Sedative-Hypnotic Drugs
Benzodiazepines:
 - Bind ...
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Description

Sedative-Hypnotic Drugs

Benzodiazepines:

 - Bind to specific GABAA receptor subunits at central nervous system (CNS) neuronal synapses facilitating GABA-mediated chloride ion channel opening frequency • enhance membrane hyperpolarization 

 - Dose-dependent depressant effects on the CNS including sedation and relief of anxiety • amnesia • hypnosis • anesthesia • coma • and respiratory depression

Barbituates:

 - Bind to specific GABA-A receptor subunits at CNS neuronal synapses facilitating GABA-mediated chloride ion channel duration • enhance membrane hyperpolarization

 - Dose-dependent depressant effects on the CNS including sedation and relief of anxiety • amnesia • hypnosis • anesthesia • coma and respiratory depression • dose-response relationship than

Newer Hyponotics:

 - Bind selectively to a subgroup of GABAA receptors, acting like benzodiazepines to enhance membrane hyperpolarization

 - Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence

Melatonin Receptor Antagonists:

 - Activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS

 - Rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms

Orexin Antagonists:

 - Blocks binding of orexins, neuropeptides that promote wakefulness 

 - Promotes sleep onset and duration

5-HT-Receptor Agonist:

Mechanism uncertain:

 - Partial agonist at 5-HT receptors but affinity for receptors also possible

 - Slow onset (1-2 weeks) of anxiolytic effects • minimal psychomotor impairment—no additive CNS depression with sedative-hypnotic drugs



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