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121 Cards in this Set
- Front
- Back
What does protein binding have to do with LA?
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the more the protein binding, the longer the duration of action.
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What property of a drug is influenced by pKa?
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onset of action
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What is the Max safe dose for Lido?
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7 mg/kg
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What is the max safe dose for procaine (novocaine)?
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14 mg/kg
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The max safe dose for chloroprocaine?
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20 mg/kg
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What is the max safe dose for tetracaine?
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1 mg/kg
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What is the max safe dose for mepivicaine?
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7 mg/kg
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What is the max safe dose for etidocaine?
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3 mg/kg
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The max safe dose for bupivicaine?
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3 mg/kg
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The max safe dose for ropivicaine?
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3 mg/kg
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the max safe dose for cocaine?
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200 mg topical
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The following are all ester LA EXCEPT:
A. Cocaine B. tetracaine C. lidocaine D. Procaine |
C
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The following are all amide LA EXCEPT:
A. etidocaine B. bupivicaine C. Lidocaine D. Chloroprocaine |
D
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The efficacy of the LA are all the same. T or F?
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True
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Which has less potential for toxicity:
A. esters B. amides |
A
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Although allergy to any LA is very rare, which of the 2 classes have more incidence of allergic reactions?
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esters
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If a pt is allergic to Lidocaine, it is OK to give them bupivicaine. T or F?
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False-all amides are out, but can receive esters
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Name the 3 basic parts of a LA molecule
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1. lipophilic part
2. linkage ( ester or amide) 3. hydrophilic part |
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2 Chemical classes of LA are?
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esters
amides |
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Esters are metabolized by:
A. cytochrome P 450 enzymes in the liver B. hydrolyzed by cholinesterase |
B
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Why are esters short acting?
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metabolized by cholinesterase, so they dont need to go to liver
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Amides are metabolized how?
A. CYP450 enzymes in the liver B. cholinesterase in plasma |
A
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Why do we add bicarb to LA?
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increasing the pH of the solution increases the % of the solution taht is non-ionized, (nonionized crosses into nerve) and speeds the onset.
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What effect does hypoxia have on LAs?
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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.
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Tissue acidosis does what to lipid solubility?
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decreases it
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Which of the LAs is the most cardiotoxic? Why?
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Bupivicaine-it preferentially binds to cardiac proteins.
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The first sign of bupivicaine overdose is what?
A. circumoral numbness B. tinnitus C. seizures D. arrest |
D
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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 |
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Mixing 2 LAs together has what effect on toxicity levels?
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The toxicities are additive
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What effect does pregnancy have on LA spread and depth?
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greater in preg. Reduce dosages
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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
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what is the relationship between ropivicaine and levobupivicaine?
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Both are isomer forms of bupivicaine. They were developed to decrease the cardiotoxic effects of bupivicaine.
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The closer the pKa is to 7.4, the _______(more or less) lipid soluble?
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more
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The higher the % of protein binding, the ____________(longer or shorter) the duration of action?
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longer
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LAs are CNS depressants-why do they cause seizures at toxic levels?
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disinhibition ( like stage 2 of anesthesia)
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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 |
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Why does LA toxicity tend to be self-limiting?
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quickly redistributes
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BZDs raise the seizure threshhold for LAs-what does this mean?
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It will take more LA to cause seizures
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Name 2 ways NE is broken down in body
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1. MAO ( in cytoplasm)
2. COMT (in synapse) |
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What kind of receptor is at the ganglion in the SNS?
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nicotinic
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What kind of receptor is at the ganglion in the PSNS?
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nicotinic
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what kind of receptor is at the effector organ in the SNS?
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adrenergic
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What kind of receptor is at the end organ in the PSNS?
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muscarinic
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What is the difference between presynaptic and postsynaptic alpha 2 agonists?
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presynaptic A2 agonists stimulate the A2 receptor, that effectively decreases NE , so it has a sympatholytic effect
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Which of the folllowing are (presynaptic) alpha 2 agonists?
A. clonidine B. isoproteronol C. dexmetedomidine D. dobutamine |
A, C
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Where are beta 1 receptors located int eh body?
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the heart only
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Where are beta 2 receptors located?
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Any place but heart
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Interference with the synthesis of NE will have (sympatholytic or sympathomimetic) effect
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sympatholytic
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Blockade of NE reuptake would have an
1. symphatholytic 2. sympathomimetic effect? |
sympathomimetic
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Three drugs that have blockade of NE reuptake?
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cocaine
imipramine amitriptyline |
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inhibition of vesicular storage of NE has
(sympathomimetic/sympatholytic) effect? |
sympatholytic
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How do indirect acting agents work?
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they do not go to receptor, but they cause bodies own NE to be released from vesicles
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2 examples of indirect acting agents we use?
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1. ketamine
2. ephedrine |
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How do direct acting agents exert their effects?
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They go directly to receptor and elicit resposne
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Examples of direct acting agents?
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levophed
phenylephrine isuprel |
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Which of the followng are examples of indirectly acting adrenergic agents?
A. phenylephrine B. isoproteronol C. ketamine D. ephedrine |
C, D
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How do agents that produce receptor blockade work?
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they block the postsynaptic receptor so NE cant attach to it
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Which of the following are examples of adrenergic receptor blockade?
A. phentolamine B. neostigmine C. edrophonium D. propranolol |
A, D
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Sympathetic effects in the heart include:
A. decreased SVR B. increased HR C. + inotropic activity |
B, C
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Sympathetic effects in GI system include:
A. increased tone and motility B. contraction of sphincters C. less secretions |
B, C
(" sympathetic stim=scared shitless.....) |
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True or false: vasculature is controlled mainly by the PSNS?
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False- controlled by SNS via A1 and B2 receptors
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If a drug blocks the enzyme tyrosine hydroxylase, how does this affect the synthesis of catecholamines?
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It reduces the production of them
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Which of the following enzymes are involved int eh metabolism of catecholamines?
A. tyrosine hydroxylase B. COMT C. MAO D. paraglycine |
B, C
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Interference with synthesis of a neurotransmitter would have which effect?
A. sympatholytic B. sympathomimetic |
A
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Name an example of a drug that illustrates mechanism 2: metabolized by same pathway as the transmitters precursor. Is this sympatholytic or sympathomimetic?
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methyldopa; sympatholytic
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Name an example of a drug that illustrates mechanism 3: blocks transport system at nerve terminal membrane. Is this sympatholytic or sympathomimetic?
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Cocaine or imipramine; sympathomimetic
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Name an example of a drug that illustrates mechanism 4: blocks transport to storage vesicle. Is this sympatholytic or sympathomimetic?
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reserpine; sympatholytic
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Name an example of a drug that works by mechanism 5: promotion of exocytosis. Is this sympathomimetic or sympatholytic?
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amphetamines ephedrine, sympathomimetic
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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
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Presynaptic alpha blockers have what effect?
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sympatholytic
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postynaptic alpha blockers have what effect?
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sympathomimetic
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Name an example of a drug that works by mechanism 7: directly acting agents. Are they sympatholytic or sympathomimetic?
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levophed, Neo, isuprel, sympathomimetic
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Name an example of a drug that works by mechanism 8: receptor blockade, Is this sympathomimetic or sympatholytic?
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inderal, regitine; sympatholytic
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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?
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This is a trick question: Neostigmine and edrophonium; parasympathomimetic
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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
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alpha agonist effect on eyes?
alpha blocker effect on eyes? |
mydriasis (dilation)
miosis (constriction) |
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Cholinergic agonist effect on eyes?
anticholinergic effect on eyes? |
miosis (pinpoint pupils, decreased IOP)
mydriasis and cycloplegia, ^IOP |
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which class of drug is contraindicated in asthmatics? Why?
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Beta blockers-d/t bronchcocontriction
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Alpha agonist effect on blood vessels?
Alpha blocker effect? |
vasoconstriction
vasodilation |
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Lungs: which receptors?
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Beta2
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heart: which receptors?
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Beta 1
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uterus: which receptor?
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beta 2
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"glands": sweat, salivary
which receptor? |
Alpha 1
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Alpha agonist effect on heart?
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reflex bradycardia ( Neo)
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Alpha blocker effect on heart?
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reflex tachycardia
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anticholinergic effect on heart?
cholinergic agonist effect on heart? |
tachycrdia ( atropine)
bradycardia |
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Beta agonists have what effect on uterus?
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relaxation (terbutaline)
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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 |
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activation of dopaminergic receptors has what effect?
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dilation of renal arteries
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activation of B1 receptors by dopamine has what effect?
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increase HR
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activation of alpha receptors by dopamine has what effect ?
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vasoconstriction
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List the following receptors sensitivity to dopamine in increasing order. (which receptor is most sensitive to dopamine?)
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1. dopamine
2. Beta 3. alpha this is why you need the highest dose for pressors, but lower dose for renal effects. |
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Ephedrine is:
A. centrally acting B. Peripherally acting C. directly acting D. indirectly acting |
all are correct
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Why is the fact that ephedrine centrl, peripherl, direct and indirect important?
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you get 4 mechanisms with one drug
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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?
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ephedrine-no reflex bradycardia
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Which part of the LA blocks the nerve: ionized or nonionized?
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ionized blocks the nerve, nonionized gets it into the nerve-Thanks Jason!
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What property of a drug is influenced by pKa?
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onset
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2 biggest reasons to add epi to LA?
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1. less toxicity with epi because it absorbed more slowly
2. lasts longer |
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Max safe dose of lido and mepivicaine are the same. What is it?
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7 mg/kg
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etidocaine, bupivicaine and ropivicaine are all the same safe max dose. what is it?
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3 mg/kg
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Why does neostigmine increase risk of PONV?
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increases peristalsis (PSNS: rest and digest)
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Why should you use caution when giving beta blockers to a diabetic?
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beta blockers create hypoglycemia, but they also block one of the first signs of hypoglycemia-tachycardia
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which class of drugs cause mydriasis and cycloplegia?
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anticholinergics
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which class of drugs cause mydriasis?
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alpha agonists
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What is the major difference between atropine and robinul?
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Robinul is quartenary amine-cant cross BBB, so no CNS effects
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which is better for a pregnant mom: atropine or robinul? Why?
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robinul-can't cross placental barrier
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Atropine or Robinul: which has sedative effect?
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atropine: can cross BBB, so can have CNS effects
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Which causes mydriasis and cycloplegia: atropine or robinul?
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atropine: can cause CNS effects
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Which is better antisialagogue: atropine or robinul?
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robinul
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Which demonstrates more increase in heart rate: atropine or robinul?
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atropine
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Which gives more smooth muscle relaxation: atropine or robinul?
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equal
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Which is better at preventing motion induced nausea: atropine or robinul?
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atropine.
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Mnemonic for atropine poisoning:
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Red as abeet, blind as a bat, dry as a bone, mad as a hatter, hot as a hare
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What does analeptic mean?
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CNS stimulant effect
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What does neuroleptic mean?
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CNS blocking effects
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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
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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
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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
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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
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stimulation of presynaptic alpha 2 receptors causes what?
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inhibition of NE release
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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?
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B1 agonist. Dumbass shouldn't have left your drink!
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