Opioid analgesics Flashcards

1
Q

Which two drugs are classified as strong opioid agonists?

A

Morphine and Methadone

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2
Q

Class of morphine

A

Strong opioid agonist

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3
Q

For which receptors does morphine have an affinity. Describe the affinity.

A

High affinity for mu receptors

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4
Q

What is the active metabolite of morphine?

A

morphine-6-glucuronide

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5
Q

Which drug is 10% opium?

A

Morphine

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6
Q

Morphine is what % opium?

A

10%

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7
Q

Morphine-6-glucuronide

A

Active metabolite of morphine

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8
Q

Morphine treats severe pain, commonly in cases of:

A

Trauma, cancer, MI

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9
Q

Which drug is considered the prototypical opioid?

A

Morphine

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10
Q

Duration of action of morphine?

A

4-6 hours

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11
Q

Which drug can be turned into heroin via acetylation?

A

Morphine

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12
Q

When you acetylate morphine, you make:

A

heroin

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13
Q

Why is heroin a much more powerful drug than morphine?

A

Acetylation makes it much more fast-acting and lipid-soluble.

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14
Q

Which strong opioid agonist is orally affective?

A

Methadone

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15
Q

Use of methadone?

A

Used for detox/controlled withdrawal from heroin and morphine

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16
Q

Duration of action of methadone?

A

15-20 hours

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17
Q

Which strong opioid agonist is mainly used for detox?

A

Methadone

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18
Q

Which drug is considered a moderate opioid agonist?

A

Codeine

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19
Q

Class of codeine?

A

Moderate opioid agonist

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20
Q

Which drug is 0.5% opium?

A

Codeine

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21
Q

Codeine is what % opium?

A

0.5%

22
Q

How is codeine used for analgesia?

A

It is metabolized into morphine.

23
Q

Codeine is less abused than morphine because it is:

A

less potent.

24
Q

How do we supplement the lower potency of codeine in providing analgesia to patients?

A

Combine it with non-opioids–multi-modal pain relief

25
Q

Which two drugs are mixed opioid agonist-antagonists?

A

Pentazocine and Buprenorphine

26
Q

Class of pentazocine?

A

Mixed opioid agonist-antagonist

27
Q

Mechanism of action of pentazocine?

A

K-receptor agonist with weak mu receptor antagonist

28
Q

Pentazocine is a K-receptor _____________ and a weak mu receptor ____________

A

agonist; antagonist

29
Q

Which mixed opioid agonist-antagonist is a K-receptor agonist?

A

Pentazocine

30
Q

Which mixed opioid agonist-antagonist is a weak mu-receptor antagonist?

A

Pentazocine

31
Q

Method of administration of Pentazocine?

A

Orally

32
Q

What level of pain does Pentazocine treat?

A

Moderate to severe pain

33
Q

Which mixed opioid agonist-antagonist precipitates withdrawal in morphine users?

A

Pentazocine

34
Q

Class of Buprenorphine?

A

Mixed opioid agonist-antagonist

35
Q

Mechanism of action of Buprenorphine?

A

Partial agonist at mu receptors and antagonist at K-receptors

36
Q

Buprenorphine is a partial ___________ at mu receptors and ___________ at K-receptors

A

Agonist; antagonist

37
Q

Which mixed opioid agonist-antagonist is a partial agonist at mu receptors?

A

Buprenorphine

38
Q

Which mixed opioid agonist-antagonist is an antagonist at K receptors?

A

Buprenorphine

39
Q

Which mixed opioid agonist-antagonist is used to manage cocaine addiction and heroin abuse?

A

Buprenorphine

40
Q

Use of buprenorphine?

A

Used to manage cocaine addiction and heroin abuse

41
Q

Which two drugs are opioid antagonists?

A

Naloxone and naltrexone

42
Q

Class of naloxone?

A

Opioid antagonist

43
Q

What type of antagonist is naloxone?

A

Competitive antagonist at opioid receptors

44
Q

Half life of naloxone?

A

1-2 hours

45
Q

Which opioid antagonist is used as an IV injection to treat opioid overdose?

A

Naloxone

46
Q

Class of naltrexone?

A

Opioid antagonist

47
Q

What type of antagonist is naltrexone?

A

Competitive antagonist at opioid receptors

48
Q

Half-life of naltrexone?

A

10 hours

49
Q

Which opioid antagonist is considered a maintenance drug for addicts and alcoholics?

A

Naltrexone

50
Q

How does naltrexone maintain abstinence for recovering alcoholics?

A

Decreases rewarding effects of alcohol