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Anesthesia Pharm > Opioids > Flashcards

Opioids Flashcards

1
Q

2 opioid structures

A

Phenanthrenes and benzylisoquinolines

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2
Q

Natural opioid

Semisynthetic opioids

A

Natural: morphine
Semi: heroin, dilaudid, codeine

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3
Q

Synthetic opioids

A

Exogenous. Fentanyl, sufentanil, alfentanil

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4
Q

Phenylpiperidines

5

A

Meperidine, fentanyl, alfentanil, sufentanil, remifentanil

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5
Q

What it means to be a partial agonist, example

A

Buprenorphine. Regardless of dose cant produce full mu receptor fx. Safer, less abuse

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6
Q

What it means to be mixed agonist/antagonist and ex

A

Nalbuphine. Agonist at one receptor (kappa) antagonist at mu, reverses resp depression

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7
Q

All endogenous and exogenous agonists act where

A

Mu receptors

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8
Q

Mu 1 receptor

5 main effects

A

Analgesia, euphoria, miosis, bradycardia, urinary ret

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9
Q

Mu 1
Where it primarily acts
What works here

A

Supraspinal, spinal to lesser degree.

All endogenous and synthetic agonists

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10
Q

Mu 2 receptor
3 main effects
Where it primarily works
What works here

A

Hypoventilation, phys dependence, constipation. Spinal. Endog/exog agonists

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11
Q

Kappa receptor
Where they are
Only what works here

A

Supraspinal and spinal

Dynorphins

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12
Q

Kappa receptor

4 main effects

A

Dysphagia, sedation, miosis, diuresis

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13
Q

Delta receptor
Where they are
What works here

A

Supraspinal and spinal

Enkephalins

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14
Q

Delta receptor

4 Main effects

A

Hypoventilation, phys dependence, constipation (minimal), and urinary retention

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15
Q

Opioid MOA

Net effect

A

Inc K conductance, ca ch inactivation, both decrease NT release

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16
Q

Opioid MOA

Activation of receptors does what

A

Decreases neurotransmission or inhib release of excitatory NTs

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17
Q

What affects onset of opioids

A

Higher % unionized, higher % unbound. Both = faster onset

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18
Q

Opioids: what pH, what part works

A

Weak base. Only unionized and unbound can diffuse from blood to tissues

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19
Q

Alfentanil vs morphine onset

A

Alf- 98% unionized, rapid onset

Morph- 23% unionized, slower onset

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20
Q

Neonate vs elderly in opioid dynamics

A

Neonate- dec elim d/t immature cyp 450. Elderly have greater brain sensitivity to drug

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21
Q

How to dose opioids, how not to

A

Based on ideal body weight (lean body mass) not actual weight in kg

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22
Q

Spinal analgesic effects produced by what

A

Receptor activation in SC and DRG

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23
Q

Supraspinal analgesia produced by what

A

Receptor activ in periaqueductal gray matter in brain

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24
Q

CNS effects of opioids

A

Analgesia, euphoria, sleep, resp dep, miosis, nausea, modest dec ICP, dec CBF

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25
Q

CNS effects
How nausea is produced
Doesnt do what 2 things

A

Chemoreceptor trigger zone

Amnesia or anesthesia

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26
Q

Advantages Of opioids in neuro anesthesia

A

Hemodynamic and cerebrovascular stability

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27
Q

CV effects

A

Doesnt impair function. Bradycardia (dose dep), dec co and bp, vasodilation

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28
Q

CV effects specific to meperidine

A

Tachycardia and myocardial depression

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29
Q

Vent effects

A

Resp dep (dose dep), dec chest wall compliance, constriction of pharyngeal/laryngeal muscles, hypercarbia, hypoxia

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30
Q

Bad effects on resp sys
Low dose
High dose

A

Low- dec rr, inc vt

Hi- dec rr and vt

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31
Q

Bad effects resp sys

A

Dec hypoxic vent drive and vent response curve reduced and shifted right

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32
Q

Resp depression onset and duration: morphine vs fentanyl

A

Onset slower for morphine and lasts longer than fentanyl

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33
Q

Factors that inc magnitude and duration of opioid resp depression: 8

A

Inc dose, bolus v gtt, speed of injec, admin of other anesthetics, dec clearance, age, alkalosis, reuptake from muscle/fat/lung tissue/intestine

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34
Q

Skeletal muscle effects

A

Rigidity (laryngeal, inhib of gaba, inc in dopamine). Can make vent difficult

35
Q

Renal/gi/liver effects

A

Urgency GU, block catecholamine release and cortisol, sphincter of oddi spasm, constipation, prolonged gastric emptying

36
Q

Opioids in epidural space undergo uptake into where

A

Fat, systemic absorption, diffusion into CSF

37
Q

Penetration into CSF depends on what

A

Lipid soluble. More soluble= quicker peak concentration

38
Q

How lipid solubility affects movement in CSF

A

Highly= limited migration d/t SC uptake

Less soluble= remains in CSF for cephalic transfer

39
Q

How lipid solubility affects vascular absorption of opioids in neuraxial anesthesia

A

More lipid soluble- quicker peak in blood.

40
Q

SE neuraxial opioids

4

A

Pruritis most common, NV, urine retention, vent depression (faster w lipophilic)

41
Q

Morphine

Solubility, binding, ionization

A

Poor lipid solubility, high protein binding. Highly ionized

42
Q

Morphine

Effects 8

A

Analgesia, sedation, euphoria, nausea, pruritis, dry mouth. Vent depression

43
Q

Morphine
IM and IV peak
DOA

A

IM- 45 min. IV- 15-30 min

DOA- 4 hrs

44
Q

Morphine

How bradycardia caused, other CV effect

A

Stim vagus directly, inhib SA node

45
Q

Morphine
Metab by what
Metabolite and potency

A

Liver. Active morphine 6 glucuronide, more potent than morphine sulfate

46
Q

Morphine

Metabolism: other role and affected by what

A

Kidneys do extrahepatic metab. Renal failure will impact d/t metabolite

47
Q

Meperidine
Structural similarity to what
___ effects

A

Atropine and LA (blocks Na ch). Muscarinic.

48
Q

Meperidine
Potent at which receptors
DOA

A

A2

2-4 hrs

49
Q

Meperidine

Effects, similarity to

A

Euphoria, sedation, analgesia, same amt as morphine

50
Q

What is normeperidine

A

Active metabolite. Lasts 3 days, 1/2 as potent. Seizures reported

51
Q

Meperidine
Used postop for what
Potency compared to morphine

A

Shivering (kappa and A2 receptors). 1/10th as potent as morphine

52
Q

Hydromorphone
Potency and effects compared to morphine
Dosing

A

5x more potent, more sedation but less euphoria than morphine. Rapid elim, q4 dosing

53
Q

Fentanyl

Comparison to morphine: solubility, duration, potency

A

More lipid soluble, shorter duration, 100x more potent

54
Q

Fentanyl

Where its taken up

A

75% 1st pass pulmonary uptake. Also fat, muscle

55
Q

Fentanyl
Dose for bolus
Dose for lollipop, when

A

1-20 mcg/kg

5-20 mcg/kg 45 min before induction

56
Q

Sufentanil

Comparison to fentanyl and to morphine

A

2x as lipid soluble and 10x more potent than fent. 1,000x more potent than morphine

57
Q

Sufentanil
Binding
Metabolism

A

Highly protein bound. Pulm 1st pass. Metab in liver. Weak active metabolite desmethylsufentanil

58
Q

Clinical use of sufentanil

A

Quicker induction and earlier emergence/extubation than morphine and fent. Good for output surgery

59
Q

Alfentanil

Onset, binding

A

Fast onset, 90% unionized, 1.4 min. Highly protein bound

60
Q

Alfentanil

Comparison to fentanyl and morphine

A

Even tho more protein bound, higher diffusable fraction than fentanyl. 1/5 as potent as fentanyl. 10-20x more potent than morphine

61
Q

Alfentanil

Useful for what

A

Rapid onset to blunt hemodynamic response to pain. Outpt surgery

62
Q

Remifentanil

Metabolism, onset, duration

A

Metab by tissue/plasma esterases. Fast onset/duration, smal Vd

63
Q

Remifentanil

Potency compared to fent and morphine

A

Sim to fent, 100x more than morphine

64
Q

Remifentanil

Clinical use

A

Blunts pain. Use gtt for interm-long surgeries when rapid recovery needed. Neuro or O/P

65
Q

Agonist/antagonist

Where receptor effects are, use, may cause what

A

Mu antagonist/partial agonist, partial agonist at kappa. Ltd vent dep, low dependence chance. Dysphoria possible.

66
Q

Nalbuphine

Works where, how, class

A

Agonist antagonist. Kappa and sigma receptors. Antagonizes resp dep but maintains analgesia. Reverses oddi spasm.

67
Q

Butorphenol

Class, acts where, analgesia

A

Agonist at kappa, antagonist or partial agonist at mu. 5x > potent than morphine. Nasal for migraines

68
Q

Naloxone

Class, where it acts

A

Opioid antagonist at mu, kappa, and delta

69
Q

Naloxone

Duration, onset

A

Less than most opioids, 1-2 min

70
Q

Naloxone

Adverse effects

A

Tachycardia, htn, dysrhythmias, pain, pulm edema (cv disease pts or healthy)

71
Q

Demerol dose

A

50-100 mg IV

72
Q

Fentanyl dose

A

1-3 mcg/kg

73
Q

Remifentanil dose

A

1-2 mcg/kg

74
Q

Alfentanil dose

75
Q

Sufentanil dose

A

0.1-0.3 mcg/kg

76
Q

Gtt for fent

A

.01-.05 mcg/kg/min

77
Q

Gtt for sufentanil

A

0.0015-0.01 mcg/kg/min

78
Q

Gtt for alfentanil

A

.25-.75 mcg/kg/min

79
Q

Gtt for remifentanil

A

0.05-.25 mcg/kg/min

80
Q

Alfentanil: loading dose, bolus

A

25-100 mcg/kg

5-10 mcg/kg

81
Q

Sufentanil
Loading dose
Bolus

A
  1. 25-2 mcg/kg

2. 5-10 mcg

82
Q

Fentanyl
Loading dose
Bolus

A

4-20 mcg/kg

25-100 mcg

83
Q

Remifentanil
Loading dose
Bolus

A

1-2 mcg/kg

.1-1 mcg/kg

84
Q

Potency of opioids

A

Sufent > remifent > fent > alfent > dilaudid > mso4 > demerol

Anesthesia Pharm (12 decks)

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