Benzodiazepines

Benzodiazepines

promote the binding of GABA to the GABAa receptor

Benzodiazepines cause what?

- sedation/ hypnosis

- decrease anxiety

- anterograde amnesia

- anticonvulsants

- muscle relaxation

Benzodiazepines are used for ...

- anticonvulsants

- sleep

- anti-anxiety

Half-life of benzodiazepines used as anticonvulsants

long half-lifes and rapid entry into the CNS

Benzodiazepines are the primary treatment for what kinds of seizures?

status epilipeticus

Half-life of benzodiazepines used for sleep

short

Half-life of benzodiazepines used for anxiety

long

GABA A receptor

ligand gated ion channel that allows chloride flux into the neuron

Benzodiazepines allow

GABA to bind more efficiently

Benzodiazepines only bind to GABA A receptors that contain....

a1, a2, a3, a5

3 multiple choice options

Compounds that show selectivity for subtypes....

show an effect based on that type

Sedative/Hypnotic

a1

anxiolytic activity

- a2

- a5

Anticonvulsant

- a1

- a2

- a3

Muscle relaxation

tied up with all subtypes

Understand this chart dont memorize

Zolpidem Ambien absorption

rapid, delayed by food

Zolpidem onset

30 min

Zolpidem half-life

2.5 hours causes increase in liver disease

Zolpidem duration

6-8 hours

Zolpidem metabolism

3A4 to an inactive metabolite (no accumulation)

Zolpidem protein binding

high

Zolpidem ADR

amnesia

Zaleplon Sonata bioavailability

30%

Zaleplon metabolism

by aldehyde oxidase to an inactive metabolite, little CP450 involved

Zaleplon half-life

1 hour

Zaleplon duration

6-8 hours

Zaleplon protein binding

60%

Zaleplon ADR

amnesia

Eszopiclone Lunesta

S isomer of zopiclone

Eszopiclone protein binding

50%

Eszopiclone metabolism

3A4 and 2E1 to one active (desmethyl) and one inactive (N-oxide) metabolites

Eszopiclone half-life

6 hours

Eszopiclone ADR

- headache

- hallucinations

- anxiety

- amnesia

- unpleasant taste

Ramelteon Rozerem

best used for sleep onset, agonist at the melatonin receptors which control sleeo-wake cycle

Ramelteon onset

30 min

Ramelteon bioavailability

1.8%

Ramelteon metabolism

1A2, first pass converts to active metabolite

Ramelteon absorption

delayed by food

Ramelteon protein binding

82%

Ramelteon ADR

- HA

- depression

- worsened insomnia