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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
Where do opioid receptors work?
Inhibition of the afferent pain transmission
26
What are the peripheral effects of opioid receptors?
Activation of distal ends of primary afferent neurons decreases their activation and excitability
27
What are the effect of opioids on the dorsal horn of the spinal cord?
Presynaptic: block release of pain modulating neurotransmiting Postsynaptic: opioids inhibits secondary afferent neurons via increase K channel conductance
28
What is the role of opioids in the descending pain pathways?
Block the inhibitory GABAergic interneurons, leading to enhance inhibition of nociception
29
What are the three sites of opioid action on the descending pain pathway?
Periaqueductal gray Rostral ventral medulla Locus coeruleus
30
Opioids provide analgesia in two general ways. What are they?
Reduce sensation and affective aspects of pain
31
In whom is sedation d/t opioids more frequent?
older folks
32
What is the COD for opioid OD?
Inhibition of the brainstem respiratory mechanism
33
What happens when there is a buildup of pCO2 d/t decreased respiration secondary to opioid use?
Reflexive cerebral vasodilation
34
What are the eye findings of opioid use?
Constriction of pupils
35
How do opioids reduce cough?
Suppress the cough center of the brain via brain stem chemoreceptor trigger zone
36
Stimulants cause what eye findings?
Mydriasis
37
What is the effect of opioids on emesis?
Stimulate the chemoreceptor trigger zone in the emetic area
38
What is the MOA of opioids as antidiarrheals?
Increasing the tone of the intestinal smooth muscle
39
What are the renal effects of opioids?
Increased tone of the muscle in the bladder and ureters
40
What are the effects of opioids on the uterus?
Decrease contractions
41
What are the cardiovascular effects of opioids?
Hypotension | Bradycardia
42
Why is histamine release with opioids?
hypersensitivity
43
How do you stop the n/v d/t opioids?
Switch opioids | Anti-emetics
44
How do you stop the sedation due to opioids?
Lower dose | Add co-analgesics
45
How do you stop the constipation associated with opioid use?
Stool softeners,
46
Opioids stimulate what enzymes in the liver?
MES
47
What is the interaction between opioids and MAOIs?
Hyperpyrexic reaction, including HTN
48
Which MAOI is highly associated with opioid interaction?
Meperidine
49
What is the MOA of morphine?
Prototype mu agonist
50
What is the MOA of fentanyl?
lipophilic mu agonist
51
What is the MOA of meperidine?
Active metabolite, is proconvulsant
52
What opioid is used as an antidepressant?
Codeine
53
What is dextromethorphan used for?
Cough suppressant
54
What is diphenoxylate used for?
Antidiarrheal
55
What is loperamide used for?
Antidiarrheal
56
What is the MOA of tramadol?
Mu agonist 5Ht/NE uptake inhibitor
57
What are the pros and cons of mixed opioids agonist-antagonists?
Produce adequate analgesia with less side effects, but enhanced psychotropic effects
58
What is the potency of hydromorphone compared to morphine?
7-10x more potent
59
How is fentanyl administered? What is the duration of action? How does its potency compare to morphine?
Transdermal 72 hour transdermal 80x greater than morphine
60
Why is Codeine okay to use for antitussive?
Produce less euphorie | Lower abuse potential
61
What are the two opioid antagonists?
Naloxone | Naltrexone
62
How fast does Naloxone work?
30 seconds if administered IV
63
What is the use of Naloxone?
treatment of OD
64
What is the use of Naltrexone?
Maintenance of drug for addicts in treatment programs
65
What is the physiological basis for tolerance to opioids?
Receptor down-regulation
66
What is cross tolerance?
Tolerance to one drug will produce tolerance to others
67
What are the parts of the brain that are a part of the reward pathway? What is the effect of opioids here?
Nucleus accumbens Central/ventral tegmental areas Opioids increase activation of dopamineric neurons
68
What is the main drug used for opioid addiction? MOA?
Methadone Strong opioid agonist with similar effects to morphine, but less withdrawal symptoms
69
What are the nose effects of opioid withdrawal?
Runny nose
70
Hyper or hypothermia with opioid withdrawal?
Hyperthermia
71
What are the eye findings with opioid withdrawal?
Pupillary dilation
72
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : morphine
Stronge | Natural
73
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : codeine
Moderate | Natural
74
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : oxycodone
Moderate | semi-synthetic
75
Strong, moderate or mixed (antagonist/agonist): pentazocine
mixed
76
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : hydromorphone
Strong | Semi-synthetic
77
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : oxymorphone
Strong | semisynthetic
78
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : methadone
Strong | Synthetic
79
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : meperidine
Strong | Synthetic
80
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : hydrocodone
Moderate | semi-synthetic
81
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : fentanyl
Strong | Synthetic
82
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : levorphanol
Strong | Synthetic
83
Strong, moderate or mixed (antagonist/agonist): tramadol
Moderate
84
Strong, moderate or mixed (antagonist/agonist)? Natural or synthetic? : propoxyphene
Moderate | Synthetic
85
Strong, moderate or mixed (antagonist/agonist): nalbuphine
Mixed
86
Strong, moderate or mixed (antagonist/agonist): buprenorphine
Mixed
87
Strong, moderate or mixed (antagonist/agonist): butorphanol
mixed
88
Strong, moderate or mixed (antagonist/agonist)?: nalorphine
Mixed
89
What is the use of dextromethorphan?
Antitussive
90
What is the use of diphenoxylate
Antidiarrheal
91
What is the use of loperamide
Antidiarrheal

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