1GABA receptors
Inhibitory, brakes
2Glutamate receptors
excitatory, gas
3ultra short barbituate onset
under a minute
4ultra short barbituate duration
a few minutes
5short barbituate onset
15-30 minutes
6short barbituate duration
4-6 hours
7intermediate barbituate onset
about 30 minutes
8intermediate barbituate duration
6-8 hours
9long barbitaute onset
about an hours
10long barbituate duration
8-12 hours
11methohexital (Brevital®) classification
ultra-short barbituate
12thiamyl (Surital®) classification
ultra-short barbituate
13thiopental (Pentothal®) classification
ultra-short barbituate
14amobarbital (Amytal®) classification
intermediate barbitaute
15pentobarbital (Nembutal®) classification
intermediate barbitaute
16secobarbital (Seconal®) classification
intermediate barbitaute
17Tuinal® (amobarbital/secobarbital combination product) classification
intermediate barbitaute
18butalbital classification
intermediate barbitaute
19butabarbital (Butisol®) classification
intermediate barbitaute
20talbutal (Lotusate®) classification
intermediate barbitaute
21 aprobarbital (Alurate®) classification
intermediate barbitaute
22phenobarbital classification
long barbituate
23Barbituate MOA
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
24What are the binding sites on the GABA-A receptor?
There are two a2, two B2, and one y2.
25a1 subunit effects
important for hypnotic effects. Z-drugs such as Zolpidem have high affinity for a1.
may be reponsible for anti-convulsant effects.
26a2 subunit effects
important for anti-anxiety effects.
27Chloral Hydrate
first depressant drug developed for the purpose of inducing sleep. rarely prescribed, replaced by z-drugs.
28Paraldehyde
relatively safe hypnotic
halitosis, 30% of dose excreted via lungs (causes bad breath)
anticonvulsant, doesn't suppress breathing at therapeutic doses
29Bromides (NaBr, KBr)
used in vetenary practice as anticonvulsant, but no longer used for patients due to toxicity
30Methaqualone
GABAR agonist
marketed as a non-barbituate sedative that is safe and non-addictive, but became schedule I drug due to addiction and overdose.
31Z-drugs
high afinity for a1 receptor on GABA-A
treats insomnia
fewer side effects that benzodiazepines
323 primary groups of Z-drugs
Imidazopyrines
Cyclopyrrolones
Pyrazolopyrimidines
33Imidazopyrines example
Zolpidem (Ambien)
34Cyclopyrrolones example
zolpiclone, eszopiclone (Lunesta)
35Pyrazolopyrimidines example
zaleplon (Sonata)
36Anti Histamines MOA
H1 receptor invers agonist
37Anti Histamines examples
diphenhydramine (Benadryl)
doxylamine
pyrilamine