E3: Opioids - med specific
Study online at https://quizlet.com/_gulos5
1. List the opioid agonists - sufentanil (500-1000x)
in order of greatest to - remifentanil (100-200x)
least potency. (8) - fentanyl (100x)
- buprenorphine (30x)
(slide 28) - alfentanil (10-20x)
- hydromorphone (5x)
- morphine (1)
- meperidine (0.1x)
2. which type of pain is continuous, dull pain over sharp, intermittent pain
morphine more effec-
tive at treating?
*can treat visceral and somatic pain
3. If you administer mor- dysphoria
phine in the absence of --> morphine has some effects at the kappa receptor
pain, what may occur?
why?
4. how do the peak times IM has a later peak time
compare between IM - IM: 45-90 mins
morphine and IV mor- - IV: 15-30 mins
phine?
5. *** - peak pharmacologic effects lag behind peak plasma concentration
Explain the pharmaco- since the CSF concentrations peaks 15-30 mins after IV injection
kinetics of morphine - CSF concentration decays more slowly
in plasma concentration - less than 0.1% of IV morphine gains access to CSF at the time of peak
and CSF concentration. plasma concentration
(3)
6. *** - poor lipid solubility
why does the peak CSF - high degree of ionization at physiologic pH
, E3: Opioids - med specific
Study online at https://quizlet.com/_gulos5
concentration of mor- - protein binding
phine lag behind the - rapid conjugation with glucuronic acid (immediately undergoes me-
peak plasma concentra- tabolism once we administer drug)
tion? (4)
7. Explain how alkalosis & alkalosis/hyperventilation/hypocarbia:
acidosis affect the plas- - increases nonionized fraction
ma & CSF concentra-
tions of morphine. acidosis/hypoventilation/hypercarbia:
- increased CSF concentration d/t increased CBF
8. T/F: There is signifi- False
cant first-pass uptake of
morphine in the lungs. --> there's rapid accumulation in kidneys, liver, and skeletal muscle
9. What are the effects of - delayed onset of analgesia
a late peak time and - late respiratory depression
slower decay time of
Morphine CSF concen-
trations? (2)
10. how is morphine metab- conjugation = glucuronic acid in liver & kidneys
olized? (2)
elimination = urine, w/ minimal biliary excretion
11. *** Morphine-3-glucuronide (M3G)
Morphine has 2 - 75-85%
metabolites. Differenti- - inactive
ate them. - detectable in plasma 1 min after IV admin
Morophine-6-glucuronide (M6G)
- 5-10%
, E3: Opioids - med specific
Study online at https://quizlet.com/_gulos5
- active
- u receptor agonist
- similar affinity to u receptor, 650x analgesic potency
12. How does elimination elimination of metabolites is longer than unchanged drug
of morphine compared - rapid decrease in plasma concentration of morphine d/t glucoronida-
to morphine metabo- tion
lites differ?
13. Which patient scenar- **renal dysfunction --> M6G accumulation is significant
ios/populations present
metabolism concerns - neonates -> decreased clearance
with Morphine? (5)
- elderly -> maintain higher plasma concentration
- MAOIs -> impairs conjugation
- female gender (greater analgesic potency, prolonged duration, de-
creased Co2 response)
14. *** - stimulation of vagal nuclei in medulla
How does morphine in- - direct depressant effect on SA/AV node
duce bradycardia? (2)
15. *** - decreased venous tone
What are the effects of - variable decreases in SVR, MAP
morphine-induced hist-
amine release?
Study online at https://quizlet.com/_gulos5
1. List the opioid agonists - sufentanil (500-1000x)
in order of greatest to - remifentanil (100-200x)
least potency. (8) - fentanyl (100x)
- buprenorphine (30x)
(slide 28) - alfentanil (10-20x)
- hydromorphone (5x)
- morphine (1)
- meperidine (0.1x)
2. which type of pain is continuous, dull pain over sharp, intermittent pain
morphine more effec-
tive at treating?
*can treat visceral and somatic pain
3. If you administer mor- dysphoria
phine in the absence of --> morphine has some effects at the kappa receptor
pain, what may occur?
why?
4. how do the peak times IM has a later peak time
compare between IM - IM: 45-90 mins
morphine and IV mor- - IV: 15-30 mins
phine?
5. *** - peak pharmacologic effects lag behind peak plasma concentration
Explain the pharmaco- since the CSF concentrations peaks 15-30 mins after IV injection
kinetics of morphine - CSF concentration decays more slowly
in plasma concentration - less than 0.1% of IV morphine gains access to CSF at the time of peak
and CSF concentration. plasma concentration
(3)
6. *** - poor lipid solubility
why does the peak CSF - high degree of ionization at physiologic pH
, E3: Opioids - med specific
Study online at https://quizlet.com/_gulos5
concentration of mor- - protein binding
phine lag behind the - rapid conjugation with glucuronic acid (immediately undergoes me-
peak plasma concentra- tabolism once we administer drug)
tion? (4)
7. Explain how alkalosis & alkalosis/hyperventilation/hypocarbia:
acidosis affect the plas- - increases nonionized fraction
ma & CSF concentra-
tions of morphine. acidosis/hypoventilation/hypercarbia:
- increased CSF concentration d/t increased CBF
8. T/F: There is signifi- False
cant first-pass uptake of
morphine in the lungs. --> there's rapid accumulation in kidneys, liver, and skeletal muscle
9. What are the effects of - delayed onset of analgesia
a late peak time and - late respiratory depression
slower decay time of
Morphine CSF concen-
trations? (2)
10. how is morphine metab- conjugation = glucuronic acid in liver & kidneys
olized? (2)
elimination = urine, w/ minimal biliary excretion
11. *** Morphine-3-glucuronide (M3G)
Morphine has 2 - 75-85%
metabolites. Differenti- - inactive
ate them. - detectable in plasma 1 min after IV admin
Morophine-6-glucuronide (M6G)
- 5-10%
, E3: Opioids - med specific
Study online at https://quizlet.com/_gulos5
- active
- u receptor agonist
- similar affinity to u receptor, 650x analgesic potency
12. How does elimination elimination of metabolites is longer than unchanged drug
of morphine compared - rapid decrease in plasma concentration of morphine d/t glucoronida-
to morphine metabo- tion
lites differ?
13. Which patient scenar- **renal dysfunction --> M6G accumulation is significant
ios/populations present
metabolism concerns - neonates -> decreased clearance
with Morphine? (5)
- elderly -> maintain higher plasma concentration
- MAOIs -> impairs conjugation
- female gender (greater analgesic potency, prolonged duration, de-
creased Co2 response)
14. *** - stimulation of vagal nuclei in medulla
How does morphine in- - direct depressant effect on SA/AV node
duce bradycardia? (2)
15. *** - decreased venous tone
What are the effects of - variable decreases in SVR, MAP
morphine-induced hist-
amine release?
