Name: | Propofol |
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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 |
Name: | Propofol |
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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
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Brand: | Diprivan, Disoprivan, Disoprofol, Rapinovet |
Category: | Anesthetics, Intravenous, Hypnotics and Sedatives, Free Radical Scavengers, Antiemetics, Anticonvulsants |
CAS number: | 2078-54-8 |
Indication: | Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus. |
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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 |
Drug interaction: |
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