13 Flashcards

1
Q

Postitively charged anesthetic will

A

act once it gets inside neural membrane. Both form of anesthetics exist, and amine groups help get pKa to 7.4 where we want these to be working.

**basic form does a better job of getting in the membrane than acidic form generally speaking. Both act, but the basic form gets in better.

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2
Q

Ester linkages ——- better than amide

A

break apart - serum cholinesterases will hydrolyze esters

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3
Q

Aromatic groups are for

A

lipophilic properties - crossing membranes.

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4
Q

Do NOT inject these things into

A

arteries - they will get into the brain.

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5
Q

Esters downsides

A

hydrolyzing leads to something being more allergenic - the hydrophobic group is allergenic.

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6
Q

Local anesthetics with an ester linkage will be hydrolyzed by

A

pseudocholinesterase and have a very short half life in the plasma

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7
Q

Local anesthetics with an amide linkage will be metabolized by

A

P450 enzymes in the liver and have a longer half life in the plasma.

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8
Q

Esters are more generally

A

allergenic

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9
Q

Amides will have an

A

I in their name prior to the “caine”

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10
Q

Local anesthetics favored in dentistry are

A

amides

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11
Q

Local anesthetics cross the axon membrane and interact with the ————— forms of the Na+ channel, blocking Na+ conductance. They are not effective outside the axon.

A

open and inactivated

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12
Q

Because local anesthetics bind to the open form of the sodium channel, they produce a more

A

rapid nerve block on axons with a more rapid firing rate.

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13
Q
  1. Functions served by ——— are more readily disrupted by local anesthetics than the —————
A

B and C fibers

motor functions served by (larger) A fibers*

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14
Q
  1. Sensory neurons are ———–in size and sensitivity
A

heterogeneous

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15
Q

The faster a fiber is blocked, the ——- it takes to recover

A

longer - first on first off.

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16
Q

Block more

A

rapid with rapidly firing nerves

17
Q

Inflamed tissue is more difficult to anesthetize.

Products released by cells in inflamed tissue lower

A

pH, making it more difficult to get sufficient levels of anesthetic inside the axon.

18
Q

If epinephrine is included, the pH is frequently lowered to ——– to stabilize the epinephrine.

A

4 or 5

19
Q

The buffering capacity at the injection site should ————-

A

neutralize this lower pH from stabilizing epinephrine

20
Q

Risk of adding bicarbonate before injection?

A

precipitating anesthetic.

21
Q

Direct effects on the heart local anesthetic.

A

Block cardiac Na+ channels Block cardiac Ca++ channels (much higher concentrations)

22
Q

Effects on the autonomic nervous system: (inhibition of sympathetic responses)

A

Depress contractility, produce hypotension

23
Q

-zosin

A

a1-adrenergic receptor blocker

24
Q

-olol

A

b-adrenergic receptor blocker

25
Q

-alol, -ilol

A

b-adrenergic receptor blocker, with a1 activity