As in other medical fields, the efficacy of neuropharmacotherapy depends on both psychosocial and biological characteristics of the patient. Patient’s gender is one of the latter. Although women are more likely to experience adverse drug effects, they still represent the minority in the first two phases of clinical trials. This results in fragmentary knowledge of potential dosage modifications in women. The paper presents an outline of sex differences that need to be considered in neuropharmacotherapy. The reported differences in pharmacokinetics are based on, among other things, different absorption due to lower gastric pH in women, longer gastrointestinal transit and lower P-glycoprotein expression. Drug distribution, which varies between men and women as a result of the different body fat percentage, also has an impact on the pharmacological response. Furthermore, there are also differences in the activity of drug metabolising enzymes, probably due to oestrogens. Additionally, a lower excretion rate may lead to insufficient drug elimination and subsequent side effects. The paper also presents examples of pharmacodynamic disparities. Neglecting gender differences in neurological pharmacotherapy may result in avoidable adverse effects or poor therapeutic outcome. Understanding the source of pharmacotherapeutic differences promotes therapy individualisation, and thus improved treatment outcomes and reduced adverse events, both in women and men.