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Benzo Chart

Benzo Comparison Chart

CategoryMidazolamLorazepamDiazepamFlumazenil
Blank Midazolam Lorazepam Diazepam Flumazenil
Trade Name Versed Ativan Valium Romazicon
Class BZDP: imidazole ring BZDP BZDP BZDP receptor antagonist
IV Sedation Dose Adult 0.05 mg/kg 0.04 mg/kg 0.1 mg/kg IV 0.2 mg/kg po; 15 mg max 0.2 mg IV; repeat 0.1 mg q min up to 1 mg/hr and 3mg max
Potency moderate Valium x5 MOST Versed x5/Valium x25 least (blank)
Available Conc. 1 mg/ml & 5 mg/ml 2 mg/ml & 4 mg/ml 5 mg/ml 0.1 mg/ml
Acid or Base Base Base Base Base
pKa (ionization) 6.15 (@7.4, > non-ionized) 11 (@7.4 >> ionized) 3.3 (@7.4, >> non-ionized) (blank)
Solubility H2O @ pH <4 (open) Lipid @ pH >4 (closed) Lipid LIPID (very) H2O in vial; Lipid @ physiologic pH
Protein Binding 94% 98% 90% competes w/ heparin at binding site 50%
Sedative/ Hypnotic? Sedative/Hyponotic Anxiolytic Sedative/Hyponotic Anxiolytic Sedative/Hyponotic Anxiolytic REVERSES
Analgesia? NO NO NO NO
Amnesia? YES YES (most potent) YES ?Reverses? (unreliable)
Effect Site Equilibration (Onset) 30-90 sec (also 1-6 min some sources) 60-120 sec 45-90 sec 2 min
Duration 10-30 min 1-2 hrs; amnesia up to 6 hrs 15-30 min 30-60 min
Action at Receptor Agonist @ GABA-Cl- influx, hyperpolarize; 2x affinity of valium Agonist @ GABA-Cl- influx, hyperpolarize; HIGH RECEPTOR AFFINITY Agonist @ GABA-Cl- influx, hyperpolarize Specific BZDP Competitive Antagonist Weak Agonist, <1% VERY HIGH RECEPTOR AFFINITY
Saturation Receptors saturable (ceiling effect):20%- anxiolysis, 30-50%-sedation, >60% hypnosis Receptors saturable (ceiling effect):20%- anxiolysis, 30-50%-sedation, >60% hypnosis Receptors saturable (ceiling effect):20%- anxiolysis, 30-50%-sedation, >60% hypnosis (blank)
Ligand or 2nd msgr? Ligand Ligand Ligand Ligand
CNS effects Dec CMRO2, CBF; No inc ICP but no ischemic protection; CO2-vasodilation response intact; elderly more sens. to cereb. depression Dec CMRO2, CBF; No inc ICP but no ischemic protection; CO2-vasodilation response intact; elderly more sens. to cereb. depression Dec CMRO2, CBF; No inc ICP but no ischemic protection; CO2-vasodilation response intact; elderly more sens. to cereb. depression Increase in ICP secondary to less sedation, not from drug itself
SC-mediated skeletal muscle relaxation Yes Yes Yes (blank)
Burst Suppressive NO NO NO NO
Sz ALL ARE ANTICONVULSANTS (slower/less potent [but more specific] than barbs): membrane stabilization (use in inadvertent IV local anesthetic); also Sz preventative ALL ARE ANTICONVULSANTS (slower/less potent [but more specific] than barbs): membrane stabilization (use in inadvertent IV local anesthetic); also Sz preventative ALL ARE ANTICONVULSANTS (slower/less potent [but more specific] than barbs): membrane stabilization (use in inadvertent IV local anesthetic); also Sz preventative No effect d/t weak agonist
CV effects Minimal Cardiac Effects; more effects with opiods; as induction agent, acts like pentothol (BP, HR) LEAST Cardiac Effects Minimal Cardiac Effects; more effects with opiods No adverse effects Perhaps d/t weak agonist
Resp. Effects Dose Depedent Depression; synergistic with opiods ANY DOSE CAN CAUSE APNEA Dose Depedent Depression; synergistic with opiods ANY DOSE CAN CAUSE APNEA Dose Depedent Depression; synergistic with opiods ANY DOSE CAN CAUSE APNEA Depression not completely reversed
Clearance Eliminated in Urine Eliminated in Urine Eliminated in Urine Very Rapid
E1/2 2 hrs 15 hrs 30 hrs (directly r/t age, up to 2x) 1 hr
Metabolism Type Hydroxylation and Conjugation Hydroxylation and Conjugation Hydroxylation and Conjugation (blank)
Metabolism No change for age/liver dx; CCB, E-mycin, **Fentanyl** interfere No change for age; Prolonged for liver failure Prolonged for age (2x)/ liver dx (5X); Cimetidine interferes No change for age/liver dx
Metabolites 2 Active: clinically irrelevant unless extreme renal failure (1- & 4-hydroxymidazolam) (inactive) 2 Active: Desmethyldiazepam (2x t1/2) Oxazepam (Serax) (inactive)
(blank) Midazolam Lorazepam Diazepam Flumazenil
Enzyme Induction (ETOH is enzyme inducer!!) CYP450: inducer - rapid metabolism competitor - slower metabolism CYP450: inducer - rapid metabolism competitor - slower metabolism CYP450: inducer - rapid metabolism competitor - slower metabolism (blank)
IV Induction/ Infusion 0.1-0.2 mg/kg, then 0.25-1 mcg/kg/min (blank) (blank) (blank)
Misc. Trivia Can be used for induction - not very smooth; takes longer to induce & emerge than STP; Little PONV/ emergence excitement; No delay in d/c times; Decrease dose for opioids, MAC, elderly, other CNS depressant; doesn't accum as much as Fent/ST Very thick solution; Limits emergence delirium from Ketamine Thick solution (organic sol); painful injection; less pain, thrombophlebitis w/ soy formulation; AVIOD IM inj; dec albumin may inc onset and effects @ start; 90-100% bioavailable; USE: evening preop sedation; skeletal musc rela May need more before BZDPs wear off; requires continuous monitoring
Dose Adjust Peds: 0.2 mg/kg IN or 0.5 mg/kg po onset 10-15 min Decrease in elderly Decrease in elderly (blank)
Created by: jestevenson
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