Term
| Local Anesthesia can be accomplished by what substances? |
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Definition
| Amines, alcohols, and toxins |
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Term
| T or F? LA's are capable of producing reversible blockade of conduction of nerve impulses |
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Definition
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Term
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Definition
| structure, speed of onset, doa, potency, protein binding, solubility |
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Term
| cocaine is found in the leaves of what shrub in andes mts in south america? |
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Definition
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Term
| Einhorn prepared the first synthetic La called? |
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Definition
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Term
| Name the first amide anesthetic? |
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Definition
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Term
| Lidocaine was synthesized by? |
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Definition
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Term
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Definition
| LAs produce a reversible, dose dependent blockade of sodium ion influx into nerve cytoplasm |
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Definition
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Term
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Definition
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Term
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Definition
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Term
| these surround, support, and insulate axon |
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Definition
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Term
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Definition
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Term
| layer of delicate collagen tissue around axon embedding it in the fascicle |
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Definition
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Term
| Over-lapping group of cells binding fascicles |
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Definition
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Term
| layers of connective tissue around fascicles |
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Definition
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Term
| This is a liquid substance containing proteins and lipids, forms insulating layer around some nerves. Prevents current from leaking out of nerve |
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Definition
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Term
| small, unmyelinated segments between schwann cells. Intense APs jump from node to node in saltatory conduction |
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Definition
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Term
| LAs are ______ in aqueous solution |
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Definition
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Term
| actual drug(LAs) are poorly soluble in h2o and produced as |
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Definition
| hydrochloride salts that are acidic and more stable |
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Term
| Epi breaks down in what solution? |
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Definition
| Alkaline, this is important when preparing LAs with epi, if no acidic solution, epi would break down |
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Term
| this preservative is added to LAs with epi making the pH 4, to further stabalize it |
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Definition
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Term
| preservative that is added to MDV, some are paraben derivatives( potent allergen) |
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Definition
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Term
| these can be cytotoxic and should not be added to LAs to be used in spinals or epidurals or iv regional |
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Definition
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Term
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Definition
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Term
| how do liposomes affect LAs? |
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Definition
slow release of LA to diffusion and prolonged duration( 48-96 hr)
can be used for chronic pain management |
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Term
| available bupivicaine liposome |
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Definition
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Term
| minimum effective dose is used to? |
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Definition
| mimimize LA toxicity, use of lowest effective concentration, and lowest effective volume |
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Term
| higher concentrations of LAs can? |
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Definition
| increase potential for nerve damage |
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Term
| concentration effect of LAs? |
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Definition
| higher concentrations will speed onset and intensity |
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Term
| differential sensitivity of LAs |
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Definition
| effects on diff nerve functions |
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Term
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Definition
| Hydrophillic,lipophillic portion, ester or amide link |
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Term
| LAs are present in equilibrium as |
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Definition
| ionized (cationic) salt and unionized base |
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Term
| chemical linkage is associated with? |
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Definition
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Term
| lipid solubility is assosciated with? |
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Definition
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Term
| dissociation constant is associated with? |
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Definition
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Term
| protein binding is associated with? |
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Definition
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Term
| Frequency dependent block is associated with? |
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Definition
| sensorimotor discriminations |
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Term
| vasodilation potential is assosciated with? |
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Definition
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Term
| tissue penetration is assosciated with |
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Definition
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Term
| what form is primarily responsible for blocking sodium influx |
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Definition
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Term
| lipophilic end consists of a? |
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Definition
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Term
| hydorphillic end consists of a ? |
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Definition
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Term
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Definition
| weak bases, packaged in salts for stability and water solubility |
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Term
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Definition
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Term
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Definition
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Term
| when u increase molecular weight |
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Definition
| u enhance potency and DOA |
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Term
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Definition
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Term
| the hydrophillic end is an |
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Definition
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Term
| What is more cardiac toxic L bupivicaine or the racemic bupivicaine? |
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Definition
| bupivicaine, these two are enantiomers |
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Term
| This is a pure S isomer and is less cardiotoxic as well |
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Definition
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Term
| the site of action for LAs are |
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Definition
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Term
| this may be a factor in some toxicity issues |
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Definition
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Term
| if highly protein bound how does this affect the placenta |
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Definition
| less crossing unwanted membranes |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
| whats the most supported theory of how LAs work |
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Definition
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Term
| LAs block voltage sodium channel and reduce influx of na ions thereby: 3things |
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Definition
| preventing outflow of K, prevent depol., and block AP |
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Term
| Do LAs change membrane potential or threshold |
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Definition
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Term
| Blockade is dependant on? |
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Definition
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Term
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Definition
| disruption of several contiguous channels to overcome nerve conduction |
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Term
| LAs block voltage sodium channel and reduce influx of na ions thereby: 3things |
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Definition
| preventing outflow of K, prevent depol., and block AP |
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Term
| Do LAs change membrane potential or threshold |
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Definition
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Term
| Blockade is dependant on? |
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Definition
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Term
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Definition
| disruption of several contiguous channels to overcome nerve conduction |
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Term
| Na channels can be in one of 3 states |
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Definition
activated open
inactivated closed
rested closed |
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Term
| LAs gain access to receptors in which state |
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Definition
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Term
| LAs bind to the channel in what state |
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Definition
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Term
| other potential site of action for LAs |
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Definition
| K and CA channel, g protein, may explain cardiac effects |
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Term
| rapid or slow firing nerves are blocked first? |
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Definition
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Term
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Definition
| alpha beta gamma and delta, its myelinated |
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Term
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Definition
| somatic motor, proprioception |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| autonomic preganglionic, myelinated |
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Term
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Definition
| pain, reflex response, autonomic postganglionic, unmyelinated |
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Term
| where do LAs work in type C fibers |
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Definition
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Term
| where do LAs work in type A delta |
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Definition
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Term
| when nodes of ranvier are exposed to LA in high concentration, how many nodes need to be blocked to prevent transmission of the impulse? |
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Definition
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Term
| why do we see diff blocks? |
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Definition
nerve function affects sensitivity
fiber diameter and myelination determine conduction velocity
fibers may have some differences in resistance to block |
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Term
| whats the order of blockade of nerve fibers |
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Definition
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Term
| What we see, order of block? |
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Definition
Autonomic
sensory
motor
proprioception (all students must pass) |
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Term
| LAs cause vasodilation except for |
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Definition
|
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Term
| differing vasodilation properties can play a role in |
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Definition
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Term
| the greater the lipid solubility, the more? |
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Definition
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Term
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Definition
| how much of drug is ionized, and influences speed of onset |
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Term
| closer to physiologic PH means it is |
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Definition
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Term
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Definition
| minimum blocking concentration |
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Term
| is tachyphylaxis seen when dosing intervals are short enough to prevent pain |
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Definition
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Term
| do long intervals resulting in pt pain cause tachyphylaxis? |
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Definition
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Term
| the MOA is unknown, thought to be central spinal acting mechanism, what topic is this regarding? |
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Definition
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Term
| absorption and distribution is only a factor with what type of LAs |
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Definition
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Term
| Plasma concentration is determined by |
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Definition
| rate of tissue distribution and rate of drug clearance and tissue absorption |
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Term
| absorption and distribution are more critical in determining |
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Definition
| the rate of offset of anesthesia |
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Term
| Absorption is affected by what 3 factors |
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Definition
site of injection
drug tissue binding
presence or absence of vasoconstrictors |
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Term
| injection into a highly vascular area results in |
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Definition
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Term
| Absorption is modified by what 3 factors |
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Definition
site of injection
drug tissue binding
presence or absence of vasoconstrictors |
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Term
| injection into a highly vascular area results in |
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Definition
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Term
| Factors that affect absorption include |
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Definition
tissue blood flow
lipid solubility of agent
pt age and cv status |
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Term
| maximum blood levels for regional occur in what order |
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Definition
| intercostal, caudal, epidural, brachial plexus |
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Term
| these reduce systemic absorption of LA from site |
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Definition
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Term
| In spinal anesthesia epi acts directly on the cord, acting on alpha receptors which inhibit release of what |
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Definition
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Term
| epi prolongs effect of LA by what percent |
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Definition
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Term
| alpha 2 agonist that can be added to produce analgesia in its own right |
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Definition
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Term
| Vasoconstrictors are less effective in |
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Definition
| highly lipid soluble long acting drugs b/c they are highly tissue bound |
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Term
| this linkage is widely distributed after IV administration, sequestration in fat, after initial rapid distribution phase( highly perfused organs) and slower distribution phase (muscle and gut) |
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Definition
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Term
| this structure has short plasma half lives |
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Definition
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Term
| these are hydrolyzed rapidly by plasma cholinesterase, resulting in very short plasma half lives |
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Definition
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Term
| this is hydrolyzed by hepatic microsomal enzymes cp450 |
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Definition
Amides
more LA toxicity in patients with impaired liver func |
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Term
| In normal liver function it can take how long to metabolize lidocaine |
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Definition
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Term
| in liver failure it can take how long to metabolize lidocaine |
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Definition
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Term
| this can extract some amide LA from circulation limiting amt sent to systemic circulation |
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Definition
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Term
| other drugs competing for cp450 can |
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Definition
|
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Term
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Definition
| hepatic clearance primarily |
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Term
| what can decrease hepatic clearance |
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Definition
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Term
| which amide is metabolized fast? |
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Definition
|
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Term
| which amide is metabolized intermediate |
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Definition
|
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Term
| which amide is metabolized slow |
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Definition
etidocaine
bupivicaine
ropivicaine |
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