Opioid & non-opioid analgesics 3 Flashcards
Which drug is associated with anticholinergic side effects?
a. meperidine
b. naloxone
c. methadone
d. remifentanil
a. meperidine
Meperidine stimulates
mu & kappa receptors
Co-administration of meperidine with a ____________ can cause serotonin syndrome
MAO inhibitor
Meperidine is structurally related to
atropine
Because meperidine is structurally related to atropine, the following can be seen
tachycardia, mydriasis, and dry mouth
Side effects of meperidine include
histamine release
antishivering effect (kappa receptor)
Meperidine is not recommended for
patient-controlled analgesia (PCA)
S/sx of serotonin syndrome include
hyperthermia, mental status changes, hyperreflexia, seizures, and death
MAO inhibitors include
phenelzine, isocarboxazid, tranylcypromine
What 2 opioid receptors are stimulated by meperidine?
Kappa
Mu
Which pharmacological characteristic accounts for the rapid onset of action of alfentanil?
a. low protein binding
b. low degree of ionization
c. high potency
d. high lipid solubility
b. low degree of ionization
Alfentanil is 90% (non-ionized or ionized)?
non-ionized
The _____________- portion of alfentanil can diffuse across the blood brain barrier
non-ionized
Alfentanil use useful for
blunting the hemodynamic response to short, intense periods of stimulation such as tracheal intubation or retrobulbar block
Alfentanil is a weak
base
The pKa of alfentanil is
6.5
Alfentanil has the fastest
onset of action compared to other opioids
Due it is lower hepatic extraction ratio, alfentanil metabolism is more susceptible to
alterations in CYP3A4 function
________________ inhibits alfentanil’s metabolism, and co-administration can result in prolonged respiratory depression
Erythromycin
Renal failure ____________ alter alfentanil clearance
does not
What opioid has the lowest non-ionized fraction at physiologic pH?
meperidine at 7%
Which agents can be used to attenuate opioid-induced hyperalgesia? (select 2.)
a. ketamine
b. clonidine
c. morphine
d. magnesium sulfate
a. ketamine
d. magnesium sulfate
Remifentanil is a rapid
on and rapid-off mu agonist
The context sensitive half time of remifentanil is
about four minutes, regardless of infusion duration
Remifentanil can cause
acute opioid-induced hyperalgesia following discontinuation
Remifentanil should not be used for
neuraxial anesthesia- the vial contains glycine that can cause skeletal muscle weakness
Remifentanil is highly (liphophilic or hydrophilic)?
liphophilic
What is the maintenance infusion of remifentanil?
0.1-1.0 mcg/kg/min.
In obese patients, the rate of remifentanil infusion is calculated with
lean body weight
Remifentanil is metabolized by
plasma esterases
Opioid induced hyperalgesia can be prevented with
ketamine or magnesium sulfate
Which opioid has the same potency as remifentanil?
fentanyl
How is remifentanil metabolized?
hydrolysis by erthyrocyte and tissue esterases (not pseudocholinesterase)
Methadone provides analgesia by all of the following ways EXCEPT:
a. mu receptor agonism
b. NMDA receptor antagonism
c. Monamine reuptake inhibition
d. cholinergic receptor antagonism
d. cholinergic receptor antagonism
Methadone is useful in the following circumstances:
chronic treatment of opioid abuse
chronic pain syndromes
cancer pain
Methadone decreases pain by three mechanisms:
Mu receptor agonist
NMDA receptor antagonist
inhibits reuptake of monoamines in the synaptic cleft
Methadone can prolong
the QT interval
Olicerdine is an
IV opioid analgesic that primarily selects for the mu-receptor
Oliceridine is indicated for
adults with acute pain when other opioid analgesics and alternative treatments fail to provide adequate pain relief
Oliceridine is contraindicated in patients with
GI obstruction or paralytic ileus
significant respiratory depression
acute or severe asthma in an unmonitored setting
Key considerations for oliceridine include
mild QT interval prolongation
increased risk of seizures in the patient with a seizure disorder
risk of hypotension when co-administered with a general anesthetic
The duration of action of methadone is
3-6 hours
The dosing of oliceridine is
loading dose IV: 1-2 mg IV
supplemental IV doses: 1-3 mg every 1-3 hours PRN
The cumulative daily dose of oliceridine should not exceed
27 mg
Is there dose adjustment needed for patients with renal impairment or mild to moderate hepatic impairment for patients taking oliceridine?
Nope
