Imidazole ring
After soluble at a pH less than 4
Closes upon injection and becomes highly lipid soluble
Potency
2-4 times more potent than diazepam
Protein bound
96-98%
Lipid soluble
Rapid uptake by the brain
Redistribution and re-uptake
VD
1-1.5 L/kg
Clearance
6-8 ml/kg/min
Elimination half life
1-4 hours
Oxidative hydroxylation
In the liver
Glucoronide conjugation
In the kidneys
Excreted
Urine
Metabolizes
Minimally active
H2 receptor antagonists added
Not affected
Cardiac response
Minimal and similar to NaP
Ventilation
Depressed with 0.15 mg/kg dose
Renal failure
Kemal effects on half life, VD, and clearance
CBF
Dose related decrease in CBF and CMRO2
Placenta
Crosses the U-P membrane