Ketorolac (Toradol)

• Generic name: Ketorolac Tromethamine
• Trade names: Toradol, Acular, Sprix (Intranasal)
• Pharmacologic category: Nonsteroidal Anti-inflammatory Drug
• FDA approved: December 20, 1991
• Habit forming? No
• Pregnancy risk factor: C

Ketorolac is a quite potent non-steroidal anti-inflammatory drug which is licensed for short term use in the management of moderate to severe postoperative pain. It is one of the newest NSAIDs.

• Onset of action: Intramuscular ~10 minutes, maximum effect within 2 hours.
  Oral ~30-60 minutes.
• Duration of action: 6-8 hours
• Metabolism: Hepatic
• Elimination half-life: 2-6 hours; prolonged 30% to 50% in elderly; up to 19 hours in renal impairment
• Excretion: Urine (92%, 61% as unchanged drug)

• Injectable formulation. Available in injectable form which can be used in situations where oral NSAIDs are excluded (eg. acute post-operative pain).
• Less nausea and sedation than narcotic analgesics.

• Expensive. One of the most expensive NSAIDs.
• Weak anti-inflammatory action. In comparison to the other NSAIDs, ketorolac has poor anti-inflammatory activity.
• Severe gastrointestinal complications. Ketorolac is reported to have the highest rate of serious gastrointestinal complications of all non-steroidal anti-inflammatory drugs. Ketorolac can cause peptic ulcers, gastrointestinal bleeding and perforation of the stomach or intestines, which can be fatal. Results of a case control study2 comparing the GI toxicity of different NSAIDs suggest that ketorolac was approximately five times more likely to cause upper GI bleeding than other NSAIDs.
• Ketorolac may cause kidney failure.

• Severe migraine headache
• Pain after surgery in children

Ketorolac is a pyrrolizine carboxylic acid derivative. It has analgesic, antipyretic and anti-inflammatory activity. The primary mechanism of action is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX).

• 1. U.S. FDA. Ketorolac (Toradol) Prescribing Information.
• 2. Garcia Rodriguez LA, Cattaruzzi C, Troncon M, Agostinis L. Risk of hospitalization for upper gastrointestinal tract bleeding associated with ketorolac, other anti-inflammatory drugs, calcium antagonists, and other antihypertensive drugs. Arch Intern Med. 1998;158(1):33-9.

Last modified: July, 2011