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Neuro > PHARM: Opiates and Pain Pharmacotherapy > Flashcards

PHARM: Opiates and Pain Pharmacotherapy Flashcards

1
Q

Where do NSAIDs work in the pain pathway?

A

modulate the initial signal transduction

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2
Q

Where do Na+ channel blockers work in the pain pathway?

A

act as local anesthetics to block signal conduction (AP generation) in nociceptive fibers

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3
Q

Where do opiods work in the pain pathway?

A

spinal cord (block pre-synaptic Na+ channels and open post-synaptic K+ channels to decrease likelihood of action potential)

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4
Q

How do NE and GABA work in the pain pathway?

A

act just like opiates

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5
Q

What receptors play a prominent role in the sensitizaiton phenomenon?

A

NMDA glutamatergic receptor

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6
Q

How is short-term sensitization achieved?

A

post-translational modifications (phosphorylation)

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7
Q

How is long-term sensitization achieved?

A

altered gene expression (phosphorylation of GRPs)

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8
Q

What is it called when pain arises from transection or mechanical damage to the nerve axon?

A

neuropathic pain

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9
Q

What receptor is OP-1?

A

delta

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10
Q

What receptor is OP-2?

A

kappa

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11
Q

What receptor is OP-3?

A

mu

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12
Q

What are OP-1 receptors specific for?

A

Enkephalins

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13
Q

What are OP-2 receptors specific for?

A

Dynorphins

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14
Q

What are OP-3 receptors specific for?

A

Endorphins

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15
Q

What occurs with activation of OP-1 receptors?

A

modulation of hormone and neurotransmitter release

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16
Q

What occurs with activation of OP-2 receptors?

A

psychotomimetic effects (decreased GI transit)

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17
Q

What occurs with activation of OP-3 receptors?

A

sedation, decreased respiration, decreased GI transit, and modulation of hormone and neurotransmitter release

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18
Q

Which opiates can be given rectally?

A

hydromorphone
morphine
oxymorphone

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19
Q

What opiates can be given in a lozenge form?

A

codeine

oxycodone

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20
Q

What opiate can be given in patch form?

A

fentanyl

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21
Q

What opiate is contraindicated in renal failure and breastfeeding?

A

codeine

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22
Q

Which opiates can be used in renal failure?

A

Fentanyl

Hydromorphone

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23
Q

Which opiate has a long half-life and can be used to treat withdrawal?

A

Methadone

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24
Q

Which opiate has a DDI with MAOIs?

A

Meperidine

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25
Q

Which opiate can cause long QT and reduced libido?

A

Methadone

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26
Q

Which opiate can cause peripheral and central anti-cholinergic effects?

A

meperidine

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27
Q

Which opiate can only be given IV?

A

remifentanil

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28
Q

Which opiates are NOT solely OP-3 agonists?

A

Codeine (OP-3 partial agonist)

Morphine (OP-3 agonist AND OP-2 minor agonist)

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29
Q

Which opiate can be converted to morphine by CYP2D6?

A

codeine

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30
Q

Which opiate has the lowest potency?

A

meperidine

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31
Q

What is interesting about meperidine metabolism?

A

it is either broken down into an inactive form or into a form that is 3X more potent

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32
Q

What opiate is a substrate for P-gp and CYP?

A

methadone

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33
Q

What is the most potent opiate?

A

fentanyl

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34
Q

Which opiate is the same potency as morphine?

A

methadone

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35
Q

Which PD drugs are contraindicated with meperidine?

A

selegiline

rasagiline

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36
Q

List the opiod partial agonists

A 
Butorphanol
Buprenorphine
Hydrocodone
Nalbuphine
Pentazocine
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37
Q

Which opiod partial agonists are only IV?

A

Butorphanol

Nalbuphine

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38
Q

Which opiod partial agonist has a very high potency and a ceiling effect?

A

Buprenorphine

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39
Q

Which opiod partial agonists is not simply a partial mu agonist?

A

Buprenorphine (partial Mu agonist and partial delta and kappa antagonist)

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40
Q

Which opiod partial agonist is metabolized by CYP3A4 and CYP2D6?

A

Hydrocodone

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41
Q

Which opiod partial agonist is used for withdrawal due to its very tight binding (long acting)?

A

Buprenorphine

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42
Q

What drug is given with Buprenorphine for withdrawal?

A

naloxene

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43
Q

True or false: opiates commonly relieve pain completely.

A

FALSE they make pain more tolerable

44
Q

What is a strange toxicity of opiates?

A

pruritis around nose

45
Q

What symptom of opiates is more common with parenteral or spinal administration?

A

urticaria

46
Q

Which opiate toxicities have minimal or no likelihood of tolerance developing (will never get better as long as you are using the drug)?

A

MIosis
Constipation
Convulsions

47
Q

Which opiate toxicity has moderate likelihood of tolerance developing?

A

bradycardia

48
Q

Why does constipation occur with opiate treatment?

A

binding to opiate receptors in enteric nervous system produces anticholinergic action (Ach usually stimulates peristalsis, so anticholinergic leads to stasis and hardening of stool)

49
Q

How do you treat opiate-induced constipation?

A
  • prophylaxis with stool softener or laxative

- careful titration with opiate antagonist

50
Q

Why does N/V occur with some people who are treated with opiates?

A

they get rapid initiation at high doses (not as likely if slow titration!

51
Q

What do you do to treat opiate-induced respiratory depression?

A
  • If in hospital setting, do not give next dose

- If overdose, try naloxone

52
Q

Why does pruritis occur with opiate treatment?

A

central action or direct stimulation of mast cells

53
Q

What is opiod rotation?

A

use of a different opiate to control pain and reduce adverse effects if a patient is “poorly responsive” to a treatment (has bad side effects)

54
Q

What is the triad of opiate overdose?

A
  • Coma
  • Pinpoint pupils
  • Respiratory depression
55
Q

Why does coma occur with opiate overdose?

A

decreased cortical stimulation via thalamus and hypothalamus

56
Q

Why does pinpoint pupils occur with opiate overdose?

A

Edinger-westphal complex sitmulated

57
Q

What drugs increase sedation and respiratory depression of opiates?

A

Sedative-hypnotics
Antipsychotics
MAOIs

58
Q

What is the mechanism by which tolerance occurs with opiates?

A

recycling of GPCRs

59
Q

What protein phosphorylates opiate receptors to lead to internalization?

A

GRK (increases receptor affinity for beta-arrestin which enhances interaction between 2 proteins and leads to internalization)

60
Q

How does endogenous enkephaline and morphine differ in respect to tolerance?

A

endogenous enkephalins have a relative balance between sensitization and resensitization while morphine has a slow perisstent desensitization and little recycling

61
Q

How has the view of receptor recycling and resensitization changed?

A

resensitizaiton is now thought to be able to occur without the need for internalization (receptor dephosphorylation can occur if GRK2 and beta-arrestin proteins are inhibited with pharmacologic agents)

62
Q

List the 3 opiate antagonists.

A

Naloxone
Nalmefene
Naltrexone

63
Q

Which opiate antagonist has a very short half-life (30-80 minutes)?

A

Naloxone

64
Q

Which opiate antagonist has a long half-life and can be used to treat opiate addiction and decrease alcohol cravings?

A

naltrexone

65
Q

What is the indication for naloxone?

A

Opiate toxicity (treat respiratory depression or progressive obtundation suggestive of imminent decline)

66
Q

Which opiate antagonist can precipitate withdrawal in dependent patients?

A

naltrexone

67
Q

Which opiate antagonist can cause abstinence, aspiration and severe pain?

A

naloxone

68
Q

What precipitates opiate withdrawal symptoms?

A

when the levels of opiate in the blood decline below a threshold level

69
Q

What are the symptoms of opiate withdrawal?

A
  • Drug seeking (craving)
  • Crawling sensation of skin, diaphoresis, rhinorrhea
  • Anxiety, fear, sleep disturbance
  • Musculoskeletal pain
  • Nausea and diarrhea
70
Q

Which symptoms are NOT present in opiate withdrawal?

A

HTN, tachycardia, hallucinations, seizures, fever, delirium

71
Q

What signs are present in opiate withdrawal?

A 
Agitation
diaphoresis
Increased lacrimation
Piloerection
Dilated pupils
72
Q

What is the short-term treatment for opiate withdrawal?

A

methadone

73
Q

What is the long-term treatment for opiate withdrawal?

A

clonidine for 21 days

74
Q

What receptors does clonidine bind to?

A

alpha-2 receptors that are regulators at both pre-synaptic and post-synaptic sites

75
Q

What symptoms of withdrawal does clonidine NOT help with?

A

Insomnia
Muscle cramps
GI symptoms

76
Q

What is the characteristic molecular occurence in addiction?

A

surge of dopamine signaling in the nucleus accumbens

77
Q

What causes the surge of dopamine signaling in the nucleus accumbens during addiction?

A
  • GPCR activation
  • Activation of ionotropic receptors
  • Modulation of biogenic amine transport
78
Q

All addictive drugs increase dopamine concentration in what structure?

A

mesolimbic projection

79
Q

True or false: every patient with physical dependence to opiates will become addicted.

A

FALSE

80
Q

What is addiction?

A

compulsive, relapsing drug use despite negative consequences

81
Q

What treatment for opiate addiction has a very poor adherence?

A

naltrexone

82
Q

What treatment for opiate addiction is favored in pregnant women?

A

Methadone (may need to increase dose in 3rd trimester)

83
Q

Which treatment for opiate addiction requires a special state and federal license?

A

methadone

84
Q

What treatment for opiate addiction is given in combination with naloxone?

A

buprenorphine

85
Q

Why do you give naloxone with buprenorphine?

A

because naloxone only works parenterally, so if the patient tries to crush up the pill and inject it to get high, it will activate the naloxone (which antagonizes the effect of the buprenorphine)

86
Q

How does naltrexone block alcohol dependence craving?

A

block elevation of dopamine levels arising from signals in the VA and arcuate nucleus

87
Q

List the NMDA antagonists.

A

Ketamine

Dextromethorphan

88
Q

When do you use ketamine?

A
  • Prevent surgery-induced sensitizaiton

- acute, severe pain

89
Q

When do you use dextromethorphan?

A

-Post-operative or chronic pain

90
Q

What are the toxicities of ketamine?

A

hallucinations
amnesia
CV pressor
increased intracranial pressure

91
Q

What are the toxicities of dextromethorphan?

A

dizziness
confusion
fatigue

92
Q

List the TCAs used for pain disorders and depression associated with chronic pain?

A
  • Amitriptyline
  • Nortriptyline
  • Imipramine
  • Desipramine
93
Q

How do TCAs work in treating pain?

A

NE and 5-HT reuptake properties in ascending corticospinal monoamine pathways

94
Q

Which anticonvulsants are used for ancillary pain?

A

pregabalin

gabapentin

95
Q

Which anticonvulsant can be used to treat trigeminal neuralgia and ancillary pain?

A

carbamazepine

96
Q

Which anticonvulsant can be used to treat neuropathy, phantom, stroke and MS?

A

lamotrigene

97
Q

What anti-convulsants work by blocking Na+ channels that get upregulated in neuropathic pain?

A

Lamotrigene

Carbamazepine

98
Q

What anti-convulsants work by inhibition of voltage gated Ca2+ channels via the alpha-2-delta subunit (prevent trafficking to the cell surface)?

A

pregabalin

gabapentin

99
Q

Which CYP interactions do TCAs have?

A

CYP2D6

100
Q

Which anticonvulsant has a BBW for Stevens Johnson Syndrome?

A

Lamotrigene

101
Q

Which anticonvulsants are dose adjusted in hepatic failure?

A

Lamotrigene

Carbamazepine

102
Q

Which anticonvulsants are dose adjusted in renal failure?

A

Pregabalin

Gabapentin

103
Q

Which anticonvulsants have an increased risk for suicidal ideation?

A

lamotrigene

104
Q

Which anticonvulsant is associated with rare agranulocytosis?

A

carbamazepine

105
Q

Which opiates are used to treat IBS diarrhea?

A

loperamide

diphenosylate (prescription)

Neuro (10 decks)

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