Benzodiazepine & Alpha 2 Agonist Dosages Flashcards
Diazepam alternate name:
Valium
Diazepam Structure:
Benzodiazepine
Diazepam MOA:
- 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
Diazepam Onset:
3 min
Diazepam Duration of action:
15-30 min
Diazepam PB:
95%
Diazepam Metabolism:
CYP3A4, 2C19, (secondary peak 6-12 h metabolite - desmethyldiazepam), Renal
Diazepam Premedication IV dose:
2-5 mg Q3-4 hr
Diazepam Anticonvulsant dose:
0.1-0.25 mg/kg
Diazepam side effects:
- A - Anxiolysis
- A - Anticonvulsant
- A - Anterograde amnesia
- S - Sedation
- S - Skeletal muscle relaxation
Contraindications/Cautions:
- M - MAC (synergistically reduces)
- D - Dependence
- B - Beers criteria (caution in older patients)
- D - Dose dependent decrease in ventilation
- D - Drowsiness
Midazolam alternate name:
Versed
Midazolam structure:
1, 4 imidazobenzodiazepine derivative
Closed ring (lipid soluble) at physiologic Ph, open ring at lower Ph (around 4)
Midazolam MOA:
- 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
Midazolam Onset IV:
1-2 min
Midazolam Duration of action:
15-20 min IV
Midazolam PB:
95%
Midazolam Metabolism:
CYP3A4 to 1-hydroxymidazolam (active metabolite 20% potency), glucuronidation, really excreted
Midazolam Sedation / anxiolytic dose:
1-2.5 mg IV
Midazolam Sedation weight based IV dose:
0.1 mg/kg (max 2mg) Q10 min
Midazolam Side Effects:
- A - Anxiolysis
- A - Anticonvulsant
- A - Anterograde amnesia
- S - Sedation
- S - Skeletal muscle relaxation
Midazolam Contraindications / cautions:
- M - MAC (synergistically reduces)
- D - Dependence
- B - Beers criteria (caution in older patients)
- D - Dose dependent decrease in ventilation
- D - Drowsiness
Remimazolam alternate name:
Byfavo
Remimazolam structure:
1, 4 imidazobenzodiazepine derivative
Carboxylic acid
Remimazolam MOA:
- 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
Remimazolam Onset:
1-2 min