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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
Q

Greater Vd of elderly and obesity of midazolam due to

A

Increased peripheral distribution resulting in prolonged duration of action

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26
Q

Only benzo used for infusion

A

Midazolam

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27
Q

Midazolam is hydroxylated via

A

Cytochrome P450

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28
Q

Midazolam is excreted in _______ as _______

A

Urine as glucuronidation conjugates

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29
Q

Diazepam Vd is large why??

A

Highly lipophillic taken into fat tissue

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30
Q

Diazepam and placental barrier

A

Crosses

31
Q

Diazepam protein binding

A

Parallels lipid solubility

32
Q

3 conditions decreasing diazepam protein binding resulting in exaggerated effects

A

Cirrhosis
ESRD
Hypoalbuminemia

33
Q

OD treatment of diazepam

A

Flumazenil

34
Q

Hemodialysis is not effective for diazepam OD

Why?

A

Bc too highly protein bound

35
Q

Diazepam is metabolized by _______ using _______

A

Hepatic microsomal enzymes

Oxidative pathways

36
Q

2 principle metabolites of diazepam

Which more potent

A

Demethyldiazepam. (Most potent)

Oxazepam

37
Q

What causes second wave of sedation 6-8 hours after diazepam administration

A

Desmethyldiazepam

38
Q

Diazepam elimination 1/2 time

A

21-37 hours

39
Q

Desmethyldiazepam elimination 1/2 time

A

48-96 hours

40
Q

Lorazepam is conjugated via _________ to _______

A

Glucuronic acid to INACTIVE metabolites

41
Q

Elimination 1/2 time of lorazepam

A

10-20 hours. But clinical effects last longer than diazepam

42
Q

Why do clinical effects of lorazepam last longer than diazepam?

A

Due to greater GABA receptor binding

43
Q

Large macromolecules that contain physically separate receptor sites for different drugs including benzos, barbs, and alcohol

______________ can occur due to this

A

GABA receptors

Cross tolerance

44
Q

2-3 times more potent than diazepam and has 2X affinity for receptors

A

Midazolam

45
Q

Sedation 1/2 life of midazolam compared to diazepam and lorazepam

A

Shorter

46
Q

Highest potency benzos

A

Lorazepam

1-2mg lorazepam equal in effect to 10-20 mg diazepam

47
Q

H2 blocker interfere with metabolism of

A

Diazepam

48
Q

Drugs inhibiting ___________ like EES and Ca+ channel blockers cause result in increased ________ action

A

Cytochrome P450

Midazolam

49
Q

Cimetidine effect on diazepam

A

Delays hepatic clearance due to inhibition of necessary enzymes for metabolism

50
Q

Paradoxical reactions with benzos occur in ______ of people

Counteract reaction with

A

1%

Flumazenil

51
Q

Mental function returns to baseline within _______ with midazolam

A

4 hours

52
Q

___________ may be used for emergence delirium in kids

A

Midazolam

53
Q

Most potent benzo amnesic

A

Lorazepam

54
Q

Midazolam and CMRO2

A

Decreases

Cannot produce isoelectric EEG

55
Q

Midazolam and ICP

A

Does not alter

56
Q

Awakening after midazolam induction

A

Slower

57
Q

Diazepam dose to abolish seizures

A

0.1 mg/kg

58
Q

Consider avoidance of diazepam with

A

Narrow angle glaucoma

59
Q

Used for ETOH withdrawal syndrome

A

Lorazepam

60
Q

BP drop with midazolam due to

A

Lower SVR not lower CO

61
Q

Does midazolam prevent HR and BP increase with DL?

A

NO

62
Q

Does diazepam have any direct action on SNS?

A

NO

63
Q

Midazolam and ventilatory depression

A

Dose dependent decrease

Worse with lung disease

64
Q

Causes decreased upper airway activity

A

Midazolam

65
Q

No increase in PaCO2 with diazepam until doses greater than

A

0.2 mg/kg

66
Q

Consider avoidance of all benzos with

A

Severe sleep apnea

Pregnancy

Myasthenia Gravis

67
Q

ESRD and midazolam

A

No effect bc inactive metabolites

68
Q

Preferred pre-med route for diazepam

A

PO

69
Q

Peak oral concentrations of diazepam

A

1 hr adults

15-30 minutes peds

70
Q

Lorazepam PO peak levels occur in ______

Therapeutic concentration lasts ______

A

2-4 hours

1-2 days

71
Q

Benzos and skeletal muscle relaxation due to

A

Spinal inernuncial neurons not NMJ

72
Q

________ and _______ are not water soluble

A

Diazepam and lorazepam

73
Q

Flumazenil dose

A

0.2mg

8-15 mcg/kg

74
Q

Flumazenil reverses benzo effects in _____

Duration______

A

2 minutes

Duration only 30-60 minutes

Pharm 2 (3rd Quarter) (6 decks)

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