Ex1 Benzo Slides Flashcards

1
Q

Receptors effected by Benzos

A

a1 GABA-A

a2 GABA-A

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2
Q

a1 GABA-A Receptor is responsible for

A

Sedation, amnesia, anticonvulsant effects. Most prominent

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3
Q

a2 GABA-A Receptor is responsible for

A

CNS mediated skeletal muscle relaxant effects and anxiolysis

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4
Q

Benzos decrease wakefulness by inhibition of ______ in the _______

A

RAS - reticular activating system

Brain stem

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5
Q

Inhibition in the ______ causes _____ effect

A

RAS

Sedative/hypnotic effects (drowsy/sleep)

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6
Q

Effects of Benzos on CNS

A

Decrease CMRO2, CBF
Increase seizure threshold
Protect against cerebral hypoxia (Midazolam > diazepam)

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7
Q

Benzo effect on Ventilation

A

Mild depression of ventilation
Decreased Vt and MV (dose dependent)
Mildly elevated CO2

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8
Q

Apnea occurs in _____% after Benzo administration in dose starting at _____ mg

A

20; 2

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9
Q

Exceptions to Benzos - ventilation

A

Flatter CO2 curve. NOT shifted.

Sensitive patients: chronic lung disease, obese, elderly

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10
Q

Special population of patients should receive what dose of Benzos?

A

1/4 dose and titrate to effect (better to avoid Benzos altogether)

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11
Q

Benzo effects on CV system

A

Decreased SVR

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12
Q

Benzos will result in _______ blood pressure due to ______

A

Decreased

Decreased SVR

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13
Q

Drugs used to reduce HR/BP which accompanies intubation

A

Opioids, beta antagonists, lidocaine

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14
Q

Most common side effects of Benzos

A

Fatigue, drowsiness

Other: dependence

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15
Q

Important side effect of benzos

A

Withdrawal syndrome - life threatening, irritability, insomnia, tremors, seizures, death

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16
Q

Long acting Benzo withdrawal will occur after _____ days, while short acting will occur after _____ days

A

2-5 days
1-2 days
After cessation

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17
Q

T or F: benzodiazepines do not induce microsomal enzymes

A

True

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18
Q

Benzos should be avoided in who?

A
Pregnant individuals (teratogenic)
Procedures identifying seizure foci
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19
Q

Benzos will create a _____ effect when combined with opioids, propofol, barbiturates, ETOH

A

Synergistic

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20
Q

Which medications will cause a synergistic effect when given with benzos?

A

Opioids, propofol, barbiturates, ETOH

21
Q

What combo of Rx is considered “cardiac stable” when given with benzos?

A

Opioids

22
Q

Important structure on midazolam

A

Imidazole ring

23
Q

Midazolam in lipid soluble form has a pH of?

A

> 4

24
Q

Midazolam in water soluble form has pH of?

A

< 4

Open ring form

25
Q

PK of midazolam

A

6.15

26
Q

What does midazolam depend on in order to main closed ring/active form?

A

pH > 5 = 99% is in active form (closed ring)

27
Q

Midazolam- responsiveness to ______ is preserved

A

Vasomotor responsiveness to CO2

Increased CO2=increased CBF

28
Q

Midazolam Sedation Dose - PO

A

0.5 mg/kg PO 30 min prior to induction in peds

29
Q

Midazolam sedation dose IV

A

1-2.5mg IV bolus

30
Q

Induction of GA - midazolam dose

A

Induction: 0.1-0.3 mg/kg

31
Q

Why does diazepam remain in body for such a long time?

A

Undergoes enterohepatic recirculation

32
Q

Diazepam metabolites undergo ______

A

Glucuronidation

33
Q

E1/2 of Diazepam

A

21-37h

34
Q

Delayed clearance and prolonged E1/2t for diazepam may be due to

A

Inhibition of CYP450 by other substances

35
Q

Diazepam metabolization is notable for

A

Desmethyl metabolite - active

E1/2t = 48-96h

36
Q

What is responsible for biphasic pattern of sedation in Diazepam?

A

Desmethyl metabolite

37
Q

Skeletal muscle effects of Diazepam

A

Muscle relaxant - SPINAL (centrally) mediated

38
Q

What muscular effect will occur with chronic administration of diazepam?

A

Tolerance to relaxant effect

39
Q

Diazepam dosing - PO

A

10-15mg peaks 1h

40
Q

Diazepam dosage IV

A

0.05-0.15 mg/kg

Titrate - start low, go slow

41
Q

Induction dose Diazepam

A

0.3-0.5mg/kg

42
Q

Rate potency of Diazepam, Lorazepam, Midazolam

A

Lorazepam > midazolam > diazepam

43
Q

Rate duration of action: diazepam, lorazepam, midazolam

A

Diazepam > Lorazepam > midazolam

44
Q

Flumazenil duration of action

A

30-60 min

Re-sedation or infusion may be required

45
Q

Dose of Flumazenil

A

0.2 mg IV reverses CNS effects in 2 minutes

46
Q

Maximum flumazenil dose

A

1mg IV

Titrate 0.1 mg each time

47
Q

Flumazenil is a _______ of the GABA A receptor

A

Competitive antagonist

48
Q

Benzos that have venous irritation and why?

A
Diazepam, lorazepam
Propylene glycol (to enhance water solubility)
49
Q

Why isn’t lorazepam used for seizures?

A

Slow onset