Drug intelligence / Profile preview

propofol

Development stage
Approved
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Intravenous
01

Overview

Propofol is an intravenous anesthetic agent primarily used for the induction and maintenance of general anesthesia and for sedation in various medical procedures. It acts rapidly to induce unconsciousness within 15–30 seconds due to its high lipid solubility and rapid distribution into the central nervous system. The primary mechanism of action is positive allosteric modulation of gamma-aminobutyric acid type A (GABA-A) receptors, enhancing inhibitory neurotransmission in the brain. At higher concentrations, it can directly activate GABA-A receptors as an agonist. Propofol may also inhibit sodium channels and modulate the endocannabinoid system by inhibiting fatty acid amide hydrolase, increasing levels of anandamide and potentially contributing to its sedative effects via CB1 receptor activation. Its clinical use is favored due to rapid onset, short duration of action (3–10 minutes), quick recovery profile, and lower incidence of postoperative nausea compared with other anesthetics.

Brand names
DiprivanPropoven
Other names
2,6-diisopropylphenol
02

Targets

NaV (Voltage-gated sodium channels)FAAH

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