentanyl Dosing

IV dose:
IV onset:
IV half-life:

A
  • dose: 50-100mcg
  • Onset: 5-10min
  • Half-life: 30min-1hr
63
Q

Fentanyl Dosing

PNB dose:

64
Q

Fentanyl Dosing

Transdermal Dose:
TD onset:
TD half-life:

A
  • dose: 12.5-100mcg
  • onset: 12-24hr
  • half-life: 20-27hr
65
Q

Fentanyl Dosing

Transmucosal Dose:
TM onset:
TM half-life:

A
  • Dose: 200-1600mcg
  • onset: 6-15min
  • half-life: 2-12hr
66
Q

Fentanyl

E 1/2 time:

A
  • 3.1-6.6 hours
67
Q

Fentanyl

Why does Fentanyl have a greater potency & more rapid onset compared to morphine?

A
  • greater lipid solubility of Fentanyl
68
Q

Fentanyl

Why does fentanyl have a shorter DOA w/ a single dose?

A
  1. rapid redistribution to inactive tissue (fat, skel. muscle)
  2. 75% of initial dose undergoes 1st pass pulmonary uptake
69
Q

Fentanyl

PB % -
Vd -

A
  • % PB - 84%
  • Vd - 335L
70
Q

Fentanyl

Interactions/SE

A

additive effects w/ other CNS depressants
* sedation/resp. depression
* constipation/n/v
* histamine release
* euphoria
* tolerance & dependence

71
Q

Hydromorphone Science

A synthetic drug and ________ ________ of analogue of morphine.
Can be formed by N-demethylation of ________.

A
  • hydrogenated ketone
  • hydrocodone
72
Q

Hydromorphone

What forms is hydromorphone available in?

What are their potencies compared to morphine?

A
  • PO 3-5x more potent
  • IV 8.5x more potent
  • rectal
73
Q

Hydromorphone

Metabolism:
Metabolites & effects
What pt population are these effects worse in?

A
  • metabolism: liver
  • Metabolites
    hydromorphone-3-glucuronide - neurotoxicity (allodynia, myoclonus, seizures)
    worse in renal insuff. pts
74
Q

Hydromorphone Dosing

IV post-op dose:
reg IV dose:
Onset:

A
  • 0.2mg IV q 3-5min
  • usually under 2mg
  • 0.2-1mg (reg. IV dose)
  • Onset: 10-15min
75
Q

Hydromorphone Dosing

Oral dose:
Onset:

A
  • dose: 2-8mg
  • onset: 30min-1hr
76
Q

Hydromorphone

DOA:
Half-life:

A
  • DOA: 3-4hrs
  • half-life: 2.3hrs
77
Q

hydromorphone

Interactions/SE

A

additive effects w/ CNS depressants
* sedation/resp. depression
* constipation/n/v
* histamine release
* euphoria
* tolerance/dependence

78
Q

Hydrocodone Science

A semi-synthetic opioid which is a ________ derivative.

79
Q

Hydrocodone

How much more potent is hydrocodone than codeine?

A

6-8x more potent

80
Q

Hydrocodone

Metabolism:
Metabolites:

A
  • CYP2D6 - hydromorphone
  • CYP3A4 - Norhydrocodone (inactive)
81
Q

Hydrocodone Dosing

What is the hydrocodone:morphine equivalence dosing?

A
  • 10 mg Morphine = 30 mg hydrocodone
82
Q

Hydrocodone Dosing

PO dose:
onset:

A
  • 2.5-10mg hydrocodone w/ 300-750 mg acetaminophen q 4-6hr
  • onset: 30min
83
Q

Hydrocodone

Peak:
E 1/2 time:

A
  • peak: 1.3 hrs
  • E 1/2 time: 3.8 hrs
84
Q

Hydrocodone

What forms are hydrocodone available in?

What other drugs is hydrocodone put in combo with?

A
  • tablet/capsule, syrup/solution, XR suspension, XR tablet
  • combo drugs: tylenol, ASA, guaifenesin, various anti-histamines
85
Q

Hydrocodone

What other drug:drug interactions are there w/ hydrocodone?

A
  • CYP inhibitors/inducers
  • sedation - opioids/benzos
  • barbs - hypotension
  • IV Mg & CCB - increased opioid effects (sedation/HoTN)
86
Q

Hydrocodone

SE:

A
  • miosis, histamine release pruritis
  • decreased hypercapnic drive/RR/airway reflexes
  • brady, HoTN
87
Q

Hydrocodone

What 3 things needs require caution w/ hydrocodone?

A
  1. alcoholism
  2. drug abuse
  3. drugs w/ tylenol
88
Q

Buprenorphine Science

A semi-synthetic ________ - ________ opioid.
Derived from the opium alkaloid ________.

A
  • agonist-antagonist
  • thebaine
89
Q

Buprenorphine

MOA/receptors

A

used for tx of opioid abuse disorder and cancer/chronic pain
* pt agonist Mu receptors
* kappa antagonist
* weak delta receptor agonist

90
Q

Buprenorphine

What are 4 advantages to using Buprenorphine in cancer and chronic pain tx?

A
  1. less resp. depression
  2. less immune suppression
  3. reduced constipation
  4. no accumulation in pts w/ impaired renal function
91
Q

Buprenorphine

What 5 preparations is Burprenorphine available as?

A
  1. Cizdol
  2. Subutex
  3. Suboxone
  4. Zubsolv
  5. Bunavail

IV, patches, PO, SL

92
Q

Buprenorophine

Metabolism:
Metabolite & effects:

A
  • CYP3A4
  • Metabolite: Norbuprenorphine
    full agonist - mu, delta, ORL-1 opioid receptors
    pt agonist - kappa
    little anti-nociceptive potency, markedly increased resp. depression
93
Q

Buprenorphine

  • Buprenorphine - Morphine Equivalence
A

0.3mg IM Buprenorphine = 10mg Morphine

94
Q

Buprenorphine

SL onset:
SL DOA:

TD patch Dose:

A
  • SL onset: 30 min
  • DOA: 6-9hrs
  • TD patch: 5-70 mcg/hr for 4-7 days
95
Q

Buprenorphine

E 1/2 time:

96
Q

Buprenorphine

SE:

A
  • drowsiness
  • n/v
  • ventilation depression - prolonged/resistant to antagonism w/ naloxone = pulm. edema

Principles of Anesthesia II - Fall 2024 (10 decks)

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