Sedatives & Hypnotics (Exam 1)

Question 1

Benzos General Effects

Answer 1

No tolerance
-Inhibition of platelet aggregation (In vitro)
-Anterograde Amnesia
-Highly plasma protein bound; highly lipid soluble
-Less CYP450 inhibition than Barbiturates

Question 2

Benzos General Uses

Answer 2

1. Anxiolytics
2. Sedation
3. Anticonvulsant
4. Skeletal Muscle Relaxation
5. Anterograde Amnesia

Question 3

Benzos Drug interaction

Answer 3

Calcium Channel Blockers
Antifungals
Cimetidine
*Fentanyl
Erythromycin

ACE FC

Question 4

Benzos MOA

Answer 4

Indirect mediator of GABA (Binds to BZE receptor on GABA, enhancing GABA site, allowing Chloride to flood through channel)

Question 5

Midazolam (Versed): Sedation

Answer 5

Peds PO: 0.25 - 0.5 mg/kg
(syrup so peak effect is 20-30 min)

Adults IV: 1 - 5 mg
***decrease dose in elderly, greater CNS sensitvity”

Question 6

Midazolam (Versed): Induction

Answer 6

IV : 0.1 - 0.2 mg/kg over 30 - 60 sec
(Give after Fentanyl 50-100 mcg 1 - 3 mins prior)

Question 7

Midazolam (Versed): Onset

Answer 7

1-2 min

Question 8

Midazolam (Versed): Peak for Children and Adults

Answer 8

Peds PO: 20-30 min (syrup)

Adults: 5 mins

Question 9

Midazolam (Versed): E 1/2 Time

Answer 9

2 hrs (SHORT)

***double in elderly d/t ↓ hepatic flow

Question 10

Midazolam (Versed): Metabolism

Answer 10

-Cyp3A4

-Active metabolites:
1-hydroxymidazolam
(1/2 activity of par3ent molecule)

-Active metabolites are conjugated and excreted by kidneys:
5X faster than Lorazepam, 10X than Diazepam

Question 11

Midazolam (Versed): Other

Answer 11

-Used primarily as pre-op med and conscious sedation

-2-3 x as potent as valium

-Amnesia lasts longer than sedation effects

Question 12

Diazepam (Valium): Induction

Answer 12

IV: 0.5 - 1 mg/kg
(Decrease 25-50% in elderly, liver dx, alcoholics, or w/ opioids)

Question 13

Diazepam (Valium): Onset

Answer 13

1-5 mins

Question 14

Diazepam (Valium): Peak

Answer 14

Peds: 15 -30 mins

Adults: 1 hr

Question 15

Diazepam (Valium): E 1/2 Time

Answer 15

20 - 40 hrs
(Extensively protein bound)

Question 16

Diazepam (Valium): Metabolism

Answer 16

-CYP 3A4

-Dissociates from GABAa Receptor faster than Lorazepam

-Desmethyldiazepam: 48-96 Hrs.
(**Causes return of drowsiness 6-8 hrs later)
-Oxazepam

-Metabolites excreted by kidneys:
10X slower than Midazolam

Question 17

Diazepam (Valium): Systems Effects

Answer 17

CNS: Can produce Isoelectric EEG

Resp: Minimal effect on ventilation

CV: Less effect on CV than Versed

Good for COPD

Question 18

Diazepam (Valium): Other

Answer 18

-Rarely used in anesthesia b/c versed is much more beneficial with quick on and off effects

Question 19

Lorazepam (Ativan): Sedation

Answer 19

Dose: 1-4 mg IV POST OP SEDATION

Question 20

Lorazepam (Ativan): Onset

Answer 20

-Slower than other BZDs d/t lower lipid solubility, takes longer to enter CNS
-Slower metabolic clearance

Question 21

Lorazepam (Ativan): Peak

Answer 21

IV: 20 - 30 mins

Question 22

Lorazepam (Ativan): E 1/2 Time

Answer 22

14 hrs

Question 23

Lorazepam (Ativan): Metabolism

Answer 23

-Metabolized to inactive metabolites
-Metabolic clearance:
5X slower than Midazolam”

Question 24

Lorazepam (Ativan): Other

Answer 24

-More Potent Sedative than amnestic compared to versed and valium
-Slower onset of action than versed and valium (30 minutes compared to (1-5 minutes). SO not much implication in anesthesia.