Opioids Flashcards

1
Q

Three opioid receptors opioids act on

A

Mu
Kappa
Delta

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2
Q

Most important opioid receptor for opioids

A

Mu

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3
Q

Opioid receptor which mediates euphoria

A

Mu

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4
Q

Opioid receptor which mediates respiratory depression

A

Mu

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5
Q

Opioid receptor which mediates dependence

A

Mu

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6
Q

Opioid receptor which mediates anxiolysis

A

Delta

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7
Q

Opioid receptor which mediates constipaton

A

Mu

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8
Q

Effect of mu stimulation on dopamine

A

Results in dopamine release from the ventral tegmental area producing euphoria

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9
Q

Effect of repeated opioid use on dopamine release

A

Mu receptors in the ventral tegmental area become less receptive
Less dopamine is released

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10
Q

Half life of methadone

A

15-22 hours

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11
Q

Affinity of buprenorphine for the mu receptor compared to morphine

A

5x higher

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12
Q

Half life of buprenorphine

A

24-42 hours with oral administration

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13
Q

Half life of naloxone

A

30-120 minutes

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14
Q

Serious respiratory adverse effect of naloxone

A

Non-cardiogenic pulmonary oedema

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15
Q

Half life of naltrexone

A

4-6 hours

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16
Q

Half life of the active metabolite of naltrexone

A

13 hours

17
Q

Length of time someone needs to have been opiate free for naltrexone to be licensed

A

7-10 days

18
Q

Active metabolite of naltrexone

A

6-βnaltrexol

19
Q

Half life of morphine

A

2-3 hours

20
Q

Half life of heroin

A

2-3 minutes

21
Q

Effect of starting buprenorphine if already taking opioids regularly

A

Can precipitate mild-moderate withdrawal - much more affinity for receptors than full agonists so displaces them

22
Q

Opioid withdrawal effects improved by alpha 2 adrenergic agonists (clonidine and lofexidine)

A

Sweating
Shivering
Runny nose
Watery eyes

23
Q

Antihypertensive effect of clonidine compared to lofexidine

A

Lofexidine has a lower antihypertensive effect

24
Q

Mechanism of action of withdrawal symptoms of jitteriness, muscle cramps, diarrhoea etc.

A

Locus coeruleus has a lot of noradrenargic neurons that have mu receptors
Exposure to opioids results in heightened activity of these neurons but the opioids themselves suppress activity
If there are no longer opioids present to suppress the activity increased amounts of norepinephrine are released