B6.017 - Opiods

Question 1

name the weak opiods

Answer 1

Oxycodone
Hydrocodone
Codeine
Tramadol
Tapentadol

Question 2

describe oxycodone

Answer 2

one of the most popular
schedule 2
1.5 morphine

Question 3

hydrocodone

Answer 3

slightly less potent than oxy
poor metabolizers can accumulate
schedule 2

Question 4

codeine

Answer 4

200x less affinity for mu receptor
CYP metabolized
Codeine APAP schedule 3
contraindicated in pts <18 bc resp depression/death

Question 5

tramadol

Answer 5

schedule 4
weak mu agonist inhibits NE and serotonin uptake
6000 x less affinity

Question 6

tapentadol

Answer 6

schedule 2
stronger mu opiod agonist and NE inh that works both ascending and descending pathways
2-3x less potent
50x less affinity
can increase serotonin but not directly

Question 7

name the strong opiods

Answer 7

1. meperidine
2. morphine
3. oxycodone
4. oxymorphone
5. hydromorphone
6. methadone
7. buprenorphine
8. fentanyl
9. sufentanil
10. alfentanil
11. remifentanil

Question 8

features of meperidine

Answer 8

IM
can lead to CNS hyperactivity/seizures
1/10 morphine
cardiac (orthostatic hypoTN, Myocardial depression)
anticolinergic
local anesthetic
coadmin with monoamine reuptake inhibitors can be fatal

Question 9

morphine

Answer 9

lost of ways to give it
morphine 3 - glucu metabolite has no opiod receptor activity
morphin 6 -glucu agonist sustains analgesia, etc.
longer BBB transit

Question 10

oxycodone

Answer 10

long acting, and higher acting preparations
abuse deterrent preparations
rapid onset of action
more potent than morphine
fewer side effects

Question 11

oxymorphone

Answer 11

semisynthetic
IR SR
10x morphine
fast
higher delta opiod receptor activity
low bioavail
alcohol can increase plasma concentration by 300%

Question 12

hydromorphone

Answer 12

analog of morphine formed by N demethylation of hydrocodone
short or long acting
5-7x morpine
active metabolite doesnt stop pain but can cause neurotoxicity

Question 13

methadone

Answer 13

used for pain but also in opiod disorder, heroin addiction maintenance
fast onset
QT prolongation, v dangerous
weak NMDA antagonism

Question 14

buprenorphine

Answer 14

alternative to methadone maintenance
often with naloxone
full agonist at mu for pian, partial at mu for respiratory depression
antagonist at kappa delta
blocks other opioids from binding, higher dose full mu may be necessary can also precipitate withdrawal if given to someone on full mu regimen

Question 15

fentanyl

Answer 15

mostly mu, little kappa delta
75-125x
transdermal buccal only for opioid tolerant
less constipation bc doesn’t pass thru GI can be used for pts with gut resorption issues
IR preps v rapid and potent you gotta train to give
PATCHHHHH

Question 16

sufentanil

Answer 16

mostly perioperative IV
rapid, short 
5-7x fentanly
dose dependent skeletal muscle rigidity
heroin deaths due to mix

Question 17

alfentanil

Answer 17

operatively given

smaller vol, low prob of accumulation

Question 18

remifentanil

Answer 18

most potent mu opiod receoptor
used for anesthesia
not met by liver (kidneys)
ester side chain linkage leads to rapid degradation by tissue and plasma esterases