Benzodiazepines Flashcards

1
Q

benzos: 5 main pharmacological effects

A
anxiolysis
sedation
anterograde amnesia
anticonvulsant actions
muscle relaxation (spinal level)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what do we use benzos for the most

A

anxiolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

benzos and muscle relaxation

A

no muscle relaxation

do not affect muscle relaxant doses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

benzos and hepatic metabolism

A

do not induce hepatic metabolism

less potential for tolerance/abuse than barbs, opioids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

benzos and cerebrovascular response

A

preserves cerebrovascular response

greater margin of safety

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

benzos replaced what for premed/MAC cases

A

barbs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

benzos structure

A

benzene ring with 7 member diazepine ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

benzos mechanism of action

A

facilitate action of GABAa

increase affinity of GABAa to receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

do benzos mimic GABAa?

A

NO, does not directly activate GABAa receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what does increase of affinity of GABA mean?

A

open Cl channel
increase in Cl in cell
hyperpolarizes cel in post synapse

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

benzos are different in 3 ways

A

potency, lipid solubility, pharmacokinetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

in general, benzos are

A

highly lipid soluble, highly bound to albumin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

if pt is drunk, do you give benzos?

A

no, the ETOH is already binding to the GABAa receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

versed preparation, shape, potency, effect site equilibration time, hepatic effect, % protein bound, redistribution/duration time, elimination T1/2

A
water soluble
imidazole ring
2-3x more potent than diazepam
0.9-5.6 min effect site equilibration, increases with age
extensive first pass effect
90-98% protein bound
rapid redistribution, short duration
T1/2 = 1-6.5 hrs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

versed metabolism

A
extensive first pass effect
hydroxylation to water soluble compound
1,4 hydroxymidazolam
1 hydroxymidazolam is an active metabolite
conjugated, excreted in urine
renal failure does not affect midazolam
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

versed CNS efects

A

decrease CMRO2, drops CBF
does not produce isoelectric EEG
preserves cerebrovascular response to CO2
does not stop ICP response to laryngoscopy
anticonvulsant, amnesic
Rare paradoxical excitation

17
Q

versed respiratory effects

A

dose dependent decrease in ventilation
speed of injection makes a big difference
with opioids, hypoxemia, hypoventilation is enhanced
depress swallowing, upper airway activity

18
Q

versed cv effects

A

at induction, decreases SVR, BP
CO unchanged
doesn’t stop HR, BP changes with intubation

19
Q

versed doses

A

premed/peds: 0.25 - 0.5 mg/kg PO, max PO 20mg
IV sedation adults: 1-2.5 mg IV up to 5 mg
induction 0.1 - 0.2 mg/kg over 30-60 sec
maintenance - incremental, infusion

20
Q

valium solubility, viscosity, pH, injection technique, protein binding, PO absorption

A
lipid soluble
in organic solvents so hurts on injection
very viscous, pH 6.6-6.9
highly protein bound
rapidly absorbed in GI
21
Q

valium metabolism

A

oxidation: n-demethylation to:
desmethyldiazepam
oxazepam
temazepam in liver

22
Q

valium and metabolites

A

desmethyldiazepam further oxidized, so liver function will affect this

23
Q

cimetadine and liver function

A

inhibits CP450 system

24
Q

valium elimination T1/2

A

21-37 hrs, longer with age

demethyldiazepam 48-96 hrs

25
Q

valium pharmacodynamics

A

minimal changes in SVR, BP, CO (<20%)

otherwise similar to midazolam

26
Q

valium dosage

A

premed/oral: 10-15 mg
premed/IV 0.2 mg/kg (reduces MAC)
induction 0.5-1 mg/kg IV

27
Q

lorazepam potency, metabolites, T1/2, metabolism, solvent

A
5-10x more potent than diazepam
inactive metabolite
T1/2 10-20 hr
less influenced by changes in liver, age
propyl glycol solvent, so hurts
28
Q

lorazepam dosage

A

premed/PO 50 mcg/kg max 4 mg

29
Q

lorazepam anesthesia usefulness

A

slow onset, limited usefulness for us

~2hrs to peak plasms [ ]

30
Q

flumazenil (romazicon) derivative

A

imidazobenzodiazipine

high affinity for benzo specific receptors

31
Q

flumazenil duration

A

30-60 min, may need to repeat doses

32
Q

flumazenil dosage

A
  1. 2 mg IV initial, wait 2 minutes

0. 1 mg IV 60 sec intervals up to 3 mg

33
Q

flumazenil use

A
can be used for differential diagnosis
IV infusion 0.1-0.4 mg/hr
antagonizes depression of ventilation, sedation
 no acute anxiety
hepatic metabolism
renal excretion