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Pharm > Opiate Analgesics > Flashcards

Opiate Analgesics Flashcards

1
Q

What kind of disease is delayed by analgesics?

A

RA

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2
Q

What are the four types of analgesics?

A
  1. opioids
  2. NSAIDs
  3. Glucocorticoids
  4. DMARDS
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3
Q

Where do analgesics work?

A

Dorsal horn afferent neurons synapse

At site of pain/inflammation

Promoting pain repression signal

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4
Q

What is the prototypical opioid analgesic?

A

Morphine

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5
Q

What are opioids used for, besides analgesia?

A

Euphoria
Relief from diarrhea
Cough suppression

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6
Q

What is opium?

A

Greek word meaning “juice” from the poppy seed

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7
Q

What is opiate?

A

Drug extracted from the exudate of the poppy

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8
Q

What is an opioid?

A

Natural or synthetic drugs that binds to the opioid receptors producing an agonist effect

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9
Q

What is a narcotic?

A

Term used to characterize pharmacological compounds used to treat moderate to severe pain

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10
Q

What is narcosis?

A

Stuporous or somnolent state

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11
Q

What are the two naturally occurring opioids?

A

Morphine and codeine

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12
Q

How does the potency or codeine compare to morphine?

A

6-7x less

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13
Q

How does the potency of morphine compare to heroin?

A

Heroin is 2x more potent than morphine

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14
Q

What are the endogenous opioids?

A

Endorphins
Enkephalins
Dynorphins

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15
Q

What are the two major endogenous opioid receptors?

A

Mu1

Mu2

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16
Q

Where are Mu1 opioid receptors located? What is their purpose?

A

Outside the spinal cord

Responsible for central interpretation of pain

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17
Q

Where are Mu2 receptors located? What is their purpose?

A

Located throughout the CNS

Responsible for supraspinal and spinal analgesia

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18
Q

What are kappa opioid receptors?

A

Modest supraspinal and spinal analgesia

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19
Q

What are delta opioid receptors?

A

Modest supraspinal and spinal analgesia

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20
Q

How well are opioids absorbed from the GI tract?

A

Well, but high first pass effect

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21
Q

What is the primary hepatic metabolism of morphine?

A

glucuronidation– morphine-6-glucuronide

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22
Q

What does the liver metabolize heroin and codeine to?

A

Morphine

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23
Q

What is the G protein that opioid receptors act on? What does this do?

A

Gi/G0 coupling, causing inhibition of adenylate cyclase, and decreased cAMP production

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24
Q

What is the MOA of opioids? (2)

A

Gi/Go excitation, causing:

  • a loss of intracellular Ca and decrease release of neurotransmitters
  • Increase postsynaptic opening of K channels, resulting in hyperpolarization
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25
Q

Where do opioid receptors work?

A

Inhibition of the afferent pain transmission

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26
Q

What are the peripheral effects of opioid receptors?

A

Activation of distal ends of primary afferent neurons decreases their activation and excitability

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27
Q

What are the effect of opioids on the dorsal horn of the spinal cord?

A

Presynaptic: block release of pain modulating neurotransmiting

Postsynaptic: opioids inhibits secondary afferent neurons via increase K channel conductance

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28
Q

What is the role of opioids in the descending pain pathways?

A

Block the inhibitory GABAergic interneurons, leading to enhance inhibition of nociception

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29
Q

What are the three sites of opioid action on the descending pain pathway?

A

Periaqueductal gray
Rostral ventral medulla
Locus coeruleus

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30
Q

Opioids provide analgesia in two general ways. What are they?

A

Reduce sensation and affective aspects of pain

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31
Q

In whom is sedation d/t opioids more frequent?

A

older folks

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32
Q

What is the COD for opioid OD?

A

Inhibition of the brainstem respiratory mechanism

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33
Q

What happens when there is a buildup of pCO2 d/t decreased respiration secondary to opioid use?

A

Reflexive cerebral vasodilation

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34
Q

What are the eye findings of opioid use?

A

Constriction of pupils

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35
Q

How do opioids reduce cough?

A

Suppress the cough center of the brain via brain stem chemoreceptor trigger zone

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36
Q

Stimulants cause what eye findings?

A

Mydriasis

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37
Q

What is the effect of opioids on emesis?

A

Stimulate the chemoreceptor trigger zone in the emetic area

38
Q

What is the MOA of opioids as antidiarrheals?

A

Increasing the tone of the intestinal smooth muscle

39
Q

What are the renal effects of opioids?

A

Increased tone of the muscle in the bladder and ureters

40
Q

What are the effects of opioids on the uterus?

A

Decrease contractions

41
Q

What are the cardiovascular effects of opioids?

A

Hypotension

Bradycardia

42
Q

Why is histamine release with opioids?

A

hypersensitivity

43
Q

How do you stop the n/v d/t opioids?

A

Switch opioids

Anti-emetics

44
Q

How do you stop the sedation due to opioids?

A

Lower dose

Add co-analgesics

45
Q

How do you stop the constipation associated with opioid use?

A

Stool softeners,

46
Q

Opioids stimulate what enzymes in the liver?

A

MES

47
Q

What is the interaction between opioids and MAOIs?

A

Hyperpyrexic reaction, including HTN

48
Q

Which MAOI is highly associated with opioid interaction?

A

Meperidine

49
Q

What is the MOA of morphine?

A

Prototype mu agonist

50
Q

What is the MOA of fentanyl?

A

lipophilic mu agonist

51
Q

What is the MOA of meperidine?

A

Active metabolite, is proconvulsant

52
Q

What opioid is used as an antidepressant?

A

Codeine

53
Q

What is dextromethorphan used for?

A

Cough suppressant

54
Q

What is diphenoxylate used for?

A

Antidiarrheal

55
Q

What is loperamide used for?

A

Antidiarrheal

56
Q

What is the MOA of tramadol?

A

Mu agonist 5Ht/NE uptake inhibitor

57
Q

What are the pros and cons of mixed opioids agonist-antagonists?

A

Produce adequate analgesia with less side effects, but enhanced psychotropic effects

58
Q

What is the potency of hydromorphone compared to morphine?

A

7-10x more potent

59
Q

How is fentanyl administered? What is the duration of action? How does its potency compare to morphine?

A

Transdermal
72 hour transdermal
80x greater than morphine

60
Q

Why is Codeine okay to use for antitussive?

A

Produce less euphorie

Lower abuse potential

61
Q

What are the two opioid antagonists?

A

Naloxone

Naltrexone

62
Q

How fast does Naloxone work?

A

30 seconds if administered IV

63
Q

What is the use of Naloxone?

A

treatment of OD

64
Q

What is the use of Naltrexone?

A

Maintenance of drug for addicts in treatment programs

65
Q

What is the physiological basis for tolerance to opioids?

A

Receptor down-regulation

66
Q

What is cross tolerance?

A

Tolerance to one drug will produce tolerance to others

67
Q

What are the parts of the brain that are a part of the reward pathway? What is the effect of opioids here?

A

Nucleus accumbens
Central/ventral tegmental areas

Opioids increase activation of dopamineric neurons

68
Q

What is the main drug used for opioid addiction? MOA?

A

Methadone

Strong opioid agonist with similar effects to morphine, but less withdrawal symptoms

69
Q

What are the nose effects of opioid withdrawal?

A

Runny nose

70
Q

Hyper or hypothermia with opioid withdrawal?

A

Hyperthermia

71
Q

What are the eye findings with opioid withdrawal?

A

Pupillary dilation

72
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : morphine

A

Stronge

Natural

73
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : codeine

A

Moderate

Natural

74
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : oxycodone

A

Moderate

semi-synthetic

75
Q

Strong, moderate or mixed (antagonist/agonist): pentazocine

A

mixed

76
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : hydromorphone

A

Strong

Semi-synthetic

77
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : oxymorphone

A

Strong

semisynthetic

78
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : methadone

A

Strong

Synthetic

79
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : meperidine

A

Strong

Synthetic

80
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : hydrocodone

A

Moderate

semi-synthetic

81
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : fentanyl

A

Strong

Synthetic

82
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : levorphanol

A

Strong

Synthetic

83
Q

Strong, moderate or mixed (antagonist/agonist): tramadol

A

Moderate

84
Q

Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : propoxyphene

A

Moderate

Synthetic

85
Q

Strong, moderate or mixed (antagonist/agonist): nalbuphine

A

Mixed

86
Q

Strong, moderate or mixed (antagonist/agonist): buprenorphine

A

Mixed

87
Q

Strong, moderate or mixed (antagonist/agonist): butorphanol

A

mixed

88
Q

Strong, moderate or mixed (antagonist/agonist)?: nalorphine

A

Mixed

89
Q

What is the use of dextromethorphan?

A

Antitussive

90
Q

What is the use of diphenoxylate

A

Antidiarrheal

91
Q

What is the use of loperamide

A

Antidiarrheal

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