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Anesth Pharm > BZD > Flashcards

BZD Flashcards

1
Q

5 main effects BZD

A

Anxiolytic
Sedation
Anterograde Amnesia
Anticonvulsant
Spinal cord mediated muscle relaxation

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2
Q

BZD replaced barbiturates. What were the BZD benefits that led to this change

A

Benzos: have less tolerance, less abuse, fewer side effects, do not induce hepatic enzymes therefore less drug interactions.

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3
Q

BZD MOA

A

Facilitates action of GABA at GABA A chloride ionophore.
Enhance affinity of receptor for GABA
Enhanced opening of Cl- Channels
Hyperpolarization of postsynaptic membrane

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4
Q

Alpha 1 Effects

A

sedative, amnestic, anticonvulsant.

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5
Q

Alpha 1 locations

A

Cerebral cortex, cerebellar cortex, thalamus

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6
Q

Alpha 2

A

Anxiolytic, skeletal muscle

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7
Q

Alpha 2 location

A

hippocampus and amygdala

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8
Q

What other things bind to GABA A receptors

A

Barbs, etomidate, prop, ETOH

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9
Q

Why is it important to know what other substances bind to GABA A receptor

A

They all have synergistic effects. Increased OD

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10
Q

BZD eeg effects

A

All decrease alpha activity

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11
Q

What effect does altering alpha wave have

A

Very relaxed, deepening into meditation.

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12
Q

Which BZD cannot cause isoelectric brain waves

A

Versed cannot make brain waves isoelectric

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13
Q

Name drug classes that have synergistic effects with BZD

A

Alpha 2 agonists, opioids, alcohol, inhaled anesthetics

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14
Q

BZD effect on clotting

A

Inhibits platelet aggregating factor. Inhibits conformational shape change of platelets from smooth to pseudopod

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15
Q

What effect of versed lasts the longest

A

The amnesia lasts longer than the sedation.

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16
Q

How is versed diluted

A

It is not diluted as it is water soluble

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17
Q

What is versed pH

A

3.5

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18
Q

At what pH is imidazole ring opened and what does this mean

A

Imidazole ring is open at pH <3.5. This is the water soluble/pronated form.

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19
Q

At what pH is imidazole ring closed and what does this mean

A

The imidazole ring is closed at pH >4.0. This makes the ring close and become lipid soluble. It is able to reach the brain.

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20
Q

Versed onset

A

1-2 mins

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21
Q

Versed peak effect

A

5 mins

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22
Q

Duration of versed

A

Short duration d/t lipid solubility and rapid redistribution

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23
Q

Versed E 1/2 time

A

2 hours. Doubled in elderly

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24
Q

Versed Vd:

A

1-1.5 L/kg (large)
Greater vd in elderly and obese

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25
Q

What is the active metabolite of versed? What percent of active versed does this metabolite exert

A

1-hydroxymidazolam
1/2 the activity of Versed

26
Q

What can cause decreased metabolism of BZD

A

Inhibition of P-450 enzymes

27
Q

What are some meds that inhibit CYP-450

A

Tagamet, calcium channel blockers, erythromycin, anti-fungal, fentanyl

28
Q

Versed metabolism compared to lorazepam? Diazepam?

A

Clearance 5x faster than lorazepam/10x faster than diazepam

29
Q

Versed CNS effects

A

-Decreases CMRO2 and CBF
-Unable to produce isoelectric EEG
-Potent anticonvulsant (even in status)
-Preserves vasomotor response to CO2, high CO2 dilates vessels/low CO2 constricts.
-no change in ICP if decreased cranial compliance (won’t cause further increase of ICP)

30
Q

Versed pulmonary effects

A

-Decreases hypoxia drive (ventilation) worsened in COPD. Transient apnea with rapid iv esp if using opioids.
-depressed swallowing reflex
-decreases upper airway activity (increased aspiration risk)

31
Q

Versed CV effects

A

Dose dependent increased HR/decreased BP
This allows CO to stay same.

32
Q

Versed sedation dose

A

Kids: 0.25-0.5 mg/kg PO
Onset 20-30 mins

Adults: 1-5 mg IV
onset: 5 mins

33
Q

Versed Induction dose

A

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

34
Q

Versed Maintenance dosing

A

Uncommon d/t quick onset/offset. Would require many IV bags to keep up.
It supplements prop, opioids, VA. Decreasing VA needed.

35
Q

Versed post op dose

A

1-7 mg/ hr IV.
Delayed awakening d/t active metabolite accumulation.
Can interfere with immune/T cells with use for 2-3 days.

36
Q

Valium onset

A

1-5 mins

37
Q

Valium E 1/2

A

20-40 hours. This makes it better option for post op sedation.

38
Q

How does Valium’s duration and E 1/2 compare to Versed

A

Valium has a shorter duration of action and a longer E 1/2.
The longer E 1/2 makes Valium a poor choice for day surgery d/t prolonged awakening r/t long E 1/2

39
Q

Which active metabolite of Valium is more potent

A

Desmethyldiazepam is nearly as potent as diazepam. It lasts (48-96 hrs)

40
Q

CNS effect Valium

A

Decreased CMRO2 and CBF
Can achieve isoelectric brain wave (versed could not)
Potent anticonvulsant (DT, status, lido tox seizures)

41
Q

Pulmonary effects of diazepam (Valium)

A

Minimal ventilation effects
Slight decrease in Vt
Increases PaCO2 after 0.2 mg/kg (worsened by simultaneous use with opioids, ETOH or either COPD)
*ventilatory suppression effects nullified by surgical stimulation

42
Q

Which BZD would be appropriate for COPD pt and why?

A

Valium would be most appropriate

Versed decreases hypoxic drive which is further worsened in COPD pts.

43
Q

Valium CV effects

A

Minimal decreases in BP/CO/SVR even with induction doses.
Great for cardiac surgery induction
Decreases BP with opioid use

44
Q

Valium neuromuscular effects

A

Decreases tonic effect of spinal neuron: skeletal muscle tone decreased, develop tolerance to muscle relaxant effects.

No action at NM junction

45
Q

Valium induction dosing

A

0.5-1.0 mg/kg

Decrease dose by 25-50% in elderly, liver disease, presence of opioids.

46
Q

How does lorazepam (Ativan) compare to Versed and Valium in regards to amnesia/sedation

A

Ativan is a more potent amnestic and sedative than both of these drugs

47
Q

Ativan preparation

A

Requires polyethylene glycol since it is insoluble in water

48
Q

How does the onset of action of Ativan compare to other BZD

A

Slower onset of action d/t being less lipid soluble (takes longer to enter CNS)
Slower metabolic clearance

49
Q

Ativan is great for what use

A

Post op sedation d/t slower metabolic clearance

50
Q

Ativan dose and peak

A

1-4 mg IV
Peak 20-30 mins. Not good for induction great for maintenance and post op sedation

51
Q

Ativan E 1/2

A

14 hours
Glucoronidation is slower than hydrolysis

52
Q

Metabolism of Ativan

A

Glucoronidation therefore less dependent on hepatic enzymes. Less affected by drugs that alter hepatic functions e.g. cimetidine (Tagamet)

53
Q

Reversal agent for BZD

A

flumazenil (Romazicon)
1.4 imidazobenzodiazepine derivative

54
Q

How does flumazenil (Romazicon) work

A

Competitive antagonist for BZD receptor.
Prevents/reverses all agonist activity of BZD

55
Q

Dose of flumazenil

A

0.2 mg IV and titrate to consciousness

Repeated in 0.1 mg q 1 minute to 1 mg total

56
Q

Reversal within 2 minutes doses to reverse sedation? Abolish therapeutic effect?

A

0.3-0.6 mg to reverse sedation

0.5 mg-1.0 mg to abolish therapeutic dose

57
Q

Why is it important to continually monitor patient after successful reversal of BZD via flumazenil

A

If the patient OD on Versed, which is fat soluble, they can resedate due to the fat stores of the medication.

58
Q

Unconscious overdose with no change after 0.5-1.0 mg flumazenil would lead one to suspect what

A

The OD was not BZD related and most likely Opioid.

59
Q

Continuous infusion dose of flumazenil

A

0.1-0.4 mg/hr

60
Q

Side effects of flumazenil

A

No known side effects.

61
Q

Contraindications of flumazenil

A

Patient on BZD for seizures

Antiepileptic seizures.
Can precipitate acute withdrawal seizures.

Anesth Pharm (4 decks)

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