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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
Q

codeine activates which receptors

A
  • mu

- delta

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26
Q

fentanyl activates which receptors

A

-mu

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27
Q

methadone activates which receptors

A

-mu

28
Q

meperidine activates which receptor

A

-mu

29
Q

naloxone antagonizes which receptors

A
  • mainly mu
  • delta
  • kappa
30
Q

naloxone antagonizes which receptors

A
  • mainly mu
  • delta
  • kappa
31
Q

naltrexone antagonizes which receptors

A
  • mainly mu and kappa

- delta

32
Q

mu agonists mnemonic

A
  • Gut motility
  • Respiratory depression
  • Analgesia
  • Physical dependence
  • Euphoria
33
Q

kappa agonists mnemonic

A
  • Gut motility
  • Analgesia
  • Miosis
  • Psychomotomimesis
  • Sedation
34
Q

delta agonists mnemonic

A
  • analgesic

- releases growth hormone

35
Q

most efficacious opiod

A

morphine

36
Q

pharmacological actions of morphine

A
  • analgesia
  • euphoria
  • respiratory depression
  • N/V
  • antitussive
  • miosis
  • vasodilation
  • histamine release
37
Q

morphine is contraindicated in who

A

pts with a brain injury because of the vasodilation

38
Q

morphine smooth muscle effects

A
  • decreased peristaltic contractions in GI and thus constipation
  • decreased bronchial function
39
Q

morphine in asthma

A
  • probably try to avoid because of the histamine release

- use lowest dose possible if it has to be used

40
Q

features of hydromorphone

A
  • mu agonist
  • short duration of action
  • highly lipophilic
41
Q

features of fentanyl

A
  • mu agonist
  • short duration of action
  • extremely potent ug doses
  • no oral dosage form
42
Q

opioid used to control patient coughing reflex in operations

A

hydromorphone

43
Q

opioid contraindicated in patients with heart disease

A

methadone - induces long QT syndrome

44
Q

features of methadone

A
  • mu agonist and NMDA antagonist
  • long duration of action
  • very difficult to use because of complicated PK
45
Q

opioid used in cancer pain

A

methadone

46
Q

features of oxycodone

A
  • mu receptor agonist
  • only oral
  • has a continuous release form (Oxycontin)
47
Q

oxycontin FDA warning

A
  • it is to be taken orally only

- crushing and taking Iv or snorting leads to lethal doses of oxycodone

48
Q

features of meperidine

A
  • kappa and mu agonist
  • anti-muscarinic effects
  • used short term
49
Q

contraindications with meperidine

A
  • MAOi antidepressant use leads to serotonin syndrome and hyperpyrexic coma
  • pts w/ renal compromise
50
Q

triad of symptoms of serotonin syndrome

A
  • cognitive (hallucinations)
  • autonomic (shivering, sweating, hyperthermia, tachycardia)
  • somatic (seizures, neurotoxicity, cardiotoxicity)
51
Q

moderate/intermediate opioids

A

codeine
hydrocodone
tramadol

52
Q

tramadol MoA

A

inhibits NE and 5HT reuptake

53
Q

non-analgesic opioids

A
  • loperamide
  • diphenoxylate
  • dextromethorphan
54
Q

pentazocine

A
  • mixed agonist/antagonist
  • agonist at kappa, antagonist at mu
  • used in post-op analgesia
55
Q

pentazocine adverse effects

A
  • dysphoria
  • hallucinations
  • psychotomimesis
56
Q

problem with mixed agonist/antagonists

A

if a patient has been using pure agonists these can cause abstinence syndrome (withdrawal)

57
Q

features of buprenorphine

A
  • partial mu agonist, weak delta antagonist

- very long duration of action

58
Q

general opioid adverse effects

A
  • severe respiratory depression
  • euphoria and sedations
  • constipation
  • N/V
  • hallucinations
  • hypotension
  • physical dependence
  • lowered seizure threshold
59
Q

only opioid that doesn’t prolong QT interval

A

meperidine

60
Q

diagnostic triad for opioid overdose

A
  • coma
  • miosis
  • depressed respiratory system
61
Q

treatment strategy for opioid overdose

A
  • ventilate patient

- administer opioid antagonist

62
Q

opioid antagonists

A
  • naloxone
  • nalmefene
  • naltrexone
63
Q

opioid use in pregnancy

A

-chronic use can lead to dependence in the fetus that will manifest in withdrawal syndrome postpartum

64
Q

opioid to especially avoid in patients with seizures

A

meperidine

65
Q

drug interactions with opioids

A
  • MAOi
  • TCA
  • sedating hypnotics and antihistamines
  • antipsychotics

PT2 Pain 5-10 (6 decks)

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