Opiates & Analgesics Flashcards

1
Q

the point the individual perceives the response as pain

A

pain threshold

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2
Q

The ability of the individual to experience pain without initiation of pain responses

A

Pain tolerance

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3
Q

Painful stimuli are sensed by peripheral nociceptive of these types of neurons via ion channels that convert stimuli to membrane potential changes

A

C or Aδ

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4
Q

Mu receptor that functions in analgesia and euphoria

A

Mu1

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5
Q

Mu receptor that functions in bradycardia and respiratory depression

A

Mu2

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6
Q

Component of G protein that modulates ion channels in opioids

A

Beta and gamma

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7
Q

What effect do opioids have on BP?

A

Causes hypotension
(at moderate to high doses)

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8
Q

What effect do opioids have on heart rate?

A

Causes bradycardia
(at moderate to high doses)

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9
Q

What effect do opioids have on repiration?

A

Depress respiration

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10
Q

Opioids can cause respiratory depression and cerebral vessel dilation, so they are contraindicated in this

A

Head trauma or severe brain injury

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11
Q

Opioid use is cautioned in patients with asthma or COPD due to the release of this

A

Histamine

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12
Q

Opioids chronically suppresse hypothalamic-pituitary-gonadal axis to trigger this

A

Opioid-induce androgen deficiency (OPIAD)

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13
Q

Opioids chronically suppress this to trigger opioid-induced androgen deficiency (OPIAD)

A

Hypothalamic-pituitary-gonadal axis

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14
Q

No opioid tolerance develops to either of these effects

A

Miosis and constipation

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15
Q

Peripheral opioid antagonist that is administered orally

A

Naloxegol

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16
Q

Peripheral opioid antagonist that is a subcutaneous injectable

A

Methylnaltrexone

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17
Q

Naloxegol and Methylnaltrexone are antagonists to this

A

Peripheral opioid antagonists

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18
Q

Benzodiazepines should not be used with these drugs due to profound sedation, respiratory depression, coma and risk of death

A

Opiates

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19
Q

This type of drug should not be used with opiates due to profound sedation, respiratory depression, coma and risk of death

A

Benzodiazepines

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20
Q

Is dependence likely when morphine is used for pain?

A

Rare

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21
Q

Does meperidine have a short or long duration of action?

A

Short

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22
Q

Meperidine is converted to this product that is not conjugated, non-analgesic, proconvulsant, and hallucinogenic

A

Normeperidine

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23
Q

Normeperidine is a product of biotransformation of this drug

A

Meperidine

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24
Q

Is Normepederidine (a product of biotransformation of meperidine) analgesic?

A

No

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25
Normepederidine (a product of biotransformation of meperidine) has these two effects
Proconvulsant Hallucinogen
26
Opiate that has anticholinergic activity, and may cause seizures
Meperidine
27
Opiate that has anticholinergic activity, and has potential for serotonin syndrome if combined with serotonin reuptake inhibitors
Meperidine
28
Opiate that is contraindicated in epilepsy, cardiac disease, and use with MAOI (due to malignant hyperthermia)
Meperidine
29
Why is Meperidine contraindicated in patients with epilepsy?
It has anticholinergic activity and cause cause seizures
30
Meperidine use is contraindication with MAOI's because concurrent use can cause this
Malignant hyperthermia
31
Meperidine use is contraindicated with this type of drug due to malignant hyperthermia
MAOIs
32
What is the main issue with use of Fentanyl, Alfentanil, Sufentanil, Remifentanil?
Potency
33
Fentanyl, Alfentanil, Sufentanil, Remifentanil are contraindicated in this
Pregnancy (respiratory depression of mother and newborns; increased sudden infant deaths)
34
Opiates where potency is an issue
Fentanyl et al. (Alfentanil, Sufentanil, Remifentanil)
35
Opiates that may cause respiratory depression of mother and newborns; increased sudden infant deaths
Fentanyl et al. (Alfentanil, Sufentanil, Remifentanil)
36
Synthetic opioid that also is an antagonist at (NMDA) receptor and weak inhibitor of norepinephrine and serotonin uptake
Methadone
37
Methadone is a synthetic opioid that also is an antagonist at this receptor
NMDA
38
Methadone is a synthetic opioid that also is an antagonist at (NMDA) receptor and weak inhibitor of uptake of these 2 compounds
Norepinephrine and serotonin
39
Opioid that may be used in nociceptive pain (mu) and neuropathic pain (NMDA and uptake inhibition)
Methadone
40
Is Methadone short or long lasting?
Long orally active
41
Does Methadone cause euphoria?
No
42
Opioid that is often combined with aspirin or acetaminophen
Codeine
43
Opioid that has a high degree of histamine release and vasodilation
Codeine
44
Codeine has a high degree of release of this
Histamine
45
What effect does Codeine have on vessels?
High degree of vasodilation
46
2 opioids that are weak inhibitors of norepinephrine and serotonin reuptake
Tramadol and Tapentadol
47
Tramadol and Tapentadol are weak inhibitors of reuptake of these two compounds
Norepinephrine and Serotonin
48
With use of Tramadol and Tapentadol, why is respiratory depression less than predicted by analgesic action?
Because they are weak inhibitors of norepinephrine and serotonin reuptake
49
Tramadol and Tapentadol may interact with this type of agent
Monoaminergic agents (especially MAO uptake inhibitors and other reuptake inhibitors)
50
Opiate that has a convulsant metabolite that restricts use to short term
Meperidine
51
This opiate and related compounds are very potent so be careful as small doses are powerful (cannot be used during pregnancy or after surgery)
Fentanyl
52
Opiate that has a long duration of action and allows once daily dosing
Methadone
53
Opiate that has a very high profile of histamine release
Codeine
54
2 opiates that enhance norepinephrine and serotonin activity that may reduce opiate-induced respiratory depression
Tramadol and Tapentadol
55
Yawning is characteristic of this stage of opiate withdrawal syndrome
Stage 1 (also involves anxiety and drug craving)
56
Piloerection ("cold turkey skin") is characteristic of this stage of opiate withdrawal syndrome
Stage 3 (also involves tachycardia, nausea and vomiting, hypertension, tremors, spasms, seizures)
57
Do mixed agonists/antagonists have physical dependence potential?
Low
58
Is withdrawal a problem with mixed agonists/antagonists?
Potential to induce withdrawal in opioid-dependent Is milder (like meperidine/Demerol)
59
Opioid that is both a partial agonist and mixed agonist/antagonist: Low antagonist action (less risk of triggering withdrawal in dependent patient) Low abuse potential
Buprenorphine
60
Does Buprenorphine have abuse potential?
Low
61
Buprenorphine has low action of this; leading to less risk of triggering withdrawal in dependent patient
Low antagonist action
62
Opioid that is both a partial agonist and mixed agonist/antagonist: Respiratory depression that does occur is not easily or fully reversed by naloxone
Buprenorphine
63
QT prolongation has been noted in this opioid that is both a partial agonist and mixed agonist/antagonist
Buprenorphine
64
Opioid that is both a partial agonist and mixed agonist/antagonist: Contraindicated in heart patients or epileptics (contraindications similar to morphine)
Pentazocine
65
Pentazocine is contraindicated in patients with either of these 2 conditions
Heart patients Epileptics
66
Butorphanol, Buprenorphine, Nalbuphine and Pentazocine are opioids that are both partial agonists and this
Mixed agonists/antagonists
67
Butorphanol, Buprenorphine, Nalbuphine and Pentazocine are opioids that are both mixed agonists/antagonists and this
Partial agonists
68
Opioid receptor antagonist that blocks craving and subjective effects of opioids and alcohol
Naltrexone
69
Combining this opioid receptor antagonist with ketoconazole (CYP 3A4 inhibitor) may trigger withdrawal, as levels may increase nearly 13 fold
Naloxegol
70
Combining Naloxegol with this drug may trigger withdrawal, as levels may increase nearly 13 fold
Ketoconazole (CYP 3A4 inhibitor)
71
Are Naloxegol or Methylnaltrexone centrally or peripherally acting for opioid-induced constipation?
Peripherally
72
Opioid receptor antagonist that may be used for alcohol dependence
Naltrexone
73
Naloxone and Naltrexone are this type of drug
Opioid receptor antagonists
74
Naloxegol and Methylnaltrexone are this type of drug
Opioid receptor antagonists (peripherally acting for opioid-induced constipation)
75
Only this isomer of opiates causes most of the action
L isomer
76
Both D or L forms of opiates can have this effect
Antitussive
77
Pinpoint pupils and depressed respiration are highly suggestive of overdose of this
Opiate
78
These 2 effects are highly suggestive of opiate overdose
Pinpoint pupils Decreased respiration
79
What are opioid receptor antagonists used for?
Opiate overdosage and reversal (Naltrexone also used for alcohol dependence)
80
Narcan nasal spray uses this opioid
Naloxone
81
Use of this opiate is associated with increased risk of QT prolongation (sudden cardiac death)
Methadone
82
Codeine is converted to this
Morphine
83
This type of opioid has lower abuse potential and may trigger withdrawal if used in a patient dependent on a different opiate
Mixed agonists/antagonists
84
Opioid that has very low antagonist activity noted, reported to have low levels of euphoria making it less likely to be abused, may be difficult to reverse using naloxone (requires very large doses at times)
Buprenorphine
85
Is withdrawal from opioids usually life-threatening or dangerous?
Rarely
86
Piloerection, mydriasis, diarrhea and yawning are important signs of this
Opioid withdrawal
87
This drug (NOT an opiate) is a selective allosteric inhibitor of voltage-gated sodium channel NaV1.8 that functions peripherally
Suzetrigine
88
This opiate may be difficult to reverse using naloxone (requires very large doses at times)
Buprenorphine
89
Which mixed opioid agonist/antagonist has the lowest risk of abuse?
Buprenorphine
90
What antagonist can reverse the respiratory depression of opiates?
Naloxone