Pharm 1 > Opioids > Flashcards

Opioids Flashcards

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1
Q

Opioids are both ___ occurring and ___ produced

A

naturally, synthetically

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2
Q

Opioids possess ____ or ___-like properties

A

opium, morphine like

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3
Q

What does “benumbing” translate from greek?

A

Narcotic –> used more as a legal term in US

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4
Q

4 categories of opioid classifications

A
  • agonists
  • partial agonists
  • agonist-antagonists
  • antagonists
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5
Q

3 chemical derivations of opioid classifications

A
  • naturally occuring
  • semisynthetic
  • synthetic compounds
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6
Q

____ ____ like ____ produce analgesia through actions at CNS receptors

A

Opioid alkaloids like morphine

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7
Q

What 3 opioid peptides have overlapping affinities for CNS receptors?

A
  • Endorphins
  • Enkephalins
  • Dynorphins
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8
Q

5 peripheral sites that bind opiate receptors?

A
  • GI system
  • Vasculature
  • Heart
  • Lung
  • Immune system
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9
Q

Supraspinal analgesia: analgesic action ___ the spine. Involves where and inhibition of what?

A
  • above
  • Supraspinal analgesia involves higher neural centers in brain and inhibition of neurons in pain pathways
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10
Q

Spinal analgesia: analgesic action __ the spine. Physiologic response?

A
  • at
  • Decreased calcium influx and decreased release of neurotransmitters involved in nociception
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11
Q

Opioids act as ____ at opioid receptors at ____ and ____ sites in the CNS and peripherally to decrease release of neurotransmitters

A

agonists, presynaptic, postsynaptic

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12
Q

what are the 3 main type of opioid receptors?

A

mu, delta, kappa

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13
Q

Endorphins are associated with __ receptors

A

mu

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14
Q

Enkephalins are associated with ___ receptors

A

delta

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15
Q

Dynorphins are associated with ___ receptors

A

kappa

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16
Q

Mu stimulation is associated with?

A
  • Supraspinal and spinal analgesia
  • Euphoria/sedation
  • Decrease in ventilation
  • Most classic clinical actions of opioid agonists
  • Mild hypothermia
  • Urinary retention
  • N/V
  • Decreased peristalsis
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17
Q

Kappa stimulation is associated with?

A
  • Supraspinal and spinal analgesia
  • Sedation/delirium/hallucinations
  • Miosis (pupil constriction)
  • Anti inflammatory actions for arthritis, etc.
  • Anti shivering
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18
Q

Delta stimulation associated with?

A
  • Supraspinal and spinal analgesia
  • Responds to enkephalins
  • modulates activity of mu receptors
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19
Q

What two drugs are Mu antagonists, Kappa partial agonists, and Delta agonists?

A

Butorphanol and Nalbuphine

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20
Q

What three drugs are mu, kappa, and delta antagonists?

A
  • Naloxone
  • Naltrexone
  • Nalmefene
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21
Q

What makes Kappa receptors different in GU actions?

A

Can lead to diuresis

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22
Q

CV effects of Mu receptor activation?

A

Bradycardia

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23
Q

Which receptor has lowest abuse potential?

A

Kappa

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24
Q

Mu 1 characteristics?

A
  • Analgesia (spinal and supraspinal)
  • Bradycardia
  • Euphoria
  • Low abuse potential
  • Miosis
  • Hypothermia
  • Urinary retention
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25
Mu 2 characteristics?
- Analgesia (spinal only) - Bradycardia - Respiratory depression - Constipation - Physical dependence
26
Mu 3 characteristics?
- Immune suppresion
27
____ and ____ are more effective orally bc of reduced first pass metabolism
Codeine and oxycodone
28
____ admin skips first pass --> rapid therapeutic levels
Intranasal
29
____ ___ serves as opioid reservoir but ___ ___ can also accumulate with high or continuous doses of high lipophilic opioids
Skeletal muscle, fatty tissue
30
Opioids are converted to ___ ___ then ____ ___
polar metabolites, renally excreted
31
Accumulation of metabolites can produce adverse effects with __ ___
renal failure
32
Plasma esterase metabolism occurs with which 2 drugs?
- Heroin - Remifentanil
33
Opioids are metabolized where?
Liver via hepatic biotransformation
34
Remifentanil is metabolized by ____ in ___ __ by nonspecific esterases
hydrolysis, plasma tissues
35
Remifentanil is dosed at what?
Lean body weight
36
Remifentanil has what kind of vD and what kind of clearance?
Low vD, high clearance --> short half life (10 min)
37
What is morphine's metabolite? considerations?
morphine-6-glucouronide - accumulates in dialysis patients - renail failure pt more prone to respiratory depression and toxicity
38
What is meperidine's metabolite? considerations?
normeperidine - neurotoxic --> accumulates in elderly or those with hepatic or renal failure - half as potent as parent compound - reduces seizure threshold, increases CNS excitability - Muscle twitches, tremors, seizures
39
4 drugs with no active metabolites
fentanyl, sufentanil, alfentanil, remifentanil
40
Opioids and metabolites are excreted primarily by ____
kidneys
41
Opioids and metabolites are excreted secondarily by ___ ___ and __ ___
biliary system and GI tract
42
Effector sites are in the ____ = must cross ____ to exhibit effects
CNS, blood brain barrier
43
Morphine with women considerations
- More potent - Slow onset - Longer duration - Lower post op opioid consumption
44
MOA of opioids involved binding ____ in ____ and __ ___
GPCRs, brain and spinal cord
45
Opioids close ____ ____ _____ ____ and open ___ ____ and _____
voltage gated calcium channels, potassium channels and hyperpolarize
46
On presynaptic neuron, opioid stimulation reduces calcium conductance which reduces what?
neurotransmitter release
47
On postsynaptic neuron, opioids increase potassium conductance which does what?
- Hyperpolarizes neuron - Decreased RMP (TP further from RMP) - More resistant to stimulation
48
Expain how G proteins work with opioids
- Opioid receptors are linked to a G protein - Agonist --> g protein stops adenylate cyclase - Reduces intracellular cAMP (second messenger) - Alters ionic currents and reduces neuronal function
49
CNS/Respiratory considerations with opioids
- Dose dependent respiratory depression - CO2 curve down and to the right - ICP can increase if hypoventilation leads to hypercarbia - Miosis --> pinpoint pupils
50
Stimulation of chemoreceptor trigger zone in ___ ____ of ____ can cause N/V
area postrema of medulla
51
Two dominant receptors in area postrema of medulla?
5HT3 receptor and D2 (dopamine type 2)
52
What causes decreased body temp with opioids?
In thermoregulation, body resets hypothalamic temperature set point which can cause lower body temps
53
Opioids have ___ ____ on SSEPs (evoked potentials)
minimal effects. Used with half MAC or as TIVA for spine cases.
54
Which 3 drugs release histamine?
- Morphine - Codeine - Meperidine
55
Does remi, fent, sufent, or alfent release histamine?
No
56
Which 3 CV effects are unaffected by opioids
- Myocardial contractility (myocardial depression can occur if combined with N20) - Baroreceptor function - Autonomic responsiveness
57
Which opioid can cause tachycardia?
Meperidine
58
Which two receptors are acted on in respiratory center in brainstem with opioids?
mu and delta
59
GI effects of opioids
- Decreased motility - Prolonged gastric emptying - Dose dependent increase in biliary duct pressure and sphincter of oddi tone (meperidine causes lowest increase)
60
Urinary retention with opioids is due to?
- Detrusor relaxation and constriction of urinary sphincter - Common with intrathecal and epidural admin
61
___ receptors can cause diuresis
Kappa
62
Opioids can cause cough suppression via depressant effect on cough center in ____
medulla
63
opioids and antitussive effects
- Protective glottal reflexes not affected - Codeine and heroin are most effective - Can lead to increase in secretions
64
Opioids and muscle rigidity
- Large IV doses --> general hypertonus of skeletal muscle - Loss of chest wall compliance - Constriction of laryngeal and pharyngeal muscles - Difficult ventilation * - Increased with use of N20
65
Muscle rigidity from opioids results from ___ ____ in the ___
mu stimulation in the CNS
66
Muscle rigidity from opioids treatment
paralysis and intubation or narcan
67
____ is a rash, itching, or feeling of warmth
Pruritus
68
Pruritus is especially prominent with ____ ____
intrathecal administration
69
Pruritus from opioids treatment
- Narcan - Nalbuphine, droperidol, antihistamines, zofran - Most effective seems mixed mu/kappa partial agonists (retains some analgesia)
70
Opioids endocrine effects intraop
- Reduce stress response to surgery - Immunosuppressant effect - Release of vasopressin and inhibition of stress induced release of corticotropin and gonadotropins from pituitary - Chronic use lowers BMR and temp
71
Neuraxial routes of admin
Epidural and intrathecal
72
_____ _____ is potent method to inject opioids directly into CSF
Spinal administration
73
____ and ____ ____ occur more often with spinal anesthesia
Pruritus and urinary retention
74
3 side effects seen with neuroaxial opioid administration
- N/V - Pruritus - Urinary retention
75
Most common serious complication of spinal anesthesia?
Respiratory depression - Delayed 8-12 hours
76
____ doses of opioids are higher than _____
Epidural, intrathecal
77
Plasma levels comparative to ___ ____, provide supraspinal anesthesia
IM administration
78
2 naturally occurring opioids agonists?
- Phenanthrene derivatives: morphine and codeine (prodrug for morphine)
79
Examples of semisynthetic opioid agonists?
- Morphine derivatives: hydromorphone, heroine, naloxone, naltrexone - Thebaine derivative: oxycodone
80
4 synthetic opioid agonists?
- Piperidines - Phenylpiperidines (meperidine, fentanyl, sufent, alfent, remifent) - Diphenylpropylamines (methadone) - Also tramadol
81
3 opioid partial agonists
- Buprenoprhine - Butorphanol - Nalbuphine
82
3 opioid antagonists
- Naloxone - Nalmefene - Naltrexone
83
With opioid dosing, small doses effects are ____ by ____
terminated by redistribution
84
With opioid dosing, multiple doses or infusions are ____ on _____ for offset
dependent on metabolism
85
Most potent opioid?
Sufentanil
86
Least potent opioid?
Meperidine
87
Rank the 7 opioids from most to least potent
1. Sufentanil 2. Fentanyl 3. Remifentanil 4. Alfentanil 5. Hydromorphone 6. Morphine 7. Meperidine
88
Morphine is more effective for ___ pain than ___ ___ pain
dull, sharp intermittent
89
When given IV, morphine ___ first then ____
sedates, analgesia
90
____ has the longest intrathecal duration
Morphine
91
______ is the least lipophilic --> slow onset
Morphine
92
Morphine is metabolized by?
Phase 2 glucuronide conjugation in the liver --> more prolonged effects from metabolite --> monitor for excess sedation in renal failure
93
Morphine causes ___ release from ___ ___
histamine, mast cells
94
Side effects of histamine release from morphine?
- Local itching, redness, hives near IV site - Hypotension or tachycardia if significant release
95
When is morphine primarily used?
post op, not as much intraop --> delayed onset and peak effects
96
Codeine is considered to be a ___ opioid. More used for ____ activity
weak, antitussive
97
With codeine, extensive conversion of the prodrug into ____ can lead to toxicity
morphine
98
___ has similar pharmacokinetic profile to morphine but is more potent
Hydromorphone
99
Hydromorphone is ___ soluble --> can be used for epidural and spinal
Lipid
100
Hydromorphone has ___ metabolites
none. use recommended for renal failure patients
101
Meperidine's metabolite ____
normeperedine --> half as analgesic, lowers seizure threshold, induces CNS excitability
102
Why would you want to consider not using meperidine in elderly or renal pt?
Long elimination half life --> accumulation
103
Co administration of meperidine with a ______ can cause ____ _____
Monoamine Oxidase inhibitor (MAOI), serotonin syndrome - Ex of MAOIs: phenelzine, isocarboxazid, tranylcypromine
104
Symptoms of serotonin syndrome
- Hyperthermia - Mental status changes - Seizures - Death
105
Side effects of meperidine
- Anticholinergic effects --> tachycardia, dry mouth, mydriasis (dilation of pupil) - Anti shivering effects --> Kappa receptor stimulation, shivering increases O2 consumption, reduced by meperidine
106
_____ has a more rapid onset and shorter duration than fentanyl
Alfentanil
107
Alfentanil is useful for:
- Blunting hemodynamic response to short, intense periods of stimulation (tracheal intubation, retrobulbar block)
108
Alfentanil has a ___ vD and ___ protein binding
Low, high
109
Time of duration from fentanyl bolus dose
20-40 minutes
110
Most widely used opioid in anesthesia
fentanyl
111
Termination of fentanyl off bolus dose is based on ___
redistribution
112
Fentanyl clearance is dependent upon ___ ____ ___
hepatic blood flow
113
Remifentanil has a ___ onset and ____ ___ duration, titratability, and simple metabolism
rapid, ultra short
114
Remifentanil infusion dose (based on what)
.05-2mcg/kg/min --> lean body weight in obese patients
115
What is the context sensitive half time of remifent?
4 minutes, regardless of infusion duration
116
addition of ester group in remifent makes it susceptible to ____
hydrolysis --> drug easily and rapidly metabolized
117
Disadvantages of remifent
- Respiratory depression and muscle rigidity --> bolus not recommended - Opioids induced hyperalgesia --> higher post op requirements --> can be prevented with ketamine or magnesium
118
Is remifent okay for epidural or intrathecal admin?
No. RIsk of glycine toxicitiy
119
Opioid induced hyperalgesia can be seen with ___, ____, and ____
Remifent, fent, and morphine
120
Explain opioid induced hyperalgesia
- Different from tolerance - Persistent admin can increase sensation of pain - Exaggerated pain response to painful stimulus
121
Few facts about sufentanil
- Most potent - Used when profound analgesia is needed (cardiac surgery common) - IV and intrathecal is effective - Shorter elimination half life than fent
122
Methadone uses:
- Chronic pain - Opioid abstinence - Heroin addiction tx --> prevents withdrawal
123
Methadone MOA
- Mu agonist - NMDA antagonist - Inhibits reuptake of monoamines in synaptic cleft
124
Methadone advantages and disadvantages
- Advantages --> high bioavailability and no active metabolites - Disadvantages --> Long half life, accumulation, longer time to reach steady state, can prolong QT
125
Why does methadone take longer to metabolize?
- highly protein bound - Slow release and lower intrinsic ability of liver to metabolize
126
Tramadol is a ___ ___ agonist
Weak mu
127
Tramadol MOA
- weak mu agonist - Inhibits norepinephrine and serotonin neuronal reuptake - Effective for mild to moderate pain
128
Tramadol advantages
- analgesia without significant respiratory depression - Decrease in post op shivering - low propensity for tolerance and abuse
129
Tramadol disadvantages
- Increased N/V periop - Increased risk of seizures (avoid in epileptics)
130
Partial opioid agonists aka ___ ___
agonist antagonists
131
Partial opioid advantages
- Analgesia with reduced risk of resp depression - Low risk of dependence - Pt's who can't tolerate full opioid agonist
132
Partial opioid disadvantages
- Ceiling effect of analgesic properties - Reduce efficacy of previously administered opioids - Acute withdrawal in opioid dependent pt - Dysphoric reactions (similar to depression)
133
Buprenorphine is a ___ ____, has ____ analgesia than morphine, ____ to reverse with naloxone, and has ___ ___ of action
mu agonist, greater, difficult, long duration (available transdermal)
134
Nalbuphine is a ____ agonist and ___ antagonist, ___ analgesia to morphine, ___ to reverse with naloxone, useful in ___ ___
Kappa, mu, similar, able, CV disease (does not increase BP or HR)
135
Butorphanol is a ___ agonist and ___ antagonist (weak), ____ analgesia than morphine, ___ to reverse with naloxone, and useful in ___ ____
kappa, mu, greater, able, post op shivering (can be given intranasal)
136
Which drug can be used in some rehab programs that also helps reduce alcohol cravings?
Buprenorphine (Subutex)
137
Acute surgical pain can be difficult to manage if pt is on ____
buprenorphine --> high mu affinity renders common opioids ineffective --> can taper down before hand but shouldn't be stopped
138
Kratom can act as a partial ___ ____
mu agonist
139
Kratom at low doses has ___ effects
stimulant
140
Kratom at high doses has ____ effects
Sedative
141
Is kratom considered safe?
no
142
Naloxone is a ____ antagonist at mu, kappa, and delta receptors
competitive
143
Naloxone has ___ duration than most opioids
shorter --> may need redosing or drip
144
Naloxone half life and duration
- Half life = 1 hour - Duration = 30-45 minutes
145
Naloxone is metabolized in?
liver --> significant first pass
146
Low dosing of ____ can be effective for reversing some side effects of epidural opioids
Naloxone
147
Naloxone side effects:
discomfort, pulmonary edema, death, N/V
148
Analgesic reversal ____ SNS in patients with pain
activates - Causes pulm edema, tachy, sudden catecholamine release --> dysrhythmias
149
Naloxone ____ the placenta
Crosses - Neonate can go into withdrawal if mom has been abusing opioids
150
Naltrexone has ___ oral efficiency and ___ duration of action than naloxone
higher, longer
151
___ ____ is tolerance to one drug producing tolerance to another similar drug
Cross tolerance
152
Tolerance develops to nearly all side effects except ___ and ____
miosis and constipation
153
Early signs of opioid withdrawal
- Diaphoresis, insomnia, restlessness
154
Late signs of opioid withdrawal
- Abdominal cramping, N/V
155
Opioid receptor locations (3)
- brain - spinal cord - peripherally --> sensory neurons and immune cells
156
Steps in opioid receptor activation with G proteins:
- Opioid binds to receptor - G protein activated - Adenylate cyclase inhibited - Less cAMP produced - Calcium conductance decreased - Potassium conductance increased
157
When "narcotized", RR affected first with ____ and ____ respirations
slower and deeper - ex: RR 8, TV 550
158
When strongly painful stimuli that you've been treating with opioids for is removed, ____ ____ may occur
Respiratory depression - ex: tourniquet pain example
159
Increased biliary duct pressure can be relieved by:
glucagon or narcan
160
Opioid recommended for renal pt?
Hydromorphone --> no known metabolites
161
Fentanyl inactive metabolites eliminated in ___ and ___
urine and bile
162
Fentanyl has first pass uptake in ___ without temporary accumulation before release
Lungs
163
Opioid induced hyperalgesia can be prevented with ___ or ____
ketamine or mag sulfate
164
Kratom has various claims of efficacy on ___ ____ or ___ ____ ____
opioid tapering or opioid replacement therapy
165
Alfentanil induction dose
150-300mcg
166
Fentanyl induction dose
50-100mcg
167
Sufent induction dose
0.1-0.3mcg/kg IBW
168
Sufent infusion dose
0.2-0.5mcg/kg/hour
169
Remifent induction dose
1mcg/kg WITH hypnotic
170
Butorphanol is a mu, kappa, delta what?
Mu antagonist, kappa partial agonist, and delta agonist
171
Nalbuphine is a mu, kappa, and delta what?
Mu antagonist, kappa partial agonist, and delta agonist
172
Mu-___ has supraspinal and spinal analgesia while Mu-___ has only spinal analgesia
1, 2
Pharm 1
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