Ototoxicity has been recognized since the 1800, when it was learned that quinine and acetylsalicylic acid provoked dizziness, tinnitus and hearing loss. Beside above mentioned other drugs also have joined the list of ototoxic substances: aminoglycoside antibiotics, loop diuretics or antineoplastic drugs. In this review pharmacological and toxicological properties of potentially ototoxic drugs, such as loop diuretics, nonsteroidal anti-inflammatory drugs (salicylates), antineoplastic and antimalarial drugs are presented. Pathophysiology and postulated mechanisms causing drug-induced ototoxicity are also discussed.