16.4
Sedatives belong to a class of drugs that calms the individual, while hypnotics induce and maintain sleep. Both categories work by slowing down the brain activity.
Sedative-hypnotic drugs suppress the CNS activity in a dose-dependent manner. Older medications like barbiturates follow a linear curve, making them potentially fatal. Newer drugs like benzodiazepines deviate from the linear curve, making them useful for short-term relief.
Sedative-hypnotic drugs primarily target GABAA ligand-gated ion channels and melatonin GPCRs.
Neurotransmitter GABA binds and opens the GABAA ion channel, allowing chloride ion influx, decreasing the resting potential and, in turn, inhibiting neuronal firing.
Barbiturates, benzodiazepines, and newer agents like zolpidem bind at different allosteric sites on the GABAA channel, promoting GABA binding and neuronal suppression.
In addition, melatonin activates MT1 and MT2 GPCRs in the anterior hypothalamus, decreasing neuronal firing and promoting sleep. Melatonin analogs, such as ramelteon, are helpful for insomnia without any dependency risk.
Sedativa zijn medicijnen die angst verlichten, terwijl hypnotica slaap opwekken. Beide soorten medicatie onderdrukken neuronale activiteit, wat leidt…
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