Sedatives - Kruse Flashcards

You may prefer our related Brainscape-certified flashcards:
1
Q

Goal of sedatives

Drugs? (8)

A

Depress CNS function, cause calm and drowsiness
- ANTI-ANXIETY

Benzodiazepines
Barbituates
Buspirone
Eszopiclone
Zaleplon
Zolpidem
Meprobamate
Ramelteon
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Drug classes (general) w/ sedation side effect (3)

Why important?

A

Antidepressants
Antihistamines
Antipsychotics

Can intensify the effects of CNS depressants

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

Sedation vs. hypnosis

How do they relate on the CNS depression scale?

A

Sedation = decreased CNS, less excitement, calm, anti-anxious

Hypnotic = drowsy, sleep

Hypnosis > Sedation

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

Describe dose-response curve for sedative-hypnotics

A

Increasing CNS effects as dose increases…

- Sedation –> Hypnosis –> Anesthesia –> Coma

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

How do barbituates and alcohol differ from benzos and newer hypnotics?

A

Barbs/EtOH = linear dose-response curve, easier coma

Benzos/newer = plateauing dose-response curve, much harder to reach coma

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

**Benzos - MoA

A

Promote lower threshold for GABA binding to GABA-A receptor, enhancing FREQUENCY/EFFICIENCY of Cl- currents

Leads to sedation, hypnosis, muscle relaxation, anxiolysis, and anticonvulsion

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

Benzos are VERY good for what?

A

Anti-anxiety effects

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

**Barbituates - MoA

A

Bind to GABA-A receptor and increase DURATION of opening time (increased Cl- currents)

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

Eszopiclone, Zaleplon, Zolpidem - MoA

A

Agonist at benzo site on GABA-A receptor

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

Ramelteon - MoA

What to avoid?

Side effects?

A

Agonist at melatonin receptors (MT1, MT2)

Fluvoxamine (SSRI)

Sleepiness, ENDOCRINE CHANGES (low testosterone, high PRL)

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

Buspirone - MoA

Use?

Benefits?

Downfalls? (2)

A

Stimulates 5-HT-1A receptors

General anxiety disorder

No risks w/ alcohol, addiction, sedation, or tolerance

  • Takes 1-2 weeks to take effect
  • Interacts w/ CYP inhibitors/inducers
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Patient w/ hepatic disease also has anxiety or panic disorder. Best Benzos to give?

A

Lorazepam, Oxazepam

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

What is the GABA-A receptor?

A

Ligand-gated CHLORIDE channel, causing hyper-polarization and reduction in the number of APs w/in the CNS

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

Flumazenil works to reverse which drugs?

A

THOSE WORKING AT THE BENZO SITE…

  • Benzos
  • Zolpidem
  • Zaleplon
  • Eszopiclone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Best uses for…

  • Zolpidem
  • Zaleplon
  • Eszopiclone
  • Ramelteon
A
Zol = those who can't fall asleep
Zal = those who can't fall asleep
Esz = those who awaken early or can't stay asleep

Ram = those who can’t fall asleep

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

Meprobamate…

  • Uses?
  • Risks?
  • Comes from?
A

Short-term anxiety relief, sedation

High tolerance, dependence, abuse

Carisoprodol (central muscle relaxant)