The plasma levels of ropivacaine HCl with 5 mcg/mL epinephrine were measured in 10 patients following scalp blockade for awake craniotomy. A mean dose of 260 mg (3.6 mg/kg) resulted in peak plasma concentrations of 1.5 +/- 0.6 mcg/mL, with a median time to peak plasma concentration of 15 minutes. The pattern of rise of plasma level was similar in all patients and rapid compared with other regional blocks (epidural, intercostal, and axillary brachial plexus block). Despite this rapid rise of plasma level, no signs of cardiovascular or central nervous system toxicity were observed. In this group of patients undergoing awake craniotomy for excision of lesions in the eloquent areas of the cerebral cortex, ropivacaine HCl with epinephrine appeared to be a safe and effective local anesthetic agent in the dosages used.