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Three compartments can be used to represent the pharmacokinetics of fentanyl: distribution (1.7 min), redistribution (13 min), and final elimination (219 min).When administered intravenously, fentanyl acts very instantly, although it may take several minutes to reach its maximum analgesic and respiratory depressive effects.As fentanyl gets more ionized, the plasma protein's binding capacity decreases.It accumulates in skeletal muscle and fat and is then progressively released into the bloodstream.


Original text

Three compartments can be used to represent the pharmacokinetics of fentanyl: distribution (1.7 min), redistribution (13 min), and final elimination (219 min). Fentanyl has a distribution volume of 4 L/kg. As fentanyl gets more ionized, the plasma protein's binding capacity decreases. Changes in pH may affect its transit between plasma and the central nervous system. It accumulates in skeletal muscle and fat and is then progressively released into the bloodstream. Fentanyl is mostly transformed by the liver, which also has a high first pass clearance rate. Approximately 75% of an IV dose is excreted in urine, mostly as metabolites, with less than 10% as the original drug. Most of the dosage—about 9%—is retrieved in the stool as metabolites. When administered intravenously, fentanyl acts very instantly, although it may take several minutes to reach its maximum analgesic and respiratory depressive effects.


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