Lecture 8 - Opioids Flashcards Preview

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Flashcards in Lecture 8 - Opioids Deck (165)
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1

Describe the analgesic pain ladder:
Step 1 - Mild

*non-narcotics*
1st choice = ASA
Alternatives = acetaminophen or NSAID

2

Describe the analgesic pain ladder:
Step 2 - Mild to Moderate

*non-narcotics + weak narcotics*
1st choice = ASA + codeien
Alternatives = codeine or Acetaminophen + codeine

3

Describe the analgesic pain ladder:
Step 3 - Moderate to Severe

*moderate strength narcotics*
1st choice = codeine or morphine
Alternatives = oxycodone, levorphanol, anileridine, oxymorphone

4

Describe the analgesic pain ladder:
Step 4 - Severe

*strong narcotics*
1st choice = morphine
Alternatives = methadone, hydromorphone

5

List 3 endogenous opioids

-endorphines
-enkaphalins
-dynorphins

6

Describe endorphins

-from pituitary and hypothalamus
-polypeptides
-from poropiomelanocortin and prodynorphin
-potent analgesics

7

Describe enkephalins

-from proenkephalin and prodynorphin
-pentapeptide ligands
-involved in modulated pain response

8

Describe dynorphins

-from proenkephalin B
-polypeptides
-physiological role not yet understood

9

Are opioids direct neurotransmitters?

No - they just make the neuron more likely to fire - but are not directly neurotransmitters

10

Describe the 3 Mechanisms of action?

1 - hyper polarization of nerves by opening K+/Ca2+ channels in 1st (receptor to medulla) and 2nd order neurons (medulla to thalamus)

2 - inhibition of ascending pathways in the CNS

3 - excitation of descending adrenergic and seratonergic pathways

11

What can opioids be used for?

-pain control
-sedation and anxiolysis
-can be used before anesthesia

12

What is the #1 cause of opioid death?

depression of respiration

13

List the 7 pharmacological effects of opioids

1 - inhibition of pain and pain perception
2 - sedation and anxiolysis
-drowsiness and lethargy
-cognitive impairment
-relaxation inhibition of pain
3 - depression of respiration (main cause of death from opioid overdose)
4 - cough suppression (opioids suppress the cough centre in the brain)
5 - reduction of intestinal motility (codeine used to treat diarrhea)
6 - pupillary constriction (KEY SYMPTOM OF OVERDOSE)
7 - nausea and vomiting (first stimulated, then inhibited)

14

_____ are used for pain, diarrhea, coughing, panic breathing (COPD)

opioids

15

What 3 things do we dose opioids by ?

by the mouth
by the clock
by the ladder

16

Briefly explain the WHO pain ladder (slide 8)

0-3: mild pain
-acetaminophen
-NSAIDs
-maybe caffeine

4-6: moderate pain
-codeine (mild opioid)

7-10: severe pain
-morphine (strong opioid)

17

If you are increasing to a stronger or different pain med, do you discontinue the original medication?

no
never
not in a million years

**never stop the lower pain control!
-pain meds work by different mechanisms so you always want to keep the pain controlled and don't want to take away any form of pain management

18

By the mouth:
-Oral dosing is ___ effective than IV

less

*because of first pass metabolism

19

Describe 3 points of by the mouth

1 - oral dosing has longer term effect requiring less frequent doses
2 - oral dosing avoids the highs and thus is less addictive
3 - oral dosing is safer in terms of overdose

20

Describe 3 points of by the clock

1 - uses less drug. It takes more drug to bring pain down than it does to maintain a person pain-free (maintain dosing)
2 - avoids the euphoria associated with release of pain, so less addictive potential
3 - avoids the development of chronic pain syndrome (from pain pathway rewirling)

21

What is the #1 problem with dosing by the clock?

Pt does not want to comply because they do not feel pain and do not want to become addicted

*have to explain to pt that by dosing by the clock, you are actually reducing risk of addiction

22

Describe points of by the ladder

1 - it assures that the safest and least potent drug required for any specific case is used
2 - avoids addictive potential because opioids (and strong opioids) are not used until required

23

_____ - weakest commonly used opioid and has the least addiction risk

codeine

24

codeine has ___% of potency of morphine

10

25

Potency of codeine is so ___, it is has it's own special step on the pain ladder (possibly now shared with tramadol)

low

26

What is codeine used for?

pain
diarrhea
coughing
inhibit breathing

27

_____ = unique weak opioid agonist

tramadol

28

What is the main downside to tramadol?

expensive

29

Unlike other opioids, tramadol has two complementary mechanisms: describe them

1 - like other opioids, activates the micro-opioid receptor

2 - weak inhibitor of norepinephrine and serotonin reuptake

30

Tramadol has ____ potential for addiction and shows greater pain control

less