Opioids Flashcards
How do you treat opioid-induced biliary spasms?
Naloxone or glucagon to relax
the sphincter muscle
Which opioid should not be used in patients taking MAOI?
Meperidine (demerol) because it can lead to serotonin syndrome
If the potency of morphine is 1, what are the relative potencies of meperidine, codeine, methadone, butorphanol, hydromorphone, nalbuphine, alfentanil, fentanyl, and sufentanil?
Most —> least potent:
sufentanyl
Fentanyl
Alfentanil
Hydromorphone
Morphine - codeine
meperidine
Are opioids lipid soluble or water soluble?
high lipid soluble
rapidly cross BBB
Which opioids are strong? medium?
The lipid solubility of opioids affects their…
onset and duration
T/F
the lungs can serve as a reservoir of opioid drug molecules
true
Opioids are classified on the basis of…
their synthesis
chemical structure
potency
receptor binding
effect at the opioid receptors
Natural opioid
morphine
Semisynthetic opioid
hydromorphone
Synthetic opioid
fentanyl
alfentanil
sufentanil
remifentanil
meperidine
piperidines
Drugs with high ___ solubility cross the BBB.
lipid
Properties affecting the passage of the drug into the brain across the blood-brain barrier
o Molecule size
o pKa : affects the degree of ionization of the molecule and depends on the plasma pH
o Protein binding: to albumin and a 1-acid glycoprotein
o Lipid solubility
The piperidines are (natural/semi-synth/synthetic).
synthetic
The piperidines
- Lipophilic opioids that rapidly cross the BBB
*shared backbone - Fentanyl
- Sufentanil
- Alfentanil
- Remifentanil
Fentanyl
o x100 more potent than morphine
o Decrease CV responses to noxious stimulation from laryngoscopy, intubation, skin incision and surgical stress
o Lasts abt 10-20 min (dose dependent)
Sufentanil
o a thienyl derivate of fentanyl and about 10-times more potent than fentanyl
o 1000x potent > morphine
o its lipophilicity is two times greater than that of fentanyl
o long acting
Remifentanil
o Is not metabolized in the liver and is 100 to 200x more potent than morphine
o methyl ester side chain that is metabolized by blood (within the erythrocyte) and tissue nonspecific esterase’s
o Rapid action & clearance (context sensitive half-life of 2-3 minutes)
o Extrahepatic clearance
o Usually infusion; decreases by 50% in as little as 40 seconds
o MAC (minimim alveo. [ ]) is reduced w a remifentanil infusion
o Very fast wake up!
Which piperidine is not metabolized in the liver?
Remifentanil
T/F
Ketamine is a non-opioid that works on opioid receptors.
True
it works at NMDA (antagonist) & opioid receptors
Requirements for inhalational anesthetics and propofol are reduced by about 50% when administering ___ IV fentanyl
1.5 to 3 μg/kg
decreases cardiovascular responses to noxious stimulation
Fentanyl
thienyl derivate of fentanyl
Sufentanil
Longer duration
good for longer cases
bonds stronger than fentanyl
Sufentanil
Benefits of using opioids
less volatile anesthetic
faster wake up
Clearance of remifentanil is ____ L/min. Liver blood flow is ___ L/min. This affirms its ____ clearance.
3-5 L/min
2-3 L/min
extrahepatic
Remifentanil plasma levels decrease by 50% in…
40 seconds
give as infusion
MAC (minimum alveolar concentration) is reduced with ____ infusion.
remifentanil
Opioid-induced hyperalgesia (OIH)
-paradoxical opioid effect
-pain sensitivity increases during/after escalating opioid treatment
-postop if using remifentanil infusion
-treated/prevented: low dose of ketamine, an N-methyl-D-aspartate (NMDA) receptor antagonist
Treatment of Opioid-induced hyperalgesia (OIH)
Antagonism of the NMDA receptor
(low dose Ketamine)
various mechanisms for OIH
-activation of the central glutaminergic system
-central nitric oxide production
-facilitation of descending pronociceptive systems.
Most piperidines are metabolized by…
CYP 450 enzyme system
most rapidly acting opioid currently available
remifentanil
T/F
Piperidine can anesthetize patients.
False
no amnesia
need other drugs
contains a methyl ester side chain that is metabolized by blood & tissue nonspecific esterases
Remifentanil
not metabolized in liver
ReMi —> Methyl ester chain