L 28 Opioids Flashcards

(37 cards)

1
Q

What are the Endogenous Opioids?

A

Endorphins
Enkephalins

Dynorphins
Endomorphins

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2
Q

Endomorphins receptor?

A

Mu

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3
Q

Dynorphins receptor?

A

Kappa

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4
Q

Enkephalins receptor?

A

Delta

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5
Q

Heroine is converted to?

A

Morphine

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6
Q

Difference between Heroin and Morphine?

A

Heroin= 2-4x more potent

crosses BBB faster

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7
Q

What drug is available as a suppository?

A

Hydromorphone

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8
Q

Hydromorphone potency? duration?

A

Hydro=
8-10x more potent
shorter duration

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9
Q

What drug is the same as hydromorphone?

A

Oxymorphone

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10
Q

Codeine potency? efficacy?

A

Codeine=
1/10 the potency of morphine
lower efficacy

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11
Q

What is Codeine converted to?

A

morphine

-> by CYP450 2D6

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12
Q

Oxycodone potency?

A

10x potency of Codeine

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13
Q

What mixtures contain Codeine?

A

Acetaminophen

NSAID

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14
Q

What are the Synthetic Compounds?

A

Meperidine

Fentanyl

Methadone

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15
Q

Meperidine potency? Duration?

A

1/8th potency of morphine

short

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16
Q

Meperidine SE?

A

toxic metabolite builds up

= seizures

17
Q

Advantages of Meperidine?

A

dec SM spasms than Morphine

no miosis

18
Q

Fentanyl potency? Onset? Duration?

A

80-100x potency of morphine

fast onset

short duration

19
Q

How is Fentanyl administered?

A

I.v. for anesthesia

20
Q

Methadone potency?

A

I.v. potency similar to morphine

oral= 4x more potency

21
Q

Methadone Tx?

A

narcotic dependence

22
Q

Methadone duration?

A

inc w/ repeated use

23
Q

What are the Opioid Antagonists?

A

Naloxone
Naltrexone

Methylnaltrexone
Naloxagol

24
Q

What are signs of OD?

A

stupor, coma

RR low

pinpoint pupils

low body temp

placid SM, jaw relaxed

25
Naloxone efficacy?
not effective orally
26
Naltrexone efficacy?
effective orally or injected
27
Methylnaltrexone Tx?
opioid induced constipation
28
Methylnaltrexone quaternary?
doesn't cross BBB
29
Naloxegol Tx?
opioid induced constipation
30
What are the Mixed Agonist-Antagonist drugs?
Butorphanol Nalbuphine
31
Butorphanol MOA? Available as?
Kappa agonist Mu antagonist nasal spray
32
Butorphanol potency?
5x more potent in women
33
Nalbuphine MOA?
Kappa agonist | Mu antagonist
34
Nalbuphine advantages?
little dysphoria compared to nalorphine less abuse potential than morphine
35
Tramadol MOA?
Mu & Delta agonist (-) reuptake of NE, SE a2 adreno agonist
36
Tapentadol MOA?
Mu & Delta agonist (-) NE reuptake
37
What drugs have actions that are synergistic for analgesia? and are antidepressant?
Tramadol Tapentadol