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QuickView for propofol (compound)


PubChem
Name: Propofol
PubChem Compound ID: 11137742
Description: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.
Molecular formula: C12H18O
Molecular weight: 181.289 g/mol
DrugBank
Identification
Name: Propofol
Name (isomeric): DB00818
Drug Type: small molecule
Description: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.
Synonyms:
Diisopropylphenol; 2,6-Diisopropylphenol
Brand: Diprivan, Disoprivan, Disoprofol, Rapinovet
Category: Anesthetics, Intravenous, Hypnotics and Sedatives, Free Radical Scavengers, Antiemetics, Anticonvulsants
CAS number: 2078-54-8
Pharmacology
Indication: Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
Pharmacology: 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).
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.
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.
Protein binding: 95 to 99%, primarily to serum albumin and hemoglobin
Biotransformation: 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.
Route of elimination: It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.
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.
Clearance: 23 - 50 mL/kg/min 1.6 - 3.4 L/min [70 Kg adults]
Toxicity: Overdosage may increase pharmacologic and adverse effects or cause death.

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)

Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TacrineThe metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Propofol, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Propofol is initiated, discontinued or if the dose is changed.
TizanidinePropofol may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.

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