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Fospropofol is metabolized in the liver by alkaline phosphatases to propofol, formaldehyde, and phosphate.The hepatic metabolism of this prodrug to an active metabolite means that peak plasma levels of propofol after the administration of a bolus of fospropofol are lower than for an equipotent dose of propofol and also that its clinical effect is more sustained.
To induce general anesthesia, propofol is the drug used almost exclusively, having largely replaced sodium thiopental. [13]It is often administered as part of an anesthesia maintenance technique called total intravenous anesthesia, using either manually programmed infusion pumps or computer-controlled infusion pumps in a process called target controlled infusion (TCI).
In pharmacology, the volume of distribution (V D, also known as apparent volume of distribution, literally, volume of dilution [1]) is the theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the blood plasma. [2]
Propofol (di-isopropyl phenol) was synthesized by Glen and colleagues in the early 1970s, [7] but its first formulations were temporarily withdrawn due to a number of adverse reactions during clinical studies. [1] In 1983, a lipid emulsion formulation of propofol was available, which carried great potential during clinical trials. [8]
Commonly used intravenous induction agents include propofol, sodium thiopental, etomidate, methohexital, and ketamine. Inhalational anaesthesia may be chosen when intravenous access is difficult to obtain (e.g., children), when difficulty maintaining the airway is anticipated, or when the patient prefers it.
The attraction between the N and O atoms is greater than the onium head repulsion. In this most populated state, the N-N distance is shorter than the optimal distance of ten carbon atoms and too short to occupy both receptive sites. This similarity between succinyl- and acetyl-choline also explains its acetylcholine-like side-effects. [20]
Propofol [6] is a non-barbiturate derivative that is thought to act by stimulating inhibitory GABA receptors and blocking excitatory NMDA receptors. It takes 40 seconds for the effects of propofol to kick in, and effects last six minutes. [3] Propofol has both sedative and amnestic effects, but provides no analgesia.
In a retrospective review of almost 32,000 people, etomidate, when used for the induction of anaesthesia, was associated 2.5-fold increase in the risk of dying compared with those given propofol. [37] People given etomidate also had significantly greater odds of having cardiovascular morbidity and significantly longer hospital stay. [37]