Benzo Chart Word Scramble

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Benzo Chart

Benzo Comparison Chart

Category	Midazolam	Lorazepam	Diazepam	Flumazenil
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 on 2008-02-11