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What are the main types of local anesthetics?
lipophilic group connected to hydrophilic groups via ester or amide bond
What are some properties of esters?
shorter duration and increased systemic toxicity
Local anesthetics are weak ____ that are predominately ______ at physiologic pH
bases, predominately ionized
Local anesthetics need to be ________ to cross membrane and once inside become ______ and bind to _______
need to be non-ionized
ionized and bind Na+ channel
What is the MOA of local anesthetics?
block Na+ w/ high affinity (more effective in rapidly firing axons) and inhibit neuronal firing
Duration of action of local anesthetics is dependent on?
time at site of action (exert effect then rapidly diffuse away)
Extent of block due to local anesthetics is dependent on?
voltage and time dependent (increases excitation threshold and slows impulse conduction)
What affects absorption?
dosage
site of inj (vascular vs fat)
drug tissue bidning
chemical properties
local blood flow
epinephrine (vasoconstricting agents)
How are amides metabolized/excreted?
liver metabolism from CYP450
toxicity more likely w/ hepatic dz or reduced hepatic BF
excreted via renal
How are esters metabolized/excretion?
butyrylcholinesterase in plasma
excreted via renal
What are local AE of local anesthetics?
tissue damage (rare)
neurotox and myotox
What are systemic AE of local anesthetics?
relative tox closely follows anesthetic potency
methemoglobinemia (benzocaine in cats/rabbits)
What are CNS AE effects of local anesthetics?
skeletal muscle twitches and tonic-clonic seizures firs signs of toxicity
What are CV AE of local anesthetics?
toxicity usually occurs at higher plasma concentrations than CNS tox
prolongation of PR and QRS intervals (due to slowed impulse control)
hypotension
decreased myocardial strength
What are some indications of lidocaine?
labeled infiltrations/nerve block/epidural
moderate topical activity (minimal local irritation)
correction of V fib and tachycardia (dogs)
prokinetic (horses)
What are AE of lidocaine?
profound cardio-depression
greater CNS
esp. cats
What local anesthetics are amides?
lidocaine, bupivacaine, mepivacaine, ropivacaine
What are indications of bupivacaine?
spinal anessthesia, infiltration blocks, epidural
analgesia post-op
cranial cruciate lig sx (liposome formulation)
What are some pharmacodynamics of bupivacaine?
longer duration of action than lidocaine (binds more resting cardiac Na, dissociates from channel slower)
more potent sensory block than motor
What are AE of bupivacaine?
cardiotoxicity
What are some indications of mepivacaine?
epidural and ventriculoectomy sx
some limb blocks (less post-inj. edema)
more potent/toxic than lidocaine
What are some indications of ropivacaine?
epidural, infiltration blocks, local blocks
slower onset and longer duration than lidocaine
What local anesthetics are esters?
benzocaine, proparacaine, tetracaine
What are some indications of benzocaine?
fish anesthesia/euthanasia
lipid soluble, topically absorbed
What are some indications of proparacaine?
topical use in ophthalmologic dx procedures
fast onset and short duration
2-3 repeat dosings can increase duration
What are some indications of tetracaine?
ophthalmological procedures needing deeper plane/longer duration than proparacaine
slow onset action, long duration
What are some AE of tetracaine?
burning/itching, chemosis (delayed)
as analgesic - diffuse epithelial keratitis that progresses to iritis, descemetitis, diffuse stormal edema
suppresses blink reflex (need eye lube, risks corneal opacification and keratitis)
What is the order of physiologic function loss in euthanasia to prevent fear/disress?
rapid loss of consciousness
loss of motor function
arrest of resp and cardiac function
permanent brain function loss
What is an acceptable method of euthanasia?
consistently produce humane death when used solely for euthanasia
What is an acceptable method with conditions of euthanasia?
may require certain conditions to be consistently humane death
may have greater potential for operator error/safety hazards
not well documented
may require secondary method to ensure death
What are some factors to consider when selecting euthanasia procedure?
reliability
time required to induce consciousness loss
compatibility w/ pt, intended animal use, purpose
emotional effect
drug availability, abuse potential
legal requirements
What is the MOA for barbiturates?
depress CNs in descending order (cerebral cortex start)
w/ OD deep anesthesia progresses to apnea due to respiratory center depression and following cardiac arrest
Barbiturates should never be used with what animals?
entering food chain
What is proper disposal of animals that have been euthanized with barbiturates?
carcass cannot contaminate food chain
burial only if carcass cannot be scavenged
consider cremation of companion animals!
What is the MOA of dissociative agents and a2 adrenergic agonists for euthanasia?
rapid loss of consciousness/muscle relaxation pre-op
may be given prior to euthanasia agents to minimize distress/fear/facilitate restraint and provide more aesthetic environment for O
How does epinephrine affect local anesthetic absorption?
a1 agonist that causes vasoconstriction
decreases diffusion of drug and prolongs duration
decreases systemic absorption and risk of systemic toxicity