Propofol Stats & Data
CC(C)c1cccc(C(C)C)c1OOLBCVFGFOZPWHH-UHFFFAOYSA-NPharmacology
DrugBankDescription
Propofol is an intravenous anaesthetic agent used for induction and maintenance of general anaesthesia. IV administration of propfol is used to induce unconsciousness after which anaesthesia may be maintained using a combination of medications. Recovery from propofol-induced anaesthesia is generally rapid and associated with less frequent side effects (e.g. drowsiness, nausea, vomiting) than with thiopental, methohexital, and etomidate. Propofol may be used prior to diagnostic procedures requiring anaesthesia, in the management of refractory status epilepticus, and for induction and/or maintenance of anaesthesia prior to and during surgeries.
Mechanism of Action
The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.
Pharmacodynamics
Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).
Metabolism
Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.
Absorption
Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.
Toxicity
Overdosage may increase pharmacologic and adverse effects or cause death. <p>IV LD50=53 mg/kg (mice), 42 mg/kg (rats). Oral LD50 (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)</p>
Indication
Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
Half-life
Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.
Protein Binding
95 to 99%, primarily to serum albumin and hemoglobin
Elimination
It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Experience Report Analysis
ErowidDemographics
Gender Distribution
Age Distribution
Reports Over Time
Effect Analysis
ErowidEffects aggregated from 16 experience reports (16 Erowid)
Effect Sentiment Distribution
Confidence Distribution
Positive Effects 4
Adverse Effects 2
Real-World Dose Distribution
62K DosesFrom 5 individual dose entries
Intravenous (n=5)
Form / Preparation
Most common forms and preparations reported
Redose Patterns
Redosing behavior across 11 reports