Ketorolac: An Extensive History of Pain Relief

Ketorolac is a hospital-strength nonsteroidal antiinflammatory drug (NSAID) that has been available for over 20 years.1 A nonselective NSAID, ketorolac inhibits prostaglandin production by inhibiting COX-1 and COX-2.2,3 It has potent analgesic activity,4 and has been extensively studied in postoperative patients.5

Popular parenteral analgesic

Ketorolac was the first NSAID approved in the United States for parenteral use as an analgesic.5 Premarketing clinical trials involving more than 5,000 patients demonstrated that ketorolac’s analgesic efficacy was similar to that of parenteral opiates in patients undergoing general and oral surgery.5

Ketorolac is widely used intramuscularly and intravenously for moderately severe acute pain: there have been more than 500 million injections in the United States since its introduction, and nearly 40 million injections in 2010 alone.6

An NSAID alternative to opioids

Ketorolac has similar efficacy to morphine and meperidine.7 A 30-mg dose of ketorolac IM delivers pain relief equivalent to that of morphine 6 mg to 12 mg.8

In two double-blind studies of postoperative patients with moderate to severe pain, IM ketorolac injection was compared with meperidine or morphine IM, and IV ketorolac was compared with morphine administered intravenously or via patient-controlled analgesia. During the first hour, the onset of analgesic action was similar for ketorolac tromethamine and the opioids, but analgesia lasted longer with ketorolac tromethamine.7

Clinical studies have also demonstrated that combining ketorolac and opioids significantly reduces the need for morphine.9,10

Ketorolac is non-narcotic

As an NSAID, ketorolac does not bind to opiate receptors.8 A study to evaluate the sedative and addictive potential of ketorolac showed no withdrawal symptoms upon cessation of dosing with ketorolac 30 mg IM four times daily for 5 days.8 Ketorolac IM also has no significant adverse effects on psychomotor measurements, including reaction time, computerized driving skills, ataxia, and sedation.8

Ketorolac: 20+ years of experience
  • Ketorolac was approved in 1989 as the first injectable NSAID1
  • In 1990, it was introduced as Toradol® Injection by Roche Laboratories11
  • More than 500 million injections administered in the United States since its introduction6
  • Toradol® Tablets were approved in 1991
  • Injection and tablet forms are currently available in generic formulation
  • Ketorolac is marketed as Acular® for the topical treatment of ocular itching due to seasonal allergies12

SPRIX® (ketorolac tromethamine) Nasal Spray is the first and only intranasal NSAID. It is indicated for the short-term (up to 5 days) management of moderate to moderately severe pain that requires analgesia at the opioid level.

Acular® is a registered trademark of Roche L.L.C.
Prescribing SPRIX® How to dose, prescribe, and dispense SPRIX®


  • Boyer KC, McDonald P, Zoetis T. A novel formulation of ketorolac tromethamine for intranasal administration: Preclinical safety evaluation. Int J Toxicol. 2010;29(5):467-478.
  • Block BM, Hurley RW, Raja SN. Mechanism-based therapies for pain. Drug News Perspect. 2004;17(3):172-186.
  • Krenzischek DA, Dunwoody CJ, Polomano RC, Rathmell JP. Pharmacotherapy for acute pain: implications for practice. Pain Manag Nurs.
    2008;9(1 Suppl):S22-S32.
  • Moodie JE, Brown CR, Bisley EJ, Weber HU, Bynum L. The safety and analgesic efficacy of intranasal ketorolac in patients with postoperative pain. Anesth Analg. 2008;107(6):2025-2031.
  • Strom BL, Berlin JA, Kinman JL, Spitz PW, et al. Parenteral ketorolac and risk of gastrointestinal and operative site bleeding. A postmarketing surveillance study. JAMA. 1996;275(5):376-382.
  • Data on file. Shirley, NY: Luitpold Pharmaceuticals.
  • Gillis JC, Brogden RN. Ketorolac. A reappraisal of its pharmacodynamic and pharmacokinetic properties and therapeutic use in pain management. Drugs. 1997;53(1):139-188.
  • SPRIX® [package insert]. Shirley, NY: American Regent, Inc; 2011.
  • Singla N, Singla S, Minkowitz HS, Moodie J, Brown C. Intranasal ketorolac for acute postoperative pain. Curr Med Res Opin. 2010;26(8):1915-1923.
  • Brown C, Moodie J, Bisley E, Bynum L. Intranasal ketorolac for postoperative pain: A phase 3, double-blind, randomized study. Pain Med. 2009;10(6):1106-1114.
  • Luitpold Pharmaceuticals, Inc. and Daiichi Sankyo, Inc. Press release. May 17, 2011.
  • Acular® [package insert]. Irvine, CA: Allergan, Inc; 2009.