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Pharmacology 1 > Opioid Dosages > Flashcards

Opioid Dosages Flashcards

1
Q

Morphine (alternate name):

A

Duramorph

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2
Q

Morphine structure:

A

Phenathrene derivative of opium

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3
Q

Morphine MOA:

A
  1. Mu, Kappa, Delta agonist
  2. Inhibit (GPCR -Gi) release of excitatory neurotransmitters Ach, NE, Dopamine, Substance P at presynaptic neurons (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
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4
Q

Morphine Onset:

A

15 min

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5
Q

Morphine Duration of action:

A

2-4 h

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6
Q

Morphine PB:

A

30%

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7
Q

Morphine metabolism:

A

Hepatic (glucuronidation)
Renal excretion

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8
Q

Morphine IV dose:

A

0.05-0.3 mg/kg
(usually 0.1 mg/kg)

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9
Q

Morphine side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
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10
Q

Morphine Contradindications / Cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - Serotonin syndrome (with MAOI, don’t give if MAOI taken within 14 days)
  5. S - Sphincter of Odds spasm (consider biliary disease or acute pancreatitis)
  6. H - Histamine Release
  7. P - Pruritus (itching)
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11
Q

Meperidine (alternate name):

A

Demerol

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12
Q

Meperidine structure:

A

Phenylpiperidine

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13
Q

Meperidine potency:

A

0.1x morphine potency

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14
Q

Meperidine MOA:

A
  1. Mu, Kappa, Delta agonist
  2. Inhibit (GPCR -Gi) release of excitatory neurotransmitters Ach, NE, Dopamine, Substance P at presynaptic neurons (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
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15
Q

Meperidine Onset:

A

5 min

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16
Q

Meperidine Duration of action:

A

2-4 h

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17
Q

Meperidine Protein Binding:

A

75%

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18
Q

Meperidine metabolism:

A

CYP3A4 (demethylation) to normeperidine,
Renally excreted

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19
Q

Meperidine IV dose:

A

IV: 25-100 mg
IV: 50mg Q 3-4 hr for pain or shivering

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20
Q

Meperidine side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
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21
Q

Meperidine Contraindications / Cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - Serotonin syndrome (with MAOI, don’t give if MAOI taken within 14 days)
  5. S - Sphincter of Odds spasm (consider biliary disease or acute pancreatitis)
  6. H - Histamine Release
  7. P - Pruritus (itching)
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22
Q

Methadone (alternate name):

A

dolophine

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23
Q

Methadone structure:

A

Synthetic opioid agonist
Racemic mixture

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24
Q

Methadone MOA:

A
  1. Mu agonist
  2. Inhibit (GPCR -Gi) the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. NMDA antagonist – inhibits serotonin and NE uptake
  5. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  6. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
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25
Q

Methadone Onset:

A

15 min

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26
Q

Methadone Duration of action:

A

4-6 hr

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27
Q

Methadone PB:

A

95%

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28
Q

Methadone elimination half time:

A

24 hr

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29
Q

Methadone Metabolism:

A

CYP3A4, 2B6
really excreted

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30
Q

Methadone IV dose:

A

2.5-10 mg Q24hr

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31
Q

Methadone side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
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32
Q

Methadone Contraindications / cautions

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - Serotonin syndrome (with MAOI, don’t give if MAOI taken within 14 days)
  5. S - Sphincter of Odds spasm (consider biliary disease or acute pancreatitis)
  6. H - Histamine Release
  7. P - Pruritus (itching)
    *8. QT Prolongation
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33
Q

Hydromorphone (alternate name)

A

Dilaudid

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34
Q

Hydromorphone structure:

A

morphone derivative

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35
Q

Hydromorphone potency:

A

10x as strong as morphine

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36
Q

Hydromorphone MOA:

A
  1. Mu agonist
  2. Inhibit (GPCR -Gi) the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
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37
Q

Hydromorphone Onset:

A

15 min

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38
Q

Hydromorphone Duration of action:

A

2-4 hr

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39
Q

Hydromorphone PB:

A

30%

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40
Q

Hydromorphone metabolism:

A

by liver (glucuronidation) into inactive metabolites and excreted by kidney and bile

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41
Q

Hydromorphone IV intra-op dose:

A

IV: 0.01-0.02 mg/kg intra-op

42
Q

Hydromorphone IV post-op pain dose:

A

IV: 0.1-0.25 mg Q 10-15 min post-op

43
Q

Hydromorphone side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
44
Q

Hydromorphone Contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - Serotonin syndrome (with MAOI, don’t give if MAOI taken within 14 days)
  5. S - Sphincter of Odds spasm (consider biliary disease or acute pancreatitis)
  6. H - Histamine Release
  7. P - Pruritus (itching)
45
Q

Fentanyl (alternate name)

46
Q

Fentanyl structure:

A

Phenylpiperidine

47
Q

Fentanyl potency

A

100x more potent than morphine

48
Q

Fentanyl MOA:

A
  1. Mu agonist
  2. Inhibit (GPCR -Gi) the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)5. Inhibition of adenylate cyclase
49
Q

Fentanyl Onset:

50
Q

Fentanyl Duration of action:

51
Q

Fentanyl PB:

52
Q

Fentanyl metabolism:

A

CYP3A4, Renal, bile

53
Q

Fentanyl IV analgesia dose:

A

IV: 1-2 mcg/kg - analgesia

54
Q

Fentanyl IV surgical stimulation dose:

A

IV 1.5-3 mcg/kg - surgical stimulation

55
Q

Fentanyl side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
56
Q

Fentanyl contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. *S - Serotonin Syndrome (pt on MAOIs, SSRIs, SNRIs, tricyclics, 5-HT3 antagonists?)
  5. S - Sphincter of Oddi spasm (consider biliary disease or acute pancreatitis)
  6. S - Skeletal muscle rigidity
  7. B - Bradycardia
57
Q

Alfentanil (alternate name)

58
Q

Alfentanil structure:

A

phenylpiperidine

59
Q

Alfentanil potency:

A

15x more potent than morpine

60
Q

Alfentanil MOA:

A
  1. Mu agonist
  2. Inhibit the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
61
Q

Alfentanil Onset:

62
Q

Alfentanil duration of action:

63
Q

Alfentanil PB:

64
Q

Alfentanil metabolism:

A

CYP3A4 - excreted by kidneys

65
Q

Alfentanil IV dose:

A

IV: 15 mcg/kg

66
Q

Alfentanil IV for unconscious state dose:

A

IV: 150-300 mcg/kg (for unconscious state)

67
Q

Alfentanil side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
68
Q

Alfentanil contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - 1. Serotonin Syndrome (pt on MAOIs?)
  5. S - Sphincter of Oddi spasm (consider biliary disease or acute pancreatitis)
  6. S - Skeletal muscle rigidity
  7. B - Bradycardia
69
Q

Remifentanil (alternate name):

70
Q

Remifentanil structure:

A

phenylpiperidine

71
Q

Remifentanil potency:

A

300x as potent as morphine

72
Q

Remifentanil MOA:

A
  1. Mu agonist
  2. Inhibit (GPCR -Gi) the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
73
Q

Remifentanil onset:

74
Q

Remifentanil duration of action:

75
Q

Remifentanil PB:

76
Q

Remifentanil metabolism:

A

plasma esterases, Renal

77
Q

Remifentanil IV push dose:

A

IV: 0.5-1 mcg/kg (over 60-90 seconds) (Ideal body weight)

78
Q

Remifentanil IV drip maintenance dose:

A

IV: 0.05-2 mcg/kg/min (ideal body weight)

79
Q

Remifentanil side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
80
Q

Remifentanil Contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - 1. Serotonin Syndrome (pt on MAOIs?)
  5. S - Sphincter of Oddi spasm (consider biliary disease or acute pancreatitis)
  6. S - Skeletal muscle rigidity
  7. B - Bradycardia
81
Q

Sufentanil (alternate name)

82
Q

Sufentanil structure:

A

Phenylpiperidine

83
Q

Sufentanil potency:

A

1000x as potent as morphine

84
Q

Sufentanil MOA:

A
  1. Mu agonist
  2. Inhibit (GPCR -Gi) the release of excitatory neurotransmitters Ach, NE, dopamine, glutamate, and substance P (pre-synaptic Ca channel inactivation)
  3. Increase post-synaptic K conductance (hyperpolarizes)
  4. Inhibits adenylate cyclase by activating GI proteins and subsequently reduces cAMP, decreasing neuronal excitability
  5. Upregulation of adenylate cyclase can lead to withdrawal symptoms if drug/inhibition is removed (chronic use)
85
Q

Sufentanil onset:

86
Q

Sufentanil duration of action:

87
Q

Sufentanil PB:

88
Q

Sufentanil Metabolism

89
Q

Sufentanil IV dose:

A

IV: 0.1-0.4 mcg/kg

90
Q

Sufentanil side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
91
Q

Sufentanil contraindications / cautions

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - 1. Serotonin Syndrome (pt on MAOIs?)
  5. S - Sphincter of Oddi spasm (consider biliary disease or acute pancreatitis)
  6. S - Skeletal muscle rigidity
  7. B - Bradycardia
92
Q

Nalbuphine (alternate name)

93
Q

Nalbuphine structure:

A

Opioid related chemically to oxymorphone and naloxone

94
Q

Nalbuphine MOA:

A

Kappa agonist
Mu antagonist

95
Q

Nalbuphine onset:

96
Q

Nalbuphine duration of action:

97
Q

Nalbuphine PB:

98
Q

Nalbuphine metabolism:

A

Glucuronidation

99
Q

Nalbuphine IV dose:

A

IV: 0.3-3 mg/kg (over 10-15 min)

100
Q

Nalbuphine IV maintenance dose (weight based):

A

0.25-0.5 mg/kg PRN

101
Q

Nalbuphine side effects (same for all narcotics):

A
  1. R - Respiratory depression
  2. A - Allergic reaction possible
  3. N - Nausea/vomiting
  4. C - Constipation
  5. H - Hypotension
102
Q

Nalbuphine contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. S - 1. Serotonin Syndrome (pt on MAOIs?)
  5. S - Sphincter of Oddi spasm (consider biliary disease or acute pancreatitis)
  6. S - Skeletal muscle rigidity
  7. B - Bradycardia
    *8. Ceiling effect 30mg

Pharmacology 1 (12 decks)

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