What are the Endogenous Opioids?
Endorphins
Enkephalins
Dynorphins
Endomorphins
Endomorphins receptor?
Mu
Dynorphins receptor?
Kappa
Enkephalins receptor?
Delta
Heroine is converted to?
Morphine
Difference between Heroin and Morphine?
Heroin= 2-4x more potent
crosses BBB faster
What drug is available as a suppository?
Hydromorphone
Hydromorphone potency? duration?
Hydro=
8-10x more potent
shorter duration
What drug is the same as hydromorphone?
Oxymorphone
Codeine potency? efficacy?
Codeine=
1/10 the potency of morphine
lower efficacy
What is Codeine converted to?
morphine
-> by CYP450 2D6
Oxycodone potency?
10x potency of Codeine
What mixtures contain Codeine?
Acetaminophen
NSAID
What are the Synthetic Compounds?
Meperidine
Fentanyl
Methadone
Meperidine potency? Duration?
1/8th potency of morphine
short
Meperidine SE?
toxic metabolite builds up
= seizures
Advantages of Meperidine?
dec SM spasms than Morphine
no miosis
Fentanyl potency? Onset? Duration?
80-100x potency of morphine
fast onset
short duration
How is Fentanyl administered?
I.v. for anesthesia
Methadone potency?
I.v. potency similar to morphine
oral= 4x more potency
Methadone Tx?
narcotic dependence
Methadone duration?
inc w/ repeated use
What are the Opioid Antagonists?
Naloxone
Naltrexone
Methylnaltrexone
Naloxagol
What are signs of OD?
stupor, coma
RR low
pinpoint pupils
low body temp
placid SM, jaw relaxed