Know this Insomnia Flashcards
Dose-Response Curves – Barbiturates vs Benzodiazepines
Anterograde amnesia= both
NO anesthesia w/BDZs
GABA binds to receptor –> opens Cl channel –> ↓ Em –> ↓ excitability
GABA binds to receptor –> opens Cl channel –> ↓ Em –> ↓ excitability
BDZs bind to site on α subunit [α1 and α2-5] intensifying the action of GABA
Presence of GABA required for BDZ effect
BARBs bind to distinct site on channel
Low dose: action similar to BDZs
Higher doses: direct interaction with channel – NO GABA required - plus inhibition of excitatory NTs
Ethanol
binds both specifically and non-specifically at distinct sites –> action similar to barbiturates
“Z”-drugs (structurally distinct from BDZs) bind to same site as BDZs [only _____] - same action
α1
Flumazenil - antagonist that binds to same site as BDZs and “Z”-drugs
Used in treatment of benzodiazepine overdose toxicity
NOT effective for BARB or ethanol toxicity
BDZs ______________ in presence of GABA only
enhance channel opening
BARBs prolong channel opening in presence of GABA and at higher doses open channel ______
directly
antagonist that binds to same site as BDZs and “Z”-drugs
Used in treatment of benzodiazepine overdose toxicity
NOT effective for BARB or ethanol toxicity
Flumazenil
α1 actions
BDZs
“Z-Drugs”
Sleep
Anticonvulsant*
Amnesia
Additive CNS Depression
α2-α5 actions
BDZs
Anxiolytic
Myorelaxant
Motor Incoordination
Tolerance
Dependence
Addiction
↓ REM
BDZ Primary Use Insomnia
Flurazepam
Temazapam
Triazolam
Primary Anx BDZ
Lorazepam
Alprazolam
Diazepam
to name a few
BDZ ↓ N3 and rem after
1 week of use
