CNS Depressants: Sedatives/Hypnotics
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GABA receptors
Inhibitory, brakes
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Glutamate receptors
excitatory, gas
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ultra short barbituate onset
under a minute
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ultra short barbituate duration
a few minutes
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short barbituate onset
15-30 minutes
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short barbituate duration
4-6 hours
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intermediate barbituate onset
about 30 minutes
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intermediate barbituate duration
6-8 hours
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long barbitaute onset
about an hours
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long barbituate duration
8-12 hours
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methohexital (Brevital®) classification
ultra-short barbituate
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thiamyl (Surital®) classification
ultra-short barbituate
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thiopental (Pentothal®) classification
ultra-short barbituate
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amobarbital (Amytal®) classification
intermediate barbitaute
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pentobarbital (Nembutal®) classification
intermediate barbitaute
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secobarbital (Seconal®) classification
intermediate barbitaute
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Tuinal® (amobarbital/secobarbital combination product) classification
intermediate barbitaute
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butalbital classification
intermediate barbitaute
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butabarbital (Butisol®) classification
intermediate barbitaute
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talbutal (Lotusate®) classification
intermediate barbitaute
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aprobarbital (Alurate®) classification
intermediate barbitaute
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phenobarbital classification
long barbituate
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Barbituate 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
Potentiate glycine (another potentially inhibitory nerotransmitter)
Inhibit glutamate (excitatory neurotransmitter)
Causes reduced neuronal excitability
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What are the binding sites on the GABA-A receptor?
There are two a2, two B2, and one y2.
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a1 subunit effects
important for hypnotic effects. Z-drugs such as Zolpidem have high affinity for a1.
may be reponsible for anti-convulsant effects.
may be reponsible for anti-convulsant effects.
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a2 subunit effects
important for anti-anxiety effects.
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Chloral Hydrate
first depressant drug developed for the purpose of inducing sleep. rarely prescribed, replaced by z-drugs.
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Paraldehyde
relatively safe hypnotic
halitosis, 30% of dose excreted via lungs (causes bad breath)
anticonvulsant, doesn't suppress breathing at therapeutic doses
halitosis, 30% of dose excreted via lungs (causes bad breath)
anticonvulsant, doesn't suppress breathing at therapeutic doses
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Bromides (NaBr, KBr)
used in vetenary practice as anticonvulsant, but no longer used for patients due to toxicity
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Methaqualone
GABAR agonist
marketed as a non-barbituate sedative that is safe and non-addictive, but became schedule I drug due to addiction and overdose.
marketed as a non-barbituate sedative that is safe and non-addictive, but became schedule I drug due to addiction and overdose.
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Z-drugs
high afinity for a1 receptor on GABA-A
treats insomnia
fewer side effects that benzodiazepines
treats insomnia
fewer side effects that benzodiazepines
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3 primary groups of Z-drugs
Imidazopyrines
Cyclopyrrolones
Pyrazolopyrimidines
Cyclopyrrolones
Pyrazolopyrimidines
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Imidazopyrines example
Zolpidem (Ambien)
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Cyclopyrrolones example
zolpiclone, eszopiclone (Lunesta)
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Pyrazolopyrimidines example
zaleplon (Sonata)
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Anti Histamines MOA
H1 receptor invers agonist
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Anti Histamines examples
diphenhydramine (Benadryl)
doxylamine
pyrilamine
doxylamine
pyrilamine
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