Local Anesthetics Flashcards
What are the two classes of local anesthetics?
Amides and esters
What is the mechanism of local anesthetics?
Bind to sodium channels and nerve membranes
Slows rate of depolarization
- threshold potential is not reached
- action potential not propagated
Are local anesthetics weak acids or weak bases?
Weak bases
Pka 7.7-9
During infection tissue becomes more acidic, how does this affect local anesthetics?
Will increase ionized portion—> more inactive (cannot pass through cell membrane)
If the pk of a local anesthetic is lower, how does this affect the onset of action
Lower pk => faster onset (closer to tissue pH)
High amounts of protein binding has what affect on duration of action of local anesthetics
Longer duration
Will water soluble or lipid soluble local anesthetics have higher potency?
Lipid soluble
What are the amide local anesthetics?
Lidocaine Bupivaciane Mepivaciane Prilocaine —> with lidocaine in EMLA cream
What is the ONLY local anesthetic that may be given Iv or used for intravenous regional anesthesia?
Lidocaine
What is the onset and duration of lidocaine?
Fast onset
Short duration (1-2hours)
What are the systemic effects of lidocaine?
Anti-arrhythmic Decrease MAC Analgesic Free radical scavenger Improves GI motility
What local anesthetic has the highest cardiovascular toxicity?
Bupivacaine
What is the onset and duration of bupivacaine?
Imtermediate onset
Duration: 3-8hours
What are the uses of mepivicaine?
Nerve block
Intra-articular
-common in large animal
What is the onset and duration of mepivaciaine?
Fast onset
Duration 1.5-3hours
What are the ester local anesthetics?
Procaine
Tetracaine and proparacaine (ophthalamic prep)
Benzocaine -laryngeal spray for intubation (not in cats!)
What site of administration will have the fastest systemic absorption of local anesthetics?
Intercostal blocks
How are esters metabolized?
Hydrolysis by plasma cholinesterase
One of the metabolizes, paraaminobenzoic acid (PABA) May amuse allergic reactions
How are amides metabolized?
Microsomal liver enzymes
-dependent on normal hepatic function
More likely to accumulate than esters