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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
What contributes to differential nerve block
Distance d/w nodes of ranvier
26
An impulse can make it through how many blocked nodes
2
27
Blockade of __ nodes eliminated conduction along myelinated nerve fiber, __ fiber
3. A.
28
Which agent can do sensory block w incomplete motor block
Bupivicaine. A delta and C fibers blocked. A alpha, beta, and gamma not completely blocked
29
Physiochemical factors for la absorption
PKA, ph, lipid solubility
30
Physiologic conditions for LA absorption
PH of tissue, pco2, temp, pt characteristics
31
High to low absorption of block
IV, tracheal, intercostal, caudal, paracervical, epidural, brachial plexus, subarachnoid, SQ
32
Ionization of LAs
Unionized diffuses across nerve membrane, once inside unionized and ionized equilibrate, ionized binds receptor inside na channel= blockade
33
Ionized form favored in which environment
Acidic drug in basic enviro. Basic drug in acidic enviro
34
Non ionized form favored when
Acidic drug in acidic enviro
35
LAs are __ in body and __ in bottle. PKA range
Basic, acidic. 7.5-9
36
___ drug penetrates nerve sheath and axon membrane to reach site of action
Non ionized
37
___ drug binds and blocks na channel
Ionized
38
In high/normal ph the rate and amt of absorption is ___
Higher
39
PKA high to low
Procaine (8.9), tetracaine (8.5), bupivicaine, chlorprocaine, lidocaine, etidocaine, mepivacaine
40
What bicarb does to block
Inc onset, enhances depth, and inc spread of block
41
What temp does to absorption
Decreasing temp reduces drug absorption across nerve membrane
42
Hasselbach eqn
Ph-pka= log nonionized/ionized
43
Most imp[ortant factor in potency. 3 most potent
Lipid solubility. Most lipid soluble: etidocaine, bupivicaine, tetracaine
44
DOA proportional to what
Amt of time LA in contact w nerve fiber
45
Most imp factor DOA
Protein binding
46
Purpose of using vasoconstrictor w LA
Inhibiting systemic absorption, prolonging effect, detecting IV injection
47
3 long acting
Tetracaine, etidocaine, bupivicaine
48
2 moderate acting
Lidocaine, mepivicaine
49
2 short acting
Procaine and chloroprocaine
50
What determines LA conc in blood
Concentration LA, tissue blood flow
51
LA metabolism
Hydrolyzed by pseudocholinesterase enzymes in plasma, less extent in liver
52
LA metabolite, exception to metab
PABA. Cocaine metab in liver mainly
53
Metabolism of amides
Liver, microsomal enzymes. More complex and slower than metab of esters. Aromatic hydroxylation, n dealkylation, amide hydrolysis
54
Onset most influenced by
PKA
55
Max dose: bupivicaine
2.5 mg/kg
56
Max dose: ropivicaine
3 mg/kg. 3.5 mg/kg w epi
57
Max dose: etidocaine
4 mg/kg
58
Max dose: lidocaine
4 mg/kg. 7 mg/kg w epi
59
Max dose: mepivicaine
4 mg/kg. 7 mg/kg w epi
60
Max dose: chlorprocaine
12 mg/kg
61
Max dose: cocaine
3 mg/kg
62
Max dose: tetracaine
3 mg/kg
63
Most cardiac toxic
Bupivicaine, cardiac arrest at low toxic levels
64
Inc risk of cv toxicity
Pregnancy, hypoxia, ph abn, cv modulating drugs
65
Dose of intralipid
20% 1.5 ml/kg rapid bolus. Gtt 0.25 ml/kg/min for 10 min
66
Allergic rxns: which more common, preservative rxn
Esters d.t paba. Methylparaben
67
Analgesia promoted by adding what to LA
Opioids, clonidine, epi
68
What prolongs DOA of ester anesthetics
Pseudocholinesterase inhibitors
69
Which drugs dec hepatic bf and dec clearance Of amide LA and cocaine
Cimetidine and propranolol
70
Procaine: what it is, use
Ester prototype, spinal anesthesia
71
Procaine: why not ideal
PKA 8.9, slow onset, 97% ionized. Short DOA. Nausea, cns SE, metabolite interferes w efficacy of sulfonamide abx
72
Tetracaine: use, DOA
Spinal and corneal anesthesia. Long, 6 hrs w epi
73
Tetracaine: implic w epidural
Not popular, slow onset and profound motor block. Toxicity risk w large doses
74
Chloroprocaine: use
OB epidural anesthesia, fast hydrolysis in serum reduces toxicity risk. Short duration
75
Lidocaine: % for topical, regional, PNB
4, 0.25-0.5, 1-2
76
Lidocaine: % for spinal and epidural
1.5-5%, 1.5-2%
77
Lidocaine metabolites
Monoethylglycinexylide 80% activity, xylidide 10%
78
Lidocaine linked to what w spinal use
Cauda equina syndrome
79
Mepivicaine: similarities
Structurally- bupivicaine. Clinically- lidocaine.
80
Mepivicaine: onset, DOA, e 1/2
Rapid, less vasodilation= longer DOA, 2 hrs
81
Mepivicaine: toxicity, not effective where
More cns toxicity than lidocaine. Topically
82
Prilocaine: metabolite, avoid in what
Ortho toluidine, toxic, avoid in OB
83
Prilocaine: max dose and what can happen
>600mg leads to conversion of hgb to methemoglobin.
84
Prilocaine: tx for methemoglobinemia
Methylene blue 1-2 mg/kg iv over 5 min
85
Etidocaine: % for Pnb, epidural
0.5-1%. 1-1.5%
86
Etidocaine: about solubility and duration
Lipid soluble, long acting, rapid onset. PKA 7.7
87
Bupivicaine: comparison to lido, good choice for what
Longer DOA and onset than lido. Good for differential nerve block (sensory > motor) and for labor or post op pain
88
Bupivicaine: concentrations for spinal, epidural, PNB
Spinal: .5-.75. Epidural: .0625-.5, PNB: .25-.5
89
Bupivicaine: ___ bound to what. SE pro
Protein, alpha 1 glycoprotein. Low incidence of neuro complic w spinal.
90
Bupivicaine SE con
Cardio toxic (0.5% or lower conc for epidural and PNB), serum e 1/2 3.5 hrs, lasts super long
91
Ropivicaine: structure, good for what
S or levo enantiomer of homolog of bupivicaine w propyl tail on pipe riding ring. Differential block
92
Ropivicaine: less ___, more ___. Use when ___ __ needed
Cardiotoxic, vasoconstriction. Larger doses
93
Ropivicaine: how its different from bupivicaine
2 active metabolites, shorter 1/2t (2 hrs) than bupiv
94
Levo bupivicaine: structure, less what
S- enantiomer of bupiv. Less cardiotoxic
95
Levo bupivicaine: 1/2t, use when
2.6 hrs, large local doses needed
96
PNB dosing dictated by what
Volume by type of block. Conc based on limitations of max dose balanced w density of block desired
97
Epidural: vol dictated by what
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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