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NURA-661-01 Anesthesia Pharm > Opioids > Flashcards

Opioids Flashcards

Dont Suck!

1
Q

▪ Opiate is the term used to designate drugs derived from ______
▪ Opioid refers to all substances, natural and synthetic, that bind to opioid receptors and produce an ______ effect

A

opium

agonist

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2
Q

Structure:

A

 Phenanthrenes

 Benzylisoquinolines

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3
Q 
Opioid Classification:
Naturally occurring =  
Semisynthetic: Analogs of \_\_\_\_\_\_\_ =  
Synthetic: Exogenous (_ groups) = 
- synthetic manufactured by \_\_\_\_\_\_\_\_\_
A

morphine

morphine, Heroin, Hydromorphone, Codeine

4, Morphinan derivatives, Diphenyl derivatives, Benzomorphans, Phenylpiperidines, synthesis

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4
Q

Synthetic Opioids (exogenous):

  1. Morphinan derivatives =
  2. Diphenyl derivatives =
  3. Benzomorphans =
  4. Phenylpiperidines =
A

Levorphenol, butorphenol
Methadone
Phenazocine, Pentazocine
Meperidine, Fentanyl, Alfentanil, Sufentanil, Remifentanil

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5
Q

Opioid Classifications =

A

Agonist
Partial agonist
Mixed agonist/antagonist
Antagonist

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6
Q

Partial agonist example =

A

buprenorphine: regardless of the dose the cannot produce full mu receptor effects like morphine

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7
Q

Mixed agonist/antagonist example =

A

nalbuphine: agonist at one receptor, kappa

and antagonist at mu, reversing resp depression

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8
Q

Antagonist example =

A

naloxone

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9
Q

Opiate Receptors
1973: researchers describe the presence of receptors
Hypothesize endogenous substances stimulated these receptors
1975: 3 endogenous agonists were identified which are…..

A

enkephalins, endorphins and dynorphins

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10
Q

Opioid Receptors
1980’s: existence of opioid receptor
Receptors: __, ____, and ____
Believed that synthetic opioids ______ action of endogenous opioids by binding to ____________
Activating pain modulating systems: ? and ?

A

mu, kappa, and delta
mimic
opioid receptors
Antinociceptive, inhibiting excitatory neurotransmitters ie. substance P

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11
Q

Mu receptors are primarily in ? and ?
Subtypes =
w/ ____ receptors thought to be involved in immune process
All ? and ? agonists act on mu receptors

A

brain and spinal cord
mu-1 and mu-2
Mu-3
endogenous and exogenous

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12
Q

Mu-1 receptor stimulates……

All ? and ? opioid agonists act on these receptors

A

 Analgesia
 Euphoria (feeling of excitement or happiness)
 Supraspinal (to a lesser degree spinal) analgesia
 Miosis - small pupil
 Bradycardia
 Urinary retention

endogenous and synthetic

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13
Q

Mu-2 receptor stimulates……

All ? and ? agonists act on these receptors

A

 Hypoventilation
 Physical dependence
 Spinal analgesia
 Constipation (marked)

endogenous and exogenous

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14
Q

Kappa receptor stimulates……

Only ? act on these receptors

A 
 Supraspinal and spinal analgesia 
 Dysphoria (feeling uneasy, unhappy or unwell)
 Sedation 
 Miosis - small pupil
 Diuresis

Only dynorphins act on these receptors

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15
Q

Delta receptor stimulates……

Only ? act on these receptors

A 
 Supraspinal and spinal analgesia 
 Hypoventilation 
 Physical DEPENDENCE! 
 Constipation (minimal) 
 Urinary retention
Only enkephalins act on these receptors
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16
Q

SLIDE 15 = TABLE 7-2

A

SLIDE 15 = TABLE 7-2

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17
Q

Mechanism of Action: ALSO KNOW SLIDE 16
 Net effect =
 Decrease in ? release
 Activation of receptors either:
1. directly decreases ?
or
2. ? the release of excitatory neurotransmitters (ie ?)

A

Increased potassium conductance, Calcium channel inactivation, Both

neurotransmitter

neurotransmission
inhibits, Substance P

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18
Q

Pharmacokinetic Features Onset of Action:
 Weak ______
 Only ? & ? opioids can diffuse from blood to target tissue thus…
▪ ______ % unionized the higher diffusible fraction and the faster the onset
▪ ______ % unbound the faster the onset

A

bases
unionized & unbound
Higher
Higher

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19
Q

Do we give an acidotic pt an increased or decreased dose?

A

increased

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20
Q

Example Pharmacokinetics and onset of Action:
Alfentanil has ? % unionized (__%) at pH 7.4
- This results in a ? onset of action
Morphine has ? onset of action
- Why? Because its % unionized at physiologic pH is only __%

A

high, 89
very rapid

slower
23

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21
Q

Slide 20 Table 7-4 =

A 
pK = know generally
%non-ionized = know
% protein bound = know
Elimination t1/2 = know
Sufentanil = understand uniqueness!!!
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22
Q

Factors Altering Pharmacokinetics & dynamics of Opioids:
 ___
 _________ show decrease rate of elimination d/t immature cyp P450
 ______ show greater brain sensitivity to the drug
 Weight- dose based on ____________________ in kg
 ______ failure
 ______ failure

A 
Age
Neonates
Elderly
lean (ideal) body mass not actual weight
Renal
Hepatic
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23
Q

Spinal Analgesia vs. Supraspinal Analgesia:
 Spinal analgesic effects produced by receptor activation in __________ and ______________
**specifically in the __________________: Direct stimulation of these receptors produces intense analgesia from inhibition of ____________ release

 Supraspinal analgesia produced by receptor activation in ______________________________

A

spinal cord and dorsal root ganglian, substantia gelatenosa, substance P
periaquaductal/periventricular gray matter in brain

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24
Q

Perioperative Central Nervous System Effects:

A 
 Analgesia 
 Euphoria 
 Drowsiness/sleep 
 Respiratory depression 
 Miosis 
 Nausea- chemoreceptor trigger zone 
 *Does not produce amnesia or anesthesia
 Modest decrease in ICP 
 Decrease CBF 
 Hemodynamic stability 
 Cerebrovascular stability
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25
Q

Advantages of opioids in neuroanesthesia:

A

Hemodynamic stability

Cerebrovascular stability

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26
Q 
Perioperative Cardiovascular Effects: 
 No impairment in CV \_\_\_\_\_\_\_\_\_ 
 Dose dependent \_\_\_\_\_\_\_\_\_\_\_ 
 Tachycardia with \_\_\_\_\_\_\_\_\_\_\_ 
 Myocardial depression with \_\_\_\_\_\_\_\_\_\_\_ 
 Decrease \_\_ and \_\_ 
 Vaso\_\_\_\_\_\_\_\_
****CV depression when MSO4 combined with \_\_\_, NOT occur when MSO4 given alone
A 
function 
bradycardia 
meperidine 
meperidine 
Decrease CO and BP 
Vasodilation
N2O
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27
Q 
Perioperative Ventilatory Effects:
 Dose dependent \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ 
*more = more
 Decrease \_\_\_\_\_\_\_\_\_\_\_ in chest wall 
 Constriction of ? and ? muscles 
 \_\_\_\_\_carbia, hyp\_\_\_\_\_
A

respiratory depression
compliance
pharyngeal and laryngeal
Hypercarbia, hypoxia

28
Q

Nontherapeutic Effects:
 _________ RR with _________ Vt (low doses)
 _________ RR and Vt (high doses)
 _________ hypoxic ventilatory drive
 Ventilatory response curve ________ and shifted to _____

A

Decrease RR with increased Vt (low doses)
Decrease RR and Vt (high doses)
Decrease hypoxic ventilatory drive
reduced and shifted to right

29
Q

Respiratory Depression
 Peak onset of respiratory depression is _______ for morphine than fentanyl
 Respiratory depression produced by morphine lasts _______ than fentanyl

A

slower

longer…..LONGER ACTING

30
Q

Factors Increasing Magnitude/Duration of Opioid-Induced Respiratory Depression:
 _________ dose
 ? vs. ?
 Speed of injection and Dr E says…..
 ______________ with other anesthetics
 ___________ effects
 _________ clearance
 ___
 _____sis- increase unionized fraction increases brain penetration of drug
 Secondary peaks in _______ levels from reuptake of opioid from muscle, fat, lung and intestine

A 
Increased
Intermittent bolus vs. cont. infusion
Here is a pearl.....NEVER give any drug fast!!!
Concurrent admin
Synergistic
Decreased
Age
Alkalosis
plasma
31
Q

Perioperative Skeletal Muscle Effects
 Skeletal muscle _______:
 Can make __________ difficult or impossible

**DrE: Give ____________ then opioid!

A 
rigidity:
 Laryngeal muscles 
 Inhibition of GABA 
 Increase in dopamine
ventilation
muscle relaxant
32
Q

Perioperative Renal/GI/Liver Effects:
 Increase pristaltic and tone of ureters =
 Blocked _______________ release and _______
*can be good thing….why?
 Spasm of ____________ with increase in biliary pressure
 __________-decrease GI motility
 __________ gastric emptying

A

urgency?

catecholamine, cortisol, analaing (?) stress response!

sphincter of Oddi = allows bile and pancreatic juice to flow between pancreas and small intestine!

Constipation

Prolonged = indirect N/V!

33
Q

Pruritis:
 Cause =
 Histamine release =
 Occurs primarily on _________________

A

unknown
most probable cause
face (particularly nose)-“fentanyl nose itch”

34
Q

Neuraxial Effects:
 Opioids placed in epidural space may undergo uptake into:
 Penetration into CSF depends upon ?
 More lipid soluble, ______ peak CSF concentration
 Cephalad movement of opioid in the CSF depends on ?
 _____ lipid soluble will be limited in migration by uptake into the spinal cord, ie. _______
 Whereas ____ soluble opioid will remain in CSF for transfer to cephalic location ie. _______
 Vascular absorption of opioid from epidural space depends on ?
 More lipid soluble, ________ peak concentrations of opioid will be in blood
 …in fact…effects may be due to systemic absorption rather than ___

A

 fat
 systemic absorption
 diffusion into CSF

lipid solubility
quicker
lipid solubility
Highly, fentanyl
less, morphine
lipid solubility
quicker
CFS
35
Q

Side Effects of Neuraxial Opioids:

A 
 Pruritis-most common 
 Nausea/vomiting 
 Urinary retention 
 Ventilatory depression 
 More rapid with lipophilic agents 
 Delayed with less lipophilic (6-12hrs)
36
Q

Morphine:
 _____ lipid solubility, ______ protein bound and highly _______
 Produces …….
 IM peak effect =
 IV peak effect =
 DoA =
Potency =
 CV Causes =
 Metabolized by _______
 Active metabolite: ____________________ < or > potency than MSO4
 _________ play a key role in the extrahepatic metabolism of morphine
 ___________ will have ill effects due to M6G

A

Poor, highly, ionized
Produces analgesia, euphoria, sedation, nausea, pruritis, dry mouth, ventilatory depression, and Histamine
IM peak effect = 45 min, IV 15-30 min
DoA = 4hrs
Potency = 1 (baseline)
CV Causes = bradycardia via direct stimulation of vagus nerve & Inhibition of SA node
liver
morphine-6-glucuronide (M6G), >
Kidneys
Renal failure (do NOT use morphine with renal insufficiencies!)

37
Q

Meperidine:
 Structurally similar to ______, exhibits muscarinic effects
 Similar to ____________ as it blocks __________
 Potent at ________ receptors agonist effects, resulting in ?
 DOA =
 Produces same amount of ________, ________ and ________ as morphine
 Active metabolite = ?, lasting _ days, _ as potent, CNS stim = ________ reported
 Used to treat postop ___________ via ? and ? receptors activity
 _th as potent as morphine

A 
atropine
local anesthetics, Na Channels
alpha-2, calming/sedative effects
2-4 hours
analgesia, euphoria, sedation
Normeperidine, 3, ½, seizures (if hx of seizures....do NOT give!)
shivering, kappa and alpha-2
1/10
38
Q 
Hydromorphone:
 _ X more potent than MSO4 
 Derivative of \_\_\_\_\_ 
 \_\_\_\_\_ elimination and redistribution 
 Q _ h dosing needed 
 \_\_\_\_\_ sedation but less euphoria than MSO4
A 
5
MSO4
Rapid
4
More
39
Q

Fentanyl:
 _____ lipid soluble than morphine with ______ DOA  __% of initial dose undergoing first pass pulmonary uptake.
 _____ redistribution to inactive tissue sites as fat, skeletal m. and lungs.
 Multiple ____ doses or __________ produces progressive saturation of inactive tissue.
 ______ concentration does not decrease rapidly and DOA is prolonged - _________ peak in ______ levels.
This is due to immobilization of sequestered drug form _______ tissue sites. Accumulates with ______ doses.

A 
More, shorter
75
Rapid
Multiple IV doses or cont. infusion
plasma, secondary, plasma, inactive, multiple

*Dr E notes:
Clinically impression that fentanyl shorter DOA than MSO4 but can have longer DOA if infusion or multiple doses.
Has large volume of distribution secondary to more lipid soluble than MSO4 and plasma conc. maintained by slow reuptake from inactive tissue sites

40
Q

Fentanyl Clinical Significance:
 Used as analgesic adjunct for _______.
 As ________ to blunt stimulation of incision, laryngoscopy.
 As sole anesthetic in large doses due to _____________ stability.
 ___ times more potent than morphine.
 Wide range of doses given = _-__ mcg/kg
 Lozenges (fent lollipop) dose = _-__mcg/kg to be given __ minutes prior to induction

A 
surgery
adjuvant
hemodynamic
100
1-20 mcg/kg
5-20mcg/kg  to be given 45 minutes prior to induction
41
Q 
Sufentanil:
 Analogue of \_\_\_\_\_\_\_ 
 _X as lipid soluble as fentanyl 
 \_\_\_\_\_ protein bound 
 Undergoes first pass \_\_\_\_\_\_\_\_\_\_ uptake 
 \_\_\_\_\_ metabolized in \_\_\_\_\_ 
 \_\_\_\_\_ active metabolite =  
 \_\_ X more potent than fentanyl. 
 \_\_\_\_ X more potent than morphine.
A 
fentanyl
2
Highly
pulmonary
Rapidly, liver
Weakly, desmethylsufentanil
10
1,000
42
Q

Dr E’s favorite =

because…….

A

Sufentanil, fast on fast off = safe

43
Q

Sufentanil Clinical Significance:
 Used as adjunct for _______ and _______.
 Compared to morphine and fentanyl produces quicker _______, earlier __________, and earlier _________.
 Used as ______ for outpatient surgery……..shut of about __ minutes before

A

surgery and induction
induction, emergence, extubation
infusion, 30min

44
Q

Alfentanil:
 Analogue of _______.
 __% unionized = very rapid ___ onset (__ min compared to fentanyl __ min and sufentanil __ min).
 _____ protein bound
 Despite more intense protein binding, alfentanil’s _________ fraction is higher than that of fentanyl.
 _th as potent as fentanyl ______ X more potent than morphine.

A 
fentanyl
90%, CNS, 1.4 min, 6.8 min, 6.2 min
Highly
diffusible
1/5, 10-20
45
Q

Alfentanil Clinical Significance:
 ____ onset is useful for blunting hemodynamic response to noxious stimuli.
 Rapid effect due to 90% of drug in _________ form.   Used as infusion for ______________.

A

Rapid
non-ionized
outpatient surgery

46
Q

Remifentanil:
 Chemically r/t _____ but unique d/t ______ linkage.
 Metabolized by ____________ (not _________________).
 _____ onset and duration.
 Very _____ Vd, minimal accumulation in tissues, even with infusion (= good for infusion?)
 Potency slightly _ fentanyl, ~100 times more potent than morphine.

A 
fentanyl, ester
tissue/plasma esterases, pseudocholinesterases
Rapid
small
>
47
Q

Remifentanil Clinical Significance:
 Used to _____ noxious stimulus.
 Infusions for interm/long surgeries where rapid ________ is desired. Such as-neurosurgery, O/P surgery.

A

blunt

recovery

48
Q

Agonist/Antagonist:
 Mu antagonist/partial agonist, and partial agonist at kappa.
 Analgesia with limited ________ depression and ___ probability of dependence.
 Side effects sim. to opioid ______.
 May cause___phoria-_____ receptors stimulation.

A

ventilatory, low
agonists
dys, kappa

49
Q

Agonist/Antagonist: Nalbuphine (nubain)
 Analgesic response equal to _________.
 Works at _____ receptors.
 Antagonizes opioid induced ___________ depression while maintaining __________.
 No adverse __ problems.
 Reverses spasm of ______________.

A 
morphine
kappa
respiratory, analgesia
CV
sphincter of Oddi = allows bile and pancreatic juice to flow between pancreas and small intestine!
50
Q

Agonist/Antagonist: Nalbuphine (nubain)
 Analgesic response equal to _________.
 Works at _____ receptors.
 Antagonizes opioid induced ___________ depression while maintaining __________, unlike ________.
 No adverse __ problems.
 Reverses spasm of ______________.

A 
morphine
kappa
respiratory, analgesia, narcan
CV
sphincter of Oddi = allows bile and pancreatic juice to flow between pancreas and small intestine!
51
Q

Agonist/Antagonist: Butorphenol (stadol)
 Acts as agonist at _____ and weak antagonist or partial agonist at _____(dose dependent).
 _ X more potent than morphine for analgesia.
 Nasal spray for _________.

A

kappa, mu
5
migraines

52
Q

Antagonist: Naloxone
 Pure opioid _________
 ______ receptor sites and reverses respiratory depression and analgesia
 __________ antagonist at mu, kappa, and delta
 Duration of action _ most opioids
 Titratable (Yes or No?)
 Onset ___ minutes, reversal is ____ dependent.

A 
antagonist
Blocks
Competitive
<
Yes (dilute, give slow, wait, titrate)
1-2 min, dose
53
Q

Naloxone (cont)
 Benign (Yes or No?)
 Reversal of opioid effects =
 _____________ in patients with CV disease.
 Can induce pulmonary edema in healthy patients due to ______________ release.

A

No!
tachy, HTN, ventricular dysrhythmias, severe pain, pulm edema and agitation!
Pulmonary edema (especially in the young?)
catecholamine

54
Q

Potency:

A

Sufentanil > Remifentanil > Fentanyl > Alfentanil > Dilaudid > MSO4 > Demerol

55
Q 
Drug Dosages: Morphine 
Via CH 7 readings: PCA
Basal rate  =
Bolus dose =  
Bolus interval =
*Dr E told Hannah to know dose for Morphine? This book dose?
A 
Via CH 7 readings: PCA
0-2 mg/h
1-2 mg
6-10 min
* Basal infusions are not typically recommended for opioid-naive patients.
56
Q

Drug Dosages: Meperidine

A

50 to 100 mg IV

*produces variable degrees of pain relief and is not always effective in patients with severe pain

57
Q 
Drug Dosages: Hydromorphone
 Via CH 7 readings: PCA
Basal rate  =
Bolus dose =  
Bolus interval =
A 
Via CH 7 readings: PCA
0-0.4 mg/h
0.2-0.4 mg
6-10 min
* Basal infusions are not typically recommended for opioid-naive patients.
58
Q

Drug Dosages: Fentanyl
Loading dose =
Infusion =
Additional bolus =

Via CH 7 readings: PCA
Basal rate =
Bolus dose =
Bolus interval =

A

1-3 mcg/kg
4-20 mcg/kg
0.01 to 0.05 mcg/kg/min or 2-10 mcg/kg/hr
25-100 mcg/kg

Via CH 7 readings: PCA
0-60 mcg/h
20-50 mcg
5-10 min
* Basal infusions are not typically recommended for opioid-naive patients.
59
Q

Drug Dosages: Sufentanil
Loading dose =
Infusion =
Additional bolus =

A
  1. 1-0.3 mcg/kg
  2. 25-2 mcg/kg
  3. 0015 to 0.01 mcg/kg/min or 0.5-1.5 mcg/kg/hr
  4. 5-10 mcg/kg
60
Q

Drug Dosages: Alfentanil
Loading dose =
Infusion =
Additional bolus =

A

10-20 mcg/kg
25-100 mcg/kg
0.25 to 0.75 mcg/kg/min or 0.5-2 mcg/kg/hr
5-10 mcg/kg

61
Q

Drug Dosages: Remifentanil
Loading dose =
Infusion =
Additional bolus =

A

1-2 mcg/kg
1-2 mcg/kg
0.05 to 0.25 mcg/kg/min or 0.1-1.0 mcg/kg/hr
0.1-1 mcg/kg

62
Q

Onset:

A

RAPID: Alfentanil 1.4min < Remifentanil < Morphine < Sufentanil 6.2min < Fentanyl 6.8min < Meperidine :SLOW

63
Q

% Non-Ionized (pH 7.4):

A 
Alfentanil = 89-90% 
Remifentanil = 58%
Morphine = 23%
Sufentanil = 20%
Fentanyl = 8.5%
Meperidine = 7%
64
Q

Protein Binding (%):

A 
Remifentanil = 66-93%
Sufentanil = 93%
Alfentanil = 92%
Fentanyl = 84%
Meperidine = 70%
Morphine = 35%
65
Q

Elimination t1/2:

A 
Fentanyl = 3.1-6.6h
Meperidine = 3-5h
Sufentanil = 2.2-4.6h
Morphine = 1.7-3.3h
Alfentanil = 1.4-1.5h
Remifentanil = 0.17-0.33h

NURA-661-01 Anesthesia Pharm (6 decks)

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