Pharmacokinetics of butorphanol tartrate administered from single-dose intranasal sprayer

George A. Davis, Anita C. Rudy, Sanford M. Archer, Daniel P. Wermeling

Research output: Contribution to journalArticlepeer-review

11 Scopus citations


Purpose. The Pharmacokinetics and tolerability of single and multiple doses of intranasal butorphanol tartrate using a single-dose, metered sprayer were studied. Methods. In this randomized, open-label, two-way crossover study, 24 healthy subjects received either 1 or 2 mg of intranasal butorphanol as a single dose (treatment A) and 1 or 2 mg of intranasal butorphanol every six hours for seven doses (treatment B). During phase 1, 12 subjects selected at random received a single 1-mg dose and the other 12 a single 2-mg dose. During phase 2, those who received the 1-mg single dose received 1 mg every six hours for seven doses. During phase 3, those who received the 2-mg single dose received 2 mg every six hours for seven doses. Serial blood samples were collected over 12 hours. Pharmacokinetic parameters were determined using noncompartmental methods. Results. Mean (coefficient of variation) values for the area under the concentration-versus-time curve (AUC) from time zero to infinity (AUC 0-∞) were 4.15 (26.4%) and 10.42 (19.6%) ng·hr/mL after single doses of 1 and 2 mg of butorphanol, respectively. At steady state, mean values for the AUC from time zero to the dosing interval (AUC0-τ) were 4.82 (40.2%) and 10.60 (22.3%) ngε·hr/mL, respectively. The accumulation indices were around 2 for both the 1- and 2-mg doses. Median time to maximum concentration values ranged from 15 to 30 minutes for each treatment. Dose-normalized parameters AUC0-∞ AUC0-τ and maximum concentration (Cmax) were significantly larger after a single 2-mg versus 1-mg dose (p < 0.05). Conclusion. Intranasal butorphanol has rapid absorption predictable accumulation after multiple closes administered with single-dose metered sprayers. Intranasal administration of butorphanol was well tolerated and adverse events were generally mild to moderate in severity and as expected for this drug.

Original languageEnglish
Pages (from-to)261-266
Number of pages6
JournalAmerican Journal of Health-System Pharmacy
Issue number3
StatePublished - Feb 1 2004


  • Absorption
  • Analgesics and antipyretics
  • Blood levels
  • Butorphanol tartrate
  • Dosage schedules
  • Drug administration routes
  • Phrmacokinetics
  • Sprays
  • Toxicity

ASJC Scopus subject areas

  • Pharmacy
  • Pharmacology
  • Health Policy


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