The notion that drugs can induce valvular heart disease (VHD) has occurred since the 1960s and has received a lot of attention in recent years. This review focuses on different aspects of this distinct valvulopathy in seven sections: (i) historical background, (ii) drug-induced VHD, is this a real entity?, (iii) its morphological and echocardiographic features, (iv) drugs associated with VHD, (v) the influence of cumulative drug dose and risk factors, (vi) the natural course of toxic valvulopathy, and (vii) practical recommendations when using potential valvulopathic drugs.