Dược Động Học :
▧ Absorption :
Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.
▧ Volume of Distribution :
* 60 L/kg [healthy adults]
▧ Protein binding :
95 to 99%, primarily to serum albumin and hemoglobin
▧ Metabolism :
Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.
▧ Route of Elimination :
It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.
▧ Half Life :
Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.
▧ Clearance :
* 23 - 50 mL/kg/min
* 1.6 - 3.4 L/min [70 Kg adults]
Độc Tính :
Overdosage may increase pharmacologic and adverse effects or cause death.
IV LD50=53 mg/kg (mice), 42 mg/kg (rats). Oral LD50 (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)