Opioid Agonists-Antagonists Flashcards
if a pt has pure opioid agonist intolerance we can give them
opioid agonist-antagonists
a-a’s have partial to no effect on these receptors
mu
a-a’s have partial effects here causing dysphoria
kappa and delta
advantages of using a-a’s
analgesia, decreased physical dependence, decreased RD, and ceiling effect
pentazocine has agonist effects on _____ and ______ and has weak _______ effects
kappa and delta; antagonist
due to some antagonism, pentazocine may cause
withdrawal symptoms
pentazocine has extensive
hepatic first pass effect (80%)
e 1/2 time of pentazocine
2-3 hours
excretion of pentazocine
kidneys; glucoronidation
pentazocine has a shorter duration than morphine in
epidurals
common s/e of pentazocine
sedation, sweating, dizziness, and dysphoria; catecholamine release causing increases in hr, bp, PA bp, and LVEDP
pentazocine crosses the _____ barrier
placental
high doses of pentazocine may cause
feeling of impending death
pentazocine may be used for
moderate chronic pain relief
butorphanol is more potent than
pentazocine
butorphanol affinities? what will this cause?
low mu, low sigma, moderate kappa; less dysphoria and more analgesia and anti shivering effects
we have rapid and complete absorption when we give butorphanol
IM
butorphenol e 1/2 time
2.5-3.5 hours
butorphanol elimination
more in bile than urine
unique s/e of butorphenol
sweating, still has dysphoria
caution with butorphenol
difficult to use with other opioid agonists
nalbuphine is equally potent to
morphine
nalbuphine is a ___ agonist
mu
e 1/2 time of nalbuphine
3-6 hours
unique cv trait of nalbuphine
great for cardiac cath patients d/t no cv effects
nalbuphine has ____ s/e than the other opioid agonists/antagonists
less
buprenorphine has a ___x greater effect on ____ receptors than morphine
50; mu
onset of buprenorphine
30 mins
buprenorphine has a prolonged resistance to
naloxone
duration of buprenorphine
8 hours
uses of buprenorphine
post op, cancer, renal colic, MI; epidural
unique s/e of buprenorphine
pulmonary edema
nalorphine is not used clinically because of it’s
high incidence of dysphoria with sigma receptors
naloxone may not be effective in reversing
bremazocine
dezocine has no
cv effects
meptazinol acts selectively on
mu1 receptors
