BACKGROUND: Social anxiety disorder (SAD), despite its low detection rates and high level of associated comorbidities, is considered a treatable condition. Although the condition's response to several drug classes is well established, the algorithms for the treatment of SAD require regular updating. OBJECTIVE: To perform a systematic literature review on the efficacy of pharmacological treatments for SAD based on controlled trials published between 2005 and 2010. METHOD: Searches were performed in the electronic databases PsycInfo, Lilacs, and Medline using the search terms "social phobia or social anxiety and treatment". RESULTS: In accordance with the inclusion criteria adopted, 29 articles were included and analyzed. The following drugs, grouped according to class, proved efficient to treat SAD: a) SSRIs: escitalopram, fluvoxamine, citalopram, GR205171, and sertraline; b) SNRI: venlafaxine; c) MAOIs: phenelzine, moclobemide; d) amino acids: f-cycloserine; and (e) anticonvulsants: tiagabine. DISCUSSION: The use of SSRIs and SNRIs to treat SAD is well established and these are still considered the first-line treatment for the condition; however, evidence suggests the future potential of D-cycloserine and anticonvulsants, whose efficacy must be confirmed by further controlled trials. The action profiles of the different medications used to treat SAD at the neurobiological level, as well as that of associated treatments, need to be explored in greater depth.