The World Health Organization has classified the leishmaniasis as a major tropical disease. An effective vaccine against leishmaniasis is not available and chemotherapy is the only effective way to treat all forms of disease. However, current therapy is toxic, expensive and the resistance has emerged as a serious problem, which has compelled the search for new antileishmanial agents. The aim of this article is to review the current aspects of the pharmacology of leishmaniasis, giving an overview from current agents clinically used to new compounds under development. Pentavalent antimonials are still the first choice among drugs used for the treatment of leishmaniasis. Alternatively, amphotericin B, pentamidine, miltefosine and paromomycin can be used. The search for new drugs is a perpetual process; including synthetic products and compounds isolated from natural sources. The current scenario of antileishmanial drugs constitute the results of effort by academics, researchers and sponsorships in order to obtain drugs available, efficient and less toxic to people infected by Leishmania parasites.