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Pharmacology 1 > Benzodiazepine & Alpha 2 Agonist Dosages > Flashcards

Benzodiazepine & Alpha 2 Agonist Dosages Flashcards

1
Q

Diazepam alternate name:

A

Valium

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2
Q

Diazepam Structure:

A

Benzodiazepine

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3
Q

Diazepam MOA:

A
  1. Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
  2. Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
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4
Q

Diazepam Onset:

A

3 min

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5
Q

Diazepam Duration of action:

A

15-30 min

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6
Q

Diazepam PB:

A

95%

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7
Q

Diazepam Metabolism:

A

CYP3A4, 2C19, (secondary peak 6-12 h metabolite - desmethyldiazepam), Renal

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8
Q

Diazepam Premedication IV dose:

A

2-5 mg Q3-4 hr

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9
Q

Diazepam Anticonvulsant dose:

A

0.1-0.25 mg/kg

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10
Q

Diazepam side effects:

A
  1. A - Anxiolysis
  2. A - Anticonvulsant
  3. A - Anterograde amnesia
  4. S - Sedation
  5. S - Skeletal muscle relaxation
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11
Q

Contraindications/Cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. D - Dose dependent decrease in ventilation
  5. D - Drowsiness
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12
Q

Midazolam alternate name:

A

Versed

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13
Q

Midazolam structure:

A

1, 4 imidazobenzodiazepine derivative

Closed ring (lipid soluble) at physiologic Ph, open ring at lower Ph (around 4)

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14
Q

Midazolam MOA:

A
  1. Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
  2. Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
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15
Q

Midazolam Onset IV:

A

1-2 min

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16
Q

Midazolam Duration of action:

A

15-20 min IV

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17
Q

Midazolam PB:

A

95%

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18
Q

Midazolam Metabolism:

A

CYP3A4 to 1-hydroxymidazolam (active metabolite 20% potency), glucuronidation, really excreted

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19
Q

Midazolam Sedation / anxiolytic dose:

A

1-2.5 mg IV

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20
Q

Midazolam Sedation weight based IV dose:

A

0.1 mg/kg (max 2mg) Q10 min

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21
Q

Midazolam Side Effects:

A
  1. A - Anxiolysis
  2. A - Anticonvulsant
  3. A - Anterograde amnesia
  4. S - Sedation
  5. S - Skeletal muscle relaxation
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22
Q

Midazolam Contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. D - Dose dependent decrease in ventilation
  5. D - Drowsiness
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23
Q

Remimazolam alternate name:

A

Byfavo

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24
Q

Remimazolam structure:

A

1, 4 imidazobenzodiazepine derivative
Carboxylic acid

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25
Q

Remimazolam MOA:

A
  1. Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
  2. Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
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26
Q

Remimazolam Onset:

A

1-2 min

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27
Q

Remimazolam Duration of action:

28
Q

Remimazolam Protein Binding:

29
Q

Remimazolam Metabolism:

A

Rapidly metabolized by nonspecific tissue esterases

30
Q

Remimazolam IV dose:

A

0.01-0.5 mg/kg

31
Q

Remimazolam Side effects:

A
  1. A - Anxiolysis
  2. A - Anticonvulsant
  3. A - Anterograde amnesia
  4. S - Sedation
  5. S - Skeletal muscle relaxation
32
Q

Remimazolam Contraindications / cautions:

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. D - Dose dependent decrease in ventilation
  5. D - Drowsiness
33
Q

Lorazepam alternate name:

34
Q

Lorazepam structure:

A

Benzodiazepine

35
Q

Lorazepam MOA:

A
  1. Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
  2. Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
36
Q

Lorazepam Onset:

37
Q

Lorazepam Duration of action:

38
Q

Lorazepam PB:

39
Q

Lorazepam Metabolism:

A

CYP3A4 glucuronidation

40
Q

Lorazepam anxiety/sedation IV dose:

41
Q

Lorazepam Side effects:

A
  1. A - Anxiolysis
  2. A - Anticonvulsant
  3. A - Anterograde amnesia
  4. S - Sedation
  5. S - Skeletal muscle relaxation
42
Q

Lorazepam Contraindications / cautions

A
  1. M - MAC (synergistically reduces)
  2. D - Dependence
  3. B - Beers criteria (caution in older patients)
  4. D - Dose dependent decrease in ventilation
  5. D - Drowsiness
43
Q

Dexmedetomidine alternate name:

44
Q

Dexmedetomidine structure:

A

S-enantiomer of medetomidine

45
Q

Dexmedetomidine MOA:

A
  1. Alpha 2 agonist (Pontine locus coeruleus)
  2. Causes K efflux from the cell and hyperpolarization
  3. Decreased NE release presynaptically
  4. GPCR: Gi (inhibit adenylyl cyclase = decrease cAMP)
  5. 1620:1 (alpha 2:alpha 1 affinity)
46
Q

Dexmedetomidine Onset:

47
Q

Dexmedetomidine Duration of action:

48
Q

Dexmedetomidine PB:

49
Q

Dexmedetomidine Metabolims:

A

Hepatic via glucuronidation

50
Q

Dexmedetomidine IV dose:

A

0.5 - 1mcg/kg (loading dose over 10 min)
Or can give smaller doses PRN usually 0.05-0.1 mcg/kg for a max of 0.5 - 1mcg/kg

51
Q

Dexmedetomidine GA adjunct IV infusion dose:

A

0.2 - 0.4 mcg/kg/hr (1mcg/kg max)

52
Q

Dexmedetomidine IV infusion dose:

A

0.2-0.7 mcg/kg/hr

53
Q

Dexmedetomidine IV MAC infusion dose:

A

0.7-1 mcg/kg/hr (for 15-20 min, titrate down as able)

54
Q

Dexmedetomidine Side effects:

A
  1. Decreased HR
  2. Decrease BP
  3. Decrease opioid requirement
  4. Spares resp drive
  5. Decrease CBF (not CMRO2)
55
Q

Dexmedetomidine Contraindications / cautions:

A
  1. Caution In hepatic impairment
  2. Avoid in low HR (<70)
  3. Avoid in hypovolemia
  4. Avoid in low BP
  5. Does not cause amnesia
  6. Provides analgesia
56
Q

Clonidine alternate name:

57
Q

Clonidine structure:

A

Dichlorobenzene

58
Q

Clonidine MOA:

A
  1. Alpha 2 agonist (Pontine locus coeruleus)
  2. Causes K efflux from the cell and hyperpolarization
  3. Decreased NE release presynaptically
  4. GPCR: Gi (inhibit adenylyl cyclase = decrease cAMP)
  5. 220:1 (Alpha 2:1 receptor affinity)
59
Q

Clonidine Onset:

60
Q

Clonidine duration of action:

61
Q

Clonidine PB:

62
Q

Clonidine Metabolism:

A

Hepatic, excreted renally 50% unchanged

63
Q

Clonidine PO dose:

64
Q

Clonidine side effects:

A
  1. Sedation
  2. Bradycardia
  3. Dry mouth
  4. Decreased GI motility
  5. Decreased sympathetic tone
65
Q

Clonidine Contraindications / cautions:

A
  1. Rebound HTN (do not hold day of surgery)
  2. Low HR
  3. Allergy
  4. Hypotension
    5.

Pharmacology 1 (12 decks)

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