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Pharmacology 1 > Opioid Dosages > Flashcards

Opioid Dosages Flashcards

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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
Methadone Onset:
15 min
26
Methadone Duration of action:
4-6 hr
27
Methadone PB:
95%
28
Methadone elimination half time:
24 hr
29
Methadone Metabolism:
CYP3A4, 2B6 really excreted
30
Methadone IV dose:
2.5-10 mg Q24hr
31
Methadone side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
32
Methadone Contraindications / cautions
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
33
Hydromorphone (alternate name)
Dilaudid
34
Hydromorphone structure:
morphone derivative
35
Hydromorphone potency:
10x as strong as morphine
36
Hydromorphone MOA:
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)
37
Hydromorphone Onset:
15 min
38
Hydromorphone Duration of action:
2-4 hr
39
Hydromorphone PB:
30%
40
Hydromorphone metabolism:
by liver (glucuronidation) into inactive metabolites and excreted by kidney and bile
41
Hydromorphone IV intra-op dose:
IV: 0.01-0.02 mg/kg intra-op
42
Hydromorphone IV post-op pain dose:
IV: 0.1-0.25 mg Q 10-15 min post-op
43
Hydromorphone side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
44
Hydromorphone Contraindications / cautions:
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
Fentanyl (alternate name)
sublimaze
46
Fentanyl structure:
Phenylpiperidine
47
Fentanyl potency
100x more potent than morphine
48
Fentanyl MOA:
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
Fentanyl Onset:
1-2 min
50
Fentanyl Duration of action:
30-60 min
51
Fentanyl PB:
75%
52
Fentanyl metabolism:
CYP3A4, Renal, bile
53
Fentanyl IV analgesia dose:
IV: 1-2 mcg/kg - analgesia
54
Fentanyl IV surgical stimulation dose:
IV 1.5-3 mcg/kg - surgical stimulation
55
Fentanyl side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
56
Fentanyl contraindications / cautions:
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
Alfentanil (alternate name)
Alfenta
58
Alfentanil structure:
phenylpiperidine
59
Alfentanil potency:
15x more potent than morpine
60
Alfentanil MOA:
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
Alfentanil Onset:
1-2 min
62
Alfentanil duration of action:
30-60 min
63
Alfentanil PB:
95%
64
Alfentanil metabolism:
CYP3A4 - excreted by kidneys
65
Alfentanil IV dose:
IV: 15 mcg/kg
66
Alfentanil IV for unconscious state dose:
IV: 150-300 mcg/kg (for unconscious state)
67
Alfentanil side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
68
Alfentanil contraindications / cautions:
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
Remifentanil (alternate name):
Ultiva
70
Remifentanil structure:
phenylpiperidine
71
Remifentanil potency:
300x as potent as morphine
72
Remifentanil MOA:
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
Remifentanil onset:
1-2 min
74
Remifentanil duration of action:
5-10 min
75
Remifentanil PB:
75%
76
Remifentanil metabolism:
plasma esterases, Renal
77
Remifentanil IV push dose:
IV: 0.5-1 mcg/kg (over 60-90 seconds) (Ideal body weight)
78
Remifentanil IV drip maintenance dose:
IV: 0.05-2 mcg/kg/min (ideal body weight)
79
Remifentanil side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
80
Remifentanil Contraindications / cautions:
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
Sufentanil (alternate name)
Sufenta
82
Sufentanil structure:
Phenylpiperidine
83
Sufentanil potency:
1000x as potent as morphine
84
Sufentanil MOA:
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
Sufentanil onset:
1-2 min
86
Sufentanil duration of action:
30-60 min
87
Sufentanil PB:
95%
88
Sufentanil Metabolism
CYP3A4
89
Sufentanil IV dose:
IV: 0.1-0.4 mcg/kg
90
Sufentanil side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
91
Sufentanil contraindications / cautions
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
Nalbuphine (alternate name)
nubain
93
Nalbuphine structure:
Opioid related chemically to oxymorphone and naloxone
94
Nalbuphine MOA:
Kappa agonist Mu antagonist
95
Nalbuphine onset:
1-2 min
96
Nalbuphine duration of action:
4-6 hr
97
Nalbuphine PB:
50%
98
Nalbuphine metabolism:
Glucuronidation
99
Nalbuphine IV dose:
IV: 0.3-3 mg/kg (over 10-15 min)
100
Nalbuphine IV maintenance dose (weight based):
0.25-0.5 mg/kg PRN
101
Nalbuphine side effects (same for all narcotics):
1. R - Respiratory depression 2. A - Allergic reaction possible 3. N - Nausea/vomiting 4. C - Constipation 5. H - Hypotension
102
Nalbuphine contraindications / cautions:
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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