86B sedative and hypnotics Flashcards
sedative vs hypnotic
sedative –> calming via reducing excitatory response to external stimuli
hypnotic –> drowsiness and sleep
**low dose - calm; high dose - sleep (continuum)
extremely high dose –> coma and death
primary target of sedative-hypnotics
GABAa receptor (ligand-gated chloride channel)
Benzodiazepine target
BDZ1/2 on gama-subunit of GABAa receptor
Meds that bind GABA receptors
General anethetics
Ethanol
Barbiturates
Benxodiazepines
benzodiazepines ending
_zepam (2 N) and _zolam (3 N)
benzodiazepine mechanism of action
- increases Cl channel opening frequency
- requires GABA to open though
General anesthetics mechanism of action of GABA
ex: propofol, etomidate
increase duration of Cl opening (higher doses work without GABA)
Barbiturates mechanism of action on GABA
Increase duration of Cl opening (higher doses work without GABA)
GABA antagonists
**Act as convulsants
Picrotoxin (non-competitive)
Penicillin (blocks open channels - needs agonist)
Bicuculline (competitive antagonists)
benzodiazepines vs bariturates at high doses
benzodiazepines (_zepams) have a ceiling effective (don’t go to coma/death at high doses)
benzodiazepine structure
7 member ring with 2 N; 2 benzenes attached
clinical uses of benzodiazepines
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