opioids

Question 1

opioid MOA

Answer 1

hyperpolarize nerve cells (open K+ channels)

inhibit NT release (block Ca2+ channels)

Question 2

opioid OD

Answer 2

pinpoint pupils

Question 3

endorphins

Answer 3

mu receptor

euphoria

Question 4

dynorphins

Answer 4

kappa receptor

dysphoria

Question 5

opioid SE

Answer 5

sedation
respiratory depression
anti-tussive
nausea/vomiting
constipation
miosis
urinary retention
biliary spasm
pruritis
orthostatic hypotension
prolong labor
bronchoconstriction

Question 6

morphine absorption

Answer 6

first pass metabolism

Question 7

morphine distribution

Answer 7

all body tissue

Question 8

morphine metabolism

Answer 8

conjugated in liver to glucronide

Question 9

morphine excretion

Answer 9

urine

Question 10

morphine toxicity

Answer 10

pinpoint pupils
respiratory depression
coma

tx:
establish airway
opioid antagonists

Question 11

morphine tolerance

Answer 11

downregulation of opioid receptors

Question 12

morphine abuse

Answer 12

euphoria

Question 13

morphine withdrawal

Answer 13

abstinence syndrome (CNS overactivity)

tx:
methadone
buprenorphine
clonidine
naltrexone

Question 14

morphone contraindications

Answer 14

COPD
asthma
increased ICP
pregnant
liver/kidney disease
hypotension

Question 15

meperidine vs morphine

Answer 15

less potent
shorter duration of action
less GI/biliary/uterine effect
anti-muscarinic effects (dilates pupil)

Question 16

meperidine toxicity

Answer 16

normeperidine causes serotonin syndrome

Question 17

fentanyl

Answer 17

highly potent
rapid onset
short duration

Question 18

fentanyl use

Answer 18

surgery
labor
cancer (transdermal patch, lozenge)

Question 19

fentanyl metabolism

Answer 19

CYP3A4

Question 20

fentanyl analogues

Answer 20

potent
rapid onset
short duration

sulfentanil
alfentanil
remifentanil

Question 21

methadonen use

Answer 21

chronic pain

opioid dependence

Question 22

oxycodone use

Answer 22

moderate/severe pain

opioid-tolerant pts (sustained release formulation)

Question 23

codeine metabolism

Answer 23

metabolized to morphine (CYP2D6)

Question 24

codeine use

Answer 24

antitussive

mild/moderate pain

Question 25

diphenoxylate use

Answer 25

use: diarrhea

low abuse potential

Question 26

pentazocine MOA

Answer 26

kappa agonist

weak mu antagonist

Question 27

pentazocine use

Answer 27

pain
pre-anesthetic
induce withdrawal

Question 28

pentazocine SE

Answer 28

psychomimetic effects
hallucination
ceiling effect

Question 29

buprenorphine

Answer 29

20x more potent than morphine

Question 30

buprenorphine MOA

Answer 30

partial mu agonist
kappa antagonist

long duration
precipitates withdrawal in morphine users

Question 31

buprenorphine SE

Answer 31

respiratory depression

Question 32

tramadol MOA

Answer 32

weak mu agonist

inhibit reuptake of NE and serotonin

Question 33

tramadol use

Answer 33

moderate pain

chronic neuropathic pain

Question 34

tramadol SE

Answer 34

respiratory depression

seizures

Question 35

naloxone

Answer 35

opioid antagonist

ineffective orally
first-pass metabolism to glucuronide

use: opioid overdoes

Question 36

naltrexone

Answer 36

opioid antagonist

high oral bioavailability
long duration of action
SE: CV

use: opioid dependence, alcoholism

Question 37

dextromethorphan

Answer 37

NMDA antagonist (antitussive)
metabolized by CYP2D6