Local Anesthetics Flashcards

1
Q

An ideal local anesthetic has _____ paralysis of sensory nerves.

A

reversible

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2
Q

Ideal local anesthetic is addictive. True or False.

A

False - nonaddictive

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3
Q

An ideal local anesthetic is ___ soluble and stable in water.

A

readily

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4
Q

an ideal local anesthetic has a pH near ____

A

neutrality

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5
Q

An ideal local anesthetic is nonirritating to tissues. True or False.

A

True

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6
Q

An ideal local anesthetic has ___ systemic toxicity.

A

minimum

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7
Q

An ideal local anesthetic is absorbed _____ (quickly, slowly)

A

slowly

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8
Q

An ideal local anesthetic is _____ and ____ detoxified.

A

readily and rapidly

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9
Q

An ideal local anesthetic is compatible with ____

A

epinephrine

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10
Q

An ideal local anesthetic has no hyperesthesia following recovery of sensation. True False.

A

True

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11
Q

An ideal local anesthetic is able to withstand heat sterilization. True or False.

A

True

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12
Q

An ideal local anesthetic is expensive. True or False.

A

False - inexpensive

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13
Q

3 parts of the molecule (which ones are hydrophilic/lipophilic?)

A

(1) Unsaturated aromatic group - lipophilic
(2) intermediate chain - site o degredation - aminoesters, aminoamides
(3) Tertiary amine - hydrophilic

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14
Q

The tertiary amine is a ____ base.

A

weak

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15
Q

the pKs of the tertiary base are above ______ pH

A

physiologic

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16
Q

At a pH of 7.4; more than 50% of drug is ____

A

ionized

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17
Q

Which form of drug interacts with cell membranes (ionized/non-ionized)?

A

nonionized

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18
Q

More nonionized drug means _____ (faster or slower) onset and ______ (higher or lower) potency.

A

faster onset; higher potency

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19
Q

_____ decreases nonionized form of drug.

A

acidosis

20
Q

Local anesthetics inhibit _____ of nerve impulses.

A

Propagation (conduction)

21
Q

Local anesthetics block ____ channels which cause rapid ______ by allowing rapid ____ movement of ____.

A

sodium; rapid depolarization; rapid inward movement of Na

22
Q

Anesthetic potency depends on…. and determines ….

A

lipid solubility; determines ability of the molecule to reach its site of action

23
Q

Ionized form of drug is used for? and nonionized?

A

ionized form to dissolve in body fluids; nonionized to enter cell membrane

24
Q

Onset of action depends on these three things

A

(1) physiochemical properties
(2) Dose and concentration
(3) Site of injection

25
Q

Anesthetics is removed by ____ circulation.

A

systemic

26
Q

Local anesthetics themselves have vascular effects. True or False.

A

True

27
Q

Local anesthetics at clinical doses cause _____ (vasoconstriction or vasodilation)?

A

Vasodilation (except cocaine

28
Q

Why is epinpehrine added in some anesthetics?

A

sometimes added to produce vasoconstriction to prolong the local anesthetic’s effect

29
Q

Not all fibers respond the same. Their sensitivity is determined by:

A

fiber size, fiber type, nerve location, length of nerve exposed to local anesthetic, time for equilibrium in tissue; agent used

30
Q

Which nerves are blocked first?

A

Sympathetic and pain fibers; followed by sensory fibers

31
Q

Which nerves are blocked last?

A

Motor fibers

32
Q

Aminoesters are rapidly hydrolyzed in plasma by _____

A

non-specific pseudocholinesterases

33
Q

Aminoamides undergo more varied metabolism usually in this organ.

A

Liver

34
Q

Metabolites are excreted in the ____

A

urine

35
Q

Side effects on systemic toxicity - CNS toxicity

A

Initially excitement; followed by depression and cardiopulmonary collapse

36
Q

Side effects on systemic toxicity - cardiovascular toxicity on the heart

A

Electrophysiological - decrease in rate of depolarization; mechanical - decrease in cardiac output

37
Q

Side effects on systemic toxicity - cardiovascular toxicity on peripheral vasculature

A

Low concentrations cause vasoconstriction; higher concentrations causes vasodilation

38
Q

Side effects on local toxicity

A

histotoxic on skeletal muscle, nerves (high concentrations), not usually significant; vasoconstriction - addition of epi, can cause tissue damage due to compromised blood supply

39
Q

Anesthetics may cause methemoglobinemia as a toxic effect. True or False.

A

True

40
Q

Allergic reactions are more common with this type of anesthetic.

A

aminoesters

41
Q

Uses of local anesthetics

A

Topical, local infiltration, peripheral (conduction) nerve block; intravenous block; epidural and spinal blocks

42
Q

Lidocaine - potency, onset, duration after infiltration, max single dose for infiltration, toxic plasma concentration, pK, protein binding %

A

Potency = 1; Onset = rapid; Duration after infiltration = 60-120 minutes; Max single dose for infiltration = 300 mg; toxic plasma concentration = >5 ug/ml; pK = 7.9; protein binding = 70%

43
Q

Mepivacaine - potency, onset, duration after infiltration, max single dose for infiltration, toxic plasma concentration, pK, protein binding %

A

potency = 1; onset = slow; duration after infiltration = 90-180; max single dose for infiltration = 300; toxic plasma concentration = >5 ug/mL; pK = 7.6; protein binding = 77%

44
Q

Bupivacaine - potency, onset, duration after infiltration, max single dose for infiltration, toxic plasma concentration, pK, protein binding %

A

potency = 4; onset = slow; duration after infiltration = 240-480 min; max single dose for infiltration = 175 mg; toxic plasma concentration = >3 toxic plasma concentration ug/mL; pK = 8.1; protein binding = 95%

45
Q

Ropivacaine - potency, onset, duration after infiltration, max single dose for infiltration, toxic plasma concentration, pK, protein binding %

A

Potency = 4; onset = slow; duration after infiltration = 240 - 480 minutes; max single dose for infiltration = 200 mg; toxic plasma concnetration = >4 ug/mL; pK = 8.1; protein binding = 94%