Bupivacaine is a local anesthetic for surgery, most commonly for oral or obstetrical procedures. It is adminstered via intrathecal injection or directly to the wound site. Bupivacaine does this through blocking the generation of action potential through increasing the threshold for activation. This in turn slows the propagation of the nerve impulse prevents the depolarization by binding to the intracellular portion of the sodium channels and blocking the ions influx into the neurons. Bupivacaine can also potentially bind to prostaglandin E2 receptors, subtype EP1 that stops the production of prostaglandins, reduce fever, inflammation and hyperalgesia. It is metabolized by the liver via glucuronic acid into the metabolite of 2,6-pipecoloxylidine by cytochrome P450 3A4. It is excreted via urine mainly unchanged.

Bupivacaine References