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Anesthesia Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Which opioid has an atropine-like ring structure creating anticholinergic side effects?

A

Meperidine

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2
Q

What is the elimination half-life of meperidine? In healthy and renal failure patients?

A

15 hours for healthy people. Can exceed 35 hours for those with renal failure

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3
Q

Pharmacodynamic differences between synthetic opioids are due to?

A

Potency, rate of equilibrium between plasma, and site of drug effect

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4
Q

How are semisynthetic opioids changed from natural or synthetic?

A

modification of the morphine molecule

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5
Q

Which opioids can cause histamine release from Mast cells?

A

Meperidine, codeine, morphine

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6
Q

Are most opioids weak acids or weak bases?

A

Weak bases

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7
Q

Bc opioids are mostly weak bases, how does the ionization of the drug change when the physiologic pH is < than the pKa?

A

When pH < pKa of a weak base, the base (aka drug) will be MORE ionized. Less drug is available to cross membranes.

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8
Q

Bc opioids are mostly weak bases, how does the ionization of the drug change when the physiologic pH is > than the pKa?

A

When pH > pKa of a weak base, the base (aka drug) will be LESS ionized. Meaning more drug is available to cross membranes.

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9
Q

What are the natural opioids we utilize?

A

Morphine

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10
Q

What are three endogenous opioid ligands?

A

Enkephalins
Endorphins
Dynorphins

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11
Q

What are the three opioid receptors?

A

Mu, Kappa, and Delta

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12
Q

What are the effects of Mu receptor stimulation?

A

Analgesia
Euphoria
Miosis
Respiratory Depression
Constipation
Bradycardia
Urinary Retention

Risk for dependence/abuse

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13
Q

What are the effects of Kappa receptor stimulation?

A

Analgesia
DYSphoria
Sedation
Less Respiratory depression***
Diuresis
Miosis

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14
Q

What are the effects of Delta receptor stimulation?

A

Analgesia
Respiratory Depression
Physical dependence
Constipation
Urinary Retention

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15
Q

How common are true opioid allergies?

A

Rare. Most are side effects, including localized histamine release (itching), orthostatic hypotension, and nausea & vomiting

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16
Q

How do opioids affect Minimal Alveoli Concentration requirements of volatile anesthetics?

A

Decreases MAC

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17
Q

Morphine is best for what kind of pain relief?

A

Moderate - Severe
It is better for continuous dull pain rather than sharp intermittent pain. ex: visceral gut/belly pain

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18
Q

What are the different routes of administration for morphine?

A

PO, IM, SC, IV, Epidural, IT

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19
Q

Morphine causes which effect first? And then followed by?

A

Sedation first and then analgesia.
Important to remember that sedation is not an indication of pain control.

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20
Q

Morphine undergoes what kind of metabolism? What is the end product?

A

Undergoes phase 2 glucuronide conjugation. Forms morphine-6-glucuronide -> an active metabolite

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21
Q

Morphine produces histamine release from tissue _____ cells which can cause _____, _______, and _____.

A

Mast Cells

Decreased SVR, Hypotension and Tachycardia

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22
Q

What is the consequence of morphine having an active metabolite?

A

Produces a more prolonged effect, often excessive sedation in renal patients.

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23
Q

What is the Adult Intrathecal (spinal) dosing of morphine?

A

0.1-0.5mg
Typically 0.2-0.25. Higher doses = pruritis

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24
Q

What is the Pediatric Intrathecal (spinal) dosing of morphine?

A

0.01mg/kg

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25
Q

What is the Adult Epidural Bolus Dose and frequency of Morphine?

A

Bolus: 2-6mg every 8-24 hours

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26
Q

What is the Adult Epidural Infusion Dose of Morphine?

A

0.2-1mg/hr

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27
Q

What is the pediatric epidural dosing for morphine? What is the Max dosing?

A

0.03-0.05mg/kg

MAX: 0.1mg/kg or 5mg/24hrs)

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28
Q

What is the adult Sedation/Analgesia IV (IM and SC same) dosing for Morphine?

A

2-20mg every 2-4hours

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29
Q

What is the pediatric Sedation/Analgesia IV dosing for Morphine?

A

IV usually dosed 0.1mg/kg

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30
Q

Is Hydromorphone natural, synthetic, or semisynthetic?

A

Semisynthetic

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31
Q

Hydromorphone has a similar pharmacokinetic profile as _______ but is more potent.

A

Morphine

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32
Q

Why is hydromorphone considered “cleaner” than morphine?

A

No active metabolites. Can be used in renal / elderly.

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33
Q

What are the routes of admin for hydromorphone?

A

PO, Rectal, IV

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34
Q

What is the adult IV analgesic dose for hydromorphone?

A

0.4-2mg IV

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35
Q

What is the pediatric IV analgesic dose for hydromorphone?

A

0.0005-0.02mg/kg IV
(0.5-20mcg/kg)

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36
Q

Is Meperidine natural, synthetic, or semisynthetic?

A

Synthetic

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37
Q

Meperidine has a similar structure to what drug? Why is this significant?

A

Atropine has atropine-like antispasmodic effects (used for shivering)

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38
Q

Meperidine is partially metabolized to?

A

Normeperidine

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39
Q

Normeperidine has _____ the analgesic effect of Meperidine.

A

Half

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40
Q

What does Meperidine do to the CNS?

A

Lowers seizure threshold and induces CNS excitability.

41
Q

What is the adult post-op shivering dose of Meperidine?

A

12.5-25mg IV

12.5 usually adequate

42
Q

A single dose of fentanyl is terminated by?

A

Redistribution, rather than metabolism and excretion.

43
Q

Where does fentanyl have significant first-pass uptake?

A

Lungs with temporary accumulation before release

44
Q

Fentanyl elimination is prolonged in which patients?

A

elderly and neonates

45
Q

Common routes of Fentantl administration?

A

Transdermal
IV, Epidural, and IT

46
Q

What is the adult intubation adjunct dose for Fentanyl?

A

1-3mcg/kg

1mcg/kg most common

47
Q

What is the adult Intrathecal (spinal) dose for Fentanyl?

A

10-25mcg
(0.010-0.025mg)

48
Q

What is the adult epidural dose for Fentanyl? When mixed with a local anesthetic?

A

10-100mcg, or mixed in local anesthetic 10mcg/ml

49
Q

For adult sedation/analgesia, what is the loading and maintenance dosing for Fentanyl?

A

Load: 0.5mcg/kg
Maintenance: 0.01-0.04 mcg/kg/hr

50
Q

How is Remifentanyl metabolized?

A

easily and rapidly by blood and tissue plasma esterases

51
Q

What is the elimination half-life of Remifentanil?

A

8-20minutes
8 minutes more common!

52
Q

What is an adverse possible side effect of Remifentanil?

A

Hyperalgesia

53
Q

Rank the potency of fentanyl, remifentanil, alfentanil, and sufentanil from highest to lowest

A

Sufentanil - most potent
Remi and fentanyl are equal in potency but different in duration of action
Alfentanil - least potent

54
Q

What is the adult induction dose of Remifentanil?

A

1-3mcg/kg over 1 min

55
Q

What are the adult general anesthesia adjunct loading, bolus, and maintenance dosing for Remifentanil?

A

Loading: 0.5-2mcg/kg
Bolus: 0.5-1mcg/kg
Maintenance: 0.05-2mcg/kg/min

56
Q

What can occur when bolusing Remifentanil?

A

Significant Bradycardia!
Skeletal Muscle Rigidity (Stiff Chest Syndrome)
can occur with all fast admin of fents

57
Q

What are sedation doses of remifentanil? both load and maintenance

A

Load over 30-60s: 0.5-1mcg/kg
Maintenance: 0.025-0.2mcg/kg/min

58
Q

Remifentanil has increased respiratory depression when given with?

A

Propofol

59
Q

How does the potency and half-life of Sufentanil compare to Fentanyl?

A

Higher potency (10x more potent) and shorter half-life than fentanyl

60
Q

Does Sufentanil cause the same hyperanalgesia effects as Remifentanil?

A

No.

61
Q

Sufentanil can be adminsiterd via?

A

IV, Epidural, or IT

62
Q

Under General Anesthesia PRN push doses of Sufentanil can be given, what dose range?

A

10-50mcg

63
Q

Depending on the intensity of the procedure under general anesthesia, sufentanil can be administered via infusion. What is the dose range? (hint- large range since it depends in procedure)

A

Anywhere from 0.3mcg/kg/hr - 2.5mcg/kg/hr

64
Q

What is the adult load and infusion sedation dosing for Sufentanil?

A

Load: 0.1-0.5mcg/kg
Infusion: 0.0005-0.01mcg/kg/min

65
Q

What is the epidural dosing for sufentanil with bupivacaine>

A

10-15mcg/10mL of 0.125 bupivacaine

66
Q

What is Methadone primarily used for?

A

Chronic pain, opioid abstinence syndromes, and heroin addiction

67
Q

What leads to Methadone’s long half-life?

A

Extensive protein binding as well as lower intrinsic ability of the liver to metabolize it

68
Q

What is the adult PO dosing of methadone?

A

2.5-10mg PO

69
Q

What is the adult IV, IM, SC dosing for Methadone?

A

2.5-5mg q8-12hrs

70
Q

How do you titrate Methadone?

A

Titrate up q3-5 days

71
Q

Methadone takes ______ time to reach steady state than other opioids

A

Longer

72
Q

Because of the long half-life of methadone, what can occur?

A

Accumulation

73
Q

Oxycodone is how much more potent than oral morphine?

A

twice as potent

74
Q

Adult PO dosing of oxycodone?

A

5-15mg immediate release q4-6h

75
Q

What is the MOA of opioids?

A

Opioid receptor (mu, kappa, and/or delta) agonists. At pre and post-synaptic sites in the central nervous system (brainstem, spinal cord)

76
Q

Mu receptors are principally responsible for what kinds of analgesia?

A

Supraspinal (pain relief mediated by central nervous system (CNS) structures above the spinal cord, primarily in the brainstem, midbrain, and cerebral cortex)
and
Spinal

77
Q

Respiratory depression is characteristic of which opioid receptor activation?

A

Mu

78
Q

Which opioid receptor has less prominent respiratory depression?

A

Kappa receptor

79
Q

Hydrocodone has similar potency and duration of action to oral ____?

A

morphine

80
Q

Dosing of hydrocodone (PO)

A

2.5-10mg q4

81
Q

Morphine 10mg = how much hydrocodone dose

A

5-10mg

82
Q

Codeine is a weak opioid compared to others. 10mg Morphine = how much codeine?

A

morphine 10mg = 120 mg codeine

83
Q

While it is not used as often anymore for its antitussive effects, what dose of codeine has been shown to be effective?

A

15mg

84
Q

Compared to other opioids, codeine is more or less likely to cause respiratory depression?

A

Less

85
Q

Adult PO codeine dose? Max daily dose?

A

15-60mg PO q 4-6

Max 120mg/day

86
Q

Pediatric PO dosing of codeine? Max doses for ages 2-6 and 6-12?

A

1-1.5mg/kg/day divided by q4-6hours

Max Dose Age 2-6 = 30mg/day max

Max Dose Age 6-12 = 60mg/day max

87
Q

What kind of opioid is Buprenorphine?

A

Synthetic Partial Mu Agonist (agonist - anttagonist)

88
Q

Does Naloxone reverse buprenorphine?

A

yes, but difficult due to the high affinity for mu receptor. my need higher or frequent redosing

89
Q

Because partial opioid agonists (agonist-antagonists) have antagonist properties, what can this do to subsequently administer opioid agonists?

A

Can reduce their efficacy

90
Q

What is an advantage to partial opioid agonists?

A

Ability to produce analgesia with limited respiratory depression

91
Q

What is the epidural dosing for Buprenorphine? What realm is this usually used for?

A

300mcg (0.3mg)

Acute pain world (lol) Dr. C’s words

92
Q

What is the intrathecal dosing of Buprenorphine? When is this a usual adjunct?

A

150mcg (0.15mg)

C-Sections - good effect

93
Q

At what dose should Buprenorphine only be given IM

A

doses greater than 0.3mg /dose

94
Q

What is the IV / IM dosing and frequency of buprenorphine?

A

0.3-0.4mg q 6-8 hours
(can repeat initial dose in 30-60 min x1)
Greater doses than 0.3mg should be given IM

95
Q

the dosing of Buprenorphine is equianalgesia to what IV morphine dose?

A

10mg IV morphine equianalgesic to 0.3-0.4 IV/IM buprenorphine

96
Q

Adult dosing of Naloxone for adult opioid overdose? Max dose?

A

0.2-4mg IV q 2-3min PRN

10mg MAX then have to start infusion

97
Q

Adult Naloxone dose for reversal of respiratory depression

A

0.04-0.4mg doses IV 2-3min titrations

98
Q

Treatment of opioid-induced pruritus with Naloxone dose

A

0.25mcg/kg/hr

99
Q

Birth to 5 years or less than 20kg Naloxone dosing?

A

0.1mg.kg IV q2-3min PRN

Anesthesia Pharmacology (5 decks)

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