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PT2 Pain 5-10 > Opiod pharmacology > Flashcards

Opiod pharmacology Flashcards

1
Q

opiod analgesics work by

A

mimicing actions of endogenous opiods in two ways

  • raising pain thresholds
  • altering CNS perception of pain
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2
Q

opiod monotherapy is not effective for which type of pain

A

chronic neuropathic pain

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3
Q

sites of action in brain of opiod

A
  • amygdala
  • limbic cortex
  • thalamus
  • hypothalamus
  • periaqueductal gray
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4
Q

sites of action of opiods

A
  • brain

- dorsal horn (spinal cord)

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5
Q

EPSNS acronym

A

endogenous pain suppressant neuronal system

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6
Q

native EPSNS endogenous activators

A

enkephalins
dynorphans
endorphans

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7
Q

EPSNS

A

-multisynaptic pathway extending from the cerebrum down the spinal cord in the dorsal horn

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8
Q

function of endogenous opiod agonists

A
  • inhibit dorsal horn projection neuron functions

- inhibit the release of pain transmitters

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9
Q

pain transmitters released by dorsal horn

A

glutamate

Substance P

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10
Q

drugs that enhance activity or prevent breakdown of endogenous opiods, NE, or 5-HT in CNS have what kind of effect

A

analgesic

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11
Q

opiods reduce pain by

A

hyperpolarizing postsynaptic neurons in dorsal horn

  • reducing Ca influx
  • increasing K efflux
  • inhibit adenylyl cyclase, decreasing cAMP
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12
Q

3 types of opiod receptors

A

mu
delta
kappa

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13
Q

mu endogenous agonist

A

endorphin

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14
Q

delta endogenous agonist

A

enkephalin

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15
Q

kappa endogenous agonist

A

dynorphin

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16
Q

receptors susceptible to tolerance development

A

mu

delta

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17
Q

receptor responsible for hallucinogenic effects

A

kappa

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18
Q

activation of mu receptors causes

A
  • analgesia
  • slowed respiration
  • slowed GI transit
  • sedation
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19
Q

activation of delta receptors causes

A
  • analgesia

- increased growth hormone release

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20
Q

activation of kappa receptors causes

A
  • analgesia
  • hallucinations
  • slows GI
  • psychotomimesis
  • miosis
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21
Q

enkephalin activate which receptors

A
  • mainly DELTA
  • mu
  • kappa
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22
Q

endorphin activate which receptors

A
  • mainly Mu

- delta

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23
Q

dynorphin activate which receptors

A
  • mainly kappa

- barely mu

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24
Q

morphine activates which receptor

A

-mu

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25
codeine activates which receptors
- mu | - delta
26
fentanyl activates which receptors
-mu
27
methadone activates which receptors
-mu
28
meperidine activates which receptor
-mu
29
naloxone antagonizes which receptors
- mainly mu - delta - kappa
30
naloxone antagonizes which receptors
- mainly mu - delta - kappa
31
naltrexone antagonizes which receptors
- mainly mu and kappa | - delta
32
mu agonists mnemonic
- Gut motility - Respiratory depression - Analgesia - Physical dependence - Euphoria
33
kappa agonists mnemonic
- Gut motility - Analgesia - Miosis - Psychomotomimesis - Sedation
34
delta agonists mnemonic
- analgesic | - releases growth hormone
35
most efficacious opiod
morphine
36
pharmacological actions of morphine
- analgesia - euphoria - respiratory depression - N/V - antitussive - miosis - vasodilation - histamine release
37
morphine is contraindicated in who
pts with a brain injury because of the vasodilation
38
morphine smooth muscle effects
- decreased peristaltic contractions in GI and thus constipation - decreased bronchial function
39
morphine in asthma
- probably try to avoid because of the histamine release | - use lowest dose possible if it has to be used
40
features of hydromorphone
- mu agonist - short duration of action - highly lipophilic
41
features of fentanyl
- mu agonist - short duration of action - extremely potent ug doses - no oral dosage form
42
opioid used to control patient coughing reflex in operations
hydromorphone
43
opioid contraindicated in patients with heart disease
methadone - induces long QT syndrome
44
features of methadone
- mu agonist and NMDA antagonist - long duration of action - very difficult to use because of complicated PK
45
opioid used in cancer pain
methadone
46
features of oxycodone
- mu receptor agonist - only oral - has a continuous release form (Oxycontin)
47
oxycontin FDA warning
- it is to be taken orally only | - crushing and taking Iv or snorting leads to lethal doses of oxycodone
48
features of meperidine
- kappa and mu agonist - anti-muscarinic effects - used short term
49
contraindications with meperidine
- MAOi antidepressant use leads to serotonin syndrome and hyperpyrexic coma - pts w/ renal compromise
50
triad of symptoms of serotonin syndrome
- cognitive (hallucinations) - autonomic (shivering, sweating, hyperthermia, tachycardia) - somatic (seizures, neurotoxicity, cardiotoxicity)
51
moderate/intermediate opioids
codeine hydrocodone tramadol
52
tramadol MoA
inhibits NE and 5HT reuptake
53
non-analgesic opioids
- loperamide - diphenoxylate - dextromethorphan
54
pentazocine
- mixed agonist/antagonist - agonist at kappa, antagonist at mu - used in post-op analgesia
55
pentazocine adverse effects
- dysphoria - hallucinations - psychotomimesis
56
problem with mixed agonist/antagonists
if a patient has been using pure agonists these can cause abstinence syndrome (withdrawal)
57
features of buprenorphine
- partial mu agonist, weak delta antagonist | - very long duration of action
58
general opioid adverse effects
- severe respiratory depression - euphoria and sedations - constipation - N/V - hallucinations - hypotension - physical dependence - lowered seizure threshold
59
only opioid that doesn't prolong QT interval
meperidine
60
diagnostic triad for opioid overdose
- coma - miosis - depressed respiratory system
61
treatment strategy for opioid overdose
- ventilate patient | - administer opioid antagonist
62
opioid antagonists
- naloxone - nalmefene - naltrexone
63
opioid use in pregnancy
-chronic use can lead to dependence in the fetus that will manifest in withdrawal syndrome postpartum
64
opioid to especially avoid in patients with seizures
meperidine
65
drug interactions with opioids
- MAOi - TCA - sedating hypnotics and antihistamines - antipsychotics

PT2 Pain 5-10 (6 decks)

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