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Propofol mechanism of action

Propofol has probably the commonly used intravenous anesthetic and is most frequently used for the induction of anesthesia. Like most intravenous anesthetics, Propofol works by increasing GABA-mediated inhibatory tone in the CNS. Propofol decreases the rate of dissociation of the GABA from the receptor, thereby increasing the duration of the GABA-activated opening of the chloride channel with resulting hyperpolarization of cell membranes. At supraclinical concentrations, it may directly activate the receptor’s chloride channel.


  1. G Trapani, C Altomare, G Liso, E Sanna, G Biggio Propofol in anesthesia. Mechanism of action, structure-activity relationships, and drug delivery. Curr. Med. Chem.: 2000, 7(2);249-71 PubMed Link