Current Pharmaceutical Design

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Propofol: Therapeutic Indications and Side-Effects

Author(s): Paul E. Marik

Affiliation: Professor of Critical Care, Department of Critical Care, University of Pittsburgh, 640A Scaife Hall,3550 Terrace Street, Pittsburgh, PA, 15261.

Abstract:

Propofol (2, 6-diisopropylphenol) is a potent intravenous hypnotic agent which is widely used for the induction and maintenance of anesthesia and for sedation in the intensive care unit. Propofol is an oil at room temperature and insoluble in aqueous solution. Present formulations consists of 1% or 2% (w / v) propofol, 10% soyabean oil, 2.25% glycerol, and 1.2% egg phosphatide. Disodium edetate (EDTA) or metabisulfite is added to retard bacterial and fungal growth. Propofol is a global central nervous system depressant. It directly activates GABAA receptors. In addition, propofol inhibits the NMDA receptor and modulates calcium influx through slow calcium ion channels. Propofol has a rapid onset of action with a dose-related hypnotic effect. Recovery is rapid even after prolonged use. Propofol decreases cerebral oxygen consumption, reduces intracranial pressure and has potent anti-convulsant properties. It is a potent antioxidant, has anti-inflammatory properties and is a bronchod ilator. As a consequence of these properties propofol is being increasingly used in the management of traumatic head injury, status epilepticus, delirium tremens, status asthmaticus and in critically ill septic patients. Propofol has a remarkable safety profile. Dose dependent hypotension is the commonest complication; particularly in volume depleted patients. Hypertriglyceridemia and pancreatitis are uncommon complications. Allergic complications, which may include bronchospasm, have been reported with the formulation containing metabisulfite. In addition, this formulation has been demonstrated to result in the generation of oxygen free radicals. High dose propofol infusions have been associated with the “propofol syndrome”; this is a potentially fatal complication characterized by severe metabolic acidosis and circulatory collapse. This is a rare complication first reported in pediatric patients and believed to be due to decreased transmembrane electrical potential and alteration of electron tra nsport across the inner mitochondrial membrane.

Keywords: propofol, metabisulfite, status epilepticus, status asthmaticus, traumatic brain injury, delirium tremens, sepsis, propofol-infusion syndrome, pancreatitis, allergy

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Article Details

VOLUME: 10
ISSUE: 29
Page: [3639 - 3649]
Pages: 11
DOI: 10.2174/1381612043382846
Price: $58