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77 Cards in this Set
- Front
- Back
Local Anesthetics Mode of Action:
Block generation of action potential by reversibly inhibiting ____ influx |
Na+
Preferentially block activated Na+ channels |
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Locals are weak bases (pKa=8-9)
(mainly ionized at physiologic pH and act). Why are they bases? |
they penetrate the cell membrane in the non-ionized form
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what kind of nerves have high sensitivity to locals?
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Thin, non-myelinated nerve fibers (sensory roots) Pain, touch, temperature
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what kind of nerves have medium sensitivity to locals?
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Thin --> medium, myelinated nerve fibers (sympathetic nerves) : vasomotor, visceromotor function
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what kind of nerves have low sensitivity to locals?
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Thick, myelinated nerve fibers (somatic nervous system): motor function
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What is the Order (timing) of nerve function block of the following:
touch, cold, motor, warmth, pain, cold, deep pressure |
1. pain
2. cold 3. warmth 4. touch 5. deep pressure 6. motor Recovery in reverse order |
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How do you know an amide from an ester by only knowing the drug name ? (without looking at the structure)
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Amides all have 2 “I”s in them. Esters have one.
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Which amide drug blocks only motor?
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Etidocaine only blocks motor.
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Esters are broken down in the blood by___________
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plasma esterases
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Amides are metabolized by the______ and excreted by the kidney
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liver
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pKa correlates with what property of local anesthetic
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speed of onset
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Adding WHAT makes local anesthetic less ionized and it crosses the membrane faster! Faster action.
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bicarb
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Example of a condition that lowers pH and may have a negative impact on the onset and the quality of the local anesthesia.
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tissue acidosis produced by infection
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Lipid solubility correlates with what characteristic of the local anesthetic
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potency
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Plasma protein binding correlates with their affinity for protein with sodium channels and predicts what about a local anesthetic
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the duration they will sustain neural blockade
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The big thing. What are Signs and symptoms of Bupivicaine toxicity ?
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metallic taste in mouth. Then seizures, coma, and cardiac arrest.
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Local anesthetics depress the CNS in a ____-dependent manner
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dose
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Low serum concentrations are used clinically for suppressing cardiac dysrhythmias, but higher concentrations induce________ activity.
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seizure
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WHAT are the principal life-threatening consequence of local anesthetic overdose?
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Convulsive seizures
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Max dose of lidocaine
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4.5 mg/kg without Epi,
7 mg/kg with Epi |
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Max dose of bupivicaine
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3 mg/kg with or w/o epi
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0.25% bupiv = ___mg/cc
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2.5mg/cc
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1% xylocaine = __mg/cc
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10mg/cc
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How many milligrams of bupiv can you give a 60 kg pt?
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60kg * 3mg/kg = 180mg
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How many ccs of .5% bupiv can you give a 60 kg pt?
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180mg / 5mg/cc = 36 cc
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Preservative _____ is used with ester compounds and may cause allergic reaction.
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PABA
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Most adverse reactions to locals are caused by_______.
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toxicity
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Tachycardia and palpitations may be from________ in some solutions of local anesthetic
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epinephrine
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Less than _% of all adverse reactions due to locals are caused by allergic mechanisms.
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1
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The ester local anesthetics produce a metabolite related to ____
____ can cause allergic reactions in some patients. Amides and some esters have a preservative (methylparaben) that resembles ____ and can cause allergic reactions. |
para-aminobenzoic acid (PABA).
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Mechanism of cocaine
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reversibly binds to and inactivates sodium channels. This inhibits excitation of nerve endings. Cocaine blocks the reuptake of dopamine, serotonin, and NE.
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How long does lidocaine last?
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30-60 min
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How long does bupivicaine last?
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120-240 min
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Cocaine is metabolized by hydrolysis by _______
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plasma pseudocholinesterases.
Also oxidative metabolism in the liver And 5% excreted unchanged |
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toxic dose of cocaine
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2-3 mg/kg
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Treatment of Cocaine Toxicity
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ABCs
Cooling blankets No known antidote What drugs may be useful? Propanolol Nitrates Calcium-channel blockers Benzodiazepines |
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short-acting ester
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chloroprocaine (Used in epidurals and spinals)
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(long-acting) ester
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Tetracaine
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2 other long acting amides
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Ropivacaine (long-acting)
Levobupivacaine (long-acting) |
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Toxic dosage of lidocaine
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4.5 mg/kg
With epi 7 mg/kg |
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Transient neurologic symptoms
of lidocaine |
Like cauda equina syndrome
Syndrome of pain and/or dysesthesia Appear 12-24 hours after surgery Most often resolves in 3-7 days Pain can be severe (even worse than surgery) |
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Most commonly used local used for epidurals. OK for spinals
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Bupivacaine
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caution with bupivicaine
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Highly cardiac toxic
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the concentration of the vapour in the lungs that is needed to prevent movement (motor response) in 50% of subjects in response to surgical (pain) stimulus
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MAC
Minimum alveolar concentration (should be "median") |
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If MAC is 1.0, then ___ MAC would block response in 95% of subjects.
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If MAC is 1.0, then 1.3 MAC would block response in 95% of subjects.
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MAC of halothane
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0.76
(the lower the more potent) |
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Hair color that increases MAC
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Red
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1L of O2 and 1L of N2O does what to MAC?
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That is 50% N2O, therefore MAC is 50% less
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Halothane (MAC = 0.74).... what is MAC w/ 60% N20?
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0.74 - 60%(0.74) = 0.29
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N2O can increase air spaces in the body. Give examples
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Pneumothorax
VAE Bowel distension Tympanic membrane pressure |
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what could the abbreviation MAC be mistaken for?
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monitored anesthesia care
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What is the blood-gas partition coefficient? Why do we care?
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An ideal anaesthetic would act extremely quickly (be highly insoluble in blood: have a low blood gas partition coefficient), BGPC is proportional to a gas's solubility
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Example of drug with low blood-gas partition coefficient and works quickly
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desflurane
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3 most important Factors Affecting the Speed of Action of Inhaled Anesthetics
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Alveolar anesthetic partial pressure
Anesthetic solubility Cardiac output (Decreased cardiac output accelerates the rate of increase of FA/FI; Fi = inspired fraction) |
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What is the significance of halothane having the largest degree of metabolism?
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halothane is liver toxic.
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What Drugs trigger MH and are Not Safe?
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Desflurane
Halothane Isoflurane Sevoflurane Xenon (Rarely Used) Succinylcholine |
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How would you diagnose malignant hyperthermia susceptible pt?
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Caffeine Halothane Contracture Test is the gold standard,
Molecular Genetic Testing for Malignant Hyperthermia (RYR1 mutation) |
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Pseudocholinesterase deficiency is an inherited enzyme abnormality that results in abnormally slow metabolic degradation of exogenous choline ester drugs such as ____________.
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succinylcholine
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This condition is recognized most often when respiratory paralysis unexpectedly persists for a prolonged period of time following administration of standard doses of succinylcholine
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Pseudocholinesterase Deficiency
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Pseudocholinesterase Deficiency is Confirmed by a laboratory assay demonstrating decreased plasma cholinesterase enzyme activity -->________ number
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Dibucaine
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milk of amnesia. It burns. Give with lido. Short acting for induction. No analgesia. Hypotensive
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Propofol
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used for intubation. Sedative. Less resp depression than propofol. Causes adrenal suppression (*). Cardiovascularly stable
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Etomidate
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hallucinogenic. Used with kids. Cariovascularly stable. Causes release of NE. If stressed pt, can cause cardiac instability b/c no more NE
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Ketamine
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can’t give in porphyria.
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Barbiturates
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alpha 2 agonist (like clonidine)
No respiratory depression New |
Dexmedetomidine
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IV Agents for sedation
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Propofol
Etomidate Ketamine Barbiturates Dexmedetomidine |
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histamine release, N/V, longer acting than fentanyl
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Morphine
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Muscle relaxant:
increases heart rate, (similar to atropine) |
Pancuronium
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Muscle relaxant:
histamine releasing |
Atracurium
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Muscle relaxant:
less histamine release |
Cis-atracurium
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If pt is hypotensive, don't use what sedative?
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propofol and thiopental
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Pt is coming in for bowel resection due to obstruction secondary to large mass. Don't give what gas?
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N2O b/c it increases bowel gas volume
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Low BP --> would avoid propofol and thiopental – could consider_____
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etomidate or ketamine
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Pt is anxious -->_________ might be warranted
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benzodiazepine
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we will need something for pain allergic to morphine -->________
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fentanyl
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Family hx of “reaction to anesthesia” --> could be MH or _____________________ deficiency --> avoid volatile agents and succinylcholine
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Family hx of “reaction to anesthesia” --> could be MH or pseudocholinesterase deficiency --> avoid volatile agents and succinylcholine
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anesthetic plan for pt with extensive past medical history and numerous meds (from packet)
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have the surgeon use local anesthesia.
We could use a little fentanyl maybe. Must titrate in slowly. |