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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
CNS effects How nausea is produced Doesnt do what 2 things
Chemoreceptor trigger zone | Amnesia or anesthesia
26
Advantages Of opioids in neuro anesthesia
Hemodynamic and cerebrovascular stability
27
CV effects
Doesnt impair function. Bradycardia (dose dep), dec co and bp, vasodilation
28
CV effects specific to meperidine
Tachycardia and myocardial depression
29
Vent effects
Resp dep (dose dep), dec chest wall compliance, constriction of pharyngeal/laryngeal muscles, hypercarbia, hypoxia
30
Bad effects on resp sys Low dose High dose
Low- dec rr, inc vt | Hi- dec rr and vt
31
Bad effects resp sys
Dec hypoxic vent drive and vent response curve reduced and shifted right
32
Resp depression onset and duration: morphine vs fentanyl
Onset slower for morphine and lasts longer than fentanyl
33
Factors that inc magnitude and duration of opioid resp depression: 8
Inc dose, bolus v gtt, speed of injec, admin of other anesthetics, dec clearance, age, alkalosis, reuptake from muscle/fat/lung tissue/intestine
34
Skeletal muscle effects
Rigidity (laryngeal, inhib of gaba, inc in dopamine). Can make vent difficult
35
Renal/gi/liver effects
Urgency GU, block catecholamine release and cortisol, sphincter of oddi spasm, constipation, prolonged gastric emptying
36
Opioids in epidural space undergo uptake into where
Fat, systemic absorption, diffusion into CSF
37
Penetration into CSF depends on what
Lipid soluble. More soluble= quicker peak concentration
38
How lipid solubility affects movement in CSF
Highly= limited migration d/t SC uptake | Less soluble= remains in CSF for cephalic transfer
39
How lipid solubility affects vascular absorption of opioids in neuraxial anesthesia
More lipid soluble- quicker peak in blood.
40
SE neuraxial opioids | 4
Pruritis most common, NV, urine retention, vent depression (faster w lipophilic)
41
Morphine | Solubility, binding, ionization
Poor lipid solubility, high protein binding. Highly ionized
42
Morphine | Effects 8
Analgesia, sedation, euphoria, nausea, pruritis, dry mouth. Vent depression
43
Morphine IM and IV peak DOA
IM- 45 min. IV- 15-30 min | DOA- 4 hrs
44
Morphine | How bradycardia caused, other CV effect
Stim vagus directly, inhib SA node
45
Morphine Metab by what Metabolite and potency
Liver. Active morphine 6 glucuronide, more potent than morphine sulfate
46
Morphine | Metabolism: other role and affected by what
Kidneys do extrahepatic metab. Renal failure will impact d/t metabolite
47
Meperidine Structural similarity to what ___ effects
Atropine and LA (blocks Na ch). Muscarinic.
48
Meperidine Potent at which receptors DOA
A2 | 2-4 hrs
49
Meperidine | Effects, similarity to
Euphoria, sedation, analgesia, same amt as morphine
50
What is normeperidine
Active metabolite. Lasts 3 days, 1/2 as potent. Seizures reported
51
Meperidine Used postop for what Potency compared to morphine
Shivering (kappa and A2 receptors). 1/10th as potent as morphine
52
Hydromorphone Potency and effects compared to morphine Dosing
5x more potent, more sedation but less euphoria than morphine. Rapid elim, q4 dosing
53
Fentanyl | Comparison to morphine: solubility, duration, potency
More lipid soluble, shorter duration, 100x more potent
54
Fentanyl | Where its taken up
75% 1st pass pulmonary uptake. Also fat, muscle
55
Fentanyl Dose for bolus Dose for lollipop, when
1-20 mcg/kg | 5-20 mcg/kg 45 min before induction
56
Sufentanil | Comparison to fentanyl and to morphine
2x as lipid soluble and 10x more potent than fent. 1,000x more potent than morphine
57
Sufentanil Binding Metabolism
Highly protein bound. Pulm 1st pass. Metab in liver. Weak active metabolite desmethylsufentanil
58
Clinical use of sufentanil
Quicker induction and earlier emergence/extubation than morphine and fent. Good for output surgery
59
Alfentanil | Onset, binding
Fast onset, 90% unionized, 1.4 min. Highly protein bound
60
Alfentanil | Comparison to fentanyl and morphine
Even tho more protein bound, higher diffusable fraction than fentanyl. 1/5 as potent as fentanyl. 10-20x more potent than morphine
61
Alfentanil | Useful for what
Rapid onset to blunt hemodynamic response to pain. Outpt surgery
62
Remifentanil | Metabolism, onset, duration
Metab by tissue/plasma esterases. Fast onset/duration, smal Vd
63
Remifentanil | Potency compared to fent and morphine
Sim to fent, 100x more than morphine
64
Remifentanil | Clinical use
Blunts pain. Use gtt for interm-long surgeries when rapid recovery needed. Neuro or O/P
65
Agonist/antagonist | Where receptor effects are, use, may cause what
Mu antagonist/partial agonist, partial agonist at kappa. Ltd vent dep, low dependence chance. Dysphoria possible.
66
Nalbuphine | Works where, how, class
Agonist antagonist. Kappa and sigma receptors. Antagonizes resp dep but maintains analgesia. Reverses oddi spasm.
67
Butorphenol | Class, acts where, analgesia
Agonist at kappa, antagonist or partial agonist at mu. 5x > potent than morphine. Nasal for migraines
68
Naloxone | Class, where it acts
Opioid antagonist at mu, kappa, and delta
69
Naloxone | Duration, onset
Less than most opioids, 1-2 min
70
Naloxone | Adverse effects
Tachycardia, htn, dysrhythmias, pain, pulm edema (cv disease pts or healthy)
71
Demerol dose
50-100 mg IV
72
Fentanyl dose
1-3 mcg/kg
73
Remifentanil dose
1-2 mcg/kg
74
Alfentanil dose
10-20
75
Sufentanil dose
0.1-0.3 mcg/kg
76
Gtt for fent
.01-.05 mcg/kg/min
77
Gtt for sufentanil
0.0015-0.01 mcg/kg/min
78
Gtt for alfentanil
.25-.75 mcg/kg/min
79
Gtt for remifentanil
0.05-.25 mcg/kg/min
80
Alfentanil: loading dose, bolus
25-100 mcg/kg | 5-10 mcg/kg
81
Sufentanil Loading dose Bolus
0. 25-2 mcg/kg | 2. 5-10 mcg
82
Fentanyl Loading dose Bolus
4-20 mcg/kg | 25-100 mcg
83
Remifentanil Loading dose Bolus
1-2 mcg/kg | .1-1 mcg/kg
84
Potency of opioids
Sufent > remifent > fent > alfent > dilaudid > mso4 > demerol

Anesthesia Pharm (12 decks)

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