Opioids Flashcards

(50 cards)

1
Q

what are the 3 types of opioid receptor subtypes

A

Mu, Kappa, and Delta

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2
Q

Name the 4 endogenous opioids

A

Endorphins, Enkephalins, Dynorphins, and Endomorphins

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3
Q

This endogenous opioid is a very long peptide that is not quickly degraded and can work either as a NT or as a hormone

A

B endorphins

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4
Q

This endogenous opioid is 5 AA long and metabolized very quickly so it only serves as a NT

A

Enkephalin

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5
Q

This endogenous opioid is about 17 AA long and metabolized even more rapidly than enkephalins and therefore only serves as a NT

A

Dynorphins

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6
Q

This endogenous opioid is only 4 AA long and metabolized very quickly so it only serves as a NT

A

Endomorphins

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7
Q

What is the primary NT for Mu receptors

A

Endomorphins

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8
Q

What is the primary NT for Kappa receptors

A

Dynorphins

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9
Q

What is the primary NT for Delta Receptors

A

Enkephalins

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10
Q

Why are B-endorphins called a promiscuous NT?

A

Because they can bind to any of the opioid receptors

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11
Q

What are the two drugs that we can get directly out of opium

A

Morphine and codeine

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12
Q

What is morphine’s effect on mood

A

`Anxialytical drug, reduces anxiety, decreases depression, can cause euphoria in some people

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13
Q

What are the 2 adverse effects you cannot develop a tolerance to for morphine

A

Constipaton and Miosis

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14
Q

How can respiratory depression be beneficial in morphine

A

For a person that is hyperventilating, it can slow their breathing down

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15
Q

This type of tolerance is like a pavlovian effect; a particular signal for getting the opioid, and the body prepares for it

A

Associated Tolerance

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16
Q

In this type of tolerance, if you are tolerant to one Mu opioid receptor, then you’ll be tolerance to other Mu receptors

A

Cross tolerance

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17
Q

Where are the sites of action for morphine

A

Dorsal horn of the spinal cord, activate descending inhibitory system, and peripheral receptors

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18
Q

Morphine is not good for what type of pain

A

Neuropathic pain

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19
Q

Name some contra-indications for opioids

A

COPD, liver or kidney disease, head injury, epilepsy, low BP, gallbladder disease, Addison’s disease, enlarged prostate, mental illness, or drug/alcohol addiction

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20
Q

Compared to morphine, this drug crosses the BBB more rapidly and is 2-4X greater potency

A

Heroin

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21
Q

Where is heroin converted into morphine

22
Q

Compared to morphine, this drug is about 8-10X more potent but has a shorter duration

A

Hydromorphone

23
Q

What is nice about Hydromorphone for cancer patients

A

It comes as a suppository for patients that have trouble swallowing

24
Q

What is the difference between oxymorphone and hydromorphone

A

Oxymorphone doesn’t have a suppository

25
Compared to morphine, this drug is about 1/10th the potency and has a lower efficacy
Codeine
26
Why do some patients not react to codeine at all
Because it's a prodrug and the liver enzyme CYP450 2D6 converts codeine to morphine and the patient may have a different enzyme that doesn't convert codeine into morphine
27
Compared to codeine, this drug is about 10X more potent and is equivalent to morphine
Oxycodone
28
These two drugs are the same as oxycodone
Hydrocodone and Dihydrocodeine
29
Which mixtures contain codeine
acetaminophen or NSAIDs
30
Name the 3 synthetic compounds
Meperidine, Fentanyl, and Methadone
31
Compared to morphine, this synthetic compound is about 1/8 potent, and has a shorter duration. You also get no mitosis with this drug
Meperidine
32
This synthetic compound is biotransformed to a toxic metabolite that builds up and can cause seizures
Meperidine
33
This synthetic compound is synergistic with gila monster venom
Meperidine
34
Compared to morphine, this synthetic compound is 80-100x more potent; it also has a fast onset and short duration
Fentanyl
35
This drug can be used IV for anesthethia, a patch, an oral slow release device or several transmuscosal preparations
Fentanyl
36
Name the 5 Fentanyl derivatives
Alfentanil, Sufentanil, Remifentanil, Carefentanil, and Lofentanil
37
This synthetic compound has a potency similar to morphine for IV, but is 4x more potent orally
Methadone
38
What are the 2 uses for methadone
for its analgesic effect and to treat opioid abuse
39
How is methadone used to treat opioid abuse
Through substitution therapy; one Mu agonist substituted for another
40
Name the 4 opioid antagonist
Naloxone, Naltrexone, Methynaltrexone, and Naloxagol
41
What are the signs of overdose
Stuporous or in a coma, RR extremely low, Pinpoint pupils, Low body temp, and Flacid skeletal muscles
42
This drug for opioid overdose has a short half-life and is not effective orally
Naloxone
43
This drug for opioid overdose has a long half-life and is available in oral form only
Naltrexone
44
Which drugs treat OIC
Methylnaltrexone, Naloxegol, Naldemedine, and Alvimopan
45
Which drugs are Mixed agonist-antagonist
Butorphanol and Nalbuphine
46
This mixed agonist-antagonist is a Kappa receptor agonist but a Mu receptor antagonist
Butorphanol
47
How is Butorphanol used
As a nasal spray
48
This mixed agonist-antagonist is 5X more potent in women than men
Butorphanol
49
This mixed agonist-antagonist is a Kappa receptor agonist and Mu receptor antagonist that has less abuse potential than morphine and little dysphoria compared to nalorphine
Nalbuphine
50
These drugs are an opioid receptor agonist (Mu and Delta) and a NE and 5-HT reuptake blocker (antidepressant) and an Alpha 2 agonist
Tramadol and Tapentadol