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Anesthesia Pharm > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

Where are afferrent and efferent neurons

A

Afferrent- dorsal roots, sensory. Efferent- ventral roots, motor

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2
Q

Myelinated nerve fiber

A

Schwan cell around axon several times

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3
Q

Unmyelinated nerve fiber

A

Single Schwann cell around several axons

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4
Q

Lytes in and out of cell

A

Extracellular: high na, low k. Intracellular: high k, low na

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5
Q

A alpha fiber function

A

Motor and proprioception

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6
Q

A beta fiber function

A

Motor, touch, pressure

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7
Q

A gamma fiber function

A

Motor/muscle tone, muscle spindle

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8
Q

A delta fiber function

A

Pain, temp touch

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9
Q

B fiber

A

Pre ganglionic autonomic

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10
Q

C fiber function

A

Dull pain, temp, touch. Postganglionic autonomic, no myelin

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11
Q

Size of fibers large to small

A

A alpha, a beta, a gamma, a delta, b fibers, C fibers

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12
Q

Large fibers have the highest what and lowest what

A

Highest conduction velocity lowest threshold for excitability

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13
Q

Sequence of anesthesia: 1 to 5

A

Sympathetic (vasodilation, warm). Loss of pain and temp. Loss of proprioception. Loss of touch and pressure. Motor block

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14
Q

Polarized state of neuron

A

Intracellular space is negative compared to extracellular

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15
Q

Movement of what maintains rmp

A

Potassium

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16
Q

Receptor for LA

A

Voltage gated na channels in inactivated closed state

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17
Q

What kind of nerve is more sensitive

A

Repetitively stimulated > resting

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18
Q

LA structure

A

Lipophilic head (aromatic ring), intermediate chain (amide nh or ester coo-) and hydrophilic tail (tertiary amine)

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19
Q

Which LAs are amides

A

I before the Caine. Lidocaine, bupivicaine, etidocaine

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20
Q

Amide link metabolism

A

Liver

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21
Q

Ester linkage metabolism

A

Hydrolyzed by non specific esterases in plasma and tissues (mostly liver)

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22
Q

What increases potency and toxicity of LA

A

Inc in length of intermediate chain w carbons. Length of terminal groups on tail and aromatic ring

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23
Q

Which LAs more potent and longer DOA

A

Lipid soluble > water soluble

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24
Q

Max dose exparel, dose depends on what

A

266 mg or 20 ml. Depends on surgical site

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25
Q

What contributes to differential nerve block

A

Distance d/w nodes of ranvier

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26
Q

An impulse can make it through how many blocked nodes

A

2

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27
Q

Blockade of __ nodes eliminated conduction along myelinated nerve fiber, __ fiber

A
  1. A.
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28
Q

Which agent can do sensory block w incomplete motor block

A

Bupivicaine. A delta and C fibers blocked. A alpha, beta, and gamma not completely blocked

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29
Q

Physiochemical factors for la absorption

A

PKA, ph, lipid solubility

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30
Q

Physiologic conditions for LA absorption

A

PH of tissue, pco2, temp, pt characteristics

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31
Q

High to low absorption of block

A

IV, tracheal, intercostal, caudal, paracervical, epidural, brachial plexus, subarachnoid, SQ

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32
Q

Ionization of LAs

A

Unionized diffuses across nerve membrane, once inside unionized and ionized equilibrate, ionized binds receptor inside na channel= blockade

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33
Q

Ionized form favored in which environment

A

Acidic drug in basic enviro. Basic drug in acidic enviro

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34
Q

Non ionized form favored when

A

Acidic drug in acidic enviro

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35
Q

LAs are __ in body and __ in bottle. PKA range

A

Basic, acidic. 7.5-9

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36
Q

___ drug penetrates nerve sheath and axon membrane to reach site of action

A

Non ionized

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37
Q

___ drug binds and blocks na channel

A

Ionized

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38
Q

In high/normal ph the rate and amt of absorption is ___

A

Higher

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39
Q

PKA high to low

A

Procaine (8.9), tetracaine (8.5), bupivicaine, chlorprocaine, lidocaine, etidocaine, mepivacaine

40
Q

What bicarb does to block

A

Inc onset, enhances depth, and inc spread of block

41
Q

What temp does to absorption

A

Decreasing temp reduces drug absorption across nerve membrane

42
Q

Hasselbach eqn

A

Ph-pka= log nonionized/ionized

43
Q

Most imp[ortant factor in potency. 3 most potent

A

Lipid solubility. Most lipid soluble: etidocaine, bupivicaine, tetracaine

44
Q

DOA proportional to what

A

Amt of time LA in contact w nerve fiber

45
Q

Most imp factor DOA

A

Protein binding

46
Q

Purpose of using vasoconstrictor w LA

A

Inhibiting systemic absorption, prolonging effect, detecting IV injection

47
Q

3 long acting

A

Tetracaine, etidocaine, bupivicaine

48
Q

2 moderate acting

A

Lidocaine, mepivicaine

49
Q

2 short acting

A

Procaine and chloroprocaine

50
Q

What determines LA conc in blood

A

Concentration LA, tissue blood flow

51
Q

LA metabolism

A

Hydrolyzed by pseudocholinesterase enzymes in plasma, less extent in liver

52
Q

LA metabolite, exception to metab

A

PABA. Cocaine metab in liver mainly

53
Q

Metabolism of amides

A

Liver, microsomal enzymes. More complex and slower than metab of esters. Aromatic hydroxylation, n dealkylation, amide hydrolysis

54
Q

Onset most influenced by

A

PKA

55
Q

Max dose: bupivicaine

A

2.5 mg/kg

56
Q

Max dose: ropivicaine

A

3 mg/kg. 3.5 mg/kg w epi

57
Q

Max dose: etidocaine

A

4 mg/kg

58
Q

Max dose: lidocaine

A

4 mg/kg. 7 mg/kg w epi

59
Q

Max dose: mepivicaine

A

4 mg/kg. 7 mg/kg w epi

60
Q

Max dose: chlorprocaine

A

12 mg/kg

61
Q

Max dose: cocaine

A

3 mg/kg

62
Q

Max dose: tetracaine

A

3 mg/kg

63
Q

Most cardiac toxic

A

Bupivicaine, cardiac arrest at low toxic levels

64
Q

Inc risk of cv toxicity

A

Pregnancy, hypoxia, ph abn, cv modulating drugs

65
Q

Dose of intralipid

A

20% 1.5 ml/kg rapid bolus. Gtt 0.25 ml/kg/min for 10 min

66
Q

Allergic rxns: which more common, preservative rxn

A

Esters d.t paba. Methylparaben

67
Q

Analgesia promoted by adding what to LA

A

Opioids, clonidine, epi

68
Q

What prolongs DOA of ester anesthetics

A

Pseudocholinesterase inhibitors

69
Q

Which drugs dec hepatic bf and dec clearance Of amide LA and cocaine

A

Cimetidine and propranolol

70
Q

Procaine: what it is, use

A

Ester prototype, spinal anesthesia

71
Q

Procaine: why not ideal

A

PKA 8.9, slow onset, 97% ionized. Short DOA. Nausea, cns SE, metabolite interferes w efficacy of sulfonamide abx

72
Q

Tetracaine: use, DOA

A

Spinal and corneal anesthesia. Long, 6 hrs w epi

73
Q

Tetracaine: implic w epidural

A

Not popular, slow onset and profound motor block. Toxicity risk w large doses

74
Q

Chloroprocaine: use

A

OB epidural anesthesia, fast hydrolysis in serum reduces toxicity risk. Short duration

75
Q

Lidocaine: % for topical, regional, PNB

A

4, 0.25-0.5, 1-2

76
Q

Lidocaine: % for spinal and epidural

A

1.5-5%, 1.5-2%

77
Q

Lidocaine metabolites

A

Monoethylglycinexylide 80% activity, xylidide 10%

78
Q

Lidocaine linked to what w spinal use

A

Cauda equina syndrome

79
Q

Mepivicaine: similarities

A

Structurally- bupivicaine. Clinically- lidocaine.

80
Q

Mepivicaine: onset, DOA, e 1/2

A

Rapid, less vasodilation= longer DOA, 2 hrs

81
Q

Mepivicaine: toxicity, not effective where

A

More cns toxicity than lidocaine. Topically

82
Q

Prilocaine: metabolite, avoid in what

A

Ortho toluidine, toxic, avoid in OB

83
Q

Prilocaine: max dose and what can happen

A

> 600mg leads to conversion of hgb to methemoglobin.

84
Q

Prilocaine: tx for methemoglobinemia

A

Methylene blue 1-2 mg/kg iv over 5 min

85
Q

Etidocaine: % for Pnb, epidural

A

0.5-1%. 1-1.5%

86
Q

Etidocaine: about solubility and duration

A

Lipid soluble, long acting, rapid onset. PKA 7.7

87
Q

Bupivicaine: comparison to lido, good choice for what

A

Longer DOA and onset than lido. Good for differential nerve block (sensory > motor) and for labor or post op pain

88
Q

Bupivicaine: concentrations for spinal, epidural, PNB

A

Spinal: .5-.75. Epidural: .0625-.5, PNB: .25-.5

89
Q

Bupivicaine: ___ bound to what. SE pro

A

Protein, alpha 1 glycoprotein. Low incidence of neuro complic w spinal.

90
Q

Bupivicaine SE con

A

Cardio toxic (0.5% or lower conc for epidural and PNB), serum e 1/2 3.5 hrs, lasts super long

91
Q

Ropivicaine: structure, good for what

A

S or levo enantiomer of homolog of bupivicaine w propyl tail on pipe riding ring. Differential block

92
Q

Ropivicaine: less ___, more ___. Use when ___ __ needed

A

Cardiotoxic, vasoconstriction. Larger doses

93
Q

Ropivicaine: how its different from bupivicaine

A

2 active metabolites, shorter 1/2t (2 hrs) than bupiv

94
Q

Levo bupivicaine: structure, less what

A

S- enantiomer of bupiv. Less cardiotoxic

95
Q

Levo bupivicaine: 1/2t, use when

A

2.6 hrs, large local doses needed

96
Q

PNB dosing dictated by what

A

Volume by type of block. Conc based on limitations of max dose balanced w density of block desired

97
Q

Epidural: vol dictated by what

A

Level of block, 1.25-1.6 ml/segment. Conc based on block density desired (labor v surgical epidural)

Anesthesia Pharm (12 decks)

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