Carpal tunnel syndrome (CTS) is the most common peripheral nerve entrapment syndrome. CTS is a compression neuropathy caused by elevated pressure in the carpal tunnel. CTS has the potential to substantially limit performance of activities of daily living for some individuals. The goal of therapy for CTS is to improve symptoms and reduce signs of the disease, as well as prevent progression and loss of hand function. There are several treatment alternatives to relieve the pressure on the median nerve, both surgical and conservative. The most common measures employed in the initial treatment of CTS are NSAIDs, local and systemic corticosteroids, diuretics and pyridoxine. However, CTS treatment usually includes a combination of pharmacotherapy with other strategies such as splinting and activity modification. Injections of corticosteroids into the carpal tunnel are often employed for cases not responding to conservative treatment. Surgery is superior to conservative therapies for most persistently symptomatic patients. The aim of this paper is to review the pharmacological agents used for relieving the symptoms of CTS.