Pharmacokinetics and safety of ketorolac following single intranasal and intramuscular administration in healthy volunteers

• Published in: Journal of clinical pharmacology Vol. 47; no. 1; p. 13
• Main Authors: McAleer, Sarah D, Majid, Oneeb, Venables, Esther, Polack, Torsten, Sheikh, Muhammed S
• Format: Journal Article
• Language: English
• Published: England 01.01.2007
• Subjects: Administration, Intranasal; Adult; Analysis of Variance; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Area Under Curve; Biological Availability; Cross-Over Studies; Dose-Response Relationship, Drug; Female; Half-Life; Humans; Injections, Intramuscular; Ketorolac - administration & dosage; Ketorolac - pharmacokinetics; Male
• ISSN: 0091-2700
• DOI: 10.1177/0091270006294597

Ketorolac was administered to 15 healthy volunteers in a phase 1, single-dose, crossover, randomized study. Subjects received open-label randomized 15- and 30-mg intramuscular (i.m.) ketorolac and blinded randomized 15- and 30-mg intranasal (i.n.) ketorolac. The i.n. ketorolac was well tolerated; the only nasal symptoms were some instances of mild irritation. The i.n. ketorolac was rapidly and well absorbed (median tmax, 0.50-0.75 hours), and the half-life was approximately 5 to 6 hours, values that were similar to those following i.m. administration. Relative bioavailability of i.n. compared to i.m. administration at the same doses was approximately 67% to 75%. Dose proportionality was noted between the 15- and 30-mg i.n. and i.m. dose levels. Thus, i.n. ketorolac offers a therapeutic alternative to i.m. administration and may provide benefits in the clinical setting.