benzodiazepines Flashcards

1
Q

trade name of midazolam

A

versed

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2
Q

how is midazolam supplied

A

5mg/mL

1mg/mL

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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

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4
Q

uses of midazolam

A

preoperative sedation
moderate sedation prior to iagnostic or radiographic procedures

ICU sedation
induction and maintenance of general anesthesia

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5
Q

what receptor does midazolam bind to?

A

GABA

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6
Q

where does midazolam work?

A

CNS
limbic system
reticular formation

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7
Q

what type of receptor is GABA

A

inhibitory

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8
Q

what ion is affected by midazolam?

A

Cl

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9
Q

what does the chloride shift due to midazolam result in?

A

hyperpolarization
less excitable state
stabilization

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10
Q

dose of midazolam IM

A

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

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11
Q

what is a typical IM dose of midazolam?

A

5 mg

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12
Q

IV dose of midazolam

A

0.01-0.03 mg/kg
q5 minues
to affect

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13
Q

max dose of IV midazolam

A

0.1-0.2 mg/kg

7 mg-14 mg for a 70 kg pt

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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

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15
Q

dose of maintenance of midazolam

A

0.05 mg/kg as needed

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16
Q

continuous infusion of midazolam dose

A
  1. 015-0.06 mg/kg/hour

0. 25-1 mcg/kg/minute

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17
Q

who gets oral midazolam

A

peds

oral, rectal, intranasal

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18
Q

onset of IM midazolam

A

~15 minutes

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19
Q

onset of IV midazolam

A

3-5 minutes

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20
Q

onset of of oral midazolam

A

10-20 minutes

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21
Q

onset of intranasal midazolam

A

4-8 minutes peds

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22
Q

peak of IM midazolam

A

0.5-1 hour

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23
Q

duration of IM midazolam

A

6 hours

mean 2 hours

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24
Q

IV single dose of midazolam duration

A

less than 2 hours

dose dependent

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25
Q

how long is midazolam’s duration with cirrhosis

A

6 hours

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26
Q

metabolism of midazolam

A

extensively hepatic

CYP3A4

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27
Q

how much of midazolam is transformed to its active metabolite

A

60-70%

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28
Q

what is midazolam’s active metabolite

A

1-hydrozymidazolam

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29
Q

half life or midazolam

A

2-6 hours

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30
Q

what conditions prolong midazolam’s half life

A
cirrhosis
CHF
obesity
renal failure- accumulation of active metabolites = prolonged sedation
elderly
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31
Q

excretion of IV midazolam

A

urine

32
Q

excretion of oral midazolam

A

urine 90%

feces 2-10 % over 5 days

33
Q

adverse reactions with midazolam Pulmonary

A

: Decreased tidal volumes and/or respiratory rate decrease
Apnea
cough

34
Q

adverse reactions with midazolam CV:

A

hypotension

35
Q

adverse reactions with midazolam CNS:

A

drowsiness, oversdeation, HA, seizure,

36
Q

adverse reactions with midazolam GI

A

N/V

37
Q

adverse reactions with midazolam MSK:

A

pain at injection site myoclonic jerks (infants)

38
Q

adverse reactions with midazolam misc.

A

Nystagmus

Dependence

Hiccups

Paradoxical reaction

39
Q

contraindications with midazolam

A

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
Q

trade name for diazepam

A

valium

41
Q

how is diazepam supplied

A

5mg/mL

42
Q

MOA for diazepam

A

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
Q

what drug does diazepam have the same MOA as?

A

midazolam and lorazipam

44
Q

uses of diazepam?

A

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
Q

dose of diazepam- anxiety

oral, IM IV

A

2-10 mg

2-4 times per day

46
Q

dose of diazepam- muscle spasm

IV IM

A

5-10 mg initially
5-10 mg in 3-4 hours
*if tetanus larger doses may be required

47
Q

dose of diazepam sedation

A

5-10 mg loading dose

48
Q

maintenance dose of diazepam sedation

A

0.03-0.1 mg/kg every 30 minutes to 6 hours

49
Q

dose of diazepam skeletal muscle relaxant

A

oral 2-20 3-4 times/day

50
Q

onset of diazepam

IV and oral

A

IV immediate

oral rapid

51
Q

duration of IV diazepam

A

20-30 minutes

52
Q

duration of oral diazepam

A

variable

53
Q

metabolism of diazepam

A

hepatic

54
Q

half-life elimination of diazepam

A

parent drug 20-50 hours in adults of

55
Q

what conditions increase half life of diazepam

A

INCREASED with neonates, elderly, hepatic disorders

56
Q

what is the major metabolite of diazepam? is it active? how long is the half-life

A

Major metabolite: active- desmethyldiazepam 50-100 hours

57
Q

peak of diazepam

A

oral 15 minutes to 2 hours

58
Q

adverse reactions with diazepam

A
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
Q

Contraindications with Diazepam

A

Hypersentivitity

MG

Resp Insufficiency

Severe hepatic insuff

Sleep apnea

Acute narrow-angle glaucoma

60
Q

trade name of lorazepam

A

ativan

61
Q

how is lorazepam supplied

A

2mg/mL

4mg/mL

62
Q

uses for lorazepam

A

Anxiety management

Short-term relief of anxiety

63
Q

MOA of lorazepam

A

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
Q

dose of lorazepam IM

A

0.05 mg/kg 2 hours before surgery

65
Q

max dose or IM lorazepam

A

4 mg

66
Q

dose of lorazepam IV

A

0.044 mg/kg 15-20 minutes before surgery

67
Q

what is the typical dose of IV lorazepam

A

2mg

68
Q

what is the max dose of IV lorazepam

A

4 mg

69
Q

how much should you not exceed of lorazepam in older than 50

A

2mg

70
Q

onset of lorazepam

A

2-3 minutes

71
Q

duration of lorazepam

A

8 hours

72
Q

metabolism of lorazepam

A

hepatic

rapid conjugation to inactive compounds

73
Q

half life elimination of lorazepam

A

14 hours adults
18 hours ESRD
42 hours neonates
18 hours 2-12 years

74
Q

peak of lorazepam

IM and oral

A

less than 3 hours IM

2 hours oral

75
Q

excretion of lorazepam

A

urine 88 %
predominately as inactive metabolites
feces 7 %

76
Q

adverse reaction with lorazepam

A

Hypotension

77
Q

contraindications with lorazepam

A

Hypersentivitity

Resp Insufficiency
*ok if vented

Sleep apnea

Acute narrow-angle glaucoma