Labetalol reduces iodine-131 MIBG uptake by pheochromocytoma and normal tissues.

Iodine-131 metaiodobenzylguanidine [131I]MIBG has proven to be an effective radiopharmaceutical for the scintigraphic localization of pheochromocytomas. Uptake of MIBG is inhibited by blockade of the neuronal uptake pathway for catecholamines ("uptake-1") and by depletion of catecholamine storage vesicle contents, but is not significantly affected by conventional alpha- and beta-adrenoreceptor blocking drugs. Labetalol is an antihypertensive agent with combined alpha- and beta-blocking properties that has been used to manage patients with suspected pheochromocytomas. We report eight patients in whom concurrent or recent therapy with labetalol significantly reduced the uptake of [131I]MIBG into salivary glands, liver, spleen, and general body background. Tumor uptake of MIBG was also reduced in two of the three patients who were proven to have pheochromocytomas. In one case, the effect of labetalol persisted for 36 hr after the drug had been discontinued. The inhibitory effect of labetalol on MIBG uptake in sympathomedullary tissues is likely to be a result of the drug's little-known, additional properties of uptake-1 blockade and depletion of storage vesicle contents, rather than its alpha- or beta-blocking effects. Additionally, labetalol would also appear to hasten clearance of MIBG from other tissues. Labetalol therapy should be discontinued for several days (possibly up to 1 wk) before undertaking [131I]MIBG scintigraphy. A comprehensive list of drugs that should be avoided in patients undergoing MIBG scintigraphy is appended.