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Pharm Unit 3 > Narcotics > Flashcards

Narcotics Flashcards

1
Q

What type of receptor is the opioid receptors?

A

GPCR

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2
Q

Effect of opioid receptor

A

decreased adenyl cyclase, Ca2+ channel activity
increase K+ channel activity
(hyperpolarizes)

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3
Q

What is the main opioid receptor targeted by analgesics?

A

u (Mu)

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4
Q

Describe morphine’s structure and sites that account for variation

A

5 ring structure

modifications at positions 3,6, and 17

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5
Q

What do opioid receptor agonists do?

A

Inhibit the release of substance P and ascending transmission of pain from dorsal horn neurons.

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6
Q

Possible mechanism of tolerance?

A

internalization/ phosphorylation of receptors

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7
Q

What two side effects do patient’s on opioids exhibit little tolerance to?

A

Miosis and constipation

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8
Q

What are the SE of opioids?

A

Miosis, constipation, respiratory depression

N/V, uticaria, bad dreams, sedation, delirium, Seizures, urinary retention

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9
Q

Where and how are opioids metaboilized?

A

Liver, conjugation w/ glucoronic acid

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10
Q

Why is the Cmax for oral opioids lower than IV?

A

first pass metabolism

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11
Q

How do you address the bolus effect of IV/IM dosing?

A

Consider CI or extended release oral formulations

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12
Q

Why are opioids often used in with adjuvants?

A

To reduce the necessary dose, decreasing unwanted SE.

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13
Q

When are opioids used?

A

To treat moderate or severe pain.

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14
Q

What metabolite of morphine is the most active/ highest potency?

A

M-6- glucuronide

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15
Q

What is morphine’s MOA?

A

Mu- opioid receptor agonist

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16
Q

What are the effects of morphine?

A

severe analgesia, mood alteration, antitussive, sedation

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17
Q

What pathway is responsible for conversion of 10% of codeine into morphine?

A

CYP2D6

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18
Q

What are the effects of codeine?

A

moderate analgesia, antitussive

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19
Q

What is codeine’s MOA?

A

Mu- opioid receptor agonist

20
Q

What concern is there for codeine use in Caucasians?

A

10% can’t convert to morphine, but still experience SE

21
Q

How does tramadol work?

A

weak Mu receptor agonist, inhibition of NE/5HT uptake

22
Q

What are the effects of tramadol?

A

moderate analgesia

23
Q

What are the effects of fentanyl?

A

severe analgesia

24
Q

How is fentanyl delivered?

A

IV or transdermal

25
Q

How long should you wait before increasing the does of fentanyl?

A

1 week

26
Q

What is MOA of fentanyl?

A

Mu-opioid receptor agonist, highly lipid soluble

27
Q

What is the MOA of methadone, oxycodone, and meperidine?

A

Mu-opioid receptor agonist

28
Q

What is methadone used to treat?

A

chronic severe pain

treatment of heroine and opioid addicts

29
Q

When initially treating with methadone, what precautions should be taken?

A

Do not raise dose more than 1/ wk

Overdose common in initial treatment

30
Q

What is oxycodone used to treat?

A

moderate to severe analgesia

31
Q

What two opioids are no longer used?

A

Meperidine and Propoxyphene

32
Q

What are Loperamide (Imodium) and Diphenoxylate (Lomotil) used to treat?

A

DIarrhea

33
Q

Loperamide (Imodium) and Diphenoxylate (Lomotil) MOA?

A

slows peristalsis by binding opioid receptors in intestine, possibly decreases GI secretions

34
Q

What is Naloxone (Narcan) used to treat?

A

opioid toxicity

35
Q

Naloxone (Narcan) MOA?

A

competitive mu, delta, and kappa opioid receptor antagonist

36
Q

SE of Naloxone?

A

can precipitate withdrawal

N/V/D, piloerection, yawning, irritabilty

37
Q

What is Naltrexone (Revia) used to treat?

A

Alcoholism

38
Q

SE of Naltrexone?

A

prolonged withdrawal- N/V, piloerection, yawning

39
Q

MOA of Naltrexone (Revia)?

A

Mu-opioid receptor antagonist

40
Q

What must you be cautious of when prescribing a opioid in combination with acetaminophen?

A

At home, OTC use. Risk of overdose

41
Q

How long between doses for oral immediate release preparations vs extended release preparations?

A

immediate- every 4 hours

extended- 8-24 hrs

42
Q

What should you not use to treat breakthrough dosing?

A

extended release opioids

43
Q

What should you do if pain is poorly responsive to opioids?

A

Try alternative route or rotate opioid

Try coanalgesic

44
Q

What must be kept in mind when changing drugs or route?

A

Equianalgesic dosing

When changing drug or route, decrease equianalgesic dose by 25-50% at first to avoid bad SE

45
Q

What should be done to avoid constipation w/ opioid use?

A

Prescribe stool softener w/ stimulant laxative at the same time you start opioid.

46
Q

If respiratory depression begins in a patient taking opioids, what should you do?

A

Give IV Naloxone (Narcan)

47
Q

How do you decrease risk of delirium in patient being treated with opioids?

A

Confirm normal liver (metabolism) / kidney (excretion) function

Pharm Unit 3 (14 decks)

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