Propofol

Propofol has revolutionized anesthesia and intensive caremedicine owing to its favorable pharmacokinetic characteristics, fast onset,and short duration of action. Propofol hasmaintained an overwhelmingly favorable safety profile.It also showed antiepileptic and anxiolytic properties in studies.

Propofol is extensively metabolized, with most of theadministered dose appearing in the urine as glucuronide conjugates. Propofol is a GABAreceptor agonist that exerts its hypnotic effect by enhancing the activity ofthe inhibitory neurotransmitter GABA. It enhances the GABA-activated inward chloridecurrent at low concentrations, and directly activates channel opening at higherconcentrations. Owing to itshigh lipophilicity, it quickly passes through the blood–brain barrier to exertits efficacy within a short period after injection.

Althoughpropofol has rapid induction and metabolism, it cannot inhibit the coughresponse, and affects the circulatory and respiratory systems during use. And studies showedthat propofol has been associated with both antiarrhythmic andproarrhythmic effects.Moreover, propofol lacks analgesic effects and specific antagonists,which increases the risk of propofol infusion syndrome and bacterialcontamination.

For more information please refer to:

1. Trapani G, Altomare C, Liso G, Sanna E, Biggio G.Propofol in anesthesia. Mechanism of action,structure-activity relationships, and drug delivery. Curr Med Chem. 2000;7:249–271.

2. Jananthan Paramsothy,Sai DheerajGutlapalli,corresponding author，Vijay Durga Pradeep Ganipineni. Propofol in ICU Settings: Understanding andManaging Anti-Arrhythmic, Pro-Arrhythmic Effects, and Propofol InfusionSyndrome. Cureus. 2023 Jun; 15(6): e40456.

3. Ning Jin, Zhiqiang Xue. Benefits of remimazolam asan anesthetic sedative for older patients: A review. Heliyon. 2024 Feb 29;10(4): e25399. Published online 2024 Feb 6. doi: 10.1016/j.heliyon.2024.e25399