Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: Biotech Laboratories (Pty) Ltd, Ground floor, Block K West, Central Park, 400 16<sup>th</sup> road, Randjespark, Midrand 1685, South Africa
Category and class: A.2.1 Central nervous system depressants: Anaesthetics.
Pharmacotherapeutic group: Other general anaesthetics
ATC code: N01AC10
Propofol (2,6-di-isopropylphenol) is a short acting anaesthetic given intravenously for the induction and maintenance of general anaesthesia. It is used for sedation in patients over the age of 16 years undergoing diagnostic procedures, in those undergoing surgery with local or regional anaesthesia, and in ventilated adult patients under intensive care. When used for anaesthesia, induction is rapid (approximately 30 seconds), as is recovery.
The mechanism of action is poorly understood. Falls in mean blood pressure and slight changes in heart rate are observed when propofol is administered for induction and maintenance of anaesthesia.
Ventilatory depression can occur following administration of propofol. Propofol reduces cerebral blood flow, intracranial pressure and cerebral metabolism. Recovery from anaesthesia is usually rapid and clear headed. Propofol has an anti-emetic effect. Propofol, at the concentrations likely to occur clinically, does not inhibit the synthesis of adrenocortical hormones.
Propofol is 98% bound to plasma proteins.
The decline in propofol concentrations following a bolus dose, or following the termination of an infusion, can be described by a three compartment open model. The first phase is characterised by a rapid distribution (half-life 2–4 minutes), followed by rapid elimination (half-life 30–60 minutes) and a slower final phase, representative of redistribution of propofol from poorly perfused tissue. Propofol is extensively distributed and rapidly cleared from the body (total body clearance 1,5–2 litres/minute).
Clearance occurs by metabolic processes, mainly in the liver, to form inactive conjugates of propofol and its corresponding quinol, which are excreted in the urine.
The pharmacokinetics are linear over the recommended range of infusion rates of propofol. Under the usual maintenance regimens, significant accumulation of propofol does not occur.
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