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Pharmacology III > CNS Drugs: Anesthetics > Flashcards

CNS Drugs: Anesthetics Flashcards

1
Q

What route of anesthesia?

injection into CSF in
lumbar region;

Blocks sympathetic fibers in
the subarachnoid space

A

spinal

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2
Q

Which type of local anesthetic?

shorter duration

increased systemic toxicity

A

Esters

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3
Q

LAs must be ______ to cross the cell membrane

A

non-ionized

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4
Q

To bind to the sodium channel, LAs must be ______. this happens where?

A

ionized, happens inside cell

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5
Q

at physiologic pH of 7.4, LAs are typically in what form?

A

ionized

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6
Q

where is the binding site for LAs on the sodium channel?

A

inner membrane

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7
Q

in general the closer the pKa is to physiologic pH, the higher the conc. of drug in the ______ form

A

non-ionized

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8
Q

pKa close to 7.4 means what for membrane transport?

A

faster

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9
Q

Lidocaine pKa is 7.8, bupivacaine is pKa 8.1… which will have a faster onset?

A

lido

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10
Q

which LA is always in the non-ionized form, with the pKa of 3.5

A

benzocaine

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11
Q

_______ can make pH more basic and therefore increase non-ionized concentrations and degree of LA transport

A

bicarb

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12
Q

LAs exhibit state-dependent blockade, which means they target channels in what states

A

open and inactivated states (rapidly firing axons)

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13
Q

What effect does increased calcium have on LA activity?

A 
diminished effects 
(hyperpolarized, more resting state channels)
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14
Q

What effect does increased potassium have on LA activity?

A

enhanced effects (depolarized, more active)

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15
Q

The below have what potency/lipid solubility compared to procaine, and what duration?

tetracaine
bupivacaine
ropivacaine

A

Long acting

16x potency

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16
Q

The below has what potency/lipid solubility compared to procaine?

lidocaine

A

4x

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17
Q

The below have which duration of action compared to procaine?

cocaine
mepivacaine
lidocaine

A

medium acting

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18
Q

The below have what potency/lipid solubility compared to procaine?

cocaine
mepivacaine

A

2x

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19
Q

procaine is ____ acting

A

short

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20
Q

Toxic effects of LAs (CNS, cardiac) depend on…

A

half-life

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21
Q

Concurrent use of ____ along LAs has the below effects

•
Decreases diffusion of drug
•
Prolongs duration of action
•
Decreases systemic absorption
•
Decreases risk of systemic toxicity
A

vasoconstrictors

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22
Q

Which type of LAs?

•
Metabolized in the liver by the CYP450s
•
Toxicity is more likely in patients with hepatic disease or
reduced hepatic blood flow
A

amides

23
Q

Which type of LAs?

•
Rapidly metabolized by butyrylcholinesterases in the
plasma
•
Mutations can affect metabolism of these LAs

A

esters

24
Q

What is the order of sensitivity of LA effects?

A

SNS > pain > touch > motor

25
Q

This happens when a block is not limited to the intended site.

it can lead to motor paralysis, respiratory impairment, hypotension

A

differential block

26
Q

____ fibers are more sensative than large ones

A

small diameter (B/C)

27
Q

Myelinated or unmyelinated fibers of similar diameter are more or less sensitive?

A

myelinated (type delta) less sensitive

28
Q

the _____ the conduction velocity, the less sensitive. Meaning motor fibers are less sensitive than pain

A

faster conduction = less sensitive

29
Q

Which LA has the following SE/Toxicity?

increased binding to cardiac Na channels, slower
dissociative times

A

bupivacaine

30
Q

What can help decrease cardiotoxicity of LAs?

A

IV lipid administration

31
Q

Cardio effects of LAs are…

A

arrhythmia, vasodilation, hypotension

32
Q

The depression of cortical inhibitory pathways can lead to…

A

severe CNS sxs, TNS

33
Q

allergic reactions are often due to PABA, which is a metabolite of which class?

A

Esters

34
Q

Which LA can produce methemoglobinemia?

A

prilocaine

35
Q

Which LA?

metabolized to PABA (allergy & sulfa inhibition)

Used for infiltration anesthesia

A

procaine

36
Q

Which LA?

preferred for ophthalmologic use

spinal anesthesia with 10% dextrose

severe toxicity w. high volume peripheral blocks

A

tetracaine

37
Q

Which LA?

topical only
high risk methemoglobinemia

A

benzocaine

38
Q

Which LA?

Rapid onset anesthesia

Preferred for infiltration blocks and epidural

not used for Spinal Blocks

A

lido

39
Q

why isn’t lido used for spinal blocks?

A

risk of TNS

40
Q

Which LA?

highest rate of clearance of amides

can cause methemoglobinemia

largely limited to dentistry

A

prilocaine

41
Q

This has more potent sensory block than motor block.

is used for epidural during labor and childbirth

A

bupivacaine

42
Q

which amide has greatest cardiotoxicity and diffuses away from cardiac channels slowly?

A

bupivacaine

43
Q

This is an S-enantiomer of bupivacaine that is less lipid soluble and cleared more rapidly

A

ropivacaine

44
Q

what advantages does ropivacaine have against bupivacaine?

A

less adverse effects, less cardiotoxic

45
Q

ropivacaine is used for…

A

peripheral/epidural

46
Q

which amide is vaso-constricting at clinical doses?

A

ropivacaine

47
Q

Mepivacaine is not used for…

A

labor

48
Q

etidocaine is the opposite of bupivacaine in that it causes…

A

motor block before sensory block (differential block)

49
Q

Which LA contains both amide and ester group?

A

articaine

50
Q

the ester group on articaine renders it open to metabolism by…

A

plasma esterases

51
Q

Where is articaine used?

A

dentistry

52
Q

The dibucaine number test measures activity of _______ to differentiate individuals with mutations and deficiency

A

butyrylcholinesterase

53
Q

dibucaine (induces/inhibits) wild type butyrylcholinesterase

A

inhibits

Pharmacology III (15 decks)

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