Psychomotor agitation is a widespread clinical problem both in patients with schizophrenia and BD. It is a highly hazardous condition, imposing significant risks in psychiatric emergency, as expressed by elevated ratios of adverse events and traumatic experiences (both for patients and medical staff). The available anti-agitation drugs have numerous disadvantages. The orally administered medications (even though preferable to patients) take hours or even days for the therapeutic effect to emerge (and also there is a risk of exacerbating agitation in between). Although rapid onset of action (15–45 minutes) is a noteworthy merit of intramuscular drugs, such an invasive strategy is far too often bound to patients’ anxiety, resistance, and traumatic experiences. The need for novel drug formulations (ideally, both integrating the benefits of injectable and orally administered tranquillizing medications, and free from their disadvantages) can be, therefore, clearly grasped. Development of inhaled loxapine exemplifies the attempts to overcome the above-delineated obstacles. As suggested by the available research base, inhaled loxapine seems to be an effective anti-agitation drug in treatment of patients with schizophrenia and BD (with the onset of action similar to the one observed in intramuscular antipsychotics). However, this formulation of loxapine is distinguished by its non-invasive route of administration, as accompanied by markedly low risk of side effects or adverse events.