Benzodiazepine

Question 1

All Benzos are great for: (5)

Answer 1

Anxiolysis 
Sedation
Anterograde Amnesia 
Anticonvulsant 
Muscle Relaxation (spinal level)

Question 2

MOA: Benzos

Answer 2

Mechanism of action:
Benzos work by increasing the affinity of the GabaA receptor for GABA.

They do not activate GABA.

Question 3

Structure of Benzos

Answer 3

Benzene ring fused with

7 member diazpine ring

Question 4

In general, Benzos are

_______ lipid soluble
_______ protein bound

Answer 4

HIGHLY lipid soluble and

HIGHLY protein bound

Question 5

short duration in versed is attributed to

Answer 5

HIGH LIPOPHILICITY, it redistributes, effect goes down.

Question 6

Effect site equilibration time of versed

Answer 6

0.9 - 5.6 minutes

Question 7

Midazolam: active metabolites

Answer 7

1. = 1-hydroxy-midazolam

Question 8

1-hydroxy-midazolam + kidneys

Answer 8

active metabolite of versed

may build in up in patients with renal insufficiency if on high doses of continuous IV versed

Question 9

metabolism of versed is slowed with medications:

Answer 9

cimetidine, erythryomycine, calcium channel blockers, anti fungal drugs,)

Question 10

Benzos + EEGs

Answer 10

Benzos are not potent enough to produce a flat line EEG

Question 11

Benzos + swallowing reflex

Answer 11

will reflex decrease swallowing reflex, can’t cough properly.

Question 12

Benzodiazepines + opiods

Answer 12

analgesic effects of opioids are reduced with Benzos

hypo ventilatory and hypoxemia synergistic effect with benzos

Question 13

CV effects of midazolam

Answer 13

decreased SVR at induction dose

BP consequently decreases

CO unchanged.

Doesn’t prevent hR/BP changes with intubation

Question 14

DOSES FOR VERSED

Answer 14

premedication/pediatrics: 0.25-.5 mg/kg PO
Max PO dose for peds: 20 mg

IV sedation/adults: 1 - 2.5 mg IV can give as high as 5 mg PRN

Induction dose: 0.1 -0.2 mg /kg over 30 - 60 sec

Maintenance: incremental or infusion

Question 15

Diazepam: CV effects

Answer 15

minimal changes in SVR, CO, BP, <20%.

Good for CV patients

Question 16

Diazepam is differentiated by

Answer 16

its prolonged duration of action , e1/2 t = 21-37 hours

Question 17

Diazepam metabolites:

Answer 17

3!
desmethyldiazepam = active
oxazepam/temazepam = NA

Question 18

Diazepam is rapidly absorbed from

Answer 18

GI tract

less first pass effect than versed

Question 19

desmethyldiazepam

Answer 19

active metabaolite

e1/2 time = 48 - 96 hrs

Question 20

Diazepam doses:

Answer 20

pre-medicaiton/oral: 10-15 mg
pre-medicaition/IV: 0.2 mg/kg (reduces MAC)
induction: 0.5 - 1 mg/kg IV
anticonvulsant: inhibit activity in hippocampus & limbic system; 0.1 mg/kg IV

Question 21

metabolism of diazepam is affected by

Answer 21

drugs that inhibit CYP450 i.e. cimetidine

metabolism will be slowed.

Question 22

flumazenil (romazicon) MOA:

Answer 22

competitive antagonist for benzo binding site, has high affinity, can knock Benzos off

Question 23

lorazepam: notable attribuets

Answer 23

5-10x potency of diazepam
metabolites are pharmacologically inactive
SLOW onset, peaks at 2 hours [[peak plasma]]

Question 24

Doses of lorazepam:

Answer 24

premedication/PO: 50 mcg/kg

Max dose: 4 mg

Question 25

flumazenil DOA:

Answer 25

30- 60 minutes.

Question 26

Flumazenil peaks in:

Answer 26

2 minutes. Must wake 2 minutes before next dose

Question 27

Flumazenil dose:

Answer 27

0.2 mg IV initial
repeat dose : 0.1 mg IV

MAX DOSE: 3 mg in 24 hr period

infusion: 0.1 - 0.4 mg/hr
0. 5 - 1 mc/kg/min

Question 28

In differential diagnosis of coma can give up flumazenil up to

Answer 28

5 mg

Question 29

comparative elimination half times for benzos

Answer 29

midazolam < lorazepam < diazapam