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Spring 2020 - Pharmacology 1 > Induction + Pain Management - Quiz 3 > Flashcards

Induction + Pain Management - Quiz 3 Flashcards

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1
Q

Etomidate

A

Causes Hypnosis

No Pain Properties

Minimal CV Effects

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2
Q

Etomidate’s Chemical Structure

A

Carboxylated Imidazole

2 Isomers: R+ is active

PG Solvent

pH: 8.1

Only induction med that is NOT racemic mixture

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3
Q

Etomidate MOA

A

Potentiates GABAA mediated Chloride Shift

Act like Barbs at Higher Doses

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4
Q

Etomidate Pharmacokinetics

A
  • Rapid half-life, Rapid Total Clearance
  • Single Dose - extremely short duration (3-5 min)
  • Peak: 1 min
  • Protein Bound
  • 3 Compartment Model
  • Hepatic extraction
  • Minimal Buildup - can redose
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5
Q

What limits use of Etomidate

A

Transient Depression of Adrenocortical Function

  • Lasts 4-8 hrs.
  • Reversible
  • increased mortality in Septic/Hemorrhaging Pts.
  • Advantage: stress free anesthetic
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6
Q

Etomidate CNS Effects

A

Decreased CBF

Decreased CMRO2

Decreased ICP while maintaining CPP

Maintains cerebral vessel response to CO2

Decrease IOP

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7
Q

Etomidate CV Effects

A

CV stability - minimal changes

except

Pts. w/ aortic stenosis or mitral valve disease - significant drop in BP, PAP, PCWP

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8
Q

Etomidate Respiratory Effects

A

Decrease Minute Volume

Compensatory increase RR

Decrease ventilatory response to CO2

Apnea followed by Hyperventilation

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9
Q

Etomidate’s other effects

A

PONV

Does NOT effect duration of seizure

Myoclonic Jerks (decreased w/ prior opioid med)

No Histamine Release

Low Allergy Risk

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10
Q

Precedex

A

Highly Selective Alpha 2 Agonist

1600 : 1 - alpha2 : alpha 1

(220 : 1 for Clonidine)

Water Soluble

D-isomer is the Active Part

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11
Q

Precedex MOA

A

Negative Feedback on a2 receptors and makes a2 agonist effects

Sleep mimics Normal sleep

Pain Properties

Tolerance happens

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12
Q

Why is Clonidine sometimes used on kids?

A

Adjunct therapy for ADHD

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13
Q

Precedex Pharmacokinetics

A

Protein Bound

Rapid Hepatic Metabolization

Excreted in Urine & Bile

Rapidly Cleared

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14
Q

Precedex CNS Effects

A

Decrease CBF

No ICP Change

No CMRO2 Change

Decrease Plasma Catecholamine

Decrease MAC Requirement

Decrease need for Opioid

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15
Q

Precedex CV Effects

A

Moderate ↓HR & ↓SVR

Bolus may cause brief increase in BP & Bradycardia

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16
Q

Precedex Respiratory Effects

A

Small ↓Tidal Volume

No signifcant change in RR

No change to CO2 Response

Mild Airway Obstruction

Synergistic w/ other Sedatives

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17
Q

What is the max infusion time for Precedex per the package insert?

A

24 Hours

Still safe after 24hrs, but you might see lack of effect and changes in blood pressure.

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18
Q

Precedex Withdrawal

A

Upregulation of Receptors

An abrupt stop = accelerated HTN

Higher risk of HTN for pts who are already at risk.

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19
Q

General Anesthetics and Preggos

A
  • Black Box Warning: causes poor cognitive and school performance for the kid
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20
Q

General Anesthetics and Preggos:

American College of Ob/Gyn

A

Disagrees w/ Black Box Warning - Can’t generalize based on animal testing

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21
Q

General Anesthetics and Preggos

JAMA

A

Sibling Study: No adverse effects in child development

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22
Q

General Anesthetics and Preggos

MASK Trial

A

Single Exposure: No deficits

Secondary Exposure: Possible deficits in processing speeds and fine motor skills

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23
Q

Nociceptive Pain

A

Has obvious site of pain

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24
Q

Nociceptive Stimulation

A

Noxious Stimuli release neural chemicals that stimulate other nociceptors

  • Bradykinin, Substance P, Potassium, Histamine, Prostaglandin, Luekotriens
  • Transmits signal to Spinal Cord
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25
Nociceptive Transmission
Action potential moves from stimuli site to dorsal horn of spinal cord, then CNS * Many pathways * A Fibers: large diameter, myelinated - sharp pain * C Fibers; small diameter, unmyelinated - dull, aching pain
26
What are released from the dorsal horn during nociceptive transmission?
Glutamate Substance P Calcitonin Peptide
27
Nociceptive Perceception
Conscious Pain Experience Impulse relayed thru thalamus
28
Nociceptive Modulation
Impulse Inhibition via Brain Stem * Body's opioid * Serotonin * Norepi * GABA
29
Neuropathic Pain
Does NOT follow pain cascade Nerve Misfire Never damage, Persistance Stimulation, Autonomic Dysfunction Burning, tingling, shocks, hyperalgesia, headache
30
What is Chronic Pain
\> 3 months or past the time of normal healing 20% of non cancer pts. receive opiods
31
Pain Monitoring
* **P**rovocative factors * **Q**uality * **R**adiation * **S**everity * **T**emporal relations
32
Opiate Addiction
\> 5 days = addiction risk 6% s/p minor surgery kept using opiates for at least 90 days Increased addiction risk for middle age (45-64 yo)
33
Who are at risk for Inadequate Pain Control
Minorities Women Elderly Cognitively Impaired Cancer/EOL
34
Optimal Length of Opioid Scripts
* General Surgery: 4-9 days * Women's Health Procedures: 4-13 days * Musculoskeletal Procedures: 6-15 days
35
How does Esmolol work for pain?
Blunts cardiovascular effects of massive sympathetic outflow Short half-life
36
Location of Opioid Receptors
Brain Spinal Cord GI Tract
37
What are the subtypes of Opioid Receptors
Delta Kappa **Mu** - primary Nociceptive
38
Delta Opioid Receptors
Brain & Peripheral Nerves Analgesia, Antidepressant, Dependence
39
Kappa Opioid Receptors
Brain, Spinal Cord, Periphery Analgesia, **Sedation**, Miosis, Dysphoria, ADH Inhibition Urinary Hesitance
40
Mu Opioid Receptors
Brain, Spinal Cord, Periphery, Intestine * Mu1: Analgesia, Dependence * **Mu2**: Resp. depression, euphoria, reduced GI motility, dependence * Mu3: Unknown
41
Nociceptive Opioid Receptors
Brain, Spinal Cord Anxiety, Depression, Appetite, Tolerance to Mu Agonist
42
How do Opiates Work
**Presynaptic:** Binds to G-Coupled Proteins (2nd msgr) - Amplifies signal --\> Inhibits Adenylate Cyclase --\> lowers cAMP --\> less Ca++ --\> stops neurotransmitter release (stopping _some_ pain signal) **Postsynaptic:** Glutamate can still bind, but opiate also binds here --\> opens K+ channel for K+ release --\> creates negative field --\> glutmate unable to cause action d/t hyperpolarization
43
NMDA Receptors & Opioids
Can reduce opioid effectiveness Glutamate overstimulation = neuropathic pain Methadone blocks NMDA
44
Which structure form of Opioids have agonist action?
Levo Rotary Forms
45
Are Opioids Ionized?
Yea, they gotta be to form a strong bond with the opioid receptor (Lipophilic with an Ionized branch)
46
How does codeine work?
Its a prodrug needing to be metabolized to turn into morphine.
47
Morphine and Pain
* Increases pain threshold and modifies pain perception * Works better for continuous dull pain vs sharp pain * Effective for visceral, skeletal, and skin pain * Most effective if given **before** surgical stimulus * Cause dysphoria if there is not pain
48
Does morphine need to enter CNS to work?
No
49
Morphine Metabolism
85%: M3G (Inactive) 10%: M6G (Active) & 100x more potent Renal failure can cause M6G buildup
50
Morphine CV Effects
Bradycardia Reduced SNS Response Histamine Release - itching, vasodilation Orthostatic Hypotension
51
Morphine Respiratory Effects
Dose dependent ventilatory depression via Mu2 Receptors ↓CO2 Response ↑Resting PaCO2 Asynchronous breathing + Cough Suppression
52
Morphine CNS Effects
Careful with Head Injuries Effects Wakefulness Pupil Constriction ↑ICP Broken Blood Brain Barrier increases morphine sensitivity
53
How does pt's EEG look on Morphine?
Looks like sleep w/ no seizure activity
54
With Morphine, sedation happens ________ pain relief and is not equivalent.
BEFORE
55
How does morphine effect the biliary tract?
Cause biliary spasms and increased pressure
56
What can be used to treat opioid induced biliary spasms?
Glucagon 2mg IV (normally used for bradycardia from beta blocker overdose)
57
Morphine and GI Tract
Constipation Biliary Colic Delayed Emptying NV from Chemoreceptor Trigger Zone Stimlulation
58
How to treat Opioid Induced Constipation
1. Senna, NOT Docusate 2. Add 2-3 OTC laxatives 3. Consider New Mu Antagonist
59
Morphine GU Effects
Have to pee but cant
60
Morphine Other Effects
No affect on NMB drugs Rapid injection = chest rigidity Exaggerated CNS depression w/ MAO inhibitors
61
Dilaudid Vs Morphine
Synthetic and has no active metabolites More Stable for Renal Dysfunction No significant Histamine Release
62
Fentanyl vs Morphine
More Potent Faster Onset (Not Instant) Shorter Duration Protein Bound More Lipophilic
63
Fentanyl Pharmacokinetics
Redistributes to Inactive Tissues Lungs store 75% of single dose Stay in blood for a while d/t reuptake from inactive tissues
64
Fentanyl Metabolism
Liver Enzymes Norfentanyl Metabolite (limited activity) Excreted in urine Can be detected in urine for 72 hrs.
65
Fentanyl CNS Effects
Modest ↑ICP No Seizure Low-Mod doses don't effect evoked potentials
66
Fentanyl CV Effects
Bradycardia ↓BP ↓CO No Histamines
67
Fentanyl Respiratory Effects
Persistent Ventilation Depression Recurrent ventilation depression from second Peak
68
What kind of drug interactions do Opioids have with Benzos?
Synergism 1+1 = 3
69
Why is there less opioid plasma concentration in cardiopulmonary bypass?
Fentanyl sticks to the machine
70
Intrathecal Fentanyl
Rapid Profound Labor Pain Relief
71
Oral Fentanyl (Actiq)
Used to reduce Pre-op Anxiety and Help with Induction
72
Fentanyl Patch
Last 3 Days Takes much longer for it to work
73
Sufentanil vs Fentanyl
5-10x more Potent Shorter Half Life than Fentanyl
74
Sufentanil Metabolism
Liver Enzymes Renal Dysnfunction = prolonged ventilation depression
75
Sufentanil CNS Effects
↓CMRO2 ↓CBF
76
Sufentanil CV Effects
Bradycardia ↓CO
77
Sufentanil Respiratory Effects
Ventilation Depression Chest rigidity
78
Alfentanil
1/5 - 1/10 as potent as Fentanyl Short half-life Fast effect-site equilibrium Useful for ICU intubation, cardioversion, retrobulbar block
79
Afentanil Metabolism
Highly Dependent on Liver
80
Remifentanil
Selective Mu Agonist Similar Potency to Fentanyl Fast site equilibrium similiar to Alfentanil Moderatly Lipophilic Structurally Unique - Ester Link
81
Remifentanil Pharmacokinetics
**Very** rapid Clearance - 3L/min Works the same in all shapes and sizes of people
82
Remifentanil Metabolism
Excreted by kidneys 6 minute half life No buildup Precisely Titratable
83
Remifentanyl CNS Effects
No ICP/IOP Change High Dose = ↓CMRO2 & ↓CBF
84
Remifentanil CV Effects
Mild ↓HR Mild ↓BP No Histamine release
85
Remifentanil Respiratory Effects
Ventilation Depression Nausea and Vomiting
86
Remifentamnil Tolerance
High Post-Op Analgesia requirement

Spring 2020 - Pharmacology 1 (11 decks)

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