Acute agitation in the psychiatric emergency setting is a common presentation, which can endanger the patient, caregivers and professional staff. Rapid and effective treatment, followed by ongoing evaluation and maintenance treatment where appropriate, is key to circumvent negative outcomes. Nonpharmacological measures are the first step in treating the acutely agitated patient, and include verbal intervention and physical restraint. Pharmacological treatment is often required to ensure the safety of the patient, caregivers and the treatment team. The need for drug delivery in uncooperative patients favours the use of intramuscular preparations for the acutely agitated patient. Intramuscular treatment options include benzodiazepines, conventional antipsychotics and atypical antipsychotics. Each of these medications offers a unique pharmacological profile that must be considered when treating acutely agitated patients, who may be unwilling or unable to accurately communicate their co-morbid conditions and concomitant medications.