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121 Cards in this Set

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What does protein binding have to do with LA?
the more the protein binding, the longer the duration of action.
What property of a drug is influenced by pKa?
onset of action
What is the Max safe dose for Lido?
7 mg/kg
What is the max safe dose for procaine (novocaine)?
14 mg/kg
The max safe dose for chloroprocaine?
20 mg/kg
What is the max safe dose for tetracaine?
1 mg/kg
What is the max safe dose for mepivicaine?
7 mg/kg
What is the max safe dose for etidocaine?
3 mg/kg
The max safe dose for bupivicaine?
3 mg/kg
The max safe dose for ropivicaine?
3 mg/kg
the max safe dose for cocaine?
200 mg topical
The following are all ester LA EXCEPT:
A. Cocaine
B. tetracaine
C. lidocaine
D. Procaine
C
The following are all amide LA EXCEPT:
A. etidocaine
B. bupivicaine
C. Lidocaine
D. Chloroprocaine
D
The efficacy of the LA are all the same. T or F?
True
Which has less potential for toxicity:
A. esters
B. amides
A
Although allergy to any LA is very rare, which of the 2 classes have more incidence of allergic reactions?
esters
If a pt is allergic to Lidocaine, it is OK to give them bupivicaine. T or F?
False-all amides are out, but can receive esters
Name the 3 basic parts of a LA molecule
1. lipophilic part
2. linkage ( ester or amide)
3. hydrophilic part
2 Chemical classes of LA are?
esters
amides
Esters are metabolized by:

A. cytochrome P 450 enzymes in the liver
B. hydrolyzed by cholinesterase
B
Why are esters short acting?
metabolized by cholinesterase, so they dont need to go to liver
Amides are metabolized how?

A. CYP450 enzymes in the liver
B. cholinesterase in plasma
A
Why do we add bicarb to LA?
increasing the pH of the solution increases the % of the solution taht is non-ionized, (nonionized crosses into nerve) and speeds the onset.
What effect does hypoxia have on LAs?
acidosis causes % of ionization to increase, making the drug less lipid sol. So, if your LA is already inside the CNS, it cant get out-it gets trapped inside the nerve.
Tissue acidosis does what to lipid solubility?
decreases it
Which of the LAs is the most cardiotoxic? Why?
Bupivicaine-it preferentially binds to cardiac proteins.
The first sign of bupivicaine overdose is what?

A. circumoral numbness
B. tinnitus
C. seizures
D. arrest
D
In situations resulting in arrest from bupivicaine toxicity:

What are 2 special considerations that differ from other LAs?
1. more difficult to resuscitate

2. treat with intralipid solution
Mixing 2 LAs together has what effect on toxicity levels?
The toxicities are additive
What effect does pregnancy have on LA spread and depth?
greater in preg. Reduce dosages
Which of the following are unique properties of cocaine? (Choose all that apply)

A. manufactured
B. topical use only
C. parasympathomimetic
D. blocks reuptake of NE into sympathetic nerves
B, D
what is the relationship between ropivicaine and levobupivicaine?
Both are isomer forms of bupivicaine. They were developed to decrease the cardiotoxic effects of bupivicaine.
The closer the pKa is to 7.4, the _______(more or less) lipid soluble?
more
The higher the % of protein binding, the ____________(longer or shorter) the duration of action?
longer
LAs are CNS depressants-why do they cause seizures at toxic levels?
disinhibition ( like stage 2 of anesthesia)
List the following symptoms of LA toxicity in increasing order of appearance:

seizures, circumoral numbness/tingling, coma, unconsciousness, muscle twitches, visual disturbances,CVS depression, resp arrest
circumoral numbness/tingling
visual disturbances
muscular twitches
seizures
unconsciouness
coma
resp arrest
CVS depression
Why does LA toxicity tend to be self-limiting?
quickly redistributes
BZDs raise the seizure threshhold for LAs-what does this mean?
It will take more LA to cause seizures
Name 2 ways NE is broken down in body
1. MAO ( in cytoplasm)
2. COMT (in synapse)
What kind of receptor is at the ganglion in the SNS?
nicotinic
What kind of receptor is at the ganglion in the PSNS?
nicotinic
what kind of receptor is at the effector organ in the SNS?
adrenergic
What kind of receptor is at the end organ in the PSNS?
muscarinic
What is the difference between presynaptic and postsynaptic alpha 2 agonists?
presynaptic A2 agonists stimulate the A2 receptor, that effectively decreases NE , so it has a sympatholytic effect
Which of the folllowing are (presynaptic) alpha 2 agonists?
A. clonidine
B. isoproteronol
C. dexmetedomidine
D. dobutamine
A, C
Where are beta 1 receptors located int eh body?
the heart only
Where are beta 2 receptors located?
Any place but heart
Interference with the synthesis of NE will have (sympatholytic or sympathomimetic) effect
sympatholytic
Blockade of NE reuptake would have an
1. symphatholytic
2. sympathomimetic
effect?
sympathomimetic
Three drugs that have blockade of NE reuptake?
cocaine
imipramine
amitriptyline
inhibition of vesicular storage of NE has
(sympathomimetic/sympatholytic) effect?
sympatholytic
How do indirect acting agents work?
they do not go to receptor, but they cause bodies own NE to be released from vesicles
2 examples of indirect acting agents we use?
1. ketamine
2. ephedrine
How do direct acting agents exert their effects?
They go directly to receptor and elicit resposne
Examples of direct acting agents?
levophed
phenylephrine
isuprel
Which of the followng are examples of indirectly acting adrenergic agents?
A. phenylephrine
B. isoproteronol
C. ketamine
D. ephedrine
C, D
How do agents that produce receptor blockade work?
they block the postsynaptic receptor so NE cant attach to it
Which of the following are examples of adrenergic receptor blockade?
A. phentolamine
B. neostigmine
C. edrophonium
D. propranolol
A, D
Sympathetic effects in the heart include:
A. decreased SVR
B. increased HR
C. + inotropic activity
B, C
Sympathetic effects in GI system include:
A. increased tone and motility
B. contraction of sphincters
C. less secretions
B, C
(" sympathetic stim=scared shitless.....)
True or false: vasculature is controlled mainly by the PSNS?
False- controlled by SNS via A1 and B2 receptors
If a drug blocks the enzyme tyrosine hydroxylase, how does this affect the synthesis of catecholamines?
It reduces the production of them
Which of the following enzymes are involved int eh metabolism of catecholamines?
A. tyrosine hydroxylase
B. COMT
C. MAO
D. paraglycine
B, C
Interference with synthesis of a neurotransmitter would have which effect?
A. sympatholytic
B. sympathomimetic
A
Name an example of a drug that illustrates mechanism 2: metabolized by same pathway as the transmitters precursor. Is this sympatholytic or sympathomimetic?
methyldopa; sympatholytic
Name an example of a drug that illustrates mechanism 3: blocks transport system at nerve terminal membrane. Is this sympatholytic or sympathomimetic?
Cocaine or imipramine; sympathomimetic
Name an example of a drug that illustrates mechanism 4: blocks transport to storage vesicle. Is this sympatholytic or sympathomimetic?
reserpine; sympatholytic
Name an example of a drug that works by mechanism 5: promotion of exocytosis. Is this sympathomimetic or sympatholytic?
amphetamines ephedrine, sympathomimetic
Name an example of a drug(s) that works by mechanism 6:

preventing the release of the transmitter.

Is this sympathomimetic or sympatholytic?
clonidine, bretylium, guanadrel; sympatholytic
Presynaptic alpha blockers have what effect?
sympatholytic
postynaptic alpha blockers have what effect?
sympathomimetic
Name an example of a drug that works by mechanism 7: directly acting agents. Are they sympatholytic or sympathomimetic?
levophed, Neo, isuprel, sympathomimetic
Name an example of a drug that works by mechanism 8: receptor blockade, Is this sympathomimetic or sympatholytic?
inderal, regitine; sympatholytic
Name a drug taht works by mechanism 9: inhibiting the enzyme that breaks down the transmitter. Is this sympatholytic or sympathomimetic? Or is this a trick question?
This is a trick question: Neostigmine and edrophonium; parasympathomimetic
Name an example of a drug that works by mechanism 10 ( Nags own invention):

messing with the second messenger system inside the cell (by giving PDE inhibitors). Is this sympatholytic or sympathomimetic?
milrinone; sympathomimetic
alpha agonist effect on eyes?
alpha blocker effect on eyes?
mydriasis (dilation)
miosis (constriction)
Cholinergic agonist effect on eyes?

anticholinergic effect on eyes?
miosis (pinpoint pupils, decreased IOP)

mydriasis and cycloplegia, ^IOP
which class of drug is contraindicated in asthmatics? Why?
Beta blockers-d/t bronchcocontriction
Alpha agonist effect on blood vessels?
Alpha blocker effect?
vasoconstriction
vasodilation
Lungs: which receptors?
Beta2
heart: which receptors?
Beta 1
uterus: which receptor?
beta 2
"glands": sweat, salivary

which receptor?
Alpha 1
Alpha agonist effect on heart?
reflex bradycardia ( Neo)
Alpha blocker effect on heart?
reflex tachycardia
anticholinergic effect on heart?
cholinergic agonist effect on heart?
tachycrdia ( atropine)
bradycardia
Beta agonists have what effect on uterus?
relaxation (terbutaline)
Matching: Drug to receptor
pure alpha
pure beta
beta with some alpha,
alpha with some beta,
dopamine,beta, alpha
pure alpha: Neo
pure beta: dobut
beta with some alpha: epi
alpha with some beta: levo
dopa, beta, alpha: dopamine
activation of dopaminergic receptors has what effect?
dilation of renal arteries
activation of B1 receptors by dopamine has what effect?
increase HR
activation of alpha receptors by dopamine has what effect ?
vasoconstriction
List the following receptors sensitivity to dopamine in increasing order. (which receptor is most sensitive to dopamine?)
1. dopamine
2. Beta
3. alpha
this is why you need the highest dose for pressors, but lower dose for renal effects.
Ephedrine is:
A. centrally acting
B. Peripherally acting
C. directly acting
D. indirectly acting
all are correct
Why is the fact that ephedrine centrl, peripherl, direct and indirect important?
you get 4 mechanisms with one drug
You have a pt with HR of 58. that you have just placed a spinal. Their BP falls to 60/40. which drug will you give: ephedrine or neo? Why?
ephedrine-no reflex bradycardia
Which part of the LA blocks the nerve: ionized or nonionized?
ionized blocks the nerve, nonionized gets it into the nerve-Thanks Jason!
What property of a drug is influenced by pKa?
onset
2 biggest reasons to add epi to LA?
1. less toxicity with epi because it absorbed more slowly
2. lasts longer
Max safe dose of lido and mepivicaine are the same. What is it?
7 mg/kg
etidocaine, bupivicaine and ropivicaine are all the same safe max dose. what is it?
3 mg/kg
Why does neostigmine increase risk of PONV?
increases peristalsis (PSNS: rest and digest)
Why should you use caution when giving beta blockers to a diabetic?
beta blockers create hypoglycemia, but they also block one of the first signs of hypoglycemia-tachycardia
which class of drugs cause mydriasis and cycloplegia?
anticholinergics
which class of drugs cause mydriasis?
alpha agonists
What is the major difference between atropine and robinul?
Robinul is quartenary amine-cant cross BBB, so no CNS effects
which is better for a pregnant mom: atropine or robinul? Why?
robinul-can't cross placental barrier
Atropine or Robinul: which has sedative effect?
atropine: can cross BBB, so can have CNS effects
Which causes mydriasis and cycloplegia: atropine or robinul?
atropine: can cause CNS effects
Which is better antisialagogue: atropine or robinul?
robinul
Which demonstrates more increase in heart rate: atropine or robinul?
atropine
Which gives more smooth muscle relaxation: atropine or robinul?
equal
Which is better at preventing motion induced nausea: atropine or robinul?
atropine.
Mnemonic for atropine poisoning:
Red as abeet, blind as a bat, dry as a bone, mad as a hatter, hot as a hare
What does analeptic mean?
CNS stimulant effect
What does neuroleptic mean?
CNS blocking effects
Which of the following are effects of beta 1 stimulation?
A. decreased HR
B. increased contractility
C. increased automaticity
D. increased HR
B, C, D
Which of the following effects are seen with alpha 2 (postsynaptic) receptor stimulation?
A. hyperpolarization of CNS cells
B. platelet aggregation
C. increased automaticity
D. Increased contractility
A, B
Stimulation of Alpha 1 receptors gives which of the following?
A. vasoconstriction
B. mydriasis
C. relaxation of bladder sphincter
D. relaxation of GI sphincters
A, B. Actually causes contraction of both sets of sphinters
Stimulation of beta 2 receptors causes which of the following?
A. bronchoconstriction
B. uterine relaxation
C. lipolysis
D. gluconeogenesis
E. stress in SRNAs
B, C, D. causes broncodilation too
stimulation of presynaptic alpha 2 receptors causes what?
inhibition of NE release
Someone at a bar slips something into your drink. You exhibit the following symptoms: HA, dizziness, nervousness, sweating, constipation, ^BP, ^ HR, ^ contratility. What kind of drug did they give you?
B1 agonist. Dumbass shouldn't have left your drink!