opioid analgesia Flashcards
side effects of opioids
- nausea
- pruritis/flushing/ sweating
- respiratory depression
opioid analgesics MOA
agonist to Mu, kappa and delta receptors which mediate main effects of endorphins
central pharmacodynamic effects with opioid analgesics (5)
- analgesia
- sedation
- mood alterations
- miosis
- seizures
- respiratory depression
- N/V (direct stim. of CTZ)
- cough suppression
do opioids have antipyretic or anti-inflammatory effects?
Nope, they might even raise the core temp
peripheral pharmacodynamic effects of opioid analgesics
- delayed gastric emptying and slowed intestinal transit
2. vasodilation (due to histamine release)
more lipohilic the opioid agent is ….
the more likely it will have an effect on the reward pathway
peripheral tolerance for SE of opioids?
yep except constipation
more recent potential concerns of opioid analgesics
- serotonin syndrome
- adrenal insufficiency
- androgen deficiency
diacetylmorphine
heroine- derived from morphine
codeine is a prodrug for
morphine
- needs to be converted to have analgesic effect
codeine duration of action
short: 4-6 hr
oxycodone short or long acting?
shortduration but there are formulas with extended release like oxycontin
methadone
long acting my receptor agonist used as a opioid withdrawal maintenance.
underlying risk of methadone
QT prolongation
meperidine
short acting otherwise it will accumulate as nor-meperidine which causes tremors and seizures and there is the potential for serotonin syndrome
diphenoxylate and loperamice
have activity in the bowel and thus is used to slow transit time and treat diarrhea
***** diphenoxylate has the potential if in high doses to produce analgesia effect but no penetration in CNS
loperamide has what possibility to happen in excess
cardiotoxicity
fentanyl
approx. 80-100x as potent as morphine, incredible dangerous. In a clinical setting it is either used as parenteral or transdermal
***it does not get absorbed orally
naloxone
binds to the mu- receptor with high affinity with quick onset but short duration (to minimize the effect of withdrawal)
opioid withdrawal
- diaphoresis
- abdominal cramping, diarrhea
- nausea and vomiting
- tachycardia
- agitation
Mixed Agonist-Antagonist Agents
Bind to mu & kappa receptors, acting as either agonists or antagonists
Can block activity of other opioids at mu- receptors
Adverse effects:
Sedation, dizziness, nausea
May induce acute w/drawal from other opioids
PAMORAs (peripheral opioid receptor antagonist)
used when another opioid is causing constipation
buprenorphine (suboxone)
withdrawal maintenance partial agonist
Weak mu-opioid receptor agonist
Also inhibits re-uptake of serotonin & norepinephrine
tramadol