Opioids and Reversals Flashcards
what is sublimaze
fentanyl
fentanyl
class/ category
Opioid agonist, synthetic (phenylpiperadine)
fentanyl
uses
- Analgesia,
- adjunct for general anesthesia,
- MAC
fentanyl
MOA
Opioid μ receptor agonist
fentanyl
dose (induction, balanced),
2-6 mcg/kg IV LBW
fentanyl
Bolus (analgesia)
1-2 mcg/kg IV LBW
fentanyl
Infustion (maintenance)
0.5-5 mcg/kg/hr LBW (associated with accumulation of drug)
Fentanyl
Onest, Peak, Duration
Onset: 30-60 sec
Peak: 3-4 min
Duration: 30-60 min
fentanyl
Metabolism, elimination, excretion
Metabolism: Hepatic
Elimination: Pulmonary (75%), Hepatic
Excretion: Renal
fentanyl
protein binding, VD, pKa
Protein binding: 84%
VD: 4 L/kg
pKa: 8.4
Fentanyl, remifentanil, Alfentanil, hydromorphone
CV effects
- ↓ HR, ↓ BP
- Orthostatic hypotension, syncope
Fentanyl, remifentanil, Alfentanil
Pulm Effects
6
- Skeletal muscle, “chest wall” rigidity with rapid administration of large doses – Treat with naloxone or neuromuscular blocker
- Typically ↓ RR, ↑ TV
- Ventilatory depression
- ↓ ventilatory response to CO2 → ↑ PaCO2 – Shifts CO2 response curve to the right
- Irregular breathing
- High doses may result in apnea
fentanyl
CNS effects
6
- ↓/↔ CBF, ↓/↔ CMRO2 ↓ ICP (if ventilation normal)
- ↓/↔ CPP
- Miosis
- Euphoria
- Sedation
- Dystonic reaction (with rapid administration)
Fentanyl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine
GI effects
- N/V
- Constipation
- Biliary spasm
- Delayed gastric emptying
T/F fentanyl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine can cause urinary retention and decrease in body temperature
TRUE!
Can fentanyl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine cause myoclonus?
Yes!
fentanyl, remifentanil, sufentanil, Alfentanil, hydromorphone, morphine can cause ‘x’ especially where?
Pruritus, especially around the nose
caution using fentayl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine with this injury, what could they cause?
Use caution with head injury – Effects on wakefulness, miosis, and ventilatory depression with ↑ PaCO2
What does Fentanyl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine do to MAC requirements?
Synergistically reduces MAC requirements
Fentanyl, remifentanil is how many more times potent than morphine?
100x more potent than Morphine
T/F fentanyl has a cross-reaction with morphine allergy
FALSE! No cross-reaction with Morphine allergy
do fentanyl, remifentanil, sufentanil, alfentanil, hydromorphone, morphine have additive potential?
YES
fentanyl can trigger what syndrome?
- May trigger serotonin syndrome
what is Ultiva
Remifentanil
remifentanil
class
Opioid agonist, synthetic (phenylpiperadine)
remifentanil
uses
- Analgesia
- adjunct for general anesthesia
- MAC
remifentanil
MOA
Opioid μ receptor agonist
remifentanil
bolus (induction, balanced)
0.5-1 mcg/kg IV LBW, administered slowly, over 1-2 min
remifentanil
Bolus (analgesia)
0.25-1 mcg/kg IV LBW, administered slowly, over 1-2 min
remifentanil
Infustion (maintenance)
0.1-1 mcg/kg/min IV, may extend up to 2 mcg/kg/min LBW
remifentanil
onset, peak, duration
Onset: 30-60 sec
Peak: 1 min
Duration: 5-10 min
remifentanil
metabolism, protein binding
Metabolism: Nonspecific plasma and tissue esterases
Protein binding: 93%
remifentanil
VD, pKa
VD: 0.39 L/kg
pKa: 7.2
remifentanil, Sufentanil
CNS effects
- ↓/↔ CBF, ↓/↔ CMRO2, ↓ ICP (if ventilation normal)
- ↓ CPP
- Miosis
- Euphoria
- Sedation
remifentanil is associated with opioid-induced ‘what’
Associated with opioid-induced hyperalgesia
prolonged administration of remifentanil can cause what?
Prolonged administration may result in tachyphylaxis
remifentanil has similar potency to which medication?
Potency similar to Fentanyl
what is sufenta
Sufentanil
Sufentanil
class
Opioid agonist, semi-synthetic (phenylpiperadine)
Sufentanil
use
Analgesia, adjunct for general anesthesia
Sufentanil
Opioid μ, κ, δ receptor agonist
Sufentanil
Bolus (induction, balanced)
0.3 mcg/kg IV LBW
Sufentanil
bolus (analgesia)
0.1-0.25 mcg/kg IV LBW
Sufentanil
Infusion (maintenance)
0.5-1.5 mcg/kg/hr IV LBW
Sufentanil
onset, peak, duration
Onset: 30-60 sec
Peak: 3-4 min
Duration: 30 min, Dose-dependent
Sufentanil
Metabolsim, elimination, active metabolite
Metabolism: Hepatic
Elimination: Pulmonary (~60%) / Hepatic
Active metabolite: Desmethylsufentanil (10% of parent drug activity)
Sufentanil
CV effects
- ↓ HR (profound ↓ may lead to ↓ CO) , ↓ BP,
- Orthostatic hypotension, syncope
Sufentanil
protein binding, VD, pKa
Protein binding: 93%
VD: 2 L/kg
pKa: 8.0
sufentanil
pulm effects
7
- Skeletal muscle, “chest wall” rigidity with rapid administration of large doses – Treat with naloxone or neuromuscular blocker
- Typically ↓ RR, ↑ TV
- Ventilatory depression
- ↓ ventilatory response to CO2 → ↑ PaCO2 – Shifts CO2 response curve to the right
- Irregular breathing
- High doses may result in apnea
- Antitussive
Fentanyl, remifentanil, sufentanil can cause histamine release?
- No histamine release
sufentanil is how many more times potent than morphine
1,000x more potent than Morphine
which medication is 10x more potent than fentanyl
sufentanil
what is Alfenta
Alfentanil
Alfentanil
class
Opioid agonist, synthetic
Alfentanil
uses and MOA
Uses: Analgesia, adjunct for general anesthesia, MAC
Mechanism of Action: Opioid μ receptor agonist
Alfentanil
Bolus (induction, balanced)
15-30 mcg/kg IV
Alfentanil
Bolus (analgesia)
5-10 mcg/kg IV
Alfentanil
Infusion (maintenance)
0.5-2 mcg/kg/min IV
Alfentanil
Onset, Peak, Duration
Onset: 30-60 sec
Peak: 1-2 min
Duration: < 10 min
Alfentanil
metabolism, elimination
Metabolism: Hepatic
Elimination: Hepatic, Renal
Alfentanil
Protein binding, VD, pKA
Protein binding: 92%
VD: 0.6 L/kg
pKa: 6.5
Alfentanil
CNS effects
- ↓/↔ CBF, ↓/↔ CMRO2[4] ↓ ICP (if ventilation normal)
- ↓ CPP
- Miosis
- Euphoria
- Sedation
- Dystonic reaction (with rapid administration)
Alfentanil is how many more times potent than morphine
10x
Alfentanil is 1/10th as potent as which medication?
1/10th as potent as Fentanyl
what is dilaudid
Hydromorphone
hydromorphone
class
Opioid agonist, semi-synthetic
hydromorphone
uses
Analgesia, adjunct for general anesthesia
Hydromorphone
MOA
Opioid μ, κ, δ receptor agonist
Hydromorphone
Bolus
0.01-0.02 mg/kg IV
Hydromorphone
onset, peak, duration
Onset: 5 min
Peak: 10-20 min
Duration: 4-5 hr
hydromorphone
metabolism, elimination
Metabolism: Hepatic
Elimination: Renal
hydromorphone, morphine
pulm effects
- Typically ↓ RR, ↑ TV
- Ventilatory depression
- ↓ ventilatory response to CO2→ ↑ PaCO2 – Shifts CO2 response curve to the right
- Irregular breathing
- High doses may result in apnea
hydromorphone
CNS effects
- ↓ CBF, possible ↓ ICP (if ventilation normal)
- Miosis
- Euphoria
- Sedation
- Agitation
hydromorphone is how many more times potent than morphine
7x more potent than Morphine
what is Duramorph or astromorph
morphine
morphine
class/ category
Opioid agonist, natural (phenanthrene)
Morphine
uses
Analgesia, adjunct for general anesthesia
morphine
MOA
Opioid μ, κ, δ receptor agonist
Morphine
dose
Bolus: 0.03-0.2 mg/kg IV TTE
Morphine
onset, peak, duration
Onset: 15-30 min
Peak: 30-90 min
Duration: 4-5 hr, dose-dependent
Morphine
metabolism, elimination
Metabolism: Hepatic and extrahepatic Renal
Elimination: Renal
morphine
protein binding, VD, pKa
Protein binding: 35%
VD: 2.8 L/kg
pKa: 7.9
morphine
active metabolites
2 and effects
Morphine-3-glucuronide (~60%): no analgesic or antianalgesic action)
Morphine-6-glucuronide (5-10%): full mu agonist → analgesia and ventilatory depression
-Longer duration than Morphine itself
-Binds with comparable affinity, 650x more analgesic potency)
-May accumulate with renal dysfunction
morphine
CV effects
- ↓ HR, ↓ BP, positional changes can lead to ↓ CO, ↓ venous return
- Orthostatic hypotension, syncope
morphine
CNS
5
- ↓/↔ CBF, ↓/↔ CMRO2 ↓ ICP (if ventilation normal)
- ↑/↓ CPP
- Miosis
- Euphoria
- Sedation
does morphine cause histamine release
YES!
morphine should be used cautionsly with patients with what condition
Use caution in patients with renal dysfunction
what is Narcan
Naloxone
Naloxone
class/ category
Opioid antagonist
Naloxone
use
Reversal of opioid-induced respiratory depression
Naloxone
MOA
Competitive antagonist at μ, κ, δ opioid receptors
Naloxone
Bolus, infusion
Bolus: 1-4 mcg/kg/ IV; titrated in 40 mcg increments every 2 min
Infusion: 2-4 mg/hr
Naloxone
onset, peak
Onset: 1-2 min
Peak: 5-15 min
Naloxone
duration, metabolism
Duration: 30-45 min
Metabolism: Hepatic
Naloxone
CV effects
SNS surge
* ↑ BP, ↑ HR
* Dysrhythmias
* Cardiac ischemia
Naloxone
Pulm effects
Pulmonary edema
Naloxone
GI effects
N/V with awakening
Naloxone may precipitate what kind of symptoms
May precipitate withdrawal symptoms in opioid-dependent patients
Naloxone may cause reversal of what?
May cause reversal of analgesia, dose-dependent
When giving Naloxone, what do you monitor for, and what may you need to do?
Monitor for recrudescence – May require repeat doses or continuous infusion for sustained opioid antagonism