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Flashcards in Sedatives - Kruse Deck (16):
1

Goal of sedatives

Drugs? (8)

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

Benzodiazepines
Barbituates
Buspirone
Eszopiclone
Zaleplon
Zolpidem
Meprobamate
Ramelteon

2

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



Why important?

Antidepressants
Antihistamines
Antipsychotics

Can intensify the effects of CNS depressants

3

Sedation vs. hypnosis



How do they relate on the CNS depression scale?

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

Hypnotic = drowsy, sleep

Hypnosis > Sedation

4

Describe dose-response curve for sedative-hypnotics

Increasing CNS effects as dose increases...
- Sedation --> Hypnosis --> Anesthesia --> Coma

5

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

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

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

6

**Benzos - MoA

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

7

Benzos are VERY good for what?

Anti-anxiety effects

8

**Barbituates - MoA

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

9

Eszopiclone, Zaleplon, Zolpidem - MoA

Agonist at benzo site on GABA-A receptor

10

Ramelteon - MoA

What to avoid?

Side effects?

Agonist at melatonin receptors (MT1, MT2)

Fluvoxamine (SSRI)

Sleepiness, ENDOCRINE CHANGES (low testosterone, high PRL)

11

Buspirone - MoA

Use?

Benefits?

Downfalls? (2)

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

12

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

Lorazepam, Oxazepam

13

What is the GABA-A receptor?

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

14

Flumazenil works to reverse which drugs?

THOSE WORKING AT THE BENZO SITE...
- Benzos
- Zolpidem
- Zaleplon
- Eszopiclone

15

Best uses for...
- Zolpidem
- Zaleplon
- Eszopiclone
- Ramelteon

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

16

Meprobamate...
- Uses?
- Risks?
- Comes from?

Short-term anxiety relief, sedation

High tolerance, dependence, abuse

Carisoprodol (central muscle relaxant)