Benzodiazapine and benzdiazapine like sedatives

Question 1

what is the MOA for Benzodiazepines

Answer 1

:Binds specific high-affinity sites on cell membranes of CNS neurons, adjacent to GABA sites -> enhances affinity of GABA receptors for circulating endogenous GABA
Binding of GABA keeps Cl- channels open -> cellular hyperpolarization

Question 2

Midazolam (versed)
class
MOA
SE
Char

Answer 2

Benzo

Bind benzo receptors in CNS to enhance GABA activity

Rebound insomnia + others

Must wean off

Question 3

Midazolam indications

Answer 3

Muscle relaxant
Management of aggressive, violent, delirious patients
Acute seizures
Moderate to severe insomnia
Inducing sedation & amnesia before medical procedures

Question 4

Diazapam
Class
Ind
MOA
Se
Char

Answer 4

Benzodiazepine

Anxiolytic
Sedative
Muscle relaxant
Seizure control

Bind benzo receptors in CNS to enhance GABA activity

Drowsiness, impaired mentation, tolerance, addiction, rebound insomnia

PO, IV
Rapidly absorbed PO
Metabolism: liver, active metabolites prolong duration of action
Withdrawal can be severe

Question 5

what is the MOA for benzo like sedatives

Answer 5

Increase GABA receptor affinity by interaction w/ receptors (neither Benzo nor Barb)

Question 6

Zolpidem/ambien

Class
Ind
MOA
SE
CHar

Answer 6

Short-acting non-benzodiazepine hypnotic

Insomnia (initiates sleep)

At high doses (10-20x):
Seizure control
Muscle relaxant

Potentiates GABA by binding GABA-A receptors at same location as Benzos

High doses: Hallucinations, amnesia

Short half-life
Works quickly

Question 7

Eszopiclone/lunesta

class
indications
MOA
Se
Char

Answer 7

Benzodiazepine-like hypnotic

Insomnia

Potentiation of GABA on Cl- channels by binding to specific receptor site not involved w/ binding of Benzos

Impaired mentation prior to sedation

Minimal SE profile, but also minimal efficacy

PO
Rapid onset (15-30 min)
No evidence for development of tolerance

Question 8

Ramelton/rozerem
Class
indication
Moa
SE

Answer 8

Melatonin receptor agonist

Insomnia

Mimics & enhances action of endogenous melatonin by binding MT1 & MT2 receptors

No anxiolytic, muscle relaxation, or amnesic effects (b/c doesn’t bind GABA-A)

Question 9

Flumazenil/romazicon
Class
Ind
MOA
SE
CHar

Answer 9

Benzo antagonist

Benzodiazepine overdose
A
ntagonizes benzodiazepine receptors

Dizziness, nausea, agitation

Rebound sedation 
Acute benzo withdrawal
Seizures 
Adverse cardiac effects
Death

IV
Rapid onset: 1-2 min
½ life: 1 hour – must give multiple doses (especially if OD on long-acting benzos)

CI: seizure hx, ingestion of add’l substances that may lower seizure threshold, tachycardia, wide QRS complex, anti-cholinergic signs, hx long-term benzo use