Transnasal administration of systemic medication offers a convenient alternative to intravenous and intramuscular routes. Butorphanol, a noncontrolled, synthetic opioid agonist-antagonist analgesic is available in a nasal spray formulation. Transnasal butorphanol appears to be a safe and effective alternative for the treatment of moderate to severe postoperative and migraine headache pain. Side effects include sedation, nausea and confusion; transnasal butorphanol also has the potential to induce abstinence syndromes in opioid-dependent patients.