Locals Chart Flashcards
trade names of bupivicaine
Marcaine Marcaine Preservative-Free Marchaine Spinal Sensorcaine Sensorcaine-MPF Sensorcaine- MPF Spinal
how is bupivicaine supplied
Racemic mixture @
- 25% = 2.5mg/mL
- 5% = 5mg/mL
- 75% = 7.5mg/mL
what is bupivicaine used for?
Subcutaneous
PNB
Epidural
Spinal
Subq dose of bupivicaine and form
0.25%
dose 2.5 mg/kg
PNB dose of bupivicaine and form
PNB 0.25-0.5%
dose 2.5 mg/kg
Epidural dose of bupivicaine and form
Epi: 0.5-0.75%
dose 2mg/kg
Spinal dose of bupivicaine and form
Spinal: 0.5-0.75%
dose 0.3 mg/kg
max dose of bupivicaine SUBQ AND PNB SAME!!
175mg
max dose of bupivicaine SUBQ AND PNB SAME WITH EPINEPHRINE
225mg
what is the MAX DOSE of Bupivicaine Epidural
170mg
**5 mg less than Subq and PNB
what is the MAX DOSE of Bupivicaine Epidural WITH EPINEPHRINE
225 mg
** this is the SAME as Subq and PNB with epinephrine
MAX DOSE WITH BUPIVICAINE
0.3 mg/kg
NO EPINEPHRINE WITH SPINALS
what is the toxic plasma concentration of bupivicaine
> 3mcg/mL
Protein binding of bupivicaine?
and what does this mean?
96%
LONG duration of action hours
*depends on dose and location for exact time
metabolism of bupivicaine
HEPATIC- ALL AMIDES
SLOWEST METABOLISM OF ALL LOCALS
w/etidocain and ropivicain
BER – toxicity risk
Amide Hydrolysis and conjugation
Aromatic hydrozylation
N-dealkylation
half life of bupivicaine
3.5 hours
what is the relationship of sensory vs. motor block with bupiviciane
sensory block often OUTLASTS motor
sensory- at site
motor 2 below
sympathetic- upto 6 above
duration of action of bupivicaine- why Subcutaneous PNB Epidural Spinal
LONG- because highly protein bound Subq: 2-8 hours PNB: 4-12 hr Epi: 2-5 hr Spinal: 1-6 hr
Adverse Reactions with Bupivicaine
what MUST you know about this drug?
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
pKa of bupivicaine and what does this mean?
8.1
*same as ropivicaine
intermediate onset
contraindications with bupivicaine
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
lipid solubility =
potency
protein binding =
duration of action
follow VERY far by lipid solubility
how does adding sodium bicarbonate to LAs affect them?
alkalinizing LAs
increases the lipophilic portion of Las
more potent- moves into cells faster
the longer the carbon backbone of LAs…
the creating the LIPID SOLUBILITY
PROTEIN BINDIN
POTENCY
DURATION OF ACTION
how does adding Epi (1:200,00) affect bupivicaine?
decreases blood levels by 10-20%
what conditions increase LAs toxicity
metabolic & respiritory ACIDOSIS
decreased SZ threshhold
decreased protein binding
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
trade name of Lidocaine
Xylocaine
Xylocaine-MPF
many topical names
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%
what is lidocaine used for?
Topical Infiltration IVRA- Beir Block- tourniquet PNB Epidural Spinal
dose of topical lidocaine AND form %
Topical – 4%, 4 mg/kg
dose of infiltration lidocaine AND form %
Infliltration: 0.5-1% 4mg/kg
dose of IVRA lidocaine
AND form %
IVRA: 0.25-0.5%, 4 mg/kg
PNB dose of lidociane AND form %
PNM: 1-1.5% 4 mg/kg
epidural dose of lidocaine and form %
Epi 1.5-2% 4 mg/kg
spinal dose of lidocaine AND form %
Spinal: 1.5-5% 1.5 mg/kg
protein binding of lidocaine and WHAT does that mean?
70%
intermediate duration
protein binding most determines duration of action
metabolism of lidocaine
Hepatic
HEPATIC- ALL AMIDES
Dealkylation → mono-ethylglycin-exylidide 80% activity of lidocaine as an anti-arrhythmic
To
Hydrolysis → xylidide 10%
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
1/2 life lidocaine
96 min
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
contraindications with Lidocaine
hypersensitivity Adam Stoke WPW severe SA, AV or IV Heart Block corn-derived dextrose- corn allergy
pregnancy category B
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
use of lidocaine for spinal?
declined
d/t
Transient Neurologic Symptoms
what is lidocaine used most often for?
IVRA
how does lidocaine IV assist during DL?
attenuate increases in IOP,ICP, IAB
Mepivacaine trade names
Carbocaine
Polocaine
uses of mepivacaine
Infiltration
PNB
Epidural
Spinal
how is Mepivacaine supplied
1% (10mg/mL)
2% (20mg/mL)
Genergic 3% (30mg/mL)
Infiltration dose of mepivacaine :
0.5-1% 5 mg/kg
PNM: dose of mepivacaine
1-1.5% 5 mg/kg
Epi: dose of mepivacaine
1.5-2% 5 mg/kg
Spinal: dose of mepivacaine
2-4% 1.5 mg/kg
% protein binding of mepivacaine and what does that mean?
78% DURATION Intermediate Lidocaine is 65% Bupivicaine is 94%
1/2 life of mepivacaine
1 hour
metabolism of mepivacaine
AMIDE
Hepatic
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
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
how are locals excreted?
amides- renal
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
WHAT is unique about Mepivacaine?
it does NOT cause vasodilation!
do NOT add epinephrine to this drug!
max dose mepivacaine infiltration PNB EPI Spinal
MAX DOSE: Infliltration: 400 mg PNB: 400mg Epi: 400 mg Spinal 100mg
max dose of lidocaine
300 mg for ALL except spinal
max dose of lidocaine with EPINEPHRINE
500 mg with Infiltration, PNB, Epidural
which forms is epinephrine NOT added with
Topical
IVRA
Spinal
contraindications of mepivacaine
Pregnancy Category C
hypersensitivity to AMIDES
trade name of Prilocaine
citanest
principal clinical uses of Prilocaine
Infiltration PNB Epidural IRVA Topical** most common
how is Prilocaine supplied
1%
2%
3%
4%
what is EMLA cream made of
prilocaine/lidocaine
dose of prilocaine Infiltration
0.5-1% 8mg/kg
dose of prilocaine PNB
1.5-2% 8mg/kg
dose of prilocaine Epidural
2-3% 8mg/kg
dose of prilocaine IRVA
0.25-0.5%
what is unique about prilocaine?
it dose not ventilate
like mepivacaine
DO NOT GIVE EPI WITH
Max dose of prilocaine for all routes: Infiltration PNB Epidural IRVA
600mg
% binding of prilocaine and what does that mean
55%
intermediate duration
metabolism of prilocaine
Most rapid metabolism of all amide Las
Metabolism it forms orthotoluidine
→ methmoglobinemia
hepatic BUT ALSO RENAL* only amide
onset of prilocaine and why
FAST with all routes
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
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
treatment of methmoglobinemia
Methylene blue 1-2 mg/kg IV over 5 min max 8mg/kg
Adverse effects of prilocaine
Methmaglobinemia
Brady, CV arrest, depression, shock, edema, hpotension
CNS: confusion, seizure, drowsiness, LOC, oral parethssia, blurred vsion, tinnitus, RD
contraindications of prilocaine
Pregnancy Cat B
Minimal vasodilation- GOOD if you can not add epi to lidocaine
Etidocaine trade name
Duranest
clinical uses of etidocaine
Infiltration
PNB
Epidural
how is etidocaine supplied?
0.5%
1%
1.5%
Dose of Etidocaine Infiltration
0.5% max 300 mg
dose of Etidocaine PNB
0.5-1% max 300mg
dose of Etidocaine Epidural
1-1.5% max 300 mg
Max of etidocaine with all routes WITH EPINEPHRINE
400mg
protein binding of etidocaine and what does that mean
94%
long duratoin
1/2 life
156 minutes
metabolism of etidocaine
AMIDE
HEPATIC
excretion of etidocaine
onset of etidocaine and WHY
SLOW
duration of etidocaine and WHY
240-480 minutes
4-8 hours
because highly protein bound
Clinical uses of cocaine
topical anesthesia
vasoconstriction of mucous membrane
how is cocaine supplied
4%
10%
dose of cocaine
topical- max 3 mg/kg
200 mg TOTAL
use 4% or 10% solution to anesthetize area being used
1/2 life of cocaine
75 minutes
metabolism of cocaine
Hepatic
Plasma cholinesterases
Major metabolies ecgoninemthyl ester and benzoyl ecgonine
peak of cocaine
Peak 15-40 minutes nasal
onset of cocaine
FAST
1 min
duration of cocaine
Topical: > 30 min
Dose dependent
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
contraindications of cocaine
Pregnancy gat C enters breast milk- congenital malformations, breast milk- irritabile
MI
NO with MAOIs of CAD pts
expensive
trade name of chloroprocaine
nesacaine
nesacaine-MPF (methylparaben-free)
clinical uses of of chloroprocaine
Infiltration
PNB
Epidural
Spinal
how is chlorocaine supplied?
nesacaine 1% or 2%
generic 2% or 3%
dose of chloroprocaine Infiltration
1%
10 mg/kg
PNBdose of chloroprocaine
2 %
10mg/kg
Epidural dose of chloroprocaine
2-3 %
10mg/kg
Spinal dose of chloroprocaine
2-3% **
PRESERVATIVE FREE
max dose of chloroprocaine with Infiltration, PNB, Epidural without epinephrine
800 mg
same for all 3
max dose of chloroprocaine with spinal
1000 mg
* never add epi spinal
max dose of chloroprocaine with Infiltration, PNB, Epidural WITH epinephrine
1000 mg
% protein bound of chloroprocaine and what does that mean?
95%
long lasting
1/2 life of chloroprocaine
0.1 hr
onset of chloroprocaine
RAPID… WHY!?
because HIGH concentrations 3%!!
even though pKa is 9.1 gradient allows it to be more to rapidly act
duration for chloroprocaine
0.5-1 %
all routes
what is most unique about chloroprocaine?
SAFEST OF ALL LOCALS!
least CNS
CV toxicity of all LAs
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
contraindications of chloroprocaine
Pregnancy category C
Immune anti-inflammatory
PRESERVATIVE FREE PREPARATIONS FOR NEUROAXIAL BLOCK
Tetracaine trade names
Ametop Pontocaine Tetcaine Altacaine TetraVisc
Clinical uses of tetracaine
Topical- optho
Spinal
dose of tetracaine topical and %
2% topical
0.2mg/kg
dose of tetracaine spinal
use 0.5%- mg/kg?
max dose of tetracaine
same for both
20mg
protein binding of tetracaine and what does that mean
76%
intermediate duration
metabolism of tetracaine
Hydrolysis by PLASMA CHOLINESTERASE
All amides
Slower than procaine
To aminobenzoic acid
onset of tetracaine
fast 5 min both routes
duration of topical tetracaine
0.5-1 hr
duration of spinal tetracaine
2-6 hours
contraindications with esters
Hypersenvsitive to ESTER LA
Caution w/decreased plasma cholinesterase levels- Dibucain #
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
what about tetracaine and PNB and IVRA
limited d/t toxicity with larger doses
trade name of procaine
procaine
spinal dose of procaine
10%
15 mg/kg
max spinal dose of procaine
1000 mg
how is procaine supplied
10% for spinals
what is procaine NOT recommended for
topical, Epidural, PNB, IVRA
protein binding of procaine
6%
rapid off NOT long duration
duration spinal procaine
0.5-1 hr
onset of procaine
slow
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)
run with procaine
Allergy to PABA (paraaminobenzoic acid)
Intralipid brand name
Intralipid
Liposyn
how is intralipid supplied
20%
100mL most common
250, 500, 1000 mL
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
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
1/2 life of intralipid
0.5-1 hr
metabolism of intralipid
Fatty acids, phospholipids and glycerol are metabolized by cells to ATP, CO2 and water
excretion of intralipid
Biliary excretion of phospholipids
adverse rxn
CV instability
Pancreatitis
Hypoproteinemia
Septicemia, fever, Allergic xn
Neuro symptoms of LA tox BUT
CV collapse may be the first symptom
composition of intralipid
100mL most common
20% = 20g Soybean Oil, 1.2g Lecithin
2.2g glycerol
NaOH & 100mL
contraindications with intralipid
Do not give with severe EGG allegy
