Locals Chart Flashcards

(158 cards)

1
Q

trade names of bupivicaine

A
Marcaine
Marcaine Preservative-Free
Marchaine Spinal
Sensorcaine
Sensorcaine-MPF
Sensorcaine- MPF Spinal
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2
Q

how is bupivicaine supplied

A

Racemic mixture @

  1. 25% = 2.5mg/mL
  2. 5% = 5mg/mL
  3. 75% = 7.5mg/mL
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3
Q

what is bupivicaine used for?

A

Subcutaneous
PNB
Epidural
Spinal

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4
Q

Subq dose of bupivicaine and form

A

0.25%

dose 2.5 mg/kg

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5
Q

PNB dose of bupivicaine and form

A

PNB 0.25-0.5%

dose 2.5 mg/kg

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6
Q

Epidural dose of bupivicaine and form

A

Epi: 0.5-0.75%

dose 2mg/kg

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7
Q

Spinal dose of bupivicaine and form

A

Spinal: 0.5-0.75%

dose 0.3 mg/kg

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8
Q

max dose of bupivicaine SUBQ AND PNB SAME!!

A

175mg

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9
Q

max dose of bupivicaine SUBQ AND PNB SAME WITH EPINEPHRINE

A

225mg

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10
Q

what is the MAX DOSE of Bupivicaine Epidural

A

170mg

**5 mg less than Subq and PNB

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11
Q

what is the MAX DOSE of Bupivicaine Epidural WITH EPINEPHRINE

A

225 mg

** this is the SAME as Subq and PNB with epinephrine

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12
Q

MAX DOSE WITH BUPIVICAINE

A

0.3 mg/kg

NO EPINEPHRINE WITH SPINALS

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13
Q

what is the toxic plasma concentration of bupivicaine

A

> 3mcg/mL

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14
Q

Protein binding of bupivicaine?

and what does this mean?

A

96%
LONG duration of action hours
*depends on dose and location for exact time

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15
Q

metabolism of bupivicaine

A

HEPATIC- ALL AMIDES
SLOWEST METABOLISM OF ALL LOCALS

w/etidocain and ropivicain
BER – toxicity risk

Amide Hydrolysis and conjugation

Aromatic hydrozylation
N-dealkylation

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16
Q

half life of bupivicaine

A

3.5 hours

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17
Q

what is the relationship of sensory vs. motor block with bupiviciane

A

sensory block often OUTLASTS motor

sensory- at site

motor 2 below

sympathetic- upto 6 above

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18
Q
duration of action of bupivicaine- why
Subcutaneous
PNB
Epidural
Spinal
A
LONG- because highly protein bound
Subq: 2-8 hours
PNB: 4-12 hr
Epi: 2-5 hr
Spinal: 1-6 hr
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19
Q

Adverse Reactions with Bupivicaine

what MUST you know about this drug?

A

CV- MOST CARDIOTOXIC*****

Binds Na channels- CV arrest, HR block, hypotension, palpitations, Ventricular arrhythmias

CNS: Anxiety, dizziness, circumoral numbness, restlessness, seizure, tinnitus, blurred vision, miosis

GI: N/V

MS: chondrolysis

Hypersensitive, anaphylaxis, itching, angioedema

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20
Q

pKa of bupivicaine and what does this mean?

A

8.1
*same as ropivicaine
intermediate onset

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21
Q

contraindications with bupivicaine

A

0.75% NEVER for OB epidural- CV arrest- difficult to resuscitate

NEVER Bier block- systemic toxicity risk with tourniquet release

Obstetrics- crosses placenta pregnancy category C never while breastfeeding

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22
Q

lipid solubility =

A

potency

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23
Q

protein binding =

A

duration of action

follow VERY far by lipid solubility

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24
Q

how does adding sodium bicarbonate to LAs affect them?

A

alkalinizing LAs
increases the lipophilic portion of Las
more potent- moves into cells faster

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25
the longer the carbon backbone of LAs…
the creating the LIPID SOLUBILITY PROTEIN BINDIN POTENCY DURATION OF ACTION
26
how does adding Epi (1:200,00) affect bupivicaine?
decreases blood levels by 10-20%
27
what conditions increase LAs toxicity
metabolic & respiritory ACIDOSIS decreased SZ threshhold decreased protein binding
28
System Absorption Rates of Various Sites
In Time I Can Please Everyone But Susie and Sally ``` IV Tracheal Intercostal Caudal Paracervical Epidural Brachial Plexus Subarachnoid (Sciatic, Femoral) Subq ```
29
trade name of Lidocaine
Xylocaine Xylocaine-MPF many topical names
30
how is lidocaine supplied?
0.5% = 5mg/mL 1% (5mL) = 10mg/mL 2% (5mL) = 20mg/mL 4% LTA 5% (2mL) = 50mg/mL 10% 100mg/mL LTA Kit- 4%
31
what is lidocaine used for?
``` Topical Infiltration IVRA- Beir Block- tourniquet PNB Epidural Spinal ```
32
dose of topical lidocaine AND form %
Topical – 4%, 4 mg/kg
33
dose of infiltration lidocaine AND form %
Infliltration: 0.5-1% 4mg/kg
34
dose of IVRA lidocaine | AND form %
IVRA: 0.25-0.5%, 4 mg/kg
35
PNB dose of lidociane AND form %
PNM: 1-1.5% 4 mg/kg
36
epidural dose of lidocaine and form %
Epi 1.5-2% 4 mg/kg
37
spinal dose of lidocaine AND form %
Spinal: 1.5-5% 1.5 mg/kg
38
protein binding of lidocaine and WHAT does that mean?
70% intermediate duration protein binding most determines duration of action
39
metabolism of lidocaine
Hepatic HEPATIC- ALL AMIDES Dealkylation → mono-ethylglycin-exylidide 80% activity of lidocaine as an anti-arrhythmic To Hydrolysis → xylidide 10%
40
onset of lidocaine and WHY
``` FAST because- pKa 7.7 Etidocaine also 7.7 second only to Mepivacaine 7.6 closest to physiologic pH most non-ionized most to cross into cell ```
41
1/2 life lidocaine
96 min
42
``` duration of lidocaine: each route Topical Infiltration IVRA- Beir Block PNB Epidural Spinal ```
``` Topical: 0.5-3 hr Infliltration: 0.5-1 hr IVRA: 0.5-1 hr PNB: 1-3 r Epi: 1-2 hr Spinal: 0.5-1 hr ```
43
contraindications with Lidocaine
``` hypersensitivity Adam Stoke WPW severe SA, AV or IV Heart Block corn-derived dextrose- corn allergy ``` pregnancy category B
44
Adverse Reactions with Lidocaine
CV collapse, bradycardia, arterial spasm, arrhythmia, increased d-fib threshold, edema, flushing, SA node depression Pronlonged PR and QRS CNS: Anxiety, dizziness, circumoral numbness, metallic rest, lethargy restlessness, seizure, tinnitus, HA, hyper-hypo-esthesia GI: N/V Hepatic- hepatic disease increases concentration- decreasing metabolism
45
use of lidocaine for spinal?
declined d/t Transient Neurologic Symptoms
46
what is lidocaine used most often for?
IVRA
47
how does lidocaine IV assist during DL?
attenuate increases in IOP,ICP, IAB
48
Mepivacaine trade names
Carbocaine | Polocaine
49
uses of mepivacaine
Infiltration PNB Epidural Spinal
50
how is Mepivacaine supplied
1% (10mg/mL) 2% (20mg/mL) Genergic 3% (30mg/mL)
51
Infiltration dose of mepivacaine :
0.5-1% 5 mg/kg
52
PNM: dose of mepivacaine
1-1.5% 5 mg/kg
53
Epi: dose of mepivacaine
1.5-2% 5 mg/kg
54
Spinal: dose of mepivacaine
2-4% 1.5 mg/kg
55
% protein binding of mepivacaine and what does that mean?
``` 78% DURATION Intermediate Lidocaine is 65% Bupivicaine is 94% ```
56
1/2 life of mepivacaine
1 hour
57
metabolism of mepivacaine
AMIDE | Hepatic
58
onset of mepivacaine and what that mean?
``` FAST dose dependent 3-20 minutes pKa 7.6 FASTEST!! 7.7 for lido and etido close to physiologic pH- non-ionized portion greatest crosses lipid layer of neuron ```
59
Duration of each route of mepivacaine: and why Infiltration: PNM: 2-4 Epi Spinal
intermediate because 76% protein bound Infliltration: 1-4 hr PNM: 2-4 hr Epi 1-3 hr Spinal1-2 hr
60
how are locals excreted?
amides- renal
61
adverse runs with mepivacaine
CV collapse, bradycardia, arrhythmia, edema, flushing, CNS: Anxiety, dizziness, circumoral numbness, metallic rest, lethargy restlessness, seizure, tinnitus, Blurred vision, miosis GI: N/V, fecal incontinence Resp: RD, arrest, hypoventilation Hepatic- hepatic disease increases concentration- decreasing metabolism MS- intra-artricular infusion related chondrolysis
62
WHAT is unique about Mepivacaine?
it does NOT cause vasodilation! | do NOT add epinephrine to this drug!
63
``` max dose mepivacaine infiltration PNB EPI Spinal ```
``` MAX DOSE: Infliltration: 400 mg PNB: 400mg Epi: 400 mg Spinal 100mg ```
64
max dose of lidocaine
300 mg for ALL except spinal
65
max dose of lidocaine with EPINEPHRINE
500 mg with Infiltration, PNB, Epidural
66
which forms is epinephrine NOT added with
Topical IVRA Spinal
67
contraindications of mepivacaine
Pregnancy Category C | hypersensitivity to AMIDES
68
trade name of Prilocaine
citanest
69
principal clinical uses of Prilocaine
``` Infiltration PNB Epidural IRVA Topical** most common ```
70
how is Prilocaine supplied
1% 2% 3% 4%
71
what is EMLA cream made of
prilocaine/lidocaine
72
dose of prilocaine Infiltration
0.5-1% 8mg/kg
73
dose of prilocaine PNB
1.5-2% 8mg/kg
74
dose of prilocaine Epidural
2-3% 8mg/kg
75
dose of prilocaine IRVA
0.25-0.5%
76
what is unique about prilocaine?
it dose not ventilate like mepivacaine DO NOT GIVE EPI WITH
77
``` Max dose of prilocaine for all routes: Infiltration PNB Epidural IRVA ```
600mg
78
% binding of prilocaine and what does that mean
55% | intermediate duration
79
metabolism of prilocaine
Most rapid metabolism of all amide Las Metabolism it forms orthotoluidine → methmoglobinemia hepatic BUT ALSO RENAL* only amide
80
onset of prilocaine and why
FAST with all routes
81
``` Duration of lidocaine and why Infiltration PNB Epidural IRVA ```
``` Intermediate b/c 55% protein bound Infiltration: 1-2 hr PNB: 1.5-3 hr Epi: 1-3 hr IVRA: 0.5-1hr ```
82
what is the biggest RXN risk with prilocaine
LEAST risk of LA toxicity with this one!! Useful for IVRA But.. then the risk of methmoglobinemia - limits its use
83
treatment of methmoglobinemia
Methylene blue 1-2 mg/kg IV over 5 min max 8mg/kg
84
Adverse effects of prilocaine
Methmaglobinemia Brady, CV arrest, depression, shock, edema, hpotension CNS: confusion, seizure, drowsiness, LOC, oral parethssia, blurred vsion, tinnitus, RD
85
contraindications of prilocaine
Pregnancy Cat B Minimal vasodilation- GOOD if you can not add epi to lidocaine
86
Etidocaine trade name
Duranest
87
clinical uses of etidocaine
Infiltration PNB Epidural
88
how is etidocaine supplied?
0.5% 1% 1.5%
89
Dose of Etidocaine Infiltration
0.5% max 300 mg
90
dose of Etidocaine PNB
0.5-1% max 300mg
91
dose of Etidocaine Epidural
1-1.5% max 300 mg
92
Max of etidocaine with all routes WITH EPINEPHRINE
400mg
93
protein binding of etidocaine and what does that mean
94% | long duratoin
94
1/2 life
156 minutes
95
metabolism of etidocaine
AMIDE | HEPATIC
96
excretion of etidocaine
97
onset of etidocaine and WHY
SLOW
98
duration of etidocaine and WHY
240-480 minutes 4-8 hours because highly protein bound
99
Clinical uses of cocaine
topical anesthesia | vasoconstriction of mucous membrane
100
how is cocaine supplied
4% | 10%
101
dose of cocaine
topical- max 3 mg/kg 200 mg TOTAL use 4% or 10% solution to anesthetize area being used
102
1/2 life of cocaine
75 minutes
103
metabolism of cocaine
Hepatic Plasma cholinesterases Major metabolies ecgoninemthyl ester and benzoyl ecgonine
104
peak of cocaine
Peak 15-40 minutes nasal
105
onset of cocaine
FAST 1 min
106
duration of cocaine
Topical: > 30 min Dose dependent
107
adverse reactions with cocaine
CV- intense vasoconstriction at ALL doses HTN, tachy, dysrhythmias, CA vasospasm, MI, ischemia, VF, increased MVO2 CNS: seizures, CVA , chronic abuse causes dopamine depletion The block of pre-synaptic reuptake of NE and Dop cause the ‘Hgih
108
contraindications of cocaine
Pregnancy gat C enters breast milk- congenital malformations, breast milk- irritabile MI NO with MAOIs of CAD pts expensive
109
trade name of chloroprocaine
nesacaine | nesacaine-MPF (methylparaben-free)
110
clinical uses of of chloroprocaine
Infiltration PNB Epidural Spinal
111
how is chlorocaine supplied?
nesacaine 1% or 2% generic 2% or 3%
112
dose of chloroprocaine Infiltration
1% | 10 mg/kg
113
PNBdose of chloroprocaine
2 % | 10mg/kg
114
Epidural dose of chloroprocaine
2-3 % | 10mg/kg
115
Spinal dose of chloroprocaine
2-3% ** | PRESERVATIVE FREE
116
max dose of chloroprocaine with Infiltration, PNB, Epidural without epinephrine
800 mg | same for all 3
117
max dose of chloroprocaine with spinal
1000 mg | * never add epi spinal
118
max dose of chloroprocaine with Infiltration, PNB, Epidural WITH epinephrine
1000 mg
119
% protein bound of chloroprocaine and what does that mean?
95% | long lasting
120
1/2 life of chloroprocaine
0.1 hr
121
onset of chloroprocaine
RAPID… WHY!? because HIGH concentrations 3%!! even though pKa is 9.1 gradient allows it to be more to rapidly act
122
duration for chloroprocaine
0.5-1 % | all routes
123
what is most unique about chloroprocaine?
SAFEST OF ALL LOCALS! least CNS CV toxicity of all LAs
124
adverse reactions of chloroprocaine
Brady, arrest, hypotension, VF CNS tox- seizures- very rare, dizziness, anxiety, restlessness, tinnitus, LOS, blurred vision Edema, erythema, pruritus, urticarial Chondrolysis RD Allergy
125
contraindications of chloroprocaine
Pregnancy category C Immune anti-inflammatory PRESERVATIVE FREE PREPARATIONS FOR NEUROAXIAL BLOCK
126
Tetracaine trade names
``` Ametop Pontocaine Tetcaine Altacaine TetraVisc ```
127
Clinical uses of tetracaine
Topical- optho | Spinal
128
dose of tetracaine topical and %
2% topical | 0.2mg/kg
129
dose of tetracaine spinal
use 0.5%- mg/kg?
130
max dose of tetracaine
same for both | 20mg
131
protein binding of tetracaine and what does that mean
76% | intermediate duration
132
metabolism of tetracaine
Hydrolysis by PLASMA CHOLINESTERASE All amides Slower than procaine To aminobenzoic acid
133
onset of tetracaine
fast 5 min both routes
134
duration of topical tetracaine
0.5-1 hr
135
duration of spinal tetracaine
2-6 hours
136
contraindications with esters
Hypersenvsitive to ESTER LA Caution w/decreased plasma cholinesterase levels- Dibucain #
137
Adverse Reactions tetracaine
CV: arrest, hypotension PULM: arrest, bronchospasm, dyspnea CNS: seizure, disy, drowsy, LOC tinnitus, blurred vision, miosis GI: N/V Heme/Onc: Methmoglobinemia Itching/anaphylaxis
138
what about tetracaine and PNB and IVRA
limited d/t toxicity with larger doses
139
trade name of procaine
procaine
140
spinal dose of procaine
10% | 15 mg/kg
141
max spinal dose of procaine
1000 mg
142
how is procaine supplied
10% for spinals
143
what is procaine NOT recommended for
topical, Epidural, PNB, IVRA
144
protein binding of procaine
6% | rapid off NOT long duration
145
duration spinal procaine
0.5-1 hr
146
onset of procaine
slow
147
metabolism of procaine
Hydrolysis by cholinesterase primarily in the plasma and to a lesser extent in the liver Intermediate RATE Hydrolyzed to PABA (paraaminobenzoic acid)
148
run with procaine
Allergy to PABA (paraaminobenzoic acid)
149
Intralipid brand name
Intralipid | Liposyn
150
how is intralipid supplied
20% 100mL most common 250, 500, 1000 mL
151
MOA intralipid
1) exogenous lipids provide an alternative source of binding of local anesthetics- LIPID SINK- High lipid partition coeff and large Vd- bupivacaine, L-bupicacaine, Ropivacaine 2) Reversal of mitochondrial fatty acid transport inhibition LA inhibit an enzyme used in mitochondrial fatty acit metabolism and transpot- b/c fatty acids are involved in 80-90% of ATP synthesis leading to CV toxicity. Lipid infusion increase the intracellularfatty acid content enough to overcome the inhibition of these enzymes by LA
152
dosing of intralipid
Bolus: 1.5 mg/kg q5min x3 70kg- 100mL 100 kg pt-150 mL Infusion 0.25 mL/kg/min 70 kg- 1000mL/hr 100kg – 1500mL/hr 2nd Infusion: 0.5 mL/kg/hr 70kg- 2000mL/hr 100kg 3000mL/hr
153
1/2 life of intralipid
0.5-1 hr
154
metabolism of intralipid
Fatty acids, phospholipids and glycerol are metabolized by cells to ATP, CO2 and water
155
excretion of intralipid
Biliary excretion of phospholipids
156
adverse rxn
CV instability Pancreatitis Hypoproteinemia Septicemia, fever, Allergic xn Neuro symptoms of LA tox BUT CV collapse may be the first symptom
157
composition of intralipid
100mL most common 20% = 20g Soybean Oil, 1.2g Lecithin 2.2g glycerol NaOH & 100mL
158
contraindications with intralipid
Do not give with severe EGG allegy