Myotoxic effects of
local anesthetics on skeletal musclefibers involve the inhibition ofsarcoplasmic reticulum Ca2+ -dependent
ATPase activity and Ca2 transport.
Lidocaine is a
local anesthetic frequently used to relieve the symptoms of
trigeminal neuralgia. The aim of this work was to test the inhibitory and/or stimulatory effect of
lidocaine on sarcoplasmic reticulum Ca2+ -dependent
ATPase isolated from rabbit temporalis muscle. Ca2+ -dependent
ATPase activity was determined by a colorimetric method
Calcium-binding to the Ca dependent
ATPase, Ca2+ transport, and phosphorylation of the
enzyme by
ATP were determined with radioisotopic techniques.
Lidocaine inhibited the Ca2+ -dependent
ATPase activity in a concentration-dependent manner. The preincubation of the sarcoplasmic reticulum membranes with
lidocaine enhanced the Ca2+ dependent
ATPase activity in the absence of
calcium ionophore.
Lidocaine also inhibited both Ca2+ uptake and
enzyme phosphorylation by
ATP but had no effect on Ca2+ -binding to the
enzyme. We conclude that the effect of
lidocaine on the sarcoplasmic reticulum Ca2+ -dependent
ATPase from temporalis muscle is due to the
drug's direct interaction with the
enzyme and the increased permeability of the sarcoplasmic reticulum membrane to Ca.