Chapter 4: Exam 1 Flashcards

1
Q

what are the 3 main components to the structure of anesthetics

A

aromatic ring, intermediate chain, and terminal amine

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2
Q

an aromatic ring contains ___________ properties, has ____________ which allows the anesthetic to penetrate the nerve membrane, and determines the _______________ of the drug

A

lipophilic
lipid solubility
potency/concentration

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3
Q

an intermediate chain is either an _________ or ___________. it distinguishes the type of ___________ and determines the site of ______________

A

ester or amide
anesthetic
biotransformation

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3
Q

the terminal amine has _____________ properties, has water solubility that ensures the drug will not precipitate on exposure to ____________, and allows the agent to disperse in the ________ and ___________ fluids

A

hydrophilic
interstitial fluid
intracellular and extracellular

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4
Q

in natural form, local anesthetics are weak ________ meaning their poorly soluble in water

A

bases

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5
Q

in cartridges, LA solution is acidified to form stable __________

A

salts

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6
Q

to be stable in solution, the ph of anesthetic must favor water soluble _________ at the time of injection

A

cations

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7
Q

this is uncharged or neutral and penetrates nerve membranes

A

base

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8
Q

this has a positive charge, bind to the receptor site, and effects the duration of the anesthetic

A

cation

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9
Q

primarily effects diffusion, onset times, and success

A

ionization

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10
Q

after injection into the tissue, the equilibrium shifts from cationic to ___________ due to pH of normal tissue

A

neutral base

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11
Q

for the anesthetic to pass through the membrane, RNH+ converts to _____

A

RN

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12
Q

depleted RN in the _________ causes the equilibrium to produce more RN

A

extracellular fluid

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13
Q

once anesthetic is exposed to the axoplasm, the equilibrium shift to favor ________

A

RNH+

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14
Q

__________ ions are available in the axoplasm

A

hydrogen

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15
Q

blocked channel = no __________ = no impulse

A

sodium

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16
Q

during the resting stage, __________ ions are bound to receptor sites within the ion channels of cell membranes

A

calcium (Ca++)

17
Q

during slow depolarization, local anesthetics compete with _______ to bind to the ion channels and to close off these channels

A

Ca++

18
Q

during depolarization, __________ are displaced, which is thought to be the most significant factor responsible for the influx of _________ into the nerve

A

Ca++
sodium

19
Q

percentages of RNH+ and RN are manipulated by the ________

A

pH

20
Q

local anesthetic solution has more __________ than _________

A

RNH+
RN

21
Q

what are the benefits to pH in local anesthetics

A

great stability
increased solubility
ease of sterilization

22
Q

increasing the pH of a solution/surrounding tissues with increase __________ molecule concentrations

A

neutral base

23
Q

lowering ph will favor ________ concentrations

A

cation

24
Q

pKa is a ________________ constant

A

dissociation

25
Q

pKa is a measurement of a molecules affinity for _________ ions

A

H+

26
Q

if pKa = pH then base concentration = ____________ concentration

A

cation

27
Q

what is phase I of cns action of LA

A

cns excitation

27
Q

how is pKa determined

A

henderson hasselbalch equation

28
Q

what is phase II of cns action of LA

A

cns depression

29
Q

what are the two possible pathways of biotransformation

A

liver or blood

30
Q

the process where LA drugs are broken down to less toxic or nontoxic metabolites before being excreted

A

biotransformation

31
Q

biotransformation follows the pathway of the liver = _________________ system (slow)

A

p450 isoenzyme

32
Q

plasma cholinesterase breaks down ______________ and ____________

A

esters and articaine

32
Q

biotransformation follows pathway of blood = plasma _______________-

A

cholinesterase

33
Q

plasma cholinesterase is made by the ____________ but distributed throughout the body

A

liver

34
Q

biotransformation of amides is primarily performed by _____________ enzymes

A

liver hepatic

35
Q

what is the exception to biotransformation of amides

A

articaine

36
Q

biotransformation of esters happens in the blood by ________________

A

plasma cholinesterase

37
Q

esters break down into _______________ acid which is thought to be the source of their antigenic tendencies

A

paraamino benzoic

38
Q

what is the only injectable ester anesthetic

A

procaine

39
Q

elimination of local anesthetics is performed by the ___________

A

kidneys