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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
Remifentanil structure
Ester
26
What is morphine metabolized by?
CYP2D6
27
What is remifentanil hydrolyzed by?
Plasma esterases
28
What is the elimination half life of remifentanil?
10min
29
Is remifentanil affect by pseudocholinesterase deficiency?
NO
30
What can kidney failure due to morphine excretion?
Prolong duration of action
31
What can accumulation of M3G and M6G in patients with renal failure lead to?
Prolonged affects including respiratory failure
32
What does normeperidine increased in renal failure lead to?
Seizures
33
What receptors in the CNS are central mediated?
Mu
34
Inhibition of what leads to respiratory depression?
Brainstem respiratory mechanisms
35
What causes chest wall rigidity?
Rapid IV dose of opioid may make difficult ventilation with bag/mask due to inhibition of nigrostriatal GABA release
36
What does mu receptor agonist lead to in regards of temperature
Hyperthermia
37
What does kappa receptor agonist lead to in regards to temperature?
Hypothermia
38
How does opioid affect cerebral perfusion?
Reduce cerebral oxygen consumption, CBF, ICP, but less than propofol or barbiturates
39
What would you give antishivering effect?
Meperidine low does most effective 25mg IV
40
CV affects with opioid
Minimal direct effects
41
What does meperidine do to CV?
May cause atropine effect (increase HR)
42
Which combo may reduce CO?
BZ + fentanyl or sufentanil
43
When does histamine release?
Bolus of morphine, hydromorphone, meperidine
44
How do you reverse respiratory depress with regional analgesia (epidural and spinal)?
Naloxone
45
What is opioid adverse affects? (7)
``` Respiratory depression Nausea and vomiting Pruritus Urticaria Constipation Urinary retention Delirium ```
46
Measure of necessary amount of drug to produce effect of a given magnitude?
Potency
47
Ability of drug to illicit pharmacological response when interacts with receptor (relationship between response and occupancy of receptor)?
Efficacy (intrinsic activity)
48
What is full agonist efficacy?
1
49
What is partial agonist efficacy?
0-1
50
What is competitive antagonist efficacy?
0
51
Extent or fraction to which drug binds to receptors at any given drug concentration
Affinity
52
How is affinity, potency, and efficacy related?
Affinity is inversely proportional with potency | Affinity is independent of efficacy
53
Common morphine agonists?
Mu and kappa
54
Common fentanyl agonists?
Mu
55
Common sufentanil agonist?
Mu, delta, and kappa
56
Common alfentanil agonists?
Mu
57
Common remifentanil agonists?
Mu
58
Common meperidine agonists?
Mu
59
Common hydromorphone agonists?
Mu
60
What is naloxone?
Antagonist only at mu, kappa, and delta
61
Naloxone onset?
1-3min
62
Onset of fentanyl
Almost immediate
63
Duration and half life of fentanyl
.5-1hr | 2-4hr
64
Metabolism of fentanyl
Phase 1 via CYP
65
Remifentanil onset
Almost immediate
66
Remifentanil duration and half life
5-10min | 10-20min
67
Remifentanil metabolism
Hydrolysis of ester linkage; nonspecific esterases
68
Morphine onset
5-10min
69
Morphine duration and half life
4hr | 2-4hr
70
Morphine metabolism
Primarily phase II glucuronidation
71
NSAIDs mechanism of action
Inhibition of cyclooxygenase (COX), which is key step in prostaglandin synthesis
72
Receptors are widely distributed in body including gut and platelets (causing bleeding)
COX1
73
Produced in response to inflammation
COX2
74
COX non selective agents affect:
Fever Inflammation Pain Thrombosis
75
COX2 selective
Increase risk of MI, thrombosis, stroke
76
What does aspirin and acetaminophen do?
Inhibit COX
77
Nonselective NSAIDs available for IV use:
Ketoroloac Ibuprofen Diclofenac
78
What are potential negative effects of nonselective NSAIDs?
Bone healing and anastomotic leak after colorectal surgery
79
What is Ketorolac NSAID?
Parental Only short term for mild to moderate pain Renal insufficiency (elevated sCr) Inhibition of platelet aggregation
80
Acetaminophen does what?
Inhibits COX1 and COX2
81
How is acetaminophen administered?
PO and IV
82
Max does of acetaminophen?
4g/24hrs
83
Hepatic impairment of acetaminophen?
Low dose <2-3g/day causation about other factors (alcohol, nutritional status, renal function) Severe impairment: contraindicated

Pharmacology (14 decks)

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