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Pharmacology > Analgesics > Flashcards

Analgesics Flashcards

1
Q

Analgesia that affects peripheral nociceptors: 3

A

Opioids
Local anesthetics
Anti inflammatory agents (COX-2-specific inhibitors, nonselective NSAIDs)

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2
Q

Analgesia that affect peripheral nerve:

A

Local anesthetic

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3
Q

Analgesia that affect spine: 4

A

Opioids
Local anesthetic
Alpha2 agonists
COX-2-specific inhibitors

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4
Q

Analgesia that affect brain: 4

A

Opioids
Alpha2 agonists
Centrally acting analgesics
Anti inflammatory agents (COX-2-specific inhibitors, nonselective NSAIDs)

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5
Q

Where are the opioid receptors located?

A

CNS and peripheral tissues

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6
Q

What are the 4 major receptors?

A

Mu
Kappa
Delta
Sigma

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7
Q

What is the G protein coupled mechanism of action?

A

Agonist leads to membrane hyperpolarization
Inhibition of AC
Reduction in cAMP
Activation of PLC

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8
Q

Opioid mechanism of action:

A

Inhibits presynaptic release and post synaptic response to excitatory NTs which are released by nociceptive neurons

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9
Q

Clinical action depends on which receptor acting upon (4):

A

Affinity at receptor
Agonist or antagonist or combo effect
Butorphanol : ag/antagonists weaker than full agonist
May antagonize action of full agonist

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10
Q

How is post synaptic neuron inhibited?

A

Open K channels to hyerpolarize

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11
Q

How is analgesia produced?

A

Binding to the G protein coupled receptors located in brain and spinal cord regions (some peripheral sensory nerve endings)

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12
Q

What is opioid induced hyperalgesia?

A

Persistent administration of opioid can increase sensation of pain

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13
Q

Which drugs can cause opioid induced hyperalgesia?

A

Morphine
Fentanyl
Remifentanil

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14
Q

Is the first pass right high or low with PO?

A

High

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15
Q

How does this impact PO to IV ratio for dosing?

A

Needs higher dose for PO to get same affect as IV

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16
Q

What is fentanyl transdermal patch for?

A

Chronic pain

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17
Q

What is intrathecal used for?

A

Spinal analgesia

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18
Q

What does opioid distribution half life depend on?

A

Lipid solubility and other characteristics

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19
Q

What is morphines half life?

A

Low- slower onset compared to fentanyl and sufentanil

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20
Q

How does redistribution to other compartments affect duration of action?

A

Limits it with single dose/small dose

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21
Q

What plays a role in longer administrations?

A

Metabolism

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22
Q

Metabolism of opioids?

A

Converted by liver to polar metabolites than excreted by kidneys

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23
Q

What is hepatic P450 metabolism?

A

Phenylpiperidine opioids extensive degradation to metabolites, only small amount of parent life for renal excretion

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24
Q

Morphine structure:

A

Codeine
Oxycodone
Hydrocodone

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25
Q

Remifentanil structure

A

Ester

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26
Q

What is morphine metabolized by?

A

CYP2D6

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27
Q

What is remifentanil hydrolyzed by?

A

Plasma esterases

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28
Q

What is the elimination half life of remifentanil?

A

10min

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29
Q

Is remifentanil affect by pseudocholinesterase deficiency?

A

NO

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30
Q

What can kidney failure due to morphine excretion?

A

Prolong duration of action

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31
Q

What can accumulation of M3G and M6G in patients with renal failure lead to?

A

Prolonged affects including respiratory failure

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32
Q

What does normeperidine increased in renal failure lead to?

A

Seizures

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33
Q

What receptors in the CNS are central mediated?

A

Mu

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34
Q

Inhibition of what leads to respiratory depression?

A

Brainstem respiratory mechanisms

35
Q

What causes chest wall rigidity?

A

Rapid IV dose of opioid may make difficult ventilation with bag/mask due to inhibition of nigrostriatal GABA release

36
Q

What does mu receptor agonist lead to in regards of temperature

A

Hyperthermia

37
Q

What does kappa receptor agonist lead to in regards to temperature?

A

Hypothermia

38
Q

How does opioid affect cerebral perfusion?

A

Reduce cerebral oxygen consumption, CBF, ICP, but less than propofol or barbiturates

39
Q

What would you give antishivering effect?

A

Meperidine low does most effective 25mg IV

40
Q

CV affects with opioid

A

Minimal direct effects

41
Q

What does meperidine do to CV?

A

May cause atropine effect (increase HR)

42
Q

Which combo may reduce CO?

A

BZ + fentanyl or sufentanil

43
Q

When does histamine release?

A

Bolus of morphine, hydromorphone, meperidine

44
Q

How do you reverse respiratory depress with regional analgesia (epidural and spinal)?

A

Naloxone

45
Q

What is opioid adverse affects? (7)

A 
Respiratory depression 
Nausea and vomiting 
Pruritus 
Urticaria 
Constipation 
Urinary retention 
Delirium
46
Q

Measure of necessary amount of drug to produce effect of a given magnitude?

A

Potency

47
Q

Ability of drug to illicit pharmacological response when interacts with receptor (relationship between response and occupancy of receptor)?

A

Efficacy (intrinsic activity)

48
Q

What is full agonist efficacy?

A

1

49
Q

What is partial agonist efficacy?

A

0-1

50
Q

What is competitive antagonist efficacy?

A

0

51
Q

Extent or fraction to which drug binds to receptors at any given drug concentration

A

Affinity

52
Q

How is affinity, potency, and efficacy related?

A

Affinity is inversely proportional with potency

Affinity is independent of efficacy

53
Q

Common morphine agonists?

A

Mu and kappa

54
Q

Common fentanyl agonists?

A

Mu

55
Q

Common sufentanil agonist?

A

Mu, delta, and kappa

56
Q

Common alfentanil agonists?

A

Mu

57
Q

Common remifentanil agonists?

A

Mu

58
Q

Common meperidine agonists?

A

Mu

59
Q

Common hydromorphone agonists?

A

Mu

60
Q

What is naloxone?

A

Antagonist only at mu, kappa, and delta

61
Q

Naloxone onset?

A

1-3min

62
Q

Onset of fentanyl

A

Almost immediate

63
Q

Duration and half life of fentanyl

A

.5-1hr

2-4hr

64
Q

Metabolism of fentanyl

A

Phase 1 via CYP

65
Q

Remifentanil onset

A

Almost immediate

66
Q

Remifentanil duration and half life

A

5-10min

10-20min

67
Q

Remifentanil metabolism

A

Hydrolysis of ester linkage; nonspecific esterases

68
Q

Morphine onset

A

5-10min

69
Q

Morphine duration and half life

A

4hr

2-4hr

70
Q

Morphine metabolism

A

Primarily phase II glucuronidation

71
Q

NSAIDs mechanism of action

A

Inhibition of cyclooxygenase (COX), which is key step in prostaglandin synthesis

72
Q

Receptors are widely distributed in body including gut and platelets (causing bleeding)

A

COX1

73
Q

Produced in response to inflammation

A

COX2

74
Q

COX non selective agents affect:

A

Fever
Inflammation
Pain
Thrombosis

75
Q

COX2 selective

A

Increase risk of MI, thrombosis, stroke

76
Q

What does aspirin and acetaminophen do?

A

Inhibit COX

77
Q

Nonselective NSAIDs available for IV use:

A

Ketoroloac
Ibuprofen
Diclofenac

78
Q

What are potential negative effects of nonselective NSAIDs?

A

Bone healing and anastomotic leak after colorectal surgery

79
Q

What is Ketorolac NSAID?

A

Parental
Only short term for mild to moderate pain
Renal insufficiency (elevated sCr)
Inhibition of platelet aggregation

80
Q

Acetaminophen does what?

A

Inhibits COX1 and COX2

81
Q

How is acetaminophen administered?

A

PO and IV

82
Q

Max does of acetaminophen?

A

4g/24hrs

83
Q

Hepatic impairment of acetaminophen?

A

Low dose <2-3g/day causation about other factors (alcohol, nutritional status, renal function)
Severe impairment: contraindicated

Pharmacology (14 decks)

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