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PHAC II > 3. Opiods > Flashcards

3. Opiods Flashcards

1
Q

What are the 3 types of endogenous opiods?

A
  • endorphins
  • enkephalins
  • dynorphins
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2
Q

Where are endorphins produced?

A

in the pituitary and hypothalamus

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3
Q

What type of drugs imitate endophins?

A

opiods

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4
Q

How do opiods affect the pain signal?

A
  • can excite inhibitory neurons

- can inhibit the pain stimulus coming up the spinal cord

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5
Q

What is the mechanism of action of opiods?

A

They cause hyperpolarization of nerves by opening K+/Ca2+ channels

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6
Q

What is the most important opiate receeptor when it comes to pain?

A

Mu

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7
Q

What would happen if a person had no mu receptors?

A

Opiates would not work and they would feel higher levels of pain.

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8
Q

Morphine, codeine, hydrocodone, oxycodone and hydromorphone are all ____________ derivatives.

A

Phenanthrene

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9
Q

Merperidine, fentanyl and sufentanil are all ___________ derivatives.

A

Phenylpiperidine

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10
Q

Methadone is a ____________ derivative

A

Diphenylheptane

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11
Q

What is diacetyl morphine also known as?

A

heroin diamorphine

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12
Q

Where can you find a natural source of opiates?

A

in the opium poppy

papaver somniferum

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13
Q

Why is diacetyl morphine so addictive?

A

Because it is 10x more lipid soluble than morphine (gets into the brain quicker)

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14
Q

What are 7 pharmacological effects?

A
  • inhibition of pain and pain perception
  • sedation and anxiolysis
  • depression of respiration
  • cough suppression
  • reduction of intestinal motility (useful for diarrhea)
  • pupillary constriction
  • nausea and vomiting
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15
Q

What should you look for in a pt if you suspect opiate overdose?

A
  • respiratory paralysis
  • reduced judgement
  • reduced cognitive ability
  • pupil constriction***
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16
Q

What is clinically useful about respiration reduction caused by opiates?

A

If a pt has a lung disorder, opiates can reduce their resp. rate to bring them more comfort.
Only used in pts that are going to die soon.

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17
Q

What are the 4 opiod uses?

A
  • pain
  • diarrhea
  • coughing
  • “panic” breathing (COPD)
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18
Q

What are the 3 dosing methods for pain?

A
  • by the mouth
  • by the clock
  • by the ladder
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19
Q

If you have a pain level of 0-3, what type of pain is this and what therapy should be given?

A

mild pain

acetaminophen

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20
Q

If you have a pain level of 4-6, what type of pain is this and what therapy should be given?

A

Moderate pain

Codeine

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21
Q

If you have a pain level of 7-10, what type of pain is this and what therapy should be given?

A

Severe pain

Morphine

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22
Q

Although oral dosing is LESS effective than IV, what are 3 benefits of oral dosing?

A
  1. Longer term effect –> less frequent doses
  2. Avoids the “highs” –> less addictive
  3. Safer in terms of overdose
23
Q

What does “by the clock” dosing imply?

Why is this a good dosing plan?

A

That you will be dosing the pt based on time and not by the pain they feel.
Good therapy because when you take doses based on pain, you will eventually need a higher and higher dose.

24
Q

What are 3 benefits of “by the clock” dosing?

A
  1. Uses less drug. (takes more drug to bring pain down than maintaining a pain-free state)
  2. avoids the euphoria with release of pain –> less addictive
  3. avoids development of chronic pain syndromes
25
Q

Why is “by the ladder” dosing the best dosing technique?

A
  • allows the safest and least potent drug to be picked for any case
  • avoids addictive potential because opiods are not used until required.
26
Q

What opiod are all other opiods compared to in terms of analgesic equivalence?

A

Morphine

27
Q

What is the weakest commonly used opiod?

What is it used for?

A
  • Codeine

- used for pain, diarrhea, coughing and breathing inhibition

28
Q

What is unique about Tramadol?

A
  • it less addictive and shows greater pain control (for some reason)
  • It has TWO complementary mechanisms against pain
    1. activates the mu-opiod receptor (like other opiods)
    2. is a weak inhibitor of norepinephrine and serotonin reuptake
29
Q

Due to first pass metabolism, oral morphine has a relatively _____ __________.

A

poor availability (~20-30%)

30
Q

How long do the effects of morphine last?

A

about 2 hours

31
Q

Oxycodone is __x as strong as morphine. How does this affect dosing?

A

2x

Will be dosed at half morphine for equivalent effects

32
Q

What is percocet?

A

oxycodone and tylenol

33
Q

What is tramacet?

A

Tramadol and tylenol

34
Q

Oxycodone has a ________ oral availability than morphine.

A

Higher

~80%

35
Q

The slow-release form of oxycodone is called _________.

A

Oxycontin

36
Q

Hydromorphone is __x _________ than morphine for pain.

A

5x stronger

37
Q

What is hydromorphone used for?

A

Used in surgical settings for moderate to severe pain (cancer, bone trauma, burns, etc)

38
Q

Fentanyl is ___x stronger than morphine.

A

80x

39
Q

What type of formulations does fentanyl come in?

A

Sublingual and transdermal patches

Sufentanyl also comes in these forms

40
Q

Is fentanyl highly hydrophilic or lipophilic?

A

Highly lipophilic, which makes it very potent

41
Q

Which is more potent, fentanyl or sufentanyl?

A

Sufentanyl. It is 10x stronger than fentanyl.

42
Q

How long does sublingual fentanyl last? transdermal?

A

1-2 hours

72-96 hours

43
Q

What is naltrexone?

A

It is an oral opiod inhibitor.
It reverses the psychotomimetic effects of opiate agonist
Also reverses hypotension and cardiovascular instability

44
Q

Will Naltrexone save a pt if they are dying from an opiod overdose?

A

NO. It will take too long to save someone from dying right that second.

45
Q

What is Naloxone?
What is it used for?
Another name?

A
  • potent opiod antagonist
  • used for quickly blocking opiod binding
  • used in emergency situation (ex. resp depression or heroin OD)
46
Q

What is the primary use of methadone?

A
  • addiction

- pt has developed resistance or toxicity to other opiods

47
Q

Why do doctors need special training to prescribe methadone?

A

Because even though it is less addictive, it has a greater risk of accidental overdose (due to very long half life –> ~5 days)

48
Q

How should you dose a pt if they are switching to a new opiod?

A

Take 30% less than the equivalent dose.

49
Q

What is physical dependance?

A

A normal response to chronic opiod administration.

50
Q

How can you avoid opiod withdrawal sx?

A

by decreasing the dose by 20-30% per day.

51
Q

What is addiction?

A
  • It is a psychological dependence.

- characterized by a “craving” for opiods

52
Q

What are some other side effects of opiods?

A
  • vomiting, then lack of vomiting
  • pinpoint pupils (OD sx)
  • vasodilation (methadone causes sweating)
  • constipation
  • decreased sex hormones, libido and fertility
53
Q

Why is constipation a dangerous side effect?

A

It can create a lot of problems in pts that have just had intestinal surgery.
You WANT pts to have intestinal movement after this type of surgery. Opiods prevent this.

PHAC II (9 decks)

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