Benzodiazepines

Question 1

Midazolam (Versed)

Drug Class
&
MOA

Answer 1

Benzodiazepine

Binds to BZD site between subunits α₁ & γ₂ of GABA_A receptor

Increases affinity of GABA to receptor & enhancing opening of Cl^- channels resulting in IPSP

Question 2

Midazolam (Versed)

Sedation Dose

Adult

Answer 2

IV: 1-5 mg

Question 3

Midazolam (Versed)

Sedation Dose

Pediatric

Answer 3

PO: 0.25-0.5 mg/kg

Question 4

Midazolam (Versed)

Induction Dose

Answer 4

IV: 0.1-0.2 mg

Over 30-60 sec

Question 5

Midazolam (Versed)

Onset
Peak
Duration
Half-life

Answer 5

Onset
IV: 1-2 min

Peak
IV: 5 min

Duration
IV: 5-10 min

Half-life
2 hrs

Question 6

Midazolam (Versed)

Metabolism & Elimination

Answer 6

Metabolism
Hepatic: CYP3A4

Elimination
Kidneys

Active Metabolite
1-hydroxymidazolam

Question 7

Midazolam (Versed)

Side Effects

Answer 7

CNS
↓ CMRO2, ↓ CBF

Respiratory
↓ in ventilation
↓ hypoxic drive

Cardiovascular
↓ BP ↑ HR

Question 8

Diazepam (Valium)

Drug Class
&
MOA

Answer 8

Benzodiazepine

Binds to BZD site between subunits α₁ & γ₂ of GABA_A receptor

Increases affinity of GABA to receptor & enhancing opening of Cl^- channels resulting in IPSP

Question 9

Diazepam (Valium)

Induction Dose

Answer 9

IV: 0.5-1 mg/kg

Question 10

Diazepam (Valium)

Anti-convulsant Dose

Answer 10

IV: 0.1 mg/kg

Question 11

Diazepam (Valium)

Onset
Peak
Duration
Half-life

Answer 11

Onset
IV: 1-5 min

Peak
IV: 15 min

Duration
IV: 15-30 min

Half-life
20-40 hrs

Question 12

Diazepam (Valium)

Metabolism & Elimination

Answer 12

Metabolism
Hepatic: CYP3A4

Elimination
Kidneys

Active Metabolite
Desmethyldiazepam & oxazepam

Question 13

Diazepam (Valium)

Side Effects

Answer 13

CNS
Potent anti-convulsant
Can produce isoelectric EEG
Return to drowsiness within 6-8 hrs d/t active metabolite

Respiratory
Slight ↓ in ventilation

Cardiovascular
Min ↓ in BP, CO, & SVR

Pain on injection site d/t propylene glycol

Question 14

Lorazepam (Ativan)

Drug Class
&
MOA

Answer 14

Benzodiazepine

Binds to BZD site between subunits α₁ & γ₂ of GABA_A receptor

Increases affinity of GABA to receptor & enhancing opening of Cl^- channels resulting in IPSP

Question 15

Lorazepam (Ativan)

Sedation Dose

Answer 15

IV: 1-4 mg

Question 16

Lorazepam (Ativan)

Onset
Peak
Duration
Half-life

Answer 16

Onset
IV: 1-2 min

Peak
IV: 20-30 min

Duration
IV: 6-10 hrs

Half-life
14 hrs

Question 17

Lorazepam (Ativan)

Metabolism & Elimination

Answer 17

Metabolism
Hepatic: Conjugated to inactive metabolites

Question 18

Flumazenil (Romazicon)

Drug Class
&
MOA

Answer 18

Benzodiazepine reversal agent

Competitive antagonist to BZD site
of GABAA receptor

Prevents/reverses all agonist activity of BZD

Question 19

Flumazenil (Romazicon)

Dosing

Answer 19

IV: 0.2 mg; followed by 0.1 mg q 1 min Titrated to Effect

Sedation Reversal: 0.3-0.6 mg

COMPLETE Reversal: 0.5-1 mg

Question 20

Flumazenil (Romizicon)

Onset
Duration

Answer 20

Onset
IV: 1-2 min

Duration
IV: 30-60 min

Question 21

Flumazenil (Romazicon)

Metabolism & Elimination

Answer 21

Metabolism
Hepatic: CYP450 to inactive metabolites

Question 22

Flumazenil (Romazicon)

Contraindication

Answer 22

Contraindicated with anti-epileptic drugs