The Sound of Evolution
Ropivacaine
Mechanism of action:
Ropivacaine mainly acts by blocking voltage-gated Na+ channels on neuronal cell membranes. In its unionized form, ropivacaine can cross the neuronal cell membrane. After entering the neuron, it is converted into an ionized form and binds to the inner binding site of the sodium channel, with particular preference for channels in the open or inactivated state. This prevents sodium influx, blocks depolarization of the neuronal membrane, and ultimately prevents the generation and forward conduction of action potentials.
Reference(s):
1. Liu BG et al. (2000). The effects of ropivacaine on sodium currents in dorsal horn neurons of neonatal rats. Anesth Analg.
2. Arlander E et al. (1998). Metabolism of ropivacaine in humans is mediated by CYP1A2 and to a minor extent by CYP3A4: an interaction study with fluvoxamine and ketoconazole as in vivo inhibitors. Clin Pharmacol Ther.