Clinical Action & Pharmacokinetics

• Mechanism: Propofol is an IV anesthetic/sedative that enhances GABAA currents by slowing deactivation and reducing receptor desensitization. It also inhibits NMDA glutamate receptors, depressing excitatory transmission, and exerts antiemetic effects by reducing serotonin in the area postrema.
• Pharmacokinetics: Follows a 3-compartment linear model. Onset is rapid (~40s) via quick blood-brain equilibration. Clearance is 23–50 mL/kg/min via hepatic conjugation to inactive metabolites excreted by kidneys. Distribution accounts for 50% of plasma decline. Infusions over 10 days accumulate in fat, extending terminal half-life to 1–3 days and delaying recovery.

Critical Administration & Dosing Rules

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