This study was undertaken to evaluate the efficacy and the safety of transnasal butorphanol (TNB) compared to intravenous butorphanol (IVB) in 186 patients experiencing moderate to severe post‐cesarean section pain. Patients were randomly assigned to five groups in a double‐blind fashion: Group I (n = 37) received 2 mg IVB, Group II (n = 38) 2 mg TNB, Group III (n = 36) 1 mg TNB followed by a repeat dose of 1 mg TNB at 60 min, Group IV (n = 38) 0. 5 mg TNB followed by a repeat dose of 0. 5 mg at 60 min, and Group V (n = 37) received placebo. All administrations were double dummy. Pain intensity and relief were noted and the incidence of side effects was recorded. Remedication with the same study drug was allowed up to 72 h. Onset of analgesia was more rapid in the 2 mg IV group compared to the three TN groups: 5 min vs 15 min, respectively. However, the 2 mg and the 1–1 mg TN groups had a longer duration of analgesia, approximately 4. 5 h, compared to 3. 0 h for the 2 mg IV group (P<0. 05). Somnolence was dose related and was the most frequent side effect, and was less frequent when the TN dose was divided into 2 doses administered 1 h apart. Multiple doses of TNB and IVB were safe and clinically acceptable up to 3 days at all doses studied. There were no incidences of nasal mucosa irritation, or cardiovascular or respiratory depression. It is concluded that transnasal butorphanol represents a safe and effective alternative to injectable butorphanol for post‐cesarean section pain and offers a better and longer duration of analgesia compared to IV butorphanol. The optimum dose seems to be 2 mg TN butorphanol and it is tolerated better when divided into 1 mg increments, given 1