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Pharm 2 (3rd Quarter) > Benzos > Flashcards

Benzos Flashcards

1
Q

Benzodiazepines are drugs with ___________ rings fused to ________ rain

A

Benzene

Diazepine

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2
Q

Where midazolam gets its name

A

Imidazole ring

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3
Q

At what pH is midazolam water soluble?

A

Yes at pH less than 4

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4
Q

At pH less than 4 what occurs with imidazole ring on midazolam to make it water soluble

A

Ring opens up

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5
Q

Midazolam pKa

A

6.1. Means at pH 6.1 1/2 ionized 1/2 non ionized

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6
Q

Diazepam pKa

A

3.4

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7
Q

____________ resembles the diazepam metabolize oxazepam

A

Lorazepam

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8
Q

6 reasons benzos and propofol have replaced barbs

A 
Less tolerance
Less abuse potential
Less addiction potential
Greater safety margin
Fewer drug reactions
NO induction of hepatic microsomal enzymes
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9
Q

Best use of benzos

A

Peds pre-op

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10
Q

Midazolam compared to Valium

A

More rapid onset

Greater amnesia

Less post-op sedation

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11
Q

5 benzodiazepine uses

A

Sedation

Anxiolytics

Anticonvulsant

Skeletal muscle relaxant

Amnesia

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12
Q

Midazolam dose

IV

PO

IM

A

IV
50-75mcg/kg peds
1-5 mg adult

PO
0.5-1 mg/kg peds MAX 20mg

0.5-1 mg/kg IM

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13
Q

Midazolam induction dose

A

0.1-0.2 mg/kg IV over 30-60seconds

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14
Q

Decrease doses of midazolam if

A

Induction if opioids used

Elderly

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15
Q

Diazepam cardiac induction dose

A

0.2-0.5mg/kg

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16
Q

Diazepam sedation dosage

A

1-2mg increments

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17
Q

Lorazepam preop dose

1-4 mg gives anterograde amnesia for up to _____ hours

A

50 mcg/kg

6 hours

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18
Q

Benzodiazepine metabolism 2 pathways

A

Glucuronidation

Hepatic microsomal enzyme metabolism

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19
Q

Glucuronidation is exclusive

A

Lorazepam, oxazepam, temazepam

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20
Q

Glucuronidation benzos metabolites

Active/inactive

A

No active metabolites

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21
Q

Hepatic microsomal enzyme metabolism active/inactive metabolites with diazepam

A

Active

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22
Q

Hepatic metabolism of diazepam leaves ______

A

Temazepam

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23
Q

Elimination 1/2 time midazolam

A

1-4 hours

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24
Q

Vd of midazolam is equal to that of diazepam due to

A

Similar lipid solubility and high protein binding

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25
Greater Vd of elderly and obesity of midazolam due to
Increased peripheral distribution resulting in prolonged duration of action
26
Only benzo used for infusion
Midazolam
27
Midazolam is hydroxylated via
Cytochrome P450
28
Midazolam is excreted in _______ as _______
Urine as glucuronidation conjugates
29
Diazepam Vd is large why??
Highly lipophillic taken into fat tissue
30
Diazepam and placental barrier
Crosses
31
Diazepam protein binding
Parallels lipid solubility
32
3 conditions decreasing diazepam protein binding resulting in exaggerated effects
Cirrhosis ESRD Hypoalbuminemia
33
OD treatment of diazepam
Flumazenil
34
Hemodialysis is not effective for diazepam OD Why?
Bc too highly protein bound
35
Diazepam is metabolized by _______ using _______
Hepatic microsomal enzymes Oxidative pathways
36
2 principle metabolites of diazepam Which more potent
Demethyldiazepam. (Most potent) Oxazepam
37
What causes second wave of sedation 6-8 hours after diazepam administration
Desmethyldiazepam
38
Diazepam elimination 1/2 time
21-37 hours
39
Desmethyldiazepam elimination 1/2 time
48-96 hours
40
Lorazepam is conjugated via _________ to _______
Glucuronic acid to INACTIVE metabolites
41
Elimination 1/2 time of lorazepam
10-20 hours. But clinical effects last longer than diazepam
42
Why do clinical effects of lorazepam last longer than diazepam?
Due to greater GABA receptor binding
43
Large macromolecules that contain physically separate receptor sites for different drugs including benzos, barbs, and alcohol ______________ can occur due to this
GABA receptors Cross tolerance
44
2-3 times more potent than diazepam and has 2X affinity for receptors
Midazolam
45
Sedation 1/2 life of midazolam compared to diazepam and lorazepam
Shorter
46
Highest potency benzos
Lorazepam 1-2mg lorazepam equal in effect to 10-20 mg diazepam
47
H2 blocker interfere with metabolism of
Diazepam
48
Drugs inhibiting ___________ like EES and Ca+ channel blockers cause result in increased ________ action
Cytochrome P450 Midazolam
49
Cimetidine effect on diazepam
Delays hepatic clearance due to inhibition of necessary enzymes for metabolism
50
Paradoxical reactions with benzos occur in ______ of people Counteract reaction with
1% Flumazenil
51
Mental function returns to baseline within _______ with midazolam
4 hours
52
___________ may be used for emergence delirium in kids
Midazolam
53
Most potent benzo amnesic
Lorazepam
54
Midazolam and CMRO2
Decreases Cannot produce isoelectric EEG
55
Midazolam and ICP
Does not alter
56
Awakening after midazolam induction
Slower
57
Diazepam dose to abolish seizures
0.1 mg/kg
58
Consider avoidance of diazepam with
Narrow angle glaucoma
59
Used for ETOH withdrawal syndrome
Lorazepam
60
BP drop with midazolam due to
Lower SVR not lower CO
61
Does midazolam prevent HR and BP increase with DL?
NO
62
Does diazepam have any direct action on SNS?
NO
63
Midazolam and ventilatory depression
Dose dependent decrease Worse with lung disease
64
Causes decreased upper airway activity
Midazolam
65
No increase in PaCO2 with diazepam until doses greater than
0.2 mg/kg
66
Consider avoidance of all benzos with
Severe sleep apnea Pregnancy Myasthenia Gravis
67
ESRD and midazolam
No effect bc inactive metabolites
68
Preferred pre-med route for diazepam
PO
69
Peak oral concentrations of diazepam
1 hr adults 15-30 minutes peds
70
Lorazepam PO peak levels occur in ______ Therapeutic concentration lasts ______
2-4 hours 1-2 days
71
Benzos and skeletal muscle relaxation due to
Spinal inernuncial neurons not NMJ
72
________ and _______ are not water soluble
Diazepam and lorazepam
73
Flumazenil dose
0.2mg 8-15 mcg/kg
74
Flumazenil reverses benzo effects in _____ | Duration______
2 minutes Duration only 30-60 minutes

Pharm 2 (3rd Quarter) (6 decks)

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