Flashcards in Sedatives - Kruse Deck (16):
Goal of sedatives
Depress CNS function, cause calm and drowsiness
Drug classes (general) w/ sedation side effect (3)
Can intensify the effects of CNS depressants
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
Describe dose-response curve for sedative-hypnotics
Increasing CNS effects as dose increases...
- Sedation --> Hypnosis --> Anesthesia --> Coma
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
**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
Benzos are VERY good for what?
**Barbituates - MoA
Bind to GABA-A receptor and increase DURATION of opening time (increased Cl- currents)
Eszopiclone, Zaleplon, Zolpidem - MoA
Agonist at benzo site on GABA-A receptor
Ramelteon - MoA
What to avoid?
Agonist at melatonin receptors (MT1, MT2)
Sleepiness, ENDOCRINE CHANGES (low testosterone, high PRL)
Buspirone - MoA
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
Patient w/ hepatic disease also has anxiety or panic disorder. Best Benzos to give?
What is the GABA-A receptor?
Ligand-gated CHLORIDE channel, causing hyper-polarization and reduction in the number of APs w/in the CNS
Flumazenil works to reverse which drugs?
THOSE WORKING AT THE BENZO SITE...
Best uses for...
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