Local Anesthetic Pharm (EB) Flashcards
Local anesthetic amides (5)
lidocaine Bupivacaine Ropivacaine Mepivacaine Prilocaine
Local anesthetic esters (4)
cocaine Procaine Tetracaine Amethocaine
Myelin layer of B nerve fibers? Function? Order of block? Effect?
Myelin layer = light Function = autonomic, preganglionic, sympathetic Order of block = 1 Effect = warmth (vasodilation)
Myelin layer of C nerve fibers? Function? Order of block? Effect? ?
Myelin layer = none Function = pain Order of block =2 Effect = loss of pain sensation
Myelin layer of Adelta nerve fibers? Function? Order of block? Effect? ?
Myelin layer = light Function = pain, temp Order of block = 2 Effect = loss of pain and temp sensation
Myelin layer of Agamma nerve fibers? Function? Order of block? Effect? ?
Myelin layer = moderate Function = muscle tone Order of block = 3 Effect = loss of proprioception
Myelin layer of Abeta nerve fibers? Function? Order of block? Effect? ?
Myelin layer = moderate Function = touch, pressure Order of block = 4 Effect = loss?
Myelin layer of Aalpha nerve fibers? Function? Order of block? Effect? ?
Myelin layer = heavy Function = motor Order of block = 5 Effect = paralysis
How does frequency of stimulation influence the onset of blockade?
traumatized tissue more sensitive to local anes blockade
Order of regional local anes blocking?
proximal regions are blocked sooner than distal regions
Which kind of fibers are blocked first (conventionally)
small sensory fibers are blocked before larger sensory and motor fibers
potency of a local anes is closely correlated to
lipid solubility
What are nerve membranes made out of to help with the potency of local anes?
lipids
What influences the speed of onset of a local anes?
pKa
PKa of local anes
weak bases = 7.6 - 9.1
At tissue pH of 7.4, < 50% of local anesthetics are
nonionized
What form of local anesthetics diffuses across the cell membrane
non-ionized
pH _ in infected tissues?
decreases
Because pH decreases in infected tissues, what happens to the non-ionized fraction of local anes? What happens to the action of localed anes?
reduced non-ionized fraction. Reduced or absent local anes action
Protein binding and duration of action of bupivacaine?
95% protein bound, Long duration
Protein binding and duration of action of lidocaine
65% protein bound, Short duration
Effect of action of local anes on vessels? What effect does this have on the drug?
vasodilation»_space; fastens uptake of drug, shortens duration of effect
Additives to a local anesthetic (3)
vasoconstrictors (epinephrine) Hyaluronidase Bicarbonate
Why is epinephrine added to a local anesthetic?
delayed absorption, prolonged action
Con of adding epinephrine to a local anesthetic?
localized ischemia possible
Why is hyaluronidase added to a local anesthetic?
increasing tissue permeability Facilitates diffusion Rapid onset
Why is bicarbonate added to a local anesthetic?
buffers G+ Faster diffusion Shortens onset and duration Injection less painful
What metabolized local anes esters into inactive compounds?
plasma cholinesterases
NB to a long IV infusion of amide local anes?
slowly metabolized by the liver so can accumulate after long IV infusion
Pros of loco-regional use of local anesthetics (3)
easy to use Effective and reliable analgesia Minimal systemic effects
CV effects of loco-regional use of local anesthetic
decreased CV responses to surgical stimulation
Effect of loco-regional use of a local anesthetic on the MAC
decreases
How are local anesthestics systemically given?
lidocaine CRI
How can lidocaine reduce hyperalgesia?
central analgesic effect when given CRI
Effect of lidocaine CRI on MAC
MAC sparing effect
Effect of lidocaine CRI on GI tract in horses?
prokinetic activity
CV effect of lidocaine CRI
anti-arrythmic properties
Effect of lidocaine CRI on inflammation
anti-oxidant and inflammatory modulator activity
CNS effects of local anes
initial CNS tox»_space; Sedation, disorientation, ataxia Muscle tremor, convulsions, respiratory depression
CV effects of local anesthestics
CV toxicity» Depress myocardial contractility Profound hypotension Arrhythmias CV collapse
What local anesthetics cause methamglobinemia?
prilocaine Benzocaine
Why should you not give 5% lidocaine
causes an irreversible block within minutes
Problems of high concentrations of local anesthetics?
tissue irritation Neurotoxicity
Problem with given epinephrine
tissue ischemia
Problem with given ester local anesthetics
allergic rxns
How do you avoid toxicity with local anesthetics (4)
know the toxic doses Weigh the pt calculate dose avoid unintentional IV inj
The toxicity of local anesthetics is _
additive
How do you tx seizures causes by local anes
benzos Propofol CRI
How do you tx CNS depression caused by local anes
supportive care Mechanical ventilation
How do you tx cardiac problems caused by local anes
supportive care Fluids O1 Atropine Antiarrythmic
How does lipid rescue work to tx local anes systemic tox?
remove lipophilic toxins from affected tissue Surrounds local anesthetic molecules in plasma
Onset of lidocaine
rapid (5 min)
duration of lidocaine
short (1-2 hrs)
uses of lidocaine
nerve block Epidural/spinal Infiltration CRI(IV)
What cardiac thing can lidocaine be used to tx?
ventricular tachycardia Arrhythmias
What animal is more sensitive to the toxic effects of lidocaine?
cats
What is the side effect of using lidocaine as a spray in order to ET tube a car?
laryngeal edema (due to additives)
duration and onset of mepivicaine?
rapid onset (5 minutes), Short duration (1-2 hrs)
routes of administration of mepivicaine
SC Local infiltraton Intra-articular
Why is mepivicaine preferred for equine nerve blocks?
less irritant than lidocaine
What major use does mepivicaine have over lidocaine?
can be used for intra-synovial analgesia
Onset of bupivacaine
slow (20-30 minutes)
Duration of bupivacaine
long duration (4-6 hours)
What drug has a higher cardiotoxicity than lidocaine?
bupivacaine
Uses of bupivacaine
nerve block Epidural/spinal
Which isomer of bupivacaine is less tocic?
L-bupivacaine
What drug damages articular cartilage?
bupivacaine
What entantiomer of ropivacaine is available?
S
Is ropivicaine more or less soluble than ropivacaine?
less
What LA: has a faster return to motor function? Why?
ropivacaine Less impact on muscle fibers
What is EMLA cream?
eutectic mixture of local anesthetics 2.5% lidocaine and 2.5% prilocaine
What is the main use of EMLA cream?
skin anesthesia prior to IV catheter
Onset of action of EMLA cream?
20-30 minutes
Why use opioids with a local anesthetic?
increase efficacy and extend duration of block
What blocks is morphine used in?
intra-articular and epidural blocks
Which a2 agonists may extend the duration and increase efficacy of local blocks?
medetomidine Dexmedetomidine
Why is ketamine use with LA?
epidural anesthesia