Benzodiazepine & Alpha 2 Agonist Dosages Flashcards
1
Q
Diazepam alternate name:
A
Valium
2
Q
Diazepam Structure:
A
Benzodiazepine
3
Q
Diazepam MOA:
A
- Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
- Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
4
Q
Diazepam Onset:
A
3 min
5
Q
Diazepam Duration of action:
A
15-30 min
6
Q
Diazepam PB:
A
95%
7
Q
Diazepam Metabolism:
A
CYP3A4, 2C19, (secondary peak 6-12 h metabolite - desmethyldiazepam), Renal
8
Q
Diazepam Premedication IV dose:
A
2-5 mg Q3-4 hr
9
Q
Diazepam Anticonvulsant dose:
A
0.1-0.25 mg/kg
10
Q
Diazepam side effects:
A
- A - Anxiolysis
- A - Anticonvulsant
- A - Anterograde amnesia
- S - Sedation
- S - Skeletal muscle relaxation
11
Q
Contraindications/Cautions:
A
- M - MAC (synergistically reduces)
- D - Dependence
- B - Beers criteria (caution in older patients)
- D - Dose dependent decrease in ventilation
- D - Drowsiness
12
Q
Midazolam alternate name:
A
Versed
13
Q
Midazolam structure:
A
1, 4 imidazobenzodiazepine derivative
Closed ring (lipid soluble) at physiologic Ph, open ring at lower Ph (around 4)
14
Q
Midazolam MOA:
A
- Binds to the benzodiazepine binding site located at the subunit cleft between the alpha and gamma subunits of GABA-A receptors
- Binding creates a greater affinity for GABA at the receptor which opens the Cl channel causing Cl influx and hyperpolarization
15
Q
Midazolam Onset IV:
A
1-2 min
16
Q
Midazolam Duration of action:
A
15-20 min IV
17
Q
Midazolam PB:
A
95%
18
Q
Midazolam Metabolism:
A
CYP3A4 to 1-hydroxymidazolam (active metabolite 20% potency), glucuronidation, really excreted
19
Q
Midazolam Sedation / anxiolytic dose:
A
1-2.5 mg IV
20
Q
Midazolam Sedation weight based IV dose:
A
0.1 mg/kg (max 2mg) Q10 min
21
Q
Midazolam Side Effects:
A
- A - Anxiolysis
- A - Anticonvulsant
- A - Anterograde amnesia
- S - Sedation
- S - Skeletal muscle relaxation
22
Q
Midazolam Contraindications / cautions:
A
- M - MAC (synergistically reduces)
- D - Dependence
- B - Beers criteria (caution in older patients)
- D - Dose dependent decrease in ventilation
- D - Drowsiness
23
Q
Remimazolam alternate name:
A
Byfavo
24
Q
Remimazolam structure:
A
1, 4 imidazobenzodiazepine derivative
Carboxylic acid
25
Remimazolam MOA:
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
26
Remimazolam Onset:
1-2 min
27
Remimazolam Duration of action:
5-10 min
28
Remimazolam Protein Binding:
95%
29
Remimazolam Metabolism:
Rapidly metabolized by nonspecific tissue esterases
30
Remimazolam IV dose:
0.01-0.5 mg/kg
31
Remimazolam Side effects:
1. A - Anxiolysis
2. A - Anticonvulsant
3. A - Anterograde amnesia
4. S - Sedation
5. S - Skeletal muscle relaxation
32
Remimazolam Contraindications / cautions:
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
Lorazepam alternate name:
Ativan
34
Lorazepam structure:
Benzodiazepine
35
Lorazepam MOA:
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
Lorazepam Onset:
1-2 min
37
Lorazepam Duration of action:
1-2 h
38
Lorazepam PB:
95%
39
Lorazepam Metabolism:
CYP3A4 glucuronidation
40
Lorazepam anxiety/sedation IV dose:
1-4 mg
41
Lorazepam Side effects:
1. A - Anxiolysis
2. A - Anticonvulsant
3. A - Anterograde amnesia
4. S - Sedation
5. S - Skeletal muscle relaxation
42
Lorazepam Contraindications / cautions
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
Dexmedetomidine alternate name:
Precedex
44
Dexmedetomidine structure:
S-enantiomer of medetomidine
45
Dexmedetomidine MOA:
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
Dexmedetomidine Onset:
5 min
47
Dexmedetomidine Duration of action:
1-2 h
48
Dexmedetomidine PB:
95%
49
Dexmedetomidine Metabolims:
Hepatic via glucuronidation
50
Dexmedetomidine IV dose:
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
Dexmedetomidine GA adjunct IV infusion dose:
0.2 - 0.4 mcg/kg/hr (1mcg/kg max)
52
Dexmedetomidine IV infusion dose:
0.2-0.7 mcg/kg/hr
53
Dexmedetomidine IV MAC infusion dose:
0.7-1 mcg/kg/hr (for 15-20 min, titrate down as able)
54
Dexmedetomidine Side effects:
1. Decreased HR
2. Decrease BP
3. Decrease opioid requirement
4. Spares resp drive
5. Decrease CBF (not CMRO2)
55
Dexmedetomidine Contraindications / cautions:
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
Clonidine alternate name:
Catapres
57
Clonidine structure:
Dichlorobenzene
58
Clonidine MOA:
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
Clonidine Onset:
30-60 min
60
Clonidine duration of action:
3-7 hr
61
Clonidine PB:
30%
62
Clonidine Metabolism:
Hepatic, excreted renally 50% unchanged
63
Clonidine PO dose:
0.1 mg PO
64
Clonidine side effects:
1. Sedation
2. Bradycardia
3. Dry mouth
4. Decreased GI motility
5. Decreased sympathetic tone
65
Clonidine Contraindications / cautions:
1. Rebound HTN (do not hold day of surgery)
2. Low HR
3. Allergy
4. Hypotension
5.
