Regional Anesthetics Flashcards
What’s the difference between nociception and pain?
Pain = perception and awareness of noxious stimulus
Nociception = activation of nociceptors while unconscious
A nociceptive stimulus causes what 2 physiologic processes to occur?
- sympathetic stimulation - catecholamine release > incr HR/BP
- stress response - ACTH release > incr cortisol/BG
What are 3 reasons to provide regional anesthesia?
-
pre-emptive analgesia - abolish afferent nociception, reduction of anesthetic/analgesic drugs
- reduction of intraoperative complications
- better intra and postoperative pain control - faster return to normal activities
- prevents stress response - better immune system activity
What is an aminoester?
- hydrolyzed by cholinesterase enzyme
- causes anaphylactoid reactions
e.g. procaine, tetracaine, benzocaine, cocaine
What is an aminoamide?
- hepatic metabolism (microsomal enzymes)
- slow metabolism
- toxicity from accumulation is more likely
e.g. lidocaine, bupivacaine, ropivacaine, mepivacaine
Local anesthetics are essentially what two types of compounds linked together?
a lipophilic unit linked to a hydrophilic unit
What is the MOA of local anesthetics?
- Local anesthetic needs to penetrate into cell to produce its effects
- Blockade of Na+ channel
- Prevents Na+ influx > no depolarization > no impulse transmission
What are the lipid properties of local anesthetics?
- lipid solubility
- correlates w/ potency: more lipid soluble = more potent (ie. bupivicaine)
- facilitates penetration thru nn membranes
- promotes sequesteration into lipid-soluble compartments (ie. myelin) > slower onset + longer duration of action
What does pKa stand for and what properties does it instill for local anesthetics?
pKa = dissociation constant
- pH at which 50% of drug is present ionized (charged) and 50% is unionized (neutral)
- unionized = lipid soluble
- degree of ionization will depend on pKa and pH of tissue
- local anesthetics are weak bases > ionized in acidic pH
- local anesthetics are ion trapped in acidic environments
What happens with the local anesthetic effect for a drug like lidocaine with a pKa of 7.8 in infected tissue with a pH of 6.5?
Much more of the drug will be ionized when injected into the infected tissue, thus there will be fewer unionized liposoluble molecules available to have an anesthetic effect
What 5 things affect the effect of local anesthetics?
- pH/pKa
- proximity
- dose
- volume
- spread
What 6 things affect the onset of local anesthetics?
- lipophilicity
- pKa
- concentration
- dose + volume
- proximity to nerve
- type of nerve
What 5 things affect the duration of local anesthetics?
- vascular effect
- tissue blood flow
- vasoconstrictor
- dose
- affinity to the Na+ receptor
Smaller nerve fiber are ______ susceptible to local anesthetic b/c shorter length of axon is required to be blocked to halt the conduction completely
_______ fibers are more susceptible to be blocked b/c local anesthetic pools near the axonal membrane
more; myelinated
Nerve block onset occurs in what order?
- pain
- cold
- warm
- touch
- deep pressure (more evident in long acting LA)
- motor function
(Pain —–> motor function)