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Flashcards in BZDs Deck (13):
1

Why are benzos much safer than barbiturates/alcohol?

Barbs/alcohol - if you keep ingesting effect/toxicity is linear until coma/death
Benzos - Caps at the anesthesia effect - ceiling effect (at normal doses)

2

BZD Structure-Activity Relationships

Ring A - aromatic (part of binding site) - C7 EWG (good) - any other position (bad)
Ring B - N1 + methyl = good but not necessary; C2 - proton acceptors (good); C3 OH - faster elimination
Ring C - not necessary, but EWG is ortho - good, para - BAD

3

BZD MOA

Bind to BZD receptor (between alpha and gamma) on GABAa receptor (Cl- channel) - allosteric
GABA must bind between alpha and beta subunits to open Cl- channel (hyper polarization)
Shifts GABA dose-response curve to the left (less GABA needed to achieve anesthetic effect

4

Why do BZDs have different effects?

Hit different receptors due to different GABA receptors!!!
Antiseizure, muscle relaxer, etc
Binds His AA in alpha subunit

5

BZ1

Sedation, amnesia, (anti-seizure)
Ambien, Lunesta, and Sonata - selective!

6

BZ2/3

Anxiolytic, muscle relaxer

7

BZD Antagonists

Flumazenil

8

Barb Binding to GABA Receptor

Different site, but increase duration of hyper polarization - shift dose-response curve further left than BZDs

9

Diazepam AD

Quick/complete absorption
High Vd

10

Lorazepam AD

Lower Vd, slower onset - longer duration

11

BZD ME

P450 and glucuronidation to urinary excretion

12

Uses of BZDs

Antianxiety/sedative
Amnesia - procedures
Hypnosis - insomnia
Anesthesia
Antiseizure
Muscle relaxer
Alcohol withdrawal

13

AEs of BZDs

Respiratory/cardiac depression
Teratogen (1st trimester)
Abuse
D/C syndrome