opioids

Question 1

analgesics

Answer 1

drugs that relieve pain WITHOUT loss of conciousness

Question 2

opioid

Answer 2

a drug that has actions similar to morphine

Question 3

endogenous opioid peptides

Answer 3

have opioid- like properties

found in cns and peripheral tissue

Question 4

3 main receptors

Answer 4

mu

kappa

delta

Question 5

most important opioid receptor to opioids.

Answer 5

MU

Question 6

Mu receptor response to activation

Answer 6

Analgesia
Euphoria
Respiratory Depression\
related to physical dependence

Question 7

Kappa receptors response to activation

Answer 7

analgesia and sedation

Question 8

three groups of opioids

Answer 8

1) pure opiod agonists

2) agonist-antagonist opiods

3) pure opiod antagonists

Question 9

pure opioid agonists

Answer 9

produce similar response to endogenous opioids
- analgesic euphoria
- sedation
-physical dependence
- respiratory depression

Question 10

2 groups of pure opioid agonists

Answer 10

1) strong opioid agonist (morphine)

2) moderate to strong opioid agonists

Question 11

agonist-antagonists opioids

Answer 11

administered alone = low level analgesia

administered with pure agonist = blocks pure agonists
- decrease analgesia

Question 12

pure opioid antagonists

Answer 12

acts as antagonists on mu and kappa receptors
- stops receptor from activating a response

REVERSAL of resp. and CNS depression caused by opioid agonist overdose

Question 13

common opioid antagonists

Answer 13

NALOXONE

Question 14

Pure agonists

Answer 14

Morphine

Question 15

morphine pharmalogic effects

Answer 15

analgesia
sedation
euphoria
resp depression
cough suppression

Question 16

morphine source

Answer 16

poppy plant

extract from opium

contains codeine (analgesic)
and papaverine (smooth muscle relaxant)

Question 17

Pharmacological Actions

Answer 17

analgesic

sense of well-being

reduces anxiety

mental clouding

• respiratory depression, urinary retention
• prolongued use = physical tolerance and physical dependence

Question 18

Morphine Therapeutic Uses

Answer 18

relief of moderate to serve pain without unconsciousness

Question 19

Mechanism of Analgesic action

Answer 19

mimics endogenous opiods at mu

Question 20

morphine adverse effects

Answer 20

Resp depression: ++ cause of overdose death
may last 4-5 hrs
Chronic use = resp tolerance occurs

Constipation- by activating me receptors in gut

Orthostatic hypotension
- blunts barocrecptor reflex and dilate arterioles and veins

Urinary retention
- increase tone sphincter and detrusor muscle

Cough Supression
- -acts on opioid receptors in medulla

Question 21

When should morphone not be used?

Answer 21

if resp rate is less than 12 breaths per minute

Question 22

How do you reverse morphine overdose

Answer 22

Naloxone

Question 23

Morphine pharmocokinetics

Answer 23

poor lipid solubility

cant cross BBB easily
- only a fraction reaches analgesic recptors

PO= ++ inactivated First Pass

Tolerance= analgesia, euphoria, sedation, resp depression

Question 24

Physical dependence of morphine

Answer 24

abstinence syndrome occurs when drug stopped due to cellular changes - once changes occur, body needs constant opioids to function normally

Question 25

How long do opioid withdrawals last? management?

Answer 25

Exterme but not LETHAL - begins 5 hours after final dose/ lasts 7-10 days withdrawal gradually - progressively smaller doses over 3 days

Question 26

Morphine Toxicity

Answer 26

classic triad -coma - resp. depression - pinpoint pupils

Question 27

treatment for opioid toxicity

Answer 27

ventilatory support opioid antagonist

Question 28

fentanyl

Answer 28

transdermal - drug placed on skin and is absorbed into blood stream trans mucosal: intranasal, buccal, rectal, sublingual bucal: between gums and cheek

Question 29

Methadone

Answer 29

used to treat opioid addiction

Question 30

methadone adverse effects

Answer 30

prolongs QT interval= potentially fatal dysthmia's

Question 31

strong opioid agonists

Answer 31

morphine (prototype) fentanyl methadone (treats opioid addiction)

Question 32

moderate to strong opioid agonists

Answer 32

less anglgesia, resp depression, lower potential for abuse Codeine

Question 33

Codeine

Answer 33

For mild- moderate pain 10% converted to morphine in liver cough suppressant

Question 34

Pure antagonist function and therapeutic uses

Answer 34

Block effects of opioid agonists treat opioid OVERDOSES relief opioid induced CONSTIPATION Reversal POSTOPERATIVE opioid effects Mgmt opioid ADDICTION

Question 35

Naloxone mechanism

Answer 35

reverses effects of opioid agonists

Question 36

how is Naloxone administered and elimiated?

Answer 36

IV IM Intranasally SubQ Elimination: liver

Question 37

Naloxone therapeutic uses

Answer 37

reversal of opioid overdose initiate with a series of small doses until crisis has passed reversal neonatal resp depression during birth

Question 38

Opioid antagonist

Answer 38

Narcan Methylnaltrexone Naloxegol Naldemedine Naltrexone

Question 39

Methylnaltrexone Naloxegol Naldemidine

Answer 39

selective mu receptor antagonists opiod-induced constaptation relief--> try other measures first work in periphery - Do not block CNS

Question 40

Naltrexone

Answer 40

PO, IM opioid abuse- prevent euphoria alcohol abuse- prevent buzz

Question 41

Non- Opioid centrally acting analgesics

Answer 41

Tramadol

Question 42

Tramadol

Answer 42

moderately stong analgesic low potential for dependence/ resp depression

Question 43

tramadol mechanism of action

Answer 43

weak action of mu receptors - works primarily by blockinh uptake of norepinephrine and serotonin --> inhibitory effects on pain transmission in spinal cord less effective than morphine more effective than codeine