opiods

Question 1

Full opioid agonists

Answer 1

morphine
fentanyl
heroin
methadone

Question 2

partial opioid agonists

Answer 2

codeine
hydrocodone
oxycodone

Question 3

mixed agonists/antagonists

Answer 3

buprenorphine

Question 4

antagonisits

Answer 4

naloxone

Question 5

weak opioid agonists/reuptake inhibitors

Answer 5

tramadol

tapentadol

Question 6

tramadol

Answer 6

serotonin uptake blocker
NE uptake blockers
weak mu-R agonist

Question 7

tapentadol

Answer 7

weak muR agonist and NE reuptake blocker

Question 8

narcotic

Answer 8

archaic term

more legal then medical referring to any substance that produces stupor associated with analgesia

Question 9

opiates

Answer 9

natural products and derivatives obtained from opium poppy

• opium
• morphine
• heroine
• codeine

Question 10

opiods

Answer 10

class of compounds that bind to opioid R 
includes agonists, antagonists, partial agonists, and mixed agonists/antagonists

Question 11

endogenous opioid agonists

Answer 11

endorphin
enkephalines
dynorphins

Question 12

muRs

Answer 12

endorpins>enkepalins>dynorphins
supraspinal and spinal analgesia
sedation
inhibition of respiration 
slowed GI transit
modulation of hormone and neurotransmitter release

Question 13

kappa Rs

Answer 13

enkephalins>endorphins=dynorphins
supraspinal and spinal analgesia
modulation of hormone and neurotransmitter release

Question 14

deltaRs

Answer 14

dynorphins>endorphins>enkephalins

Question 15

other Rs

Answer 15

sigma
TLR-4
ORL-1

Question 16

ORL-1

Answer 16

orphan opioid R like
cloned ‘orphan R’
similar structure to opioid R
different fnx (no effec on pain, hyperalgesia, or inflammation)
different ligands - nocipetin = orphanin FQ

Question 17

opioid Rs

Answer 17

all GPCRs
inbitis cyclic AMP
open G-protien modulated KChS -> hyperpolarization
reduce presynaptic Ca influx inhibiting NT release

Question 18

brain stem

Answer 18

opioid R influence respiration, cough, nausea, vomiting, BP, pupillary diameter, stomach secretion

Question 19

medial thalamus

Answer 19

mediates deep pain that is poorly localized

Question 20

spinal cord

Answer 20

receipt and integration of incoming sensory information, activation of these R attenuates painful afferent stimuli

Question 21

hypothalamus

Answer 21

affect neuroendocrine secretion

Question 22

limbic system

Answer 22

high density of opioid Rs in amygdala

Question 23

periphery

Answer 23

peripheral sensory nn fibers and nn terminals inhibit Ca influx and release of excitatory and pro-inflammatory substances

Question 24

immune cells

Answer 24

have opioid Rs, but fnx is unknown

Question 25

major efects of activating mu

Answer 25

``` analgesia euphoria miosis respiratory depression physiological dependence reduced GI motility ```

Question 26

major efects of activating kappa R

Answer 26

``` less abuse potential and physical dependence dysphoria psychotomimetic less miosis and respiratory depression then mu analgesia sedation vasodilation increased urinary output ```

Question 27

miosis

Answer 27

d/t indirect parasympathetic actions little or no tolerance develops against this almost all other causes of coma cause mydriasis

Question 28

opioids and CV system

Answer 28

no major effects on BP or heart rate b/d of respiratory depression and CO2 retention cerebral vessels dilate -> increased ICP therefore use is CI in severe brain injury

Question 29

opioids and Histamine

Answer 29

opioids release H2 from mast cells | CI in asthmatics

Question 30

opioids and first pass

Answer 30

variable morphine- very high codeine and oxycodone less

Question 31

opioids and pregnancy

Answer 31

do cross placental barrier therefore CI

Question 32

fentayl PK

Answer 32

``` highly lipophilic slowly metabolized but short acting b/c distributes to fatty tissues 100x more potent then morphine IV, epidural, intrathecal ```

Question 33

morphine

Answer 33

``` binds all opioid Rs highest affinity for mu low oral availability high efficacy for analgesia high abuse potential ```

Question 34

uses of morphine

Answer 34

analgesic- best with severe, constant pain acute pulmonary edema acute MI

Question 35

morphine and acute pulmonary edema

Answer 35

reduced perception of SOB anxiolytic effects reduction in cardiac preload and afterload

Question 36

opioids and cough suppression

Answer 36

low doses maybe d/t activation of sigma R dextromethorphan codeine

Question 37

opioids and diarrhea

Answer 37

low doses loperamide (cannot X BBB) diephnoxylate (+atropine) difenoxin (+atropine)

Question 38

uses of fentanyl

Answer 38

epidural for labor | oral transumucosal and patch for CA pts

Question 39

methadone

Answer 39

synthetic, PO effectice opioid equally potent as morphine, but induces

Question 40

meperidine

Answer 40

syntheitic opioid used for acute pain binds both mu and kappa respiratory depression DILATES pupils not useful for diarrhea or cough less effects on smooth mm (can be used in obstetrics) toxic metabolite causes seizures so cannot be used >48hrs

Question 41

heroin

Answer 41

schedule I 3x more potent then morphine greater lipid solubility so more CNS effects more exaggerated euphoria

Question 42

codeine

Answer 42

mu effects w/low doses | kappa effects w/high doses

Question 43

hydrocodone

Answer 43

relatively pure mu actiavtion

Question 44

oxycodone

Answer 44

relatively pure mu derivative of codeine high PO effects sustained release product (oxycotin)

Question 45

bupreoprhine

Answer 45

mixed opioid agonist/antagonists depends on R subtype partial agonist at mu major use is for opioid detox

Question 46

mixed opioid agonist/antagonists

Answer 46

can precipitate withdrawl symptoms

Question 47

naloxone

Answer 47

``` opioid antagonist short acting used to Tx opioid overdose precipitates withdrawal syndrome can be used to Tx drug-fee addicts ```

Question 48

primary symptoms of opioid overdose

Answer 48

triad: lethargy/coma depressed respiration pinpoint pupils

Question 49

secondary symptoms of opioid overdose

Answer 49

``` hypotension hypothermia w/cold or clammy skin pulmonary edema convulsions hypoxia w/dilated pupils ```