Despite its nephrotoxic potential, the aminoglycoside antibiotic gentamicin (GM) is still considered to be an important agent against life-threatening infections. The goal of reducing or protecting against its nephrotoxicity has attracted much effort and attention during the last decade. This article reviews some of the literature published during the last decade on the effects of agents that ameliorate or augment GM nephrotoxicity. Notable among the ameliorating agents are antioxidant agents. These include different classes of compounds that include beta blockers (e.g. carvedilol), superoxide dismutase mimetic agents (e.g. M40403), hormones (e.g. melatonin), iron chelators (e.g. deferrioxamine), vitamins (vitamin C and E) and medicinal plants (e.g. garlic). Other ameliorating agents include antibiotics (e.g. ceftriaxone), antiplatelet drugs (e.g. trapidil) and Ca++ agents that may augment GM nephrotoxicity include cyclosporin and the Ca++-channel blocker verapamil.