Small molecule
PubChem CID 4943
Propofol
Diprivan
- Mechanism of action
- GABA-A receptor positive allosteric modulator (general anesthetic)
- In plain language
- The fast-acting IV anesthetic that dials up the brain's natural 'calm down' signal (GABA) at a different spot than sleeping pills and anti-anxiety drugs use, working in about a minute and wearing off almost as fast once the infusion stops.
- How it works
- Propofol is an intravenous general anesthetic that acts on GABA-A receptors, the same inhibitory chloride-channel family targeted by benzodiazepines and zolpidem already on this site — but at a mechanistically distinct site. Propofol binds in a pocket near the extracellular ends of the beta-subunit transmembrane segments, at the alpha/beta subunit interface, rather than the alpha/gamma interface used by benzodiazepines, and its action does not require the gamma subunit. At the lower concentrations used for sedation, propofol acts as a positive allosteric modulator, enhancing GABA-evoked chloride currents; at the higher concentrations used to induce general anesthesia, it can directly activate the channel even without GABA bound. Clinically, propofol's defining feature is its pharmacokinetics: rapid equilibration between plasma and brain produces anesthesia within about a minute of an IV bolus, and for short infusions, recovery is driven mainly by redistribution of drug out of the brain into peripheral tissue rather than by hepatic metabolism, giving it a rapid, clean offset unlike the longer-acting benzodiazepine sedatives.
- Therapeutic applications
- Per FDA-approved labeling, DIPRIVAN (propofol) is indicated for induction of general anesthesia in patients 3 years of age and older, maintenance of general anesthesia in patients 2 months of age and older, initiation and maintenance of Monitored Anesthesia Care (MAC) sedation in adults, sedation for adults in combination with regional anesthesia, and ICU sedation of intubated, mechanically ventilated adult patients. It is not recommended for induction of anesthesia below age 3 or maintenance of anesthesia below 2 months, and is not indicated for pediatric ICU or MAC sedation.
- Class
- Small molecule
- Therapeutic area
- CNS / Anesthesia
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