Gender identity disorder (GID), or transsexualism, is an increasingly recognized medical condition with an expanding body of medical literature to support the use of established therapeutic guidelines. Transsexualism can be effectively managed through exogenous cross-sex hormone administration used to induce development of desired sex characteristics, as well as use of other agents, such as aldosterone antagonists, aimed at decreasing physical characteristics of the undesired sex. Many complications can arise with the use of the available therapies, and these must be considered before determining the appropriate course of action. This review describes methods, including both pharmacotherapy and surgical interventions, for effective medical management of both male and female adults with GID. In addition, specific goals of therapy as well as safety aspects with long-term use of pharmacotherapeutic agents are discussed. This review also discusses some special considerations for treating patients with significant, yet common, comorbid diseases such as human immunodeficiency virus infection, acquired immunodeficiency syndrome, and viral hepatitis, as these conditions may complicate the clinical course and preclude some patients from using certain therapies. Pharmacist involvement in the management of transsexualism can be extremely beneficial to patients and other health care providers. Pharmacists can help determine the appropriate therapy, optimize dosages, monitor for adverse effects, and educate patients on what to expect during their therapy. Pharmacists should become knowledgeable about guidelines and current literature on transsexualism, understand the monitoring parameters for safe and effective therapy, and establish themselves as partners in the collaborative management of this disorder.
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