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AU14 Pharmacology > Exam 2; Local Anesthetics and Spasmolytics > Flashcards

Exam 2; Local Anesthetics and Spasmolytics Flashcards

1
Q

This is any agent that can reversibly block the electrical activity of excitable tissues

A

local anesthetic

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2
Q

What are the two actions of local anesthetics

A

decrease neuronal conduction

block impulse conduction in the heart

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3
Q

How are local anesthetics used as painkillers

A

temporary analgesia without loss of consciousness

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4
Q

All local anesthetics have what two ends

A

automatic (lipophilic)

amino (hydrophilic)

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5
Q

This part of the local anesthetic can get though the neuronal membrane

A

lipophilic

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6
Q

This part of the local anesthetic is inside the membrane or cell, this end gets ionized

A

amino

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7
Q

Local anesthetics in the non-ionized form get through the neuronal membrane and once inside, what occurs

A

the hydrophilic side is ionized and binds to a specific site on the sodium channel of the excitable membrane/tissue; blocking the Na channel

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8
Q

What are the three events of local anesthetics blocking the Na channels

A

decreases neuronal conduction
decreases repolarization rate
increases refractory period

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9
Q

What will increase effect of the local anesthetic

A

Na channels are open; neurons not fire more rapidly

will have open channels more often and affected more

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10
Q

Which size of neurons are generally more susceptible to local anesthetics

A

smaller neurons

pain more susceptible than motor neurons

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11
Q

Which type of myelination of neurons is more susceptible to local anesthetics

A

myelinated neurons

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12
Q

Which speed of firing is more susceptible to local anesthetics

A

faster the firing rate the more susceptible

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13
Q

What is the sensitivity ranking regarding, warm, cold, pain, motor, and touch/pressure

A

pain > cold > warm > touch/pressure > motor

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14
Q

What is the major distinction between local anesthetics

A

their duration of action

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15
Q

This type in linkage has a relatively short duration

A

ester linkage

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16
Q

The ester is metabolized by what

A

plasma cholinesterase

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17
Q

What is the half like of ester linked LAs

A

minutes

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18
Q

This type of linkage is fairly long

A

amide linkage

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19
Q

The amide is metabolized by what

A

in the liver by CYP450

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20
Q

What is the half life of amide linked LAs

A

hours

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21
Q

Local anesthetics are weak bases or acids

A

bases

22
Q

In an acidic environment, the local anesthetic will be what

A

more ionized

23
Q

In infected tissues which tend to be more acidic, what happens to the local anesthetic

A

the molecules don’t readily enter the cell and LA activity is decreased

24
Q

Repeated use of an epidural anesthetic can do what

A

lower pH and cause tachyphalaxis

25
Q

These are used with local anesthetics to increase duration of action (except for cocaine)

A

vasoconstrictors (like Epi.)

26
Q

What are the three topical routes of administration of a LA

A

skin
mucosa
eye

27
Q

What are the three routes of administration of injection of LA

A

infiltration
direct nerve block
spinal or epidural

28
Q

Regardless of route of administration, all local anesthetics can be what

A

systemically absorbed

29
Q

Which linkage of LA is more likely to cause an allergic reaction

A

esters

30
Q

This ester LA inhibits the re-uptake of NE in the CNS

A

cocaine

31
Q

What is cocaine used for

A

ophthalmic; nasal surgery

32
Q

This is an ester LA with low solubility so a long duration of action and is used topically

A

benzoxaine

33
Q

This ester LA has a short half-life and is not used topically because it doesn’t readily pass through the mucous membranes

A

procaine

34
Q

These are ester LAs that are used in the eye

A

benoxinate and proparacaine

35
Q

These is an amino amide LA used IV for cardiac arrthymia and produces a lupus like syndrome in slow acetylators

A

procainamide

36
Q

This is the most common amino amide LA and is used IV for arrthymias

A

lidocaine

37
Q

What are some CNS side effects of lidocaine

A

tremors
slurred speech
drowsiness

38
Q

What is it that distinguishes the amino amide LAs

A

all the names contain “two i’s” and “-caine”
articaine
mevpicane

39
Q

What are the six CNS side effects of local anesthetics

A 
disorientation
drowsiness
slurred speech
tongue numbness 
tinnitus (ringing in the ears)
burred vision
40
Q

What is the side effect on the cardiovascular system of LAs

A

alter the heart rhythm

41
Q

What are the two specific side effects of cocaine

A

vasoconstrictor

CNS effects

42
Q

This is an irreversible sodium channel blocker that can cause muscle weakness, respiratory paralysis, and death

A

tetrodotoxi

43
Q

This is an irreversible sodium channel blocker that can cause muscle weakness, respiratory paralysis, and death; from the red tide

A

saxitoxin

44
Q

This is excessive muscle contraction; muscle hypertonia

A

spasticity

45
Q

What results in spasticity

A

neuronal damage; injury, stroke, MS, CP, ALS

46
Q

What is the treatment for spasticity

A

either alter the innervating neurons or act directly on muscle

47
Q

This is a GABA agonist that increases the activity of inhibitory neurons; treatment for spasticity

A

baclofen

48
Q

This is a minor tranquilizer and muscle relaxant that increases GABA activity; treatment for spasticity

A

diazepam and other benzodiazepines

49
Q

This is an α2 agonist; inhibiting motor neurons; treatment for spasticity

A

tizanidine

50
Q

This is a treatment for spasticity; neuronal effects

A

botulinum toxin

51
Q

This acts directly on muscle cells and inhibits the stimulus induced release of Ca from the muscle SR; decreasing availability of Ca for muscle; treatment for spasticity

A

dantrolene

52
Q

What are two side effects of dantrolene

A

muscle weakness

hepatitis

AU14 Pharmacology (29 decks)

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