Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

CNS Pharma > Slides 1 > Flashcards

Slides 1 Flashcards

(50 cards)

Start Studying
1
Q

What do local anesthetics do?

A

They reversibly block impulse conduction along nerve axons that utilize sodium channels as the
primary means of action potential generation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are local anesthetics used for?

A

1) To block pain sensation from specific areas of the body.

2) To block sympathetic vasoconstrictor impulses to specific areas of the body.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

At least three nociceptors

are recognized:

A

1) Acid
2) Injury
3) Heat

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What does a nerve ending have?

A

Opioid receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What do opioid receptors do?

A

Inhibit action potential generation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does the axon have?

A

Na+ and K+ channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What do Na+ and K+ channels do?

A

Propagate action potentials

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Synaptic transmission involves:

A

The release of substance P, a neuropeptide (NP), and glutamate and activation of their receptors on the secondary neuron.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What modulates the transmission process?

A

Alpha2 adrenoceptors and opioid receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the ionotropic glutamate receptors?

A

1) α-amino-3-hydroxy-5-methylisoxazole-4-
proprionic acid (AMPA) receptors
2) Kainic acid (KA) receptors
3) N-methyl-D-aspartate (NMDA) receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Where are AMPA receptors found?

A

In all neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are AMPA receptors permeable to?

A

Na+ and K+, but NOT to Ca+2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Where are KA receptors found?

A

1) Hippocampus
2) Cerebellum
3) Spinal cord

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are KA receptors permeable to?

A

Na+ and K+, and some to Ca+2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Where are NMDA receptors found?

A

In all neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are NMDA receptors permeable to?

A

Na+, K+, and Ca+2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Peptides often coexist with ___ in the same neuron.

A

A conventional nonpeptide transmitter

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Substance P is contained in and released from:

A

Small unmyelinated primary sensory neurons in the spinal cord and brain stem.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What does substance P do?

A

Causes a slow EPSP in target neurons = transmit noxious stimuli.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Substance P is also released with:

A

Glutamate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is the first local anesthetic introduced into clinical practice for ophthalmic use, in 1884?

22
Q

What is the chronic use of cocaine associated with?

Study These Flashcards
A

Psychological dependence (addiction).

23
Q

What was synthesized to improve upon the clinical properties of cocaine in 1905, and became the dominant local anesthetic for about 50 years?

24
Q

What anesthetic was discovered in 1943 that is now the most widely used local anesthetic?

25
What is the chemical makeup for most local anesthetics?
A lipophilic group (aromatic) connected to an ionizable group (tertiary amine) via an ester or amide linkage.
26
Local anesthetics are: a) Strong acids b) Strong bases c) Weak acids d) Weak bases
d) Weak bases
27
Local anesthetics exist in the body as:
Either uncharged bases or cations.
28
Which is the most active form: Uncharged bases or cations? Why?
The cationic form, because it can't exit from the closed channels
29
Why do local anesthetics also exist in an uncharged form?
Because it's important for rapid penetration of biologic membranes, since the receptor is not accessible from the external side of the cell membrane.
30
Local anesthetics are less effective when:
Injected into infected tissue, because low pH cause ionization of the drug.
31
What does low pH do to local anesthetics?
Causes ionization of the drug.
32
Esters have a shorter duration of action than amides, because:
They are more prone to hydrolysis
33
What are the classifications of local anesthetics?
1) Amides | 2) Esters
34
What are some examples of amide local anesthetics?
1) Lidocaine (Lignocaine) 2) Bupivicaine 3) Ropivacaine 4) Mepivacaine 5) Levobupivicaine 6) Prilocaine
35
What are some examples of ester local anesthetics?
1) Cocaine 2) Procaine 3) Tetracaine 4) Benzocaine
36
What is the local anesthetics' primary mechanism of action?
Blockade of voltage-gated sodium channels.
37
How do local anesthetics carry out their mechanism of action?
Local anesthetics bind to receptors near the intracellular end of the sodium channel and block the channel in a time and voltage dependent fashion.
38
What happens when progressively increasing concentrations of | a local anesthetic are applied to a nerve fiber?
1) The threshold for excitation increases 2) Impulse conduction slows 3) The rate of rise of the action potential declines 4) The action potential amplitude decreases 5) The ability to generate an action potential is completely abolished.
39
On what basis do nerve fibers differ significantly in their susceptibility to block by local anesthetics?
On the basis of differences in size and degree of myelination.
40
Which fibers are blocked first by local anesthetics?
The smaller B and C fibers.
41
Which fibers are blocked last by local anesthetics?
Motor fibers
42
What are the side effects of local anesthetics?
1) Motor paralysis = a) Limits cooperation during obstetric delivery b) Impairs respiratory activity 2) Autonomic nerve block = hypotension and urinary retention (from bladder function interference) 3) Some (bupivacaine and ropivacaine) cause lethal arrhythmias in high concentrations.
43
Which local anesthetic has an antiarrhythmic effect on the heart at concentrations lower than those needed to produce nerve block?
Lidocaine
44
What is the half life of ester-based local anesthetics?
<1 minute
45
Absorption of the local anesthetic to the | systemic circulation from the site of application depends on many factors such as:
Local blood | flow
46
Application to a highly vascular area results in | __(low/high) blood levels of the local anesthetic.
High
47
What do vasoconstrictor substances (like epinephrine) do?
Reduce the systemic absorption of the local | anesthetic from the injection site
48
How do vasoconstrictors reduce systemic absorption of the local anesthetic from the injection site?
By decreasing | blood flow, and prolonging its local effect (systemic toxic effects of local anesthetic is also reduced)
49
What does epinephrine do when used in spinal anesthesia?
Stimulates α2 adrenoceptors = inhibits release of substance P (neurokinin-1) and reduce sensory neuron firing = enhances and prolongs local anesthesia
50
Which 2 α2-agonists | have been used to augment local anesthetic effect in the subarachnoid space and peripheral nerves?
1) Clonidine | 2) Dexmedetomidine

CNS Pharma (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions