In vitro metabolism of mivacurium chloride (BW B1090U) and succinylcholine.
The in vitro rates of metabolism of mivacurium chloride and succinylcholine in pooled human plasma were compared. In addition, the rate of metabolism of mivacurium in buffered solutions of butyrylcholinesterase (E.C. 3.1.1.8) and acetylcholinesterase (E.C. 3.1.1.7) was determined. Succinylcholine concentrations were measured spectrophotometrically, and mivacurium concentrations were determined with a high-pressure liquid chromatographic assay. The hydrolysis of mivacurium in plasma followed first-order kinetics, and the rate of hydrolysis decreased as plasma was serially diluted. The Michaelis-Menten constant (Km) for mivacurium metabolism in plasma was 245 mumol/L, and the maximum velocity (Vmax) was 50 U/L; the Km for succinylcholine was 37 mumol/L, and Vmax was 74 U/L. At comparable multiples of the Km the hydrolysis rate of mivacurium was 70% of that of succinylcholine. Mivacurium was metabolized significantly in solutions containing butyrylcholinesterase, but only minimally in solutions containing acetylcholinesterase.
Cook
D R
DR
Department of Anesthesiology, University of Pittsburgh, Pennsylvania.
Stiller
R L
RL
Weakly
J N
JN
Chakravorti
S
S
Brandom
B W
BW
Welch
R M
RM
D002091:Butyrylcholinesterase / Q000502:physiology; D006207:Half-Life; D006801:Humans; D066298:In Vitro Techniques; D007546:Isoquinolines; D008657:Metabolic Clearance Rate; D000077590:Mivacurium; D003473:Neuromuscular Nondepolarizing Agents / Q000493:pharmacokinetics*; D013390:Succinylcholine / Q000493:pharmacokinetics*
D007546:Isoquinolines; D003473:Neuromuscular Nondepolarizing Agents; D000077590:Mivacurium; D002091:Butyrylcholinesterase; D013390:Succinylcholine