Developed originally as an antimalarial agent, hydroxychloroquine sulfate (HCQS) is often used as a slow-acting drug in treating disorders of connective tissue. Over the past two decades, several data have been accumulated on the systemic effects of HCQS, expanding the potential uses of this drug in different therapeutic classes. The purpose of this article was to conduct a narrative review with qualitative approach on clinical, pharmacokinetic and technological aspects of HCQS, aiming to gather relevant pieces of information for the development of new therapeutic approaches to this drug. A search of the literature of scientific experimental and theoretical studies in the period 1980-2013 was performed. According to the data collected, among the activities HCQS, there are the indications for the treatment of autoimmune diseases such as lupus erythematosus and rheumatoid arthritis. Reports also indicate that HCQS improves insulin sensitivity, ability to reduce thromboembolic events, reduction of lipid levels and treatment for infection by human immunodeficiency virus. The evidence found out ocular and cutaneous adverse effects and the formation of three chiral active metabolites, what encourages studies to evaluate the kinetic behavior of HCQS and the intrinsic physicochemical characteristics of the drug, which is yet poorly described in the literature.