benzodiazepines Flashcards

1
Q

trade name of midazolam

A

versed

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

how is midazolam supplied

A

5mg/mL

1mg/mL

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

MOA of midazolam

A

binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system
limbic system
reticular formation
enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions
this shift in chloride ions results in hyper polarization (less excitable state)
stabilization

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

uses of midazolam

A

preoperative sedation
moderate sedation prior to iagnostic or radiographic procedures

ICU sedation
induction and maintenance of general anesthesia

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

what receptor does midazolam bind to?

A

GABA

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

where does midazolam work?

A

CNS
limbic system
reticular formation

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

what type of receptor is GABA

A

inhibitory

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

what ion is affected by midazolam?

A

Cl

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

what does the chloride shift due to midazolam result in?

A

hyperpolarization
less excitable state
stabilization

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

dose of midazolam IM

A

0.07 - 0.08 mg/kg 30-60 minues prior to surgery

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

what is a typical IM dose of midazolam?

A

5 mg

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

IV dose of midazolam

A

0.01-0.03 mg/kg
q5 minues
to affect

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

max dose of IV midazolam

A

0.1-0.2 mg/kg

7 mg-14 mg for a 70 kg pt

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

how is dosage affected for midazolam if the patient is unpremeditated vs. premedicated

A

premeditated dose much smaller
pre- 0.05-0.2
non-pre 0.3-0.35 mg/kg

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

dose of maintenance of midazolam

A

0.05 mg/kg as needed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

continuous infusion of midazolam dose

A
  1. 015-0.06 mg/kg/hour

0. 25-1 mcg/kg/minute

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

who gets oral midazolam

A

peds

oral, rectal, intranasal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

onset of IM midazolam

A

~15 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

onset of IV midazolam

A

3-5 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

onset of of oral midazolam

A

10-20 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

onset of intranasal midazolam

A

4-8 minutes peds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

peak of IM midazolam

A

0.5-1 hour

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

duration of IM midazolam

A

6 hours

mean 2 hours

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

IV single dose of midazolam duration

A

less than 2 hours

dose dependent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
how long is midazolam's duration with cirrhosis
6 hours
26
metabolism of midazolam
extensively hepatic | CYP3A4
27
how much of midazolam is transformed to its active metabolite
60-70%
28
what is midazolam's active metabolite
1-hydrozymidazolam
29
half life or midazolam
2-6 hours
30
what conditions prolong midazolam's half life
``` cirrhosis CHF obesity renal failure- accumulation of active metabolites = prolonged sedation elderly ```
31
excretion of IV midazolam
urine
32
excretion of oral midazolam
urine 90% | feces 2-10 % over 5 days
33
adverse reactions with midazolam Pulmonary
: Decreased tidal volumes and/or respiratory rate decrease Apnea cough
34
adverse reactions with midazolam CV:
hypotension
35
adverse reactions with midazolam CNS:
drowsiness, oversdeation, HA, seizure,
36
adverse reactions with midazolam GI
N/V
37
adverse reactions with midazolam MSK:
pain at injection site myoclonic jerks (infants)
38
adverse reactions with midazolam misc.
Nystagmus Dependence Hiccups Paradoxical reaction
39
contraindications with midazolam
Hypersentivitity NO intrathecal or epidural of parenteral forms containing preservatives- benzyl alcohol Acute narrow-angle glaucoma Concurrent use of potent inhibitors of CYP3A4 (amprenavir, atazanavir, ritonavir)
40
trade name for diazepam
valium
41
how is diazepam supplied
5mg/mL
42
MOA for diazepam
Binds to stereospecific benzodiazepine receptors on the post-synaptic GABA neuron at several sites within the central nervous system Including the limbic system reticular formation Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions The shift of chloride ions results in hyperpolarization (LESS excitable state) and stabilization
43
what drug does diazepam have the same MOA as?
midazolam and lorazipam
44
uses of diazepam?
Anxiety disorders ETOH withdrawal Skeletal muscle relaxant Convulsant disorders Pre-opertive sedation Moderate sedation for procedures or radiographic procedures ICU sedation *same MOA as Midazolam
45
dose of diazepam- anxiety | oral, IM IV
2-10 mg | 2-4 times per day
46
dose of diazepam- muscle spasm | IV IM
5-10 mg initially 5-10 mg in 3-4 hours *if tetanus larger doses may be required
47
dose of diazepam sedation
5-10 mg loading dose
48
maintenance dose of diazepam sedation
0.03-0.1 mg/kg every 30 minutes to 6 hours
49
dose of diazepam skeletal muscle relaxant
oral 2-20 3-4 times/day
50
onset of diazepam | IV and oral
IV immediate | oral rapid
51
duration of IV diazepam
20-30 minutes
52
duration of oral diazepam
variable
53
metabolism of diazepam
hepatic
54
half-life elimination of diazepam
parent drug 20-50 hours in adults of
55
what conditions increase half life of diazepam
INCREASED with neonates, elderly, hepatic disorders
56
what is the major metabolite of diazepam? is it active? how long is the half-life
Major metabolite: active- desmethyldiazepam 50-100 hours
57
peak of diazepam
oral 15 minutes to 2 hours
58
adverse reactions with diazepam
``` MANY Hypotension, Vasodilation Amnesia, Ataxia, Confusion, Depression Drowsiness, Fatigue Headache, Slurred speech, Vertigo Paradoxical reactions ``` Rash, Jaundice, Phlebitis, Pain at injection Constipation, Diarrhea, Nausea Salivation changes Incontinence, Urinary retention Dysarthria, Tremor, Weakness, Diplopia Apnea, Asthma, Decreased RR
59
Contraindications with Diazepam
Hypersentivitity MG Resp Insufficiency Severe hepatic insuff Sleep apnea Acute narrow-angle glaucoma
60
trade name of lorazepam
ativan
61
how is lorazepam supplied
2mg/mL | 4mg/mL
62
uses for lorazepam
Anxiety management Short-term relief of anxiety
63
MOA of lorazepam
Binds to stereospecific benzodiazepine receptors on the post-synaptic GABA neuron at several sites within the central nervous system Including the limbic system reticular formation Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions The shift of chloride ions results in hyperpolarization (LESS excitable state) and stabilization
64
dose of lorazepam IM
0.05 mg/kg 2 hours before surgery
65
max dose or IM lorazepam
4 mg
66
dose of lorazepam IV
0.044 mg/kg 15-20 minutes before surgery
67
what is the typical dose of IV lorazepam
2mg
68
what is the max dose of IV lorazepam
4 mg
69
how much should you not exceed of lorazepam in older than 50
2mg
70
onset of lorazepam
2-3 minutes
71
duration of lorazepam
8 hours
72
metabolism of lorazepam
hepatic | rapid conjugation to inactive compounds
73
half life elimination of lorazepam
14 hours adults 18 hours ESRD 42 hours neonates 18 hours 2-12 years
74
peak of lorazepam | IM and oral
less than 3 hours IM | 2 hours oral
75
excretion of lorazepam
urine 88 % predominately as inactive metabolites feces 7 %
76
adverse reaction with lorazepam
Hypotension
77
contraindications with lorazepam
Hypersentivitity Resp Insufficiency *ok if vented Sleep apnea Acute narrow-angle glaucoma