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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phenol) was synthesized by Glen and colleagues in the early 1970s, [7] but its first formulations were temporarily withdrawn due to a number of adverse reactions during clinical studies.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]
Propofol is highly protein-bound in vivo and is metabolized by conjugation in the liver. [86] The half-life of elimination of propofol has been estimated to be between 2 and 24 hours. However, its duration of clinical effect is much shorter, because propofol is rapidly distributed into peripheral tissues.
Minimum alveolar concentration or MAC is the concentration, often expressed as a percentage by volume, of a vapour in the alveoli of the lungs that is needed to prevent movement (motor response) in 50% of subjects in response to surgical (pain) stimulus.
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 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]
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.
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Propofol – It is a highly lipid-soluble, GABA agonist. [15] The dosage is 1.5 mg/kg (usually 100 to 200 mg). It has quick onset of action, can cross the blood-brain barrier, wide tissue distribution, and can be hepatically cleared by the body quickly. [15] In the elderly, the rate of Propofol clearance is low.