Typical antipsychotic agents are commonly associated with hyperprolactinemia, which, in turn, leads to sexual dysfunction. The mechanism of action underlying this clinical phenomenon is mediated by the dopamine-blocking action of typical antipsychotic medications, which results in excessive prolactin secretion and secondary effects on gonadal function. This antipsychotic-induced sexual dysfunction is unacceptable to patients and is associated with nonadherence to medication, impacting on the overall clinical outcome and treatment success. Development of first-line atypical antipsychotic agents that do not affect prolactin production is therefore an important advance for patients requiring long-term antipsychotic therapy.