CNS Depressants: Sedatives/Hypnotics

Inhibitory, brakes

excitatory, gas

under a minute

a few minutes

15-30 minutes

4-6 hours

about 30 minutes

6-8 hours

about an hours

8-12 hours

ultra-short barbituate

ultra-short barbituate

ultra-short barbituate

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

intermediate barbitaute

long barbituate

Potentiate GABA (binds to GABA-A receptor, increases duration of GABA activation)
Potentiate glycine (another potentially inhibitory nerotransmitter)
Inhibit glutamate (excitatory neurotransmitter)
Causes reduced neuronal excitability

There are two a2, two B2, and one y2.

important for hypnotic effects. Z-drugs such as Zolpidem have high affinity for a1.
may be reponsible for anti-convulsant effects.

important for anti-anxiety effects.

first depressant drug developed for the purpose of inducing sleep. rarely prescribed, replaced by z-drugs.

relatively safe hypnotic
halitosis, 30% of dose excreted via lungs (causes bad breath)
anticonvulsant, doesn't suppress breathing at therapeutic doses

used in vetenary practice as anticonvulsant, but no longer used for patients due to toxicity

GABAR agonist
marketed as a non-barbituate sedative that is safe and non-addictive, but became schedule I drug due to addiction and overdose.

high afinity for a1 receptor on GABA-A
treats insomnia
fewer side effects that benzodiazepines

Imidazopyrines
Cyclopyrrolones
Pyrazolopyrimidines

Zolpidem (Ambien)

zolpiclone, eszopiclone (Lunesta)

zaleplon (Sonata)

H1 receptor invers agonist

diphenhydramine (Benadryl)
doxylamine
pyrilamine