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Opioid analgesics and antags
Pharmacology
25
Medical
Professional
02/04/2012

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Cards

Term
mu receptor
Definition
supraspinal analgesia
miosis
resp depression
euphoria
physical and behav dependence
Term
kappa receptor
Definition
spinal analgesia
weak miosis
sedation
Term
these have a high affinity for delta receptors
Definition
Met and Leu enkephalin
Term
has a high affinity for delta and mu rec
Definition
Beta endorphins
Term
has a high affinity for delta and mu rec
Definition
Beta endorphins
Term
high affinity for kappa
Definition
sigma
Term
opiate affect on resp depression
Definition
decreased response to CO2 and dec automaticity
Term
opiate effect on miosis
Definition
stimulation of Edinger westphal nucleus

**Meperidine is exception**
Term
opiate effects on GI
Definition
increased tone and decreased motility
Term
this increases potency of opiates
Definition
acetylation at 3 and 6
Term
this produces antags in opiates
Definition
allyl substitutions
Term
this greatly increases potency
Definition
stabilizing the C ring
Term
morphine
Definition
standard IM analgesic
Term
Heroin
Definition
5-10 more potent than morphine
great lipid solubility
Term
methadone
Definition
good oral analgesic

maintenance med
Term
meperidine
Definition
short duration of action
anti-cholinergic effects

metabolite is excitatory and cannot be treated by antags
Term
fentanyl
Definition
VERY potent and short acting
stimulant in horse racing
Term
hydrocodone
Definition
cough suprressant
Term
propoxyphene
Definition
dextro form is active
Term
pentazocine
Definition
antag/partial ag at mu

activation of kappa receptors
Term
buprenorphine
Definition
antag at kappa receptor


alternative in methadone maintenance
Term
tramadol
Definition
weak partial ag at mu
release serotonin
blocks norep uptake

**RLS, acid reflux, and fibromyalgia**
Term
Naloxone
Definition
mu antag
blocks kappa at higher doses
precipitation of w/d
Term
naltrexone
Definition
longer acting antag
maintenance therapy who are not physcially dependent
Term
opioid treatment of diarrhea
Definition
loperamide and diphenoxylate
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