Opioids Flashcards

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

A

the brain

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
Q

Compared to morphine, this drug is about 1/10th the potency and has a lower efficacy

A

Codeine

26
Q

Why do some patients not react to codeine at all

A

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
Q

Compared to codeine, this drug is about 10X more potent and is equivalent to morphine

A

Oxycodone

28
Q

These two drugs are the same as oxycodone

A

Hydrocodone and Dihydrocodeine

29
Q

Which mixtures contain codeine

A

acetaminophen or NSAIDs

30
Q

Name the 3 synthetic compounds

A

Meperidine, Fentanyl, and Methadone

31
Q

Compared to morphine, this synthetic compound is about 1/8 potent, and has a shorter duration. You also get no mitosis with this drug

A

Meperidine

32
Q

This synthetic compound is biotransformed to a toxic metabolite that builds up and can cause seizures

A

Meperidine

33
Q

This synthetic compound is synergistic with gila monster venom

A

Meperidine

34
Q

Compared to morphine, this synthetic compound is 80-100x more potent; it also has a fast onset and short duration

A

Fentanyl

35
Q

This drug can be used IV for anesthethia, a patch, an oral slow release device or several transmuscosal preparations

A

Fentanyl

36
Q

Name the 5 Fentanyl derivatives

A

Alfentanil, Sufentanil, Remifentanil, Carefentanil, and Lofentanil

37
Q

This synthetic compound has a potency similar to morphine for IV, but is 4x more potent orally

A

Methadone

38
Q

What are the 2 uses for methadone

A

for its analgesic effect and to treat opioid abuse

39
Q

How is methadone used to treat opioid abuse

A

Through substitution therapy; one Mu agonist substituted for another

40
Q

Name the 4 opioid antagonist

A

Naloxone, Naltrexone, Methynaltrexone, and Naloxagol

41
Q

What are the signs of overdose

A

Stuporous or in a coma, RR extremely low, Pinpoint pupils, Low body temp, and Flacid skeletal muscles

42
Q

This drug for opioid overdose has a short half-life and is not effective orally

A

Naloxone

43
Q

This drug for opioid overdose has a long half-life and is available in oral form only

A

Naltrexone

44
Q

Which drugs treat OIC

A

Methylnaltrexone, Naloxegol, Naldemedine, and Alvimopan

45
Q

Which drugs are Mixed agonist-antagonist

A

Butorphanol and Nalbuphine

46
Q

This mixed agonist-antagonist is a Kappa receptor agonist but a Mu receptor antagonist

A

Butorphanol

47
Q

How is Butorphanol used

A

As a nasal spray

48
Q

This mixed agonist-antagonist is 5X more potent in women than men

A

Butorphanol

49
Q

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

A

Nalbuphine

50
Q

These drugs are an opioid receptor agonist (Mu and Delta) and a NE and 5-HT reuptake blocker (antidepressant) and an Alpha 2 agonist

A

Tramadol and Tapentadol