Benzodiazepines
Mechanism
- Positive allosteric modulators at the GABA-A receptor - bind the alpha/gamma interface
- inc FREQUENCY of chloride channel opening (barbiturates inc DURATION - hence barbiturates have no ceiling and are far more lethal)
- Require endogenous GABA -> ceiling effect -> relatively safe in isolated overdose
- Effects: anxiolysis, sedation, hypnosis, anterograde amnesia, anticonvulsant, muscle relaxation
- Subunit specificity: alpha1 -> sedation/amnesia; alpha2/3 -> anxiolysis/myorelaxation
- "Z-drugs" (zolpidem, zopiclone) are alpha1-selective non-benzodiazepines - same receptor, same risks
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