Psych: Opiates Flashcards
Which receptor produces all: analgesia, respiratory depression, sedation, euphoria, dependence, and constipation?
Mu
Kappa only causes analgesia, sedation, and constipation
MOA of morphine, codeine, hydrocodone, and meperidine?
Mu and kappa pure agonists
MOA of pentazocine
Mu antagonist
kappa agonist
MOA of butorphanol?
Mu partial agonist
Kappa agonist
MOA of buprenorphine
Mu partial agonist
Kappa antagonist
MOA of nalaxone and naltrexone?
Mu and Kappa antagonists
Why are larger oral doses needed compared parenteral doses needed for the same effect?
Larger oral doses due to first pass metabolism
-conjugation
With prolonged use of opioids what do you develop?
Tolerance
-only to analgesia, euphoria, and sedation and resp depression
Physical dependence
What does not develop tolerance when using opiods?
Constipation and miosis
What drugs/other meds should you avoid when on opiods?
Alc and other CNS depressants
Also avoid anticholinergic drugs
-exacerbate adverse effects
What is the triad of opioid overdose?
Coma, respiratory depression, and PINPOINT pupils
How much stronger is fentanyl than morphine?
100x more potent
ROI of fentanyl?
IM, IV, transdermal, transmucosal, nasal spray, lozenge, buccal tablets
LOTS
Clinical use of alfentanil/remifentanil/sufentanil?
Induction and maintenance of anesthesia
Is remifentanil quick or slow onset?
Rapid onset with brief duration
Why is meperidine use declining?
Short half life
Adverse interactions with other drugs
Toxic metabolite
Does meperidine cause the pinpoint pupils seen in other opioids?
Nope
Besides mu opoids agonist, what other receptor does methadone work at?
NMDA antagonist
Does methadone have long or short duration of action?
Long
Which opioid causes QT prolongation?
Methadone
How is hydromorphine different than plain old morphine?
More water soluble
-so can be diluted for injection
10% of codiene is broken down into morphine by which CYP?
CYP2D6
-required for analgesic effects
Which two opioids are used as cough suppressants?
Codeine and dextromethorphan (does not bind Mu)
Which CYP metabolizes oxycodone?
CYP3A4
What is the treatment for opioid overdose?
Naloxone
-can cause immediate withdrawal effects
How is naltrexone useful in opioid addiction?
Prevents euphoria seen
How is naltrexone useful in alcohol addiction?
Reduces craving and heavy drinking
MOA of methylnaltrexone?
mu opioid antagonist
-doesnt cross BBB
Clinical use of methylnaltrexone?
Opioid induced constipation
MOA of loperamide?
Mu opioid agonist
-does not cross BBB
Clinical use of loperamide?
Acute and chronic diarrhea
What happens if you ingest loperamide in large quantities?
Can cuase torsades de pointes
Which drugs should you not use with renal insufficiency?
Meperidine and codeine
Which drugs should you not use with hepatic insufficiency?
Meperidine, codeine, and methadone
What adverse effects can happen if you combine opioids with anticholinergic?
Increased constipation and urinary retention
What adverse effects can happen if you combine opioids with MAOIs?
Hyperpyrexic coma