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Spring 2020 - Pharmacology 1 > Pain Management + Local Anesthetics - Midterm Wrap Up > Flashcards

Pain Management + Local Anesthetics - Midterm Wrap Up Flashcards

1
Q

Meperidine

A

Opioid Agonist at Mu & Kappa

Derived from Phenylepiperidine

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2
Q

Meperidine’s structure is similiar to…

A

Atropine

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3
Q

What analogues were developed from Meperidine?

A

All the Fentanyl’s

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4
Q

Meperidine Metabolism

A

90% Hepatic

Demethylation to Normeperidine –> Meperidinic Acid

Excreted by Kidneys

Renal Impairment = Buildup

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5
Q

Meperidine Pharmacokinetics

A

3-5 hr. Half-Life

Protein Bound

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6
Q

Normeperidine

A

1/2 Analgesia of Meperidine

15 hr. Half-life; > 35 hrs. for renal pts.

CNS Stimulation & Toxicity - myoclonus + seizure

Demerol Delirium

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7
Q

Meperidine CV Effect

A

Decrease SNS Reflex

Orthostatic Hypotension > Morphine

Tachycardia (Atopine-like)

Big Dose = ↓Inotropy

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8
Q

Meperidine Respiratory Effect

A

Ventilation depression > Morphine

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9
Q

Meperidine Serotonin Syndrome

A

Autonomic Instability

  • HTN
  • ↑HR
  • ↑Temp + Diaphoresis
  • Rigidity
  • Hyperreflexia
  • Confusion
  • Coma, Seizure
  • Coagulopathy
  • Metabolic Acidosis
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10
Q

What to give for Post-Op Shivering?

A

Demerol: 12.5 - 25 mg

Sufentanil, Ultram, Clonidine, Ketamine

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11
Q

Slide 77

A
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12
Q

Methadone

A

Mu Agonist + NMDA Antagonist

Variable 8-60 hr. Half-life
(Unpredictable)

QT Prolongation

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13
Q

Opioid Agonist-Antagonist Meds

A

Pentazocine

Bremazocine

Dezocine

Naluphine

Buprenorphine

Nalorphine

Butorphanol

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14
Q

Opioid Agonist-Antagonist

A

Binds to Mu (+ delta, kappa)

Part Agonist: limited Mu effect

Part Competitive Antagonist: no mu effect

Effects subsequent Opioid administration

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15
Q

Opioid Agonist-Antagonist Advantages

A

Pain relief w/ limited ventilation depression

Low addiction risk

Effect Ceiling, but can still die

For pts. who cant tolerate pure opiates

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16
Q

Opioid tolerance can occur ______ dependence.

Opioid dependence cannot occur ________ tolerance

A

Tolerance can occur without dependence

Dependence cannot occur without tolerance = addiction

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17
Q

Opioid Antagonists

A

Small structural changes convert agonist into antagonist

Subbing alkyl for methyl group

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18
Q

What is the N-alkyl derivative of Oxymorphone?

A

Naloxone

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19
Q

What are the Pure Opioid Antagonists?

A

Naloxone

Natrexone

Nalmefene

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20
Q

Opioid antagonists and the Receptor

A

High receptor affinity

Bumps off agonist and binds to mu receptor for antagonism

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21
Q

Naloxone

A

Nonselective Antagonist at all 3 Opioid Receptors

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22
Q

What does nalaxone do?

A

Treats ventilation depression

(also treats newborn with opioid mom)

Reverses Overdose

Detects Physical Dependence

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23
Q

Naloxone Duration of Action

A

30-45 min

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24
Q

Naloxone Metabolism

A

Liver Enzymes

60-90 min Half-life

May redose

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25
Q

Naloxone Side Effects

A

Return of Pain

NV r/t Injection Speed

Sympathetic Outflow

(Tachy, HTN, P. Edema, Dysrhythmias)

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26
Q

Tramadol

A

Mu Agonist

Weak SNRI

No metabolite

Interacts with SSRIs

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27
Q

Tramadol Contraindication

A

Seizure Disorder

Can also cause new onset Seizure

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28
Q

NSAIDs MOA = COX Inhibition

(Cyclo-Oxygenase Enzyme)

A

Platelet Inhibition + GI Mucosal Thinning = Bleed

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29
Q

Toradol

A

COX2 Inhibitor - Celecoxib - no mucosal thinning effect, but still has platelet inhibition

  • Black Box Warning - GI Bleeds, Peptic Ulcers, Bleeding in General
  • Contracindicated for Labor & Deliver - inhibits fetal circulation
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30
Q

Toradol Side Effects

A

ARF

GI

CHF

Platelet Malfunction

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31
Q

Ofirmev

A

15 min Onset

4-6 hr. Duration

Liver Toxicity

MOA: reduced PG production, weak COX inhibition

Napqi metabolite, mucomyst binds to makes it non toxic

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32
Q

Endocannabinoid System

A

2 Major: 2AG & AEA

Slows Down Pain Impulses by reducing cAMP

Lipophilic

CB1 Receptor on Postsynaptic Terminal

Inhibits Ca++ –> Inhibits Neurotransmitter release

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33
Q

Where are CB1 Receptors Found?

A

Everywhere

Brain, Liver, Reproductive System, CV System

Skeletal Mucles, GI

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34
Q

Where are CB2 Receptors?

A

Pheripheral Tissues

Immune Cells

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35
Q

THC

A

Psychoactive

CB1 Agonist

Weak CB2

CYP Metabolized

Antiseizure, muscle relaxant, ↑appetite, antioxidant, sedative

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36
Q

CBD

A

Not Psychoactive

Reduces THC effects

Low CB1 & CB2 affinity

CYP Metabolism

Anxiolytic, Anti-Seizure, Antioxidant

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37
Q

Cannabis Side Effects

A

Tachycardia

HTN

Cough, Wheeze, Sputum

Euphoria, Disorientation, Confusion

Psychosis, Depression

38
Q

What is Gabapentin Used For?

A

Used for Neuropathy > Seizure Control

39
Q

Gabapentin MOA

A

Blocks Alpha 2 Delta Ca+ Channels –> Increases GABA reduction in Glutamate

40
Q

Gabapentin for Post-Op Pain

A

Give PreOp

Improved Post-Op Pain

Reduce Opiate Requirement

Highest Risk: Increased PostOp Sedation

41
Q

Gabapentin ADRs

A

Well tolerated

Neutropenia

Dizziness/Ataxia

Fatigue

Nystagmus/Diplopia

NV

Gabapentin + Opiate = Severe Resp. Distress

42
Q

Local Anesthetics

A

Reversibly block electrical impulses along nerve fiber

43
Q

What happens to the nerve fiber when you remove the Local Anesthetic?

A

Spontaneous & Complete return of nerve conduction w/o damage

44
Q

What is the effectiveness of a Local Anesthetic dependent on?

A

Physiochemical Properties of the Anesthetic

&

Anatomy of Nerve being Blocked

45
Q

What is the Axolemma

A

Cell membrane of an axon

46
Q

What are Schwanna Cells

A

Cells that cover the axon(s)

47
Q

Nodes of Ranvier

A

Nerve segments b/t Schwann cells that dont contain myelin

48
Q

What is Saltatory Conduction?

A

Jumping of Action Potentials from node to node

49
Q

Fasciculi

A

Bundles of Axons

50
Q

How do Local Anesthetic effect Actional Potentional?

A

Hyperpolarizes and keeps the nueron to just below resting potential

51
Q

A-Alpha Fibers

A

Biggest Diameter

Most Myelination

Fastest Conduction

Motor Function & Propioception

52
Q

A-Beta Fibers

A

4-15µm Diameter

Second Fastest Conduction

Motor, Touch & Pressure Sensation

53
Q

A-Gamma Fibers

A

4-15µm Diameter

Muscle Spindles & Reflex

54
Q

A-Delta Fibers

A

3-4µm Diameter

Slowest Conducting A Fiber

Pain & Temperature Sensation

55
Q

B Fibers

A

4µm Diameter

Slower Conduction & Less Myelination than A FIbers

Preganglionic Autonomic Nerves

56
Q

C Fibers

A

1-2µm Diameter

Slowest Conduction

Pain & Temperature Impulses

Unmyelinated

57
Q

Less Myelination makes the neuron ________ sensitive to Local Anesthetics

A

Less Myelination makes neuron more sensitive to LA

58
Q

How do Local Anesthetics work on Spinal Nerves

A

B Fibers –> C FIbers –> A Fibers

Motor Sensation is lost last

59
Q

Local Anesthetic MOA

A

Reversibly Block Na+ Channels

Receptors are inside cell and like the charged form of LA.

Lipophilic to enter cells, w/ an ionized portion to bind

60
Q

Local Anesthetics Chemical Structure

A

Unsaturated Aromatic Ring

Tertiary Amine

Intermediate Carbon Group - where they differ

61
Q

What are the different Intermediate Groups for Local Anesthetics?

A

Ester & Amide

Determines how it will be metabolized and allergy potential

62
Q

Local Anesthetics - Esters

A

No “i’s” in the first part of name

Procaine

Chloroprocaine

Tetracaine

Cocaine

63
Q

Local Anesthetics - Amides

A

Lidocaine

Prilocaine

Mepivacaine

Ropivacaine

Bupivacaine

Levobupivacaine

Etidocaine

64
Q

What determines Local Anesthetic Onset of Action?

A

Lipid Solubility / Amount of Non-Ionization

pKa

65
Q

Local Anesthetic with a pKa closest to physiological pH will have a _________ concentration of non-ionized form

A

Closer to Body’s pH = Higher Concentration of Non-Ionized Form

66
Q

How do Local Anesthetics travel in the body?

A

Injection of LA –> Non Specific Tissue or Blocks Nerve —> Bloodstream – Systemic tissue distribution –> Liver —> Renal Excretion

67
Q

What effects Local Anesthetic Duration of Action?

A

Highly lipid soluble = longer duration

Highly lipid soluble also = more protein bound

68
Q

Converting Local Anesthetic Percentage of Concentration to mL

A
  1. Take percentage number, add “gram”
  2. Put that number over “100 mL”
  3. Convert to milligrams

Ex:

1% —> 1gram/100mL x 1mg/.001gram = 10mg/mL

69
Q

Local Anesthetics Pharmacokinetics

A

LA’s are meant to stay in area of injection

Higher LA concentration = Faster Onset

Systemic Absorption = termination of effect

70
Q

What does systemic absorption of Local Anesthetics depend on?

A

Blood Flow

71
Q

How does Epinephrine effect Local Anesthetics?

A

↑Duration of Action

↑Nerve Uptake

↑Analgesia Quality

↓Systemic Toxicity

↓Vascular Absorption

72
Q

Local Anesthetics blocks sodium channels

What else can happen because of this?

A

Vasodilation, increasing LA absorption, limiting its duration and increases toxicity

Does not apply to

Cocaine

73
Q

Which highly perfused organs are responsible for initial uptake of Local Anesthetics?

A

Brain

Lung

Heart

Liver

Kidney

74
Q

Which moderately perfused tissues provide the greatest reservoir for Local Anesthetics

A

Muscle mass due to its large mass

75
Q

What are Procaine and Benzocaine metabolized into?

A

P-Aminobenzoic Acid (PABA)

↑Allergic potential

Persian, Jewish, Alaskan have high risk for abnormal pseudocholinesterase

76
Q

Amide LA Metabolism

A
  • Liver Enzymes - P450
  • Rate of Metabolism
    • Prilo>Lido>Mepiva>Ropiva>Bupiva
  • ↓Liver Function = ↑Toxicity
77
Q

Buildup of which metabolites convertes Hgb to Methemoglobin?

A

Prilocaine & Benzocaine Spray metabolites

Treat with Methylene Blue: 1-2mg/kg over 5 min

78
Q

Signs an Symptoms of Methemoglobinemia

A

Brown Gray Cyanosis

Tachypnea

Metabolic Acidosis

79
Q

What are added to Local Anesthetics to increase the Safety, Quality, Intensity, and Rate of Onset?

A

Opioids

Sodium Bicarbonate

Epinephrine

80
Q

What else factors into Local Anesthetic Toxicity?

A

Accidental Intravascular Injection

and

Excessive Dose

81
Q

Cardiac Effects of Local Anesthetic Toxicity

A

As toxicity inceases….

HTN & Tachycardia –> Bradycardia, Hypotension, Arrythmias –> Asystole

82
Q

Cerebral Effects of Local Anesthetic Toxicity

A

As toxicity increases…

Mental Abnormalities –> Confusion, Dizziness, Tinnitus, Metal taste –> Seizure

83
Q

Local Anesthetic CNS Toxicity Management

A
  1. Assure Adequate Airway & Ventilation
  2. Give Anti-seizure Med

CNS Toxicity can progress to Cardiac Arrest

84
Q

How does Local Anesthetic Toxicity in the CV compare to CNS?

A

CV is more resistant to Toxicity

CV Toxicity = Super Bad, No Antidote

85
Q

Local Anesthetic Cardiovascular Toxicity

A

LA slows everything down

  • Reduces heart automaticity, refractory period, contractility & conduction
  • Vasodilation
  • Bradycardia + Heart Block + Hypotension = Cardiac Arrest
86
Q

What happens if you accidentally give Bupivacaine Intravascularly?

A

Severe Cardiotoxicity

To fix, you need HIGH doses of pressors & prolonged resuscitation effort.

87
Q

What is Intralipid?

A

10-30% Lipid Emulsion

Binds with Lipophilic LA rather than just let it float around in bloodstream

Propofol wouldn’t work for this

88
Q

Transient Neuro Symptoms of Spinal Anesthesia

A

Dysesthesia, Burning, Lower Extremity & Butt Aches

Lasts 10 days - 2 wks

Lidocaine: 13% Incidence, then Bupivicaine is #2

89
Q

What is a Eutectic Mixture (EMLA)

A

Adding two liquids together = solid (creams)

Apply 1 hr before for effect

90
Q

What is the risk for applying Local Anesthetics to Mucous Membranes?

A

Absorption to systemic circulation & toxicity

91
Q

Topical Cocaine

A

Unique d/t Vasoconstriction

Blocks Epi & Norepi Uptake - Ventricular Arrhythmias

B-Blocks increase HTN = stroke & MI

Spring 2020 - Pharmacology 1 (11 decks)

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