Opioid Analgesics Flashcards

1
Q

How is morphine metabolized?

A

By conjugation with glucuronic acid in the liver

*slowed metabolism in impaired renal and liver patients

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2
Q

Morphine therapeutic effects

A
Analgesia
Dull pain > sharp pain 
Act at peripheral, spinal, and brain level 
Sedation
Euphoria
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3
Q

Major side effect of morphine

A

Respiratory depressoin

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4
Q

Mechanism of respiratory depression

A

decreased sensitivity of the chemoreceptors to CO2

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5
Q

What is the first dose effect?

A

Nausea and vomiting after the first time you take opioid (due to trigger of the CTZ) - develop tolerance

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6
Q

Which effects do not develop tolerance to morphine?

A

Constipation

Miosis

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7
Q

Which opioid is associated with biliary pain?

A

Morphine

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8
Q

Which opioid can cause pruritus and itching due to histamine release?

A

Morphine

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9
Q

Which opioid prolongs labor and is consequently contraindicated in pregnancy?

A

Morphine

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10
Q

What are the contraindications of morphine

A

Decreased respiratory reserve
Head injuries (obscure signs/increase pressure)
CNS tumors
Pregnancy

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11
Q

What happens when morphine is combined with ETOH?

A

dissolves the coating of morphine of sustained release causing sudden dangerous release

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12
Q

What is the difference between codeine and morphine potency

A

Codeine 10x LESS potent

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13
Q

Codeine MOA

A

Prodrug converted to morphine by CYP2D6

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14
Q

What is a concern with codeine metabolism with some patients?

A

Ultra fast metabolizers will get morphine effects

worry about with children

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15
Q

Which analgesic is used for cough suppression?

A

Codeine

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16
Q

What are some key differences between codeine and morphine?

A

Less likely to cause addiction

More likely to cause constipation

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17
Q

Which analgesic has been combined with soda “sizzurp”

A

Codeine

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18
Q

Which is the most commonly prescribed analgesic that it has now become a schedule three drug?

A

Hydrocodone

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19
Q

True or false oxycodone is more potent than codeine

A

True

20
Q

Which analgesic is 100x more potent than Morphine?

A

Fentanyl

21
Q

Which drug is used for neuroleptanalgesia for cardiac patients?

A

Fentanyl

22
Q

Compared to morphine what are some key effects that only fentanyl has?

A

Does not induce histamine release
Cardiovascular system is less affected (cardiac stability during surgery)
High addiction potential

23
Q

Which opioid is metabolized very slowly?

A

Methadone

24
Q

Duration of action of methadone

A

1/2 life: 15 hr acute, 22 hr chronically

25
Q

What are some serious side effects of methadone?

A

Cardiovascular effects
QT prolongation
Torsades de pointes

26
Q

Which opioid is used to maintain addicts but not cure them?

A

Methadone

27
Q

How does maintenance therapy work?

A

Addict is given low dose methadone for slow onset and prevent immediate rush, long duration last throughout day, prevents withdrawal symptoms satisfies dependence
must go to methadone clinic

28
Q

Which drug is a rapid acting, more lipid soluble agent that has a high abuse potential and schedule 1 drug?

A

Heroin

29
Q

Buprenorphine MOA

A

Partial agonist at Mu

Antagonist at Kappa (prevent dysphoria)

30
Q

Which paritial agonist analagesic has a cieling effect for analgesia and respiratory depression?

A

Buprenorphine

31
Q

Which analgesic lacks dysphoric effects?

A

Buprenorphine

32
Q

Which analgesic can also treat opioid dependence outside of a maintenance clinic but will also precipitate withdrawal?

A

Buprenorphine

33
Q

Which drug was designed to be a Kappa agonist and minimal mu agonist but failed

A

Pentazocine

34
Q

Pentazocine MOA

A

Partial agonist mu and kappa

Kappa&raquo_space;> Mu

35
Q

Difference between Pentazocine and Buprenorphine?

A

Pentazocine produces dysphoria at high doses, Buprenorphine does not

36
Q

which analgesic is used safely as an anti-diarrheal OTC?

A

Loperamide

37
Q

Which drug is an anti-diarrheal agent but it still requires an Rx?

A

Diphenoxylate

38
Q

Which drug prefers the D-isomer and thus is used to treat cough and not pain?

A

Dextromethorphan

39
Q

Which drug is used to antagonize opioid effects in overdose?

A

Naloxone (Narcan)

40
Q

Naloxone MOA

A

Competitive antagonist of opioid receptors

Full agonist&raquo_space; partial agonist

41
Q

Which antagonist has been approved for nasal spray use?

A

Naloxone (good for patients because they are unconscious and cannot swallow)

42
Q

Which antagonist is used to treat opioid dependence by preventing the effects of opioids?

A

Naltrexone

43
Q

Which drug is now being added to opioids to prevent abuse if crushed and injected?

A

Naloxone (Narcan)

44
Q

Which opioid antagonist is used to treat opioid induced constipation?

A

Methylnaltrexone

45
Q

Methylnaltrexone MOA

A

Does not cross BBB (cannot prevent opioid analgesia) limited to the gut and prevent constipation