Benzodiazepines and Flumazenil

Question 1

Benzodiazepine Class

Answer 1

Hypnotic

Question 2

Benzodiazepine Uses (5)

Answer 2

Sedative

Anxiolytic

Amnesiac (Provides anterograde amnesia, not retrograde amnesia)

Anticonvulsant (increases seizure threshold)

Muscle relaxant

Question 3

Benzodiazepine MOA

Answer 3

Enhances the response to the GABA A receptor

Question 4

Benzodiazepine IV Additive

Answer 4

Propylene glycol is added to diazepam and lorazepam to enhance water solubility.

Propylene glycol can cause venous irritation

Midazolam does not require propylene glycol , because it contains an imidazole ring

Question 5

Benzodiazepine DOA from Shortest to Longest

Answer 5

DOA: midazolam < lorazepam < diazepam

Question 6

Benzodiazepine Potency from Most to Lease

Answer 6

Potency: Lorazepam > midazolam > diazepam

Question 7

Benzodiazepine Distribution

Answer 7

Highly protein bound

Question 8

Benzodiazepine Metabolism

Answer 8

Metabolized by the liver

Question 9

Benzodiazepine Excretion

Answer 9

Excreted by the kidneys

Question 10

Midazolam Dosing (2)

Answer 10

Premed:
Titrated 0.5-2 mg IV (adult)
.2-.6 mg/kg PO

Induction dose: 0.1 - 0.3 mg/kg

Question 11

Midazolam Onset, Peak, and Duration

Answer 11

Onset: 1 minute
Peak: 2 – 5 minutes
DOA: 6-15 minutes

Question 12

Midazolam Distribution

Answer 12

Highly protein bound (95%)

Question 13

Midazolam Metabolism

Answer 13

Metabolized by the CYP 450 system in the liver

Active metabolite: 1-hydroxymidazolam

Question 14

Midazolam Excretion

Answer 14

Excreted by the kidneys

Question 15

Midazolam Precautions

Answer 15

May be related to post operative delirium in the elderly

Question 16

Midazolam CV Effects (2)

Answer 16

Sedation dose: Minimal effects

Induction dose: decrease BP and decrease SVR

Question 17

Midazolam Respiratory Effects (3)

Answer 17

Reduce muscular tone in upper airway

Decrease CO2 and hypoxia response

Patients with COPD are more sensitive depressant effects

Question 18

Midazolam CNS Effects (5)

Answer 18

Anterograde amnesia

Anticonvulsant

Anxiolysis

Antispasmodic

No analgesia

Question 19

Flumazenil Class

Answer 19

Competitive antagonist of Benzodiazepines (GABAa)

Question 20

Flumazenil Metabolism (dosing consideration)

Answer 20

Short half life – risk for rebound effect

Question 21

Flumazenil Dosing

Answer 21

Initial dose is 0.2 mg IV and titrated in 0.1 mg increments to prevent rebound effect

Question 22

Flumazenil Onset and DOA

Answer 22

Onset: 1-3 minutes

DOA: 3 – 30 minutes

Question 23

Flumazenil Precautions (2)

Answer 23

Caution for those on chronic benzodiazepines, may cause acute withdraw

Rebound Effect of Benzodiazepines