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Local Anesthesia can be accomplished by what substances? |
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Definition
Amines, alcohols, and toxins |
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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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Definition
structure, speed of onset, doa, potency, protein binding, solubility |
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cocaine is found in the leaves of what shrub in andes mts in south america? |
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Einhorn prepared the first synthetic La called? |
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Name the first amide anesthetic? |
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Lidocaine was synthesized by? |
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Definition
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Definition
LAs produce a reversible, dose dependent blockade of sodium ion influx into nerve cytoplasm |
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these surround, support, and insulate axon |
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layer of delicate collagen tissue around axon embedding it in the fascicle |
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Definition
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Over-lapping group of cells binding fascicles |
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Definition
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layers of connective tissue around fascicles |
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Definition
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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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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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LAs are ______ in aqueous solution |
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Definition
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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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preservative that is added to MDV, some are paraben derivatives( potent allergen) |
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Definition
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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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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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lipid solubility is assosciated with? |
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Definition
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dissociation constant is associated with? |
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Definition
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protein binding is associated with? |
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Definition
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Frequency dependent block is associated with? |
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Definition
sensorimotor discriminations |
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vasodilation potential is assosciated with? |
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Definition
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tissue penetration is assosciated with |
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Definition
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what form is primarily responsible for blocking sodium influx |
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Definition
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lipophilic end consists of a? |
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Definition
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hydorphillic end consists of a ? |
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Definition
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Definition
weak bases, packaged in salts for stability and water solubility |
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Definition
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Definition
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when u increase molecular weight |
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Definition
u enhance potency and DOA |
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Definition
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the hydrophillic end is an |
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Definition
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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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the site of action for LAs are |
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Definition
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this may be a factor in some toxicity issues |
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Definition
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if highly protein bound how does this affect the placenta |
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Definition
less crossing unwanted membranes |
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whats the most supported theory of how LAs work |
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Definition
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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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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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Definition
somatic motor, proprioception |
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autonomic preganglionic, myelinated |
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pain, reflex response, autonomic postganglionic, unmyelinated |
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where do LAs work in type C fibers |
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Definition
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where do LAs work in type A delta |
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Definition
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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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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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differing vasodilation properties can play a role in |
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Definition
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the greater the lipid solubility, the more? |
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Definition
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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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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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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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