Local Anesthetics Flashcards

1
Q

Local anesthesia can be accomplished by many substances such as

A

amines, alcohols and many toxins

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2
Q

Pressure on nerve endings can result in

A

Anesthesia

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3
Q

What is the prototype local anesthetic

A

Cocaine

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4
Q

What plant in the Andes mountains does cocaine come from?

A

Erythroylon Coca

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5
Q

Who isolated the pure alkaloid in 1860?

A

Albert Niemann

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6
Q

Who in 1884 completed the first study reporting it’s value as a stimulant, treatment for ETOH and MSO4 addiction, antiasthmatic, local anesthetic and aphrodisiac

A

Sigmund Freud

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7
Q

What was the first synthetic LA?

A

Procaine- made in 1905 by Einhorn

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8
Q

What was the first amide anesthetic?

A

Dibucaine 1932

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9
Q

When was Tetracaine first used?

A

1930

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10
Q

When was lidocaine first sythesized?

A

1943 by Lofgren

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11
Q

How is a nerve action potential generated?

A

Following an increase the permability of the membrane to sodium ions

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12
Q

How do LA’s work?

A

Local anesthetics produce a reversible, dose-dependent blockade of sodium ion influx into nerve cytoplasm.

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13
Q

What is an Axon

A

functional unit of the nerve

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14
Q

What is an axolema

A

The nerve cell membrane

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15
Q

What is the axoplasm?

A

the intracellular components

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16
Q

What do Schwann cells do?

A

surround, support, insulate axon

17
Q

What is a fascicle?

A

A bundle of axons

18
Q

What is the endoneurium?

A

layer of delicate collagen tissue around axon embedding it in the fascicle

19
Q

What is the Perineurium

A

Over-lapping group of cells binding fascicles

20
Q

What is the Epineurium?

A

Layers of connective tissue around fascicles These layers must be penetrated by LA to produce it’s effect

21
Q

What is Myelin?

A

liquid substance containing proteins and lipids, forms insulating layer around some nerves. Basically prevents current from leaking out of nerve.

22
Q

What are nodes of Raniver?

A

small, unmyelinated segments between Schwann cells. Contain large numbers of Na channels allowing intense APs which can “jump” from node to node. (saltatory conduction)

23
Q

What is important about the nodes of Ranvier and diffusion of LA’s?

A

Limited diffusion barrier at the nodes of Ranvier= Primary site of LA action

24
Q

Is a nerve blockade concentration dependent?

A

Yes- It ends when the concentration of LA falls below a minimum effective point Requires disruption of several, contiguous channels

25
Q

What are LA’s in aqueous solution?

A

Weak bases

26
Q

Since the actual drug (LA’s) is poorly water soluble how are they produced?

A

usually produced as water soluble hydrochloride salts which are acidic and more stable.